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akn
05-08-2014, 11:59 AM
15309

Description:
Cabergoline is a selective dopamine receptor agonist. This
agent is highly specific in its actions, with a strong affinity
for the dopamine D2 receptor, and a low affinity for
dopamine D1, A1-adrenergic, A2-adrenergic, 5-HT1serotonin,
and 5-HT2-serotonin receptors. Its main clinical
use is for the treatment of hyperprolactinemia, or the
hypersecretion of prolactin from lactotropes in the anterior
pituitary (pituitary tumor is a common cause of this
disorder). It is also applied in the management of
Parkinson's disease. Cabergoline effectively inhibits
prolactin secretion, which it does by mimicking the actions
of dopamine on the D2 receptor (dopamine normally
serves as negative feedback for prolactin release). As a
targeted agonist of the dopamine D2 receptor, cabergoline
should not affect other pituitary hormones like growth
hormone (GH), luteinizing hormone (LH), corticotrophin
(ACTH), or thyroid stimulating hormone (TSH).
Prolactin is a somatotropic hormone, in the same family as
human growth hormone (somatropin).lt is a single peptide
hormone, containing a chain of 199 amino acids. This
makes it similar to (though slightly larger than) growth
hormone, which is made of 192 amino acids. Any similarity
between these two hormones, however, ends at structure.
Prolactin is not an anabolic agent (at least not to skeletal
muscle) but a lactation hormone. Most of its physiological
value is in women, and becomes apparent during
pregnancy when it aids in milk production. Cabergoline,
likewise, is sometimes used to suppress lactation
postpartum if there is a particular medical need for it. In
men, prolactin has no known therapeutic value, and high
levels are associated with impotence, infertility, and
sometimes even gynecomastia (whether or not it has a
causative role here remains the subject of much debate).
Although this is almost never associated with males, high
levels of prolactin have actually been related to lactating
gynecomastia in a very small percentage of steroid-using
athletes. This disorder is often characterized by small fluid
discharge that becomes noticeable with the squeezing of
one's gynecomastic nipple. Although the situation can
become worse, the first sign of this is often enough to scare
the individual away from their current regimen of steroids.
Gynecomastia is not automatically (or even normally)
associated with lactation, so this is a somewhat rare
phenomenon. It is probably caused by an unusual
imbalance of hormones (androgens, estrogens, and
progestins can all be involved and play varying roles),
and/or a particular personal sensitivity to the disorder.
When it does occur, however, cabergoline has been looked at as a remedy for the potentially embarrassing situation.
High prolactin levels (as would be associated with the need
for cabergoline) are not regularly documented in steroidusing
athletes, further underscoring the relative
uncommon nature of this disorder. We do know that
estrogen plays a stimulatory role here, and likely is the key
to increasing prolactin secretion in males.838 839 840 Other
studies, however, show suppressive actions toward
prolactin from other hormones including androgens.841
This is perhaps why an actual hormonal imbalance, and not
necessarily high estrogen, may be the cause of lactating
gynecomastia. Scanning the medical books, there are few
studies even looking at prolactin levels and steroid use,
and those few are relatively inconclusive. One study
analyzed the effects of testosterone enanthate and
propionate in men and noted a significant prolactin
increase 4 days after injection.842 Yet another noted a 7fold
increase in estrogen (to values typical for women) in 5
power athletes self-administering testosterone and other
steroids, yet no consistent effect on prolactin secretion.843
A third self-administration study with athletes,844 and a
fourth clinical with nandrolone,845 failed to show an
increase in prolactin levels.
History:
Cabergoline was developed during the 1980s. The most
popular trade name for this agent is Dostinex, which is
produced in the u.S. and many other countries by the giant
pharmaceutical conglomerate Pharmacia. Dostinex
retained market exclusivity on cabergoline in the U;S. for
many years, but between 2005 and 2007 several generic
versions were approved for sale by the FDA. This includes
products from Barr, Ivax, and Par Pharm. Cabergoline is
widely available internationally, and can be found in more
than 3-dozen different countries. Outside the u.S. the
Dostinex trade name still dominates most markets, and can
be found in Argentina, Australia, Austria, Belgium, Brazil,
Canada, Chile, Czech Republic, Denmark, Finland, France,
Germany, Greece, Hong Kong, Ireland, Israel, Italy, Malaysia,
Mexico, Netherlands, Norway, New Zealand, Poland Portugal, Russia, South Africa, Singapore, Spain, Sweden,
Switzerland, Turkey, United Kingdom, and Venezuela. In
addition to Dostinex, cabergoline is marketed under at
least 1-dozen other trade names.
How Supplied:
Cabergoline is most commonly supplied in tablets of
500mcg.
Structural Characteristics:
Cabergoline is an ergot derivative with the chemical
designation 1-[(6-allylergolin-8beta-yl)carbonyl]-1-[3(
dimethylamino)propyl]-3-ethylurea.
Side Effects:
The most common side effects reported with cabergoline
use include headache, nausea, and vomiting, which
occurred in 26, 27, and 20/0 of patients (respectively)
receiving the medication during one clinical trial.846 Other
potential side effects include (but are not limited to)
constipation, dry mouth, abdominal pain, diarrhea,
dizziness, vertigo, fatigue, anxiety, anorexia, malaise,
depression, insomnia, hot flashes, heart palpitations,
hypotension, breast pain, and acne, however nausea and
headache were the most prominent side effects. Many
side effects are dose related, further reason for starting off
with the lowest possible therapeutic dose and working
up. The prescribing information does not mention death
as a clear consequence of an overdose, but it does list
hallucinations, low blood pressure, and nasal congestion.
Note that overdose patients may need supportive
measures to raise blood pressure.
Administration:
When used medically to inhibit prolactin secretion,
cdbergoline is given in an initial dosage of 500mcg per
week.This may be taken in one single dose or divided into
2 or more doses on separate days. The dose may be
increased by 500mcg per week at monthly intervals until
a desired physiological response is achieved. Dosage is
most commonly maintained at 1mg per week, although
doses up to 4.5 mg may be used in some cases.When used
by athletes/bodybuilders to inhibit prolactin secretion (as
with lactating gynecomastia), doses on the lower end of
the therapeutic range are most commonly used. The user
typically starts with a dosage of 250mcg per application (a
half tablet) twice per week. This is used for four weeks, at
which point the dosage might be adjusted upwards to a
full tablet if needed (1 mg per week). In clinical medicine
this drug may be taken for 6 months or longer, although
athletes/bodybuilders usually find a 4-6 week course of
therapy (combined with an intelligent rearrangement of
the offending drugs) most appropriate.
Availability:
Cabergoline is not widely used by bodybuilders and
athletes, and consequently is not commonly traded in
black market commerce. The drug itself is widely available
in legitimate medical commerce.

Masher59
05-08-2014, 12:29 PM
Good write up. It makes me horny!

Presser
11-18-2015, 04:56 PM
bump

Presser
02-07-2024, 03:01 PM
https://i0.wp.com/www.musclechemistry.com/wp-content/uploads/2024/02/dostinex-caborgoline.webp?resize=220%2C150&ssl=1 (https://www.musclechemistry.com/dostinex-caborgoline-to-combat-trenbolone-and-nandrolone-side-effects/)
5 hours ago
DOSTINEX (caborgoline) to combat Trenbolone and Nandrolone Side Effects (https://www.musclechemistry.com/dostinex-caborgoline-to-combat-trenbolone-and-nandrolone-side-effects/)DOSTINEX5 hours ago
DOSTINEX (caborgoline) to combat Trenbolone and Nandrolone Side Effects.



(https://www.musclechemistry.com/dostinex-caborgoline-to-combat-trenbolone-and-nandrolone-side-effects/)