C10AA03 - Pravastatin |
Propably not porphyrinogenic |
PNP |
Rationale
Pravastatin is not a substrate of CYP enzymes.
Chemical description
HMG-CoA reductase inhibitor.
Therapeutic characteristics
Pravastatin is indicated for the treatment of hypercholesterolemia and cardiovascular prevention.
Less common side effects are dyspepsia, abdominal pain, nausea, vomiting, constipation and diarrhoea.
Metabolism and pharmakokinetics
Pravastatin is not a substrate of CYP3A enzymes (Flockhart 2007) and is metabolized by non-P450-dependent pathways (Corsini 1999, Masubuchi 2007) and is also excreted mainly unchanged (Neuvonen 2008). 50 % is bound to plasma proteins and the elimination half-life is 1.5-2 hours.
In vitro studies have shown that pravastatin has no effect on either CYP3A or CYP2B6 (Dickins 2004, Kocarek 2002).
Personal communication
Thunell, patient report (n=1): tolerated.
IPNet drug reports
Uneventful use reported in 4 patients with acute porphyria.
References
- Scientific articles
- Corsini A, Bellosta S, et al. New insights into the pharmacodynamic and pharmacokinetic properties of statins. Pharmacol Ther. 1999 Dec;84(3):413-28. #1322
- Dickins M. Induction of cytochromes P450. Curr Top Med Chem. 2004;4(16):1745-66. PMID 15579106. #1323
- Kocarek TA, Dahn MSm, et al. Regulation of CYP2B6 and CYP3A expression by hydroxymethylglutaryl coenzyme A inhibitors in primary cultured human hepatocytes. Drug Metab Dispos. 2002 Dec;30(12):1400-5. PMID 12433810. #4417
- Masubuchi Y, Horie T. Toxicological significance of mechanism-based inactivation of cytochrome p450 enzymes by drugs. Crit Rev Toxicol. 2007 Jun;37(5):389-412. PMID 17612953. #1326
- Neuvonen PJ, Backman JT, Niemi M. Pharmacokinetic comparison of the potential over-the-counter statins simvastatin, lovastatin, fluvastatin and pravastatin. Clin Pharmacokinet. 2008;47(7):463-74. PMID 18563955. #1327
- Drug interaction databases
- Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). #1213
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