Temazepam
Temazepam is a short-acting benzodiazepine that produces sedative,1 hypnotic, anxiolytic, muscle relaxant, and anticonvulsant effects.1 Although its chemical synthesis was established by 1965, it was initially employed as a military sedative-hypnotic before gaining widespread civilian prescription for the treatment of severe insomnia, panic disorders, and anxiety. It has since become one of the most frequently prescribed benzodiazepines internationally. Like all benzodiazepines, it carries a risk of dependence with repeated use.2
Contents
Dosage & Duration
Dosage
Duration
Subjective Effects
The temazepam experience is dominated by heavy sedation, anxiety relief, and physical relaxation rather than any form of sensory alteration. As a hypnotic benzodiazepine, its effects pull strongly toward sleep, with dose-dependent improvements in sleep onset and total sleep time. At moderate to high doses, memory formation becomes unreliable, and coordination and clarity of thought are noticeably impaired; residual grogginess and impaired cognitive and motor performance can carry over into waking hours.
Physical
Pronounced sedation, muscle relaxation, and a heavy, sleep-directed body feeling are the primary physical effects, frequently accompanied by dizziness and a loss of motor coordination.
Sedation
Uncomfortable
Cognitive
The headspace is characterized by anxiety suppression alongside a general dulling and slowing of thought. Confusion can occur at higher doses, and anterograde amnesia is common, leaving recall of the period after ingestion partial or absent.
Suppressions
Reagent Testing
Loading reagent data
Pharmacology
Pharmacodynamics
Temazepam acts as a positive allosteric modulator at GABA-A receptors via the benzodiazepine binding site.1 This binding enhances the affinity of the inhibitory neurotransmitter GABA for the receptor, increasing the frequency of chloride ion channel opening and resulting in neuronal hyperpolarization.1 Temazepam also interacts with the translocator protein (TSPO).
Pharmacokinetics
Temazepam is very well absorbed orally, with 90 to 100% of an administered dose reaching the bloodstream owing to minimal first-pass metabolism of approximately 5 to 8%.12 The drug is 96% bound to plasma proteins.2 It is principally metabolized in the liver through direct glucuronide conjugation (Phase II), with less than 5% undergoing demethylation to oxazepam, which is subsequently eliminated as its glucuronide.1 Because metabolism is predominantly Phase II conjugation, temazepam is considered largely devoid of CYP450 interactions.1 The glucuronide metabolites have no demonstrable CNS activity.1 The terminal elimination half-life ranges from 3.5 to 18 hours, with a mean of approximately 9 hours.2 Following a single dose, 80 to 90% is excreted in the urine predominantly as the O-conjugate metabolite, with 3 to 13% appearing in the feces.1
Dangerous
Highest riskThese combinations are considered extremely harmful and should always be avoided. Reactions to these drugs taken in combination are highly unpredictable and have a potential to cause death.
Unsafe
AvoidThere is considerable risk of physical harm when taking these combinations, they should be avoided where possible.
Caution
Use cautionThese combinations are not usually physically harmful, but may produce undesirable effects, such as physical discomfort or overstimulation. Extreme use may cause physical health issues. Synergistic effects may be unpredictable. Care should be taken when choosing to use this combination.
Tolerance
Benzodiazepines, Barbiturates
Harm Potential
Addiction & Dependence
Psychological
HighTemazepam has a high potential for psychological addiction and is considered significantly more addictive than other benzodiazepines. It produces euphoria more commonly than most benzodiazepines and has the highest preference ratings among recreational drug users due to its rapid onset, perceived strength, and subjective 'high'.
Physical
Extremely HighPhysical dependence develops readily with regular use, and abrupt discontinuation can be life-threatening, potentially resulting in severe withdrawal syndrome, seizures, or death.2 Withdrawal symptoms can occur even from standard therapeutic doses after short-term use.3 Gradual tapering under medical supervision is essential for cessation.
Toxicity
Pronounced CNS depression occurs at therapeutic doses, including impairment of memory, learning, motor coordination, and reaction time; at higher doses or in overdose, confusion, coma, and absent reflexes may develop.
Respiratory depression can occur at higher doses and has proven fatal even when temazepam is taken alone, which is unusual among benzodiazepines.1
Severe hepatic impairment decreases temazepam elimination by approximately half; hyperplastic liver nodules were observed in female mice at the highest doses in animal studies.2
Psychosis Risk
Psychotic states have been reported rarely in the medical literature following abrupt withdrawal from benzodiazepines, even from therapeutic doses.4 Hallucinations are listed as a less common side effect occurring in under 0.5% of users. Paradoxical reactions including aggression, violent behavior, and agitation occur rarely, with an incidence below 1% in the general population.
Seizure Risk
Sudden discontinuation after regular use can result in potentially life-threatening seizures; this risk is a primary concern with benzodiazepine withdrawal and necessitates gradual tapering rather than abrupt cessation.2 Paradoxical increased seizure activity may occur in epileptic individuals. Antipsychotics increase the severity of withdrawal convulsions.
History & Culture
Legality
International
1961 Single Convention: temazepam is not scheduled.
1971 Convention on Psychotropic Substances: Schedule IV.
1988 Convention: temazepam is not listed in precursor Tables I or II.
By Country
References
Source Pages
Citations
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Further Reading
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