Chlorambucil
- Atc Codes:L01AA02
- CAS Codes:305-03-3
- PHARMGKB ID:305-03-3
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Unlabeled Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Genes that may be involved
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Leukeran; Belgium: Leukeran; Bulgaria: Leukeran; Czech Republic: Leukeran; Denmark: Leukeran; Finland: Leukeran; France: Chloraminophène; Germany: Leukeran; Ireland: Leukeran; Italy: Leukeran; Latvia: Leukeran; Lithuania: Leukeran; Luxembourg: Leukeran; Malta: Leukeran; Netherlands: Leukeran; Poland: Leukeran; Portugal: Leukeran; Romania: Leukeran; Slovakia: Leukeran; Slovenia: Leukeran; Spain: Leukeran; Sweden: Leukeran; UK: Leukeran.
North America
Canada: Leukeran; USA: Leukeran.
Latin America
Argentina: Leukeran; Brazil: Leukeran; Mexico: Leukeran.
Drug combinations
Chemistry
Chlorambucil: C~14~H~19~Cl~2~NO~2~. Mw: 304.21. Benzenebutanoic acid, 4-[bis(2-chloroethyl)amino]-. 4-[p-[Bis(2-chloroethyl)amino]phenyl]butyric acid. CAS-305-03-3.
Pharmacologic Category
Antineoplastic Agents; Alkylating Agents; Nitrogen Mustard Analogs. (ATC-Code: L01AA02).
Mechanism of action
Interferes with DNA replication and RNA transcription by alkylation and cross-linking the strands of DNA. Possesses some immunosuppressive activity, principally due to suppression of lymphocytes.
Therapeutic use
Chronic lymphocytic leukemia. Hodgkin’s lymphoma. Non-Hodgkin lymphoma. Breast and ovarian carcinoma. Testicular carcinoma. Choriocarcinoma.
Pregnancy and lactiation implications
Animal studies demonstrated teratogenicity. Crosses the human placenta. Adverse renal effects (unilateral agenesis) following exposure during 1^st^ trimester (case reports). Probably mutagenic and also teratogenic (chromosomal damage documented). Use not recommended during lactation.
Unlabeled use
Nephrotic syndrome. Waldenström’s macroglobulinemia. Intractable idiopathic uveitis and related conditions, including Behcet’s syndrome. Autoimmune hemolytic anemias associated with cold agglutinins. Systemic lupus erythematosus. Severe, chronic rheumatoid arthritis. Vasculitis associated with rheumatoid arthritis. Mycosis fungoides. Sarcoidosis.
Contraindications
Hypersensitivity to chlorambucil or any component of the formulation. Hypersensitivity to other alkylating agents (may have cross-hypersensitivity). Pregnancy.
Warnings and precautions
May cause bone marrow suppression (lymphopenia). Affects human fertility, including azoospermia (when administered to prepubertal and pubertal males) and amenorrhea. Possibly carcinogenic with chronic therapy (acute myelocytic leukemia and secondary malignancies). Seizures observed (higher risk if history of nephrotic syndrome and high pulse doses). Rare instances of severe skin reactions (e.g. erythema multiforme, Stevens-Johnson syndrome) reported. Avoid administration of live vaccines to immunocompromised patients.