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idarubicin

Pharmacology/OncologyHematologicCardiovascularIntegumentary

Summary

Idarubicin is an anthracycline chemotherapeutic agent, most commonly used in the treatment of acute myeloid leukemia (AML), often in combination with cytarabine (7+3 regimen). Like other anthracyclines, its major dose-limiting toxicity is cardiotoxicity, and it also causes myelosuppression and alopecia.

Detail

Idarubicin is a semisynthetic anthracycline antibiotic derived from daunorubicin, with increased lipophilicity allowing greater cellular uptake and oral bioavailability (though typically given IV). Mechanism of action: intercalates into DNA, inhibits topoisomerase II, leading to DNA strand breaks and generation of free radicals that damage DNA, RNA, and cell membranes, ultimately causing apoptosis of rapidly dividing cells.

Clinical use: Primarily used in induction therapy for acute myeloid leukemia (AML), typically combined with cytarabine (the '7+3' regimen—7 days of cytarabine, 3 days of anthracycline). Also used in acute promyelocytic leukemia (APL) in combination with all-trans retinoic acid (ATRA).

Adverse effects (shared with other anthracyclines like doxorubicin and daunorubicin): - Cardiotoxicity: dose-dependent, cumulative, can cause dilated cardiomyopathy and arrhythmias; mechanism involves free radical formation and lipid peroxidation of cardiac myocyte membranes (cardiac tissue has relatively low catalase/antioxidant defenses). Dexrazoxane (iron chelator) can be used to reduce cardiotoxicity risk. - Myelosuppression (neutropenia, thrombocytopenia) - Alopecia - Severe local tissue necrosis if extravasation occurs (vesicant) - Red-orange discoloration of urine - Secondary malignancies (e.g., therapy-related AML) with long-term use due to topoisomerase II inhibition

High-yield board associations: Anthracyclines (doxorubicin, daunorubicin, idarubicin, epirubicin) all share the 'cardiotoxicity + myelosuppression + alopecia' toxicity triad. Idarubicin is specifically associated with AML induction chemotherapy. Monitor cardiac function (ECHO/MUGA) before and during treatment due to cumulative dose-related cardiotoxicity risk.

Sources

  • First Aid for the USMLE Step 1
  • Katzung's Basic and Clinical Pharmacology
  • Goldman-Cecil Medicine
  • UpToDate: Acute myeloid leukemia treatment regimens

Reviewed by Medusa editorial — medical student review. Information here is for study reference only and is not medical advice. Spotted an error? Let us know.