by Dharkam

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Disclaimer: Discussion of pharmaceutical agents below is presented for information only. Nothing here is meant to take the place of advice from a licensed health care practitioner. Consult a physician before taking any medication.

GHB is one of the most popular yet clandestine substances used by bodybuilders. In fact, ask any high level competitor willing to divulge his favorite stack, he will probably omit GHB -- not that he is lying, but rather he is overlooking it. GHB is a given, especially as a dieting aid. No need to mention it, it is so obvious. On the other hand, GHB will probably not do much cosmetically on its own. GHB appears more as the cornerstone of a stack rather than the key compound. Before exploring the why's and how's of GHB in bodybuilding, let's first see how this molecule is perceived by the medical community.

The discovery of GHB

GHB was first discovered and introduced by the French scientist Henri Laborit in 1960 [1]. Laborit was a pioneer in the field of eutonology. That is the study of the methods that permit us to maintain or to restore biological homeostasis in the human body. He created GHB while he was searching for a GABA analog able to cross the Blood-Brain-Barrier (BBB) so that it could easily enter the brain.

GHB -- which stands for Gamma-hydroxybutyrate de sodium in French or Gamma-hydroxybutyrate in English -- was soon sold in France (1961) as as an anesthetic agent Gamma-OH [2]. Gamma-OH is a very popular compound in Europe. Though it was designed to be administered intravenously, European bodybuilders drink Gamma-OH from ampules. In the US, you will probably not find Gamma-OH but you will certainly find some generic, cheaper brands of GHB.

What does the science literature tell us about GHB?

Our body also produces GHB. Some minute amounts of GHB were first found inside the brain. Later, some traces were found in other tissues, but it is GHB's impact on the brain which has retained the attention of the medical community [3]. So far no physiological function of GHB has been uncovered, so many consider it as an experimental compound rather than a regular drug. Laborit immediately saw GHB as a very beneficial and important metabolite. He was impressed by its anti-oxidant and anti-ischemic properties which could potentially protect the brain against various types of damage. He went so far as to propose it to treat Parkinson disease in psychiatry or to heal morphine addicts [4].

Laborit's view of GHB contrasts with much of the medical community. GHB is regarded more as a dangerous compound because of the harmful interactions seen with alcohol or some street drugs. But as I said, Laborit was both a genius and a pioneer and was far smarter than our average M.D.

GHB and sleep

GHB is a metabolite of GABA (gamma-aminobutyrate), an important neurotransmitter. As I said, unlike GABA it can readily enter the brain. On the other hand, GHB is able to increase GABA level in brain by various mechanisms. An oral intake of GHB can increase the level of this molecule 100-fold in the brain which can cause some unexpected supraphysiological reactions. As a Central Nervous System (CNS) depressant, GHB has been involved in sleep [3]. In that regard, it has been compared to melatonin. The brain's concentrations reached after an infusion of Gamma-OH are so high that it knocks you out immediately. This explains the classification of the drug as an anesthetic. Morphine administration also increases the brain concentration of GHB. Some speculate that GHB mediates part of the analgesic actions of morphine though there is no definite proof of this.

According to Laborit, oral GHB induces "slow wave sleep followed rapidly by paradoxical sleep." As with natural sleep, an increased release of growth hormone (GH) rapidly ensues. Laborit speculated that an increased level of brain serotonin was involved in both phenomena [4].

Some Gamma-OH users do not fall asleep but rather experience either a short lived state of drowsiness, lethargy or euphoria. Others cannot sleep anymore. This is explained by the different dosages of GHB used as well as personal reactions to it. More often that not, you are likely to fall asleep. Unlike most sleeping pills, GHB induces a more natural sleep and its effects do not vanish after a short while. Laborit frequently prescribed Gamma-OH to patients of all walks of life. He reported that after 6 years of continual oral use, no psychotic disturbance has been reported. On the contrary, "the anxiolytic and recuperative effect of this drug is appreciated by many users" [4].

GHB and growth hormone

Among the bodybuilding community, the fact that GHB induces a strong release of GH has done more to popularize this compound that any of its other effects. However as we will see later, I do not think the GH release is the major reason why bodybuilders keep using GHB.

GHB is very different from many other GH releasers such as amino acids. With the latter, high doses are required and the scientific literature does not report consistent results. Very little GHB is needed to induce a strong GH release -- and this GH response to GHB administration is consistent in the scientific literature. Furthermore, unlike with amino acids, oral GHB works very well.

The latest study to date reported a 2-fold increase in the amount of secreted GH with only 2.5 grams of oral GHB in humans [5]. Higher doses (3 to 3.5 grams) failed to induce a higher GH release. Unlike with higher doses, the 2.5 grams amount did not produce any side effects. So, this should serve as a scientific basis as a safe dosage for bodybuilders. This is also approximately what bodybuilders were using instinctively.

Gamma-OH contains 2.42 grams of sodium GHB, which means 2 grams of pure GHB. Drinking 2 vials at a time would be too much. On the other hand, if you have access to a generic brand, you may have an easier time fine tuning your daily intake. You can take GHB once or twice a day. Of course, the main occasion to take GHB is at night, but an extra morning intake is also very popular in Europe in addition of the nocturnal use.

Some dieters stack GHB with Clonidine (an alpha 2 adrenoceptor agonist -- that is the opposite of Yohimbine) which is another known GH releaser in an attempt to induce an even stronger GH surge. I do not recommend this stack. It is unhealthy, as many interactions between GHB and Clonidine could develop. Also I doubt that the GH release shows much increase with both agents, as GHB alone should bring us toward the maximal upper limit of release already.

GHB and cortisol

This is a far more controversial subject. Most bodybuilders assume that as a calming agent, GHB should lower the secretion of the stress hormone cortisol, especially at night. This is perceived as a major benefit because cortisol release keeps increasing as the night goes on. GHB is assumed to combat this increase. Unlike the impact of GHB on GH, these assumptions are not backed up by the majority of scientific literature.

It certainly makes sense that a relaxing agent should depress cortisol level. However the very early studies in which GHB was infused demonstrated that GHB was raising rather than reducing cortisol secretion [6]. Van Cauter's study confirmed that oral GHB tended to increase cortisol secretion in the first part of the night even if this was not consistent at the lowest dose compared to higher intakes. With the highest doses (3.5 grams) and not with the lowest amount, cortisol secretion was reduced during the second part of the night maybe as a negative feedback [5]. I certainly would not use that much GHB in hopes to reduce my cortisol secretion. GHB should therefore not be considered as a cortisol inhibitor. As well, we now know that reducing cortisol levels alone is not the way to go in order to get bigger, even though this is a common belief in the bodybuilding literature. Those who tried failed miserably.

GHB and other hormones

Another side effect of GHB is that it is able to induce a strong release of prolactin [5]. Prolactin is a lactating hormone which tends to promote the development of gynecomastia. If you already have this condition, prolactin can help you get some milk out of it.

Though GHB tends to promote hypothermia, it does not seem to have any negative impact on the thyroid hormones [7]. On the other hand, it does not accelerate thyroid activity which could have been useful while on a diet. Laborit also claimed that many of his patients reported an aphrodisiac effect of GHB, especially the women [4]. I have yet to meet a male bodybuilder reporting this side effect. Maybe is it the steroids which hid it.

What has the experience of bodybuilders shown us about GHB?

GHB while on synthetic GH

Probably most bodybuilders start using GHB because of the GH release. Although this GH release will help you get leaner during a low calorie diet, I do not think it will do much for muscle growth. Studies have failed to detect any increase in IGF-1 level as a result of the acute use of GHB [5]. This means that the GH threshold needed to accelerate anabolism was not reached despite the GHB.

While GHB alone does not produce sufficient GH for anabolism, it can be used to amplify the benefit of GH injections. It seems to be beneficial to use GHB at night a bit before a GH injection. Exogenous GH is likely to stop our own production of GH. This is costly not only in terms of muscle mass but also financially. If you have to make up for the drop of your natural production by injecting more GH, this is a huge waste of money. On the other hand, a simple capsule of GHB can at least restore the natural GH production at night. Therefore, you end up adding your natural GH to the synthetic one rather than subtracting it. This is going to greatly increase the potency of your GH stack and better maintain your body homeostasis.

GHB while on steroids and Clenbuterol

While on a serious androgen stack (which means more than a gram a day), it becomes very hard to fall asleep. If you add clenbuterol and the starvation due to a diet, the effect is magnified. Though its effect is short-lived, GHB will help induce drowsiness. At the correct low doses, you should not suffer from the excitatory effect of GHB. Its overall calming effect will be a welcome relief. As Laborit has mentioned, GHB promotes recuperation, which is an added benefit for those who have trouble falling asleep.

GHB while on a diet

Bodybuilders' low calorie diets are usually very rich in proteins and low in both carbs and fats. Though very effective for losing weight, this type of diet is unhealthy for several reasons. One of them is that it promotes the formation of lots of hydrogen ions (acids) which will acidify the blood leading to a continual state of acidosis. That is undesirable, because it will promote the oxidation (destruction) of the proteins you ingest as well as your muscle proteins. This is particularly true of glutamine which is wasted at an accelerated rate during the state of chronic acidosis. Bodybuilders are generally unaware of this risk, or else they minimize it. It's a costly mistake, as acidosis has a very negative repartitioning effect. It induces muscle wasting while it promotes fat conservation.

GHB will partially combat the state of acidosis while on a diet. GHB gives rise to the formation of basic agents (bicarbonates) [8]. These are the molecules that will fight and neutralize acids. If you are not on a diet or do not follow a high protein regimen, the alkalizing effect of GHB is of no value. Your body will get rid of the antacids. If you are in a state of acidosis because of your diet, this particular action of GHB will spare some of your muscle mass while permitting fat loss. The extra GH release due to GHB will also help you to get rid of the extra acid and therefore spare your muscle mass and glutamine. If you are not in a state of acidosis, this anti-catabolic action of GHB will not appear.

You may wonder if the alkalizing actions of GHB might help you train harder. The theory would go like this:

The muscle burn sensation at the end of a set is due to the excessive local formation of acids.

This intracellular acid has a depressing impact on muscle strength.

By fighting acid, GHB would help you get some extra reps.

It does not appear to be the case. The alkalizing effects of GHB are mostly due to the formation of bicarbonates. Although bicarbonates are excellent for neutralizing the circulating acids, they are poor buffers of the intracellular acid. So while you can look forward to the muscle sparing action of GHB during a very low calorie diet, do not look for GHB to increase muscle strength during training.

GHB and potassium

When people see an article about potassium they generally skip to something more interesting. In this case, please read on as it is very important not only for your muscle mass but also your health. Many bodybuilders report cramps while on GHB. It is unlikely that GHB is the main mediator of those cramps.

Some of the drugs taken by bodybuilders induce cramps as a side effect. Clenbuterol for example. The addition of GHB may exacerbate this tendency, and a low calorie diet will act like oil on the fire. GHB tends to promote electrolyte imbalance which paradoxically is going to be helpful for bodybuilders if we exclude the cramps and the possible negative influence on heart rate of course.

GHB promotes the intracellular accumulation of potassium [8]. While too much potassium in the heart may lead to an irregular heart beat, it will assist the growth in the skeletal muscle. Unfortunately, an accelerated entry of cellular potassium is going to empty the blood of this mineral, which may be the reason why GHB promotes cramping.

This shortage of potassium can easily be overcome by using oral potassium pills [8]. The heart is the problem here. The more potassium you would ingest, the more you would grow except that it might also kill you. So you have to watch your extra potassium intake. As soon as you feel that your heart is beating abnormally, you know that you are using too much potassium even though the cramps may still be annoying. I suggest to use extra magnesium (around a gram a day depending on your weight) in order to combat the potential side effects associated with extra potassium while getting the most benefits out of it. While we are on the subject of supplementation, be also careful whenever you stop GHB. The extra intracellular (especially muscle) potassium is going to quickly leave the muscles and pass in the blood. This time, you run the risk of having too much potassium in your blood. So you want to reduce or stop your potassium supplementation for a short while whenever GHB is discontinued.

I said that the accumulation of potassium in the muscle cells is very positive for muscle growth. Hard training and severe diet both tend to reduce the intracellular accumulation of potassium while promoting the invasion of sodium. A state of high intracellular sodium and low potassium inside the muscle will promote wasting while the reverse situation will favor growth. So this is a very positive effect of GHB. Alone, it may not do much but used in synergy with anabolics, it will enhance their muscle building effects.

During a low calorie diet, potassium losses in urine are accelerated, depleting the body (and therefore our muscles) of its potassium. This phenomenon has been shown to contribute to the muscle catabolism experienced during low cal diets by increasing the overall acidosis. The potassium sparing action of GHB is therefore another advantage of this compound while on a diet.

Is GHB dangerous?

As all drugs, GHB is to be considered and handled with care. A minority of people will react very unexpectedly to it. So make sure it does not happen to you by using small doses first and build up from there. Of course, do not drive while under the influence of GHB. Needless to say that you do not want to use GHB along with alcohol or other street drugs.

To conclude, GHB is a very popular compound. It has some very useful effects for bodybuilders, especially while on a diet. This is probably not due to its well known and characterized effect on GH. But any serious bodybuilder will tell you he is much better off dieting with rather than without GHB, even if he does not have a clue about what GHB is doing and how it is working.

Bibliography:

1. Laborit H. (1974). Etude pharmacologique du glycolate de Gamma hydroxybutyrate d'éthyle. Agressologie. 15: p. 31.

2. Snead OC. (1977). Gamma-hydroxybutyrate. Life Sci. 20: p. 1935.

3. Cash CD. (1996). What is the role of the Gamma-hydroxybutyrate receptor? Med Hypothesis. 47: p. 455.

4. Laborit H. (1972). Correlations between protein and serotonin synthesis during various activities of the central nervous system (slow and desynchronized sleep, learning and memory, sexual activity, morphine tolerance, aggressiveness and pharmacological action of sodium Gamma-hydroxybutyrate. Res Com Chem Pathol Pharmacol. 3: p. 51.

5. Van Cauter E. (1997). Simultaneous stimulation of slow-wave sleep and growth hormone secretion by Gamma-hydroxybutyrate in normal young men. J Clin Invest. 100: p. 745.

6. Oyama T. (1964). Effect of Gamma-hydroxybutyrate on adrenocortical function. Agressologie. 8: p. 441.

7. Oyama T. (1972). Effect of Gamma-hydroxybutyrate anesthesia and surgery on plasma thyroid-stimulating hormone (TSH) and thyroxine levels in man. Agressologie. 13: p. 75.

8. Chateau J. (1987). Alcalose métabolique. Association de Gamma-hydroxybutyrate de sodium et d'hémisuccinate d'hydrocortisone. Cahiers Anesthéol. 35: p. 571.