Factors affecting the metabolism and distribution of phenazepam in subcellular fractions of animal hepatocytes

Metabolism and intracellular distribution of 14C-phenazepam and its derivatives were studied in rat and mice liver tissue. Phenazepam was found mainly in microsomal fraction of the animal hepatocytes, where rapid turnover of the substance occurred. The metabolites formed were uniformly distributed in the cell and penetrated into other tissues. The rates of phenazepam metabolites conjugation and binding with proteins were dissimilar in rat and mice tissues. Metabolism of phenazepam was shown to depend on doses of the drug administered. Incorporation of phenazepam into liposomes affected distinctly its turnover in mice tissues.