Also known as 4-hydroxybutyric acid, gamma-Hydroxybutyric acid is a neurotransmitter and a depressant. It is a precursor to the amino acids glutamate, glycine, and gamma-aminobutyric acid (GABA). It can act as a weak agonist of the GHB receptor.
GHB is a depressant that can act on the central nervous system. It is commonly used as a strength enhancer and an aphrodisiac. According to some bodybuilders, it can help them build muscle and reduce fat. However, new reports state that people are using GHB as a “date rape” drug.
It is related to the amino acids 1,4 butanediol and gamma butyrolactone. These substances are commonly sold as party drugs on the Internet and in health food stores. GHB has been used as a general anesthetic and for treating alcoholism, narcolepsy, and cataplexy. It can also be used illegally as a recreational drug.
It can be produced through fermentation. It is commonly used as a salt, which is known as sodium -hydroxybutyrate, potassium -hydroxybutyrate, or sodium oxybate. GHB is also present in small amounts in various beverages such as wine, beef, and citrus fruits.
Prescription forms of GHB, such as sodium oxybate, are commonly used to treat narcolepsy. People also use it for other conditions, such as opioid withdrawal, depression, and alcohol use disorder. Unfortunately, there is currently no evidence supporting these uses.
History
In 1874, Alexander Zaytsev published his work on the chemical family that includes GHB. In the 1960s, Henri Laborit conducted the first extended study on the use of GHB in humans. It was used in various ways, such as during childbirth and obstetric surgery. It was also studied as an anxiolytic. In 1964, it was marketed as an intravenous anesthetic in Europe. However, it was not widely used due to how it can cause seizures. In 2006, it was still authorized in Italy and France.
In May 1990, GHB was marketed as a dietary supplement that can help with various conditions, such as weight control and sleep. In November 1989, L-tryptophan was removed from the market after batches of the product contaminated with traces of impurities were found to cause allergic reactions. In 2001, the FDA allowed the sales of dietary supplements containing this amino acid to resume.
In November 1989, the CDC received a report of 57 cases of severe illness related to the use of GHB supplements. Although no deaths were reported, nine people had to be admitted to an intensive care unit. The FDA then warned the public about the use of GHB.
Unfortunately, GHB was still being sold and manufactured illegally. In the 1990s, it was also used as a date rape drug. The DEA made numerous seizures and the FDA issued multiple warnings.
What is Gamma Hydroxybutyrate Used For?
Known as blue nitro, liquid ecstasy, grievous bodily harm, and fantasy, Gamma Hydroxybutyrate (GHB) is a drug that produces a wide range of effects. It is a neurotransmitter in the mammalian brain and acts as an agonist at GABA-B receptors. The receptors are found in the anterior cingulate cortex (ACC) and insula, which are involved in body awareness and relaxation.
Several studies have investigated the pharmacological and behavioural profiles of GHB. The pharmacological studies have focused on the effect of the compound on brain targets, the receptors, and the pharmacokinetics of the compound.
In the behavioural studies, GHB was reported to produce a variety of subjective effects. These included enhanced feelings of body awareness, relaxation, sociability, and a desire for sex.
In the behavioural studies, GHB had some analgesic effects, but was inadequate for reducing pain. It was also studied as a tool to help patients with absence seizures. Its toxic effects have also been examined. It has been found to have a number of adverse interactions, including with other depressants.
In addition to these toxic effects, GHB can cause serious health problems, including addiction. It is illegal in the United States and Canada. In 2002, the FDA approved Xyrem, a sodium salt of the compound, as a prescription drug. However, Xyrem requires a patient to enroll in a restricted access program.
Earlier this year, the US Food and Drug Administration issued a warning about the dangers of using GHB. The agency stated that it can be lethal if taken in combination with other drugs.
Medical Usage
In medical use, GHB is commonly used to treat narcolepsy and alcohol use disorder. It is also sometimes used off-label for treating fibromyalgia. There is currently no evidence supporting its effectiveness compared to other drugs for treating this condition.
In addition, GHB is also used as an active ingredient in a prescription drug known as sodium oxybate. It is approved in the US to treat cataplexy and excessive daytime sleepiness associated with narcolepsy.
Studies have shown that GHB can improve sleep by decreasing the tendency for REM sleep in tests that are modified to measure sleep latency. The FDA’s approval of the labeling for sodium oxybate does not imply that GHB has carcinogenic or teratogenic properties. Its safety profile relative to ethanol also explains why it is being considered as a potential alternative to alcohol.
Recreational Usage
Known as an intoxicant, GHB has many street names. Its effects can be similar to those of MDMA and ethanol, such as disinhibition, euphoria, enhanced libido, and amnesia. A review of the two drugs revealed that the risks of using GHB and ethanol were similar. At higher doses, it can cause various side effects, such as drowsiness, dizziness, hallucinations, amnesia, and unconsciousness.
Polydrug toxicity is one of the most common causes of death resulting from GHB consumption. Co-administration with other drugs, such as alcohol, can cause a potentiation effect. This can occur if the drugs bind to the gamma-aminobutyric acid receptor sites. In combination with alcohol, the effects of GHB can cause vomiting and respiratory arrest. Death can then occur due to this combination.
Most recreational doses of GHB are around 1–2 grams. At higher doses, this can lead to deleterious effects, such as reduced motor function. Other types of salt compounds, such as magnesium and calcium, have also been identified. However, the sodium salt is the most common.
Prodrugs, such as -butyrolactone, can convert to GHB in the blood stream and stomach. Other substances, such as 1,4-butanediol, can also be used as a combination of GHB and other harmful chemicals. These two compounds are usually found as pure liquids. However, they can be mixed with other harmful solvents for industrial use.
GHB can be produced using a process that involves mixing its two main components, GBL and sodium hydroxide. Since its precursors are easy to find, it is not commonly produced in illicit laboratories. Instead, it is usually made at home by low-level producers.
In 2006, a UK parliamentary committee reported that GHB was less harmful than alcohol and tobacco when it comes to social harms, physical harm, and dependence.
Party Usage
In the 1990s, GHB became popular as a club drug due to its ability to act as an aphrodisiac and a euphoriant. Its various terms, such as liquid ecstasy, lollipops, liquid X, and liquid E, refer to the drug’s use in the dance scene.
Sports and athletics
Due to the use of GHB as an enhancement drug, some professional athletes have been known to use it. However, there is no proof that it can improve their performance.
Combination with alcohol
Studies have shown that GHB can reduce the rate of alcohol elimination in humans. This could explain why people who consume both alcohol and GHB experience respiratory arrest. A review of the data collected over a decade showed that most of the deaths attributed to GHB were caused by respiratory depression.
Neurotoxicity
Multiple studies have shown that GHB can affect the working memory, spatial memory, and learning abilities of rats. It has also been known that the drug can decrease the expression of the N-methyl-D-aspartate receptor in the cerebral cortex. These findings suggest that the neurotoxic effects of GHB can be caused by the effects of oxidative stress.
Addiction
Repeated drug use can affect the balance of circuits in the brain that control various aspects of cognition and memory. When rats are forced to consume large amounts of GHB, they will frequently prefer to consume the drug’s solution instead of water.
Withdrawal
People who use GHB are also prone to experiencing withdrawal symptoms such as anxiety and insomnia. These conditions usually resolve within a couple of days. In severe cases, the patient may require hospitalization. The treatment for this condition involves considering the individual’s age, comorbidity, and the drug’s pharmacological pathways.
For people who are suffering from severe withdrawal, the usual treatment involves taking a combination of medications, such as benzodiazepines. However, in some cases, a larger dose is required. Baclofen has also been suggested as an alternative to these drugs.
Although baclofen has been used as an adjunct to the treatment of GHB withdrawal, more research is needed to confirm its effects on humans. It is believed that the drug works through the same receptors as GHB, and therefore, it is more effective at reducing the effects of the drug.
Although the condition is widely discussed in textbooks, many general practitioners, psychiatrists, and emergency physicians do not have a good understanding of GHB withdrawal.
PHARMACOLOGY
GHB has at least two binding sites in the nervous system. It is an agonist and a weak agonist of the GHB receptor and the gamma-aminobutyric acid receptor, respectively. It is produced naturally and functions similarly to other neurotransmitters in the brain.
It has been known that GHB activates the oxytocin receptor in the supraoptic nucleus. If taken orally, the drug does not affect the ability of the gamma-aminobutyric acid (GABA) to cross the blood-brain barrier. In addition, it increases the blood content of certain amino acids.
Serotonin turnover in the tissue can be stimulated by GHB as the amount of tryptophan is increased in the brain. This is because the serotonin-producing cells in the region are known to be involved in regulating mood and sleep. In addition, the effects of GHB on the region can trigger neuropsychiatric events.
At therapeutic doses, GHB enters the brain at high levels and activates the receptor of the gamma-aminobutyric acid (GABA) complex, which is responsible for the drug’s sedative effects.
The exact role of the GHB receptor in the effects of the drug is not known. However, it is widely believed that the drug has the highest affinity for the receptors located in the cortex and the hippocampus.
Although there is currently limited evidence supporting the role of the GHB receptor in the effects of the drug, it has been known that the activation of this receptor can cause the release of glutamate, a neurotransmitter that is known to be a major excitatory factor.
Legality
In the US, GHB was placed on the list of controlled substances in March 2000. However, it is currently used in the treatment of sodium oxybate, which is a drug that is classified as a Schedule III substance.
On March 20, 2001, the UN’s drug control agency placed GHB on its list of controlled substances. This drug was added to the list of substances that are classified as psychotropic.
In the UK, GHB was first classified as a class C drug in 2003. In October 2013, the Advisory Committee for Medicines and Healthcare Devices (ACMD) recommended that the drug be upgraded to schedule II, which is in line with the UN’s recommendations. On January 7, 2015, the drug was moved to schedule 2.
GHB is regulated in Hong Kong according to the city’s Dangerous Drugs Ordinance, which only allows health professionals and university researchers to use it. The substance can only be obtained through a prescription, and anyone who gives it without a prescription faces a fine of HK$10,000.
In Hong Kong, the penalty for manufacturing or trafficking of the substance is a life imprisonment sentence and a fine of HK$150,000. The possession of the substance without a license is also illegal.
In Canada, GHB has been placed on the list of controlled substances since November 6, 2012. Prior to that date, it was regarded as a Schedule III substance, similar to LSD and amphetamines.
In Australia and New Zealand, GHB, GBL, and 1,4-B are all illegal substances. Also, the substance gamma hydroxybutyric acid (GABA) is not allowed in these countries. This is because it cannot cross the blood-brain barrier. Despite this, some legislators believed that other analogues should be covered as well.
Attempts to circumvent the GHB’s classification have led to the unauthorized sale and use of various derivatives, such as 4-methyl-GHB and -valerolactone. These compounds are considered illegal because they are substantially similar to GBL or GHB. Therefore, the possession, importation, use, and sale of these compounds are considered illegal.
In Chile, GHB is considered a controlled substance due to its classification as a psychiatric substance and narcotics.
In Switzerland and Norway, GHB is only available through a prescription and is regarded as a narcotic. It can only be obtained through this trade name, Xyrem.
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