Temazepam Other names: Methyloxazepam Hydroxydiazepam Oxydiazepam N-Methyloxazepam

Chemical formula: C₁₆H₁₃ClN₂O₂  Molecular mass: 300.74 g/mol  PubChem compound: 5391

Pharmacodynamic properties

Temazepam is a benzodiazepine with hypnotic and sedative effects as well as anxiolytic activity.

Temazepam effects are likely to be due to potentiation of gamma-aminobutyric acid (GABA), although other neurotransmitters may also be affected. Evidence suggests a close molecular association between the sites and action for GABA and the benzodiazepines.

Pharmacokinetic properties

Absorption

Temazepam is readily absorbed from the gastro-intestinal tract, although the exact rate of absorption depends on the formulation. Peak plasma levels are reached within 50 minutes if given orally, with multidosing steady state reached by the third day.

Distribution

It is about 96% bound to plasma protein. Temazepam is also found in breast milk in small amounts and may exert its effects on the infant.

Biotransformation

Temazepam is mainly metabolised in the liver with a terminal half-life of between 8 and15 hours. This half-life depends on time of dose (morning administration has longer half-life than evening) and age of patient (elderly patients experience a longer half-life).

Elimination

80% is excreted in the urine in the form of its inactive glucuronide conjugate together with small amounts of the demethylated derivative, Oxazepam, also in conjugated form. Only approximately 12 % appears in the faeces.

Preclinical safety data

Not applicable.

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