Chlorambucil

Indications
 Oral
Hodgkin's disease
Adult: 200 mcg/kg daily. Not to exceed 100 mcg/kg/day if the bone marrow is hypoplastic or if there is lymphocytic infiltration in the bone marrow. Once remission is establised, start maintenance at 30-100 mcg/kg/day.
Oral
Non-Hodgkin's lymphoma
Adult: 100 mcg/kg daily. Not to exceed 100 mcg/kg/day if the bone marrow is hypoplastic or if there is lymphocytic infiltration in the bone marrow. Once remission is establised, start maintenance at 30-100 mcg/kg/day.
Oral
Chronic lymphocytic leukaemia
Adult: 100-200 mcg/kg daily (usually 4-10 mg once daily) for 3-8 wk. Not to exceed 100 mcg/kg/day if the bone marrow is hypoplastic or if there is lymphocytic infiltration in the bone marrow. Once remission is establised, start maintenance at 30-100 mcg/kg/day.
Elderly:
Oral
Waldenstrom's macroglobulinaemia
Adult: Initially, 6-12 mg daily until leucopenia develops. Maintenance: 2-8 mg daily.

Special Populations: Daily dose should not exceed 100mcg/kg if the bone marrow is hypoplastic or if there is lymphocytic infiltration in the bone marrow.
Contraindications
 Hypersensitivity. Pregnancy and lactation. Porphyria.
Warnings / Precautions
 Renal or hepatic dysfunction. Perform blood counts regularly. Seizure disorder, bone marrow suppression. Patient who has received radiation therapy, myelosuppressive drugs or has a depressed baseline leukocyte/platelet count within the previous 4 wk. Increased incidence of acute leukaemias and other secondary malignancies.
Adverse Reactions
 Reversible progressive lymphocytopenia and neutropenia; GI disturbances; hepatotoxicity; skin rashes; peripheral neuropathy; central neurotoxicity including seizures; interstitial pneumonia, pulmonary fibrosis. High doses may produce azoospermia and amenorrhoea. Sterility when given to boys at or before puberty.
Potentially Fatal: Severe bone marrow suppression, carcinogenic and human infertility.
Overdose Reactions
 May cause reversible pancytopenia. Neurological toxicity ranging from agitated behavior and ataxia to multiple grand mal seizures may also occur. Management includes monitoring CBC closely and general supportive measures. Appropriate blood transfusions may be given, if necessary. Chlorambucil is not dialysable.
Drug Interactions
 Impairs immune response to vaccines, possible infection after admin of live vaccines.
See Below for More chlorambucil Drug Interactions
Mechanism of Actions
 Chlorambucil interferes with DNA replication and RNA transcription by alkylation and cross-linking cellular DNA strands, thus leading to disruption of the nucleic acid function.
Absorption: Rapid and almost complete from the GI tract (oral).
Distribution: Protein-binding: Extensive.
Metabolism: Extensively hepatic; converted to phenylacetic acid mustard.
Excretion: Urine (as metabolites and unchanged drug); 1.5 hr (elimination half-life).
Administration
 Should be taken on an empty stomach. (Take on an empty stomach. Ensure adequate hydration. Swallow whole, do not chew/crush.)
Storage Conditions
 Oral: Refrigerate at 2-8°C.
ATC Classification
 L01AA02 - chlorambucil ; Belongs to the class of alkylating agents, nitrogen mustard analogues. Used in the treatment of cancer.
Storage
 Oral: Refrigerate at 2-8°C.
Available As
  • Chlorambucil 2 mg
  • Chlorambucil 5 mg

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