Flunitrazepam and lormetazepam do not affect the pharmacokinetics of the benzodiazepine antagonist Ro 15-1788.
Following a single intravenous dose of 0.1 mg/kg, the pharmacokinetics of Ro 15-1788, a specific benzodiazepine antagonist, have been investigated in 20 healthy male volunteers. In random order injection of Ro 15-1788 has been preceded (5 min) by intravenous dosing with 0.06 mg/kg of lormetazepam (n = 6), 0.03 mg/kg of flunitrazepam (n = 8) or placebo (n = 6). The rapid elimination of the antagonist could be characterized by an elimination half-life between 0.9 to 1.4 h and a total plasma clearance of 727 to 1440 ml/min. These single dose studies indicate that the disposition of Ro 15-1788 was not affected by the acute coadministration of both benzodiazepines.
D000293:Adolescent; D000328:Adult; D014151:Anti-Anxiety Agents; D001569:Benzodiazepines / Q000037:antagonists & inhibitors; D001570:Benzodiazepinones / Q000378:metabolism*; D005442:Flumazenil; D005445:Flunitrazepam / Q000494:pharmacology*; D006801:Humans; D007700:Kinetics; D008140:Lorazepam / Q000031:analogs & derivatives* / Q000494:pharmacology; D008297:Male
D014151:Anti-Anxiety Agents; D001570:Benzodiazepinones; D001569:Benzodiazepines; D005442:Flumazenil; D005445:Flunitrazepam; C023842:lormetazepam; D008140:Lorazepam