Idalek (Solution) Instructions for Use

Marketing Authorization Holder

Pharmatsel, LLC (Russia)

Manufactured By

Biolek Joint-Stock Company, JSC (Ukraine)

ATC Code

L01DB06 (Idarubicin)

Active Substance

Idarubicin (Rec.INN registered by WHO)

Dosage Form

Idalek

Solution for intravenous administration 1 mg/1 ml: 5 ml or 10 ml fl. 1 or 10 pcs.

Dosage Form, Packaging, and Composition

10 ml – vials (1) – cardboard packs.
10 ml – vials (10) – cardboard packs.
5 ml – vials (1) – cardboard packs.
5 ml – vials (10) – cardboard packs.

Clinical-Pharmacological Group

Antineoplastic antibiotic

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

Establish the dosage regimen individually based on the specific anticancer therapy protocol, disease stage, and patient hematological status.

Administer intravenously. The typical adult dose for induction therapy of acute myeloblastic leukemia is 12 mg/m² daily for 3 days, administered as a slow intravenous injection over 10-15 minutes into the tubing of a freely running intravenous infusion of 0.9% Sodium Chloride solution.

Repeat this course after a 3 to 4 week interval, provided that severe non-hematological toxicity is absent and full bone marrow recovery has occurred.

Do not exceed a cumulative dose of 150-200 mg/m² to minimize the risk of irreversible cardiotoxicity.

Adjust the dose for patients with hepatic impairment: reduce dose by 50% for serum bilirubin levels between 26 and 51 µmol/l; omit the dose if serum bilirubin exceeds 51 µmol/l.

Adjust the dose for patients with renal impairment: reduce dose by 50% for serum creatinine levels above 200 µmol/l.

Monitor peripheral blood counts, hepatic and renal function, plasma uric acid, and cardiac function (ECG, echocardiography) regularly 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 uric acid formation.

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 it during lactation, the issue of discontinuing breastfeeding should be decided.

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

Experimental studies have established the teratogenic and embryotoxic effects of idarubicin.

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 contracted or after contact with sick individuals), with herpes zoster, or other acute infectious diseases.

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

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 diseases, as well as in the case of prior 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 output are necessary.

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

During the use of idarubicin, urine may turn red.

Experimental studies have established the carcinogenic and mutagenic effects of idarubicin.

Drug Interactions

With the simultaneous use of idarubicin with drugs that have myelotoxic effects, 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 25°C (77°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.