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nelsons stuff???
- Thread starter GLEN
- Start date
needtogow2007612 said:
A lot of people? I thought is was only 5'4" 57 year old solidspine who takes two grams of gear a week in order to pretend he's a bodybuilder.
Personally, I have no problem with anyone else, even bros who may disagree with me.
Okay, that's all I have to say. I'll let others comment.
floridalife
New member
I'm sick of the bullshit, propoganda, unqualified advice and rediculous sales pitch this site has been nothing but a freaking soap opera lately
Sweetsrcool
New member
umm what the hell is going on and who cares, are there people on here who are trying to rip others off by faking as a source how messed up o by the way im a source now to, i have like one bottle of bla and bla that ill sell you for a shit load of money. LOL
A
Anthony Roberts
Guest
needtogow2007612 said:
People like both products. Nelson designed one, myself the other. The products are both good and work. You're buying a product for the results, not because of who designed it, right?
A lot of people here liked Yohimburn, which was originally thought up by Dan Duchaine, and sold as "yo-be-lean" by his girlfriend...but it didn't work because Dan thought it up...it worked because it was a good product.
Sesamin/Sesalean is also a good product which was sold by a former sponsor here, and everyone liked it...but it was thought up by a guy (not the former sponsor) who was later banned on these forums by that same sponsor who later decided to carry the same product. It works because it works, not because of who developed it...
Remember, you're buying something for results, not because of the inventor.
solidspine
New member
I am 5'5"
I have not been 5'4" for at least 45 years,
If the product is not herbal life, sand and sugar the manufacture will give you a sample to evaluate,
Ask for a sample to evaluate
I think lying and plagiarizism (sp) is compulsive.
Let’s see if you can get this straight,
I have not been 5'4" for at least 45 years,
If the product is not herbal life, sand and sugar the manufacture will give you a sample to evaluate,
Ask for a sample to evaluate
I think lying and plagiarizism (sp) is compulsive.
Let’s see if you can get this straight,
metalgodz1
New member
sounds like days of our lives repeat. fraud is pretty strong language! Up there with scammer, thief. how about alittle gratitude for people just trying to help! To many soap box preachers trying to prop themselves up! All this backbiting is childs play.I think getting your books published,and doing somthing positive with your life {awsome! }Its the little people with jealousy, spite , and envy, that I have a problem with. whatever you focus on increases! look for good, Its your choice to to buy or not, to agree or not. I learn from everybody , even if its what not to do or say. Lets take this site to a higher place , rather than a lower one!
solidspine
New member
In the state of Louisiana one of the experts here is being sued, the term fraud is one of his charges,
Not strong language just a quote from the court in Louisiana, a legal term.
If the other charges and the charge of fraud are upheld you can determine for yourself how much gratitude to offer for the help being given and when the term scammer is appropriate. Are they really trying to help you, or is it more important to help themselves.
Are you taking advice from people with experience or from people whose main or sole purse is to sell stuff, what is this stuff, why is it used? There are a million questions; one answer is it gives them money that is the only conclusive fact that is known. Everything else is antidotal at best.
I will see what the courts have to say. And will not be shy about publishing the outcome.
Not strong language just a quote from the court in Louisiana, a legal term.
If the other charges and the charge of fraud are upheld you can determine for yourself how much gratitude to offer for the help being given and when the term scammer is appropriate. Are they really trying to help you, or is it more important to help themselves.
Are you taking advice from people with experience or from people whose main or sole purse is to sell stuff, what is this stuff, why is it used? There are a million questions; one answer is it gives them money that is the only conclusive fact that is known. Everything else is antidotal at best.
I will see what the courts have to say. And will not be shy about publishing the outcome.
Pat_McCrotch
New member
Id like to see a link to the case of the state of LA vs fraud
ben dovergurl
New member
Stryker1992
Well-known member
needtogow2007612 said:
Yah, this is getting fucked up. I have guys tell me that they have liked unleashed, post cycle and myogenx, some of them have been here for a while.
I appreciate Nelson and I also find Solidspine to be interesting, however, I am tired of the fighting, it is distracting.
I am going to be trying Unleashed and post cycle. I am also trying derma. If these things do or do not work I will tell everyone I know. I think everyone knows I am invested in the sport, this community, and I am pretty even tempered. Even if my report is only anecdotal! (LOL on spelling for Solid!)
I am no one when it comes to steroids but I have an MS in Exercise Physiology and a PhD in Sports Psychology. I can tell you research can prove anything depending on what is published; this goes for big pharmacies to Joe Blow with a TV invention. There are many sides to everything and everyone is different. Aspirin can cure headaches for one guy and give another ulcers. That is just the way it is. I think I am able to know enough to know my own body and what it is responding to. If that works for others cool!
If you want to be pissed at anyone go after GNC and all the pro BB’s that gave us false hope when we were young by selling us shit that took all of our hard earned cash and did not add one damn good thing! That is what really pisses me off! Mr. O on the cover of some fucking protein powder from Joe Weider acting like this did it for him!
YOU CANT SLANDER SOMEONE AND HIS NAME AND HIS PRODUCT WITHOUT SOME BASE TO DO SO....MOST PEOPLE SEEM TO LIKE THESE PRODUCTS
WHAT IS YOUR BASIS FOR THE ATTACk> PERS OR DO YOU JUST NOT LIKE THE PRODUCT
NELSON IF HE IS SLAMMING YOU ITS CALLED SLANDER , IF IT BHURTS YOUR NAME MONEY WISE, HE MUST PROVE WHAT HE SAYS=
WHAT IS YOUR BASIS FOR THE ATTACk> PERS OR DO YOU JUST NOT LIKE THE PRODUCT
NELSON IF HE IS SLAMMING YOU ITS CALLED SLANDER , IF IT BHURTS YOUR NAME MONEY WISE, HE MUST PROVE WHAT HE SAYS=
solidspine
New member
What bais would that be,
Ahhhh oh I got one Lying, and Fraud ahhh what else,
Selling sugar as protein,
Please name a board where nelson has not been kicked off, please one board, one, in North America, or the world.
He is a COMPULSIVE LIAR about to be revealed. The guy is a liar and likes to start problems when nobody is around for rebuttal. Please do not believe anything the guy ever states in regards to other people. The guy has written like 1 good calves article, and another on arms...other than this, he is a scam and a liar!
Nelson is a flat out idiot just wanting to make an extra buck promoting shitty products. The guy always thinks he is getting picked on. He will tell you to put up a study supporting your facts/opinions, but yet has NEVER once put one up himself. He asks for studies, but then in the past, has always stated that they are worthless...especially if they disagree with him. I've seen half the members on that thread tear him a new asshole, but yet he still thinks he is picked on, or they are lying...and then he will start calling them names and actually talks down to them like they are ignorant.
Do yourself a favor and do a search under fukkenshredded's and see how he made Nelson look like the idiot he is in regards to exercise and cardio. Seriously, the guy was owned so bad by FS, that even Nelson's big mouth had no kind of rebuttal. He was shut down hard.
He is promoting Dermacrine, a product that he has never even tried.
Nelson has put out freakin' magazine articles....nothing in regards to research! Nothing but opinionated editorials people. He is not a scientist. Ask him to provide any kind of scientific publications, and he will not do it, because he has never done one!
Nelson has always been the putz of the on-line discussion boards. Nobody likes him, well at least outside of a very small group, and he is just there to help raise money for discussion boards by hyping up worthless products that otherwise would have been failures quicker. He is a loser, and he will win over some hard earned money from newbies that are naive, but eventually, even the newbies will figure out how much of a lying douchebag he is.
lifthard2005
New member
solidspine
New member
It is dangerous & irresponsible to promote products with out clinical efficacy, the FDA is responsible for overview of this industry, but it is out of hand.
Untested, in a clinical controlled study are simply foolish to take, unless the actual ingredients are innocuous, like sugar.
The roid store is an example; they are selling vitamins, supplements and sugar,
But deceiving people into thinking they are actually buying gear.
What would you call this?
Fraud?
False advertising?
Really immaterial, they are conning newbie’s. Who think they are buying gear without a prescription, and just getting worthless sugar and vitamins?
I am not a fan of this or of Nelsons promotion and arguing and total BS demeanor.
Most of us here are smart enough not to get suckered; he is testy because he does not like disagreement or being called out, or trying to speak with authority.
I won’t tell you anything about gear unless I have used it and used it extensively. \
Anti-e, PCT, supplements also,
To get in to a pissing contest with uneducated people who have one motive to sell crap, is really frustrating, but to let them spew lies, to a large audience with out any documentation or support, is immortal, so I will continue to say bull shit every time they try it.
If they don’t like it, go back to all the boards they have been kicked off
Untested, in a clinical controlled study are simply foolish to take, unless the actual ingredients are innocuous, like sugar.
The roid store is an example; they are selling vitamins, supplements and sugar,
But deceiving people into thinking they are actually buying gear.
What would you call this?
Fraud?
False advertising?
Really immaterial, they are conning newbie’s. Who think they are buying gear without a prescription, and just getting worthless sugar and vitamins?
I am not a fan of this or of Nelsons promotion and arguing and total BS demeanor.
Most of us here are smart enough not to get suckered; he is testy because he does not like disagreement or being called out, or trying to speak with authority.
I won’t tell you anything about gear unless I have used it and used it extensively. \
Anti-e, PCT, supplements also,
To get in to a pissing contest with uneducated people who have one motive to sell crap, is really frustrating, but to let them spew lies, to a large audience with out any documentation or support, is immortal, so I will continue to say bull shit every time they try it.
If they don’t like it, go back to all the boards they have been kicked off
This is supposedly the Steroid Discussion forum, all these supplements should be in the supplement forum and all the drama should go to the C&C. I agree this place has been a mess for a while. Easy fix would be for the moderators to start moving threads to the proper forums and for the one's who make the posts pushing supplements to start posting in the supplement forum and for the one's who want to start drama, go to the C&C. But all that makes too much sense.
solidspine
New member
You like the law, you like law suits, you want to know the definition of
FRAUD AND SLANDER?
KNOCK YOUR SELF OUT.
Posted by IBE
IBE SUES Anthony Roberts, non-fiction
Many people who have been following the progression of IBE over the last few years, are probably aware of the troubles we have been having with Anthony Roberts aka Anthony Connors in his attempts to discredit our company and products. Well this is a message to him and any others who make it their business to spread lies and slander as truth. Below is a copy of the now officialy filed Lawsuit against Anthony Roberts in the State of Louisiana.
http://ibe-technology.com/ANTHONY1.jpg
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Also, we have a copy of the letter that was mailed to Mr. Roberts on March 21st requesting for him the remove/retract such statements. This was the final of many, many attempts via email and contact with our lawyer to have him make such retractions. He has responded only with mockery and even further accounts of libel against IBE.
http://ibe-technology.com/ANTHONY6.jpg
http://ibe-technology.com/ANTHONY7.jpg
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http://ibe-technology.com/ANTHONY9.jpg
We also, have several accounts since the letter date on March 21st of copied and filed alongside the lawsuit in regards to our Epistane product testing and even a statement from bodybuilding.com where he states "even if I helped bring them down". Not very smart to openly admit having participated in actions to try to bring a company down after they have asked on multiple occassions for you to cease and desist.
http://ibe-technology.com/ANTHONY15.jpg
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floridalife
New member
oh shit! lol
DonCorleone562
New member
thats some serious law ownage!
S
straintendons
Guest
Nelson Montana said:
solidspine is more knowledgable about steroids than you'll ever be nelson. go back to playing guru with ar
S
Sam5
Guest
You'll never know till you try it whether it works or not. I myself am not a big fan of supplemenatation. A multi, protein powder is about it. I think we are all getting too worked up here. Most here seem intelligent enough to be able to discern between the propaganda and what truly is. I know I do. You don't spend over 2/3 of your life reading nutritional mags, books about anabolics, PDR's, and as false as some of them are, musclemags, to know nothing about what you are doing. Take what you want and need and leave the rest.
straintendons said:
Wow. two whole posts and you're a solidspine fan. Impressive.
Look, I can't go tit for tat everything this idioat says, so let's just hit the biggies.
He says I've plagerized -- yet he hasn't cited one example of it. He then goes off on a rant about Anthony.
He says I sell sugar for protein. That's just something he pulled out of his ass.
He says I've never used steroids. Wrong again. I never used as much as him so he thinks that makes him more knowledgable.
He says I've never used anti-e's. How does he knows this? How can anyone be so stupid to think he could possibly know this? Seriously, I don't think too many people think he's smart -- they just like that he's taking on someone with a name. As they say; "The losers only go after the guy with the ball."
I've spent 20 years in this game and all it takes is some idiot to concoct some nonsense and they'll always be some fool who believes it.
He talks about the funkinshredded thing about cardio. Well, my theories on cardio have been discussed, agreed with and/or endorsed by people such as Charles Poliquin, Lou Shuler, Eric Serrano, Dave Draper, Mauro Di Pasqulae, Dan Duchaine, Don Howorth, Dennis Weiss, Ian King and others. Who the fuck is Funkinshreded??? Some guy that yells "OWNED!" on a message board. And solidspine applauds. Is anyone else?
He has never tried any of my products nor has he even read the research involved. Read the reviews. Not every PF product has gotten a good review but my products have an average of a 97% positive approval rating.
In short -- he's an asshole, plain and simple.
No one has to agree with me entirely. I offer debate, interest, contoversy and perspective from 25 years of experience and the first hand accounts of some of the top scientists, theorists and pro bodybuilders in the world. Not impressed? Fine. But this jerk off is just an insect who is spewing hate and it's getting really annoying. He doesn't care about real bodybuilding. He just follows me around disrupting every thread I'm on. He's doing 4 grams of gear a week because he has nothing else in life. And he appeals to others like him. Sad.
But as long as he keeps getting attention, like a petulant child, he'll keep doing it. And only a fool would encourage it.
Am I wrong? This reeks of Juice Authority and Fonz who eventually took up so much time I had to leave. Some members of the board cheered their heros. Meanwhile, the idiots were banned for scamming. Good bros they were.
Enough.
Sweetsrcool
New member
Ya Know I have no idea who either of you are, Sounds like you both might have to much free time to be having arguments on the net (JK) Take it easy ya guys
S
Sam5
Guest
I don't use anti-e's. Yet, I'm bigger and more knowledgable than most in my gym. I think that is a personal thing and dependent not only on how your body reacts to steroids but what your goals are too. I strongly suggest staying away from anti'e's unless they are absolutely needed, i.e. gyno. I don't think not using one thing or another means your less of a competitor or knowledgable person. Gavin Kane, for those who know him, never uses em either and suggests staying away from them. I did not get this from him, I've never used em, but it made me smile when I saw him post about it. And for the record, this is an allright board, but Gavin Kane is probably one of the most knowledgeable guys on the net, and I am very critical of people that think they are knowledgeable when they are not. Another very knowledgeable guy goes by the handle Enanthanator and is a mod on a few boards. THese guys go out of their way to help others out and they really don't have the time to do so. Just though that I would put that out there for those seeking real solid knowledge. I'm not one to blow other peoples horn when it is not warranted but these guy's and several others at these boards are top frigging notch.
solidspine
New member
Good Bye Nelson Montana, time to move on again, and again, and again........
Thanks for the compliments, keep it up, keep selling sugar,
And when you get kicked off this website, like you have been kicked off every where else, Guess what, I will still be here, posting, like I have for the past 10 years
Clinical research is over your head. You just insist people believe what you say simply because you say it,
you are going to get your ass kicked over here constantly just like everywhere else you have been.
Your views are not about knowledge--but about money and promotion to make more money. Unfortunately selling sugar to newbie’s.
I just hope you don't influence newbie’s with all your misinformation
Smart people know better. You are use to talking to teenagers in high school who want to know what supps to buy ---clueless,
Which forum were you kicked off of and exposed by Jenetic? I can remember can you?
You Do you remember Jenetic? Correct?
You have never made a sane comment about anything I have ever said, only personal attacks, and petty angry remarks slanderous comments all meaningless, but you are terrified some one will expose you again, and again, like they have on every forum in North America.
he's an asshole, plain and simple-You are the Einstein of the board, lets see how long you make it this time,
would you like to measure it in weeks, days or hours,
Good Bye,
Thanks for the compliments, keep it up, keep selling sugar,
And when you get kicked off this website, like you have been kicked off every where else, Guess what, I will still be here, posting, like I have for the past 10 years
Clinical research is over your head. You just insist people believe what you say simply because you say it,
you are going to get your ass kicked over here constantly just like everywhere else you have been.
Your views are not about knowledge--but about money and promotion to make more money. Unfortunately selling sugar to newbie’s.
I just hope you don't influence newbie’s with all your misinformation
Smart people know better. You are use to talking to teenagers in high school who want to know what supps to buy ---clueless,
Which forum were you kicked off of and exposed by Jenetic? I can remember can you?
You Do you remember Jenetic? Correct?
You have never made a sane comment about anything I have ever said, only personal attacks, and petty angry remarks slanderous comments all meaningless, but you are terrified some one will expose you again, and again, like they have on every forum in North America.
he's an asshole, plain and simple-You are the Einstein of the board, lets see how long you make it this time,
would you like to measure it in weeks, days or hours,
Good Bye,
S
straintendons
Guest
lets just put it this way nelson, your trying to sell somthin but solidspine isnt, which makes him less bais and therefore more honest about what comes out of his mouth unlike the smelly shit that comes outa yours 
lol smelly nelson.. hopefully that'll catch on.. smelly nelson smelly nelson come and play with me, choo choo, smelly nelson smelly nelson one big family.. what ya think nelsy? like my song??
lol smelly nelson.. hopefully that'll catch on.. smelly nelson smelly nelson come and play with me, choo choo, smelly nelson smelly nelson one big family.. what ya think nelsy? like my song??
mrwhiterightsnow
New member
i have been here since march of 03' under many different account, and i have always been under the impression that Nelson was a down to earth, very experimental individual who seems to be somewhat safe with his body as far as use goes and has always tried to be helpful to fellow members. without ever meeting him, i would say he is legit, and more trustable than many i would think to trust on this board with advice, and products if hes come up with some
A
Anthony Roberts
Guest
solidspine said:
I suspect that it will be the other way around. Just my thoughts.
O
odoyal rulez
Guest
Solid Spine knows his shit....NM doesnt know shit, and AR is a piece of shit...just summarizing this thread.
TrenAman
New member
Under 3 usernames I have been on this site for almost 2yrs. In that time frame you can sort people out. SS knows what the fuck he is talking about and NM.. well.. just listen how EVERYONE feels about him, for every 10 guys blasting him there is 1 guy "prolly NM with a different username" saying he is OK. Point is, SS has greatly contributed to this forum and others. NM's posts.. well.. people just eat him alive on everyone!
AR, to say SS would be banned before NM is a joke. You would only make SS's arguement fact. It is all about $$ and sugar pills.
AR, to say SS would be banned before NM is a joke. You would only make SS's arguement fact. It is all about $$ and sugar pills.
A
Anthony Roberts
Guest
Make what a fact? That EliteFitness.com is a business? I think that's pretty well established. Sometimes, however, it becomes necessary to lose money (and drop a sponsor/author) because they bring the site down...but although I've seen it happen here (last month), I don't think Nelson fits into that category. My opinion is that when that sponsor was dropped, they took a bunch of people loyal to them over to their forums, and it's basically those people who continue to attack sponsors/authors on this site.
I would bet almost any amount of money that the people who have been attacking myself and Nelson are all regular posters and members of that recently dropped sponsors' own message forum. In fact...people who were regular members of that old site (in it's former incarnation...like Fonz. et al) were the people who attacked Nelson in the past as well.
Perhaps when that cancer was removed as a sponsor, it was an incomplete operation...and we need to go back in and remove the rest of the cancerous cells.
Just a thought.
I would bet almost any amount of money that the people who have been attacking myself and Nelson are all regular posters and members of that recently dropped sponsors' own message forum. In fact...people who were regular members of that old site (in it's former incarnation...like Fonz. et al) were the people who attacked Nelson in the past as well.
Perhaps when that cancer was removed as a sponsor, it was an incomplete operation...and we need to go back in and remove the rest of the cancerous cells.
Just a thought.
Anthony Roberts said:
There may be some of that. But I think it's also ignorance and fear.
Some people don't know what to think so what are they going to support? A chance to think more deeply? Or some guy who shouts and destroys? Of course, a small mind will chose the later. It's easier. It appeals to a more base sense. It makes them feel big because they fear their inadaquancies. And the last thing they want is a reminder of their inadaquacies.
Some people are sheep -- they pick a team, a clique, a political party, a religion, a guru -- you name it...and they follow and defend it to the death. It hasn't nothing to do with rational thought. That's too hard. They don't wait to get the facts. The accusations are good enough...and oh so great to believe -- even if they aren't true. They'll repeat the lies and recruit others with weak will. Strength in numbers. It's been going on since the dawn of time so I don't have much hope of it stopping here.
Then there are those who can think for themselves. They aren't afraid to stand apart from the herd. It can get lonely in that spot , but if you have character, it's the only choice. I'm sure many of you know what I'm talking about. I can see. There are a lot of smart bros here. But it's the empty barrel that makes the most noise.
There are plenty of people here with a lot to offer and even when someone may have a difference of opinion with me or anyone else, he or she will sure as hell can recogonize a disruptive blowhard when they see him.
The worst part of it all is the fact that we have to spend time with all this. In businesses I've run, when I saw a problem, I got rid of it. If someone was a disruption, even if he had a few cronies on his side, he'd be gone. Everyone was better off. That should be done here. But it's not my call.
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worldclass
Banned
Has it really escaped your attention that since this site kicked off it's smartest member and moderator it's gone down farther than at any point in it's history. That a desperate attempt to bring someone to fill the void resulted in Nelson and you. Nelson was run off this board twice because he did not understand the science of anything he posted about. You were so afraid of Macrophage you ran and hid every time he challenged your theories. Now that there is no one to expose you and Nelson you have balls of steel. Ban the world if they don't conform. Are you going to ban IBE and the judge that rules in their favor?
The decision to take this board to where it is now was a mistake. It's lost traffic, veteran members, lots of money, and is a hatefest because people liked the board the way it was when they got here over the last decade. You've soiled it. It's odd to me that you brag about tearing it down. How could you be proud of what you've done? You act like Bush about Iraq. Everyone sees it but you.
worldclass said:
It must be great to have such confidence in your own bullshit.
I was run off the board? Don't be a dope. I left becauseI had better things to do than fight with morons. The people who harrassed me were found to be scammers. One guy didn't even work out. Another was busted for fraud.
These are the people you're defending? These are the people you want back?
The internet is an amazing thing. Idiots think because they have equal say that what they say was equal merit. Bully mentality runs rampant.
What I don't understand is; if all this bothers you so much, why the hell are you here? I sure as hell wouldn't waste my time with something that I felt wasn't worthwhile. Or do you think this is your private little sandbox and everyone has to do as you say?
Leave -- you and ss and odyz and the three or four others with nothing better to do than gripe. Leave the forum for those who want to learn, have fun and engage in interesting conversation.
Why is it always the people with nothing to offer who take down every thread? Oh yeah, I just answered my own question. Destroying is easy. It's all they can do.
Pat_McCrotch
New member
Nelson Montana said:
is it 20 or 25 years experience you said both?
Pat_McCrotch
New member
Anthony Roberts said:
so now AR is an expert on cancer. When is that book coming out?
errn247 said:
Is it really that important? Okay, since we're hear to debate minutia.
I got involved in bodybuilding very young -- 14 years old. And this was a time when it wasn't popular. When I was AROUND 15 years old ( Maybe I was 16?") when I saw Arnolds first apperence in the States at the Brooklyn Academy of Music in 1969. (He lost to Sergio Oliva).
I knew a lot as a young man , but had the worst genetics in the world. Everyone I coached got bigger than me!
I was on and off with BB until 1976 or so. (When was Pumping Iron?) I got back into it again at that point. That was the day there was always someone with a bagful of bottles of 100 d-bol for 10 bucks. But I was natty. The training I experienced both personally and among others at that time was beyond brutal and an aproach I haven't seen since. It was truly hardcore.
Wife, kid, job, etc, etc. Walked away from it for a while. Got back into it in 1996. (97?) Discovered a whole new method of training that gave me gains in my late 30's I'd never gotten before. Did my first cycle at age 41 -- or 42. (Bad with exact dates).
Began writing for various mags. Wrote on the administartion of steroids (Steroids For Health) which is considered by many to be one of the first and most influential reports on safe steroid use for the bodybuilder. I had the balls to disagree with Dan Duchaine -- the foremost authority at the time. He called me to say I was right.
I went from trying to find as much information as I could on Dan, Dave Draper, Charles Poliquin, Paul Borresson, Dan Lurie, Dareem Charles...to having their home phone numbers.
I'm 53. It's 2007. So excluding my little lapses along the way, how long would you say I've been involved in bodybuilding? But that wasn't really what you wanted to know, right?
Then of course there's solidspine. He's a guy on a message board who makes shit up.
It's your choice whose point of view you feel is more worthy of consideration.
O
odoyal rulez
Guest
Im not stirring up anything...I just dont want the newbs to fall for your bullshit.
You want facts?
You endorsed a product that had been out for 5 weeks that you never even used before as a replacement PCT for a steroid cycle.
Thats an undeniable fact, everyone here read that thread.
Fact
Anythony Roberts is a liar, a conman, and an excon. He is affiliated with "The Roid Store" which took hard earned money from one of our servicemen in Afghanistan, because he had no clue it was a bullshit site.
Nothing you two guys ever post on this site will ever matter because the people that know about you two are not going to sit here and watch you give out horsehit advice to people that fell here from googlesearching and assume because you inflate your shitty fake resumes that you know what your talking about.
Stick to the training forums where you can actually contribute and stay off this one...and AR just needs to disapear from here.
You want facts?
You endorsed a product that had been out for 5 weeks that you never even used before as a replacement PCT for a steroid cycle.
Thats an undeniable fact, everyone here read that thread.
Fact
Anythony Roberts is a liar, a conman, and an excon. He is affiliated with "The Roid Store" which took hard earned money from one of our servicemen in Afghanistan, because he had no clue it was a bullshit site.
Nothing you two guys ever post on this site will ever matter because the people that know about you two are not going to sit here and watch you give out horsehit advice to people that fell here from googlesearching and assume because you inflate your shitty fake resumes that you know what your talking about.
Stick to the training forums where you can actually contribute and stay off this one...and AR just needs to disapear from here.
floridalife
New member
yeah well because someone has worked out for 20 years and taken a cycle or two DOES NOT make them an expert or give them the right to give people advice. That's really been bugging me lately. This is life or death in many cases, advice should come from dcotors, people with degrees people who have severely studied the compounds and know it from a science point of view, etc. Now if someone has been juicing, hgh etc for 20 + years and on TOP of that really studied and researched then i would be curious to hear what they have to say.. but I'm sick of bogus advice, people becomoing overnight book writers because they know how to copy and paste, and rediculous joke products being slung left and right
MichaelScott
New member
i come here to try and learn and NM posts are long propoganda filled commercials.
odoyal rulez said:
..
A
Anthony Roberts
Guest
odoyal rulez said:
I'm not affiliated with the Roid Store. I don't know why you seem to think I am affiliated with a company that one of my friends owns. I don't make a cent from that business.
Also...you're correct. Someone needs to disappear.
floridalife said:
..
silver_shadow
New member
dude can you break that into paragraphs and make it a little easier for usSam5 said:
O
odoyal rulez
Guest
NO. I SAID IT LOOKED GOOD AND IT MIGHT BE WORTH A TRY EVEN THOUGH I DON'T MAKE A PENNY FROM IT. THIS IS WHAT HAS YOUR PANTIES IN A TWIST?
No, no you didnt...this is just you backpedaling once again and tripping over your words. Lets look at what you actually said.
Recommendations
Always use the lowest amount of any drug to get the maximum effect.
Always add a natural substance to safely improve the effects of the drug regime.
For natties in-between cycles; "Post Cycle" along with "CytogenX" or "Dermacrine" are more than enough to keep excess estrogen at bay.
For those on HRT: 1/4 mg of a-dex 3X's a week plus low dose CytogenX, Dermacrine or Post Cycle.
ALWAYS, ALWAYS, More than enough...thats not saying its worth a try asshole, thats you endorsing products for your clique that youve never used.
Once again, you lose....I guess your going to say "whatever kid" and go crawl back into your hole.
No, no you didnt...this is just you backpedaling once again and tripping over your words. Lets look at what you actually said.
Recommendations
Always use the lowest amount of any drug to get the maximum effect.
Always add a natural substance to safely improve the effects of the drug regime.
For natties in-between cycles; "Post Cycle" along with "CytogenX" or "Dermacrine" are more than enough to keep excess estrogen at bay.
For those on HRT: 1/4 mg of a-dex 3X's a week plus low dose CytogenX, Dermacrine or Post Cycle.
ALWAYS, ALWAYS, More than enough...thats not saying its worth a try asshole, thats you endorsing products for your clique that youve never used.
Once again, you lose....I guess your going to say "whatever kid" and go crawl back into your hole.
A
Anthony Roberts
Guest
Sam5 said:
Think about that statement logically. There isn't one published author over on those sites (combined membership, roughly 5% of Elite's), and not one industry-relevant contact for Nelson. I could yell out my window and reach as many people.
Nelson is here, with nearly 150k members, on a site that is sponsored by the company which produces his supplements, and published his books.
Why would he waste his time (as a professional) on a site that has no professional value to him?
Think about that logically.
That's all I'm saying.
floridalife
New member
yawn
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Sam5
Guest
As I can see, and as you have stated, it is all about selling for you. Which is fine, we all have to make money. I really don't think there are a whole lot more people that post here than at most boards. Now there may be alot of lurkers, that I do not know. I was coming from the standpoint of wanting to gain and exchange "real" knowledge. Being a published author does not make you the guru as you seem to think you are.Anthony Roberts said:
Challenge the creds of people like Gavin all day if you want, he has his hands full training IFBB clients, but then you probably don't believe that because of your dislike for him, and that is fine, but don't discredit him because he is not a published author. That is cool that you are, congratulations, it takes time and dedication to write a book. Even if you were to come over to any of the other boards and tout your book and knowledge, I really don't think it would fly, despite the low membership numbers.
Your playing the numbers game and that is smart for you because it is about exposure. So far, as I've said, I'm not a fan. I don't hate you or anything, I just would'nt personally waste money on your book when I do fine as is and feel that I can get more valuable knowledge from others. Thats all I'm saying.
odoyal rulez said:
You're taking one thing out of context and using it to claim I didn't say something? Dude, you have to do better than that.
Nevertheless, everything stated was true.
You may want to watch your words big guy. You're getting dangerously close to being banned.
To Sam5. Points well taken. But remember one thing. NOT EVERYTHING IS OPINION. If T levels are raised after an injection, they are raised. If they're not , they're not. That is indeed provable. A fact is sometimes a fact and offering a non fact is not a viable alternative.
I don't know who Gavin is or anybody else on one of a million message boards. Who cares?
I knew one guy who was actually very knowledgeable who ripped hundreds of people off by selling them a newsletter that was never sent. His excuse was that he needed money to pay for his legal fees for being busted with drugs. There are a million guys like this all over the place.
It's amazing. People get thousands of dollars worth of information here for FREE and they complain when the same person makes an honest recommendation for a good product now and then. Grow the fuck up.
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Anthony Roberts
Guest
Sam5 said:
Yes, since I'm a professional, it's about making money for me...Making money doing something I love, though. But making money and being a full time professional allows me to devote myself full time to research and affords me the industry connections and contacts to produce a higher quality of work than if I had to do another job to support myself. It's symbiotic with the people who support me financially by purchasing my products and publishing my articles. I get paid, therefore affording me the means and opportunity produce a high quality product, which they benefit from.
Ok...without being condescending (seriously) you're overlooking too many things regarding using the internet and internet message boards, to effectively discuss marketing (of the type both myself and Gavin engage in). Suffice to say (and again, I'm not being a dick) , you don't really have a grasp of internet marketing and internet based sales. It's not really something I want to get into, but I've spent more time than I care to admit learning about marketing, and the forums are almost completely unimportant for marketing, relative to the site, the main page, the URL, the mailing list, etc...
I wish Gavin nothing but the best, and hope he eventually acheives all of his goals in the industry.
But regarding marketing, it's a lot to go into, and not really interesting. The forums, suffice to say, are the least important revenue stream, all things considered. Look where those sites rank on SEO or Google or whatever, to see what I'm talking about...then compare them to the sites I regularly write for.
I haven't challenged anyone's credentials with my last post...I hope it doesn't look that way. I was simply saying that you are looking at things from an inappropriate point of view. If you're a professional, you do what you do to make money. Those sites will not put a single cent more in Nelson's bank account, and likely do not have the potential to do so.
Finally, not only have I never called myself a "guru" I actually shun the title. In the intro to my book, I say that I'm not a guru, in fact.
(ALSO...I have IFBB clients as well. Just an FYI. It's not a huge deal.)
I don't mean this to be nasty, but think about your post and invitation to Nelson from a professional point of view, and ask yourself if you'd go to those boards yourself if you were him.
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Sam5
Guest
I agree, there are lots of people all over the net that claim to be whoever they claim to be. And I agree about the test levels and all that. I hope the product thing was not aimed at me because I really don't care about that.Nelson Montana said:
On another note though. How do you expect to have a good number of customers behaving the way you do. I mean, your an outright dick. There is no short way around the bush on that one. No matter how much you know or think you know, your a very abrasive person who couldn't sell icewater to a man in Hell. And that my friend is pure, unadulterated fact. You may know alot about bodybuilding, but in order to capitalize you have a lifetime to learn about how to treat people and shmooz. You may not like everyone, but if your a salesman, you sure as hell better conduct yourself better than you do.
Let me guess, I'll bet there is another tough guy remark soon to follow. Don't make a fool of yourself anymmore than you have to, Einstein. LMFAO.
A
Anthony Roberts
Guest
Sam5 said:
As I said in my last post, the forums are the least important part of sales. Honestly, statistically speaking, the EF e-mail mailers, the books on the main page, etc...are much more important.
Look at the google rating for the main page, then for a thread in the forum, and you'll see what I mean. Less than 2% of every visitor to a main page ever goes to the forums, and even then only about 1-2% register...even less post.
Stil think that forums are that important? Or think the people you mention on other forums will go very far being the gods of the internet steroid forums? Give it an honest think.
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Sam5
Guest
I understand what your saying, and I understand how marketing works on the net, I just think that the money should not be so involved on the forums. And from what you said, I don't think there is a reason to make it such a prescence in the forums since it is such a low percentage of total sales. I myself don't come here to buy products, books, or really anything else for that matter. I come here for the exchange of knowledge and it just seems that there is a lot of solicitation going on between the lines.Anthony Roberts said:
And I guess if I don't like it, then I should go elsewhere, which I do. If your training pro's then yes, that is something to speak of. It gives you credibility in my book.
A
Anthony Roberts
Guest
Sam5 said:
Pro Bodybuilders? Not in my book. It means you're third or fourth rate, as a trainer.
Honestly, if you're a first rate trainer, you're training people in the NFL, NBA, College, or MLB.
Think about that. Then tell me where you rate someone who hasn't been published, and is "the man" on some 5k member forums, and doesn't train people in a premier prefessional or Collegiate environment.
You've kept up with me so far...now I'm asking you for one more leap. Think about how you define success and credibility, and think about what I'm saying, and think about whether you want to re-evaluate how you view things, people, etc...
R
Ross
Guest
Training for an ATHLETIC goal is COMPLETELY differerent than training for a BODYBUILDING goal.
Comparing Kobe Bryant to Ronnie Coleman is just absurd.
I still love you Anthony.
FYI, Anthony knows his shit...
Comparing Kobe Bryant to Ronnie Coleman is just absurd.
I still love you Anthony.
FYI, Anthony knows his shit...
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Sam5
Guest
I don't think I view people in an innappropriate way at all. I didn't have all the facts. If you're training NFL'ers and such then you are very successful and my hat is off to you. But that is not where it stops. Being that this is the internet then you must show your creds in some way that will make these kinds of claims believeable. Now I know what you will say to this. I train pro athletes, why would I care about such a little man as yourself or others on the forums. Well, ROSS, in another thread was very helpful to me, and he consistently showed his knowledge post after post and didn't argue with anyone really. In fact he ignored the slams and only responded appropriately to the nonargumentative comments made in the thread. This was impressive and I offered to buy his book because of his great salemanship, that is money in his pocket. And one guy can turn into many guys. You can make money anywhere man and it all adds up.Anthony Roberts said:
I re-evaluate how I view people when I get facts that require me to re-evaluate. Hell this arguement for all of it's brandishing of ego's may turn out to be quite productive. And in all honesty, I think the ego's were put away a few responses ago.
A
Anthony Roberts
Guest
Sam5 said:
I'm not saying that I do or don't train professional athletes...what I'm saying is that calling someone a "top trainer" or something like that when they train BodyBuilders is kind of myopic. The IFBB "pro's" I work with have jobs...being a "professional" (insert occupation) is what you do for a living...most IFBB "professionals" can not earn a living from competition. A professional in any other sport pretty much can earn a living...hence being professional.
The reality is that the world's top trainers (those who are literally the best, not Keyboard-Cowboys who online train)...would likely almost never bother with training a bodybuilder.
Thus, to say someone is a top or elite or world class trainer, when they train professionals in perhaps the lowest (professional) rung of professional competitions. It's harder to get a job training athletes at a DIII college as an assistant coach than it is to get a job training in bodybuilding. And chances are that the DIII college will have more people in the crowd at their games than are at the Mr.O.
Think about this (training, consulting, writing, etc...) in professional (and broad) terms, and then look where different people are. Look at who is posting on the internet vs/ writing books, etc...
As Nelson has said in the past, many people who are Keyboard Cowboys and e-Experts on the 'net are basically not even in the industry in any real measure of the word. This is what I'm saying about training credentials, writing credentials, etc...
Just do me a favor and look at things in terms of reality, not e-reality.
Also...if you take a look at some guru's....whom do they talk about (me). And whom do I talk about? I almost never mention anyone else in my field.
I did an article with Collins, Kneller, Llewellyn, Berardi etc...I did one with Cy Wilson....think about why (*whoever) wasn't included in those articles, or asked to work with the best in the business, then think about where they actually stand in this industry.
Check out my home page and see what people in the (real/professional) industry have said about me. I've got comments from a coach/trainer from UConn on there, head of a huge nutritional company, etc...
Honestly...just evaluate things with some real world attention, not just forum-B.S. Look who posts my articles (they're on literally every aas site on the 'net) and look who posts...whoever you think is credible's...look where more are posted and where more are in general...think about things with an eye towards professional criteria and evaluate. Now ask yourself:
"If Roberts has influence on the 5 top sites for AAS info, why would someone who aspires to be in that field bash him, and virtually insure he'll never be on those sites?"
See what I'm saying?
You'll come around to seeing it like me I think.
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Sam5
Guest
I think looking at bodybuilders as low rung is myopic ina way. The simple fact is that it is undergraound and always has been. Bodybuilding is not normal. This does not mena that they are not pro's. You're getting into semantics here kinda like when you were debating the whole convict thing. Stop it.lol Yes genetics plays into it but bodybuilding requires a great amount of know how to actually be successful at it. Allright, with every post you're going to pick something that I said to debate against. We've been as productive as we can possibly be here so for all practical purposes, I believe it would be nice to be done.Anthony Roberts said:
Ich verschwende an dich keine Mühe mehr. Alles in ordnung.
Sam5 said:
I'm a dick?
You actually bring up a good point. If I'm looking for business, shouldn't I be kissing ass and telling people what they want to hear and agreeing with everyone and calling them bro? Yeah. But what's more important to me than selling a few bottles of something is telling the truth the best I know how. If that comes off a little gruff, what can I tell you. ( I'm from New York!)
That's why I'll let someone know if they're compromising their heath. More often than not, they get pissed. That's a lost potential customer. That's another member who might want to take me down. But I don't care.
I can't tell you how many issues have been debated against me that are now considered standard thinking.
The comparison of milligram strength.
The over use of anti-e's.
Decas supposed non estrogenic qualities
Lowering SHBG to increase free tetosterone
The catabolic nature of cardio
Scam supplements such as tribulus and vitex
The folly of carb free diets.
Exposing Bill Phillips and Scott Conelly
Why winstrol can't cause gyno
The fact that green tea contains thyroid damaging flouride.
The estrogenic effects of pro hormones
Exposing Victor Conte
The proper way to train smaller muscle groups
The benefits of Primobolin
The benefits of avenacosides A&B
The uselessness of glutamine.
All of these subjects and more were points of contention where board members lambasted me. Today, most everyone is in agreement with what I said. What happened?
Meanwhile, other "good bros" piled on and tried to discredit me while selling their own snake oil. Today, they're gone.
But I have one thing going for me. I've been proven right. Does that make me a dick? Yeah, in some eyes maybe. But I'd rather be a rightious dick than a popular fraud.
Pat_McCrotch
New member
Nelson Montana said:
I was just asking. Alot of people who are full of shit cant get thier numbers right and when your underfire for your works it is important to sound credible when giving your history. Thats it.
S
Sam5
Guest
You know, when it comes down to it, your probably all good guys. The internet makes it tough to really look at things in a realistic way, as Anthony put it. That is just the way it is.
When you have a theory, and that is what every idea starts out as when using the scientific method, and it is not commonly understood by the masses then you must expect that you are going to have "discourse".
Alot of people though DaVinci was nuts too.
I'm interested in the whole glutamine is worthless thing. I've never wasted my money on it, but would be interested to know what your thought is on that. Don't disappoint me.
God, I gotta get a job. This is pathetic, I've never had more time on my hands than I have since becoming a worthless college student.
When you have a theory, and that is what every idea starts out as when using the scientific method, and it is not commonly understood by the masses then you must expect that you are going to have "discourse".
Alot of people though DaVinci was nuts too.
I'm interested in the whole glutamine is worthless thing. I've never wasted my money on it, but would be interested to know what your thought is on that. Don't disappoint me.
God, I gotta get a job. This is pathetic, I've never had more time on my hands than I have since becoming a worthless college student.
errn247 said:
Understood. No problem.
Sam5 back in 1999 I came out saying that glutamine is worthless -- for several reasons.
The theory sounded good. Glutamine is the most abundant amino in muscle. For this reason the supp companies knew they could sell it. But glutamine is a NON essential amino. Does that mean we don't need it? No. It means the body makes it on its own from other proteins. (Actually BCAA"S)
Stands to reason -- eat enough protein, the body will make enough glutamine.
I've also been around long enoght to know about isolated aminos. They just aren't very effective. If they weren't in 1979, chances are they won't be in 1999.
And another thing...you can take ANY amino, and by itself it looks amazing.
I also remember the studies done back in the 70's with arginine. It releases growth hormone , when taken IV. That got me searching about the oral administration of glutamine. (And remember, at this time I had a bit of an inside track to the supp industry). There was not a single peer reviewed study done with oral glutamine.
The same goes with ZMA by the way but that's another story. The only test was done by BALCO!!!
Anyway, my conclusion: oral supplemental glutamine is worthless.
The verdict, by the then "gurus" such as Lyle McDonald, Bill roberts, Pat Arnold, Will Brink as well as every internet "know it all" was the same ..... NELSON IS AN IDIOT! HE DOESN'T KNOW SCIENCE! HE"S JUST SAYING THAT BECAUSE HE DOESN"T SELL IT! WHERE"S HIS DEGREE IN NUTRITION? BLAH BLAH BLAH BLAH
Well, guess what? I was right.
There have been subsequent studies on the effects and absorbtion of glutamine and its effect on muscle synthesis. The verdict every time. No effect. Not even an increase of glutamine in the bloodstream. Why? Because of my common sense theory form the start. The body was not meant to take it that way! It makes it on its OWN!
Hope you're not disappointed.
R
Ross
Guest
Nelson Montana said:Understood. No problem.
Sam5 back in 1999 I came out saying that glutamine is worthless -- for several reasons.
The theory sounded good. Glutamine is the most abundant amino in muscle. For this reason the supp companies knew they could sell it. But glutamine is a NON essential amino. Does that mean we don't need it? No. It means the body makes it on its own from other proteins. (Actually BCAA"S)
Stands to reason -- eat enough protein, the body will make enough glutamine.
I've also been around long enoght to know about isolated aminos. They just aren't very effective. If they weren't in 1979, chances are they won't be in 1999.
And another thing...you can take ANY amino, and by itself it looks amazing.
I also remember the studies done back in the 70's with arginine. It releases growth hormone , when taken IV. That got me searching about the oral administration of glutamine. (And remember, at this time I had a bit of an inside track to the supp industry). There was not a single peer reviewed study done with oral glutamine.
The same goes with ZMA by the way but that's another story. The only test was done by BALCO!!!
Anyway, my conclusion: oral supplemental glutamine is worthless.
The verdict, by the then "gurus" such as Lyle McDonald, Bill roberts, Pat Arnold, Will Brink as well as every internet "know it all" was the same ..... NELSON IS AN IDIOT! HE DOESN'T KNOW SCIENCE! HE"S JUST SAYING THAT BECAUSE HE DOESN"T SELL IT! WHERE"S HIS DEGREE IN NUTRITION? BLAH BLAH BLAH BLAH
Well, guess what? I was right.
There have been subsequent studies on the effects and absorbtion of glutamine and its effect on muscle synthesis. The verdict every time. No effect. Not even an increase of glutamine in the bloodstream. Why? Because of my common sense theory form the start. The body was not meant to take it that way! It makes it on its OWN!
Hope you're not disappointed.
Nelson, that is NOT entirly accurate:
1: JPEN J Parenter Enteral Nutr. 1990 Jul-Aug;14(4 Suppl):137S-146S. Links
Safety and metabolic effects of L-glutamine administration in humans.Ziegler TR, Benfell K, Smith RJ, Young LS, Brown E, Ferrari-Baliviera E, Lowe DK, Wilmore DW.
Department of Surgery, Brigham and Women's Hospital, Boston, Massachusetts.
A series of dose-response studies was conducted to evaluate the clinical safety, pharmacokinetics, and metabolic effects of L-glutamine administered to humans. Initial studies in normal individuals evaluated the short-term response to oral loads of glutamine at doses of 0, 0.1, and 0.3 g/kg. A dose-related increase in blood glutamine occurred after oral loading and elevation of amino acids known to be end products of glutamine metabolism occurred (including alanine, citrulline, and arginine). No evidence of clinical toxicity or generation of toxic metabolites (ammonia and glutamate) was observed. Glutamine was infused intravenously in normal subjects over 4 hr at doses of 0.0125 and 0.025 g/kg/hr. In addition, glutamine was evaluated as a component of parenteral nutrition solutions (0.285 and 0.570 g/kg/day) administered for 5 days to normal subjects. Intravenous administration of glutamine was well tolerated without untoward clinical or biochemical effects. Subsequent studies in patients receiving glutamine-enriched parenteral nutrition for several weeks confirmed the clinical safety of this approach in a catabolic patient population. In addition, nitrogen retention appeared to be enhanced when glutamine was administered at a dose of 0.570 g/kg/day in a balanced nutritional solution providing adequate calories (145% of basal) and protein (1.5 g/kg/day). Nitrogen balance in patients receiving lower doses of glutamine (0.285 g/kg/day) was similar to that in patients receiving standard formulations. Further controlled clinical trials of the metabolic efficacy, tolerance, and dose response of glutamine in other patient groups are necessary to determine the appropriate use of glutamine enrichment of nutrient solutions.
PMID: 2119459 [PubMed - indexed for MEDLINE]
R
Ross
Guest
I also disagree with you on Tribulus EXTRACT. Tribulus Terrestris PLANT is worthless GARBAGE. A STANDARDIZED Tribulus EXTRACT is NOT:
The Journal of Alternative and Complementary Medicine
Sexual Effects of Puncturevine (Tribulus terrestris) Extract (Protodioscin): An Evaluation Using a Rat Model
Apr 2003, Vol. 9, No. 2 : 257 -265
Kalamegam Gauthaman, MBBS
Department of Obstetrics and Gynaecology, National University Hospital, National University of Singapore, Singapore
Adaikan P. Ganesan, PhD, DSc
Department of Obstetrics and Gynaecology, National University Hospital, National University of Singapore, Singapore
R. N. V. Prasad, FAMS, FRCOG, DSc
Department of Obstetrics and Gynaecology, National University Hospital, National University of Singapore, Singapore
Objective: Apart from its claims for improvement of sexual functions in men, the puncturevine plant (Tribulus terrestris: TT) has long been considered as an energizer and vitalizer in the indigenous system of medicine. Sexual behavior and intracavernous pressure (ICP) measurements were taken in rats to scientifically validate the claim of TT [containing protodioscin (PTN)] as an aphrodisiac.
Materials and methods: Forty sexually mature male Sprague-Dawley rats were randomly divided into four groups of 10 each. Group I served as a control group and groups II, III, and IV were treated with three different doses of TT extract (2.5, 5 and 10 mg/kg body weight, respectively), orally, once daily for 8 weeks. Weight was recorded and the rats from all four groups were subjected to sexual behavior studies with primed females and various parameters namely mount and intromission frequencies (MF and IF, respectively), mount, intromission and ejaculation latencies (ML, IL, and EL, respectively) as well as postejaculatory interval (PEI) were recorded. In addition, blood pressure and ICP were recorded for all rats at the end of study.
Results: Increases in body weight (by 9, 23, and 18% for groups II, III & IV) and ICP (by 43% and 26% for groups III and IV) were statistically significant compared to the control group. Increases in MF (by 27% and 24%) and IF (by 19% and 22%) for the groups III and IV were statistically significant. Decreases in ML (by 16%, 23%, and 22% for groups II, III, and IV) and PEI (by 20% for group III) were statistically significant compared to the control.
Conclusions: The weight gain and improvement in sexual behavior parameters observed in rats could be secondary to the androgen increasing property of TT (PTN) that was observed in our earlier study on primates. The increase in ICP which confirms the proerectile aphrodisiac property of TT could possibly be the result of an increase in androgen and subsequent release of nitric oxide from the nerve endings innervating the corpus cavernosum.
This paper was cited by:
Botanical therapies in sexual dysfunction
Binu Tharakan, Bala V. Manyam
Phytotherapy Research. 2005, Vol. 19, No. 6: 457
CrossRef
The Journal of Alternative and Complementary Medicine
Sexual Effects of Puncturevine (Tribulus terrestris) Extract (Protodioscin): An Evaluation Using a Rat Model
Apr 2003, Vol. 9, No. 2 : 257 -265
Kalamegam Gauthaman, MBBS
Department of Obstetrics and Gynaecology, National University Hospital, National University of Singapore, Singapore
Adaikan P. Ganesan, PhD, DSc
Department of Obstetrics and Gynaecology, National University Hospital, National University of Singapore, Singapore
R. N. V. Prasad, FAMS, FRCOG, DSc
Department of Obstetrics and Gynaecology, National University Hospital, National University of Singapore, Singapore
Objective: Apart from its claims for improvement of sexual functions in men, the puncturevine plant (Tribulus terrestris: TT) has long been considered as an energizer and vitalizer in the indigenous system of medicine. Sexual behavior and intracavernous pressure (ICP) measurements were taken in rats to scientifically validate the claim of TT [containing protodioscin (PTN)] as an aphrodisiac.
Materials and methods: Forty sexually mature male Sprague-Dawley rats were randomly divided into four groups of 10 each. Group I served as a control group and groups II, III, and IV were treated with three different doses of TT extract (2.5, 5 and 10 mg/kg body weight, respectively), orally, once daily for 8 weeks. Weight was recorded and the rats from all four groups were subjected to sexual behavior studies with primed females and various parameters namely mount and intromission frequencies (MF and IF, respectively), mount, intromission and ejaculation latencies (ML, IL, and EL, respectively) as well as postejaculatory interval (PEI) were recorded. In addition, blood pressure and ICP were recorded for all rats at the end of study.
Results: Increases in body weight (by 9, 23, and 18% for groups II, III & IV) and ICP (by 43% and 26% for groups III and IV) were statistically significant compared to the control group. Increases in MF (by 27% and 24%) and IF (by 19% and 22%) for the groups III and IV were statistically significant. Decreases in ML (by 16%, 23%, and 22% for groups II, III, and IV) and PEI (by 20% for group III) were statistically significant compared to the control.
Conclusions: The weight gain and improvement in sexual behavior parameters observed in rats could be secondary to the androgen increasing property of TT (PTN) that was observed in our earlier study on primates. The increase in ICP which confirms the proerectile aphrodisiac property of TT could possibly be the result of an increase in androgen and subsequent release of nitric oxide from the nerve endings innervating the corpus cavernosum.
This paper was cited by:
Botanical therapies in sexual dysfunction
Binu Tharakan, Bala V. Manyam
Phytotherapy Research. 2005, Vol. 19, No. 6: 457
CrossRef
- Ross - said:
Okay, this one showed a SHORT TERM increase in blood level from oral loading. (Which can cause stomach upset). But there was no increase in nitrogen retention except in the group that received it intravenously! THAT CONFIRMS MY POINT!
- Ross - said:
I've also seen this study -- from the Journal of ALTERNATIVE medicine.
Some wild leaps in speculation there. A 27% increase in sexual activity among 40 rats? That's like one more rat fucking. Sorry, I just don't buy it.
R
Ross
Guest
Tribestan Clinical Studies
3. CLINICAL STUDIES
3.1. Materials and methods
The experimental data from Tribestan administration have been clinically confirmed so far by three groups of researchers: by the Higher Military Medical Institute under the guidance of Prof. I. Viktorov, Corresponding Member of the Bulgarian Academy of Sciences; by the Medical University of Sofia; State University Hospital of Endocrinology, Gerontology and Geriatry, under the guidance of Prof. E. Bozadzhieva, and by the National Institute of Obstetrics and Gynecology - under the guidance of Prof. M. Protich.
The studies were carried on 212 male individuals, aged between 14 and 60 years. The therapeutic properties of Tribestan were studied in patients with partial or complete impotence. Both the tolerance and the adverse effects of the product were studied. The studies were carried out by the method of simple blind experiment, using placebo. In nozological terms, the studies covered various types of male impotence: idiopathic oligoasthenozoospermia - 39 patients, resection of the left internal testicular vein in varicocele, with subsequent oligoasthenozoospermia - 50 patients; inflammatory process of the prostate with oligo- and azoospermia - 53 patients, primary and secondary male hypogonadism - 20 patients, impotentia coeundi - 50 patients. The product was individually administered to all patients who had not received hormonal agents for at least one month prior to the treatment.
The duration of the treatment depended on acuteness of the disease - 30 - 60 days on the average (Bozadzhieva et al., and Protich et al.) and 90 days (Victorov et al.). the mean daily dose was 3 - 6 filmtablets of 0.250g. Some of the patients were favorably affected by 3 tablets daily (Protich et al.), whereas the other research teams administered 6 tablets (3 x 2). The andrological state was used as the basis for the adequate evaluation of the reproductivity of the patients by all three teams. The basic parameters of sperm were observed, i.e. volume and pH of the ejaculate, concentration of spermatozoa (number/1ml), percentage of motile spermatozoa, mean rate of population motility and percentage of pathological forms of the spermatozoa. Detailed case history on the sexual behavior of the patients was recorded prior to and after the therapeutic Tribestan course. The effect of the product on hair growth was observed in some patients. One of the teams (Bozadzhieva et al.) also observed the changes in the serum levels of gonadotropins, progesterone, testosterone, estradiol and cholesterol. The other team (Victorov et al.) followed up the changes in testosterone serum levels in the Tribestan treated patients. The hormonal levels were radioimmunologically determined using kits and reagents provided by the French-Italian-Belgian Association CEA-IRE-SORIN. The results from these studies were statistically assessed by variation analysis.
3.2. Results
Significant changes in spermatozoon motility were found after Tribestan intake for 60 days (with a daily dose of 3 filmtablets) by males with idiopathic oligoasthenozoospermia. The number of spermatozoa with normal motility, as well as the mean motility rate, were increased.
The percentage of the motile spermatozoa was 29, on the average, prior to the treatment and reached up to 36.66 after the treatment (p < 0.005). The mean motility rate of spermatozoa prior to the treatment was 1.95 mm/sec, after the treatment - 3.63 respectively (p < 0.001). No changes were observed in the ejaculate volume. In both cases (before and after treatment) the ejaculate volume was within the limits of the norm, about 4 ml on the average. The number of spermatozoa in the treated patients was higher by 3 ml/ml ejaculate on the average. In some cases, normalization of the spermogram occurred during repeated treatment with a daily dose of 6 tablets. In these cases, the improvement of the spermogram (normalization of the increased viscosity, increased ejaculate volume, increased concentration and accelerated motility of the spermatozoa) was accompanied be elevation of the serum levels of the lutenizing hormone and testosterone, and reduction of the estradiol level.
The patients with idiopathic azoospermia after 90-day treatment with a daily dose of 1.5g are of particular interest. The results were significant in three of all 7 patients treated. No spermatozoa were detected prior to the treatment. After the treatment, 3.5-million/1ml ejaculate were recorded in one of the patients, 15 million/ml in the second and 28 million/ml in the third. The percentage of motile spermatozoa in the first patient was 10, and in the other two - between 25 and 30. The motility rate of the spermatozoa was about 5 mm/sec. In two of the patients, 30 - 40 spermatozoa per field were observed, and in the third - about 5 spermatozoa per field after the treatment, compared with the absence of any prior to the treatment. One of the patients failed to be affected by the product. The studies on the patients from that nozological group continued with the administration of maintenance dose.
The clinical comparison of the results from the treatment with provirone of patients with idiopathic azoospermia and after Tribestan administration revealed a favorable effect on three of the patients (out of 6), unsuccessfully treated with provirone for a long period of time. The results in the patients with varicocele and oligoasthenozoospermia as regards the motility of the spermatozoa were identical in the reports of all research teams, regardless of the differences in the doses and duration of the treatment. Protich et al. found an average of 26.88% motile spermatozoa prior to the treatment and after 60-day course with a dose of 1 tablet, three times daily - 39% (p < 0.02) with a mean motility rate of spermatozoa 2.06 mm/sec prior to the treatment and 4.44 mm/sec post treatment respectively. No change in the ejaculate volume was found. The other team (Victorov at al.) observed more pronounced changes in the ejaculate volume after 90-day treatment with a daily dose of 1.5 g (4.5 ml compared to 1 - 2 ml prior to the treatment, i.e. an average of 1.55 ml of ejaculate volume in all patients). The number of spermatozoa in 1 ml reached the values in 100% of the patients treated. The mean percentage of motile spermatozoa prior to the treatment was 2.06 and was increased to 33.09 (Tables 1,2,3).
Table 1. Results of Tribestan treatment (1 tablet 3 times daily for 60 days) of 38 males with idiopathic oligoasthenozoospermia (represented in mean values)
Indices Before treatment After treatment
a. Concentration of spermatozoa, million/ml 22.97 26.66
b. Motility, % 29.00 35.66*
c. Motility rate, mm/sec. 1.95 3.76*
Table 2. Results of Tribestan treatment (1 tablet 3 times daily for 60 days) of 16 males after varicocele operation with existing oligoasthenozoospermia
Indices Before treatment After treatment
a. Concentration of spermatozoa, million/ml 21.31 26.75
b. Motility, % 11.53 39.06*
c. Motility rate, mm/sec. 2.00 4.44*
Table 3. Results of Tribestan treatment (2 tablets 3 times daily for 90 days) of 36 males after varicocele operation and existing oligoasthenozoospermia
Indices Before treatment After treatment
a. Concentration of spermatozoa, million/ml 40.60 76.00*
b. Motility, % 3.05 33.09*
c. Motility rate, mm/sec. 2.06 4.44*
*The data are statistically significant.
The results of Tribestan administration to patients with unilateral or bilateral hypothrophy of the testes and azoospermia deserve particular attention. The patients complained of a sense of heaviness and distention, as well as of a slight pain in the testes between 40th and 60th day after the start of the treatment with a daily dose of 6 tablets. Upon examination, a slight pain in the testes occurred upon palpation, as well as a slight swelling, with no other evidence of pathological changes. Improvement both as regards the ejaculate volume and the concentration and motility of the spermatozoa was observed towards the end of the treatment. The testosterone serum level was elevated from 1.75 mg/ml to 3.75 mg/ml. The pain in the testicular region upon palpation abated within 2 - 3 months after treatment. Tribestan administration to patients with chronic inflammatory process of the prostate and disorders in the spermogram led to insignificant changes in these cases when the inflammatory process had been treated previously.
No changes were found in patients with chronic inflammation of the prostate (not treated previously). Out of 14 patients with reduced libido and absence of pathology in the male genital organs, treated for 30-days (daily dose - 2 tablets, three times), 12 manifested obvious improvement of the libido, one patient - a slight improvement (after a 60-day treatment cycle) and no effect was observed in another one. Out of a total of 36 patients with chronic prostatitis and reduced libido, 15 were very favorably affected by the end of the treatment cycle (a total dose of 90 - 100 g), 12 - favorably, and in 9 of the cases with a duration of the inflammatory process over 5 years, no effect occurred. The patients with hypotrophy of the testes and idiopathic azoospermia had no complaints as regards the libido, but in the course of the treatment aimed at improving the spermogram an apparent libido enhancement was recorded. Out of 9 patients treated for one of the gravest forms of male hypogonadism (Klinefelter's syndrome, due to chromosomal anomalies), the libido was enhanced in three of the patients, erection was reported in two and sexual intercourse and masturbation were reported in another two patients. Elevated levels of lutenizing hormone after the treatment were found in these patients. The levels of the remaining sexual hormones and cholesterol were reduced. Two of the patients with secondary insufficiency of sexual glands (Noonan's syndrome) attained improvement of the libido and erections during the treatment. The self-confidence was improved in one of them, and in the second - hair grew in the male genital region.
The results of the treatment of three patients with cryptorchidism (one of them with uncorrected malformation) comprised improvement of the libido and often masturbation. The duration of the erection was prolonged in one patient from that group, aged 37. The spermogram of the same patient was significantly better compared to the initial status one month after treatment, i.e. on day 90 ftehr the beginning. One patient with secondary hypogonadism reported hair growing in the axillary and genital region, parallel with enhanced libido and frequent masturbation.
The serum testosterone levels were elevated in 20 patients from various nozological groups, the initial and final values being within the norm. In seven patients with testosterone serum level below the lower limit of the norm, the physiological levels were reached after the treatment, whereas in the rest of the patients with normal initial levels, the testosterone was not significantly changed after treatment.
3.3. Tolerance and side effects
All clinicians engaged in the studies reported a very good tolerance and no drug-related side effects. The clinical laboratory data on Tribestan treated males showed no deviations in the blood count, ESR, flocculation tests and urine.
3.4. Discussion of the results
The clinical studies of all three research teams on a total of 212 patients (males with disorders in the sexual function) confirmed the experimental data on a pronounced stimulating effect of the new Bulgarian phytochemical preparation on the sexual functions. It restored and improved the libido in all forms of impotentia coeundi after the administration of a mean daily dose of 1.5 g for 30 - 40 days. This suggests that not only the diminished libido was stimulated, but also that a therapeutic effect on both primary and secondary male hypogonadism was present. The assumption that the product was a favorable effect on spermatozoa motility after 60-day administration corresponds to the experimental data, according to which it stimulates both the mitosis and maturation of the germinal cells.
It is well known that at least 80 days elapse from the time of the division of the spermatogonia till the formation of a mature spermatozoon in males, hence the concentrations of the spermatozoa in the semen are different within that period. The team that used a therapeutic course of 90 days observed very good results in terms of both the motility and the concentration of the spermatozoa in the ejaculate. The studies of ejaculate from patients receiving the product for 60 days proved its apparent effect on the motility of the spermatozoa and an insignificant effect on their concentration on the basis of identical initial spermatozoal levels, as well as the presence of identity in the nozological groups prior to the treatment. This confirms the fact that the minimum therapeutic cycle should last at least as long as one complete germinal cycle (i.e. 80 - 90 days in males). Both idiopathic oligo- and azoospermia are diseases with so far undistinguished etiology. The serum levels of sex steroids are not changed in the majority of the patients with such deviations and good therapeutic levels of the product are observed. No data are available from testes biopsy that can throw light as to which of the phases of this complicated process of spermatogenesis has been affected pathologically and hence favorably affected by the product. Kumanov at al. advanced the hypothesis of diminished central effect of the product, associated with its mechanism of action, based on the elevated level of the lutenizing hormone. On the other hand, they admitted the existence of a peripheral effect, which could be responsible for the effect of the product on hair growth.
The reduced level of serum cholesterol under the effect of the product provided grounds for the same authors to assume that it also had an effect of cholesterol metabolism. The mechanism of action of Tribestan has not been elucidated so far. It can be concluded, on the basis of the clinical studies carried out so far, that it has a very good stimulating and therapeutic effect in all forms of impotentia coeundi, as well as a very good therapeutic effect in patients with oligoasthenospermia. The product has a very good tolerance and no undesired side effects. Based on the date presented so far, we recommend Tribestan for the treatment of impotentia coeundi and generaldi, due to oligospermia and diminished motility of spermatozoa.
2. PHARMACOLOGICAL STUDIES
2.1. Methods characterizing the stimulating effect on spermatogenesis
Spermatogenesis is a complicated process, covering proliferation of the spermatogonia, long-lasting process of the tissue meiosis and numerous changes in the spermatids during their preformation. The effect on the sexual cells can occur during the reproductive period - mitotic division of the spermatogonia or during the maturation of the spermatozoa. The effect on Tribestan on mitosis and maturation of the gonocytes has been studied using quantitative cytological methods. After oral administration of Tribestan in a single daily dose of 70 mg/kg body mass for 20 days, the testes of 8 rats were fixed in neutral formol-calcium and in Serra's solution, and later embedded in paraffin. The testes of 8 untreated animals were used as control. The histological preparations from the testes were stained with hematoxylin (after Mayer) and fast-green (after Yordanov, 1976). Spermatogonia, spermatocytes and spermatids of 40 cross-sections through the seminiferous tubules were counted for each animal from both experimental and control groups (a total of 640), with identical diameter of the tubules (determined by eyepiece micrometer) in phase VII, according to the classification of Leblond and Clermon (1952).
Using light microscopy, the thickening of the layer of the spermatogenesis cells was observed in the cross-sections of the seminiferous tubules and a narrowing of their lumen in the treated animals. That resulted from the increased number of rows of sexual cells (Fig. 1). The number of spermatogonia in the 8 experimental animals (i.e. in 320 sections of the seminiferous tubules) was 58 spermatogonia on the average per seminiferous tubule (between 48 and 63). The number of spermatogonia in one seminiferous tubule in the control animals was 36 (between 36 and 40 spermatogonia per tubule). The mean number of spermatocytes in a seminiferous tubules was identical to that of the spermatogonia. The number of spermatids in phase VII varied from 148 to 180 per seminiferous tubule in the treated animals (mean value 176). Their number in the control animals was between 112 and 125 (mean 119). The preparation significantly increased the number of spermatogonia, spermatocytes and spermatids in the testes of rats, with no other effect on the diameter of the seminiferous tubules.
Figure 1. Stimulating effect of Tribestan on spermatogenesis
2.2. Effect on DNA synthesis in gonocytes
The preparation's effect on DNA synthesis in the sexual cells has been studied by cytohistoradiography. The testes of rats treated with Tribestan (for 7 days) and with 3H-thymidine (every second day), and later with colchicine (3 hours prior to decapitation), were fixed in Serra's solution and embedded in paraffin. The sections were covered with Ilford liquid emulsion and left to stay for 25 days. A higher number of 3H-thymidine-labelled spermatogonia type "A" and "B" was found in the treated rats compared to the control animals (Fig. 2).
The mean number of spermatogonia per section from the seminiferous tubules was 56 in the treated animals, 41 of them labeled with radioisotopes. These numbers were 50 and 18 respectively, in the control animals. The increased number of spermatogonia, with 3H-thymidine included for the treated animals, suggested an intensified DNA synthesis under the effect of Tribestan, as well as an increased number of spermatogonia during the phase V of the cell cycle.
Figure 2. Effect of Tribestan on DNA synthesis. The percentage of 3H-thymidine-labelled spermatogonia versus their total number
2.3. Effect on Leydig and Sertoli cells in the testes
It is well known that Leydig and Sertoli cells participate in the process of spermatogenesis. Quantitative cytological methods were used for the evaluation of the effect of the Tribestan on these cells. The results show that the number of Sertoli cells was increased in the seminiferous tubules of Tribestan-treated animals, compared to the controls (Fig. 3).
The mean number of Sertoli cells in a section of the seminiferous tubule in the treated animals was 29 versus 19.50 in the controls (increase by 40%). The cytological studies of the testes showed no differences in the number of Leydig cells between the experimental and control animals.
Figure 3. Effect of Tribestan on Leydig and Sertoli cells
2.4. Effect on concentration, motility and survival of spermatozoa
The concentration, motility and viability of spermatozoa in the epididymis of rats treated for 30 days with Tribestan were studied immediately after decapitation. Sodium citrate was used as diluent. The mean spermatozoa number per ml was higher by two million in the treated animals, compared to the controls (Fig. 4).
The number of motile spermatozoa under the microscope was 8% higher in the treated animals. Furthermore, their spermatozoa were more viable. The loss of their advancing movements could be observed on the 75th minute, on the average, and in the control animal group - by the 45th minute (Fig. 5).
Figure 4. Effect of Tribestan on the concentration and motility of rat spermatozoa
Figure 5. Effect of Tribestan on the viability of rat spermatozoa
2.5. Effect on the sexual libido
The effect of Tribestan on the sexual behavior was studied on male pigs with confirmed lasting impotence. The preparation was administered orally and its effect on the sexual behavior and sexual reflexes was followed up daily. Individual animal reaction to the preparation was observed. The libido and sexual reflexes were restored in 71% of the animals with complete absence of libido, treated with a daily dose of 70 mg/kg for 10 days. In the animals with poor libido and long reflex period of sexual reflexes, recovery was recorded in 100% of the cases.
2.6. Studies on serum concentration of the hormones from the hypophyseal-gonadal axis
The experiments were carried out on healthy subjects (8 male and 8 female), aged between 28 and 45 years (Milanov et al., 1981). The preparation was administered orally in a dose of one tablet, three times daily at 8-hour intervals for 5 days. The basal hormonal levels were determined before and after the intake of the Tribestan (at 8:00 am and at noon). The concentrations of the luteinizing (LH) and follicle-stimulating (FSH) hormones were determined by kits provided by Biodata (Italy). Serum testosterone was determined by the method of R.H.Williams (1967), serum estradiol - by the method of C.P.Orezyk (1974), using kits provided by the Sorin (Belgium). The results reveal that the drug elevated the level of the luteinizing hormone and testosterone in the orally treated healthy males, not affecting FSH (Fig. 6).
In the females, the concentration of FSH and estradiol were increased under the effect of Tribestan, whereas the testosterone concentration was not significantly changed (Fig. 7). The results show that the preparation has an effect on the hormones from the hypophyseal-gonadal axis, while at the same time not disturbing the hormonal balance in the body, thus enabling its administration as an agent stimulating the reproductive function.
Figure 6
Figure 7. Effect of Tribestan on the concentration of hormones of the hypophyseal-gonadal axis in blood plasma of healthy males
Figure 8. Effect of Tribestan on the plasma concentration of hypophyseal-gonadal axis hormones in healthy women
2.7. Effect on the central nervous system
The screening system for neuro-pharmacological tests (R.Nikolov, 1980) was used in the studies. The following parameters of the treated animals were observed during the first stage of the screening: awareness, mood, motor activity, muscle tone and somatic reflexes.
The second stage of the screening covered the administration of many substances with an effect on the central nervous system, e.g. corazol, strychnine, nicotine, arecoline, phenamine, sodium hexobarbital, reserpine. The drug was applied itraperitoneally to albino mice, H line, with a body mas of 18 - 22 g.
With a dose of 100 mg/kg body mass (1/4 of LD50), the drug had no effect on the behavior of the contact animals in the cage. During observations out of th cage, the animals became more excited, with enhanced reactivity. Their muscle tome was simultaneously reduced. In that dose, the drug inhibited moderately the corazol-induced convulsions, but the other reflexes were suppressed. The maximum tolerance dose - 300 mg/kg body mass - led to reduction of the motor activity, slight disturbance of gait and lower muscle tome of the limbs and stomach.
2.8. Effect on the cardiovascular system
The effect of the drug on the blood pressure values of cats under urethan narcosis was studied by the method of Ludwig Zyon (S.Vankov, 1981). The drug was injected intramuscularly and itraperitoneally as 10% aqueous solution. The intramuscular application of the drug in doses of 50, 100 and 150 mg/kg body mass had no significant effect on the blood pressure of the urethanized cats. A significant hypotensive effect was observed with the intraperitoneal application of the drug in a dose of 150 mg/kg body weight, advancing from the 5th to the 10th minute after application. The values of the arterial pressure decreased by 20% compared to the initial ones. The oral administration of Tribestan in a dose of 150 mg/kg on awake dogs had no effect on the blood pressure. The oral administration in doses of 50, 100 and 150 mg/kg body mass had no effect on the autonomic nervous system of the urethanized cats.
2.9. Pharmacokinetic studies
The experiments were carried out on albino, Wistar rats (180 - 200 g body mass) in 1981 by N.Dikova and V.Ognianova. the unchanged protodioscine in plasma, bile and urine was measured by thin-layer chromatography. Semi-quantitative measures were recorded, standardized by the precisely determined protodioscine concentrations. To determine the concentration of plasma protodioscine, the animals were intravenously injected single doses of 50 and 200 mg/kg body mass. Citrate blood was withdrawn 2, 4, 10, 20, 30, 45, 60, 90, 120 and 180 min after injection. To determine protodioscine excretion in the bile the animals were treated intravenously and orally with single doses of 50 and 200 mg/kg.
The bile was dynamically collected: up to the 6th hour, from the 6th to the 9th hour, from the 9th to the 24th hour after each application. Twenty-four-hour urine was collected. The results show that protodioscine was rapidly eliminated from the plasma and its concentrations were insignificant after the 180th minute. About 12 to 14% protodioscine were excreted in the bile and about 6 - 7 % in the urine within 24 hours after the intravenous administration of the doses of 50 and 200 mg/kg. Protodioscine from 2 to 4% were excreted with the bile after oral administration. No measurable concentration of unchanged protodioscine was found in 24-hour urine after oral administration.
2.10. Toxicological studies (G.Tanev, S.Zarkova, 1980)
2.10.1. Acute toxicity
The acute toxicity of Tribestan was studied after intraperitoneal and oral application to albino mice, H line (18 - 20 mg body mass) and albino rats (160 - 180 g body mass). LD50 was also studied. It was concluded that the product can be included in the group of practically non-toxic substances. LD50 was 1942 mg/kg body mass with intraperitoneal application to mice and over 10,000 mg/kg body mass - with oral administration. The mean lethal dose of Tribestan with intraperitoneal application to rats was 750 (375 +/- 1,500 ) mg body mass, and after oral administration - over 10,000 mg/kg.
2.10.2. Subacute toxicity
The Tribestan was administered orally to albino Wistar rats for 30 and 90 days in the following doses: 75 mg/kg, 150 mg/kg, 225 mg/kg and 300 mg/kg body mass. No increased lethality was observed, nor a change in the behavior of the animals. No significant changes were observed in the routine clinical-laboratory and biochemical indices, nor morphological changes in the internal organs.
2.10.3. Chronic toxicity
Tribestan was administered orally to albino rats for 6 months in doses of 75 mg/kg and 150 mg/kg body mass, as well as in 75 mg/kg body mass for 180 days to Beagle dogs. The following toxic symptoms were looked for: changes in behavior, changes in the hematological, biochemical, functional and morphological parameters. No significant changes were found both in the behavior and in the reflexes of the animals. No increased lethality was observed. No pathological deviations from the physiological values were found in all hematological and clinical-chemical indices studied. No pathological changes in the structure of the internal organs, related to the toxic effect of the preparation, were detected.
Teratological and embryotoxic studies were simultaneously performed, as well as some experiments to follow the pre- and postnatal development (Z.Ilieva, 1980).
No teratogenic and embryotoxic action, nor deleterious effect on the development of the first generation after its littering, were found after the oral administration of the product in a dose of 750 mg/kg body mass to pregnant Wistar rats.
Studies were carried out to exclude the possible carcinogenic potential of Tribestan during a long-term treatment of rats (Gendzhev, 1981).
Increased incidence of neoplasms compared to the control animals was not observed with daily doses of 50 and 150 mg/kg body weight, administered orally for 23 months. No toxic damage was found morphologically in the rat organs.
2.11. Discussion of the results
The experimental data on the biological activity of Tribestan show that its oral administration to rats significantly increased the number of spermatogonia, spermatocytes and spermatids, without any changes in the diameter of the seminiferous tubules. This fact is associated with the confirmed stimulating effect on spermatogenesis as a whole. It is well known that DNA synthesis occurs in the s-phase of the mitotic cycle. A fact of certain interest is that a significant increase of type A and B spermatogonia was found in the rats simultaneously treated with Tribestan and 3H-thymidine during the s-phase.
Hence, it can be concluded that the product intensifies the mitotic activity of spermatogonia. The cytologically detected increased incidence of Sertoli cells, caused by the product, presupposes that the mitosis of these cells has also been stimulated. The important role of Sertoli cells in the regulation of spermatogenesis is well known (Lacy, 1967; Kerr and Klester, 1974, Steinberger, 1971), hence the increased number of Sertoli cells during Tribestan treatment should be associated with the intensification of spermatogenesis. No changes were identified in the Leydig cells of the experimental animals, which suggests that the effect of the product on the spermatogenesis probably does not include these cells. The literature data show that the proliferation of spermatogonia in mammals and birs is FSH-stimulated (Stoinberger et al., 1964; Mancini et al., 1966; Ishiis and Furua, 1975; Krueger et al., 1974). The authors presume that the effect of FSH on spermatogenesis is due to Sertoli cells. The radioimmunological studies on healthy males showed no changes in the FSH-level under Tribestan effect, which suggests presence of a selective effect of the product on gonocytes. On the other hand, elevated LH-levels were found in Tribestan treated healthy males, which suggests the existence of central action.
The pharmacokinetic studies reveal no measurable concentrations of the product in the plasma after oral administration to rats, but spots unidentified so far were detected by the chromatographic methods.
The authors (Dikova and Ognyanova) presume a biotransformation of the product in the body. In such cases, some of the metabolites formed during the biotransformation can be expected to possess a stimulating effect at hypothalamic level.
The effect on the libido of the male pigs is clearly manifested. Tribestan not only stimulates the libido, but also possesses a therapeutic effect as well in the cases of impotence, manifested in complete absence of libido. The effect of the product on the quality of the spermatozoa clearly shows that the spermatozoa of the treated animals are more viable and more resistant, suggesting a better fertility. Many researchers believe that the sexual behavior of the animals and the motility of the spermatozoa depend on testosterone levels. Other authors think that the sexual behavior is modulated by dehydrotestosterone. The problem of the mode of modulation of the sexual behavior remains debatable. If we assume that androgen-like factors are formed through biotransformation in the body, they would not induce changes in the interstitial cells.
Special attention should be paid to the harmlessness of the product. No evidence of acute, subacute and chronic toxicity has been found during the experimental behavioral, hematological, functional, biochemical and morphological studies. No data on carcinogenic and teratogenic effect are available.
The fact that the product has an effect on the hormonal balance in the body, without disordering its regulatory mechanisms, is of equal importance. The combined action of the drug (stimulation of sexual libido and spermatogenesis) and the absence of adverse effects, characterize it as an original agent for the treatment of males with disordered sexual function.
3. CLINICAL STUDIES
3.1. Materials and methods
The experimental data from Tribestan administration have been clinically confirmed so far by three groups of researchers: by the Higher Military Medical Institute under the guidance of Prof. I. Viktorov, Corresponding Member of the Bulgarian Academy of Sciences; by the Medical University of Sofia; State University Hospital of Endocrinology, Gerontology and Geriatry, under the guidance of Prof. E. Bozadzhieva, and by the National Institute of Obstetrics and Gynecology - under the guidance of Prof. M. Protich.
The studies were carried on 212 male individuals, aged between 14 and 60 years. The therapeutic properties of Tribestan were studied in patients with partial or complete impotence. Both the tolerance and the adverse effects of the product were studied. The studies were carried out by the method of simple blind experiment, using placebo. In nozological terms, the studies covered various types of male impotence: idiopathic oligoasthenozoospermia - 39 patients, resection of the left internal testicular vein in varicocele, with subsequent oligoasthenozoospermia - 50 patients; inflammatory process of the prostate with oligo- and azoospermia - 53 patients, primary and secondary male hypogonadism - 20 patients, impotentia coeundi - 50 patients. The product was individually administered to all patients who had not received hormonal agents for at least one month prior to the treatment.
The duration of the treatment depended on acuteness of the disease - 30 - 60 days on the average (Bozadzhieva et al., and Protich et al.) and 90 days (Victorov et al.). the mean daily dose was 3 - 6 filmtablets of 0.250g. Some of the patients were favorably affected by 3 tablets daily (Protich et al.), whereas the other research teams administered 6 tablets (3 x 2). The andrological state was used as the basis for the adequate evaluation of the reproductivity of the patients by all three teams. The basic parameters of sperm were observed, i.e. volume and pH of the ejaculate, concentration of spermatozoa (number/1ml), percentage of motile spermatozoa, mean rate of population motility and percentage of pathological forms of the spermatozoa. Detailed case history on the sexual behavior of the patients was recorded prior to and after the therapeutic Tribestan course. The effect of the product on hair growth was observed in some patients. One of the teams (Bozadzhieva et al.) also observed the changes in the serum levels of gonadotropins, progesterone, testosterone, estradiol and cholesterol. The other team (Victorov et al.) followed up the changes in testosterone serum levels in the Tribestan treated patients. The hormonal levels were radioimmunologically determined using kits and reagents provided by the French-Italian-Belgian Association CEA-IRE-SORIN. The results from these studies were statistically assessed by variation analysis.
3.2. Results
Significant changes in spermatozoon motility were found after Tribestan intake for 60 days (with a daily dose of 3 filmtablets) by males with idiopathic oligoasthenozoospermia. The number of spermatozoa with normal motility, as well as the mean motility rate, were increased.
The percentage of the motile spermatozoa was 29, on the average, prior to the treatment and reached up to 36.66 after the treatment (p < 0.005). The mean motility rate of spermatozoa prior to the treatment was 1.95 mm/sec, after the treatment - 3.63 respectively (p < 0.001). No changes were observed in the ejaculate volume. In both cases (before and after treatment) the ejaculate volume was within the limits of the norm, about 4 ml on the average. The number of spermatozoa in the treated patients was higher by 3 ml/ml ejaculate on the average. In some cases, normalization of the spermogram occurred during repeated treatment with a daily dose of 6 tablets. In these cases, the improvement of the spermogram (normalization of the increased viscosity, increased ejaculate volume, increased concentration and accelerated motility of the spermatozoa) was accompanied be elevation of the serum levels of the lutenizing hormone and testosterone, and reduction of the estradiol level.
The patients with idiopathic azoospermia after 90-day treatment with a daily dose of 1.5g are of particular interest. The results were significant in three of all 7 patients treated. No spermatozoa were detected prior to the treatment. After the treatment, 3.5-million/1ml ejaculate were recorded in one of the patients, 15 million/ml in the second and 28 million/ml in the third. The percentage of motile spermatozoa in the first patient was 10, and in the other two - between 25 and 30. The motility rate of the spermatozoa was about 5 mm/sec. In two of the patients, 30 - 40 spermatozoa per field were observed, and in the third - about 5 spermatozoa per field after the treatment, compared with the absence of any prior to the treatment. One of the patients failed to be affected by the product. The studies on the patients from that nozological group continued with the administration of maintenance dose.
The clinical comparison of the results from the treatment with provirone of patients with idiopathic azoospermia and after Tribestan administration revealed a favorable effect on three of the patients (out of 6), unsuccessfully treated with provirone for a long period of time. The results in the patients with varicocele and oligoasthenozoospermia as regards the motility of the spermatozoa were identical in the reports of all research teams, regardless of the differences in the doses and duration of the treatment. Protich et al. found an average of 26.88% motile spermatozoa prior to the treatment and after 60-day course with a dose of 1 tablet, three times daily - 39% (p < 0.02) with a mean motility rate of spermatozoa 2.06 mm/sec prior to the treatment and 4.44 mm/sec post treatment respectively. No change in the ejaculate volume was found. The other team (Victorov at al.) observed more pronounced changes in the ejaculate volume after 90-day treatment with a daily dose of 1.5 g (4.5 ml compared to 1 - 2 ml prior to the treatment, i.e. an average of 1.55 ml of ejaculate volume in all patients). The number of spermatozoa in 1 ml reached the values in 100% of the patients treated. The mean percentage of motile spermatozoa prior to the treatment was 2.06 and was increased to 33.09 (Tables 1,2,3).
Table 1. Results of Tribestan treatment (1 tablet 3 times daily for 60 days) of 38 males with idiopathic oligoasthenozoospermia (represented in mean values)
Indices Before treatment After treatment
a. Concentration of spermatozoa, million/ml 22.97 26.66
b. Motility, % 29.00 35.66*
c. Motility rate, mm/sec. 1.95 3.76*
Table 2. Results of Tribestan treatment (1 tablet 3 times daily for 60 days) of 16 males after varicocele operation with existing oligoasthenozoospermia
Indices Before treatment After treatment
a. Concentration of spermatozoa, million/ml 21.31 26.75
b. Motility, % 11.53 39.06*
c. Motility rate, mm/sec. 2.00 4.44*
Table 3. Results of Tribestan treatment (2 tablets 3 times daily for 90 days) of 36 males after varicocele operation and existing oligoasthenozoospermia
Indices Before treatment After treatment
a. Concentration of spermatozoa, million/ml 40.60 76.00*
b. Motility, % 3.05 33.09*
c. Motility rate, mm/sec. 2.06 4.44*
*The data are statistically significant.
The results of Tribestan administration to patients with unilateral or bilateral hypothrophy of the testes and azoospermia deserve particular attention. The patients complained of a sense of heaviness and distention, as well as of a slight pain in the testes between 40th and 60th day after the start of the treatment with a daily dose of 6 tablets. Upon examination, a slight pain in the testes occurred upon palpation, as well as a slight swelling, with no other evidence of pathological changes. Improvement both as regards the ejaculate volume and the concentration and motility of the spermatozoa was observed towards the end of the treatment. The testosterone serum level was elevated from 1.75 mg/ml to 3.75 mg/ml. The pain in the testicular region upon palpation abated within 2 - 3 months after treatment. Tribestan administration to patients with chronic inflammatory process of the prostate and disorders in the spermogram led to insignificant changes in these cases when the inflammatory process had been treated previously.
No changes were found in patients with chronic inflammation of the prostate (not treated previously). Out of 14 patients with reduced libido and absence of pathology in the male genital organs, treated for 30-days (daily dose - 2 tablets, three times), 12 manifested obvious improvement of the libido, one patient - a slight improvement (after a 60-day treatment cycle) and no effect was observed in another one. Out of a total of 36 patients with chronic prostatitis and reduced libido, 15 were very favorably affected by the end of the treatment cycle (a total dose of 90 - 100 g), 12 - favorably, and in 9 of the cases with a duration of the inflammatory process over 5 years, no effect occurred. The patients with hypotrophy of the testes and idiopathic azoospermia had no complaints as regards the libido, but in the course of the treatment aimed at improving the spermogram an apparent libido enhancement was recorded. Out of 9 patients treated for one of the gravest forms of male hypogonadism (Klinefelter's syndrome, due to chromosomal anomalies), the libido was enhanced in three of the patients, erection was reported in two and sexual intercourse and masturbation were reported in another two patients. Elevated levels of lutenizing hormone after the treatment were found in these patients. The levels of the remaining sexual hormones and cholesterol were reduced. Two of the patients with secondary insufficiency of sexual glands (Noonan's syndrome) attained improvement of the libido and erections during the treatment. The self-confidence was improved in one of them, and in the second - hair grew in the male genital region.
The results of the treatment of three patients with cryptorchidism (one of them with uncorrected malformation) comprised improvement of the libido and often masturbation. The duration of the erection was prolonged in one patient from that group, aged 37. The spermogram of the same patient was significantly better compared to the initial status one month after treatment, i.e. on day 90 ftehr the beginning. One patient with secondary hypogonadism reported hair growing in the axillary and genital region, parallel with enhanced libido and frequent masturbation.
The serum testosterone levels were elevated in 20 patients from various nozological groups, the initial and final values being within the norm. In seven patients with testosterone serum level below the lower limit of the norm, the physiological levels were reached after the treatment, whereas in the rest of the patients with normal initial levels, the testosterone was not significantly changed after treatment.
3.3. Tolerance and side effects
All clinicians engaged in the studies reported a very good tolerance and no drug-related side effects. The clinical laboratory data on Tribestan treated males showed no deviations in the blood count, ESR, flocculation tests and urine.
3.4. Discussion of the results
The clinical studies of all three research teams on a total of 212 patients (males with disorders in the sexual function) confirmed the experimental data on a pronounced stimulating effect of the new Bulgarian phytochemical preparation on the sexual functions. It restored and improved the libido in all forms of impotentia coeundi after the administration of a mean daily dose of 1.5 g for 30 - 40 days. This suggests that not only the diminished libido was stimulated, but also that a therapeutic effect on both primary and secondary male hypogonadism was present. The assumption that the product was a favorable effect on spermatozoa motility after 60-day administration corresponds to the experimental data, according to which it stimulates both the mitosis and maturation of the germinal cells.
It is well known that at least 80 days elapse from the time of the division of the spermatogonia till the formation of a mature spermatozoon in males, hence the concentrations of the spermatozoa in the semen are different within that period. The team that used a therapeutic course of 90 days observed very good results in terms of both the motility and the concentration of the spermatozoa in the ejaculate. The studies of ejaculate from patients receiving the product for 60 days proved its apparent effect on the motility of the spermatozoa and an insignificant effect on their concentration on the basis of identical initial spermatozoal levels, as well as the presence of identity in the nozological groups prior to the treatment. This confirms the fact that the minimum therapeutic cycle should last at least as long as one complete germinal cycle (i.e. 80 - 90 days in males). Both idiopathic oligo- and azoospermia are diseases with so far undistinguished etiology. The serum levels of sex steroids are not changed in the majority of the patients with such deviations and good therapeutic levels of the product are observed. No data are available from testes biopsy that can throw light as to which of the phases of this complicated process of spermatogenesis has been affected pathologically and hence favorably affected by the product. Kumanov at al. advanced the hypothesis of diminished central effect of the product, associated with its mechanism of action, based on the elevated level of the lutenizing hormone. On the other hand, they admitted the existence of a peripheral effect, which could be responsible for the effect of the product on hair growth.
The reduced level of serum cholesterol under the effect of the product provided grounds for the same authors to assume that it also had an effect of cholesterol metabolism. The mechanism of action of Tribestan has not been elucidated so far. It can be concluded, on the basis of the clinical studies carried out so far, that it has a very good stimulating and therapeutic effect in all forms of impotentia coeundi, as well as a very good therapeutic effect in patients with oligoasthenospermia. The product has a very good tolerance and no undesired side effects. Based on the date presented so far, we recommend Tribestan for the treatment of impotentia coeundi and generaldi, due to oligospermia and diminished motility of spermatozoa.
2. PHARMACOLOGICAL STUDIES
2.1. Methods characterizing the stimulating effect on spermatogenesis
Spermatogenesis is a complicated process, covering proliferation of the spermatogonia, long-lasting process of the tissue meiosis and numerous changes in the spermatids during their preformation. The effect on the sexual cells can occur during the reproductive period - mitotic division of the spermatogonia or during the maturation of the spermatozoa. The effect on Tribestan on mitosis and maturation of the gonocytes has been studied using quantitative cytological methods. After oral administration of Tribestan in a single daily dose of 70 mg/kg body mass for 20 days, the testes of 8 rats were fixed in neutral formol-calcium and in Serra's solution, and later embedded in paraffin. The testes of 8 untreated animals were used as control. The histological preparations from the testes were stained with hematoxylin (after Mayer) and fast-green (after Yordanov, 1976). Spermatogonia, spermatocytes and spermatids of 40 cross-sections through the seminiferous tubules were counted for each animal from both experimental and control groups (a total of 640), with identical diameter of the tubules (determined by eyepiece micrometer) in phase VII, according to the classification of Leblond and Clermon (1952).
Using light microscopy, the thickening of the layer of the spermatogenesis cells was observed in the cross-sections of the seminiferous tubules and a narrowing of their lumen in the treated animals. That resulted from the increased number of rows of sexual cells (Fig. 1). The number of spermatogonia in the 8 experimental animals (i.e. in 320 sections of the seminiferous tubules) was 58 spermatogonia on the average per seminiferous tubule (between 48 and 63). The number of spermatogonia in one seminiferous tubule in the control animals was 36 (between 36 and 40 spermatogonia per tubule). The mean number of spermatocytes in a seminiferous tubules was identical to that of the spermatogonia. The number of spermatids in phase VII varied from 148 to 180 per seminiferous tubule in the treated animals (mean value 176). Their number in the control animals was between 112 and 125 (mean 119). The preparation significantly increased the number of spermatogonia, spermatocytes and spermatids in the testes of rats, with no other effect on the diameter of the seminiferous tubules.
Figure 1. Stimulating effect of Tribestan on spermatogenesis
2.2. Effect on DNA synthesis in gonocytes
The preparation's effect on DNA synthesis in the sexual cells has been studied by cytohistoradiography. The testes of rats treated with Tribestan (for 7 days) and with 3H-thymidine (every second day), and later with colchicine (3 hours prior to decapitation), were fixed in Serra's solution and embedded in paraffin. The sections were covered with Ilford liquid emulsion and left to stay for 25 days. A higher number of 3H-thymidine-labelled spermatogonia type "A" and "B" was found in the treated rats compared to the control animals (Fig. 2).
The mean number of spermatogonia per section from the seminiferous tubules was 56 in the treated animals, 41 of them labeled with radioisotopes. These numbers were 50 and 18 respectively, in the control animals. The increased number of spermatogonia, with 3H-thymidine included for the treated animals, suggested an intensified DNA synthesis under the effect of Tribestan, as well as an increased number of spermatogonia during the phase V of the cell cycle.
Figure 2. Effect of Tribestan on DNA synthesis. The percentage of 3H-thymidine-labelled spermatogonia versus their total number
2.3. Effect on Leydig and Sertoli cells in the testes
It is well known that Leydig and Sertoli cells participate in the process of spermatogenesis. Quantitative cytological methods were used for the evaluation of the effect of the Tribestan on these cells. The results show that the number of Sertoli cells was increased in the seminiferous tubules of Tribestan-treated animals, compared to the controls (Fig. 3).
The mean number of Sertoli cells in a section of the seminiferous tubule in the treated animals was 29 versus 19.50 in the controls (increase by 40%). The cytological studies of the testes showed no differences in the number of Leydig cells between the experimental and control animals.
Figure 3. Effect of Tribestan on Leydig and Sertoli cells
2.4. Effect on concentration, motility and survival of spermatozoa
The concentration, motility and viability of spermatozoa in the epididymis of rats treated for 30 days with Tribestan were studied immediately after decapitation. Sodium citrate was used as diluent. The mean spermatozoa number per ml was higher by two million in the treated animals, compared to the controls (Fig. 4).
The number of motile spermatozoa under the microscope was 8% higher in the treated animals. Furthermore, their spermatozoa were more viable. The loss of their advancing movements could be observed on the 75th minute, on the average, and in the control animal group - by the 45th minute (Fig. 5).
Figure 4. Effect of Tribestan on the concentration and motility of rat spermatozoa
Figure 5. Effect of Tribestan on the viability of rat spermatozoa
2.5. Effect on the sexual libido
The effect of Tribestan on the sexual behavior was studied on male pigs with confirmed lasting impotence. The preparation was administered orally and its effect on the sexual behavior and sexual reflexes was followed up daily. Individual animal reaction to the preparation was observed. The libido and sexual reflexes were restored in 71% of the animals with complete absence of libido, treated with a daily dose of 70 mg/kg for 10 days. In the animals with poor libido and long reflex period of sexual reflexes, recovery was recorded in 100% of the cases.
2.6. Studies on serum concentration of the hormones from the hypophyseal-gonadal axis
The experiments were carried out on healthy subjects (8 male and 8 female), aged between 28 and 45 years (Milanov et al., 1981). The preparation was administered orally in a dose of one tablet, three times daily at 8-hour intervals for 5 days. The basal hormonal levels were determined before and after the intake of the Tribestan (at 8:00 am and at noon). The concentrations of the luteinizing (LH) and follicle-stimulating (FSH) hormones were determined by kits provided by Biodata (Italy). Serum testosterone was determined by the method of R.H.Williams (1967), serum estradiol - by the method of C.P.Orezyk (1974), using kits provided by the Sorin (Belgium). The results reveal that the drug elevated the level of the luteinizing hormone and testosterone in the orally treated healthy males, not affecting FSH (Fig. 6).
In the females, the concentration of FSH and estradiol were increased under the effect of Tribestan, whereas the testosterone concentration was not significantly changed (Fig. 7). The results show that the preparation has an effect on the hormones from the hypophyseal-gonadal axis, while at the same time not disturbing the hormonal balance in the body, thus enabling its administration as an agent stimulating the reproductive function.
Figure 6
Figure 7. Effect of Tribestan on the concentration of hormones of the hypophyseal-gonadal axis in blood plasma of healthy males
Figure 8. Effect of Tribestan on the plasma concentration of hypophyseal-gonadal axis hormones in healthy women
2.7. Effect on the central nervous system
The screening system for neuro-pharmacological tests (R.Nikolov, 1980) was used in the studies. The following parameters of the treated animals were observed during the first stage of the screening: awareness, mood, motor activity, muscle tone and somatic reflexes.
The second stage of the screening covered the administration of many substances with an effect on the central nervous system, e.g. corazol, strychnine, nicotine, arecoline, phenamine, sodium hexobarbital, reserpine. The drug was applied itraperitoneally to albino mice, H line, with a body mas of 18 - 22 g.
With a dose of 100 mg/kg body mass (1/4 of LD50), the drug had no effect on the behavior of the contact animals in the cage. During observations out of th cage, the animals became more excited, with enhanced reactivity. Their muscle tome was simultaneously reduced. In that dose, the drug inhibited moderately the corazol-induced convulsions, but the other reflexes were suppressed. The maximum tolerance dose - 300 mg/kg body mass - led to reduction of the motor activity, slight disturbance of gait and lower muscle tome of the limbs and stomach.
2.8. Effect on the cardiovascular system
The effect of the drug on the blood pressure values of cats under urethan narcosis was studied by the method of Ludwig Zyon (S.Vankov, 1981). The drug was injected intramuscularly and itraperitoneally as 10% aqueous solution. The intramuscular application of the drug in doses of 50, 100 and 150 mg/kg body mass had no significant effect on the blood pressure of the urethanized cats. A significant hypotensive effect was observed with the intraperitoneal application of the drug in a dose of 150 mg/kg body weight, advancing from the 5th to the 10th minute after application. The values of the arterial pressure decreased by 20% compared to the initial ones. The oral administration of Tribestan in a dose of 150 mg/kg on awake dogs had no effect on the blood pressure. The oral administration in doses of 50, 100 and 150 mg/kg body mass had no effect on the autonomic nervous system of the urethanized cats.
2.9. Pharmacokinetic studies
The experiments were carried out on albino, Wistar rats (180 - 200 g body mass) in 1981 by N.Dikova and V.Ognianova. the unchanged protodioscine in plasma, bile and urine was measured by thin-layer chromatography. Semi-quantitative measures were recorded, standardized by the precisely determined protodioscine concentrations. To determine the concentration of plasma protodioscine, the animals were intravenously injected single doses of 50 and 200 mg/kg body mass. Citrate blood was withdrawn 2, 4, 10, 20, 30, 45, 60, 90, 120 and 180 min after injection. To determine protodioscine excretion in the bile the animals were treated intravenously and orally with single doses of 50 and 200 mg/kg.
The bile was dynamically collected: up to the 6th hour, from the 6th to the 9th hour, from the 9th to the 24th hour after each application. Twenty-four-hour urine was collected. The results show that protodioscine was rapidly eliminated from the plasma and its concentrations were insignificant after the 180th minute. About 12 to 14% protodioscine were excreted in the bile and about 6 - 7 % in the urine within 24 hours after the intravenous administration of the doses of 50 and 200 mg/kg. Protodioscine from 2 to 4% were excreted with the bile after oral administration. No measurable concentration of unchanged protodioscine was found in 24-hour urine after oral administration.
2.10. Toxicological studies (G.Tanev, S.Zarkova, 1980)
2.10.1. Acute toxicity
The acute toxicity of Tribestan was studied after intraperitoneal and oral application to albino mice, H line (18 - 20 mg body mass) and albino rats (160 - 180 g body mass). LD50 was also studied. It was concluded that the product can be included in the group of practically non-toxic substances. LD50 was 1942 mg/kg body mass with intraperitoneal application to mice and over 10,000 mg/kg body mass - with oral administration. The mean lethal dose of Tribestan with intraperitoneal application to rats was 750 (375 +/- 1,500 ) mg body mass, and after oral administration - over 10,000 mg/kg.
2.10.2. Subacute toxicity
The Tribestan was administered orally to albino Wistar rats for 30 and 90 days in the following doses: 75 mg/kg, 150 mg/kg, 225 mg/kg and 300 mg/kg body mass. No increased lethality was observed, nor a change in the behavior of the animals. No significant changes were observed in the routine clinical-laboratory and biochemical indices, nor morphological changes in the internal organs.
2.10.3. Chronic toxicity
Tribestan was administered orally to albino rats for 6 months in doses of 75 mg/kg and 150 mg/kg body mass, as well as in 75 mg/kg body mass for 180 days to Beagle dogs. The following toxic symptoms were looked for: changes in behavior, changes in the hematological, biochemical, functional and morphological parameters. No significant changes were found both in the behavior and in the reflexes of the animals. No increased lethality was observed. No pathological deviations from the physiological values were found in all hematological and clinical-chemical indices studied. No pathological changes in the structure of the internal organs, related to the toxic effect of the preparation, were detected.
Teratological and embryotoxic studies were simultaneously performed, as well as some experiments to follow the pre- and postnatal development (Z.Ilieva, 1980).
No teratogenic and embryotoxic action, nor deleterious effect on the development of the first generation after its littering, were found after the oral administration of the product in a dose of 750 mg/kg body mass to pregnant Wistar rats.
Studies were carried out to exclude the possible carcinogenic potential of Tribestan during a long-term treatment of rats (Gendzhev, 1981).
Increased incidence of neoplasms compared to the control animals was not observed with daily doses of 50 and 150 mg/kg body weight, administered orally for 23 months. No toxic damage was found morphologically in the rat organs.
2.11. Discussion of the results
The experimental data on the biological activity of Tribestan show that its oral administration to rats significantly increased the number of spermatogonia, spermatocytes and spermatids, without any changes in the diameter of the seminiferous tubules. This fact is associated with the confirmed stimulating effect on spermatogenesis as a whole. It is well known that DNA synthesis occurs in the s-phase of the mitotic cycle. A fact of certain interest is that a significant increase of type A and B spermatogonia was found in the rats simultaneously treated with Tribestan and 3H-thymidine during the s-phase.
Hence, it can be concluded that the product intensifies the mitotic activity of spermatogonia. The cytologically detected increased incidence of Sertoli cells, caused by the product, presupposes that the mitosis of these cells has also been stimulated. The important role of Sertoli cells in the regulation of spermatogenesis is well known (Lacy, 1967; Kerr and Klester, 1974, Steinberger, 1971), hence the increased number of Sertoli cells during Tribestan treatment should be associated with the intensification of spermatogenesis. No changes were identified in the Leydig cells of the experimental animals, which suggests that the effect of the product on the spermatogenesis probably does not include these cells. The literature data show that the proliferation of spermatogonia in mammals and birs is FSH-stimulated (Stoinberger et al., 1964; Mancini et al., 1966; Ishiis and Furua, 1975; Krueger et al., 1974). The authors presume that the effect of FSH on spermatogenesis is due to Sertoli cells. The radioimmunological studies on healthy males showed no changes in the FSH-level under Tribestan effect, which suggests presence of a selective effect of the product on gonocytes. On the other hand, elevated LH-levels were found in Tribestan treated healthy males, which suggests the existence of central action.
The pharmacokinetic studies reveal no measurable concentrations of the product in the plasma after oral administration to rats, but spots unidentified so far were detected by the chromatographic methods.
The authors (Dikova and Ognyanova) presume a biotransformation of the product in the body. In such cases, some of the metabolites formed during the biotransformation can be expected to possess a stimulating effect at hypothalamic level.
The effect on the libido of the male pigs is clearly manifested. Tribestan not only stimulates the libido, but also possesses a therapeutic effect as well in the cases of impotence, manifested in complete absence of libido. The effect of the product on the quality of the spermatozoa clearly shows that the spermatozoa of the treated animals are more viable and more resistant, suggesting a better fertility. Many researchers believe that the sexual behavior of the animals and the motility of the spermatozoa depend on testosterone levels. Other authors think that the sexual behavior is modulated by dehydrotestosterone. The problem of the mode of modulation of the sexual behavior remains debatable. If we assume that androgen-like factors are formed through biotransformation in the body, they would not induce changes in the interstitial cells.
Special attention should be paid to the harmlessness of the product. No evidence of acute, subacute and chronic toxicity has been found during the experimental behavioral, hematological, functional, biochemical and morphological studies. No data on carcinogenic and teratogenic effect are available.
The fact that the product has an effect on the hormonal balance in the body, without disordering its regulatory mechanisms, is of equal importance. The combined action of the drug (stimulation of sexual libido and spermatogenesis) and the absence of adverse effects, characterize it as an original agent for the treatment of males with disordered sexual function.
R
Ross
Guest
4. CLINICAL STUDIES IN FEMALES WITH ENDOCRINE INFERTILITY OR POSTMENOPAUSAL SYNDROME
A team from the T. Kirkova Obstetric-Gynecological Hospital in Sofia, Bulgaria, headed by P. Tabakova, studied the therapeutic effect of Tribestan on the endocrine function in females. The first clinical experiments were performed on patients with dysovular syndrome and infertility, and later broadened on patients with pre- and perimenopausal syndrome. The females with postcastration menopause were included in a separate group.
Administration schedules:
Group A: Women with dysovular disturbances and infertility
Schedule recommended by the manufacturer: 1 - 2 tablets, 3 times daily for 2 to 3 months.
Authors' schedule: 1 tablet 3 times daily to 2 tablets three times daily from the 5th to the 14th day of menstrual cycle for a period of 2 - 3 months.
After the follow up of certain parameters for assessment of the comprehensive effect of Tribestan individually administered, the group was subjected to combined treatment with Tribestan and a hormonal drug stimulating the ovulation:
Tribestan in compliance with schedule 2 + stimovul (organon) 1 - 2 tablets daily from the 5th to the 14th day of the cycle for total of 3 months.
Tribestan in compliance with schedule 2 + clostilbegite (Hungary) 1 - 2 tablets daily from the 5th to the 9th day of the cycle for a total of 3 months.
Group B: Women with perimenstrual syndrome
Tribestan - 2 tablets, three times daily for 20 days and reduced dose of 1 tablet daily every 4 - 5 days, reaching down to the maintenance dose of 1 tablet, twice daily for a strictly individual period, depending on the effect attained.
Tribestan - 2 tablets, twice daily for 30 days with subsequent reduction of the dose to 1 tablet every 4 - 5 days.
Tribestan - 1 tablet, three times daily, without a break, for a long-term period (up to 1 year).
Clinical patient group.
Group A: Fifty-one women with diagnosed primary and secondary endocrine infertility, treated at the T. Kirkova Obstetric and Gynecological Hospital in Sofia within the 1983 - 1984 period. Fifteen of them were treated in compliance with Schedule 1, the rest - in compliance with Schedule 2. After a three-month observation period, 20 of them underwent the combined treatment in compliance with Schedule 3. Parallel control studies were carried out on a similar group receiving hormonal drugs: stimovul (organon) - 62 women; clostilbegite (Hungary) - 21 women; fertodur (Schering) - 29 women. The total number of the patients included in the study was 163.
Group B: Fifty women with diagnosed natural or postcastration menopausal syndrome, treated within the 1986 - 1987 period. A pilot study on 12 patients was carried out as early as 1984. A treatment was initiated with 2 placebo tablets, three times daily, for a period of 20 - 30 days to 46 out of 50 women (92%), immediately after the final diagnosis and depending on the stage of the clinical picture characterizing the menopause. After the evaluation of the effect of the placebo tablets, the treatment was continued with Tribestan according to the above schedules.
4.1. Parameters observed and evaluated
Clinical patient group A:
The final treatment result is classified in three types:
Normalization of ovulation with a subsequent pregnancy; normalization of ovulation without pregnancy; no effect. The following indices were evaluated: subjective changes in terms of the general conditions and libido; onset and duration of menstruation; basal temperature; changes in the hormonal vaginal cyto-smears; level of pregnadiol, 17-KS and 17-OH-KC in the urine; histological changes in the endometrium. Echographic and folliculometry were performed; radioimmunological control of gonadotrophic and sex steroids; hysterosalpingography and laparoscopy for evaluation of the fallopian tubes and the effect of the product on them.
Clinical patient group B:
The treatment results were classified in conformity with the clinical picture: abatement of menopausal complaints; reduction of these complaints; no effect. The following parameters and symptoms were recorded: neuro-vegetative and neuro-psychic complaints; intensity and frequency of hot flashes, depression and hyperexcitability, apathy, etc.; changes in the cardiovascular system - changes in pulse and extrasystoles, etc.; urinary disorders, pruritus of the outer genitalia, hormonal cyto-smears; blood count and blood sugar profile. Ultrasound diagnostics and radioimmunological control of gonadotrophic and steroid control were performed. The changes in the libido were evaluated.
4.2. Results and discussion
Group A:
Fifteen patients were treated in compliance with Schedule 1. No significant changes in the parameters characterizing the existence of ovulation were recorded in any of them. Furthermore, some undesired side effects were observed, such as longer menstrual cycle, excessive libido, general excitation and insomnia associated with it, and drastic decrease of libido and general weakness in the cases of abrupt withdrawal of the drug at the end of the 3rd month or reduction of the dose by only 50%. This necessitated the use of schedule 2 in the other 36 patients. The data are illustrated further in the paper in figures and tables. The distribution of the patients according to age is presented in Fig. 1. The predominating part of them are in the 20 - 30 age group and only two were over the age of 36. Nineteen of the patients had primary hormonal infertility and 18 - secondary; i.e. both groups covered and almost identical number of patients (Fig. 2). The distribution of the patients as regards their previous treatment is presented in Fig. 3. It is evident that 36% of them have not been treated prior to the study, almost equal is the percentage of the patients with previous hormonal treatment or surgical correction of ovaries - 20 - 30%, and the group of women subjected to combined hormonal-surgical therapy is least. Table 1 presents the lower incidence (33.3%) of the cases with unsatisfactory Tribestan treatment, compared with clostilbegite (52.4%) or fertodur (76%). No doubt, best results were obtained with stimovul, which normalized ovulation with a subsequent pregnancy in 39%; normalized ovulation with no subsequent pregnancy - 35.5% and without effect - in 26%. On the basis of these results, it is clear that Tribestan possesses a considerably more moderate effect: 24 of all 36 treated female patients turned out to be with normal ovulation, but pregnancy was diagnosed in only 2 of them and no effect was recorded in 12 females. Twenty women were simultaneously treated with Tribestan and ovulation stimulant. The effect of the combined treatment was better that that of the individual administration of the drugs. The effect was probably complex: the hormonal stimulation of ovulation was combined with the enhanced libido and improved general and psychosomatic status of the childless couple, especially if our recommendation was followed and the wife also received Tribestan. No adverse effects were reported after intermittent administration of Tribestan.
Table 1. Comparative data on the effect of Tribestan, Stimovul, Clostilbegite and Fertodur on females with endogenous infertility
Groups according
to treatment mode Number
of patents Therapeutic results
Normalized ovulation
with pregnancy Normalized ovulation
without pregnancy No effect Adverse
effects
Treated with
Tribestan 36 2 (5.6%) 22 (61.1%) 12 (33.3%) None
Stimovul 62 24 (38.7%) 22 (35.5%) 16 (25.8%) 4 (6.6%)
Clostilbegite 21 4 (19.0%) 6 (28.6%) 11 (52.4%) 8 (38.1%)
Fertodur 29 2 (6.9%) 5 (17.2%) 22 (75.9%) 3 (10.6%)
Total 148 32 55 61 15
Group B:
The distribution of the female patients into groups according to age is presented in Table 1. Only 4 of them are younger than 40 years and 2 are above 60 years. The main part (80%) of the treated women is aged between 40 and 55. Natural menopause was registered in 26 patients and the other 24 (48%) were with postoperative castration climacterium (Table 2). The duration of menopausal syndrome is presented in Table 3. It can be seen that the menopause occurred one year prior to the start of the Tribestan treatment in most of the female patients, mainly female patients with post-surgical menopause.
EFFECTS OF TRIBESTAN IN MENOPAUSE
Table 1. Distribution of female patients according to age
Age group (years) Number of patients Percentage
30 - 35 1 2%
36 - 39 3 6%
40 - 44 8 16%
45 - 49 19 38%
50 - 54 13 26%
55 - 59 4 8%
60 2 4%
Total 50 100%
Table 2. Distribution of female patients according to the type of their menopause
Type of Menopause Number of patients Percentage
Natural 26 52%
Postoperative 24 48%
Total 50 100%
Table 3. Distribution of female patients according to the duration of menopause
Duration of Menopause (months) Number of patients Percentage
< 12 19 38%
12 - 35 16 32%
36 - 60 7 14%
> 60 8 16%
Total 50 100%
Some of the basic symptoms predominated in the clinical picture of menopause in the group studied, presented in Tables 4 and 5.
Table 4. Distribution of the female patients according to the presence of some symptoms prior to Tribestan treatment
Symptoms Number of patients Percentage
Hot flashes 50 100%
Perspiration 39 78%
Depression 27 54%
Hyperexcitability 22 44%
Insomnia 41 82%
Anxiety 18 36%
Sense of heaviness of the cardiac region 30 60%
RR - changes 11 22%
ECG - changes 8 16%
Table 5. Distribution of the female patients according to the type of sexual libido
Type of sexual libido Number of patients Percentage
Normal 2 4.0
Low 20 40.0
Very low 28 56.0
Total 50 100.0
The neurovegetative symptoms were rather common in the treated women. Hot flashes were recorded in 100% of them, perspiration - in 78%, insomnia - in 82%, groundless hyperexcitation - in 44%. The sense of heaviness in the cardiac region predominated among the cardiovascular changes - 60%, but changes in the arterial pressure and ECG were observed in 16 women (22%). The libido remained unchanged in 2 women (compared to the preceding condition). Strong initial decrease to complete loss of desire for sexual contacts were reported in 56% of all female patients. It should be stressed that the intake of placebo tablets, prior to the treatment, by 46 out of a total of 50 women led to no favorable effect on any of the complaints (Table 6).
Table 6. Distribution of the female patients to the duration of placebo intake
Duration of course (days) Number of patients Percentage
0 4 8%
14 6 12%
15 - 20 32 64%
21 - 30 8 16%
Total 50 100%
Complete or almost complete effect on all or on the majority of the symptoms was observed in 49 out of 50 female patients, according to symptoms selected in the classification (98%). Only in one woman Tribestan had no favorable effect on the menopausal syndrome and she was transferred to another treatment. Table 7 shows that the treatment course required the intake of less that 110 to 180 tablets for attaining a favorable effect in 50% of the treated women. In 10% of the women, that dose was higher - 190 - 220 tablets. The mean effective doses are presented in Table 8, suggesting that the majority of the female patients took over 100 tablets per therapeutic course. The effect obtained is kept by maintenance dose of 2 - 3 tablets daily in 85% of the women (Table 9).
Table 7. Distribution of the female patients according to the total effective dose of Tribestan
Initial dose (tablets/day)
Number of Tablets 3 x 1 2 x 2 3 x 2 Total
No % No % No % No %
< 60 2 4% - - - - 2 4%
60 - 100 5 10% 5 10% 8 16% 18 36%
110 - 180 - - 7 14% 18 36% 25 50%
190 - 220 - - 1 2% 1 2% 2 4%
> 220 - - - - 3 6% 3 6%
Total 7 14% 13 26% 30 60% 50 100%
Table 8. Total Tribestan effective dose
Total Effective Dose
Dose
(tablets/day) Number Mean Confidence limit
(mean ± 1.96 SEM)
3 x 1 7 68.6 53.0 ÷ 84.2
2 x 2 13 115.4 93.7 ÷ 137.1
3 x 2 30 141.5 113.7 ÷ 169.3
Table 9. Distribution of the female patients according to the maintenance dose of Tribestan
Maintenance dose (tablets/day) Number of patients Percentage
2 x 1 27 55.1%
3 x 1 14 28.6%
2 x 2 8 16.3%
Total 49* 100.0%
*1 patient without effect
High level of estrogens was recorded only in 14% during the dynamic cytological follow up of the vaginal cyto-smears, whereas it was low or very low in 44% (Table 10).
Table 10. Distribution of the female patients in conformity with the level of progesterone/estrogen in hormonal cytological study
Level Number of patients Percentage
High 7 14%
Normal 1 2%
Low 6 12%
Very Low 16 32%
Total 30* 100%
*20 patients without cytological examination
The radioimmunological studies are presented in Tables 11 and 12.
Table 11. Radioimmunological studies
Hormone Tribestan administration No Confidence limit
(mean ±1.96SEM)
FSH Prior to
After 46
42 51.38 ÷ 72.34
42.30 ÷ 59.74
LH Prior to
After 42
43 32.45 ÷ 46.05
29.62 ÷ 38.38
Prl Prior to
After 42
37 265.20 ÷ 378.20
200.60 ÷ 267.60
Table 12. Radioimmunological studies
Hormone Tribestan treatment No Confidence limit
(mean ± 1.96 SEM)
E2 Prior to
After 42
40 0.10 ÷ 0.22
0.20 ÷ 0.54
Prg Prior to
After 32
34 5.00 ÷ 10.30
4.14 ÷ 7.44
Tst Prior to
After 41
45 1.15 ÷ 1.74
0.96 ÷ 1.30
The variation analysis reveals that the mean values and the confidence interval are within the norm for adults. The comparison of these data prior to and after treatment shows that the gonadotrophic hormones tend to a reduction compared to the initial values, whereas no such tendency was observed in the ovarial hormones, on the contrary, even an insignificant increase was observed, in E2 in particular. These data could be responsible for the favorable effect on the menopausal complaints, as well as on the considerable enhancement of the libido in 2/3 of the female patients treated. In this case the effect of Tribestan is identical, but in some cases it is better than that of ambosex, a drug containing estrogens and testosterone, at the same time its adverse effects - virilization and tendency to body weight gain - were avoided with Tribestan.
4.3. Side effect in treatment with Tribestan
No faints spells, vomiting, allergic reactions, intolerance, etc. have been observed. The product is well tolerated. It should be pointed out that after the attaining of the desired effect, the abrupt reduction of the effective dose to the maintenance dose leads to a sudden and complete triggering of almost the whole range of symptoms of the menopausal syndrome. This is why, the transition from the effective to the maintenance dose should be very gradual and within a longer time period.
CONCLUSION
Our long-term experience with Tribestan administration in the treatment of mainly female infertility, but also quite often in males, gives us the confidence to recommend it in the cases of disordered formation of gametes, disturbed or absent libido, and other disorders leading to non-ovular menstrual cycle, dyskinetic changes of the fallopian tubes and qualitative changes in male sperm.
The combination of Tribestan with appropriate hormonal drugs leads to the potentiation of its positive effect. The opinion of the research team, based on the experience during the last several years with more than 150 females with natural and postoperative menopause, is that Tribestan can successfully be used for the treatment of menopausal syndrome in women.
A team from the T. Kirkova Obstetric-Gynecological Hospital in Sofia, Bulgaria, headed by P. Tabakova, studied the therapeutic effect of Tribestan on the endocrine function in females. The first clinical experiments were performed on patients with dysovular syndrome and infertility, and later broadened on patients with pre- and perimenopausal syndrome. The females with postcastration menopause were included in a separate group.
Administration schedules:
Group A: Women with dysovular disturbances and infertility
Schedule recommended by the manufacturer: 1 - 2 tablets, 3 times daily for 2 to 3 months.
Authors' schedule: 1 tablet 3 times daily to 2 tablets three times daily from the 5th to the 14th day of menstrual cycle for a period of 2 - 3 months.
After the follow up of certain parameters for assessment of the comprehensive effect of Tribestan individually administered, the group was subjected to combined treatment with Tribestan and a hormonal drug stimulating the ovulation:
Tribestan in compliance with schedule 2 + stimovul (organon) 1 - 2 tablets daily from the 5th to the 14th day of the cycle for total of 3 months.
Tribestan in compliance with schedule 2 + clostilbegite (Hungary) 1 - 2 tablets daily from the 5th to the 9th day of the cycle for a total of 3 months.
Group B: Women with perimenstrual syndrome
Tribestan - 2 tablets, three times daily for 20 days and reduced dose of 1 tablet daily every 4 - 5 days, reaching down to the maintenance dose of 1 tablet, twice daily for a strictly individual period, depending on the effect attained.
Tribestan - 2 tablets, twice daily for 30 days with subsequent reduction of the dose to 1 tablet every 4 - 5 days.
Tribestan - 1 tablet, three times daily, without a break, for a long-term period (up to 1 year).
Clinical patient group.
Group A: Fifty-one women with diagnosed primary and secondary endocrine infertility, treated at the T. Kirkova Obstetric and Gynecological Hospital in Sofia within the 1983 - 1984 period. Fifteen of them were treated in compliance with Schedule 1, the rest - in compliance with Schedule 2. After a three-month observation period, 20 of them underwent the combined treatment in compliance with Schedule 3. Parallel control studies were carried out on a similar group receiving hormonal drugs: stimovul (organon) - 62 women; clostilbegite (Hungary) - 21 women; fertodur (Schering) - 29 women. The total number of the patients included in the study was 163.
Group B: Fifty women with diagnosed natural or postcastration menopausal syndrome, treated within the 1986 - 1987 period. A pilot study on 12 patients was carried out as early as 1984. A treatment was initiated with 2 placebo tablets, three times daily, for a period of 20 - 30 days to 46 out of 50 women (92%), immediately after the final diagnosis and depending on the stage of the clinical picture characterizing the menopause. After the evaluation of the effect of the placebo tablets, the treatment was continued with Tribestan according to the above schedules.
4.1. Parameters observed and evaluated
Clinical patient group A:
The final treatment result is classified in three types:
Normalization of ovulation with a subsequent pregnancy; normalization of ovulation without pregnancy; no effect. The following indices were evaluated: subjective changes in terms of the general conditions and libido; onset and duration of menstruation; basal temperature; changes in the hormonal vaginal cyto-smears; level of pregnadiol, 17-KS and 17-OH-KC in the urine; histological changes in the endometrium. Echographic and folliculometry were performed; radioimmunological control of gonadotrophic and sex steroids; hysterosalpingography and laparoscopy for evaluation of the fallopian tubes and the effect of the product on them.
Clinical patient group B:
The treatment results were classified in conformity with the clinical picture: abatement of menopausal complaints; reduction of these complaints; no effect. The following parameters and symptoms were recorded: neuro-vegetative and neuro-psychic complaints; intensity and frequency of hot flashes, depression and hyperexcitability, apathy, etc.; changes in the cardiovascular system - changes in pulse and extrasystoles, etc.; urinary disorders, pruritus of the outer genitalia, hormonal cyto-smears; blood count and blood sugar profile. Ultrasound diagnostics and radioimmunological control of gonadotrophic and steroid control were performed. The changes in the libido were evaluated.
4.2. Results and discussion
Group A:
Fifteen patients were treated in compliance with Schedule 1. No significant changes in the parameters characterizing the existence of ovulation were recorded in any of them. Furthermore, some undesired side effects were observed, such as longer menstrual cycle, excessive libido, general excitation and insomnia associated with it, and drastic decrease of libido and general weakness in the cases of abrupt withdrawal of the drug at the end of the 3rd month or reduction of the dose by only 50%. This necessitated the use of schedule 2 in the other 36 patients. The data are illustrated further in the paper in figures and tables. The distribution of the patients according to age is presented in Fig. 1. The predominating part of them are in the 20 - 30 age group and only two were over the age of 36. Nineteen of the patients had primary hormonal infertility and 18 - secondary; i.e. both groups covered and almost identical number of patients (Fig. 2). The distribution of the patients as regards their previous treatment is presented in Fig. 3. It is evident that 36% of them have not been treated prior to the study, almost equal is the percentage of the patients with previous hormonal treatment or surgical correction of ovaries - 20 - 30%, and the group of women subjected to combined hormonal-surgical therapy is least. Table 1 presents the lower incidence (33.3%) of the cases with unsatisfactory Tribestan treatment, compared with clostilbegite (52.4%) or fertodur (76%). No doubt, best results were obtained with stimovul, which normalized ovulation with a subsequent pregnancy in 39%; normalized ovulation with no subsequent pregnancy - 35.5% and without effect - in 26%. On the basis of these results, it is clear that Tribestan possesses a considerably more moderate effect: 24 of all 36 treated female patients turned out to be with normal ovulation, but pregnancy was diagnosed in only 2 of them and no effect was recorded in 12 females. Twenty women were simultaneously treated with Tribestan and ovulation stimulant. The effect of the combined treatment was better that that of the individual administration of the drugs. The effect was probably complex: the hormonal stimulation of ovulation was combined with the enhanced libido and improved general and psychosomatic status of the childless couple, especially if our recommendation was followed and the wife also received Tribestan. No adverse effects were reported after intermittent administration of Tribestan.
Table 1. Comparative data on the effect of Tribestan, Stimovul, Clostilbegite and Fertodur on females with endogenous infertility
Groups according
to treatment mode Number
of patents Therapeutic results
Normalized ovulation
with pregnancy Normalized ovulation
without pregnancy No effect Adverse
effects
Treated with
Tribestan 36 2 (5.6%) 22 (61.1%) 12 (33.3%) None
Stimovul 62 24 (38.7%) 22 (35.5%) 16 (25.8%) 4 (6.6%)
Clostilbegite 21 4 (19.0%) 6 (28.6%) 11 (52.4%) 8 (38.1%)
Fertodur 29 2 (6.9%) 5 (17.2%) 22 (75.9%) 3 (10.6%)
Total 148 32 55 61 15
Group B:
The distribution of the female patients into groups according to age is presented in Table 1. Only 4 of them are younger than 40 years and 2 are above 60 years. The main part (80%) of the treated women is aged between 40 and 55. Natural menopause was registered in 26 patients and the other 24 (48%) were with postoperative castration climacterium (Table 2). The duration of menopausal syndrome is presented in Table 3. It can be seen that the menopause occurred one year prior to the start of the Tribestan treatment in most of the female patients, mainly female patients with post-surgical menopause.
EFFECTS OF TRIBESTAN IN MENOPAUSE
Table 1. Distribution of female patients according to age
Age group (years) Number of patients Percentage
30 - 35 1 2%
36 - 39 3 6%
40 - 44 8 16%
45 - 49 19 38%
50 - 54 13 26%
55 - 59 4 8%
60 2 4%
Total 50 100%
Table 2. Distribution of female patients according to the type of their menopause
Type of Menopause Number of patients Percentage
Natural 26 52%
Postoperative 24 48%
Total 50 100%
Table 3. Distribution of female patients according to the duration of menopause
Duration of Menopause (months) Number of patients Percentage
< 12 19 38%
12 - 35 16 32%
36 - 60 7 14%
> 60 8 16%
Total 50 100%
Some of the basic symptoms predominated in the clinical picture of menopause in the group studied, presented in Tables 4 and 5.
Table 4. Distribution of the female patients according to the presence of some symptoms prior to Tribestan treatment
Symptoms Number of patients Percentage
Hot flashes 50 100%
Perspiration 39 78%
Depression 27 54%
Hyperexcitability 22 44%
Insomnia 41 82%
Anxiety 18 36%
Sense of heaviness of the cardiac region 30 60%
RR - changes 11 22%
ECG - changes 8 16%
Table 5. Distribution of the female patients according to the type of sexual libido
Type of sexual libido Number of patients Percentage
Normal 2 4.0
Low 20 40.0
Very low 28 56.0
Total 50 100.0
The neurovegetative symptoms were rather common in the treated women. Hot flashes were recorded in 100% of them, perspiration - in 78%, insomnia - in 82%, groundless hyperexcitation - in 44%. The sense of heaviness in the cardiac region predominated among the cardiovascular changes - 60%, but changes in the arterial pressure and ECG were observed in 16 women (22%). The libido remained unchanged in 2 women (compared to the preceding condition). Strong initial decrease to complete loss of desire for sexual contacts were reported in 56% of all female patients. It should be stressed that the intake of placebo tablets, prior to the treatment, by 46 out of a total of 50 women led to no favorable effect on any of the complaints (Table 6).
Table 6. Distribution of the female patients to the duration of placebo intake
Duration of course (days) Number of patients Percentage
0 4 8%
14 6 12%
15 - 20 32 64%
21 - 30 8 16%
Total 50 100%
Complete or almost complete effect on all or on the majority of the symptoms was observed in 49 out of 50 female patients, according to symptoms selected in the classification (98%). Only in one woman Tribestan had no favorable effect on the menopausal syndrome and she was transferred to another treatment. Table 7 shows that the treatment course required the intake of less that 110 to 180 tablets for attaining a favorable effect in 50% of the treated women. In 10% of the women, that dose was higher - 190 - 220 tablets. The mean effective doses are presented in Table 8, suggesting that the majority of the female patients took over 100 tablets per therapeutic course. The effect obtained is kept by maintenance dose of 2 - 3 tablets daily in 85% of the women (Table 9).
Table 7. Distribution of the female patients according to the total effective dose of Tribestan
Initial dose (tablets/day)
Number of Tablets 3 x 1 2 x 2 3 x 2 Total
No % No % No % No %
< 60 2 4% - - - - 2 4%
60 - 100 5 10% 5 10% 8 16% 18 36%
110 - 180 - - 7 14% 18 36% 25 50%
190 - 220 - - 1 2% 1 2% 2 4%
> 220 - - - - 3 6% 3 6%
Total 7 14% 13 26% 30 60% 50 100%
Table 8. Total Tribestan effective dose
Total Effective Dose
Dose
(tablets/day) Number Mean Confidence limit
(mean ± 1.96 SEM)
3 x 1 7 68.6 53.0 ÷ 84.2
2 x 2 13 115.4 93.7 ÷ 137.1
3 x 2 30 141.5 113.7 ÷ 169.3
Table 9. Distribution of the female patients according to the maintenance dose of Tribestan
Maintenance dose (tablets/day) Number of patients Percentage
2 x 1 27 55.1%
3 x 1 14 28.6%
2 x 2 8 16.3%
Total 49* 100.0%
*1 patient without effect
High level of estrogens was recorded only in 14% during the dynamic cytological follow up of the vaginal cyto-smears, whereas it was low or very low in 44% (Table 10).
Table 10. Distribution of the female patients in conformity with the level of progesterone/estrogen in hormonal cytological study
Level Number of patients Percentage
High 7 14%
Normal 1 2%
Low 6 12%
Very Low 16 32%
Total 30* 100%
*20 patients without cytological examination
The radioimmunological studies are presented in Tables 11 and 12.
Table 11. Radioimmunological studies
Hormone Tribestan administration No Confidence limit
(mean ±1.96SEM)
FSH Prior to
After 46
42 51.38 ÷ 72.34
42.30 ÷ 59.74
LH Prior to
After 42
43 32.45 ÷ 46.05
29.62 ÷ 38.38
Prl Prior to
After 42
37 265.20 ÷ 378.20
200.60 ÷ 267.60
Table 12. Radioimmunological studies
Hormone Tribestan treatment No Confidence limit
(mean ± 1.96 SEM)
E2 Prior to
After 42
40 0.10 ÷ 0.22
0.20 ÷ 0.54
Prg Prior to
After 32
34 5.00 ÷ 10.30
4.14 ÷ 7.44
Tst Prior to
After 41
45 1.15 ÷ 1.74
0.96 ÷ 1.30
The variation analysis reveals that the mean values and the confidence interval are within the norm for adults. The comparison of these data prior to and after treatment shows that the gonadotrophic hormones tend to a reduction compared to the initial values, whereas no such tendency was observed in the ovarial hormones, on the contrary, even an insignificant increase was observed, in E2 in particular. These data could be responsible for the favorable effect on the menopausal complaints, as well as on the considerable enhancement of the libido in 2/3 of the female patients treated. In this case the effect of Tribestan is identical, but in some cases it is better than that of ambosex, a drug containing estrogens and testosterone, at the same time its adverse effects - virilization and tendency to body weight gain - were avoided with Tribestan.
4.3. Side effect in treatment with Tribestan
No faints spells, vomiting, allergic reactions, intolerance, etc. have been observed. The product is well tolerated. It should be pointed out that after the attaining of the desired effect, the abrupt reduction of the effective dose to the maintenance dose leads to a sudden and complete triggering of almost the whole range of symptoms of the menopausal syndrome. This is why, the transition from the effective to the maintenance dose should be very gradual and within a longer time period.
CONCLUSION
Our long-term experience with Tribestan administration in the treatment of mainly female infertility, but also quite often in males, gives us the confidence to recommend it in the cases of disordered formation of gametes, disturbed or absent libido, and other disorders leading to non-ovular menstrual cycle, dyskinetic changes of the fallopian tubes and qualitative changes in male sperm.
The combination of Tribestan with appropriate hormonal drugs leads to the potentiation of its positive effect. The opinion of the research team, based on the experience during the last several years with more than 150 females with natural and postoperative menopause, is that Tribestan can successfully be used for the treatment of menopausal syndrome in women.
R
Ross
Guest
LAST but certainly not LEAST: The reason why MOST Tribulus "supplements" do not work:
COMPARATIVE ANALYTICAL INVESTIGATION OF TRIBULUS TERRESTRIS PREPARATIONS
D.Obreshkova, T.Pangarova, S.Milkov and D.Dinchev
Publication in Pharmacia, vol. XLV, bk. 2/1998, 11.
Sopharma Ltd.
Summary: A comparative investigation in respect to qualitative and quantitative composition of raw materials from Tribulus terrestris L. and a variety of preparations from different origin have been performed. The results obtained concerning furostanol saponins indicate that most of the raw materials are either impurified products derived from Tribulus terrestris or from the powdered plant itself. The content of protodioscin and protogracillin in the preparations except for Bulgarian Tribestan film tablets (Sopharma) are in insignificant amount.
Tribulus terrestris L. Zigophyllaceae has long been quite popular in the folk medicine of the Oriental countries and Bulgaria as a medicinal plant in the treatment of sexual deficiency. Based on that information an original non-hormonal natural product Tribestan has been developed in Chemical Pharmaceutical Research Institute [13, 16, 17, 20] and is in production by Sopharma Joint Stock Co., Bulgaria.
The active components of Tribestan are steroid saponins of furostanol type [3, 12, 14, 15]. The two dominating furostanol bisglycosides have been identified as protodioscin and protogracillin [18] and have been tested biologically as pure substances [24].
As far as Tribestan is non-hormonal phytochemical preparation, the drug has an effect on the hormonal balance in the body [1, 8, 9, 12]. Simultaneously with emphasis upon sexual system, Tribestan has shown a general stimulating action such as motor activity, muscle tone, restorative tonic for vigor, vitality and stamina. For that reason Tribestan is suitable and successfully applied in bodybuilding and in force sports.
Toxicological studies [11], teratogenic [5] and carcinogenic [2] investigations, clinical check ups [7, 10, 23] show that Tribestan has a very good tolerance and no undesired side effects.
It may be remarked that a number of containing Tribulus terrestris are on sale in the U.S.A., with a claim of a high stimulating action. Tribulus terrestris L. is still a plant of high interest nowadays [21].
The purpose of our study is to determine furostanol saponins [4, 5, 6] in a number of raw materials of different origin as a lot of American preparations in comparison with Bulgarian Tribestan substance and filmtablets produced by Sopharma.
Materials and Methods
The analytical method used for quantitative determination of furostanol saponins [4] has been accepted by registration of Tribestan in the United States.
Results and Discussion
The results obtained are shown in Table 1 for raw materials from Tribulus terrestris and in Table 2 for Tribulus terrestris preparations.
It is obvious that most of the raw materials and preparations contain different amount of furostanol saponins, much less than those in the Bulgarian preparation. They vary in dependence on their origin.
Table 1 Source Tribulus terrestris raw materials Principle furostanol saponin Conternt of Furostanol saponins calculated with reference to Protodioscin per cent
Sopharma Tribestan
- Lot No. 01196 Protodioscin, Protogracillin 51.6
- Lot No. 21296 Protodioscin, Protogracillin 52.6
- Lot No 10197 Protodioscin, Protogracillin 53.0
- Lot No 20297 Protodioscin, Protogracillin 57.0
Dabur, India VI-1006 Unknown 0.1
Kaiser Pharmaceuticals Taiwan - Product # 856 Lot # 18204 Protogracillin 0.2
Pharmabul, USA - Lot # 9610819, 3-7-97, 40 mesh Protodioscin, Protogracillin 1.5
Technical Sourcing International Inc. (TSI) lot # SM971016 Saponin 90%, Furostanol 15% Protogracillin 20.0
Hackettstown 07840
- Batch # TTR-9705
-Batch # TTR-9801
Protogracillin
Protogracillin
3.5
4.5
China origin
-No 8745/5/20/98
-No 5424CB/5/20/98
Protogracillin
Unknown
3.2
less than 0.1
Table 2 Source Tribulus terrestris preparations Principle furostanol saponin Conternt of Furostanol saponins calculated with reference to Protodioscin per cent in grams per tablet/capsule
Sopharma Tribestan
- Lot No. 120798 Protodioscin, Protogracillin 0.1050
- Lot No. 70298 Protodioscin, Protogracillin 0.1144
- Lot No 70498 Protodioscin, Protogracillin 0.1189
LifeTime Sports Nutrition's MALE POWER II Protodioscin, Protogracillin 0.0080
Gero Vita International GemiX Protodioscin, Protogracillin 0.0051
Biotest Laboratories TRIBEX 500 Protogracillin 0.0216
SciFi's 19-NOR TRIBUSTENE Protogracillin 0.0083
Prolab's CHRYSIN ANDROSTEN Unknown 0.0003
Optimum Nutrition's ANDRO STACK 850 Protogracillin 0.0040
AST Research's ANDRO PLEX 700 Protodioscin, Protogracillin 0.0047
Muscletech's ANOTESTEN Protodioscin, Protogracillin 0.0159
Twinlab's TRIBULUS FUEL Protogracillin 0.0051
Twinlab's TESTOSTERONE FUEL BOOSTER Protogracillin 0.0030
Klein Laboratories/Sports One ANDRO-XS Protogracillin 0.0047
Universal Laboratories ANDRO STACK Unknown 0.0005
Natural Balance/Per Products ANDRO MAX Protodioscin, Protogracillin 0.0049
Bodyonic's TRIBESTROL PINNACLE Protodioscin, Protogracillin 0.0080
Engineered & Applied Science ANDRO 6 Protodioscin, Protogracillin 0.0091
Pharmabul's TRIBESTAN Protodioscin, Protogracillin 0.0053
Nuntritional Technologies, Inc. TRIBULUS TERRESTRIS Protogracillin 0.0029
ASN's PHYTOBUL Protogracillin 0.0051
Golden's TETRAGEN Protodioscin, Protogracilllin 0.0092
References
1. Dikova, N et V. Ognyanova. Pharmacokinetic studies on Tribestan - Anniversary scientific session '35 Years Chemical Pharmaceutical Research Institute, Sofia, 1983.
2. Gendjev, Z. Studies on Tribestan carcinogenicity. Scientific-Technical Report, 1983.
3. Gyulemetova, R. - Diploma thesis, 1973.
4. Gyulemetova, R., et al. On Tribestan standardization - Pharmazie, 37, 1982, 4.
5. Ilieva, Z. Embriotoxic and teratological studies on Tribestan, Scientific-Technical report, 1981.
6. Kiosava Shu et M. Hatoh - Chem. Pharm. Bull., 16, 1968, No. 6, 1162.
7. Koumanov, F. et al. Clinical trial of Tribestan - Exper. Med. 1982, No. 2.
8. Milanov, S. et al. Tribestan effect on the concentration of some hormones in the serum of healthy subjects.
9. Nicolov, R. Neuropharmacological study on Tribestan. Scientific-Technical Report, 1981.
10. Protich, M. et al. Clinical trial on Tribestan on infertile males. Scientific-Technical report, 1981.
11. Tanev, G. and S. Zarkova: Toxicological studies on Tribestan. Scientific-Technical report, 1981.
12. Tomova, M. et D.Panova - Pharmacia (Sofia), 4, 211.
13. Tomova, M., D. Panova, S. Zarkova et V., Dikov license (II) 11450, 30 1/02 A 61 K/1966.
14. Tomova, M, et al. - Planta medica, 3, 1974, 213.
15. Tomova, M. et al. - Planta medica, 3, 1974, 233.
16. Tomova, M., R. Gyulemetova et S. Zarkova - aut. lic. (11) 27584 a 61 K 35/1978.
17. Tomova, M., et R. Gyulemetova - aut. license (11) 2, 2(51) A 1K 35/1978.
18. Tomova, M. et R. Gyulemetova - Planta Medica, 2, 188.
19. Tomova, M. et al. Steroidal saponins from Tribulus terrestris L., Varna, 1981.
20. Tomova, M. et al. - License 68478/18.01.1985
21. Yan Wang et al. Steroidal saponins from fruits of Tribulus terrestris. - Phytochemistry, 45, 1996, No. 4, 1996.
22. Vankov, S. On Tribestan pharmacology. Scientific-Technical Report, 1980.
23. Viktorov, L et al. Clinical trial of Tribestan - 1 Med., 2, 1982.
24. Zarkova, S. - Dissertation, 1978.
D. Obreshkova
Central Laboratory
Sopharma Ltd.
16 Iliensko Chaussee St.
Sofia, Bulgaria 1220
COMPARATIVE ANALYTICAL INVESTIGATION OF TRIBULUS TERRESTRIS PREPARATIONS
D.Obreshkova, T.Pangarova, S.Milkov and D.Dinchev
Publication in Pharmacia, vol. XLV, bk. 2/1998, 11.
Sopharma Ltd.
Summary: A comparative investigation in respect to qualitative and quantitative composition of raw materials from Tribulus terrestris L. and a variety of preparations from different origin have been performed. The results obtained concerning furostanol saponins indicate that most of the raw materials are either impurified products derived from Tribulus terrestris or from the powdered plant itself. The content of protodioscin and protogracillin in the preparations except for Bulgarian Tribestan film tablets (Sopharma) are in insignificant amount.
Tribulus terrestris L. Zigophyllaceae has long been quite popular in the folk medicine of the Oriental countries and Bulgaria as a medicinal plant in the treatment of sexual deficiency. Based on that information an original non-hormonal natural product Tribestan has been developed in Chemical Pharmaceutical Research Institute [13, 16, 17, 20] and is in production by Sopharma Joint Stock Co., Bulgaria.
The active components of Tribestan are steroid saponins of furostanol type [3, 12, 14, 15]. The two dominating furostanol bisglycosides have been identified as protodioscin and protogracillin [18] and have been tested biologically as pure substances [24].
As far as Tribestan is non-hormonal phytochemical preparation, the drug has an effect on the hormonal balance in the body [1, 8, 9, 12]. Simultaneously with emphasis upon sexual system, Tribestan has shown a general stimulating action such as motor activity, muscle tone, restorative tonic for vigor, vitality and stamina. For that reason Tribestan is suitable and successfully applied in bodybuilding and in force sports.
Toxicological studies [11], teratogenic [5] and carcinogenic [2] investigations, clinical check ups [7, 10, 23] show that Tribestan has a very good tolerance and no undesired side effects.
It may be remarked that a number of containing Tribulus terrestris are on sale in the U.S.A., with a claim of a high stimulating action. Tribulus terrestris L. is still a plant of high interest nowadays [21].
The purpose of our study is to determine furostanol saponins [4, 5, 6] in a number of raw materials of different origin as a lot of American preparations in comparison with Bulgarian Tribestan substance and filmtablets produced by Sopharma.
Materials and Methods
The analytical method used for quantitative determination of furostanol saponins [4] has been accepted by registration of Tribestan in the United States.
Results and Discussion
The results obtained are shown in Table 1 for raw materials from Tribulus terrestris and in Table 2 for Tribulus terrestris preparations.
It is obvious that most of the raw materials and preparations contain different amount of furostanol saponins, much less than those in the Bulgarian preparation. They vary in dependence on their origin.
Table 1 Source Tribulus terrestris raw materials Principle furostanol saponin Conternt of Furostanol saponins calculated with reference to Protodioscin per cent
Sopharma Tribestan
- Lot No. 01196 Protodioscin, Protogracillin 51.6
- Lot No. 21296 Protodioscin, Protogracillin 52.6
- Lot No 10197 Protodioscin, Protogracillin 53.0
- Lot No 20297 Protodioscin, Protogracillin 57.0
Dabur, India VI-1006 Unknown 0.1
Kaiser Pharmaceuticals Taiwan - Product # 856 Lot # 18204 Protogracillin 0.2
Pharmabul, USA - Lot # 9610819, 3-7-97, 40 mesh Protodioscin, Protogracillin 1.5
Technical Sourcing International Inc. (TSI) lot # SM971016 Saponin 90%, Furostanol 15% Protogracillin 20.0
Hackettstown 07840
- Batch # TTR-9705
-Batch # TTR-9801
Protogracillin
Protogracillin
3.5
4.5
China origin
-No 8745/5/20/98
-No 5424CB/5/20/98
Protogracillin
Unknown
3.2
less than 0.1
Table 2 Source Tribulus terrestris preparations Principle furostanol saponin Conternt of Furostanol saponins calculated with reference to Protodioscin per cent in grams per tablet/capsule
Sopharma Tribestan
- Lot No. 120798 Protodioscin, Protogracillin 0.1050
- Lot No. 70298 Protodioscin, Protogracillin 0.1144
- Lot No 70498 Protodioscin, Protogracillin 0.1189
LifeTime Sports Nutrition's MALE POWER II Protodioscin, Protogracillin 0.0080
Gero Vita International GemiX Protodioscin, Protogracillin 0.0051
Biotest Laboratories TRIBEX 500 Protogracillin 0.0216
SciFi's 19-NOR TRIBUSTENE Protogracillin 0.0083
Prolab's CHRYSIN ANDROSTEN Unknown 0.0003
Optimum Nutrition's ANDRO STACK 850 Protogracillin 0.0040
AST Research's ANDRO PLEX 700 Protodioscin, Protogracillin 0.0047
Muscletech's ANOTESTEN Protodioscin, Protogracillin 0.0159
Twinlab's TRIBULUS FUEL Protogracillin 0.0051
Twinlab's TESTOSTERONE FUEL BOOSTER Protogracillin 0.0030
Klein Laboratories/Sports One ANDRO-XS Protogracillin 0.0047
Universal Laboratories ANDRO STACK Unknown 0.0005
Natural Balance/Per Products ANDRO MAX Protodioscin, Protogracillin 0.0049
Bodyonic's TRIBESTROL PINNACLE Protodioscin, Protogracillin 0.0080
Engineered & Applied Science ANDRO 6 Protodioscin, Protogracillin 0.0091
Pharmabul's TRIBESTAN Protodioscin, Protogracillin 0.0053
Nuntritional Technologies, Inc. TRIBULUS TERRESTRIS Protogracillin 0.0029
ASN's PHYTOBUL Protogracillin 0.0051
Golden's TETRAGEN Protodioscin, Protogracilllin 0.0092
References
1. Dikova, N et V. Ognyanova. Pharmacokinetic studies on Tribestan - Anniversary scientific session '35 Years Chemical Pharmaceutical Research Institute, Sofia, 1983.
2. Gendjev, Z. Studies on Tribestan carcinogenicity. Scientific-Technical Report, 1983.
3. Gyulemetova, R. - Diploma thesis, 1973.
4. Gyulemetova, R., et al. On Tribestan standardization - Pharmazie, 37, 1982, 4.
5. Ilieva, Z. Embriotoxic and teratological studies on Tribestan, Scientific-Technical report, 1981.
6. Kiosava Shu et M. Hatoh - Chem. Pharm. Bull., 16, 1968, No. 6, 1162.
7. Koumanov, F. et al. Clinical trial of Tribestan - Exper. Med. 1982, No. 2.
8. Milanov, S. et al. Tribestan effect on the concentration of some hormones in the serum of healthy subjects.
9. Nicolov, R. Neuropharmacological study on Tribestan. Scientific-Technical Report, 1981.
10. Protich, M. et al. Clinical trial on Tribestan on infertile males. Scientific-Technical report, 1981.
11. Tanev, G. and S. Zarkova: Toxicological studies on Tribestan. Scientific-Technical report, 1981.
12. Tomova, M. et D.Panova - Pharmacia (Sofia), 4, 211.
13. Tomova, M., D. Panova, S. Zarkova et V., Dikov license (II) 11450, 30 1/02 A 61 K/1966.
14. Tomova, M, et al. - Planta medica, 3, 1974, 213.
15. Tomova, M. et al. - Planta medica, 3, 1974, 233.
16. Tomova, M., R. Gyulemetova et S. Zarkova - aut. lic. (11) 27584 a 61 K 35/1978.
17. Tomova, M., et R. Gyulemetova - aut. license (11) 2, 2(51) A 1K 35/1978.
18. Tomova, M. et R. Gyulemetova - Planta Medica, 2, 188.
19. Tomova, M. et al. Steroidal saponins from Tribulus terrestris L., Varna, 1981.
20. Tomova, M. et al. - License 68478/18.01.1985
21. Yan Wang et al. Steroidal saponins from fruits of Tribulus terrestris. - Phytochemistry, 45, 1996, No. 4, 1996.
22. Vankov, S. On Tribestan pharmacology. Scientific-Technical Report, 1980.
23. Viktorov, L et al. Clinical trial of Tribestan - 1 Med., 2, 1982.
24. Zarkova, S. - Dissertation, 1978.
D. Obreshkova
Central Laboratory
Sopharma Ltd.
16 Iliensko Chaussee St.
Sofia, Bulgaria 1220
I remember reading all that stuff in the 90's. It would have more credence if the study weren't conducted by Sopharma -- the distributors of Tribistan.
I'd like to believe some of that data and there may even be something to it. But after 15 years of this stuff being around with little response I have to give up on it. Besides, there are much better things around today. Fadogia Agrestis and Avenacodises blow away Trib.
Look, it would be easy enough to make a Trib supplement. No one has a patent on it. But my experience is that it sucked. I've tried all the reincarnations of it. They all sucked. My personal studies using blood test showed it did nothing, whereas avenacosides did quite a bit. That's the proof I need. I have to go with what I believe to be better.
For more on why Trib sucks, go here: http://proteinfactory.com/shop/product.php?productid=109&cat=0&page=1
I'd like to believe some of that data and there may even be something to it. But after 15 years of this stuff being around with little response I have to give up on it. Besides, there are much better things around today. Fadogia Agrestis and Avenacodises blow away Trib.
Look, it would be easy enough to make a Trib supplement. No one has a patent on it. But my experience is that it sucked. I've tried all the reincarnations of it. They all sucked. My personal studies using blood test showed it did nothing, whereas avenacosides did quite a bit. That's the proof I need. I have to go with what I believe to be better.
For more on why Trib sucks, go here: http://proteinfactory.com/shop/product.php?productid=109&cat=0&page=1
R
Ross
Guest
Nelson Montana said:
Can you give me some information on your testosterone-booster? What are the active ingredients? Sounds like it has some good feedback so far.
There have always been moderators on this board that promoted their products (Mr. X, Ulter, Macro). For the most part they used their knowledge for the benefit of the less experienced first and hawked their products when it was appropriate.
I do notice a "harder sell" going on these days although the things that people are accusing Nelson of (making absolute statements and being a dick) I would ascribe more to Primordial Performance. Still the majority or your posts Nelson seem to be aimed at selling something. I could be wrong, it'd just my perception.
I have no doubt that you know more than me about steroids and bodybuilding. But I have been in technical sales for 18 years now and I'll share some of my experience; for what it's worth.
People are more likely to buy from someone they consider a "friend"
You can bully someone into a sale once but forget about ever selling to that individual again (no repeat business).
No one is ever right all the time and new discoveries happen all the time. So absolute statements should be kept to an absolute minimum. They're just traps waiting to come back to haunt you at a later date.
If people like you (and more importantly trust your motives) they'll forgive you when you're wrong and gladly give you second, third, and even fourth chances to get it right.
I do notice a "harder sell" going on these days although the things that people are accusing Nelson of (making absolute statements and being a dick) I would ascribe more to Primordial Performance. Still the majority or your posts Nelson seem to be aimed at selling something. I could be wrong, it'd just my perception.
I have no doubt that you know more than me about steroids and bodybuilding. But I have been in technical sales for 18 years now and I'll share some of my experience; for what it's worth.
People are more likely to buy from someone they consider a "friend"
You can bully someone into a sale once but forget about ever selling to that individual again (no repeat business).
No one is ever right all the time and new discoveries happen all the time. So absolute statements should be kept to an absolute minimum. They're just traps waiting to come back to haunt you at a later date.
If people like you (and more importantly trust your motives) they'll forgive you when you're wrong and gladly give you second, third, and even fourth chances to get it right.
nydj66 said:
No argument. But I can't find a single post where I bully anyone into buying anything. Three quaters of my posts aren't about any product at all. I just don't suffer fools lightly. I will speak out. But never once have I refused to offer help. The problem is, I'm an activist and a contrarian in this field. That means I offer a different persepctive on certain topics. (Ironic that I would be accused of cutting and pasting). And a different perspective isn't always easily accepted.
Sure, I can just sit back an help ala' macro and ulter (both who pushed much harder than me). But they didn't have as much to offer.
S
Sam5
Guest
Boy, I know back when I was natural Tribestan worked wonders for me. Horny all the time, increased my LBM, and ended up getting some sorority girl pregnant. I think it works for me. Anyways, all I can say at this point is Jesus, I can't hang with this. This thread is getting to complicated for me. A good man always knows his limitations.
Sam5 said:
Mmmm...sorority girls.
.
R
Ross
Guest
Nelson Montana said:
Do you ever admit when you're wrong?
V
VooDooChild
Guest
Nelson Montana said:
So you dont agree with this rat story, but the one done with myogenx and albino rats you do agree with? How is one rat study ok and the other is not?
As long as the rat study helps your products sell, you guys are all for it. But as soon as a study discredits your products, you guys say its hogwash, and outdated.. To this date, where is the human or clinical studies done with myogenx?? There is none.. Where is all the positive feedback now? I havnet seen a thread in a longtime..
And if your going to use an herb or unproven supplement to help with PCT, that is just foolish. HCG, Clomid, and nolva have worked well for many, and why would anyone take a chance? This is our health we are talking about..
B
basskiller
Guest
that wasn't a rant about hooker.. He owned hooker..LMAO
Nelson Montana said:
VooDooChild said:
..
- Ross - said:
Do you?
Where are we going with this?
Sure, I've been off base on things now and then, as is everyone in the field. But I've been right a lot more, and often in the face of intense opposition.
off_safety
New member
worldclass said:
this is all that needs to be said about this thread.
off_safety said:
True. If you're an idiot. But I think most of the members are smarter than that.
That guys information is flat out incorrect. But you can agree with it if being ignorant makes you happy.
R
Ross
Guest
Nelson Montana said:Do you?
Where are we going with this?
Sure, I've been off base on things now and then, as is everyone in the field. But I've been right a lot more, and often in the face of intense opposition.
Amen brotha!
If ANYONE understands THAT, it's me.
off_safety
New member
no need to call names, nelson. youve been exposed again and again. you have no credibility.
off_safety said:
I wouldn't call baseless accusations being "exposed." Oh wait, Juice Authority exposed me. He was the guy who argues with me about how off base I was about Clomid, then went on the board crying that it didn't work for him.
And yeah, Fonzie exposed me. You know, the guy who was kicked off for scamming.
Then again there was Ulter, the roid expert who stayed on year round. He's the one who weighs 160 pounds in case you didn't recognize him.
Or maybe it was someone else yo're thinking of. The fat diet guru? The guy who pretended to be a chemist and wound up in jail? The guy who died from DNP? Or is it the what's his name -- Fast400? You know. The bodybuilding expert who admits he never weight trained.
All this "exposure" really hurts my credibility -- if you're a moron.
noclue9415
New member
ive looked at your posts for a looooooooooooong time and i think your a good bro trying to help out. In fact, i think your a genius. I know much of what i do because of reading the posts of people like you. This is my first week posting on this board, so i dont have any credibility, but your cool with me.Nelson Montana said:
A
Anthony Roberts
Guest
- Ross - said:
Do you inject your Glutamine? Because the benefits of this study are not from Oral Glutamine, but rather from using it parenternally (direct to the blood).
As for Tribulus, it's shady as hell for a "study" to be conducted by the company who produces it. Here's an independant study on Tribulus, published in an actual peer-reviewed medical journal:
J Ethnopharmacol. 2005 Oct 3;101(1-3):319-23.
The aphrodisiac herb Tribulus terrestris does not influence the androgen production in young men.
Neychev VK,
Mitev VI.
Department of Chemistry and Biochemistry, Medical University, 2 Zdrave str., Sofia-1431, Bulgaria. [email protected]
OBJECTIVE: The aim of the current study is to investigate the influence of Tribulus terrestris extract on androgen metabolism in young males. DESIGN AND METHODS: Twenty-one healthy young 20-36 years old men with body weight ranging from 60 to 125 kg were randomly separated into three groups-two experimental (each n=7) and a control (placebo) one (n=7). The experimental groups were named TT1 and TT2 and the subjects were assigned to consume 20 and 10 mg/kg body weight per day of Tribulus terrestris extract, respectively, separated into three daily intakes for 4 weeks. Testosterone, androstenedione and luteinizing hormone levels in the serum were measured 24 h before supplementation (clear probe), and at 24, 72, 240, 408 and 576 h from the beginning of the supplementation. RESULTS: There was no significant difference between Tribulus terrestris supplemented groups and controls in the serum testosterone (TT1 (mean+/-S.D.: 15.75+/-1.75 nmol/l); TT2 (mean+/-S.D.: 16.32+/-1.57 nmol/l); controls (mean+/-S.D.: 17.74+/-1.09 nmol/l) (p>0.05)), androstenedione (TT1 (mean+/-S.D.: 1.927+/-0.126 ng/ml); TT2 (mean+/-S.D.: 2.026+/-0.256 ng/ml); controls (mean+/-S.D.: 1.952+/-0.236 ng/ml) (p>0.05)) or luteinizing hormone (TT1 (mean+/-S.D.: 4.662+/-0.274U/l); TT2 (mean+/-S.D.: 4.103+/-0.869U/l); controls (mean+/-S.D.: 4.170+/-0.406U/l) (p>0.05)) levels. All results were within the normal range. The findings in the current study anticipate that Tribulus terrestris steroid saponins possess neither direct nor indirect androgen-increasing properties. The study will be extended in the clarifying the probable mode of action of Tribulus terrestris steroid saponins.
PMID: 15994038 [PubMed - indexed for MEDLINE]
