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a nitrogen mustardalkylating agent used as an antineoplastic agent.



Pharmacologic class: Alkylating agent, nitrogen mustard

Therapeutic class: Antineoplastic, immunosuppressant

Pregnancy risk category D

FDA Box Warning

• Drug may suppress bone marrow function severely and is carcinogenic.

• Drug causes infertility and is probably mutagenic and teratogenic.


Interacts with cellular DNA to produce cytotoxic cross-linkage, which disrupts cell function. Cell-cycle-phase nonspecific.


Tablets: 2 mg

Indications and dosages

Chronic lymphocytic leukemia, malignant lymphoma, Hodgkin's disease

Adults: Initially, 0.1 to 0.2 mg/kg/day P.O. for 3 to 6 weeks as a single dose or in divided doses. Maintenance dosage is based on CBC but shouldn't exceed 0.1 mg/kg/day.

Off-label uses

• Idiopathic membranous nephropathy

• Meningoencephalitis associated with Behçet's disease

• Rheumatoid arthritis


• Hypersensitivity to drug or other alkylating agents

• Pregnancy or breastfeeding


Use cautiously in:

• hematopoietic depression, infection, other chronic debilitating diseases

• history of seizures or head trauma

• patients who have undergone radiation or other chemotherapy

• elderly patients

• females of childbearing age

• children (safety and efficacy not established).


• Before starting therapy, assess for history of seizures or head trauma.

• After full-course radiation or chemotherapy, wait 4 weeks before giving full doses (because of bone marrow vulnerability).

• To minimize GI effects, drug may be given at bedtime with antiemetic, especially if high dosage is prescribed.

Adverse reactions

CNS: peripheral neuropathy, tremor, confusion, agitation, ataxia, flaccid paresis, seizures

EENT: keratitis

GI: nausea, vomiting, diarrhea

GU: sterile cystitis, amenorrhea, sterility, decreased sperm count

Hematologic: anemia, leukopenia, thrombocytopenia, neutropenia, bone marrow depression

Hepatic: jaundice, hepatotoxicity

Metabolic: hyperuricemia

Musculoskeletal: muscle twitching

Respiratory: interstitial pneumonitis, pulmonary fibrosis

Skin: rash, erythema multiforme, epidermal necrolysis, Stevens-Johnson syndrome

Other: drug fever, allergic reaction, secondary malignancies


Drug-drug. Anticoagulants, aspirin: increased risk of bleeding

Immunosuppressants, myelosuppressants: additive bone marrow depression

Live-virus vaccines: decreased antibody response to vaccine, increased risk of adverse reactions

Drug-diagnostic tests. Alanine aminotransferase, alkaline phosphatase, aspartate aminotransferase, uric acid: increased levels (may reflect hepatotoxicity)

Granulocytes, hemoglobin, neutrophils, platelets, red blood cells, white blood cells (WBCs): decreased counts

Drug-herbs. Astragalus, echinacea, melatonin: interference with immunosuppressant action

Patient monitoring

Monitor CBC with white cell differential and platelet count weekly.

• Monitor WBC count every 3 to 4 days.

• Assess liver function test results.

Patient teaching

• Instruct patient to immediately report unusual bleeding or bruising, fever, nausea, vomiting, rash, chills, sore throat, cough, shortness of breath, seizures, amenorrhea, unusual lumps or masses, flank or stomach pain, joint pain, lip or mouth sores, or yellowing of skin or sclera.

• Tell patient to take drug with full glass of water.

• Inform patient that drug may increase his risk for infection. Advise him to wash hands frequently, wear a mask in public places, and avoid people with infections.

• Instruct patient to contact prescriber before receiving vaccines.

• Advise female patient to use reliable contraception.

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and herbs mentioned above.


/chlor·am·bu·cil/ (klor-am´bu-sil) an alkylating agent from the nitrogen mustard group, used as an antineoplastic.


An anticancer drug that is a derivitive of nitrogen mustard and is used to depress the proliferation and maturation of lymphocytes in diseases such as leukemia.


an alkylating agent.
indications It is prescribed in the treatment of a variety of malignant neoplastic diseases, including chronic lymphocytic leukemia and Hodgkin's disease.
contraindications Bone marrow depression or known hypersensitivity to this drug prohibits its use. It is not given during pregnancy or within 28 days of chemotherapy or radiation therapy. Pregnancy should be avoided for 1 month after discontinuing use.
adverse effects Among the more serious adverse reactions are bone marrow depression, GI disturbance, skin rash, and hepatotoxicity.


Leukeran Oncology An alkylating chemotherapeutic of the nitrogen mustard family, used for lymphomas and other CAs Adverse effects BM suppression, leukemia, infertility, convulsions


A nitrogen-mustard drug used in the treatment of LEUKAEMIA and LYMPHOMAS including HODGKIN'S DISEASE. The drug is on the WHO official list. A brand name is Leukeran.


Drugs that prevent or reduce the immune response. They are used in the treatment of a variety of severe inflammations such as uveitis, scleritis, keratoconjunctivitis sicca, Behçet's syndrome, sympathetic ophthalmia, and to prevent corneal graft rejection. They include the corticosteroids (e.g. prednisolone), ciclosporin (cyclosporine), tacrolimus, and cytotoxic agents (e.g. azathioprine, chlorambucil, cyclophosphamide, methotrexate). It must be noted that immunosuppressants render the patient more susceptible to infection because immunity is reduced.


a nitrogen mustard derivative used as an antineoplastic agent.
References in periodicals archive ?
Chemotherapy regimens used were FC in 38 (83%), FCR 5(11%), CVP 1(2%) and chlorambucil in 2(4%) patients (Table-I).
Notably, ibrutinib was associated with a 98% OS rate versus 85% for chlorambucil at 24 months.
GlaxoSmithKline and Genmab's Arzerra has received marketing authorisation from the European Commission for use as first-line treatment for chronic lymphocytic leukaemia in combination with chlorambucil or bendamustine for patients ineligible for fludarabine-based therapy, it was reported on Friday.
Cyclophosphamide therapy was applied on 15 patients, chlorambucil on 3 patients and cyclosporine A on 17 patients.
Moreover, it is used in combination with chlorambucil, a known teratogen.
On April 17, the Food and Drug Administration approved the agent for use in combination with chlorambucil in previously untreated patients with chronic lymphocytic leukemia, for whom fludarabine-based therapy is considered inappropriate.
2) Adjunctive therapy with immunosuppressive agents such as cyclophosphamide, methotrexate (10-15 mg per week), chlorambucil, or azathioprine may be needed if a patient does not respond adequately to steroids alone.
Obinutuzumab and chlorambucil combination is now evaluated in a phase III study of patients with previously untreated CLL.
A variety of alternate immunosuppressive therapies have been employed with some success, including azathioprine, cyclophosphamide, methotrexate, mycophenolate mofetil, cyclosporine, and chlorambucil.
He had been treated with several cycles of chlorambucil, endoxane and melphalan for chronic lymphatic leukaemia and, in 1997, autologous bone marrow transplantation.
The team evaluated results from 33 patients who were treated with prednisolone and chlorambucil, 37 patients with ciclosporin and 38 who were provided with supportive therapy alone.
Whereas acetochlor and alachlor were active in both the ARE-bla and ARE-luc assays, chlorambucil and melphalan were inactive across all assays.