Idarubicin (Lyophilisate) Instructions for Use

Marketing Authorization Holder

OMK, LLC (Russia)

Manufactured By

Biozenta Lifescience Pvt. Ltd. (India)

ATC Code

L01DB06 (Idarubicin)

Active Substance

Idarubicin (Rec.INN WHO registered)

Dosage Form

Idarubicin

Lyophilizate for the preparation of solution for intravenous administration 5 mg

Dosage Form, Packaging, and Composition

Lyophilizate for the preparation of solution for intravenous administration

5 mg – vials – carton packs – By prescription

Pharmacotherapeutic Group

Antineoplastic agent, antibiotic

Pharmacological Action

Antineoplastic agent from the group of anthracycline antibiotics. The mechanism of action is associated with the induction of DNA breaks and interaction with topoisomerase II.

Pharmacokinetics

After intravenous administration, C_max in nucleated blood cells and bone marrow cells is reached within a few minutes. It is metabolized both in the liver and outside it with the formation of the main metabolite idarubicinol, which does not differ in activity from idarubicin. The concentrations of idarubicin and idarubicinol in nucleated blood cells and bone marrow cells are 400 and 200 times higher, respectively, than in blood plasma. The binding of idarubicin to plasma proteins is 97%, and of idarubicinol – 94%.

The T_1/2 of idarubicin averages 22 hours, and that of idarubicinol is 2 times longer. It is excreted by the kidneys – less than 5% and with bile in the form of idarubicinol.

Indications

Acute myeloblastic leukemias in adults.

ICD codes

Dosage Regimen

Determine the dosage individually based on the therapeutic protocol, disease stage, and patient’s hematological status.

Administer intravenously. The typical induction dose for adults with acute myeloid leukemia is 12 mg/m² daily for 3 days, in combination with cytarabine.

Adjust the dose for patients with hepatic impairment. Reduce the dose by 50% if serum bilirubin is between 21.4 to 51.3 µmol/L. Omit the dose if bilirubin exceeds 51.3 µmol/L.

Adjust the dose for patients with renal impairment. Reduce the dose if serum creatinine is elevated.

Do not exceed the cumulative dose limit to minimize the risk of cardiotoxicity.

Reevaluate the regimen based on the patient’s response and the severity of myelosuppression. A second induction course may be required.

Monitor complete blood counts, liver and kidney function, and cardiac function (ECG, echocardiography) prior to and during therapy.

Adverse Reactions

From the hematopoietic system leukopenia, thrombocytopenia, anemia.

From the cardiovascular system cardiomyopathy, development of heart failure, arrhythmias, myocardial infarction.

From the digestive system nausea, vomiting, mucositis, abdominal pain, diarrhea; rarely – enterocolitis with perforation, impaired liver function.

From the urinary system nephropathy due to increased formation of uric acid.

Dermatological reactions alopecia.

Contraindications

Severe hematopoietic disorders, severe heart disease, pregnancy, hypersensitivity to idarubicin, severe liver dysfunction (bilirubin level above 85.5 µmol/ml).

Use in Pregnancy and Lactation

Idarubicin is contraindicated during pregnancy. If it is necessary to use during lactation, the issue of discontinuing breastfeeding should be decided.

Women of childbearing potential receiving idarubicin therapy should use reliable methods of contraception.

In experimental studies, the teratogenic and embryotoxic effects of idarubicin have been established.

Use in Hepatic Impairment

Contraindicated in severe liver dysfunction (bilirubin level above 85.5 µmol/ml). In case of impaired liver function, dose adjustment of idarubicin is necessary depending on the plasma bilirubin level.

Use in Renal Impairment

In case of impaired renal function, dose adjustment of idarubicin is necessary depending on the plasma creatinine level.

Geriatric Use

The risk of developing a cardiotoxic effect is increased in patients over 60 years of age.

Special Precautions

The use of idarubicin is not recommended in patients with chickenpox (including recently had or after contact with sick people), with herpes zoster, or other acute infectious diseases.

Idarubicin should be used with caution in patients with gout or nephrolithiasis (including in the anamnesis).

In case of impaired liver or kidney function, dose adjustment of idarubicin is necessary depending on the plasma bilirubin or creatinine level.

The risk of developing a cardiotoxic effect is increased in patients over 60 years of age and in patients with a history of cardiovascular disease, as well as in the case of previous therapy with anthracyclines in a high total dose.

Vaccination of patients and their family members is not recommended.

During treatment, monitoring of peripheral blood counts, plasma uric acid concentration, laboratory parameters of liver and kidney function, regular ECG, cardiac ultrasound, radiography, and determination of cardiac stroke volume are necessary.

In case of extravasation, local tissue necrosis at the injection site is possible.

Against the background of idarubicin use, urine may turn red.

In experimental studies, the carcinogenic and mutagenic effects of idarubicin have been established.

Drug Interactions

With the simultaneous use of idarubicin with drugs that have a myelotoxic effect, an increase in toxic effects on hematopoiesis is possible.

When used in combination with uricosuric drugs, the risk of developing nephropathy increases.

Storage Conditions

Store at 2°C (36°F) to 30°C (86°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.