Written by justis berg
25 May 2010


Extreme Muscle Enhancement

By Carlon M. Colker, M.D., FACN

Clomid®: Off-Label Deliverance for Juice-Heads

Clomiphene citrate (also known as Clomid® or to be precise, 2-[p-(2-chloro-1,2-diphenylvinyl)phenoxy] triethylamine citrate) is a drug with FDA approval for use in women struggling with fertility issues. As it induces ovulation, Clomid is generally one of the first drugs that couples will be introduced to if the issue arises. Clomid® is used to induce ovulation in women with ovulatory disorders. It is also used to assess ovarian function and the likelihood that a woman can still produce viable eggs.

Ask the older and more traditional reproductive endocrinologists, and they will tell you Clomid® is not a drug for men. But in recent years the more cutting-edge endo-practitioners have discovered a valued 'off-label' use for Clomid® in men with low sperm count due to genetic factors or in former juice-heads recovering after years of anabolic steroid drug abuse. Of course while it hasn't stopped numerous male bodybuilders from exploiting Clomid® as a testosterone supporting drug to optimize muscular development, it's not how it is used in proper practice.

Interestingly, Clomid® is a somewhat mysterious and complex medication whose mechanism of action is not fully understood. What we do know is that it works in the body somewhere high up along the estrogen axis but is capable of reacting with any tissue in the body that has estrogen receptors. While the action of Clomid® in the female physiology certainly takes place at the level of the hypothalamus and pituitary, it may also involve the ovaries, endometrium, vagina, and/or cervix. The action in the male also appears to take place at the level of the hypothalamus and pituitary, but may also act at the level of the adrenals, peripheral fatty tissues, liver, and/or testicles.

Basically what we know is that Clomid® influences the way the estrogen hormone estradiol influences three other hormones. The first is gonadotropin-releasing hormone (GnRH), a hormone produced by the hypothalamus (a gland located in the skull center above the pituitary gland) that affects the release of hormones in the pituitary. The other two are produced by the anterior lobe of the pituitary and are called follicle-stimulating hormone (FSH) and luteinizing hormone (LH).

While physicians are not in agreement on the precise pharmacokinetics, it appears that Clomid® fools the body into believing that the estrogen level is low. Furthermore, we know Clomid® competes with estrogen for estrogen-receptor-binding sites and probably delays the replenishment of intracellular estrogen receptors. There is also some data suggesting that Clomid® has both estrogenic and anti-estrogenic properties, but the test results show a variable response from one species to the next and one receptor site to the next.

The locker room, black market, and Internet chat lore is that Clomid® blocks the production of estrogen. Unfortunately, this is a reckless misinterpretation of the mechanism, because the drug will certainly not reduce your estrogen or the problems that come along with having high estrogen. In fact, in the male physiology, it actually stimulates some degree of estrogen production, though not nearly as much as testosterone. So that's why 'use' and not 'abuse' is the key with this drug, as with any.

Along the same estrogen-blocking reputation, some morons also claim that Clomid® is effective in reducing gynecomastia ('bitch tits'). Well, more lies. If you are not careful, Clomid® can in some cases actually cause gynecomastia. So from that standpoint, one needs to watch not only their testosterone levels, but also their estradiol.

To be as accurate as I can be, the activity of Clomid® is probably achieved by interfering with the inhibitory effects of estrogen, both at the level of the hypothalamus and at the level of the pituitary. In a process called negative feedback, the higher the estrogen, the more the hypothalamus and pituitary reduce the production of gonadotropin hormones. Clomid® seems to simply come in and occupy the estrogen receptors at these levels, while at the same time not activating them. The result is that there ends up being more GnRH, FSH, and LH. In the female, FSH and LH results in the release of mature eggs (a process called ovulation). In the male physiology, the release of these gonadotropins will stimulate testosterone (via LH) and sperm production (via FSH).

Typically, male bodybuilders use 50-mg tablets taken orally each day for up to six months each year. While Clomid® is not a steroid, has no androgenic activity, and does not appear to interfere with pituitary-adrenal or pituitary-thyroid function, it is still not a drug for sport ergogenic use. In fact, there are no adequate or well-controlled studies that demonstrate the effectiveness of Clomid® in men. What is cited in the literature are gynecomastia and testicular tumors reported in males using Clomid® long-term. Although in fairness, it should be noted that the cause and effect relationship between reports of testicular tumors and Clomid® may be nonsense.

Yet Clomid® abuse has risen sharply among male bodybuilders and athletes in recent years. I attribute this to the fact that it is relatively easy to take because it is an oral medication available in tablet form (most guys want to avoid needles). It is also more readily accessible when compared to more highly visible sporting drugs of abuse. As far as fertility drugs in this class go (and I think they are all grotesquely over-priced), it is relatively inexpensive. But Clomid® will still cost you about $10 per pill.

In my practice, when an experienced bodybuilder abuses anabolic steroids over a continuous amount of time without going off-cycle (many months or years), sperm production shuts down, making a man infertile. This may also occur in a man with a legitimate reason to take continuous testosterone drugs. This side effect may not pose a health problem, but it truly sucks if you are trying to get your wife pregnant. In my experience, it's not as big a deal for older bodybuilders (50+) who have been through marriage and kids. As long as their wedding tackle still operates, they generally don't care if their ejaculate is bereft of sperm.

But for the younger set who aspire to build a family, this result can be alarming, to say the least. The general profile is that of a bodybuilder between the ages of 28 and 43, with a history of continuous anabolic steroid abuse, and no time off between cycles. This scenario is growing with ever-increasing frequency, as more and more bodybuilders are resistant to go off-cycle.

Recall that in the 'old days,' bodybuilders would spend a significant time of the year off-cycle to clean out. It was only around contest time that they would start the heavy juicing. Also, guys abuse much higher doses for longer periods as well. There was a time when guys were either on a low dose for a longer stretch, or a higher dose for a shorter period, depending on their philosophy. But only now has there ever been high-dose, long-duration abuse.

When this occurs, sperm production grinds to a halt. The condition is diagnosed by testing semen under the microscope for sperm. Typically, there should be 20 million or more sperm visible per cc. In those with infertility due to continuous anabolic steroid use, often one doesn't see even a single sperm!

Assuming this type of anabolic steroid abuse is at the root cause and not some genetic factor, sperm production should eventually resume. But in my experience, this may take anywhere from six months to five years in order for the system to correct itself. Also, a small percentage of really heavy abusers never seem to recover, and they remain infertile for life.

So what good news do I have for you if you don't want to roll the dice on the waiting game to see if your sperm production picks up while watching your hard-forged muscle mass shrivel into nothingness? Well, the good news is Clomid®. Though not yet FDA-approved for this purpose, once off anabolic steroids, Clomid® is being used to rescue the hormonal axis and thus trigger sperm production.

Generally, we start with 25 mg per day. But doses can go as high as 75 mg per day, depending on the responsiveness of hormone production. The drug is started after anabolic steroids are stopped. Simply stated, if you're still abusing, you're cruising for a bruising. Blood levels of testosterone, LH, and FSH are all tested again in four to six weeks, to assess the responsiveness of the pituitary and testes. If the numbers don't budge much, the dose is increased. The good news is that approximately two-thirds of these patients respond within a matter of months, and guys can subsequently get their wives pregnant.

Just know that you won't see viable sperm in the semen again for about three months. So, unlike the blood tests, there is no sense in retesting semen before that time. But once you do find sperm again, you are good to go. Of course, if your body successfully resumes producing viable sperm, there is always the option of immediately harvesting a sample and cryogenically storing it for future in-vitro fertilization (IVF). This gives patients that truly have a medical need for testosterone to resume use if they so desire, while still having the ability to inseminate. Interestingly, there are occasions in which the Clomid® actually does the trick and the hormonal cycle is reactivated. As a result, some patients never have to go back on testosterone drugs, as their levels spontaneously normalize after a little Clomid® stimulation.

Again, one can always forgo the Clomid®, stop the juice, and just wait it out. In my experience, most reproductive endocrinologists will tell you that you still have roughly the same chance of recovery. But as I said already, you may be talking about years down the road. Most couples understandably don't want to wait that long— or take the chance that once they get to that point, they find out that their plumbing hasn't fixed itself. So in these particular types of cases, I actually advise my patients that it is better to address it earlier with a drug like Clomid® because the longer the axis remains dormant, the less likely I feel it will be successfully reawakened.

Finally, I've come across a number of dip-shit bodybuilders over the years who used Clomid® as a regular part of their cycle. Whenever I asked them why they did it, none could ever explain why. This ignorance is born out of not really knowing why they were taking a drug in the first place and only taking it because someone they thought knew what they were talking about told them to do it.

The fact is that it has no place in a cycle. For example, it defies logic to use it with testosterone, because the effect of testosterone is to decrease production of LH at the level of the pituitary gland. This is the opposite action of Clomid®. Provided there is no negative feedback driven by high testosterone levels, Clomid® should cause LH to increase and thus, in time, stimulate production of one's own natural testosterone.

Double-dipping by stacking Clomid® on a backdrop of anabolic steroids is pointless because an unnaturally high anabolic steroid level will negatively modulate LH production at the level of the pituitary. This is the opposite of what Clomid® is trying to do. As I see it, it is only off-cycle in the way I discussed, or at the very least, coming off-cycle, that Clomid® has its greatest utility.

Dr. Colker's book, Extreme Muscle Enhancement: Bodybuilding's Most Powerful Techniques is available by calling 1-800-310-1555 or ordering the book online at www.prosource.net. MYO-T12™ is available at www.myot12.com. In addition, if you have a question for Dr. Colker, check out www.musculardevelopment.com, MD Forums, MD Staff and Pros, Extreme Truth With Carlon Colker, M.D.!