Herbal Medicine -Gamma Butyrolactone
23 November 2007Common Trade Names
Blue Nitro, Firewater, Gamma G, GBL, GH Revitalizer, Insom-X, Invigorate, Longevity, Remforce, Renewtrient, Revivarant
Common Forms
Liquid and powder.
Source
Gamma butyrolactone occurs naturally in humans and decreases in concentration with age. Gamma hydroxybutyric acid (GHB) is converted to gamma butyrolactone in the stomach by gastric acid after oral administration. GHB is a short-chain fatty acid metabolite of gamma aminobutyric acid (GABA), which is found in all body tissues, with the highest concentration in the brain.
Chemical Components
Gamma butyrolactone is chemically related to both GHB and 1,4Âbutanediol (BD).
Actions
When ingested orally, gamma butyrolactone is converted to GHB in the stomach. GHB is distributed rapidly within the body and easily crosses the blood-brain barrier. It is then converted to succinic semialdehyde and then to succinic acid or, possibly, GABA by way of Krebs’ cycle. GHB is a naturally occurring inhibitory neurotransmitter and has the highest concentration in the basal ganglia. It is thought to be involved in sleep cycle mediation, temperature regulation, cerebral glucose metabolism and blood flow, memory, and emotion. At low doses, GHB decreases dopaminergic activity, and at high doses, it can stimulate dopamine release. Complete GHB function and metabolism are complex and incompletely understood.
Reported Uses
Many claims have been made for gamma butyrolactone. It has been promoted to induce sleep, enhance sexual activity, build muscle, release growth hormone, cause weight loss, and relieve depression and stress. No human clinical trials support these observations.
GHB is approved as an anesthetic in some countries, and FDA approval is pending for its use as an investigational drug to treat narcolepsy.
Dosage
No dosing regimen is available.
Adverse Reactions
CNS: aggression, agitation, amnesia, anxiety, CNS depression, coma, combativeness, confusion, euphoria, hypothermia, seizures, unconsciousness.
CV: bradycardia, tachycardia.
GI: vomiting.
Musculoskeletal: hypotonia, myoclonus.
Respiratory: slow respiratory rate.
Skin: sweating.
Interactions
Alcohol: Increased effects of alcohol. Avoid administration with gamma butyrolactone.
CNS depressants: Increased effects of CNS depressants. Avoid administration with gamma butyrolactone.
Contraindications And Precautions
Gamma butyrolactone is considered unsafe. The use of products that contain gamma butyrolactone has been associated with more than 55 cases of serious adverse reactions and at least 1 death. Together, gamma butyrolactone, GHB, and BD account for more than 122 case reports of serious illnesses and at least 3 deaths reported to the FDA.
Special onsiderations
Alert On March 13,2000, GHB was classified by the FDA as a Schedule I controlled substance. Because gamma butyrolactone is a precursor to GHB, according to the FDA, it can be treated as a Schedule I controlled substance if it is intended for human consumption.
On January 21,1999, the FDA issued a warning about products that contain gamma butyrolactone and asked manufacturers to issue a recall. This action was initiated because of the emergence of GHB and gamma butyrolactone as drugs of abuse, most notably as “date rape” drugs, because of their euphoric and sedative effects.
Gamma butyrolactone has been advertised on the Internet and in health food stores and bodybuilding magazines. With the FDA implications, manufacturers have been renaming their products and substituting BD for gamma butyrolactone. Ingesting this drug can be just as dangerous as ingesting gamma butyrolactone and produces the same serious adverse effects. There have also been reports of potential GHB abusers making their own product by mixing gamma butyrolactone, water, and sodium hydroxide. This type of “kitchen chemistry” is popular among adolescents and young adults and can lead to serious injury because of the unknown amount of each ingredient.
Alert Gamma butyrolactone is associated with many of the same adverse effects as GHB. Comatose events and at least one death have been documented with the use of gamma butyrolactone. Effects of GHB are dose-related, with short-term amnesia and hypotonia at
10 mg/kg; drowsiness and sleep at 20 to 30 mg/kg; and bradycardia, bradypnea, a hypnotic state, nausea, and vomiting at 50 to 70 mg/kg. Higher doses cause seizures and cardiopulmonary depression. Adverse reactions usually resolve within 4 to 6 hours but may take 3 to 4 days. Supportive treatment with a focus on airway protection is recommended for GHB toxicity. One study advocates the use of physostigmine, 2 mg I.V., as an antidote for GHB .
Points of Interest
Gamma butyrolactone, as a solvent, can be used in the production of pesticides, herbicides, and plant growth regulators. It is also an ingredient in commercial floor strippers. This solvent can be combined with water and sodium hydroxide to create GHB.
Commentary
Few studies have been conducted on the use of gamma butyrolactone in humans. GHB has been investigated and found to be unsafe in the public forum. Although the FDA has allowed GHB to have investigational status, it is still considered an unapproved and illegal drug. Because gamma butyrolactone is a precursor to GHB, it has been given the same restrictions. Gamma butyrolactone, GHB, and BD cannot be recommended for any use. Because of the multiple case reports of serious injury and even death, it is best to avoid these dietary supplements.
Tagged under:body tissues, gamma aminobutyric acid, gamma butyrolactone, gamma hydroxybutyric acid, Herbal Medicines, hypothermia stomach
