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 ofcabergoline (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 physiological 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 calorie-restricted 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.
|Brand name||Parlodel, Bromocriptine mesylate, Bromed, Criten, Grifocriptina, Bromo-Kin, Pavidel, Gynodel, Bromocriptine|
Bromocriptine Mesylate History
Bromocriptine has been used widely in clinical medicine for its indicated used since the 1970s. It 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 therapeutic uses.
How is Bromocriptine Mesylate 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 2.87 mg of bromocriptine mesylate.
Structural Characteristics of Bromocriptine Mesylate
Bromocriptine mesylate is an ergot derivative with the chemical designation (5’S)-2-bromo- 12’-hydroxy-2’-(1- methylethyl)-5’-(2-methylpropyl)-ergotaman-3’,6’,18-trione methanesulphonate.
Bromocriptine Mesylate 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 low a 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.
Bromocriptine Mesylate 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.
Bromocriptine Mesylate 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.
Wlliam Llewellyn (2011) - Anabolics