Trade Names:Leukeran- Tablets 2 mg
Chlorambucil is a bifunctional alkylating agent of the nitrogen mustard type. A cell cycle nonspecific drug, chlorambucil interacts with cellular DNA to produce a cytotoxic cross-linkage.
Rapidly and completely absorbed. T max is within 1 h. C max is about 1 mcg/mL.
99% protein bound (albumin). Crosses the placenta.
Rapidly and extensively metabolized in the liver to phenylacetic acid mustard (active).
The t ½ is 1.5 h (chlorambucil) and 2.4 h (phenylacetic acid mustard). 15% to 60% is excreted in urine after 24 h (less than 1% as chlorambucil or phenylacetic acid mustard).
Chronic lymphatic leukemia; malignant lymphomas including lymphosarcoma, giant follicular lymphoma, and Hodgkin disease.
Ovarian and testicular carcinoma, non-Hodgkin lymphoma, Waldenström macroglobulinemia.
Prior resistance or hypersensitivity.
PO 0.1 to 0.2 mg/kg/day (4 to 10 mg/day) for 3 to 6 wk. Hodgkin disease usually requires 0.2 mg/kg/day, whereas lymphomas or chronic lymphocytic leukemia usually require 0.1 mg/kg/day.MaintenanceAdults
PO Doses should not exceed 0.1 mg/kg/day and may be as low as 0.03 mg/kg/day. Doses of 2 to 4 mg/day are typical.
Store tablets in refrigerator (36° to 46°F).
None well documented.
None well documented.
Confusion; agitation; ataxia; hallucinations; tremors; muscular twitching; flaccid paresis; peripheral neuropathy; seizures; myoclonia.
Rash; urticaria; skin hypersensitivity (including rare reports of skin rash progressing to erythema multiforme, toxic epidermal necrolysis, and Stevens-Johnson syndrome).
Nausea; vomiting; diarrhea; oral ulceration; mucositis.
Sterile cystitis; reversible and permanent sterility.
Bone marrow suppression; leukemia.
Interstitial pneumonia; pulmonary fibrosis.
Acute myelogenous leukemia; drug fever; secondary malignancies.
WarningsBone marrow damage
Chlorambucil can severely suppress bone marrow function.Carcinogenesis
Because of its carcinogenic properties, do not give to patients with conditions other than chronic lymphatic leukemia or malignant lymphomas.Fertility
Chlorambucil has caused chromatid or chromosome damage in men. Reversible and permanent sterility have occurred in men and women.Mutagenicity and teratogenicity
Probable in humans.
Document total cumulative dose.Infection
Monitor patient for signs and symptoms of bacterial, viral, or fungal infection. Report to health care provider immediately if noted.WBC/Platelet count
Implement infection control measures if WBC drops; implement bleeding precautions if platelet count drops.
Category D .
Safety and efficacy not established.
Use with caution because of the greater frequency of decreased hepatic, renal, or cardiac function, and concomitant diseases or other drug therapy.
Chromosome or chromatid damage may occur.
Ensure women of childbearing potential are not pregnant when therapy is initiated and are using effective contraception during treatment.
Skin rash progressing to erythema multiforme, toxic epidermal necrolysis, or Stevens-Johnson syndrome may occur.
Ensure that daily dose does not exceed 0.1 mg/kg in patient with confirmed hypoplastic bone marrow or bone marrow infiltration.
Do not give a full dosage before 4 wk after a full course of radiation therapy or chemotherapy because of the vulnerability of the bone marrow to damage under these conditions.
Rare, focal, or generalized seizures have occurred in adults and children at therapeutic daily doses, pulse dosing regimens, and in acute overdosage. Exercise caution when administering chlorambucil to patients with a history of seizure disorders, head trauma, or to patients receiving other potentially epileptogenic drugs.
Reversible pancytopenia, neurological toxicity ranging from agitated behavior and ataxia to multiple grand mal seizures.
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