Cabergoline (Dostinex)
Dostinex was originally introduced to the bodybuilding community by the anti-aging crowd. About a decade ago, the only place you could really find this stuff being sold was on mail order lists for various life-extension clinics. Although they are, frankly, a very weird bunch of people, the life-extensionistas were among the first to find and make available a lot of the stuff that eventually found its way into athletic circles, like Dostinex and other such nootropics (drugs that increase mental activity).
Dostinex is one of those drugs. I first saw it on an anti-aging clinic’s price list about a decade ago, and more recently, I saw it being discussed by various people who are “in the know” on the internet. The former fact made it slightly interesting to me, while the latter had exactly the opposite effect. Actually, I first mentioned it in an ancillary article I wrote several years ago, but recently I decided to do some more research on it, and I have to admit, it’s a very interesting drug. Before I explain what it does, I think a discussion of some important hormones and enzymes are in order.
Dostinex is usually employed by bodybuilders to combat prolactin and effects related to prolactin…that’s so before we go any further, lets , it’s very important to understand exactly what that hormone is. Prolactin is a single-chain protein, very closely related to growth hormone. It is secreted by what’s known as lactotrophs in the anterior part of your pituitary gland. In addition, Prolactin is also synthesized and secreted by many other cells in the body, like immune cells, in the brain, and in women is even secreted by the decidua, in the uterus of pregnant women.
If you’ve done any reading at all on prolactin, you have probably come across the fact that its major effects are felt by the mammary gland, and that stimulating mammary gland development and milk production are its primary role. While this is true, many issues have prolactin receptors, and although the anterior pituitary is the major source of prolactin, it is actually synthesized and secreted in several other tissues. Too much prolactin expression can even be responsible for certain types of pituitary tumors. But the most prevalent side effect we see from it in bodybuilders is development of excess mammary tissue and milk production. Unfortunately, mammary gland development and milk production are among its major effects. Great if you are a cow, but not so great if you are a bodybuilder. Yeah, that’s right- too much prolactin can cause galactorrhea (excessive or spontaneous secretion of milk). The other prevalent side effect is sexual dysfunction. I suspect that the average male bodybuilder doesn’t want anything to do with any of that.
Excessive secretion of prolactin – which is known as hyperprolactinemia - is a relative common disorder in humans. This condition has numerous causes, including prolactin-secreting tumors and therapy with certain drugs, like anabolic steroids.
Common symptoms of hyperprolactinemia in women can include menstrual irregularities, and galactorrhea (which was covered in the preceding paragraph). Sadly, men who have hyperprolactinemia tend to have most of the same symptoms; enlarged mammary glands, milk production, and also have some other side effects to contend with, such as hypogonadism, decreased libido (sex drive), decreased sperm production and impotence, but at least they very rarely produce milk, although it’s possible...and disgusting.
Of course, we can put a stop to possible prolactin related side effects, if we can get some dopamine secretion going on. You see, dopamine is a major prolactin-inhibiting chemical and sends a message to your body to decrease its rate of prolactin secretion. Basically, it’s secreted into your blood, binds to receptors on lactotrophs (remember them?), and then inhibits the synthesis and secretion of prolactin. That’s important, because it works in two ways…it prevents both the synthesis and the production of prolactin.
This is where Dostinex comes in…
Dostinex (Cabergoline) is a dopamine agonist. Dopamine is a chemical, found in the brain, which transmits nerve impulses and is involved in the formation of epinephrine. More likely than not, this is why the Life-Extentionistas are very big on this drug. Dopamine is also released by the hypothalamus, and hormone can inhibit the release of prolactin from the anterior lobe of the pituitary, so given all the bad things that we have already seen to be a result of excess. If you use anabolic steroids, Dostinex will help you reduce the chance of any of these prolactin related side-effects. It has actually been shown in numerous studies to have a very high success rate in lowering prolactin and prolactin related conditions and side-effects (1) (2).In fact, for management of hyperprolactinemia and it’s symptoms (got milk?), Dostinex is the preferred treatment in terms of effectiveness as well as having very few undesirable side effects (3). It does this very well for both men and women, it should be noted…almost identically actually (4)
Since it lowers prolactin very efficiently, Dostinex will even get rid sexual dysfunction caused by excess prolactin (5) (which is (anecdotally at least) highly correlative with the use of certain steroids like the Nandrolones and Trenbolones (Deca and Tren). This is great news for everyone who loves Tren and Deca, because those two steroids are really great additions to almost any cycle- but many people avoid using them because of the possibility of them causing impotence (often called “deca dick”).
Using Dostinex will allow you to include steroids like Tren and Deca in any cycle- and even combine them in the same cycle- without worrying about sexual dysfunction. In fact…even if you aren’t experiencing any sort of sexual dysfunction, Dostinex will shorten the time you need to recover and gain an erection between orgasms, and can significantly enhance all parameters of sexual drive and function (6). In other words, if you’re not worried about sexual issues and you take Dostinex anyway…it’ll still help you out in bed. And from what I have heard, it’s well worth the money for that effect.
Of course you can actually use Dostinex safely for an extended amount of time (many studies go on for months if not years, and its efficacy and safety are well documented), but women need to be more careful than men, and certainly need to discontinue using it if they’re pregnant or trying to conceive. SO Dostinex can help you, the average steroid user, by combating gyno-like effects, as well as galactorrhea, and sexual dysfunction. Sounds great, right? Of course it is…but since Dostinex is a dopamine agonist, which means it’s good for a whole lot more.
ou see Dopamine is what’s called a monoamine, which is naturally produced in the body by modifying an amino acid.
Dopamine
And it’s this structure which makes it very interesting to us. Dostinex as you already know is what’s known as a dopamine “agonist”- or substance that triggers a response in a specific body tissue or group of cells by binding to specific receptor on or inside the cells, as if it were actually the bodily substance that usually binds to that receptor. Probably the one that most people are familiar with, with regards to agonists is ephedrine, which is an andrenergic agonist. This is why ephedrine makes you feel “wired”…it “feels” like adrenaline to your body. Cabergoline is a dopamine agonist…which makes it “feel” like dopamine to your body.
Dostinex
So what does that mean? Well, in the brain, dopamine helps control the flow of information from other areas of the brain. So a dopamine agonist will help you process information more quickly, and possibly improve your memory also. Some athletes use Dostinex because it helps them learn new motor skills more quickly and thus they can learn new techniques or plays at a faster rate than their competition; needless to say this gives the athletes using Dostinex a huge advantage over their competition. This ability to work on your bodies information pathways and nervous system are doubtless why it’s been successfully been used to fight Parkinsons disease (7)(8).
But does this actually work in real athletes? Well, actually, that’s why I started reading about Dostinex. See, I have the fortune of being able to basically call some of the most famous strength coaches in the world whenever I want. And, recently the last time I spoke to one about training and anabolic steroids, I asked him about different training programs for a person on steroids- and his answer said that it depends on whether that person was taking a nootropics or not. And as you may remember, Dostinex is a nootropic. It was that conversation that made me really take a closer look at Dostinex. And of course, that strength coach told me that his athletes have used nootropics with great success. The down side of knowing internationally renowned strength coaches is that their sense of humor is usually a little off, and if you have the fortune of being able to pick their brains on training, you also invariably have the misfortune of ending up on their group e-mail list which gets you a whole host of bizarre forwarded e-mails…
In fact, when you don’t have enough dopamine, you may even have difficulty concentrating…low dopamine levels have also been cited as a possible underlying cause for Attention deficit disorder (ADD) and Attention deficit/ Hyperactivity disorder (ADHD). In fact, many several medications used to treat ADD and ADHD will also serve to stimulate dopaminergic, and this could be one of their possible mechanisms of action.
Dopamine is also what’s called a “pleasure chemical”…it’s usually released by your body when you experience a rewarding experience such as eating your favorite food, having sex, winning the lottery….whatever. Interestingly, since this “happy” effect is felt when you are satiated from food, it’s highly possible that Dopamine agonists will cause you to feel “full” more often and decrease desire for food without the discomfort that dieting usually brings. Dopamine is released when you eat a nice big meal…so…a dopamine agonist like Dostinex may make you not want to eat as much, and help you feel full even if you don’t eat enough. Dostinex, therefore, may be of great interest to precontest bodybuilders and other dieters, who want to avoid some of the discomfort and anxiety that calorie restriction can bring.
Certain recreational drugs also have a lot to do with their effects on dopamine. Cocaine is what is known as a dopamine transporter blocker; what this means is that it competitively inhibits dopamine uptake to increase the amount of time released dopamine is active in your body. This makes you feel good, while the dopamine is floating around your body. Methamphetamine is another illicit (illegal) recreational drug that acts on dopamine as well. It actually serves to competitively inhibit dopamine uptake as well as increasing dopamine flow through a dopamine transporter pathway. That’s how those drugs make you “feel good.” Dostinex is, of course, neither physically nor mentally addictive, but since it is a dopamine agonist, its users often experience an enhanced positive sense of well being. So besides helping with all of the things discussed earlier, Cabergoline will also just make you feel damn good.
So now that I told you about it, I’ll tell you how much Dostinex do you need to start experiencing these effects…or basically, how I’m going to use it, now that I did all this research on it!
From the reading I’ve done, you only need about half a milligram (1/2mg) a week to experience all of the anti-prolactin, prosexual, antidepressant, and cognitive effects of Dostinex, but that’s on the very low end of the effectiveness scale. This stuff has an extremely long active life in the body, so once a week dosing is fine…but if it were me, and I were taking this stuff, I’d probably be using about .25mgs-.5mgs twice a week.
It should be taken before bed-time, because it may actually help you sleep a bit better, (9), Can be taken with or without food and not alter the pharmacokinetics (how it functions in your body) (10), and (incidentally) according to the literature is a much more efficient drug than Bromocriptine(11).
I think once people find out about this drug, it’s going to find it’s way into quite a few bodybuilders’ cycles alongside Tren, Deca, or both…and athletes are going to take advantage of it’s uses for skill acquisition and motor co-ordination help…and all the other stuff…the prosexual properties and general “feel good” properties of Dostinex make it a great choice for anyone interested in …err…feeling good and having better sex…which I suspect is basically everyone, not just bodybuilders and athletes. I guess I should have paid more attention to this stuff when it started appearing on those Life-Extension club pricelists a decade ago…but at least I figured it out now….even if I happen to be a bit late on this one.
