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RO 15-1788: benzodiazepine antagonist

Six healthy volunteers received a single oral dose of 20mg diazepam alone and in combination with oral RO 15-1788 [Roche] 200mg. While diazepam did not affect immediate recall, it did significantly impair learning capacity. This effect on learning capacity was abolished by concurrent RO 1 5-1788. The impairment of psychomotor performance and changes in subjective mood were most pronounced 2.5 hours after diazepam alone. These effects were completely prevented by concurrent RO 15-1788. 26.5 hours after the administration of the diazepam + RO 15-1788 combination there was a mild degree of residual sedation which was not seen at the same time after the administration of diazepam alone. RO 15-1788 does not appear to affect the bioavailability of diazepam since the AUCs for diazepam were similar with and without concurrent RO 15-1788. The antagonistic effects of RO 15-1788 are probably a result of activity at the benzodiazepine receptor level. O'Boyle, C. et al.: British Journal of Anaesthesia 55: 349 (Apr 1983)

0156-2703/83/0528-0005/0$01.00/0 © ADIS Press INPHARMA 28 May 1983 5