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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.
• 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.
CNS: peripheral neuropathy, tremor, confusion, agitation, ataxia, flaccid paresis, seizures
GI: nausea, vomiting, diarrhea
GU: sterile cystitis, amenorrhea, sterility, decreased sperm count
Hematologic: anemia, leukopenia, thrombocytopenia, neutropenia, bone marrow depression
Hepatic: jaundice, hepatotoxicity
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
☞ Monitor CBC with white cell differential and platelet count weekly.
• Monitor WBC count every 3 to 4 days.
• Assess liver function test results.
• 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.