RO 15‐1788 antagonises the central effects of diazepam in man without altering diazepam bioavailability

• Published in: British journal of clinical pharmacology Vol. 14; no. 5; pp. 677 - 682
• Main Authors: Darragh, A., Lambe, R., Kenny, M., Brick, I., Taaffe, W., O'Boyle, C.
• Format: Journal Article
• Language: English
• Published: Oxford, UK Blackwell Publishing Ltd 01.11.1982
• Subjects: Adult; Benzodiazepinones - pharmacology; Biological Availability; Diazepam - antagonists & inhibitors; Diazepam - blood; Double-Blind Method; Emotions - drug effects; Flumazenil; Humans; Male; Psychomotor Performance - drug effects
• ISSN: 0306-5251; 1365-2125
• DOI: 10.1111/j.1365-2125.1982.tb04956.x

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.