Adult: For remission induction in patients with previously untreated, relapsed or refractory cases: In combination with cytarabine: 12 mg/m2 daily for 3 days via slow inj over 5-15 minutes into a free-flowing infusion of 0.9% NaCl solution or 5% dextrose in water; a 2nd induction cycle may be given as necessary. Alternatively, 8 mg/m2 daily for 5 days, either as monotherapy or combination therapy. Dosing interruption or dose reduction may be required according to individual safety or tolerability. Treatment protocols may vary among countries or individual products (refer to country- or product-specific guidelines). Child: For remission induction: In combination with cytarabine: 10-12 mg/m2 daily for 3 days via slow inj over 5-15 minutes into a free-flowing infusion of 0.9% NaCl solution or 5% dextrose in water. Dosing interruption or dose reduction may be required according to individual safety or tolerability. Treatment protocols may vary among countries or individual products (refer to country- or product-specific guidelines).
Intravenous Acute lymphoblastic leukaemia
Adult: As 2nd-line treatment of relapsed cases: 12 mg/m2 daily for 3 days via slow inj over 5-15 minutes into a free-flowing infusion of 0.9% NaCl solution or 5% dextrose in water, as a single agent. Dosing interruption or dose reduction may be required according to individual safety or tolerability. Treatment protocols may vary among countries or individual products (refer to country- or product-specific guidelines). Child: As 2nd-line treatment of relapsed cases: 10 mg/m2 daily for 3 days via slow inj over 5-15 minutes into a free-flowing infusion of 0.9% NaCl solution or 5% dextrose in water, as a single agent. Dosing interruption or dose reduction may be required according to individual safety or tolerability. Treatment protocols may vary among countries or individual products (refer to country- or product-specific guidelines).
Oral Acute myeloid leukaemia
Adult: For remission induction in patients with previously untreated, relapsed or refractory cases: Monotherapy: 30 mg/m2 daily for 3 days. Combination therapy with other anti-leukaemic agents: 15-30 mg/m2 daily for 3 days. Dosage depends on the patient's haematological status, and the dose of other cytotoxic agents when used concurrently.
Oral Advanced breast cancer
Adult: After failure of 1st-line chemotherapy not including anthracyclines: Monotherapy: 45 mg/m2 as a single dose or divided over 3 consecutive days; may be repeated every 3-4 weeks depending on haematological recovery. Max cumulative dose: 400 mg/m2.
Renal Impairment
Mild to moderate: Dose reduction may be needed. Severe: Contraindicated.
Hepatic Impairment
Mild to moderate: Dose reduction may be needed. Severe: Contraindicated.
Administration
May be taken with or without food. May be taken w/ a light meal.
Reconstitution
Powder for inj: Reconstitute 5 mg, 10 mg, or 20 mg vial with 5 mL, 10 mL, or 20 mL, respectively, of sterile water for inj to make a final concentration of 1 mg/mL. Solution for inj: May draw up 1 mg/mL solution into a syringe (for administration) or further dilute in 0.9% NaCl solution or dextrose 5% in water.
Incompatibility
IV: May precipitate with heparin, and degrade in alkaline solutions.
Contraindications
Severe cardiomyopathy, recent MI, severe arrhythmias, persistent myelosuppression, uncontrolled infections. Previous treatment with Max cumulative doses of idarubicin or other anthracyclines and anthracenediones. Severe hepatic and renal impairment. Pregnancy and lactation. Concurrent administration of live or live-attenuated vaccines.
Special Precautions
Patient with risk factors for cardiotoxicity (e.g. pre-existing heart disease, active or dormant CV disease, anaemia, bone marrow depression, infection, leukaemic pericarditis or myocarditis, prior or concomitant mediastinal/pericardial radiotherapy, coadministration with cardiotoxic drugs such as trastuzumab); active gastrointestinal disease with increased risk of bleeding. Ensure adequate hydration, and consider urine alkalinisation or anti-hyperuricaemic prophylaxis to minimise possible complications of tumour lysis syndrome. Avoid extravasation. Children. Mild to moderate hepatic and renal impairment.
Adverse Reactions
Significant: Gastrointestinal toxicity (including abdominal pain, nausea, vomiting, diarrhoea, mucositis or stomatitis), secondary leukaemia, hyperuricaemia (secondary to tumour lysis syndrome), oligospermia or azoospermia; phlebosclerosis, phlebitis/thrombophlebitis or extravasation (leading to local tissue necrosis) at the site of inj. Rarely, severe enterocolitis with perforation. Cardiac disorders: Bradycardia, sinus tachycardia, tachyarrhythmia, asymptomatic reduction of LVEF. General disorders and administration site conditions: Fever, chills. Gastrointestinal disorders: Abdominal burning sensation, gastrointestinal tract bleeding. Infections and infestations: Infections. Investigations: Elevated bilirubin and liver enzymes, ECG changes. Metabolism and nutrition disorders: Anorexia. Nervous system disorders: Headache. Renal and urinary disorders: Red colouration of urine. Skin and subcutaneous tissue disorders: Alopecia, itch, rash, sensitivity of irradiated skin (radiation recall reaction). Vascular disorders: Haemorrhage. Potentially Fatal: Cardiomyopathy which may lead to CHF, acute arrhythmias, severe myelosuppression (e.g. severe leucopenia, thrombocytopenia, neutropenia, anaemia) leading to infection or haemorrhage.
Evaluate pregnancy status prior to use in patients who may become pregnant. Obtain CBC with differential and platelet count, and cardiac (LVEF), hepatic (AST, ALT, bilirubin) and renal (serum creatinine) functions prior to and during therapy; serum electrolytes and uric acid. Monitor for signs of gastrointestinal toxicity, infections, extravasation at the infusion site.
Overdosage
Symptoms: Acute myocardial toxicity (e.g. cardiac failure, severe arrhythmias), severe myelosuppression, and increased severity of gastrointestinal toxicity. Management: Supportive treatment including blood transfusions, reverse-barrier nursing and administration of antibiotics. Symptomatic treatment of mucositis is required.
Drug Interactions
Additive myelosuppressive effects with other agents having a similar action (e.g. other anti-cancer drugs). Increased risk of cardiotoxicity with other cardiotoxic agents (e.g. trastuzumab, cyclophosphamide, paclitaxel) or other cardioactive compounds (e.g. Ca channel blockers). Potentially Fatal: Concurrent administration of live or live-attenuated vaccines may result in serious infections.
Action
Description: Mechanism of Action: Idarubicin is an antimitotic and cytotoxic agent that works by intercalating between deoxyribonucleic acid (DNA) base pairs and interacting with topoisomerase II, resulting in blockade of DNA and ribonucleic acid (RNA) synthesis, and fragmentation of DNA. Pharmacokinetics: Absorption: Rapidly absorbed (oral). Absolute bioavailability: 18-39% (oral). Time to peak plasma concentration: 2-4 hours (oral). Distribution: IV: Rapidly distributed into body tissues. Plasma protein binding: 97% (idarubicin); 94% (idarubicinol). Metabolism: Extensively metabolised in the liver primarily to idarubicinol (active metabolite). Excretion: Oral: Mainly via faeces (61%, primarily as idarubicinol); urine (30%; 1-2% as unchanged drug, approx 5% as idarubicinol). Terminal plasma half-life: 10-35 hours (idarubicin). Plasma half-life: 33-60 hours (idarubicinol). IV: Mainly via bile; urine (lesser extent). Terminal half-life: 15 hours (idarubicn); 72 hours (idarubicinol). Plasma half-life: Approx 20-22 hours (idarubicin); approx 45 hours (idarubicinol).
Chemical Structure
Idarubicin Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 42890, Idarubicin. https://pubchem.ncbi.nlm.nih.gov/compound/Idarubicin. Accessed Aug. 25, 2021.
Storage
Cap: Store below 25°C. Powder for inj: Store at or below 25°C. Reconstituted solution: Stable for at least 48 hours between 2-8°C and 24 hours between 20-25°C. Protect from light. Solution for inj: Store between 2-8°C. Protect from light. Do not freeze. This is a cytotoxic drug. Follow applicable procedures for receiving, handling, administration, and disposal.
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