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Dostinex and other Meds/AAS
- Thread starter liftr486
- Start date
I'm not a DR. or RX. but I have been on Welbutrin, Zoloft, and Clonopine while using AAS and Cabaser(Dostinex) and didn't have any propblems. I believe that as long as you don't mix SSRI's (Welbutrin etc) with an MAO inhibiter than you should be OK. But if you are worried ask a RX, one of their main jobs is to know and stop a possible drug contradiction.liftr486 said:
liftr486 said:
No contraindications for any of the above. When in doubt Google it.
From Wikipedia, the free encyclopedia
Cabergoline
Systematic (IUPAC) name
N-[3-(Dimethylamino)propyl]-N-[(ethylamino)carbonyl]- 6-(2-propenyl)-8g-ergoline-8-carboxamide
or
1-[(6-allylergolin8β-yl)- carbonyl]-1- [3-(dimethylamino)propyl]-3-ethylurea
Identifiers
CAS number 81409-90-7
ATC code G02CB03 N04BC06
PubChem 54746
DrugBank APRD00836
Chemical data
Formula C26H37N5O2
Mol. mass 451.604 g/mol
Pharmacokinetic data
Bioavailability First-pass effect seen; absolute bioavailability unknown
Protein binding Moderately bound (40% to 42%); concentration- independent
Metabolism Hepatic, predominately via hydrolysis of the acylurea bond or the urea moiety
Half life 63-69 hours (estimated)
Excretion Urine (22%), feces (60%)
Therapeutic considerations
Pregnancy cat. C(US)
Legal status ℞-only(US)
Routes Oral
Cabergoline (brand names Dostinex® and Cabaser®), a lysergic acid amide derivative, is a potent dopamine receptor agonist on D2 receptors.[1] It also acts on dopamine receptors in lactophilic hypothalamus cells to suppress prolactin production in the pituitary gland. It is frequently used as a second-line agent in the management of prolactinomas when bromocriptine is ineffective.
Contents [hide]
1 Pharmacokinetics
2 Carcinogenity
3 Uses
4 Off-label/recreational uses
5 Contraindications and precautions
6 Pregnancy and lactation
7 Side effects
7.1 Valvular heart disease
8 Interactions
9 Dosage
10 References
[edit] Pharmacokinetics
Following a single oral dose, resorption of cabergoline from the gastrointestinal (GI) tract is highly variable, typically occurring within 0.5 to 4 hours. Ingestion with food does not alter its absorption rate. Human bioavailability has not been determined since the drug is intended for oral use only. In mice and rats the absolute bioavailability has been determined to be 30 and 63 percent, respectively. Cabergoline is rapidly and extensively metabolized in the liver and excreted in bile and to a lesser extent in urine. All metabolites are less active than the parental drug or inactive altogether. The human elimination half-life is estimated to be 63 to 68 hours in patients with Parkinson's disease and 79 to 115 hours in patients with pituitary tumors.
[edit] Carcinogenity
In rodents a dose-dependent increase in malignant tumors has been found. The correlation is thought to be species specific. No clinical data exists on carcinogenity in humans.
[edit] Uses
Monotherapy of Parkinson's disease in the early phase.
Combination therapy, together with levodopa and a decarboxylase inhibitor such as carbidopa, in progressive-phase Parkinson's disease.
Adjunctive therapy of prolactin-producing pituitary gland tumors (microprolactinomas).
In some countries also: ablactation and dysfunctions associated with hyperprolactinemia (amenorrhea, oligomenorrhea, anovulation, and galactorrhea).
[edit] Off-label/recreational uses
It has at times been used as an adjunct to SSRI antidepressants as there is some evidence that it counteracts certain side effects of those drugs, such as reduced libido and anorgasmia. It also has been suggested online that it has a possible recreational use in reducing or eliminating the male refractory period. It is also used by bodybuilders to control gynecomastia caused by elevated prolactin levels caused by use of anabolic steroids such as Nandrolone.
[edit] Contraindications and precautions
Hypersensitivity to ergot derivatives
Pediatric patients (no clinical experience)
Severely impaired liver function or cholestasis
Co-medication with drugs metabolized mainly by testosterone cypionate P450 such as erythromycin and ketoconazole, because increased plasma levels of cabergoline may result (although cabergoline undergoes minimal CYP450 metabolism).
Cautions: severe cardiovascular disease, Raynaud's disease, gastroduodenal ulcers, active gastrointestinal bleeding, hypotension.
[edit] Pregnancy and lactation
Pregnancy: Approximately 100 female patients became pregnant under therapy with cabergoline for hyperprolactinemic conditions. The incidence of spontaneous abortions and congenital abnormalities was comparable to nontreated patients. Nevertheless, women wishing to become pregnant should wait a period of four weeks after discontinuation of cabergoline. Patients becoming pregnant under therapy should terminate cabergoline immediately, if possible.
Lactation: In rats cabergoline was found in the maternal milk. Since it is not known if this effect also occurs in humans, breastfeeding women should not be treated.
[edit] Side effects
Approximately 200 patients with newly diagnosed Parkinson's disease participated in a clinical study of cabergoline monotherapy. Seventy-nine (79) percent reported at least one side effect. These side effects were chiefly mild or moderate:
GI tract: Side effects were extremely frequent. Fifty-three percent of patients reported side effects. Very frequent: Nausea (30%), obstipation (22%), and dry mouth (10%). Frequent: Gastric irritation (7%), vomiting (5%), and dyspepsia (2%).
Psychiatric disturbances and central nervous system (central nervous system): Altogether 51 percent of patients were affected. Very frequent: Sleep disturbances (somnolence 18%, insomnia 11%), vertigo (27%), and depression (13%). Frequent: dyskinesia (4%) and hallucinations (4%).
Cardiovascular: Approximately 30 percent of patients experienced side effects. Most frequent were hypotension (10%), peripheral edema (14%) and non-specific edema (2%). Arrhythmias were encountered in 4.8%, palpitations in 4.3%, and angina pectoris in 1.4%.
In a combinatiion study with 2,000 patients also treated with levodopa, the incidence and severity of side effects was comparable to monotherapy. Encountered side effects required a termination of cabergoline treatment in 15% of patients. Additional side effects were infrequent cases of hematological side effects, and an occasional increase in liver enzymes or serum creatinine without signs or symptoms.
As with other ergot derivatives, pleuritis, exudative pleura disease, pleura fibrosis, lung fibrosis, and pericarditis are seen. These side effects are noted in less than 2% of patients. They require immediate termination of treatment. Clinical improvement and normalization of X-ray findings are normally seen soon after cabergoline withdrawal.
The reported incidence and severity of side effects in hyperprolactinemic patients was comparable.
[edit] Valvular heart disease
In two studies published in the New England Journal of Medicine on January 4, 2007, cabergoline was implicated along with pergolide in causing valvular heart disease.[2][3] Both drugs are ergot-derived dopamine agonists, although their molecular skeletons are different. As a result of this, the FDA removed pergolide from the U.S. market on March 29, 2007.[4] Since cabergoline is not approved in the U.S. for Parkinson's Disease, but for hyperprolactinemia, the drug remains on the market. Treatment for hyperprolactinemia requires lower doses than that for Parkinson's Disease, diminishing the risk of valvular heart disease.
[edit] Interactions
No interactions were noted with levodopa or selegiline. The drug should not be combined with other ergot derivatives. Dopamine antagonists such as antipsychotics and metoclopramide inhibit the clinical action of cabergoline and should therefore not be used concomitantly. The use of antihypertensive drugs should be intensively monitored because excessive hypotension may result from the combination.
[edit] Dosage
Parkinson's disease: Monotherapy: Initial dose should be 0.5 mg daily. The usual maintenance dose is 2 to 4 mg daily. Combination therapy: Usually 2 to 6 mg daily.
Tumors of the pituitary gland and other hyperprolactinemic conditions: Initially 0.5 mg per week, slowly titrated to 4.5 mg per week, if necessary.
Ablactation: According to specific treatment scheme.
[edit] References
^ Dostinex at www.rxlist.com. Retrieved on 2007-04-27.
^ Schade, Rene; Andersohn, Frank & Suissa, Samy et al. (2007-01-04), "Dopamine Agonists and the Risk of Cardiac-Valve Regurgitation", New England Journal of Medicine 356 (1): 29-38, <http://content.nejm.org/cgi/content/full/356/1/29>
^ Zanettini, Renzo; Antonini, Angelo & Gatto, Gemma et al. (2007-01-04), "Valvular Heart Disease and the Use of Dopamine Agonists for Parkinson's Disease", New England Journal of Medicine 356 (1): 39-46, <http://content.nejm.org/cgi/content/full/356/1/39>
^ Food and Drug Administration Public Health Advisory (2007-03-29). Retrieved on 2007-04-27.
[show]v • d • eErgolines
Lysergic acid derivatives Bromocriptine, Cabergoline, Ergine,Ergonovine, Ergotamine, Lysergic acid, Lysergol, LSD, D-Lysergic acid hydroxyethylamide, Lisuride, Methergine, Methysergide, Pergolide
Hallucinogenic lysergamides AL-LAD, ALD-52, BU-LAD, CYP-LAD, DAL, DAM-57, Ergonovine, ETH-LAD, LAE-32, LSD, LPD-824, LSM-775, D-Lysergic acid N-(α-hydroxyethyl)amide, Methylergonovine, MLD-41, PARGY-LAD, PRO-LAD
Other ergolines Ergoline
Natural sources Argyreia nervosa, Claviceps spp., Ipomoea tricolor, Ipomoea violacea, Rivea corymbosa
[show]v • d • eAnti-parkinson drugs: dopaminergic agents (N04B)
Dopa and derivatives Levodopa, Melevodopa, Etilevodopa
Adamantane derivatives Amantadine
Dopamine agonists Apomorphine, Bromocriptine, Cabergoline, Dihydrexidine, Dihydroergocryptine mesylate, Fenoldopam, Lisuride, Pergolide, Piribedil, Pramipexole, Quinpirole, Ropinirole, Rotigotine, SKF 38393, SKF 82958
MAOIs Selegiline, Rasagiline
Other Tolcapone, Entacapone, Budipine
Retrieved from "http://en.wikipedia.org/wiki/Cabergoline"
Categories: Lysergamides
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This page was last modified 03:48, 22 December 2007. All text is available under the terms of the GNU Free Documentation License. (See Copyrights for details.)
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galaxy said:
We are talking about if these drugs cause adverse reactions WITH Dostinex.
I think you are pointing out the side effects of these drug on their own.
Where did you find that Cabergoline in conjuction with Klonopin causes sleep problems. KLONOPIN causes sleep problems. We don't want to mix Chantix and Wellbutrin. Please correct me if I am mistaken.
liftr486
New member
everyone responds differently to different drugs. all SSRIs did not work for me but the SNRI has worked for me. Wellbutrin works on the dopamine receptors as I understand it and chantix on the nicotine receptors. it has really done wonders compared to the otc stuff they have.
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