• Molecular NameDiltiazem
  • Synonymd-cis-Diltiazem
  • Weight386.664
  • Drugbank_IDDB00343
  • ACS_NO42399-41-7
  • Show 3D model
  • LogP (experiment)2.7
  • LogP (predicted, AB/LogP v2.0)7.38
  • pka7.7
  • LogD (pH=7, predicted)7.38
  • Solubility (experiment)0.465 mg/ml
  • LogS (predicted, ACD/Labs)(ph=7)-8.22
  • LogSw (predicted, AB/LogsW2.0)0.0
  • Sw (mg/ml) (predicted, ACD/Labs)0.0
  • No.of HBond Donors1
  • No.of HBond Acceptors1
  • No.of Rotatable Bonds5
  • TPSA20.23
  • StatusFDA approved
  • AdministrationN/A
  • PharmacologyA non-DHP member of the group of drugs known as benzothiazepines, which are a class of calcium channel blockers, used in the treatment of hypertension, angina pectoris, and some types of arrhythmia. It is also an effective preventive medication for migraine. It is a class 3 anti-anginal drug, and a class IV antiarrhythmic. It incites very minimal reflex sympathetic changes.
  • Absorption_value91.0
  • Absorption (description)After oral administration, diltiazem is rapidly absorbed (approx. 90%) from the gastro-intestinal tract
  • Caco_2-4.38
  • Bioavailability38.0
  • Protein binding78.0
  • Volume of distribution (VD)3.3 L/kg
  • Blood/Plasma Partitioning ratio (D_blood)14 to 23% unbound drug in serum.
  • MetabollsmUndergoes extensive first-pass hepatic metabolism via deacetylation, N-demethylation, O-demethylation and oxidative deamination. Metabolites are A1, MA, MB, MX, M1, M2, M4 and M6.
  • Half life4.4 h
  • Excretion2 to 4% of administered dose appears unchanged in the urine. Metabolites are excreted via bile, urine and faeces, and it can be found in breast milk.
  • Urinary Excretion<4
  • Clerance11.8 ml/min/kg
  • ToxicityNine diltiazem metabolites have been identified in the urine of humans. These metabolites are more slowly excreted (with a half-life of total radioactivity of approximately 20 hours), and attain concentrations in excess of diltiazem The two primary metabolites of diltiazem are desacetyldiltiazem and desmethyldiltiazem. The desacetyl metabolite is approximately 25% to 50% as potent a coronary vasodilator as diltiazem and is present in plasma at concentrations of 10% to 20% of parent diltiazem.
  • LD50 (rat)N/A
  • LD50 (mouse)LD50=740mg/kg