Classifications: antineoplastic; alkylating agent; Therapeutic: antineoplastic; nitrogen mustard
Pregnancy Category: D
2 mg tablets
Potent aromatic derivative of the alkylating agent nitrogen mustard which is slowest acting and least toxic of the nitrogen
mustards. A cell-cycle nonspecific drug (kills both resting and dividing cells), it causes cytotoxic cross linkage in DNA,
thus preventing synthesis of DNA, RNA, and proteins. Myelosuppression in therapeutic doses is moderate and rapidly reversible.
Lymphocytic effect is marked; thus it is effective in treatment of various lymphomas.
As single agent or with other antineoplastics in treatment of chronic lymphocytic leukemia, malignant lymphomas including
lymphosarcoma, Hodgkin's disease, and giant follicular lymphoma, and in treatment of carcinoma of the ovary, breast, and
Nonneoplastic conditions: vasculitis complicating rheumatoid arthritis, autoimmune hemolytic anemias associated with cold
agglutinins, lupus glomerulonephritis, idiopathic nephrotic syndrome, polycythemia vera, macroglobulinemia.
Hypersensitivity to chlorambucil or to other alkylating agents; administration within 4 wk of a full course of radiation
or chemotherapy; full dosage if bone marrow is infiltrated with lymphomatous tissue or is hypoplastic; smallpox and other
vaccines; pregnancy (category D), lactation.
Excessive or prolonged dosage, pneumococcus vaccination, history of seizures or head trauma.
Route & Dosage
|Malignant Diseases (Lymphomas, Hodgkin's Disease, etc.)
Adult: PO 0.10.2 mg/kg/d (usual dose 410 mg/d)
Child: PO 0.10.2 mg/kg/d in single or divided doses
- Control nausea and vomiting by giving entire daily dose at one time, 1 h before breakfast or 2 h after evening meal, or
at bedtime. Consult physician.
- With confirmation of bone marrow depression (low platelet and neutrophil counts or peripheral lymphocytosis), it is recommended
that dosage not exceed 0.1 mg/kg.
- Store in tightly closed, light-resistant container.
Adverse Effects (≥1%) Body as a Whole:
Drug fever, skin rashes, papilledema, alopecia
, peripheral neuropathy
, sterile cystitis
(high doses). GI:
of gastric discomfort, hepatotoxicity. Hematologic: Bone marrow depression
: leukopenia, thrombocytopenia
May have to adjust dose of allopurinol, colchicine
because of chlorambucil-associated hyperuricemia.
Rapidly and completely from GI tract. Peak:
1 h. Distribution:
Extensively bound to plasma
and tissue proteins
; crosses placenta. Metabolism:
In liver. Elimination:
60% in urine as metabolites within 24 h. Half-Life:
Assessment & Drug Effects
- Lab tests: CBC, Hgb, total and differential leukocyte counts, and serum uric acid initially and at least once weekly during
- Leukopenia usually develops after the third week of treatment; it may continue for up to 10 d after last dose, then rapidly
return to normal.
- Avoid or reduce to minimum injections and other invasive procedures (e.g., rectal temperatures, enemas) when platelet count
is low because of danger of bleeding.
- Monitor for S&S of skin rashes, which are rare, but appear to show a consistent pattern: pustular eruption on mouth, chin,
cheeks; urticarial erythema on trunk that spreads to legs. The rash occurs early in treatment period and lasts about 10 d
after last dose.
Patient & Family Education
- Keep appointments with physician. During treatment it is dangerous to go longer than 2 wk without a clinical examination
and blood studies.
- Notify physician if the following symptoms occur: unusual bleeding or bruising, sores on lips or in mouth; flank, stomach,
or joint pain; fever, chills, or other signs of infection, sore throat, cough, dyspnea.
- Report immediately the onset of cutaneous reaction.
- Drink at least 1012 glasses [240 mL (8 oz) each] of fluid per day, if not contraindicated, and report to physician
if urine output decreases below normal amounts.
- Report to physician immediately if pregnant, as there is a potential hazard to the fetus.