Premazepam

Drugbox
IUPAC_name = 3,7-Dihydro-5-phenyl-6,7-dimethyl-pyrrole [3,4-e] [1,4] diazepin-2-(1"H")-one


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CAS_number = 57435-86-6
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PubChem = 72104
DrugBank =
C = 15 | H = 11 | N = 3 | O = 3
molecular_weight = 253.30 g/mol
bioavailability =
metabolism = Hepatic
elimination_half-life = 10 - 13 hours
excretion = Renal
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Premazepam, known by its full chemical name 3,7-dihydro-5-phenyl-6,7-dimethyl-pyrrole [3,4-e] [1,4] diazepin-2-(1 H) -one, is a benzodiazepine derivative. [cite journal | journal = Drug Metab Dispos | year = 1984| month = Mar-Apr | volume = 12 | issue = 2 | pages = 257–63 | title = Metabolic fate of premazepam, a new anti-anxiety drug, in the rat and the dog | author = Assandri A | coauthors = Barone D, Ferrari P, Perazzi A, Ripamonti A, Tuan G, Zerilli LF | pmid = 6144494] It is a partial agonist of benzodiazepine receptors and has been shown to possess both anxiolytic and sedative properties in human subjects.

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. [cite journal | journal = Int J Clin Pharmacol Ther Toxicol | year = 1984| month = May | volume = 22 | issue = 5 | pages = 273–7 | title = Pharmacokinetics and metabolism of premazepam, a new potential anxiolytic, in humans | author = Vitiello B | coauthors = Buniva G, Bernareggi A, Assandri A, Perazzi A, Fuccella LM, Palumbo R | pmid = 6146571] [cite journal | journal = Psychopharmacology (Berl) | year = 1985 | volume = 86 | issue = 4 | pages = 464–7 | title = In vivo interaction of premazepam with benzodiazepine receptors: relation to its pharmacological effects | author = Mennini T | coauthors = Barone D, Gobbi M | pmid = 2863844 | doi = 10.1007/BF00427909]

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. [cite journal | journal = Br J Clin Pharmacol | year = 1984 | month = Aug | volume = 18 | issue = 2 | pages = 127–33 | title = The psychopharmacological effects of premazepam, diazepam and placebo in healthy human subjects | author = Golombok S | coauthors = Lader M | pmid = 6148956 | url = http://www.pubmedcentral.nih.gov/picrender.fcgi?artid=1463527&blobtype=pdf | format = PDF ]

References