Interaction potential of lercanidipine, a new vasoselective dihydropyridine calcium antagonist.
Article Details
- CitationCopy to clipboard
Klotz U
Interaction potential of lercanidipine, a new vasoselective dihydropyridine calcium antagonist.
Arzneimittelforschung. 2002;52(3):155-61. doi: 10.1055/s-0031-1299873.
- PubMed ID
- 11963641 [ View in PubMed]
- Abstract
Using some calcium channel blockers of the dihydropyridine-type (amlodipine (CAS 88150-42-9, felodipine (CAS 72508-76-3), lercanidipine (CAS 100472-26-7), nifedipine (CAS 21829-25-4), nitrendipine (CAS 39562-70-4)) as example the interaction potential of these substances will be compared in terms of affecting metabolism and transport of drugs. The cytochrome P450 (CYP) isoform CYP3A4 and the P-glycoprotein (P-gp), respectively, will have a high impact for both pharmacokinetic processes, as all 5 calcium channel blockers are substrates of CYP3A4 and in addition nifedipine, nitrendipine and felodipine represent inhibitors of P-gp, which can cause an increase in the plasma levels of digoxin (model substrate of P-gp). If inducers (e.g. rifampicin, anticonvulsants, St John's wort) or inhibitors (ketoconazole, itraconazole, erythromycin, clarithromycin, nefazodone, fluvoxamine, fluoxetine, sertraline, ritonavir, indinavir, amprenavir, saquinavir or grapefruit juice) of CYP3A4 are concomitantly administered pharmacokinetic interactions could be expected to a variable extent. Some alternative drugs are mentioned which will not affect CYP3A4. In addition to these putative pharmacokinetic interactions also pharmacodynamic interactions with other cardiovascular active substances might be considered and some caution should be exercised if vasodilators are given as comedication.
DrugBank Data that Cites this Article
- Drug Enzymes
Drug Enzyme Kind Organism Pharmacological Action Actions Erythromycin Cytochrome P450 3A4 Protein Humans NoSubstrateInhibitorDetails Fluoxetine Cytochrome P450 3A4 Protein Humans NoSubstrateInhibitorDetails Fluvoxamine Cytochrome P450 3A4 Protein Humans UnknownSubstrateInhibitorDetails Grapefruit Cytochrome P450 3A4 Protein Humans UnknownInhibitorDetails Itraconazole Cytochrome P450 3A4 Protein Humans NoSubstrateInhibitorDetails Lercanidipine Cytochrome P450 3A4 Protein Humans UnknownSubstrateInhibitorDetails Nefazodone Cytochrome P450 3A4 Protein Humans UnknownSubstrateInhibitorDetails Nitrendipine Cytochrome P450 3A4 Protein Humans UnknownSubstrateDetails Sertraline Cytochrome P450 3A4 Protein Humans UnknownSubstrateInhibitorDetails St. John's Wort Cytochrome P450 3A4 Protein Humans UnknownSubstrateInducerActivatorDetails - Drug Interactions
Drugs Interaction Integrate drug-drug
interactions in your softwareDigoxinNefazodone The serum concentration of Digoxin can be increased when it is combined with Nefazodone. 
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