L01DB06 - Idarubicin |
Propably not porphyrinogenic |
PNP |
Rationale
Substrate of CYP 2C9 and 2D6, but no reports of interference with CYP-metabolism of other drugs. Not listed as CYP-inducer. Side effects such as nausea and vomiting may be potentially porphyrinogenic through reduction in caloric intake.
Chemical description
Idarubicin is a semisynthetic anthracycline.
Therapeutic characteristics
Idarubicin is an anthracycline antibiotic with antineoplastic actions similar to those of doxorubicin. It is used alone or with other drugs, in the treatment of acute myeloid leukaemias, acute lymphoblastic leukaemia, and advanced breast cancer. It is administered intravenously. Common adverse reactions of idarubicin that can be confused with an acute porphyric attack are acute nausea, abdominal pain and vomiting. Side effects such as nausea and vomiting may be potentially porphyrinogenic through reduction in caloric intake.
Metabolism and pharmacokinetics
Idarubicin is extensively metabolismed in the liver. It is rapidly metabolized by bioreduction via P450 reductases to idarubicinol, the principal active metabolite (Celic, 2008). No observations of interference with CYP-metabolism of other drugs. Colburn found that idarubicin is a substrate of CYP 2D6 AND 2C9, and an inhibitor of 2D6. No observations of acceleration of CYP metabolism of other drugs and not listed as CYP inducer (Rendic, 2002).
References
- Scientific articles
- Rendic, S. Summery of information on human CYP enzymes: human P450 metabolism. Drug metabolism reviews 2002; 34(1&2), 83-448. #1025
- Celik H, Arinç E. Bioreduction of idarubicin and formation of ROS responsible for DNA cleavage by NADPH-cytochrome P450 reductase and its potential role in the antitumor effect. J Pharm Pharm Sci. 2008;11(4):68-82. PMID 19183515. #2012
- Colburn DE, Giles FJ, et al. In vitro evaluation of cytochrome P450-mediated drug interactions between cytarabine, idarubicin, itraconazole and caspofungin. Hematology. 2004 Jun;9(3):217-21. PMID 15204103. #4580
- Drug reference publications
- McEvoy GK, editor. Idarubicin. The AHFS Drug Information 2008. Bethesda, MD: American Society of Health-System Pharmacists; 2009. Electronic version (06.05.10). #2014
- Sweetman SC, editor. Martindale: The complete drug reference. Idarubicin. Pharmaceutical Press 2009. #2015
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