Oxazepam is the first of a chemical series of compounds, the 3-hydroxybenzodiazepinones. A therapeutic agent providing versatility and flexibility in control of common emotional disturbances, this product exerts prompt action in a wide variety of disorders associated with anxiety, tension, agitation and irritability, and anxiety associated with depression. Oxazepam has distinguished itself clinically from other benzodiazepines by virtue of its excellent tolerance. Because of its excellent tolerance, dosage is very flexible, and it is, therefore, possible to utilize oxazepam in a wide spectrum of anxiety-related disorders including the psychoses. Oxazepam has been administered to humans by the oral route only. Usual ranges for kinetic parameters are: elimination half-life, 5 to 15 hours; volume of distribution, 0.6 to 2.0 L/kg; clearance, 0.9 to 2.0 ml/min/kg. Age and liver disease have a minimal influence on oxazepam kinetics, but renal disease is associated with a prolonged half-life and increased volume of distribution.

Demoxepam is a major pharmacologically active metabolite of the benzodiazepine chlordiazepoxide, the first drug within the class to gain approval by the Food and Drug Administration for use as an anticonvulsant, muscle relaxant and sedative hypnotic. Demoxepam has been shown to have antianxiety activity in man. The eventual elimination of demoxepam from the plasma was slow, with a range in half-life of 14-95 hr. The half-life of demoxepam was markedly longer than that of chlordiazepoxide. Demoxepam has an inhibitory effect on in vitro [3H]tryptophan binding to rat hepatic nuclei.