Xyrem is distributed by Jazz Pharmaceuticals, Inc. (Palo Alto,
CA). It is an oral solution of sodium oxybate prescribed for
narcoleptic patients to treat extreme daytime sleepiness and
cataplexy. Xyrem is also known as sodium oxybate which is the
same as gamma hydroxybutyric acid (GHB), a drug of abuse.
GHB is endogenously produced and present in the central
nervous system (CNS) in small concentrations. Accidental
overdosing has led to many hospitalizations and deaths.
Because of the tendency to abuse GHB, it was classified as
a schedule I controlled substance. This meant that GHB had
a high potential for abuse and no medical purpose. However,
in 2002, because of a series of clinical trials that demonstrated
that the compound reduces cataplexy attacks, it was approved
for use under the trademark Xyrem. Since GHB had previously
been used as a ‘date-rape’ drug, Xyrem is considered a schedule
III controlled substance and is distributed in accordance with
strict FDA regulations. Xyrem may only be ordered through the
‘Xyrem Success Program.’ Illegal use is punishable under
federal and state laws.
GHB (sodium salt) (exempt preparation) (Item No. 15661) is an analytical reference standard categorized as a CNS depressant. GHB is a metabolite of γ-butyrolactone . It has a high potential for abuse. GHB is regulated as a Schedule I compound in the United States. GHB (sodium salt) (exempt preparation) (Item No. 15661) is provided as a DEA exempt preparation. This product is intended for research and forensic applications.
4-Hydroxybutyric acid sodium salt is an agonist to both GHB and GABAB neural receptors, exhibiting neurotransmitter-like effects. It has been used as a general anesthetic in treatment for sleep disorders and clinical depression, but also has been identified as a “date rape drug”.
Xyrem is used as a prescription drug for the treatment of
cataplexy in patients with narcolepsy. It can also be used illegally
for recreational purposes as well as drug-facilitated sexual
assault.
The substance is related to γ-aminobutyric
acid, a cerebral metabolite that is supposed to
be sleep inducing. When given i.p., it produces
a shallow anesthesia (tolerance stage a: paralysis
of the spinal cord and mesencephalon, slight
relaxation of the muscles) that
resembles natural sleep as seen via the electroencephalograph.
It is employed as an anesthetic
during labor and in combination anesthesia
with nitrous oxide, barbiturates, or neuroleptanalgesics.
Xyrem is a water-soluble white to off-white powder, which can
be disposed by dumping the oral solution down the sanitary
sewer system. This is the preferred method of disposal for drugs
which have a high potential for abuse and/or accidental
overdose.
GHB is endogenously present in the brain and at low concentrations
binds to GHB receptors that are excitatory. This effect
can cause euphoria, making it a drug of abuse at ‘rave’ parties.
However, at higher concentrations, Xyrem is a CNS depressant
and this is the main mechanism of its toxicity. The negative
effects are mediated by the gamma-aminobutyric acid (GABA)B
receptors. The maximum stimulation of these receptors by GHB
is w69% when compared to the binding of a GABAB receptor
agonist. Therefore, the drug appears to be a weak agonist of the
GABA-binding site of GABAB receptors. Overdose can lead to
respiratory arrest and death. The combined use of other sedative
hypnotic agents or alcohol can exacerbate the toxicity of Xyrem.
