Pharmacokinetics of diltiazem in selected animal species and human beings

摘要: The absorption, distribution and elimination of diltiazem hydrochloride in rodent canine species are reviewed. drug is well absorbed but undergoes first pass metabolism after oral administration. Diltiazem extensively distributed, 52 to 81 percent bound serum protein, depending on the studied. metabolized liver by several pathways; deacetylation, N-demethylation, O-demethylation primary degradative steps. metabolites excreted urine feces, indicating that biliary excretion occurs. There some evidence for enterohepatic cycling. rapidly eliminated (t 1/2 = 2.24 hours) beagle dogs, relatively short half-life appears be a result high level plasma clearance (46.1 +/- 4.8 ml/min/per kg body weight). A comparison with hepatic blood flow dog indicates at rate dependent flow.