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

Br J Clin Pharmacol. 1982 Nov;14(5):677-82. doi: 10.1111/j.1365-2125.1982.tb04956.x.

Abstract

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.

Publication types

  • Clinical Trial
  • Randomized Controlled Trial

MeSH terms

  • Adult
  • Benzodiazepinones / pharmacology*
  • Biological Availability
  • Diazepam / antagonists & inhibitors*
  • Diazepam / blood
  • Double-Blind Method
  • Emotions / drug effects
  • Flumazenil
  • Humans
  • Male
  • Psychomotor Performance / drug effects

Substances

  • Benzodiazepinones
  • Flumazenil
  • Diazepam