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Take your Nolvadex with GRAPEFRUIT JUICE for better effectivity

BigBazooka

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It's known that Sildenafil Citrate (Viagra's active compound) is metabolized through isoentzyme CYP3A4. Then again, grapefruit juice acts like a weak CYP3A4 inhibitor, which leads to better efficiency with Viagra.

Well one thing I didn't know, was that tamoxifen (the active compound of Nolvadex) is also a drug that metabolizes through CYP3A4. So guess what? That means that the same grapefruit juice trick applies also to Nolvadex. So to sum things up: when you're taking Viagra OR Nolvadex, flush them down with a glass (or two) of grapefruit juice.

Oh, there's tons of stuff in PubMed about this. Here's some links.


http://www.ncbi.nlm.nih.gov/htbin-post/Entrez/query?uid=9153299&form=6&db=m&Dopt=b

http://www.ncbi.nlm.nih.gov:80/entr...ve&db=PubMed&list_uids=10348797&dopt=Abstract
 
ulter said:
It grapefruit trick applies to any oral med. It increases the blood level of winny,if taken orally, by 139%. You should always drink gf juice with your meds.

It only effects oral meds that are broken down through CYP3A4 and P450 activity. 17aas are in this class, but not all oral medications.

Ingestion of three 8oz glasses per day is needed; or ingestion of one double concentrated glass (a glass of grapefruit juice with concentrate mixed in) about an hour before ingestion to get this effect.

In juice, the more bitter, the better as it shows a higher naringin content (one of the items thought responsible for this effect); I'll probably use grapefruit extract from now on to save on carbs and for ease of use.
 
Last edited:
ulter said:
It grapefruit trick applies to any oral med. It increases the blood level of winny,if taken orally, by 139%. You should always drink gf juice with your meds.


Damn! 140 percent!! I figured it would be around 25% or something...
 
THeMaCHinE said:


It only effects oral meds that are broken down througy CYP3A4 and P54 activity. 17aas are in this class, but not all oral medications.

Ingestion of three 8oz glasses per day is needed; or ingestion of one double concentrated glass (a glass of grapefruit juice with concentrate mixed in) about an hour before ingestion to get this effect.

In juice, the more bitter, the better as it shows a higher naringin content (one of the items thought responsible for this effect); I'll probably use grapefruit extract from now on to save on carbs and for ease of use.

Very impressive - you wouldn't happen to have a link to the study. I'd be interested in reading more on it.
 
EAST_COAST_BODYBUILDER how about arrimidex, would it work for that?

Yes, it works for arimidex as well. In some cases with some meds such as Rx anti depression drugs, heart meds, script sleeping pills etc. it may work to well and lead to an overdose. There are numerous documented medical reports of this, most often in the elderly.
 
MadCow1 said:


Very impressive - you wouldn't happen to have a link to the study. I'd be interested in reading more on it.

I have some of it handy in PDF form; actually what I posted is a conglomeration of a number of studies that I looked into -- so I'm not sure exactly what came from where. I'll see if I can dig any of the original links up -- it was some time ago that I looked into this.


Something that I just read about though, is that grapefruit juice can actually block some types of medications as well; here's an excerpt from an article in PSA Rising Magazine:

New Caution Over Blocking Interaction
     In the latest study, published in the April 1999 issue of Pharmaceutical Research, Dr. Andrea Soldner and other scientists at UCSF show that grapefruit juice can actually inhibit the body's absorption of certain drugs including:

* Vinblastine (for combating cancer)
* Cyclosporine (for supressing organ rejection following transplant)
* Losartan (for controlling high blood pressure)
* Digoxin (for treating congestive heart failure)
* Fexofenadine (for alleviating allergy symptoms)

This blocking of drug activity occurs because an unknown substance in grapefruit juice activates a naturally-produced chemical, P-glycoprotein, in the intestinal tract. When grapefruit juice interacts with P-glycoprotein, the result is an increased likelihood that certain drugs will be stopped from entering the bloodstream.
     "These findings help to clarify some major discrepancies we've noticed in the impact of grapefruit juice on various types of medications," said Dr. Leslie Benet, professor of Biopharmaceutical Sciences at UCSF and director of the study. Patients already taking grapefruit juice with their medications can continue to do so, he said. But patients on drugs identified as specifically affected by this blocking effect, " may get a further increase in absorption by taking their drugs a couple of hours after a glass of grapefruit juice."
     According to Dr. Benet, patients who have not previously taken their drugs with grapefruit juice "should be very cautious in doing so, since we now recognize, depending on the drug, that grapefruit juice may either increase or decrease levels of drug in the blood, leading to potential concerns for toxicity or lack of efficacy."
 
Ironically, going back to look for some of the original links I had, I came across this blurb about viagra and gf juice:

Viagra and grapefruit juice -- not a good mix

The original formulation of the protease inhibitor saquinavir -- Invirase -- became available in North America around the mid-1990s. However, Invirase was poorly absorbed. The manufacturer suggested that taking Invirase with concentrated grapefruit juice would enhance the absorption of this drug. This effect occurs because grapefruit juice contains compounds that impair the activity of certain enzymes in the intestine -- enzymes that help break down Invirase.

A few years later, doctors began to use another protease inhibitor, ritonavir (Norvir), in combination with Invirase. Ritonavir is much more effective than grapefruit juice at inhibiting enzymes in the intestine and liver. Examples of other drugs affected by grapefruit juice include the following:


* beta blockers – Cardizem (diltiazem)
* sedatives/sleeping pills – Halcion (triazolam), Versed (midazolam)
* transplant drug – cyclosporine (Neoral, Sandimune)
Now it appears that grapefruit juice can also affect the absorption of the popular erectile dysfunction drug Viagra (Sildenafil). Because erectile dysfunction is common in some males with HIV/AIDS, we report on the interaction between grapefruit juice and Viagra.

Study details
Researchers in Köln, Germany, conducted a study using 24 healthy, HIV negative male subjects whose average age was 29 years. The men received a glass of grapefruit juice on an empty stomach and then one hour later another glass of grapefruit juice with Viagra 50 mg. Blood samples were collected over the next 24 hours. A week later the experiment was repeated with water being substituted for grapefruit juice.

Results
Researchers found that the absorption of Viagra increased by 23% when taken with grapefruit juice instead of water. Grapefruit juice also delayed the absorption of Viagra. This latter point is important because Viagra is supposed to be taken one hour before sex, and taking the drug with grapefruit juice may result in disappointment for some users of Viagra.

The grapefruit juice used in this study was white juice and supplied by Döhler-Euro Citrus NBI, GmbH. Other brands, types and doses of grapefruit juice may have different effects. The researchers suggest that the combination of Viagra and grapefruit juice be "avoided."

Men who use protease inhibitors are usually prescribed less-than-normal doses of Viagra because protease inhibitors can raise levels of Viagra several times greater than normal, which can cause dangerous side effects. Therefore, men who use protease inhibitors and Viagra may wish to also avoid taking Viagra with grapefruit juice.
-- Sean R. Hosein
REFERENCES
1. Jetter A, Kinzig-Schippers M, Walchner-Bonjean M, et al. Effects of grapefruit juice on the pharmacokineticsof sildenafil. Clinical Pharmacology and Therapeutics 2002;71:21-29.

2. Hyland R, Roe EG, Jones BC and Smith DA. Identification of the cytochrome P450 enzymes involved in the N_demethylation of sildenafil. British Journal of Clinical Pharmacology 2001;51(3):239_248.

3. Muirhead GJ, Wulff MB, Fielding A, et al. Pharmacokinetic interactions between sildenafil and saquinavir/ritonavir. British Journal of Clinical Pharmacology 2000;50(2):99_107.
 
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