RO 15-1788 antagonises the central effects of diazepam in man without altering diazepam bioavailability.
1 In a double-blind, placebo controlled study, the efficacy of Ro 15-1788, a new benzodiazepine antagonist, in blocking the cognitive, psychomotor and subjective effects of diazepam, was investigated in a group of six healthy male volunteers. 2 The central effects of orally administered diazepam (40 mg) were most pronounced 1 h after dosing and persisted for 9 h with decreasing severity. 3 Concurrent oral administration of Ro 15-1788 (200 mg) completely prevented the impairment in cognitive and psychomotor function observed after diazepam alone. 4 The duration of action of Ro 15-1788 was shorter than that of diazepam. 5 Plasma diazepam levels after administration of the diazepam/antagonist combination were very similar to those observed following diazepam alone.
D000328:Adult; D001570:Benzodiazepinones / Q000494:pharmacology*; D001682:Biological Availability; D003975:Diazepam / Q000037:antagonists & inhibitors* / Q000097:blood; D004311:Double-Blind Method; D004644:Emotions / Q000187:drug effects; D005442:Flumazenil; D006801:Humans; D008297:Male; D011597:Psychomotor Performance / Q000187:drug effects
D001570:Benzodiazepinones; D005442:Flumazenil; D003975:Diazepam