Parlodel® (bromocriptine mesylate) anti prolactin profile

akn

Musclechemistry Member
Description:
Bromocriptine mesylate is a dopaminomimetic ergot
derivative with D2 dopamine receptor agonist and D1
dopamine receptor antagonist activities. It is used most
commonly as a prolactin inhibitor in cases of
hyperprolactinemia, a growth hormone suppressant in
acromegaly (high doses are required), and as an adjunctive
medication to levodopa in the management of Parkinson's
disease. The structure and activity of this drug are very
similar to that of cabergoline (Dostinex). In the
athletic/bodybuilding communities, bromocriptine is
sometimes used to induce fat loss or combat elevated
prolactin levels subsequent to anabolic/androgenic
steroid use (a rare occurrence, sometimes marked by
lactating gynecomastia).
The most vocal proponent of bromocriptine use for fat loss
is probably Lyle McDonald, author of the online e-Book
Bromocriptine: An Old Drug With New Uses. In this book
McDonald describes how the drug can be used to
normalize the metabolism, such that some of the normal
physiol,ogical responses to dieting (which begin to slow
the loss of body fat as the duration of dieting increases) are
hindered. A lot of this focuses on leptin, a hormone looked
at as sort of a fat thermostat, telling your brain how much
adipose tissue you have on your body and how many
calories you are regularly consuming (an "anti-starvation"
hormone). Dieting tends to lower leptin levels significantly,
which causes your body to respond in an appropriate way
for survival (it tries to hold on to its nutrient stores as much
as possible). Maintaining normal leptin stimulation could
be key to keeping any diet productive, and bromocriptine
may indeed allow us to do that.
The human medical data concerning the potential role this
drug might play in supporting ongoing fat loss is
encouraging. In cases where it was given while dieting,
bromocriptine was capable of increasing total fat loss by a
statistically significant degree, and seemed to extend the
duration in which the diet was most effective. In one case,
both placebo and treatment groups were noticing a
measurable fat loss during the first 6 weeks of calorie
restriction. Only the bromocriptine group, however,
continued to lose significant amounts of weight for the
remaining 12 weeks of intervention. Dieting plateau, or a
point in which continued fat loss drastically slows or stops,
is a common issue among those undertaking a calorierestricted
diet for the purpose of reducing body fat mass. A
drug that can prevent or delay this plateau may logically be
able to increase the overall effectiveness of dieting for
many individuals.
History:
Bromocriptine has been used widely in clinical medicine
for its indicated used since the 1970s.lt is also much more
widely distributed than its counterpart medication
cabergoline, which is used for a similar set of clinical
indications. In the U.S., the most common brand name is
Parlodel, which is sold by Novartis. The drug is available in
dozens of countries, and is sold under a similarly large
number of different trade names including (but not limited
to) Bromed, Criten, Grifocriptina, Bromo-Kin, Pavidel, and
Gynodel. Bromocriptine remains a common medication
today in most developed nations for its intended
thera peutic uses.
How Supplied:
Bromocriptine mesylate is most commonly supplied in
tablets of 2.5 mg and 5 mg. The doses are expressed in
terms of base bromocriptine, so each 2.5 mg tablet
contains 2.87mg of bromocriptine mesylate.
Structural Characteristics:
Bromocriptine mesylate is an ergot derivative with the
chemical designation (5'S)-2-bromo-12'-hydroxy-2'-(1methylethyl)-
S'-(2-methylpropyl)-ergotaman-3~6~18-trione
methanesulphonate.
Side Effects:
Bromocriptine can produce a number of unwanted side
effects, the most notable being low blood pressure,
dizziness, confusion and nausea.These side effects do tend
to be dose related, with the low recommended doses used
in bodybuilding are not likely to be much trouble for many.
Further, initial nausea sometimes goes away after a couple
of applications, once the user becomes accustomed to the
drug. However, the strong incidence of any unwelcome
side effects should warrant discontinuing therapy,
especially if blood pressure is becoming negatively
affected (too Iowa drop). Less common adverse reactions
include anxiety, dry mouth, edema, seizures, fatigue,
headache, lethargy, nasal congestion, rash, elevated liver
enzymes, and changes in urinary frequency.
Administration:
When used medically to treat disorders marked by
hyperprolactinaemia (hyper secretion of prolactin), an
initial dosage of 1.25 mg to 2.5 mg per day is usually
recommended.This may be increased by 2.5 mg every 2-7
days until an acceptable therapeutic dosage is
established. This may require taking as much as 20-30 mg
per day. When used (off-label) to support fat loss, dieting
individuals commonly take between 2.5 mg and 5 mg per
day. This is given in a single morning dose, due to the
relatively long half-life of the drug. This may be used in
short dieting cycles, and should not be considered for
long-term weight management. Similar dosing schedules
are common when used by athletes and bodybuilders to
counter lactating gynecomastia, although higher doses
may be required in some instances. A 4-6 week course of
therapy, combined with a rearrangement of offending
steroids, is usually undertaken.
Availability:
Bromocriptine is produced in most developed countries,
including the United States where it is sold as a generic
drug and under the Parlodel brand name.The brand name
product comes in the form of both 2.5 mg tablets and 5
mg capsules, with 100 doses per bottle. At the pharmacy,
100 5 mg capsules may cost nearly $400. In some nations,
this price may be as low as $50 to 200 ($.50 to $1.00 per
dose) for generic and other brands of bromocriptine.
Bromocriptine is not widely diverted for sale on the black
market, but can be found circulating on occasion.
 
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