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chlorambucil (Leukeran)
Tradename: Leukeran.
Indications:
1) chronic lymphocytic leukemia
a) induction 0.1-0.2 mg/kg/day for 3 weeks
b) 0.4 mg/kg every 2-4 weeks
2) Hodgkin's disease
3) non-Hodgkin's lymphoma
- 16 mg/m2/day for 5 days every 4 weeks
4) macroglobulinemia
5) polycythemia vera
6) trophoblastic neoplasms
7) ovarian neoplasms
8) nephrotic syndrome unresponsive to conventional therapy
9) minimal change disease [3]
Contraindications:
- pregnancy*
* contraception indicated during therapy
Dosage: Tabs: 2 mg.
Pharmacokinetics:
1) well absorbed orally
2) food slows absorption
3) metabolized by liver
4) 1/2life 1-2 hours
Adverse effects:
1) common (> 10%)
- myelosuppression
- onset 7 days
- nadir 10-14 days
- recovery 28 days
- increased incidence of secondary malignancy, especially acute myelogenous leukemia (AML)
2) less common (1-10%)
- menstrual changes*, skin rashes, hyperuricemia, diarrhea, oral ulceration*, nausea/vomiting
3) uncommon (< 1%)
- drug fever, hepatic necrosis, weakness, rash, leukopenia, thrombocytopenia, tremors, twitching, confusion, agitation, ataxia, hallucinations, seizures, peripheral neuropathy, fertility impairment (oligospermia, amenorrhea) pulmonary fibrosis (cumulative effect), keratitis, hepatotoxicity, skin hypersensitivity
* notify physician if bleeding or sore throat occurs
Drug interactions:
- barbiturates may increase the toxicity of chlorambucil
Mechanism of action: alkylating agent
Interactions
drug adverse effects of alkylating agents
General
alkylating agent nitrogen mustard
Properties
MISC-INFO: elimination route LIVER
1/2life 1-2 HOURS
pregnancy-category D
Database Correlations
PUBCHEM correlations
References
- Kaiser Permanente Northern California Regional Drug
Formulary, 1998
- Drug Information & Medication Formulary, Veterans Affairs,
Central California Health Care System, 1st ed., Ravnan et al
eds, 1998
- Deprecated Reference