Products
Chlorambucil is commercially available in the form of film-coated tablets (Leukeran). It has been approved in many countries since 1957.
Structure and properties
Chlorambucil (C14H19Cl2NO2, Mr = 304.2 g/mol) is an aromatic nitrogen-lost derivative. It exists as a white crystalline powder that is practically insoluble in water. The effects are due to the active metabolite phenylacetic acid mustard (PAAM).
Effects
Chlorambucil (ATC L01AA02) has cytostatic, immunosuppressive, mutagenic, and teratogenic properties. It inhibits DNA replication, cell proliferation, and induces cell death.
Indications
- Hodgkin’s disease
- Non-Hodgkin’s lymphoma
- Chronic lymphocytic leukemia
- Waldenström’s disease (Waldenström macroglobulinemia)
Dosage
According to the professional information. The tablets are taken once or several times a day on an empty stomach. Hands should be washed immediately after contact with the tablets. Parts of the tablets should not be inhaled or come into contact with the skin or eyes.
Contraindications
- Hypersensitivity
- Pregnancy and lactation
Full precautions can be found in the drug label.
Interactions
Drug-drug interactions have been described with live vaccines, purine nucleoside analogues, other cytostatic agents, and phenylbutazone.
Adverse effects
The most common potential adverse effects include bone marrow suppression (leukopenia, neutropenia, thrombocytopenia, pancytopenia, anemia), nausea, vomiting, diarrhea, oral mucositis, and secondary hematologic malignancies such as leukemia.
