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a nitrogen mustardalkylating agent used as an antineoplastic agent.
Miller-Keane Encyclopedia and Dictionary of Medicine, Nursing, and Allied Health, Seventh Edition. © 2003 by Saunders, an imprint of Elsevier, Inc. All rights reserved.



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.

McGraw-Hill Nurse's Drug Handbook, 7th Ed. Copyright © 2013 by The McGraw-Hill Companies, Inc. All rights reserved


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.
The American Heritage® Medical Dictionary Copyright © 2007, 2004 by Houghton Mifflin Company. Published by Houghton Mifflin Company. All rights reserved.


Leukeran Oncology An alkylating chemotherapeutic of the nitrogen mustard family, used for lymphomas and other CAs Adverse effects BM suppression, leukemia, infertility, convulsions
McGraw-Hill Concise Dictionary of Modern Medicine. © 2002 by The McGraw-Hill Companies, Inc.


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.
Collins Dictionary of Medicine © Robert M. Youngson 2004, 2005


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.
Millodot: Dictionary of Optometry and Visual Science, 7th edition. © 2009 Butterworth-Heinemann
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Notably, ibrutinib was associated with a 98% OS rate versus 85% for chlorambucil at 24 months.
He was treated with chlorambucil and remained stable until February 2010 when he developed a chest infection and was found to have a lymphocyte count of 236x[10.sup.9]/L, ANC of 0.9x[10.sup.9]/L, hemoglobin 6g/ dL (DAT negative), and platelets of 71x[10.sup.9]/L.
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Gazyva/Gazyvaro is currently approved in more than 40 countries in combination with chlorambucil for people with previously untreated chronic lymphocytic leukemia.