Pharmacokinetics and metabolism of diltiazem in man

Acta Cardiol. 1980;35(1):35-45.


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.

MeSH terms

  • Administration, Oral
  • Adult
  • Benzazepines / metabolism*
  • Biological Availability
  • Capsules
  • Diltiazem / administration & dosage
  • Diltiazem / blood
  • Diltiazem / metabolism*
  • Female
  • Humans
  • Kinetics
  • Male
  • Middle Aged
  • Models, Biological
  • Tablets


  • Benzazepines
  • Capsules
  • Tablets
  • Diltiazem