Smart Drug Update:

The Emergence of GHB Alternatives

One of the things I predicted, in the face of the government’s war on GHB, was that alternatives would quickly emerge into the marketplace. GHB’s ubiquitous presence in foods of both animal and plant origin is a reflection of its universal and essential place in carbohydrate metabolism. The problem with any genuine attempt to suppress the use of GHB through coercion (i.e., force of law) is that all the related chemicals that can become converted into GHB must also eventually become suppressed. The folly of suppressing (i.e., criminalizing) an entire pathway of nutritional metabolism remains to be appreciated by lawmakers. The only historical analogy that can be used to draw a comparison is Prohibition, the “great experiment” to ban alcohol. Like GHB, alcohol is a ubiquitous metabolite of both plant and animal biochemistry. The abject failure of Prohibition by almost any standard of judgment should give us pause to consider the wisdom of trying to prohibit GHB, not to mention all its precursors and metabolites.

Consequences of Prohibition

Just as prohibition drove citizens to begin home-brewing their own alcoholic beverages, the FDA’s campaign of bureaucratic terrorism towards GHB has driven people to home-brew their own GHB. And just as Prohibition spawned the emergence of an entire “criminal” class devoted to “boot-legging” alcoholic beverages and distillates, people are now being arrested and prosecuted for selling GHB. The first police actions against people selling “GHB kits” (the GHB precursor butyrolactone, packaged with the hydrolysis catalyst hydroxide) have recently taken place. As we reported in the last issue, A Pure Source was raided by Florida police. This issue we report that Bond-Tech has been raided, also by Florida police. Presumably, the principals behind these companies are presently being threatened with felony prosecutions should they fail to assist authorities in “setting up” their fellow vendors, distributors and customers for further raids and arrests.

As the witch hunt for GHB is expanding, the marketplace is adapting. The gamma-butyrolactone that was being sold in premeasured kits (with easy directions for use), will now be sold as a high-purity solvent (without directions) which the FDA has only limited jurisdiction to regulate. Several GHB-like products have already emerged as dietary supplements and are being openly sold. RenewTrient (see report in last issue) contains butyrolactone, which hydrolyzes into GHB (see Figure.). The Revitalize Plus product label lists “fully reduced succinic semialdehyde,” a fancy-sounding and somewhat obscure description of the GHB precursor gamma-hydroxybutyraldehyde (GHB-aldehyde), which is rapidly oxidized into GHB by the human body (see Figure B). There are also new supplement products based on gamma-hydroxybutanol (i.e., 1,4-butanediol, or GHB-alcohol), another substance which is oxidized into GHB by the body. I have personally experimented with RenewTrient, gamma-butyrolactone, Revitalize Plus, and GHB-alcohol and found that all of them approximate the subjective GHB experience to a significant degree.

Despite the public spirited motivations of lawmakers to “help” people with their “GHB problems,” laws criminalizing GHB are only driving people toward the above GHB alternatives (GHB precursors). The wisdom of such a public policy, were it intentional and deliberate, is arguably negligent. Despite prohibitionist rhetoric about the “lethality” of this “designer, date-rape drug,” GHB is a fundamentally non-toxic substance which can easily be used safely with relatively simple labeling instructions that the average “reasonable man” has no problem understanding. Because the public policy driving people towards GHB alternatives is unintentional and deniable (“That’s not what we were trying to do!”), bad policy will probably be followed by more bad policy as lawmakers try to “fix” the problem they created — without losing face. This latter element makes it unlikely that GHB laws will ever be repealed by the people who enacted them. Face-saving also makes it impossible for lawmakers to tolerate GHB alternatives.

Gamma-Aminobutyrate

GABA (gamma-aminobutyrate) has been available in the dietary supplement market for many years. GABA is an inhibitory neurotransmitter whose receptors lower muscle tone, promote relaxation, diminish anxiety, and stimulate digestion. However, GABA is selectively rejected bythe blood-brain barrier. The effects of oral supplementation are limited primarily to peripheral (body) effects.

Excess GABA is quickly metabolized into succinic semialdehyde (see Figure B) by transfer of the GABA amino group to another molecule (transamination). Succinic semialdehyde can either be oxidized to succinic acid or reduced to GHB, depending on the metabolic needs of the body. GHB is able to cross the blood-brain barrier. Succinic acid goes into cellular energy production pathways (see Figure B).

GABA produces mild-to-moderate relaxation in doses from 500 mg to 2000 mg. It is usually sold in 500 mg capsules and tablets.

Gamma-Butyrolactone

Gamma-butyrolactone is an dehydrated form of GHB, normally present in only trivial amounts in aqueous (water) solutions at neutral pH (i.e., in biological fluids). At acidic pH, and in dry environments, the lactone is favored. In aqueous environments, GHB and butyrolactone are in equilibrium with each other, slowly converting back and forth (see Figure B). It may take days for this interconversion to reach equilibrium (i.e., when the rate of lactone hydrolysis into GHB equals the rate of GHB dehydration into lactone).

In concentrated form, gamma-butyrolactone is an greasy-feeling solvent with a characteristic, unpleasant smell. Dilute lactone solutions remind me of the smell of stale water that first comes out of a garden hose that has been baking in the sun all day. In other words, it’s not pleasant, but it is less objectionable than the average B vitamin.

I find butyrolactone to be significantly stronger than GHB in many respects. Sub-gram doses produce a strong GHB-like hypnotic effect. This effect may be slower in onset than GHB on an empty stomach, yet faster than GHB when taken after food. In other words, butyrolactone’s effect does not seem to be affected as much by food as does GHB’s effect. I have tried doses varying from 15 drops to 40 drops (28 drops equals 1 gram of lactone). 15 drops produces a mild sedative effect that helps me get to sleep, but can be resisted indefinitely when I am reading. The hypnotic effect from 40 drops is overpowering and produces similar vestibular effects (dizziness) immediately before falling asleep as does 2-3 grams of GHB. I do not experience much nausea from butyrolactone (or GHB), but I suspect that others might. My usual dose for getting to sleep is 20-25 drops.

One of butyrolactone’s advantages over GHB is its much longer duration of action. GHB is rapidly metabolized (within an hour of consumption), whereas butyrolactone is metabolized only after hydrolysis, which extends the sleep-inducing properties of butyrolactone. With GHB, I can wake up after only 3 hours of sleep. With butyrolactone, I never wake up with less than 6 hours of sleep, and usually 7-8 hours. It is also possible that the longer action of butyrolactone may become a liability with higher doses that are not fully cleared within the 6-8 hour sleep period. I felt a bit lethargic the morning after taking 40 drops, until I took my morning shower. I’d like to hear if other people notice this effect, or not.

Gamma-Hydroxybutyraldehyde

According to the label, Revitalize Plus contains “fully reduced succinic semialdehyde.” Since this is not a legitimate chemical name, I can only infer that it contains either 1)GHB (once-reduced succinic semialdehyde), 2) gamma-hydroxybutyraldehyde (twice-reduced succinic semialdehyde, or 3)gamma-hydroxybutanol (thrice-reduced succinic semialdehyde). Having been told verbally that it does not contain the first or third options, I am left with a presumption that it must contain gamma-hydroxybutyraldehyde (which I have not confirmed by analysis).

Generally, aldehydes oxidize into acids very readily. This means that hydroxybutyraldehyde readily oxidizes into GHB (see Figure B). Indeed, Revitalize Plus produces a strong GHB-like effect quite quickly. I tried about 3/4 fl. oz. the first night, which should have been about 1.5 grams of GHB once metabolized (oxidized). I slept quite well through the night. The next night, I tried 2 fl. oz. The effect was consistent with a much larger dose of GHB, with some mild nausea before falling asleep. I fell asleep rapidly. The next morning, I woke up at my usual time. However, I felt queasy. The queasiness got worse throughout the morning, and I began to have difficulty staying focused on my reading and writing. By the middle of the afternoon, I gave up and took a nap. It wasn’t until the next morning that I felt back to normal.

I cannot be sure that the Revitalize Plus was the source of my discomfort, but I felt bad enough to be unwilling to risk trying it again. I have concerns that the butyraldehyde may present some degree of aldehyde toxicity like that of acetaldehyde (the toxic metabolite of alcohol). Aldehydes are known to be active cross-linking agents (an anti-metabolic and pro-aging effect) and they may place undue stress on the antioxidant defense system (especially on reduced glutathione levels).

Based on my experience and these theoretical concerns, I can only caution readers to pay close attention to possible adverse effects from the use of this product. Anybody trying it, please let me know what you experience.

Gamma-Hydroxybutanol

Gamma-hydroxybutanol (GHB-OH) is a colorless oily liquid with a mild smell. It mixes with water at any concentration, but its syrupy consistency is slow to disperse. GHB-OH is also known as 4-hydroxybutanol, 1,4-butanediol, 1,4-butylenediol and tetramethylene glycol.

Like butyrolactone, GHB-OH is much more slowly metabolized than GHB. I find its hypnotic effect deep and powerful, lasting through the night, and maybe then some. I’ve tried doses of 10-30 drops (26 drops equal 1 gram), and the latter dose makes for a languorous waking up. Despite a general feeling of lassitude, I feel especially rested after having taken GHB-OH.

Commercial Applications

Widespread use of GHB precursors in commerce and industry will make them almost impossible to prohibit. Butyrolactone alone is distributed in tanker truck loads to many industries. It is used 1) to butylate pharmaceuticals and other chemicals, 2) to manufacture the amino acid methionine, 3) to manufacture polyvinylpyrrolidone (a polymer used to make PVP-iodine, blood plasma extenders, toothpaste, photographic films, adhesives, fabric finishes, cosmetics and skin-care products, and to clarify beer and wine), 4) in the manufacture of polystyrenes and acrylate polymers, 5) to clean metal parts of tars, oils, greases and varnishes, 6) to strip paints and varnishes, and 7) to process and finish textiles.

GHB-OH also has widespread industrial uses. It is used 1) as a solvent, 2) to make plasticizers and humectants (moisturizers), 3) to synthesize pharmaceuticals, 4) to make polyurethanes and terephthalate (polyester) polymers, 5) to manufacture industrial quantities of tetrahydrofuran, a major solvent and industrial chemical.

Call for Anecdotal Reports

Due to legal imperatives, people are beginning to use these GHB alternatives at a rapid pace. Research with these nutritional supplements is much less robust than with GHB. Caution is indicated. Should any of our readers try any of these products, please share your experiences with us. We’ll be glad to do an update on what we learn in a future issue.