Skip to content

Gamma hydroxybutyric acid

Gammahydroxybutyrate(GHB) is a chemical found in the brain and other areas of the body. Gamma hydroxybutyrate can also be produced synthetically in the laboratory. GHB used to be available in the US as a dietary supplement, but it was taken off the market in 1990 due to safety concerns. GHB and two closely related chemicals, gamma butyrolactone(GBL) and butanediol (BD), have been linked to 3 deaths and 122 cases of serious side effects. Despite this, clandestine production and sales continued. Continued interest may have been fueled by GHB's reputation as a so-called date rape drug. In 2000, GHB was defined as a Class 1 controlled substance under the Date Rape Drug Prohibition Act in the US, placing it in the same legal category as heroin and other hard drugs. Although the manufacture, sale and possession of GHB is prohibited in the US, a prescription form of GHB is still available.

GHB is used to support weight loss and muscle building, as well as to relieve symptoms of fibromyalgia including pain, fatigue and sleep problems. It is also used as an alternative to L-tryptophan to promote relaxation and sleepiness. People who have been addicted to alcohol or drugs sometimes use GHB to control their withdrawal symptoms. In addition, GHB is used to promote sexual arousal. The prescription form of GHB is approved to treat narcolepsy, a sleep disorder caused by the brain's inability to control the sleep-wake cycle. People suffering from narcolepsy experience uncontrollable bouts of sleep during the day, as well as problems controlling their muscles, paralysis and hallucinations. Doctors also use GHB intravenously to relieve pain and reduce pressure in the head after a head injury.

How does GHB work?

The natural function of GHB in the body may be to slow down brain activity during sleep. Gamma hydroxybutyrate affects several neural pathways in the brain, which include the pain relief system and increasing growth hormone levels.

How effective is GHB?

Gamma hydroxybutyrate may be effective in treating loss of muscle control and weakness associated with narcolepsy. Taking GHB appears to help people suffering from narcolepsy sleep at night, making them feel less sleepy during the day. GHB also appears to help reduce temporary paralysis symptoms that occasionally occur in narcolepsy patients. GHB may also be effective for pain and sleep problems associated with fibromyalgia, as well as in supporting alcohol withdrawal and suppressing withdrawal symptoms from heroin, opium or morphine withdrawal. There is insufficient scientific data to make a statement regarding the effectiveness of GHB when used to reduce body weight, increase muscle growth, stimulate sexual arousal and reduce blood pressure in the brain following head injury. Further scientific research is needed to evaluate the effectiveness of GHB in these applications.

Safety and side effects

The prescription drug gamma hydroxybutyrate is potentially safe and safe for adults when used under close medical supervision for the treatment of narcolepsy. The use of gamma hydroxybutyrate (GHB) as a dietary supplement is not safe and is also illegal. The use of gamma hydroxybutyrate or the closely related drugs gamma butyrolactone (GBL) and butanediol (BD) has been linked to at least 3 deaths and 122 cases of serious side effects.

GHB can cause serious side effects including headache, hallucinations, drowsiness, confusion, nausea, vomiting, agitation, diarrhea, sexual arousal, leg numbness, vision problems, mental changes, argumentativeness, memory loss, chest tightness, serious breathing and heart problems, seizures, coma and death. GHB can be addictive. Long-term use of gamma butyrolactone can lead to withdrawal symptoms serious enough to require inpatient hospitalization. GHB has some serious interactions with prescription medications.

Precautions and warnings

Pregnancy and lactation: GHB is not safe or safe to use during pregnancy and lactation. It has been associated with life-threatening side effects.

Slow heartbeat: GHB should be avoided as it can cause a slow heartbeat.

Epilepsy: GHB could cause epileptic seizures in people with epilepsy.

High blood pressure: GHB could increase blood pressure and should therefore be avoided by people who suffer from high blood pressure.

Surgeries: GHB can affect the central nervous system. There are concerns that a combination of GHB may cause excessive drowsiness when combined with anesthetics and other nervous system numbing drugs used during surgery. For this reason, the use of GHB should be discontinued at least 2 weeks before planned surgery.

Interactions

Gamma hydroxybutyrate should not be taken in conjunction with the following drugs and substances:

Alcohol

Alcohol can cause drowsiness and dizziness. Taking GHB in combination with alcohol could significantly increase the drowsiness and dizziness caused by alcohol and lead to serious side effects. For this reason, GHB should not be used if you have been drinking alcohol.

Amphetamines

Amphetamines are active substances that can accelerate the function of the nervous system. GHB can slow down the function of the nervous system. Taking GHB in combination with amphetamines can lead to serious side effects.

Medication for mental disorders (antipsychotic agents)

GHB can affect the brain. Certain medications for mental disorders can also affect the brain. Taking GHB in conjunction with these medications could increase the effects and side effects of GHB. For this reason, GHB should not be used if you are taking medication for mental disorders.

Anticonvulsant medications

Anticonvulsant medications affect chemicals in the brain. GHB is converted in the body into one of these brain chemicals called GABA. Taking GHB with anticonvulsant medications could reduce the effects of GHB.

Muscle relaxants

Muscle relaxants can cause drowsiness. GHB can also cause drowsiness. Taking GHB in combination with muscle relaxants can cause excessive drowsiness and serious side effects. For this reason, GHB should not be used when taking muscle relaxants.

Naloxone

GHB can affect the brain. Taking naxolone in combination with GHB could reduce the effects of GHB on the brain.

Sedatives (benzodiazepines and CNS suppressants): GHB can cause drowsiness and dizziness. Drugs that cause drowsiness are called sedatives. Taking GHB in combination with sedatives can cause serious side effects, so GHB should not be used if you are taking sedatives.

Medications for pain (narcotics): Some pain medications can cause drowsiness and dizziness. GHB could also cause drowsiness and dizziness. Taking GHB in combination with some pain medications can lead to serious side effects. For this reason, GHB should not be used when taking pain medication.

Dosage

The following dosages have been investigated in scientific studies:

Oral

  • For narcolepsy and its symptoms: A dose of 25 mg per kilogram of body weight was taken at bedtime and 3 hours later. GHB should only be used under intensive medical supervision.
  • For the treatment of alcohol dependence: 50 to 150 mg per kilogram of body weight divided into 3 to 6 single doses were used per day.

References

  1. Addolorato G, Cibin M, Caprista E, et al. Maintaining abstinence from alcohol with gamma hydroxybutyric acid. [Lancet 1998;351:38.
  2. Anon. FDA alert on misuse of consumer products containing GHB, GBL and BD. Food and Drug Administration, Rockville, MD. June 15, 1999. available at: http://www.fda.gov/cder/graphics/ghb.gif
  3. Anon. Important message for health professionals: Report serious adverse events associated with dietary supplements containing GBL, GHB or BD. Food and Drug Administration, Rockville, MD. August 25, 1999. available at: http://vm.cfsan.fda.gov/~dms/mwgblghb.html
  4. Anon. Multistate outbreak of poisonings associated with illicit use of gamma hydroxy butyrate. JAMA 1991;265:447-8.
  5. Broughton R, Mamelak M. The treatment of narcolepsy-cataplexy with nocturnal gamma-hydroxybutyrate. Can J Neurol Sci 1979;6:1-6.
  6. Cash CD. Gamma-hydroxybutyrate: an overview of the pros and cons for it being a neurotransmitter and/or a useful therapeutic agent (abstract). Neurosci Biobehav Rev 1994;18:291-304.
  7. Cash CD. What is the role of the gamma-hydroxybutyrate receptor? Med Hypotheses 1996;47:455-9.
  8. Dyer J, Roth B, Hyma B. Gamma-hydroxybutyrate withdrawal syndrome. Ann Emerg Med 2001;37:147-53.
  9. Dyer JE. Gamma-hydroxybutyrate: a health-food product producing coma and seizure-like activity (abstract). Am J Emerg Med 1991;9:321-4.
  10. FDA Talk Paper. FDA Warns About GBL-Related Products. 1999. available at: vm.cfsan.fda.gov/~lrd/tpgbl2.html
  11. FDA Talk Paper. FDA Approves Xyrem for Cataplexy Attacks in Patients with Narcolepsy. Issued July 17, 2002. Availbale at: http://www.fda.gov/bbs/topics/ANSWERS/2002/ANS01157.html
  12. Feigenbaum JJ, Howard SG. Gamma hydroxybutyrate is not a GABA agonist (abstract). Prog Neurobiol 1996;50:1-7.
  13. Ferrara SD, Tedeschi L, Frison G, Rossi A. Fatality due to gamma-hydroxybutyric acid (GHB) and heroin intoxication. J Forensic Sci 1995;40:501-4.
  14. Gallimberti L, Canton G, Gentile N, et al. Gamma-hydroxybutyric acid for treatment of alcohol withdrawal syndrome. Lancet 1989;2:787-9.
  15. Gallimberti L, Cibin M, Pagnin P, et al. Gamma-hydroxybutyric acid for treatment of opiate withdrawal syndrome. Neuropsychopharmacology 1993;9:77-81.
  16. Gallimberti L, Ferri M, Ferrara SD, et al. Gamma-hydroxybutyric acid in the treatment of alcohol dependence: a double-blind study. Alcohol Clin Exp Res 1992;16:673-6.
  17. Gallimberti L, Schifano F, Forza G, et al. Clinical efficacy of gamma-hydroxybutyric acid in treatment of opiate withdrawal. Eur Arch Psychiatry Clin Neurosci 1994;244:113-4.
  18. Galloway GP, Frederick SL, Staggers FE Jr, et al. Gamma-hydroxybutyrate: an emerging drug of abuse that causes physical dependence. Addiction 1997;92:89-96.
  19. Gerra G, Caccavari R, Fontanesi B, et al. Naloxone and metergoline effects on growth hormone response to gamma-hydroxybutyric acid. Int Clin Psychopharmacol 1995;10:245-50.
  20. Harrington RD, Woodward JA, Hooton TM, et al. Life-threatening interactions between HIV-1 protease inhibitors and the illicit drugs MDMA and gamma-hydroxybutyrate. Arch Intern Med 1999;159:2221-4.
  21. Hillory J. Farias and Samantha Reid date-rape drug prohibition act of 2000. 106th Congress of the United States of America. HR 2130.
  22. Hoes MJ, Vree TB, Guelen PJ. Gamma-hydroxybutyric acid as hypnotic. Clinical and pharmacokinetic evaluation of gamma-hydroxybutyric acid as hypnotic in man. Encephale 1980;6:93-9.
  23. Ingels M, Rangan C, Bellezzo J, Clark R. Coma and respiratory depression following the ingestion of GHB and its precursors: Three cases. J Emerg Med 2000;19:47-50.
  24. Kalra MA, Hart LL. Gammahydroxybutyrate in narcolepsy. Ann Pharmacother 1992;26:647-8.
  25. Maitre M. The gamma-hydroxybutyrate signaling system in brain: organization and functional implications (abstract). Prog Neurobiol 1997;51:337-61.
  26. Mamelak M. Gammahydroxybutyrate: an endogenous regulator of energy metabolism (abstract). Neurosci Biobehav Rev 1989;13:187-98.
  27. Mason P, Kerns II W. Gamma Hydroxybutyric Acid (GHB) Intoxication. Acad Emerg Med 2002;9:730-39.
  28. Otto A. Acquaintance rape drug may one day help instead of hurt (news). Pharmacy Today. American Pharmaceutical Association, Washington, DC. April 2000:17.
  29. Price G. In-patient detoxification after GHB dependence. Br J Psychiatry 2000;177:181.
  30. Scharf MB, Brown D, Woods M, et al. The effects and effectiveness of gamma-hydroxybutyrate in patients with narcolepsy. J Clin Psychiatry 1985;46:222-5.
  31. Scharf MB, Hauck M, Stover R, et al. Effect of gamma-hydroxybutyrate on pain, fatigue, and the alpha sleep anomaly in patients with fibromyalgia. Preliminary report. J Rheumatol 1998;25:1986-90.
  32. Scrima L, Hartman PG, Johnson FH Jr, et al. The effects of gamma-hydroxybutyrate on the sleep of narcolepsy patients: a double-blind study. Sleep 1990;13:479-90.
  33. Scrima L, Hartman PG, Johnson FH Jr, Hiller FC. Efficacy of gamma-hydroxybutyrate versus placebo in treating narcolepsy-cataplexy: double-blind subjective measures. Biol Psychiatry 1989;26:331-43.
  34. Smith KM. Drugs used in acquaintance rape. J Am Pharm Assoc 1999;39:519-25.
  35. Timby N, Eriksson A. Gamma-hydroxybutyrate-associated deaths. Am J Med 2000;108:518.
  36. Tunnicliff G. Significance of gamma-hydroxybutyric acid in the brain. Gen Pharmacol 1992;23:1027-34.
  37. Tunnicliff, G. Sites of action of gamma-hydroxybutyrate (GHB)-a neuroactive drug with abuse potential. J Toxicol Clin Toxicol 1997;35:581-90.
  38. Van Cauter E, Plat L, Scharf MB, et al. Simultaneous stimulation of slow-wave sleep and growth hormone secretion by gamma-hydroxybutyrate in normal young Men (abstract). J Clin Invest 1997;100:745-53.