Sedative-hypnotic properties of a new benzodiazepine in comparison with flurazepam. Pharmacological and clinical findings.
The sedative-hypnotic effects of a new benzodiazepine, 1-(2-hydroxyethyl)-3-hydroxy-7-chloro-1,3-dihydro-5-(o-fluorophenyl)-2H-1,4-benzodiazepin-2-one (SAS 643), were compared with those of flurazepam in mice and rats as well as in a double-blind clinical trial. It was found that SAS 643 has a potency 2--4 times greater than that of flurazepam while it is about one half less toxic than the latter drug. The results of the clinical trial confirm the greater activity of SAS 643 and indicate that the new benzodiazepine causes a significantly less amount of hangover than flurazepam.
D000368:Aged; D000818:Animals; D014151:Anti-Anxiety Agents / Q000494:pharmacology*; D001570:Benzodiazepinones / Q000494:pharmacology* / Q000627:therapeutic use / Q000633:toxicity; D001794:Blood Pressure / Q000187:drug effects; D002415:Cats; D002986:Clinical Trials as Topic; D004341:Drug Evaluation; D004569:Electroencephalography; D004986:Ether / Q000494:pharmacology; D005106:Exploratory Behavior / Q000187:drug effects; D005260:Female; D005479:Flurazepam / Q000494:pharmacology* / Q000633:toxicity; D006339:Heart Rate / Q000187:drug effects; D006591:Hexobarbital / Q000494:pharmacology; D006801:Humans; D006993:Hypnotics and Sedatives / Q000627:therapeutic use / Q000633:toxicity; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D011817:Rabbits; D051381:Rats; D012119:Respiration / Q000187:drug effects; D012890:Sleep / Q000187:drug effects; D007319:Sleep Initiation and Maintenance Disorders / Q000188:drug therapy
D014151:Anti-Anxiety Agents; D001570:Benzodiazepinones; D006993:Hypnotics and Sedatives; D004986:Ether; D006591:Hexobarbital; D005479:Flurazepam