 |
|
|
|
|
|
|
|
|
|
|
|
|
 |
|
|||||||||||
 |
 |
 |
 |
 |
 |
 |
 |
 |
 |
 |
 |
|
 |
 |
 |
 |
 |
 |
|
||||||
 |
 |
 |
 |
 |
 |
|
||||||
 |
 |
 |
 |
 |
 |
|
||||||
Explaining Differences Between RenewTrient,
SomatoPro, And Other GHB Precursors
by Ward Dean, M.D.
Many people (including physicians) have discovered that gamma hydroxy
butyric acid (GHB) is not the dangerous, highly toxic "designer"
date-rape drug the media and government want us to believe. These people
who have responsibly used GHB have found it to be one of the most beneficial
substances known. GHB occurs naturally in every mammalian cell, and is
a vital metabolite in the body’s energy-producing system, the Krebs’
cycle (Fig. 1). GHB has neurotransmitter functions as well. When ingested,
it is metabolized harmlessly into carbon dioxide and water.
GHB’s most common use is as a safe, non-toxic, rarely-addictive relaxant and sleep-inducing agent. Other benefits of GHB include lowering cholesterol, alleviating pain of diabetic peripheral neuropathy, and reducing oxygen requirements of the heart and brain. It has been used successfully in the treatment of reflex sympathetic dystrophy (RDS), chronic fatigue, fibromyalgia, schizophrenia, Parkinson’s disease, depression, anxiety, migraine headaches, and many other chronic conditions. It is also a powerful growth hormone stimulant, with many users reporting loss of body fat and modest increase in muscle mass.
However, just as its numerous benefits were coming to be widely known, the federal government began prosecuting manufacturers and distributors of GHB under questionable interpretations of the law. They also promoted its being labeled by the media as "the date rape drug." To solidify their weak legal position, the FDA and DEA began influencing state legislatures to enact laws to criminalize GHB at the state level. At the time this is written (September, 1999), over twenty states have "scheduled" GHB as a controlled substance, with possession being a felony.
Because of government pressure, the supply of legitimate commercial GHB manufacturers declined. As sources for GHB dried up, manufacturers searched for ways to continue to legally provide the benefits of GHB to the public. Fortunately, the scientific literature was replete with obscure studies on GHB and its precursors (substances which can be converted into another substance). These scientific articles described several GHB precursors, and confirmed that they, too, were natural substances contained in foods and in our bodies. The literature also confirmed the safety of these substances, as well as contained descriptions of their clinical effects.
Consequently, just as the availability of GHB declined, a number of products began to appear in gyms and health food stores, and were offered on the internet—all claiming to produce the same effects as GHB—but which did not contain GHB as an ingredient!
GHB Precursors
These non-GHB-containing products generally contain one of two industrial solvents as their active ingredients. These substances—1,4-butanediol (BD) and gamma butyrolactone (GBL)—are known by a dizzying number of names (see box). BD and GBL have wide applications in industry, and are essential in the manufacture of a number of other chemicals, and in the plastics industry. Incredible as it seems, these "industrial chemicals" (1) occur naturally in our bodies, (2) are virtually non-toxic, and (3) convert completely and rapidly into GHB after ingestion.
Although the effects of these two substances (and the products that contain them) are very similar, because they all ultimately convert into GHB, there are subtle differences in their activities, and in their conversion pathways. Users of these products should be aware of these differences. This article explains these differences.
1, 4-Butanediol (BD)
Butanediol is a "diol lipid" neutral fat found naturally in yeast, corn, and rat liver (Bergelsen, et al, 1966). BD has numerous industrial applications, particularly in the plastics industry where it is used in the manufacture of polyurethanes, and in the synthesis of the plasma expander polyvinylpyrrolidone.
Scientists found that the enzyme alcohol dehydrogenase—the same enzyme the body uses to metabolize alcohol—converts BD into GHB (Fig. 2). Consequently, ingestion of BD results in sedation, euphoria, and other effects—just like GHB! (no kidding). A principal difference between the two substances is that the sleep induction time (i.e., the time from the ingestion of a sleep-inducing dose until the onset of sleep) is almost twice as long for BD compared to GHB. However, the duration of sleep induced by BD is longer than GHB (GHB has a tendency to "snap" people awake in the middle of the night, due to its short half life). BD is like "timed release" GHB.
1, 4, Butanediol (BD): aka tetramethylene
glycol; butylene glycol; tetramethylene 1, 4-diol; 1,44-dihydroxybutane.
SomatoPro
Revitalize Plus
Serenity
Enliven
GHRE
NRG3
Thunder Nectar
Weight Belt Cleaner
Also: Cherry fX Bombs, Lemon fX Bombs, Orange fX Rush (These last 3 products
also contain other unknown (by me) ingredients).
Unfortunately, people who do not tolerate alcohol well, or who become inebriated on very small amounts of alcohol will not benefit from BD, because they lack adequate concentrations of the enzyme (alcohol dehydrogenase) to efficiently convert BD to GHB. Examples of people who may not benefit from BD include many women (because women generally have lower concentrations of alcohol dehydrogenase in their blood) and some races like Asians, Eskimos, and American Indians (again, because of low levels of alcohol dehydrogenase). These groups have higher percentages of people with low levels of AD. Also, because BD and alcohol use this same enzyme for their metabolism, BD-containing products should definitely not be combined with alcohol, due to the blockade of conversion to GHB and accumulation of BD (Poldrugo and Snead, 1984), and increased likelihood of fatty liver (Bessman and McCabe, 1972). Furthermore, the effects of any BD that did convert to GHB would be potentiated by the alcohol.
BD appears to be extremely safe. For example, scientists who conducted toxicological studies on animals with BD which lasted as long as two years stated that the "toxicological profile of 1, 4 butanediol reflects that of gamma hydroxybutyric acid…No organ-specific toxicity occurred in the toxicology studies…. 1,4 butanediol should be considered not carcinogenic in animals [including humans] and no further evaluation of 1, 4 butanediol is needed…. [italics added]" (http://www.lycaeum.org/drugs/ synthetics/ghb/bdo.ghb.html)
Nevertheless, several congeners (a person or thing resembling another in nature or action) of BD are toxic. For example, 2-butene-1, 4-diol and 2-butyne-1, 4-diol can cause depression of motor activity, marked vasodilation of the extremities, profuse diarrhea, and even death. The butyne congener is about twice as toxic as the butene congener (Taberner and Pearce, 1974). Thus, although the safety of BD has been well established, it is important to verify the purity of the product. Any product manufactured by a responsible company will be glad to supply a certificate of analysis, verifying the purity of the product.
Gamma Butyrolactone (GBL)
Gamma-butyrolactone (GBL) is another GHB precursor. Although GBL is known by many names (see box), it is usually listed on these dietary supplements as 2(3)-furanone dihydro. 2(3)-furanone dihydro is actually an archaic chemical name for GBL. GBL is used industrially as an engine degreaser, paint stripper and solvent. In addition to its extensive use in industry, food grade and pharmaceutical grade GBL is also widely used in a number of products ultimately intended for human ingestion or infusion. Two of these are as a blood plasma extender and as a clarifying agent in beer and wine. Thus, despite the unappetizing thought of consuming "the active ingredient in engine degreaser," GBL is an extremely safe and potentially highly beneficial substance with industrial, dietary and pharmaceutical uses.
Gamma butyrolactone (GBL): aka
2(3H) furanone dyhydro; 1, 2-butaneolide, 4-hydroxybutanoic acid lactone;
4-deoxytetronic acid; tetrahydro-2-furanone, and others.
RenewTrient
Longevity
Revivarant
G.H. Revitalizer
Gamma G, Blue Nitro
Insom-X
Remforce
Firewater
Invigorate
GBL, like BD, is rapidly and completely absorbed into the bloodstream, and then converts to GHB via the enzyme lactonase (Fig. 2). GBL causes a more rapid induction of sleep than GHB, and a more prolonged sleep than GHB (Sprince, et al, 1966). Consequently, those who are bothered by the short (usually 3-4 hours) sleep duration and early-awakening characteristics of GHB may prefer either GBL or BD.
The safety of GBL has been well established. In an article on a now-unreachable government website, I found a report of GBL toxicity studies which lasted two years. In these studies, extremely high doses of GBL were administered to rats and mice of both sexes five days per week, via gavage feeding (i.e., stomach tubes). Female rats were administered doses of 450 mg/kg, male rats received 225 mg/kg, and male and female mice received 525 mg/kg. These doses were as much as ten times higher than equivalent, sleep-inducing doses in humans.
The results of the study revealed some surprising effects. Among the findings: Male rats receiving GBL showed a slightly higher survival rate. This effect was attributed to a lower incidence of mononuclear cell leukemia. There was no change in survival of the female rats, but female dosed rats had lower incidences of mammary gland cysts and tumors. Additionally, liver tumors were decreased in both male and female mice. At the end of the study, the mean body weights of dosed mice (both male and female) were lower than the controls. This finding is consistent with the frequent reports of weight loss reported by human GBL consumers!
The overall conclusions of this study are that GBL in extremely high doses is exceptionally safe, actually reduces the incidence of leukemia and mammary and hepatic tumors, and extends the lifespan of male rats. Thus, GBL is an extremely safe substance with a number of unique benefits for human health.
BD/GHB/GBL Cautions
As with BD, it is important to avoid combining GHB or GBL with alcohol, tranquilizers, sleeping pills, depressants, sedatives, or barbiturates, as the depressive effects may be additive. As a precaution, people should inform those around them that they are taking GBL or GHB, and therefore may be unarousable for several hours.
There have been instances where people have been inappropriately taken to an emergency room when their friends found them unconscious and unarousable, and assumed they were in danger. These individuals invariably woke up about three hours later, wondering where they were and why all these strange people were doing things to them. Unless other drugs or alcohol have been consumed with these substances, the only treatment necessary is to allow the sleeping person to wake up naturally.
Conclusion
I believe that GHB/GBL/BD-containing dietary supplements are among the most beneficial substances known to man. These products are effective in alleviating a wide variety of conditions, as well as enhancing sleep and overall quality of life for people of all ages. But like many other beneficial substances, they must be used wisely and judiciously. I strongly recommend that people be knowledgeable about all substances they take. If one is looking primarily for a safe relaxant and long-term sleep-inducing agent, BD would be the first choice. Alternately, those seeking short-term sleep effects, or who are genetically predisposed to low levels of alcohol dehydrogenase, including women, GBL would be the preferred choice. For more in-depth information I recommend my book, GHB-The Natural Mood Enhancer (or the forthcoming, Therapeutic Benefits of GHB) as a primer on the benefits, cautions, history and politics regarding this much-maligned but very safe and beneficial substance.
References
1. Bergelson, L.D., Vaver, V.A., Prokazova, N.V., Ushakov, A.N., and Popkova, G.A. Diol lipids. Biochimica et Biophysica Acta, 1966, 116: 511-520.
2. Bessman, Samuel P., and McCabe, Edward R.B. 1,4-butanediol—A substrate for rat liver and horse liver alcohol dehydrogenases. Biochemical Pharmacology, 1972, 21: 1135-1142.
3. NTP summary report on the metabolism, disposition and toxicity of 1,4 butanediol.(http://www.lycaeum.org/drugs/synthetics/ghb/bdo.ghb.html)
4. Lettieri, John, and Fung, Ho-Leung. Improved pharmacological activity via pro-drug modification: Comparative pharmacokinetics of sodium gamma-hydroxybutyrate and gamma butyrolactone. Research Communications in Chemical Pathology and Pharmacology, 1978, 22: 1, 107-118.
5. Poldrugo, Flavio, and Snead, O. Carter. 1, 4 butanediol, gamma hydrocybutyric acid, and ethanol. Relationships and interactions. Neuropharmacology, 1984, 23: 1, 109-113.
6. Roth, R.H., and Giarman, N.J. Evidence that central nervous system depression by 1, 4-butanediol is mediated through a metabolite, gamma-hydroxybutyrate. Biochemical Pharmacology, 1968, 17: 735-759.
7. Roth, Robert H., Giarman, Nicholas J. Con-version in vivo of gamma aminobutyric acid in the rat. Biochemical Pharmacology, 1969, 18: 247-250.
8. Sprince, Herbert, Josephs, Joseph A., and Wilpizeski, Chester R. Neuorpharmacological effects of 1, 4-butanediol and related congeners compared with those of gamma-hydroxybutyrate and gamma-butyrolactone. Life Sciences, 1966, 5: 2041-2052.
9. Taberner, P.V., and Pearce, M.J. Hypothermic and toxic actions of 2-butyne-1, 4-diol and other related diols in the rat. J. Pharm. Pharmac., 1974, 26: 597-604.
GHB Articles by Dr. Ward Dean
