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Cabergoline - Dostinex
Pharmaceutical Name: Cabergoline
Drug Classification: Dopamine-Receptor Agonist
Active Life: approximately 7 days
Cabergoline is a drug most often medically prescribed for its ability to
inhibit prolactin secretion via its action as a dopamine agonist. Used in the
treatment of such diseases as Parkinson's disease (1), acromegaly (2),
restless leg syndrome (3), Cushing�s syndrome (4), hyperprolactinemia (5),
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 cabergoline is extremely effective while presenting
little risk in terms of serious side effects to the health of the user when
used for this purpose.
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 (6, 7). In fact even in
men with regular healthy levels of prolactin cabergoline can help to
temporarily reduce the amount of the hormone that is secreted which leads to
such advantages as an increase sex drive, improvement in sexual function
(quality of erection) as well as reducing the refractory period for users (the
amount of time between erections) (8).
Cabergoline works to inhibit secretion of prolactin because it is a dopamine
receptor agonist. This means that it acts upon dopamine receptors in the same
way as dopamine does in the body. Dopamine acts as a prolactin inhibitor by
binding to receptors in the lactotrophs in the pituitary gland and signals for
these to cease the synthesis and secretion of prolactin.
While dopamine exhibits an ability to inhibit the secretion of prolactin it of
course has numerous other functions in the body, with cabergoline being able
to mimic the action of dopamine and also performing many of these. These
functions 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 cabergoline can help increase the likelihood that individuals that are
quitting smoking be successful (9). Dopamine can also help improve brain
function. For this reason cabergoline 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 cabergoline by steroid users remains for the
treatment of prolactin related side effects.
The anabolic steroids that can lead to excessive levels of prolactin are
primarily nandrolone and nandrolone-derived compounds. Steroids such as deca
durabolan, trenbolone, and durabolan all can have this effect. For this reason
users of these drugs may want to have a compound such as cabergoline in their
possession to treat negative side effects related to prolactin if they should
develop at any point during a steroid cycle.
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. Essentially estrogen stimulates the secretion of
prolactin via the disruption of the inhibitory effect of dopamine (10). 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 enough, administration
of cabergoline should be sufficient to inhibit any further overproduction.
Use/Dosing of Cabergoline - Dostinex
Due to the extremely long active life of the drug, approximately seven days,
users only have to administer their doses once or twice per week to see good
results. In terms of the dosing that healthy individuals would need to use to
suppress prolactin levels raised by their use of anabolic steroids,
anecdotally many users report seeing their best results with dosing in the
range of one half of a milligram to one and a half milligrams of cabergoline
per week. This dose range should be sufficient for the majority of users but
larger doses can be used as there appears to be little worry for users in
terms of toxicity except at extremely high doses that would be impractical to
administer unintentionally (11, 12).
Cabergoline reaches its peak plasma concentration within two to three hours if
administered orally. The drug is metabolised by the liver with a relatively
large amount of the drug experiencing a first pass effect (13). Users are able
to take the drug with or without food; there is no impact on the absorption
rate or action of the compound in either case. In healthy subjects it has been
determined that the elimination half-life of cabergoline is between
sixty-three and one hundred and nine hours (13). There is no reliable data on
the detection time of the compound.
In terms of the duration of time that users can administer cabergoline, there
is very little research that has been completed on the subject. As will be
discussed in the Risks/Side Effects portion of this profile below there are
some indications that there may be risk factors involved in the long term use
of the drug but no definitive conclusions can be made. However, at least in
terms of the short term finding, it appears that cabergoline is a relatively
safe drug for use by healthy adults for long periods of time.
Risks/Side Effects of using Cabergoline - Dostinex
When compared to the other most popular dopamine-receptor agonist
bromocriptine mesylate, cabergoline is seemingly better tolerated and at least
as efficient, if not more so, at reducing prolactin levels in users (7, 14).
Although bromocriptine mesylate is relatively free of any significant negative
side effects users often complain of serious stomach discomfort and other
additional gastrointestinal problems while taking the drug. Cabergoline has
shown a far smaller propensity to produce this effect. However there are still
those that find the drug causes reactions such as stomach upset, vomiting and
nausea among some users but less frequently then with bromocriptine mesylate.
Due to the fact that cabergoline is a relatively new drug there is little long
term research that is available that gages the long term safety of the
compound. For this reason there are several sporadic reports of fairly serious
ailments that could be attributed to the drug. For example there have been
reports of conditions including such things as hair loss (15), inhibition of
the secretion of adrenal gland hormones (16), and even heart disease (17).
However none of these side effects have been reported in anyway close to being
statistically significant and therefore they are not considered to be a valid
concern for users.
Although for the most part cabergoline 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 cabergoline
will not negatively impact fertility in women long term or short term. There
is even some evidence that use of the drug during pregnancy should not have
any negative impacts (18), 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.
References
1. Nakatsuka A, Nagai M, Yabe H, Nishikawa N, Nomura T,
Moritoyo H, Moritoyo T, Nomoto M. Effect of clarithromycin on the
pharmacokinetics of cabergoline in healthy controls and in patients with
Parkinson's disease. J Pharmacol Sci. 2006 Jan;100(1):59-64.
2. 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.
3. Benes H, Heinrich CR, Ueberall MA, Kohnen R. Long-term safety and efficacy
of cabergoline for the treatment of idiopathic restless legs syndrome: results
from an open-label 6-month clinical trial. Sleep. 2004 Jun 15;27(4):674-82.
4. Pivonello R, Ferone D, Lamberts SW, Colao A. Cabergoline plus lanreotide
for ectopic Cushing's syndrome. N Engl J Med. 2005 Jun 9;352(23):2457-8.
5. Jackson J, Safranek S, Daugird A. Clinical inquiries. What is the
recommended evaluation and treatment for elevated serum prolactin? J Fam Pract.
2005 Oct;54(10):897-8, 901.
6. Nickel M, Moleda D, Loew T, Rother W, Gil FP. Cabergoline treatment in men
with psychogenic erectile dysfunction: a randomized, double-blind,
placebo-controlled study. Int J Impot Res. 2006 May 18; [Epub ahead of print]
7. De Rosa M, Colao A, Di Sarno A, Ferone D, Landi ML, Zarrilli S, Paesano L,
Merola B, Lombardi G. Cabergoline treatment rapidly improves gonadal function
in hyperprolactinemic males: a comparison with bromocriptine. Eur J Endocrinol
1998 Mar;138(3):286-93.
8. Kruger TH, Haake P, Haverkamp J, Kramer M, Exton MS, Saller B, Leygraf N,
Hartmann U, Schedlowski M. Effects of acute prolactin manipulation on sexual
drive and function in males. J Endocrinol. 2003 Dec;179(3):357-65.
9. Frishman WH, Mitta W, Kupersmith A, Ky T. Nicotine and non-nicotine smoking
cessation pharmacotherapies. Cardiol Rev. 2006 Mar-Apr;14(2):57-73.
10. Gillam MP, Middler S, Freed DJ, Molitch ME. The novel use of very high
doses of cabergoline and a combination of testosterone and an aromatase
inhibitor in the treatment of a giant prolactinoma. J Clin Endocrinol Metab.
2002 Oct;87(10):4447-51.
11. Gillam MP, Fideleff H, Boquete HR, Molitch ME. Prolactin excess: treatment
and toxicity. Pediatr Endocrinol Rev. 2004 Nov;2 Suppl 1:108-14.
12. Johansen SS, Karkov J. A fatal overdose of the ergot derivative
cabergoline. Forensic Sci Int. 2004 Nov 10;146(1):47-51.
13. Del Dotto P, Bonuccelli U. Clinical pharmacokinetics of cabergoline. Clin
Pharmacokinet. 2003;42(7):633-45.
14. Bolko P, Jaskula M, Wasko R, Wolun M, Sowinski J. The assessment of
cabergoline efficacy and tolerability in patients with pituitary prolactinoma
type. Pol Arch Med Wewn. 2003 May;109(5):489-95.
15. Miwa H, Kondo T. Hair loss induced by dopamine agonist: case report and
review of the literature. Parkinsonism Relat Disord. 2003 Oct;10(1):51-2.
16. Pivonello R, Ferone D, de Herder WW, de Krijger RR, Waaijers M, Mooij DM,
van Koetsveld PM, Barreca A, De Caro ML, Lombardi G, Colao A, Lamberts SW,
Hofland LJ. Dopamine receptor expression and function in human normal adrenal
gland and adrenal tumors. J Clin Endocrinol Metab. 2004 Sep;89(9):4493-502.
17. Horvath J, Fross RD, Kleiner-Fisman G, Lerch R, Stalder H, Liaudat S,
Raskoff WJ, Flachsbart KD, Rakowski H, Pache JC, Burkhard PR, Lang AE. Severe
multivalvular heart disease: a new complication of the ergot derivative
dopamine agonists. Mov Disord. 2004 Jun;19(6):656-62.
18. Ricci E, Parazzini F, Motta T, Ferrari CI, Colao A, Clavenna A, Rocchi F,
Gangi E, Paracchi S, Gasperi M, Lavezzari M, Nicolosi AE, Ferrero S, Landi ML,
Beck-Peccoz P, Bonati M. Pregnancy outcome after cabergoline treatment in
early weeks of gestation. Reprod Toxicol. 2002 Nov-Dec;16(6):791-3.
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