The pharmacological profile of chlordesmethyldiazepam and other benzodiazepines

Abstract

The pharmacological profile of chlordesmethyldiazepam was studied in mice and compared with that of other benzodiazepines (diazepam, lorazepam, clonazepam, nitrazepam, oxazepam, flunitrazepam, medazepam and chlordiazepoxide). All the drugs were administered perorally and their anticonvulsive activity (antagonism towards pentetrazole-induced clonic convulsions), anxiolytic action (the four-plate test), myorelaxant activity (the rota-rod test), sedative effect (inhibition of the locomotor activity) and neurotoxic effect (abolition of the righting reflex) were estimated. Chlordesmethyldiazepam revealed an anticonvulsive action (ED50 = 0.11 mg/kg), anxiolytic activity (MED = 2 mg/kg), myorelaxant action (ED50 = 17.5 mg/kg), sedative effect (ED50 = 34 mg/kg) and neurotoxic action (NTD50 = 190 mg/kg). Considering the potency of action (ED50) in respective tests and the therapeutic indices (NTD50/ED50 ratio), chlordesmethyldiazepam in respect of its profile resembles most lorazepam and diazepam.