Prediction of the parameters of the accumulation of 1,4-benzodiazepine derivatives in the body of mice based on their excretory kinetics
Vasilinin, G.B.; Zin'kovski, G.V.; Golovenko, N.I.; Stankevich, E.A.; Andronati, S.A.
Farmakologiia i Toksikologiia 49(6): 88-92
1986
ISSN/ISBN: 0014-8318 PMID: 2880750 Document Number: 274463
Kinetics of 14C-7-bromo-5-phenyl-1,2-dihydro-3H-1,4-benzodiazepin-2-one (I) excretion from the mouse body following a single and long-term administration of the compound was studied. It was shown that kinetics of excretion of total radioactive material in the urine and feces is a sum of monoexponential processes. Prediction of the compound accumulation in the mouse body during its long-term administration was performed. Parameters of accumulation of the compound, diazepam, chlordiazepoxide and phenazepam were compared. Significant, reciprocally compensated changes in relative efficacy and the rate of excretion of total radioactivity in the urine and feces during a long-term administration were noted. It is recommended to take into consideration the events studied at a chronic administration of derivatives of 1,4-benzodiazepine.