Pharmacology · Antitumour antibiotics
Idarubicin !
A more fat-soluble anthracycline that enters cells quickly. Used with cytarabine to treat acute myeloid leukaemia in adults.
Updated 2026-11-01
The crystal shows idarubicin intercalated in a short DNA duplex.
Mechanism of action
Idarubicin is daunorubicin without the methoxy group at position 4, which makes it highly lipophilic and speeds its uptake into cells. It intercalates in DNA and inhibits topoisomerase II, causing DNA breaks in leukaemic blasts.
- High lipophilicity: fast entry into cells
- Intercalates in DNA and traps topoisomerase II
- DNA breaks kill leukaemic blasts
Pharmacokinetics
- Absorption
- Given slowly into a running intravenous infusion.
- Elimination
- Liver and kidney clearance; doses are reduced in hepatic or renal impairment.
Indications
- Acute myeloid leukaemia in adults, with other antileukaemic drugs.
Adverse effects
Common
- Nausea, vomiting and mouth sores
- Hair loss
- Abnormal liver tests
Contraindications
- Pre-existing bone-marrow suppression from earlier treatment, unless the benefit justifies the risk
- Pre-existing heart disease or high previous anthracycline doses: the benefit is weighed against the cardiac risk first
Key interactions
- Previous anthracyclines or other cardiotoxic drugs
- Higher risk of cardiac toxicity.
- Mediastinal radiotherapy
- Raises the risk of heart damage.
What is monitored
- Blood counts closely during and after induction
- Ejection fraction (echocardiogram or MUGA) before, during and after treatment, by the same method each time.
- Liver and kidney function before each dose
Administration and safety
- Vesicant: given only into a free-flowing intravenous line, never intramuscularly or subcutaneously; the site is checked before and during the dose.
- Suspected extravasation (burning, stinging, swelling): stop the drug, try to aspirate without flushing, apply ice intermittently, elevate the limb and notify; dexrazoxane may be used in adults.
- Look-alike risk with daunorubicin, doxorubicin and epirubicin: the full name is checked.
- Hazardous drug: prepared and given following hazardous-drug handling procedures (impervious gloves, no skin contact) and disposed of as cytotoxic waste.
Nursing care
- Independent double check of drug, patient, route and cycle before giving it (high-alert medicine).
- Neutropenic and bleeding precautions; daily check for fever, bleeding and mouth sores.
- Teaching: report shortness of breath, swelling of the legs, palpitations or fast weight gain, even months after treatment.
Pregnancy and breastfeeding
Used in pregnancy only if the benefit justifies the risk to the fetus; a fetal death after second-trimester exposure has been reported.
Test yourself
Think of the answer, then tap the question to see it.
What structural change distinguishes idarubicin from daunorubicin, and what does it change?
It lacks the methoxy group at position 4, making it more lipophilic with faster cellular uptake.
What is idarubicin's indication?
Acute myeloid leukaemia in adults, combined with other antileukaemic drugs.
Which toxicity occurs in essentially every patient given therapeutic doses of idarubicin?
Severe myelosuppression.
Related drugs
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Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: DailyMed - IDARUBICIN HYDROCHLORIDE injection, solution (DailyMed (U.S. National Library of Medicine), 2025); Goodman & Gilman's The Pharmacological Basis of Therapeutics, 14th ed., ch. 70 (McGraw Hill, 2023); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).
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Representative model, for educational purposes only.