♦Chlorambucil
(klor-am’-byoo-sil)
Leukeran
Pregnancy Category D
Mechanism of Action
Chlorambucil is a nitrogen mustard derivative that works as an alkylating agent by interfering with DNA replication and the transcription of RNA and by disrupting the functioning of nucleic acid.
Indications
♦ Palliative treatment of chronic lymphocytic leukemia
♦ Advanced malignant (non-Hodgkin’s) lymphoma
♦ Hodgkin’s disease
♦ Unlabeled uses: Macroglobulinemia, polycythemia vera, trophoblastic neoplasms, ovarian neoplasms, nephrotic syndrome, advanced breast cancer
Metabolism/Excretion
Metabolized in the liver and excreted in the urine. Half-life: 1 hour.
Dosage Range
♦ Adult: For initiation of therapy or short courses of therapy, the usual dosage is 0.1 to 0.2 mg/kg given as a single dose for 3 to 6 weeks. The usual dosage comes out to 4 to 10 mg/day. Alternatively, adults may receive 3 to 6 mg/day. Dose modifications should be made if chloram-bucil is given within 4 weeks after a full course of radiation treatment or if myelosuppression occurs. The recommended dose should not exceed 0.1 mg/kg/day or 6 mg/day. It is also believed that short courses of chloram-bucil are safer than continuous maintenance therapy, although both are effective. The manufacturer states that continuous therapy may appear to maintain patients in remission and suggests that the drug should be withdrawn in those patients to determine whether maintenance therapy is necessary. The maintenance dose should not exceed 0.1 mg/kg per day and may be as low as 0.03 mg/kg or 2 to 4 mg daily.