Introduction to Pramipexole


by Mike Arnold

Diagnosing the Problem

In today’s ultra-competitive society, the use of performance enhancing drugs in sport has become commonplace, enabling athletes to attain a degree of athletic prowess inconceivable to previous generations. While the performance advantages associated with a pharmaceutically altered state are clear, it does not come without risk. Whether one chooses to utilize AAS, growth hormone, insulin, or any of the other numerous performance enhancers currently available, the likelihood of encountering some type of undesirable side effect(s) is nearly guaranteed. However, by taking the proper preventative action, one can minimize and in many cases prevent these negative side effects from occurring altogether, thereby allowing the individual to achieve his/her goals in the healthiest and most pleasant manner possible.

Of all the potential side effects connected to AAS use, decreased libido and sexual dysfunction are regarded as two of the most undesirable and for good reason. Not only do they interfere with one of man’s most prized activities, but they fly in the face of everything we stand for. Simply put, they are an anomaly to the bodybuilding lifestyle; a contradiction. As a self-made alpha-male, the BB’r is a visual representative of masculinity and virility. He exudes all the physical qualities associated with man-hood in both form and function. Portraying such an image without being able to perform in the bedroom is akin to someone wearing Tap-Out clothing, yet not being able to fight. The two just don’t belong together.

Although excess estrogen and testosterone deficiency are often responsible for these side effects, elevated prolactin, which has begun to afflict steroid users with increasing frequency, also deserves its share of the blame. When it comes to the latter, we can fairly point the finger at both trenbolone and nandrolone—two mainstays in the world of AAS—but with both of these drugs having been around for decades, why have we just recently started to witness an increased incidence of sexual dysfunction and reduced libido?

There are two primary reasons for this—a dramatic rise in trenbolone use over the last decade and an overall increase in AAS dosage among BB’rs/strength trainers. The rapid expansion of UGLs, which has made legitimate trenbolone available to all at an affordable price, provides the opportunity to experiment with much higher dosages than was typical back in days when Parabolan was the #1 (and only) trenbolone drug on the market. At a dose of only 76 mg/amp, 150-300 mg per week was considered standard. As with most drugs, the larger the dose, the greater the likelihood of experiencing adverse effects. This is especially true when combined with other prolactin elevating agents, such as nandrolone. Regardless, personal response is highly variable, with each person reacting differently to individual drugs, combinations of drugs, and dosages. Whereas one may be able to handle outrageous amounts of both trenbolone and nandrolone without issue, another may experience every side effect in the book when administering small doses of just a single drug, even when paired with large amounts of testosterone. None the less, the large majority of users will experience at least some degree of sexual dysfunction, with a smaller portion suffering complete impotence. The only way to accurately gauge your own response is through experimentation.

Although steroids are the primary culprit when it comes to prolactin-induced side effects, certain GH peptides also have the potential to increase prolactin levels, although to a much smaller extent than the aforementioned AAS. Generally speaking, the increase in prolactin witnessed with this class of supplementation is inconsequential, as levels do not rise high enough to cause problems. In fact, this effect is so mild that levels usually remain within a normal physiological range. However, when combined with other prolactin elevating drugs, they may add further fuel to the fire, giving cause for consideration. Lest anyone decide to shy away from GH peptides for this reason, let me again reassure you that when used alone—and often even when used with other prolactin elevating drugs—the benefits far outweigh the risks. It is only when one’s prolactin levels are already high that they increase the potential for side effects. Of the different GH peptides on the market today, only GHRP-6, GHRP-2, and Hexarelin are capable of increasing prolactin levels.


What is Prolactin?

Most commonly referred to as the lactation hormone, prolactin is responsible for the production of breast milk in nursing mothers and also plays a critical role in the growth & development of the mammary glands. Despite its connotation with pregnancy, it is a diverse hormone, having influence over a large number of functions and being implicated in over 300 separate actions. When it comes to steroid users, most are interested in circumventing just two of these—the development of glandular tissue in the breast (gyno) and lactation.

However, prolactin also encourages bodyfat storage by directly increasing the production of a specific protein called lipoprotein lipase (LPL). Lipoprotein lipase plays an important role in fuel metabolism by hydrolyzing triglycerides from circulating plasma chylomicrons (chylomicrons are fat globules which transport dietary triglycerides from the small intestine into circulation) and other low-density lipoproteins, providing free fatty acids to adipose tissue for storage. The higher one’s LPL levels, the more likely one is to accumulate bodyfat. Prolactin has also been shown to increase estrogen receptor concentration within breast tissue, increasing one’s sensitivity to circulating estrogen and making the individual more susceptible to gynecomastia and other estrogenic side effects.

When reviewing the effects of elevated prolactin on the male body, it becomes readily apparent that it is in one’s best interest to keep this hormone under control. While some of the side effects associated with increased prolactin are readily recognizable, others, such as increased bodyfat and estrogen receptor proliferation, are frequently attributed to other causes or not recognized at all. Regardless of one’s awareness, excess prolactin will wreak hormonal havoc on the body, directly working against our BB’ing goals while simultaneously initiating the development of female secondary sex characteristics. All bad—all preventable.

Choosing your Medicine

Until recently, alleviating hyperprolactinemia (excess prolactin) involved the routine administration of one of various side effect-laden pharmaceutical preparations. In many cases, the accompanying side effects were worse than the primary condition one was trying to treat, negating the drug’s beneficial effects and leaving the BB’r between a rock and a hard place. For years bromocriptine was the first-line of defense when it came to lowering prolactin. It was effective, readily available, and reasonably priced, but many found the resultant side effects just too much to handle.

Dizziness, lightheadedness, nausea, vomiting, drowsiness, dyskinesia (uncontrollable body movements), abdominal pain, and loss of appetite are just a few of the potential side effects associated with this drug. Because of this, many would refuse to continue taking it after a just a few weeks of use, instead opting to either deal with the original condition or eliminate the offending drug from their program. Like many 1st generation anti-prolactin drugs, bromocriptine demonstrates poor selectivity in its actions. In laymen’s terms, this means it affects not only the intended target, but multiple other bodily functions/systems as well, which greatly increases the probability of experiencing unwanted and unnecessary side effects.

Newer, 2nd generation anti-prolactin drugs, such as pramipexole, are much more specific in their actions, making them safer and more effective. A good comparison between 1st and 2nd generation would be steroids and S.A.R.M.s. Both are used for the same medical purposes, but both affect the body in completely different ways. Steroids, although certainly effective at turning on protein synthesis, also interfere with the cardiovascular, renal, hepatic, reproductive, and adrenal systems, among others, while S.A.R.M.s demonstrate a high degree of specificity in their actions, allowing them to bypass the aforementioned systems and work almost solely on stimulating muscle growth. 2nd generation anti-prolactin drugs work in much the same way, but unlike the steroid vs. S.A.R.M. comparison, pramipexole is also more effective at lowering prolactin levels than bromocriptine, making it the superior drug all the way around.

The Dopamine Connection

Anti-prolactin drugs, such as pramipexole, work by mimicking the activity of a substance in the brain called dopamine, thereby classifying them as dopamine agonists. Dopamine itself is a neurotransmitter; a chemical messenger between nerve cells in the brain. When levels of this neurotransmitter are normal the body functions properly, but if levels become imbalanced serious problems can develop, such as Parkinson’s or Restless Leg Syndrome.

However, in order for dopamine to have an effect it must first attach to dopamine receptor sites, which are found on the surface of the cell. Once attached, the receptor receives, recognizes, and responds to this chemical signal. As a dopamine agonist, pramipexole works by stimulating these same receptor sites, thereby producing the same effects as dopamine, but you may be wondering, how is this relevant to prolactin?

As one of the predominant regulators of prolactin, dopamine has a direct impact on its production. More specifically, dopamine works to reduce prolactin levels by attaching to D3 receptors, which inhibit the production of prolactin by lactotrophs (lactotrophs are prolactin producing cells located in the pituitary). Acting as a dopamine substitute, pramipexole works through the same mechanism, fooling the body into thinking that dopamine levels are high. This shuts down, or reduces the production prolactin, depending on the dosage administered.
Exactly how the steroids trenbolone and nandrolone increase prolactin levels, we can’t be sure, but one thing we do know is that many who use these drugs have experienced dramatic elevations of this hormone—sometimes far above normal levels. This can and often does lead to one or more of the aforementioned side effects. Pramipexole works to address the issue directly, shutting down prolactin production at its root.

Pramipexole vs. Cabergoline

Of all the anti-prolactin drugs currently on the market, pramipexole and cabergoline are widely considered the best. They have the least side effects and are the most effective. However, there are differences between them. Which is better? Ultimately, it will be a matter of personal opinion, as there are several factors one must take into consideration before coming to any conclusions. Below I will provide some of these differences so you can make an educated decision in your own best interest.

In terms of side effects, they are very similar when viewing the clinical data. Still, what happens in the real-world does not always mimic what happens in the lab, so with that in mind, I will tell you that opinions can vary significantly on this subject. Some people respond better to one than another, but this is really only an issue at the onset of treatment, as side effects tend to diminish as the body adapts to the drug’s presence. The most common side effects for both drugs include tiredness and nausea, but these can be reduced, or even eliminated by gradually titrating one’s does upward over a few weeks, rather than rushing straight into a higher dosing range (we will talk more about that in a minute).

In term of dosing frequency, Caber is typically administered 2X weekly to as much as EOD, although 2-3X weekly is the most common. With Pramipexole, its shorter half-life requires daily dosing in order to maintain fairly even concentrations of the drug in the bloodstream. In terms of cost, pramipexole usually has the upper-hand when it comes to the amount of money one needs to spend up-front, although the lower dosing of cabergoline tends to balance it out in the long-run.

One downside associated with cabergoline is the large percentage of fake and bunk products circulating on the marketplace. Simply put, cabergoline is much less likely to be real than pramipexole and there are a few reasons for this. For one, cabergoline can only be purchased from UGL’s, various online pharmacies, or by prescription, while pramipexole can be sold by anyone, including peptide-research chemical companies. This is due to the inability of cabergoline to remain stable in a solution. Legally, peptide-research chemical companies cannot sell drugs in a form which implies human use, such as pills or capsules, so they are limited to selling their products in a solution for “research” purposes.

Why is this an advantage for pramipexole? Because UGL’s and online pharmacies do not subject their products to the same rigorous, independent lab testing that certain peptide-research chemical companies do, nor can they provide evidence of it, as they are illegal operations. If you receive a bunk product you have absolutely no recourse—and they know that. Obviously, there are certain advantages connected to these illicit operations, such as being able to obtain various, illegal drugs, but in terms of quality control, they are severely lacking compared to U.S. land-based pharmacies and the upper-tier peptide-research chemical companies, which frequently have all of their products produced by U.S compounding pharmacies and subsequently 3rd party lab-tested. Since peptide-research companies sell legal drugs—or drugs in a form permissible for human purchase—they can legally have each and every batch of every product they sell independently tested for both purity & potency by legitimate U.S. labs. This is a guarantee you simply can’t find with UGL’s and internet pharmacies, unless you are certain the product you are receiving is a pharmacy-grade product.

For example, the recent batch of pramipexole by Iron Mag Research Chems, which inspired me to write this article, was recently tested at just under 99% purity. I saw the mass-spec reports, so I can confirm the claim. The point here is that while there is certainly real cabergoline out there, quite a bit of it is fake and it is not always possible to discern what is legitimate and what is not. Personally, I have been burned more than once by someone who supposedly sold “good” caber.

One side benefit of pramipexole is its ability to increase GH levels—quite substantially I might add. Clinically, pramipexole has been shown to increase growth hormone levels in a dose-dependent fashion. Not too a bad for a “side effect”, if you ask me. As you can see, the best drug will be the one that not only provides the least amount/intensity of side effects (you won’t know until you try them), but what benefits you find to be most important.

Administering Pramipexole

For the purpose of prolactin suppression (gyno, lactation, sexual dysfunction, libido, etc), pramipexole is normally administered at a dose of .5-1.0 mg/ day. However, one should not begin there, but gradually increase their dose over a period of 2-3 weeks in order to minimize side effects. If using liquid-based products, find an oral syringe capable of measuring in small increments and begin at .125 mg/day for the first 3-4 days. Afterwards, move to .25 mg/day for 3-4 days, 3.75 for 3-4 days, and finally .5 mg for 3-4 days. If necessary, continue using this gradual progression scheme up to 1 mg/day.

Few people will need more than 1mg daily when using a properly dosed product, even when using very high dosages of trenbolone and/or nandrolone. The goal should be to use the lowest effective dose possible, as there is no advantage to using more than necessary, aside from increased growth hormone production. While some may find this to be a worthy goal in itself, I believe there are better, less side effect-prone alternatives for increasing levels of this hormone, such as GH peptides or exogenous growth hormone itself. Lastly, with tiredness being a common side effect of these products, most prefer to administer pramipexole shortly before bed, as it will help induce a sound sleep without significantly impairing wakefulness the following day, although tiredness may persist for the first couple weeks as the body adapts. Gradually increasing the dose over time is the best way to minimize/avoid this side effect.

These days, with a number of proven, cost-effective anti-prolactin drugs on the market, there is no reason to have to deal with any side effects arising from elevated prolactin levels. Those who choose to use low-moderate doses of trenbolone and/or nandrolone often find that a single 60 ml bottle, when dosed at the typical 1mg/ml, can last for up to 4 months of continuous use or longer, depending on personal response. So, expense is much less of a concern than it is with many other BB’ing drugs.

If you are like me and are unable to use some of your favorite steroids for longer than 4-5 weeks at a stretch without experiencing unacceptable side effects, then perhaps pramipexole is something you may want to consider. It’s cheap, easy to obtain, and works well. As a prospective weapon in our BB’ing arsenal, pramipexole does exactly what it is supposed to, earning it a place alongside our other reliable ancillaries.

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