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RO 15‐1788 antagonises the central effects of diazepam in man without altering diazepam bioavailability.
Author(s) -
Darragh A.,
Lambe R.,
Kenny M.,
Brick I.,
Taaffe W.,
O'Boyle C.
Publication year - 1982
Publication title -
british journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.216
H-Index - 146
eISSN - 1365-2125
pISSN - 0306-5251
DOI - 10.1111/j.1365-2125.1982.tb04956.x
Subject(s) - diazepam , benzodiazepine , antagonist , pharmacology , medicine , placebo , oral administration , bioavailability , anesthesia , alternative medicine , receptor , pathology
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.