Acute Porphyria Drug Database

C08CA03 - Isradipine
Propably not porphyrinogenic
PNP

Side effects
Abdominal discomfort is a common side effect of isradipine.
Rationale
Isradipine is a substrate CYP 3A4. It is also a week inhibitor of CYP 3A4, but it is not a mechanism- based inhibitor.
Chemical description
Dihydropyridine calcium antagonist.
Therapeutic characteristics
Isradipine is used in the treatment of essential hypertension.
Metabolism and pharmacokinetics
Isradipine is a substrate of CYP3A4. At least 6 biologically inactive metabolites have been identified and mainly consist of mono acids of the pyridine derivative and a cyclic lactone product (Micromedex). In an in vitro study isradipine was found to be a week competitive inhibitor (Wang 1999). The results of an in -vivo study indicate that isradipine is not a clinically significant inhibitor of CYP3A4 in humans (Beckman 1999) and the SPC also states that isradipine does not seem to inhibit the cytochrome P450 enzymes, in particular CYP3A4, to a clinically significant extent.
Personal communication
Uneventful use reported in one patient (C. Andersson).
IPNet drug reports
Uneventful use reported in 1 patient with acute porphyria.

References

  1. Scientific articles
  2. Backman JT, Wang JS et al. Mibefradil but not isradipine substantially elevates the plasma concentrations of the CYP3A4 substrate triazolam. Clin Pharmacol Ther. 1999 Oct;66(4):401-7. #1286
  3. Wang JS, Wen X, et al. Midazolam alpha-hydroxylation by human liver microsomes in vitro: inhibition by calcium channel blockers, itraconazole and ketoconazole. Pharmacology & toxicology , 1999, Vol.85(4), p.157-161 PMID 10563513. #4405
  4. Drug reference publications
  5. Micromedex® 2.0 (online). Labetalol. Comparative efficacy. (Drugdex System). (Sist oppdatert:2. november 2015). #1287
  6. Summary of Product Characteristics
  7. The electronic Medicines Compendium (emc). Summary of Product Characteristics (SPC). Prescal. #1288

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