Written by John Morgenthaler and Dan Joy. This
article is excerpted and adapted from a chapter of a book, Better Sex Through
Chemistry available from CERI and Smart Publications, P.O. Box 4667, Petaluma,
CA 94955 (phone: 707-769-8078).
Many doctors are upset that politics has made GHB illegal in some countries.
Its great usefulness and lack of side-effects do not warrant such restriction.
Users have been forced onto the "grey market" in order to obtain it.
GHB, or gamma-hydroxybutyrate, is a normal component of mammalian metabolism.
It is found naturally in every cell in the human body and is most properly
considered a nutrient. In the brain, the highest amounts are found in the
hypothalamus and basal ganglia (Gallimberti, 1989). GHB is found in greater concentrations
in kidney, heart, skeletal muscles, and brown fat tissues (Chin and Kreutzer,
1992). It is believed to be a neurotransmitter, although the jury is still out
as to whether it exhibits all of the properties required for fulfillment of
this function (Chin and Kreutzer, 1992). It is both a
metabolite and precursor of the inhibitory neurotransmitter GABA
(gamma-aminobutyric acid, or gamma-aminobutyrate), another nutrient to which it
bears a close structural relationship. GHB, however, does not act directly on
GABA receptor sites (Chin and Kreutzer, 1992).
GHB was first synthesized about thirty years ago by Dr. H. Laborit, a French
researcher interested in exploring the effects of GABA in the brain. Because
little or no GABA crosses the blood-brain barrier, Laborit synthesized GHB,
which substitutes a hydroxy group for an amino group. This difference allows
GHB to cross the blood brain barrier where some of it is metabolized into GABA
(Vickers, 1969).
As it turned out, Laborit found that GHB exhibited a range of effects beyond
those expected from GABA. Over the intervening years, numerous researchers have
extensively studied GHB’s effects. It is has come to be used in Europe as a
general anesthetic, a treatment for insomnia and narcolepsy (a daytime sleeping
disorder), an aid to childbirth (increasing strength of contractions,
decreasing pain, and increasing dilation of the cervix), a treatment for
alcoholism and alcohol withdrawal syndrome, and for many other uses.
During the 1980s, GHB was widely available over-the-counter in health food
stores, purchased largely by body builders for its ability to stimulate growth
hormone release which aids in fat reduction and muscle building. In the last
few years it has been gaining popularity as a “recreational” drug offering a
pleasant, alcohol-like, hangover-free “high” with potent prosexual effects.
Scientific Reports on GHB
For the thirty years prior to 1990, the scientific papers on GHB were unanimous
in reporting numerous beneficial physiological effects and the absence of
long-term negative effects. In 1964, Laborit listed “very low toxicity” as one
of the “principle elements” of the compound’s
pharmacology. In a 1969 report on GHB’s anesthetic uses, Vickers referred to
GHB as “a truly nontoxic hypnotic” and repeatedly emphasized its “lack of
toxicity.” Vickers cited evidence that GHB demonstrates “no toxic effects on
the liver and kidney.” In 1972, Laborit described the body’s metabolism of GHB
and stressed “the absence of any need of detoxification by the organism.”
As recently as 1989, this scientific consensus on GHB’s benign nature remained
unchanged. Gallimberti’s study from that year on its uses in treating alcohol
withdrawal in humans notes that “GHB’s action...seems to be without serious
side effects.” His almost off-hand reference to the “safety of GHB” shows how
well established this property of the nutrient had become.
Then, on
Of the ten “poisonings” reported, four involved “unknown doses,” four featured
the “coingestion” of other drugs (usually alcohol), one involved unmedicated
epilepsy, and another a history of grand mal seizures. Since alcohol and other
central nervous system (CNS) depressants are not recommended with GHB, and
because GHB is contraindicated for epileptics, such cases are not unexpected. Chin
and Kreutzer acknowledge that the “more severe reactions...generally occurred
when patients took an unmeasured dose, a particularly large dose, or several
doses within a short period of time.” Such problems are easily avoided by
following the directions for GHB’s use.
Although the specific clinical details of these ten cases are too lengthy to go
into here, one point needs addressing - the use of the terms “coma” and
“seizures” in descriptions of these cases. At a sufficiently high dose, GHB can
cause clonus, a rapid, rhythmic contraction and relaxation of muscles which
would be better described as muscle spasm or uncontrollable twitching than a
seizure. GHB can also cause intense drowsiness, abrupt sedation, and deep sleep
which is probably better described as unarrousability or deep sedation than
coma. Vickers (1969) described it as a “nontoxic coma,” which blunts some of
the inflammatory connotations of the term coma.
Regardless of their alarmist tone, the authors confirm that “there have not
been any reported deaths” and that “if product use is discontinued, full
recovery with no long term side effects is universal.” They concluded that “the
prognosis for people who experience GHB poisoning is quite good.”
The degree to which the pleasant state of GHB euphoria may be psychologically
addicting may not be fully appreciated. Anybody with known attraction or
addiction to tranquilizers or alcohol should pay special heed to this
possibility. In the few cases of GHB abuse that we have investigated, there were
pre-existing use/abuse patterns with alcohol and/or tranquilizers. Ironically,
it was GHB’s lack of toxicity that led to increased frequency of use (numerous
times per day) that characterized what can only be called classic cases of
psychological addiction. Without the dehydration and CNS irritation of alcohol,
or the side effects of tranquilizers, there was no incentive to moderate or
curtail GHB use. Fortunately, few people seem to have such overwhelming
attraction to the GHB state. Even Chin and Kreutzer minimize GHB’s abuse
potential by stating, “No investigator (has) reported any long term adverse
effects, addictive or dependent qualities associated with discontinued usage of
the drug.”
Why Was GHB Banned?
It seems likely, then, that at least some of the motives behind the 1990 FDA
ban of GHB were other than those of public safety. Such a ban constitutes the
only means of Federal control of a substance neither scheduled by the DEA nor
approved by the FDA as a drug. In the absence of a genuine public health
concern, such control might have been motivated by a desire to protect the
pharmaceutical industry (with which the FDA is closely intertwined) from
competition from a safer, more effective and less expensive alternative to
sleeping pills. Is it a coincidence that the FDA has also banned L-tryptophan,
another nutrient that functions as a safe and effective sleep aid?
What Are the Real Concerns?
As with most substances, unpleasant and possibly dangerous side effects can be
associated with excessive doses of GHB. A dose usually only about twice the
amount required for relaxation or a prosexual effect can, as one user put it,
“knock you out but fast.” In this respect, GHB is probably comparable to
alcohol: if you drink twice as much as you normally would, you probably
wouldn’t function very well. Despite its general safety and lack of toxicity,
the safe use of GHB requires information, preparation, caution, and good
judgment. In other words, follow the usage guidelines.
How Does It Feel?
Most users find that GHB induces a pleasant state of relaxation and
tranquility. Frequent effects are placidity, sensuality, mild euphoria, and a
tendency to verbalize. Anxieties and inhibitions tend to dissolve into a
feeling of emotional warmth, well being, and pleasant drowsiness. The “morning
after” effects of GHB lack the unpleasant or debilitating characteristics
associated with alcohol and other relaxation type drugs. In fact, many users
report feeling particularly refreshed, even energized,
the next day.
The effects of GHB can generally be felt within 5-20 minutes after ingestion.
They usually last no more than 1 1/2-3 hours, although they can be indefinitely
prolonged through repeated dosing. The effects of GHB are very dose dependent.
Small increases in the amount ingested lead to significant intensification of
the effect. Higher levels feature greater giddiness, silliness, and
interference with mobility and verbal coherence, and maybe even dizziness. Even
higher doses usually induce sleep.
The Actions of GHB in the Body
GHB temporarily inhibits the release of dopamine in the brain. This may cause
increased dopamine storage, and later increased dopamine release when the GHB
influence wears off (Chin and Kreutzer, 1992). This effect could account for
the middle-of-the-night wakings common with use of higher GHB doses, and the
general feelings of increased well being, alertness and arousal the next day.
At the same time GH is being released, prolactin levels also rise. Serum
prolactin levels increase in a similar time-dependent manner as GH, peaking at
five-fold above baseline at 60 minutes (Takahara, 1977). This effect, unlike
the release of GH, is entirely consistent with GHB’s inhibition of dopamine.
Other compounds which lessen dopamine activity in the brain (such as the
neuroleptic Thorazine) have been shown to result in prolactin release. Although
prolactin tends to counteract many of the beneficial effects of GH, the
sixteen-fold increases in GH probably overwhelm the five-fold increases in
prolactin.
GHB is completely metabolized into carbon dioxide and water, leaving absolutely
no residue of toxic metabolites (Vickers, 1969; Laborit, 1972). Metabolism is
so efficient that GHB can no longer be detected in urine 4-5 hours after it is
taken by injection (Laborit, 1964).
GHB activates a metabolic process known as the “pentose pathway” which plays an
important role in the synthesis of protein within the body (Laborit, 1972). It
also causes a “protein sparing” effect (Laborit, 1964) which reduces the rate
at which the body breaks down its own proteins. These properties, along with
GHB’s effect on growth hormone, underlie its common use as an aid to
muscle-building and fat loss.
Anesthetic (large) doses of GHB are accompanied by a small increase in blood
sugar levels, and a significant decrease in cholesterol. Respiration becomes
slower and deeper. Blood pressure may rise or fall slightly, or remain stable,
but a moderate slowing of the heart is consistent (Vickers, 1969; Laborit,
1964). A slight drop in body temperature also occurs (Laborit, 1964).
GHB also stimulates the release of acetylcholine in the brain (Gallimberti,
1989).
Other Uses of GHB
GHB has a decades long track record of use as a
general anesthetic. Administered intravenously, an anesthetic dose of GHB is in
the range of 4-5gm for a 150 pound (68kg) person (Vickers, 1969). Its
advantages as an anesthetic include low toxicity, relatively few
contraindications, slowing of the heart rate without loss of blood pressure,
the absence of irritation to the veins with intravenous administration, muscle
relaxation, absence of respiratory depression (usually), reduction of body
temperature (hypothermia), and various protective and anti-shock actions
(Laborit, 1964). However, GHB can almost never be used in anesthesia without the
additional administration of other drugs (Vickers, 1969) because it does not
produce complete surgical anesthesia except in children (Laborit, 1964). The
autonomic nervous system remains active during GHB-induced anesthetic coma, and
thus the body continues to respond to surgical stimuli through increases in
heart rate, blood pressure, and cardiac output, as well as through sweating,
peripheral vasoconstriction, vocalization, and reflex muscle action (Vickers,
1969). Local anesthetics or other drugs which suppress these responses must
therefore also be used, like the way a dentist or orthodontic surgeon might use
Novocaine to kill pain along with nitrous oxide to render a patient
unconscious.
It is suspected that part of GHB’s protective function involves a slowing of
the metabolism of brain cells, thus reducing their requirements for oxygen and
glucose (Chin and Kreutzer, 1992; Artru, 1980). Another factor in GHB’s
anti-shock capability may be the marked vasodilation induced in the liver and
kidney, thus increasing blood flow to those vital organs.
15 INDs (Investigational New Drug Applications) have
been filed with the FDA for 1) improving sleep patterns and maintaining daytime
alertness in narcolepsy, 2) reducing schizophrenic symptoms, 3) stabilizing
Parkinson’s disease, 4) reducing nocturnal myoclonus
(painful leg cramps at night), 5) improving memory problems, 6) stimulating
natural growth hormone release, 7) decreasing pain and improving sleep in
fibromyalgia, 8) relieving symptoms in Huntington’s chorea, 9) regulating
muscle tone in dystonia musculorum
deformans, 10) controling tardive dyskinesia symptoms, 11)
decreasing drug withdrawal symptoms (alcohol and opiates), 12) decreasing
hyperactivity and learning disabilities in children, 13) inducing sedation and
tranquilization, 14) relieving anxiety [in fact, it has been recommended as the
anti-anxiety agent of choice for potentially suicidal patients], and 15)
lowering cholesterol.
GHB and Sex
Scientists and doctors have traditionally been reluctant to ascribe aphrodisiac
properties to any substance, although this tendency may have abated somewhat in
recent years. It is a testament, then, to the power the GHB’s sexual effects
that they were clearly acknowledged in the scientific literature by 1972. Dr.
Laborit wrote:
“A last point should still be mentioned: the (GHB)
action on man which could be called ’aphrodisiac.’ We cannot present any animal
experiments on this subject. However, the oral form has now been sufficiently
used so that, as generally agreed, no doubt can subsist as to its existence.”
We have identified four main prosexual properties: 1-disinhibition,
2-heightening of the sense of touch (tactility), 3-enhancement of male erectile
capacity, and 4-increased intensity of orgasm.
Perhaps the foremost prosexual property of GHB is disinhibition. Some users
suggest that GHB’s other sexual benefits are secondary effects, made possible
(or at least amplified) by this loosening of psychosomatic constraint. A number
of people have commented that this disinhibition is particularly marked among
women.
Women often report that GHB makes their orgasms longer and more intense, as
well as more difficult or time-consuming to achieve, especially at higher
doses. As with its other effects, GHB’s impact on female orgasm seems highly
sensitive to small adjustments in dosage.
Legal Status and Availability
For the latest details, including what is happening in court, please visit
<a href='http://www.ceri.com/ghbmad.htm'
target='web'>CERI’s page on GHB Madness</a>.
In some European countries, GHB is an approved drug available by prescription.
Local doctors, pharmacists and government bureaucrats should be able to provide
country-by-country specifics.
GHB is growing in popularity and seems to be widely available in the
underground “gray market.” Since most of the GHB available through such
channels is of the “bootleg” variety, manufactured by non-professional
“kitchen” chemists, concerns about quality and purity should be kept in mind.
Caveat emptor (buyer beware)!
Safety Issues
As has been emphasized, the overall safety of GHB is well established, and no
deaths attributable to GHB have been reported over the thirty year period that
this compound has been in use (Vickers, 1969; Chin and Kreutzer, 1992). In
fact, as of 1990, only 46 adverse reactions had been reported in the
Side Effects
According to Dr. Gallimberti (1989), the action of GHB is “without serious side
effects.” Some research programs have reported no side effects at all.
Nonetheless, it’s clear that some minor side effects can occur. Those most
commonly experienced are drowsiness, dizziness, nausea, and sometimes vomiting.
As a sedative-hypnotic, GHB’s effects bear some similarity to those of alcohol
and tranquilizers. GHB not only “may cause drowsiness” like these other drugs,
it will almost invariably do so. Ataxia, or incoordination, can also be a side
effect of GHB. Do not drive a vehicle or operate dangerous machinery while
under the influence of GHB.
As mentioned, clonic movements (muscle contractions or “seizures”) have been
observed during the onset of GHB induced sleep. Headache is sometimes reported.
A moderate slowing of the heart rate is a consistent effect, and small changes
in blood pressure can take place. Likewise, orthostatic hypotension (a sudden
drop in blood pressure caused by standing up quickly) has also been reported.
Sometimes this is experienced as brief dizziness, and rarely people can briefly
lose consciousness. At very high doses, cardiac and respiratory depression can
occur.
Sufficiently large doses of GHB can cause sudden sedation and loss of
consciousness. Do not take such doses except when reclining on a bed or sofa.
It is also a bad idea to take such doses in the presence of people who don’t
know anything about GHB. You may alarm your family or friends and wake up in an
emergency room (with a large medical bill).
More unusual and extreme reactions have included diarrhea, lack of bladder
control, temporary amnesia, and sleep-walking. Whatever side effects may be
noted, they are often much more severe when GHB is combined with other central
nervous system depressants (Chin and Kreutzer, 1992, Gallimberti, 1989;
Takahara, 1977; Vickers, 1969).
Contraindications
Although contraindications for GHB have been described as “remarkably few”
(Vickers, 1969), those who suffer from any of the following conditions should
not use GHB: severe illness of any kind, epilepsy, eclampsia (convulsions),
bradycardia (slowed heart beat) due to conduction problems (left bundle branch
block is an example of conduction difficulty), Cushing’s syndrome, severe
cardiovascular disease, hyperprolactinemia, and severe hypertension
(Gallimberti, 1989; Vickers, 1969).
Severe alcoholism is sometimes mentioned as a contraindication for GHB (Smart
Drugs II, page 244) even though GHB has been used quite successfully in the
treatment of withdrawal symptoms. The explanation for this seeming
contradiction probably lies in the likelihood that severe alcoholics may
combine GHB with alcohol.
GHB should not be used with benzodiazepines (“minor tranquilizers” such as
Valium and Xanax), phenothiazines (“major tranquilizers” like Thorazine and
Stellazine), various painkillers (barbiturates and opiates), alcohol,
anticonvulsants (Dilantin and phenobarbital) and even many over-the-counter
allergy and sleep remedies, without direct medical supervision.
Dosage
Determining the ideal dose is probably the trickiest
aspect of working with GHB. The amount required for a given level of effect
will vary from person to person, and the dose-response curve is fairly steep.
Overestimating the dose can have consequences ranging in seriousness from
ruining your plans for the evening to waking up in the emergency ward as a
result of panic on the part of concerned, but uninformed friends or relatives.
Once you have found the levels that give you the effects you desire, they will
remain consistent. Tolerance to GHB does not develop. However, recent alcohol
consumption may decrease the effect of a given dose of GHB (Fadda, 1989).
Most people find that a dose in the range of 0.75-1.5gm is suitable for
prosexual purposes, and that a quantity in the range of 2.5gm is sufficient to
force sleep.
Some people think that GHB might lower potassium levels and should therefore be
taken with potassium supplementation. Some research papers have identified such
an effect, others have not. If you want to play it safe, take a potassium
supplement equal to 10% of the GHB dose.