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Anxiolytic - Sedative - Muscle
Relaxant 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.
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.
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.
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