 |
|
|
|
|
|
|
|
|
|
|
|
|
 |
|
|||||||||||
 |
 |
 |
 |
 |
 |
 |
 |
 |
 |
 |
 |
|
 |
 |
 |
 |
 |
 |
|
||||||
 |
 |
 |
 |
 |
 |
|
||||||
 |
 |
 |
 |
 |
 |
|
||||||
"Blue Nitro" - An Explosive Media Campaign
This article first appeared
in the February 1999 issue of Vitamin
Research News
Media Campaign by Ward Dean, M.D
"Blue Nitro Worries Poison Experts" screamed the headline of
the San Francisco Examiner on Monday, January 11. The active ingredient
in Blue Nitro is butyrolactone (GBL), which is readily converted by the
body into GHB (gamma hydroxybutyric acid). The same article states, "Medical
professionals are warning that the chemical composition of the liquid
creates more risks than benefits." Although this is the view of GBL
propagated by the media, there is another view that has a much more positive
outlook.
On November 2nd, 1999, the Attorney General of Florida issued an "Emergency Order" which declared "isomers, esters, ethers, salt isomers and ethers of GHB" (which included GBL) were classed as controlled substance (Schedule II) in Florida. Subsequently, law enforcement officers raided manufacturers of GBL-containing nutritional supplements in Florida.
While this broad (overly broad, we believe) edict includes substances like RenewTrient, it also includes gasoline, paint thinner, nail polish remover, polyester and even apples. However, so far this far-reaching provision has only been selectively applied in Florida against manufacturers of GBL-containing nutritional supplements.
[We suggest you contact your state legislators to encourage them to vote against any pending legislation to further restrict sales of these beneficial dietary supplements.]
Recently, a number of popular over the counter GHB-precursor supplements have been introduced, such as BlueNitro and Olympia Nutrition’s RenewTrient. These products share the same active ingredient, usually listed as 2(3)-furanone dihydro-. 2(3)-furanone dihydro- is actually an archaic chemical name for the commonly known solvent, gamma-butyrolactone (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.
When discussing solvents and human health, we should also keep in mind that a number of "solvents" have beneficial dietary and therapeutic uses. Life itself could not exist without copious amounts of a solvent used for countless industrial and human applications—the "universal solvent" oxygen di-hydro, better known as water. Also, when considering the safety of consuming "paint stripper," think of another "industrial solvent"-di-methyl-sulfoxide (DMSO).
DMSO, a by-product of the paper-making industry, is a solvent that is helpful for many conditions and is also widely sold in many health food stores. DMSO exerts powerful anti-inflammatory and pain-relieving actions. Because DMSO is able to rapidly penetrate the skin and be absorbed into the body, it can reach areas that are hard to treat by other means.
Because of its safety and range of benefits, it is not such a great leap to consider moving from the topical use of DMSO to using it intravenously and orally as alternate means of getting it into the body. For example, to treat systemic arthritis involving multiple joints, I recommend that my patients consume about one teaspoon per day. (In orange juice, it’s really not that bad). DMSO is extremely safe.
Legality and Safety of GBL
Like DMSO, GBL has many beneficial effects and is equally safe. GBL is converted rapidly and completely by the body into GHB by the enzyme lactonase (Fig. 1). Thus, products like RenewTrient are legal in nearly all states even where GHB has been made a controlled substance.
But what about its safety? Frankly, I had the same question. I had the same aversion to drinking "paint thinner" as everyone else. The answer, it turns out, lay in a mind-boggling article I found on the internet, from, of all places, a U.S. government web site (http://ntp-server.niehs.nih.gov/htdocsLT-Studies/TR406.html) (I understand that the article can no longer be found there!) The article described studies lasting two years, in which 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 is 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, despite any initial concerns, GBL is an extremely safe substance with a number of unique benefits for human health.
Benefits of GBL - Safe, Natural Sleep
The most common use of GHB (and GBL) is as a safe, non-toxic, non-addictive sleep-inducing agent. In lower doses, rather than leading to sleep, these substances induce a mild euphoric state, much like a glass or two of wine. Unlike alcohol, however, which may damage brain and liver cells and produce free radical-generating toxins (acetaldehyde), GHB is cleanly metabolized (via the Krebs cycle) into carbon dioxide and water.
There are absolutely no toxic or addictive metabolites. And, while GHB is being metabolized, it is converted into succinates, which actually enhance body metabolism. Consequently, when any dose of GHB wears off, instead of feeling "drugged," the person is alert and refreshed.
Clinical Conditions
Some of the clinical conditions for which GHB has been used include narcolepsy, depression, anxiety, schizophrenia, Parkinson’s disease, ADD, fibromyalgia, and alcohol and opiate withdrawal. I believe it is also the substance of choice for a wide variety of chronic pain syndromes, including peripheral neuropathy, phantom limb syndrome, neuralgia from nerve root involvement, trigeminal neuralgia, and migraine headaches.
Other effects of GHB include normalization of abnormal EKGs, reduction of cholesterol, reduction of brain and heart oxygen requirements (thereby potentially reducing the risk of strokes and heart attacks), and stimulation of growth hormone release. I believe it is the combination of growth hormone release and enhancement of metabolism that results in the weight loss that many GHB users experience. Although all of the previous clinical effects are well documented for GHB, the same results will be experienced by GBL users because of its rapid and complete conversion into GHB in the body.
Differences in effects between GHB and GBL
Oral GBL is rapidly converted into GHB. Over half of a consumed dose of GBL is converted into GHB in less than one minute! GBL is also absorbed much faster than GHB, and appears to have even greater activity than when GHB is consumed directly.1 Blood plasma concentrations of GHB rise faster and remain elevated longer when GBL is administered, compared with an equal dose of GHB (Fig. 2). This longer action of GBL often prevents the early awakening which frequently occurs with GHB. Consequently, GBL has been considered by some to be almost a "timed-release" form of GHB.
How to use GBL (RenewTrient)
Most GBL products, like RenewTrient, have a pre-measured cap for administering sleep-inducing doses. However, like many other products, there is an individual variability in the effects that GBL has on different people. Therefore, I always advise people just starting to try GBL to start with a low dose, usually not more than a teaspoonful, and then increase the dosage as tolerated.
Most people find that extremely low doses have both an energy-producing as well as a mood-enhancing effect. At low doses, many people report improved performance. A slightly higher dose causes a mild euphoria. A dose of one ounce (more or less) normally induces a sound, restful sleep. If awakening occurs in the middle of the night, I recommend repeating the dose to return to sleep. GHB greatly enhances the depth and efficiency of stage III and IV sleep which results in a significant elevation of growth hormone release.
GHB/GBL Cautions
It is important to avoid combining GHB or GBL with alcohol, tranquilizers, sleeping pills, depressants, sedatives, or barbiturates, as the depressive effects may be addictive. 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.
I believe that GHB/GBL is one of the most beneficial substances known to man. It is 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, it must be used wisely and judiciously. I strongly recommend that people be knowledgeable about all substances they take. Consequently, I recommend my book, GHB-The Natural Mood Enhancer, as a primer on the benefits, cautions, history and politics regarding this much-maligned but very safe and beneficial substance.
References
1.Lettieri, John, and Fung Improved pharmacological activity via pro-drug modification: Comparative pharmacokinetics of sodium gamma-hydroxybutyrate and gamma butyrolactone. Research Communications in Chemical Pathology and Pharmacology, Vol 22, No. 1, October 1978, 107-117.
2.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, Vol 17, 735-759.
GHB Articles by Dr. Ward Dean
