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. 2015 Feb;21(6):806–822. doi: 10.2174/1381612820666141024151119

Table 3.

Detailed metabolic profile of calcium channel blockers.

Calcium channel blocker name Metabolites Enzymes References
Amlodipine Pyridine derivative CYP3A4 [69]
  De-amino amlodipine CYP3A4 [69]
  Ester hydrolysis of the S-methoxycarbonyl group Carboxylesterases [69]
  Amlodipine glucuronides UDP-Glucuronosyltransferase [69]
Diltiazem N-desmethyl diltiazem CYP3A4 [70]
  O-desacetyl-N-desmethyl diltiazem CYP3A4 [70]
Felodipine Dehydro felodipine CYP3A4 [71]
Isradipine Pyridine of isradipine CYP3A4 [72]
  Carboxylic acid of isradipine CYP3A4 [72]
  Carboxylic acid of isradipine pyridine CYP3A4 [72]
Nifedipine Pyridine of nifedipine CYP3A4 [79]
  Carboxylic acid of nifedipine CYP3A4 [79]
  Carboxylic acid of nifedine pyridine CYP3A4 [79]
Nimodipine Dehydro nimopidine CYP3A4 [74, 98]
  Carboxylic acid of nimopidine CYP3A4 [74, 98]
  Cardoxylic acid of dehydronimopidine CYP3A4 [74, 98]
Nisoldipine Hydroxylation of the isobutyl moiety CYP3A4 [75]
  Dehydrogenation of the 1, 4-dihydropyridine system CYP3A4 [75]
  Oxidative ester cleavage CYP3A4 [75]
  Hydroxylation of one of the methyl groups in 2-position and subsequent oxidation to the carboxylic acid CYP3A4 [75]
  Hydroxylation of one of the methyl groups in 6-position and subsequent oxidation to the carboxylic acid CYP3A4 [75]
  Oxidation of one of the methyl groups of the isobutyl moiety to the carboxyl group reduction of the aromatic nitro group CYP3A4 [75]
  Glucuronidation UDP-Glucuronosyltransferase [75]
Nitrendipine Dehydro nitredipine CYP3A4 [76]
  Carboxylic acid of nitrendipine CYP3A4 [76]
  Cardoxylic acid of dehydronitrendipine CYP3A4 [76]
Verapamil O-Desmethyl verapamil   [77, 78]
  O-Desmethyl verapamil (D-702) CYP2C8, CYP2C18, CYP2C9 [77, 78]
  O-Desmethyl verapamil (D-703) CYP2C8, CYP2C9 [77, 78]
  Norverapamil CYP2C8, CYP3A4, CYP3A5, CYP1A2 [77, 78]
  D-617 CYP2C8 [77, 78]