Elimination kinetics of the novel prodrug cinazepam possessing psychotropic activity in mice.

2011

Abstract The kinetics of excretion of the novel tranquilizer cinazepam (3-hydroxy-7-bromo-5-( ortho -chlorophenyl)-1,2-dihydro-3H-1,4-benzdiazepin-2-one hemisuccinate (I)) in mice after a single administration and different schemes of multiple administration were determined. Mass balance was studied daily in excretions of mice (feces and urine) for 5-10 days. We observed that monoexponen-tial renal excretion of 14 C-cinazepam and its metabolites predominated with all dosage regimens. Cinazepam and its metabolites were almost fully (> 90%) eliminated in urine and feces over the period of study (5-10 days), which means that no significant accumulation of the drug in the body occurred. The kin…