Quazepam and flurazepam: differential pharmacokinetic and pharmacodynamic characteristics.
Quazepam and flurazepam share pharmacokinetic properties that result in prevention of early-morning insomnia, daytime rebound anxiety, and withdrawal rebound insomnia. Yet sleep laboratory and performance studies demonstrated that during a 1- to 4-week administration period quazepam had a low potential for causing daytime drowsiness or impairment. This profile may be related to several factors, such as differences in quazepam's metabolic pathways; plasma pharmacokinetics; rate of brain uptake, redistribution, and clearance; as well as differences in receptor binding and kinetics.
Pharmaceuticals Division, Radian Corporation, Austin, Tex.
J M
JM
Hilbert
D
D
Battista
D000818:Animals; D014151:Anti-Anxiety Agents / Q000378:metabolism / Q000493:pharmacokinetics / Q000494:pharmacology; D001569:Benzodiazepines / Q000493:pharmacokinetics* / Q000494:pharmacology; D001570:Benzodiazepinones / Q000378:metabolism; D006224:Cricetinae; D005479:Flurazepam / Q000031:analogs & derivatives / Q000378:metabolism / Q000493:pharmacokinetics* / Q000494:pharmacology; D006801:Humans; D006993:Hypnotics and Sedatives / Q000378:metabolism / Q000493:pharmacokinetics* / Q000494:pharmacology; D007700:Kinetics; D051379:Mice; D015394:Molecular Structure; D051381:Rats; D012453:Saimiri; D007319:Sleep Initiation and Maintenance Disorders / Q000188:drug therapy; D014018:Tissue Distribution
D014151:Anti-Anxiety Agents; D001570:Benzodiazepinones; D006993:Hypnotics and Sedatives; D001569:Benzodiazepines; C039103:2-oxoquazepam; D005479:Flurazepam; C025130:quazepam; C020965:norflutoprazepam