Bromocriptine

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by Lyle McDonald - Bromocriptine is a dopamine agonist drug (meaning it acts like dopamine in the brain), primarily activating the dopamine D2 receptors. It's main use is for the treatment of high prolactin, Parkinson's disease, and acromegaly; it was also used by bodybuilders in the 80's for it's GH releasing properties. However, it's metabolic effects are far greater than that.

In genetically obese rats, bromocriptine normalizes metabolism and there are many good reasons to think it will do the same in humans. Bromocriptine has use during dieting (to minimize the negative adaptations), muscle gain when very lean, and may be beneficial post-steroid cycle. It may also be useful for diabetes treatment and may have pro-sexual effects.

Bromocriptine has a half-life of roughly 12-14 hours, and dosing is 2.5-5 mg/day taken in the morning.

Bromocriptine is the chemical name of active ingredient in Parlodel. Parlodel is a registered trademark of Sandoz Pharmaceuticals in the United States and/or other countries.

Bromocriptine Resources

Parlodel Prescribing Information
Bromocriptine Pictures

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Pharmaceutical Name: Bromocriptine Mesylate
Drug Classification: Dopamine-Receptor Agonist
Active Life: approximately 20-30 hours



Bromocriptine mesylate is a drug most often medically prescribed for its ability to inhibit growth hormone and prolactin secretion via its action as a dopamine agonist. Used in the treatment of such diseases as acromegaly (1), hyperprolactinemia (2), and Cushing’s syndrome (3) among others, the drug has been adopted by bodybuilders and strength athletes as a means to combat prolactin related side effects caused by certain anabolic steroids. For this purpose bromocriptine mesylate is extremely effective while exhibiting no serious side effects to the health of the user.



Steroid users should be concerned about excessive prolactin levels because of the side effects associated with them. Prolactin is a naturally occurring hormone primarily produced by the lactotrophs located in the pituitary gland, with a minority amount of the hormone being produced by other tissues/cells of the body. Prolactin plays a major role in lactation in most mammals including humans. It both stimulates milk production as well as inducing lobuloalveolar growth of the mammary gland. Obviously both of these side effects would be of great concern to bodybuilders and strength athletes from both a health and cosmetic standpoint. Decreased sex drive, sperm production and sexual function may also be related to elevated levels of this hormone.

The anabolic steroids that can lead to excessive levels of prolactin are primarily nandrolone and nandrolone-derived compounds. Steroids such as deca durabolin, trenbolone, and durabolin all can have this effect. For this reason users of these drugs may want to have a compound such as bromocriptine mesylate in their possession to treat negative side effects related to prolactin if they should develop at any point during a steroid cycle.

Bromocriptine mesylate helps to reduce prolactin levels in humans by mimicking the actions of dopamine, thus it being a dopamine-receptor agonist (2). Dopamine inhibits the secretion and synthesis of prolactin by binding to the receptors in the lactotrophs, thereby negating the possible action of them to secrete prolactin itself. Therefore bromocriptine mesylate can bind to these receptors in the lactotrophs just as dopamine can. This action of course should prevent any abnormal prolactin levels from occurring in steroid users as they relate to any use of nandrolone or nandrolone-derived steroids.

A secondary factor in controlling the levels of prolactin in users of anabolic steroids is the amount of circulating estrogen in their systems. Estrogen has an apparent positive effect on the amount of prolactin produced, with the more estrogen that is produced being related to the amount of prolactin that is produced accordingly. For this reason often times prolactin can be controlled by way of the reduction of estrogen levels. Use of aromatase inhibitors can be used for this purpose. However when prolactin levels reach a point where a reduction of estrogen levels does not inhibit excessive prolactin secretion, administration of bromocriptine mesylate should be sufficient to inhibit any further overproduction.

While dopamine exhibits an ability to inhibit the secretion of prolactin it of course has numerous other functions in the body, with bromocriptine mesylate being able to mimic the action of dopamine and also performing many of these. These include creating a sense of wellbeing or contentment via a chemical reaction in the body, most often released during pleasurable or satisfying physical actions. It has even been shown that dopamine-receptor agonists such as bromocriptine mesylate can help increase the likelihood that individuals that are quitting smoking be successful (4). Dopamine can also help improve brain function. For this reason bromocriptine mesylate is sometimes prescribed to sufferers of Parkinson’s disease. For the average user however it may help in improving memory or even motor functions, although if normal dopamine levels are already being produced by the user this effect will likely be minimal at best. However the primary reason for use of bromocriptine mesylate by steroid users remains for the treatment of prolactin related side effects.


Use/Dosing

Due to the active life of bromocriptine mesylate a user is able to only administer the dosage once per day, ideally taking their dose at approximately the same time every day to maintain levels of the drug within their system at all times.

In terms of dosing the maximum required dosage for user would be 2.5 milligrams per day. This is the largest dosage that is used therapeutically to treat hyperprolactinemia in clinical studies and in regular medical treatment of the condition. However most users that are using the drug to combat prolactin-induced side effects as a result of steroid use should be able to use dosages smaller then this. Doses as low as .5 milligrams per day have been effective enough for many users to quell the negative side effects related to high prolactin levels. However larger doses may be necessary for some up to, and including, 2.5 milligrams per day.

Studies have demonstrated that bromocriptine mesylate is safe for use for extended periods of time, with those that suffer from diseases such as acromegaly and Cushing’s syndrome often administering the drug for years or even decades at a time. However for use by steroid users it should definitely not present any serious or significant health issues when run for relatively short periods of time if needed when using anabolic compounds that could increase prolactin levels in the user.


Risks/Side Effects

The potential side effects associated with the use of bromocriptine mesylate are for the most part related to the discomfort of the user but not the general health of him or her. Frequently reported side effects include insomnia, fatigue, light-headedness, nasal congestion, stomach cramps, constipation, diarrhea, nausea, vomiting, and headaches. Many of these side effects can be avoided by the user by administering their dose of the drug with food. However for some many of these side effects are also a result of using a larger then needed dose. If side effects become unbearable reduction of the dosage being administered may relieve many of the symptoms.

Although for the most part bromocriptine mesylate will not be used or be beneficial for women in a bodybuilding/strength athletics sense, the drug itself has been found not to be harmful to women. In fact, it has been shown that bromocriptine mesylate will not negatively impact fertility in women long term or short term (5). There is even some evidence that use of the drug during pregnancy should not have any negative impacts (6), although this should most definitely be considered a risky undertaking for normally healthy women and should always be used in consultation with a medical doctor.

Toxicity with this compound does not appear to be a concern as there is no evidence that it negatively impacts organs or other tissues in the body (7). Also due to the adverse side effects presented by the drug, namely stomach upset, overdosing on bromocriptine mesylate in a short period of time would be difficult. For these reasons users should not be concerned with toxicity as a result of the normal use of this drug.



References

1. Selvarajah D, Webster J, Ross R, Newell-Price J. Effectiveness of adding dopamine agonist therapy to long-acting somatostatin analogues in the management of acromegaly. Eur J Endocrinol. 2005 Apr;152(4):569-74.

2. Gillam MP, Fideleff H, Boquete HR, Molitch ME. Prolactin excess: treatment and toxicity. Pediatr Endocrinol Rev. 2004 Nov;2 Suppl 1:108-14.

3. Francia G, Davi MV, Montresor E, Colato C, Ferdeghini M, Lo Cascio V. Long-term quiescence of ectopic Cushing's syndrome caused by pulmonary neuroendocrine tumor (typical carcinoid) and tumorlets: Spontaneous remission or therapeutic effect of bromocriptine? J Endocrinol Invest. 2006 Apr;29(4):358-62.

4. Frishman WH, Mitta W, Kupersmith A, Ky T. Nicotine and non-nicotine smoking cessation pharmacotherapies. Cardiol Rev. 2006 Mar-Apr;14(2):57-73.

5. Atmaca A, Dagdelen S, Erbas T. Follow-up of pregnancy in acromegalic women: different presentations and outcomes. Exp Clin Endocrinol Diabetes. 2006 Mar;114(3):135-9.

6. Bronstein MD. Prolactinomas and pregnancy. Pituitary. 2005;8(1):31-8.

7. Gillam MP, Fideleff H, Boquete HR, Molitch ME. Prolactin excess: treatment and toxicity. Pediatr Endocrinol Rev. 2004 Nov;2 Suppl 1:108-14.