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Diazepam is a benzodiazepine with CNS depressant properties and a somewhat flatter dose-response slope than the sedative-hypnotic drugs. In laboratory animals, it produces, in varying doses, taming, disinhibitory, sedative, anticonvulsant, muscle relaxant, ataxic and hypnotic effects.

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Diazepam is relatively devoid of autonomic effects and does not significantly reduce locomotor activity at low doses, or depress amphetamine-induced excitation. In high doses, it activates the drug metabolizing enzymes in the liver. Diazepam also possesses dependence liability and may produce withdrawal symptoms, but has a wide margin of safety against poisoning.

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Metabolism studies in animals and man have indicated that oral diazepam is rapidly absorbed from the gastrointestinal tract. Peak blood levels are reached within 1-2 hours after administration. The acute half-life is 6-8 hours with a slower decline thereafter, possibly due to tissue storage.

In humans, comparable blood levels of diazepam were obtained in maternal and cord blood indicating placental transfer of the drug. Diazepam may appear in human breast milk.


With the parenteral form, peak blood levels are reached within 15 minutes after i.v. administration and are of the same magnitude as after oral administration. The respective half-life is approximately 2-3 hours.

The distribution and fate of tritium-labeled diazepam in man has indicated that the drug has a rapid and extensive uptake by tissues. Although the radioactivity in the blood appears to represent mainly the intact drug, diazepam was shown to be excreted exclusively in the form of its metabolites. The two major metabolites are oxazepam glucuronide and N-desmethylated diazepam.

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