Bromocriptine Profile
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 of bromocriptine
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 of bromocriptine
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.
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