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Dostinex (Cabergoline)

Dostinex is the pharmacy trade name for the drug cabergoline, 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, 5-HT1-serotonin, 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). Carbergoline 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). It 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. 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 noticed 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, 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 offered a very effective remedy for the sometimes embrassing situation.

High prolactin levels (as would be associated with the need for Dostinex) are commonly not documented in steroid-using 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. Other studies, however, show suppressive actions toward prolactin from other hormones including androgens. This is perhaps why an actual hormonal imbalance, and not necessarily high estrogen, would be the cause of lactating gynecomastia. Scanning the medical books, we find few studies even looking at prolactin levels and steroid use, and those few are relatively inconclusive. One looking at the effects of testosterone enanthate and propionate in men noted significant prolactin increase 4 days after injection. Yet another noted a 7-fold 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. A third self-administration study with athletes, and a fourth clinical with nandrolone, failed to show an increase in prolactin levels.

Although foreseeing the need for an anti-prolactin is difficult, the use of Dostinex itself is relatively simply should one become apparent. The typical protocol involves not taking the drug daily, but administering it only twice per week. The user starts with a dosage of .25mg per application, or a 1/2 tablet. This is used for four weeks, at which point the dosage might be adjusted upwards to a full tablet if needed. In clinical medicine this dosage may be further increased to 1mg (2 tablets) in some cases, however the high cost of the drug (and relative low levels of prolactin compared to those produced with some tumor disorders) usually precludes such use in bodybuilders. The drug itself is usually taken for 6 months or longer in a medical setting, although athletes usually find a 4 – 6 week course of therapy (combined with an intelligent rearrangement of the offending drugs) most appropriate.

Since effects are relatively infrequent with Dostinex use, and most reported events are mild or moderate in nature. The most common complaints were headache, nausea, an vomiting, which occurred in 26%, 27%, and 2% of patients (respectively) receiving the medication during one clinical trial. 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 their prominences tended to be much lower than those of nausea and headache. Many 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. It is also noted that overdose patients may need supportive measures to raise blood pressure.

Overall, Dostinex can be considered a relatively safe drug, with a side effect profile that is not much different than many drugs on the market. There are some risks with its use, but these do not appear to be very high, and in most cases are far outweighed by the potential benefits to the patient. Dostinex is a drug with limited use in bodybuilding, but a need does present itself from time to time. Note that this is a drug that should be employed to treat lactating gynecomastia, specifically the aspect of lactation. This expensive drug should not be employed as a general remedy for gynecomastia. It is certainly no replacement for Nolvadex, Clomid, or any one of the many aromatase inhibitors. Dostinex should logically be used only subsequent to a blood test reporting high levels of prolactin, or an obvious episode of lactation.

Parlodel (Bromocriptine Mesylate)

Bromocriptine 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 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 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 focuses on leptin, a hormone looked at as sort of a fat themostat, 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 signficantly, 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 date on this drug is very encouraging. In cases where it was given while dieting, bromocriptine was capable of increasing fat loss by a measurable 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 good level of fat loss during the first 6 weeks of calorie restriction, however only the bromocriptine group continued to lose noticeable amounts of weight for the remaining 12 weeks of intervention. Looking over the dosing regimens of several human studies like this, McDonald is recommending that dieting bodybuilders take between 2.5 and 5mg per day. This is given in a single morning dose, due to the relatively long half-life of the drug.

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 probably 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. Obviously the strong incidence of any unwelcome side effects should warrant discontinuing therapy, especially if your 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 or changes in urinary frequency.