Pharmacokinetics and metabolism of diltiazem in man.
Dilitazem, a coronary vasodilating agent, after oral administration of four different doses, was well and rapidly absorbed. The pharmacokinetics of the drug followed a two-compartment model, with a rapid distribution and an elimination with a half-life of 4-7 hours. After chronic treatment the pharmacokinetic parameters were practically unchanged and therefore no accumulation of the drug was observed. The comparison between capsule and tablet preparations showed that both forms had a similar bioavailability. Diltiazem was extensively metabilized and only a few percent of the drug was found in urine. Several metabolites, also present as conjugates, have been identified by means of gas chromatography-mass spectrometry.
D000284:Administration, Oral; D000328:Adult; D001552:Benzazepines / Q000378:metabolism*; D001682:Biological Availability; D002214:Capsules; D004110:Diltiazem / Q000008:administration & dosage / Q000097:blood / Q000378:metabolism*; D005260:Female; D006801:Humans; D007700:Kinetics; D008297:Male; D008875:Middle Aged; D008954:Models, Biological; D013607:Tablets
D001552:Benzazepines; D002214:Capsules; D013607:Tablets; D004110:Diltiazem