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Action/Kinetics:
Inhibits nucleic acid synthesis and interacts with the enzyme topoisomerase II. Rapidly taken up into cells due to significant lipid solubility.
t
1/2 (terminal): 22 hr when used alone and 20 hr when used with cytarabine. Metabolized in the liver to the active idarubicinol, which is excreted through both the bile and urine. Both idarubicin and idarubicinol are significantly bound (97% and 94%, respectively) to plasma proteins.
Uses:
In combination with other drugs (often cytarabine) to treat AML in adults, including French-American-British classifications M1-M7. Comparison with daunorubicin indicates that idarubicin is more effective in inducing complete remissions in clients with AML.
Contraindications:
Lactation. Preexisting bone marrow suppression induced by previous drug therapy or radiotherapy (unless benefit outweighs risk). Administration by the IM or SC routes.
Special Concerns:
Safety and effectiveness have not been demonstrated in children. Skin reactions may occur if the powder is not handled properly.
Side Effects:
GI: N&V;, mucositis, diarrhea, abdominal pain, abdominal cramps,
hemorrhage.
Hematologic:
Severe myelosuppression.
Dermatologic: Alopecia, generalized rash, urticaria, bullous erythrodermatous rash of the palms and soles, hives at injection site.
CNS: Headache,
seizures altered mental status.
CV: CHF,
serious arrhythmias including atrial fibrillation, chest pain, MI, cardiomyopathies decrease in LV ejection fraction.
NOTE: Cardiac toxicity is more common in clients who have received anthracycline drugs previously or who have preexisting cardiac disease.
Miscellaneous: Altered hepatic and renal function tests, infection (95% of clients), fever, pulmonary allergy, neurologic changes in peripheral nerves.
Overdose Management:
Symptoms: Severe GI toxicity, myelosuppression.
Treatment: Supportive treatment including antibiotics and platelet transfusions. Treat mucositis.
How Supplied:
Injection: 1 mg/mL;
Powder for injection: 5 mg, 10 mg, 20 mg
Dosage
?IV
Induction therapy in adults with AML.
12 mg/m
2/day for 3 days by slow (10-15 min) IV injection in combination with cytarabine, 100 mg/m
2/day given by continuous infusion for 7 days or as a 25-mg/m
2 IV bolus followed by 200 mg/m
2/day for 5 days by continuous infusion. A second course may be given if there is evidence of leukemia after the first course. The drug should not be given if the bililrubin level is greater than 5 mg/dL.
