Premazepam

Premazepam

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Systematic (IUPAC) name
6,7-dimethyl- 5-phenyl- 3,7-dihydropyrrolo[3,4-e] [1,4]diazepin- 2(1H)-one
Pharmacokinetic data
Metabolism	Hepatic
Biological half-life	10 - 13 hours
Excretion	Renal
Identifiers
CAS Number	57435-86-6
ATC code	none
PubChem	CID 72104
Chemical data
Formula	C15H11N3O3
Molar mass	253.30 g/mol[[]]

Premazepam is a benzodiazepine derivative. It is a partial agonist of benzodiazepine receptors and has been shown to possess both anxiolytic and sedative properties in human subjects.

Properties

The initial doses of premazepam given to human test subjects demonstrated similar psychological test results to those produced by diazepam. It was also demonstrated that initial dosing with premazepam produces similar sedative effects as compared with diazepam, although psychomotor impairments are greater with premazepam than with diazepam after initial dosing. However, with repeated dosing for more than one day premazepam causes less sedation and less psychomotor impairment than diazepam. Premazepam possesses sedative and anxiolytic properties. Premazepam produces more slow wave and less fast wave EEG changes than diazepam. Tests have shown that 7.5 mg of premazepam is approximately equivalent to 5 mg of diazepam.

Pharmacology

Premazepam is a pyrrolodiazepine benzodiazepine and acts as a partial agonist at benzodiazepine receptors. The mean time taken to reach peak plasma levels is 2 hours and the mean half life of pramazepam in humans is 11.5 hours. About 90% of the drug is excreted in unchanged form. Of the remaining 10% of the drug none of the metabolites showed any pharmacological activity. Thus premazepam produces no active metabolites in humans.

See also

• Benzodiazepine
• Benzodiazepine dependence
• Benzodiazepine withdrawal syndrome
• Long term effects of benzodiazepines