Increased risk of malignancy with chronic immunosuppression. Malignancy (eg, post-transplant lymphoma, hepatosplenic T-cell lymphoma) reported in patients with inflammatory bowel disease. Physician should be familiar with this risk as well as mutagenic potential and possible hematologic toxicities.
Purine antagonist antimetabolite
Adjunct therapy for prevention of rejection in renal homotransplantation. Management of active rheumatoid arthritis (RA) to reduce signs and symptoms.
Adjunct Therapy for Prevention of Rejection in Renal Homotransplantation:
Initial: 3-5mg/kg/day, beginning at the time of transplant
Usually given as a single daily dose on the day of, and in a minority of cases 1-3 days before, transplantation
Initial: 1mg/kg/day (50-100mg) given qd or bid
Titrate: May increase dose by 0.5mg/kg/day increments beginning at 6-8 weeks and thereafter by steps at 4-week intervals
May be considered refractory if no improvement after 12 weeks
Use lowest effective dose; decrease by 0.5mg/kg/day or 25mg/day every 4 weeks to lowest effective dose while other therapy is kept constant
Oliguric patients may have delayed clearance; give lower doses
Tab: 50mg*, (Azasan) 75mg*, 100mg* *scored
(RA) Pregnancy, patients previously treated with alkylating agents (eg, cyclophosphamide, chlorambucil, melphalan).
Renal transplant patients are known to have an increased risk of malignancy. Risk of post-transplant lymphomas may be increased with aggressive immunosuppressive treatment; maintain therapy at the lowest effective levels. Acute myelogenous leukemia as well as solid tumors reported in patients with RA. Severe leukopenia, thrombocytopenia, anemias (eg, macrocytic anemia, pancytopenia), and severe bone marrow suppression may occur. Myelotoxicity risk may be increased in patients with intermediate thiopurine S-methyl transferase (TPMT) activity. Increased risk of severe, life-threatening myelotoxicity in patients with low or absent TPMT activity; consider alternative therapies. Caution in patients having one non-functional allele who are at risk for reduced TPMT activity; dose reduction is recommended in patients with reduced TPMT activity. Reduce dose or d/c temporarily if rapid fall in or persistently low leukocyte count, or other evidence of bone marrow depression occurs. Delayed hematologic suppression may occur. TPMT testing cannot be a substitute for CBC monitoring. Consider early drug discontinuation in patients with abnormal CBC results that do not respond to dose reduction. May cause fetal harm. GI hypersensitivity reaction characterized by severe N/V reported. Increased risk for bacterial, viral, fungal, protozoal, and opportunistic infections, including reactivation of latent infections that may lead to serious, including fatal, outcomes. JC virus-associated infection resulting in progressive multifocal leukoencephalopathy (PML) reported; consider reducing the amount of immunosuppression in patients who develop PML.
Malignancy, hematologic toxicities, infections, N/V.
See Contraindications. Combined use with disease-modifying antirheumatic drugs cannot be recommended. Caution with concomitant aminosalicylate derivatives (eg, sulfasalazine, mesalazine, olsalazine); may inhibit TPMT enzyme. Allopurinol inhibits one of the inactivation pathways; reduce azathioprine dose to approx 1/3-1/4 of the usual dose and consider further dose reduction or alternative therapies for patients with low or absent TPMT activity. Drugs that may affect leukocyte production (eg, co-trimoxazole) may lead to exaggerated leukopenia, especially in renal transplant recipients. ACE inhibitors may induce anemia and severe leukopenia. May inhibit anticoagulant effect of warfarin. Use of ribavirin for hepatitis C has been reported to induce severe pancytopenia and may increase the risk of azathioprine-related myelotoxicity.
PREGNANCY AND LACTATION
Category D, not for use in nursing.
MECHANISM OF ACTION
Purine antagonist antimetabolite; an imidazolyl derivative of 6-mercaptopurine (6-MP). In homograft survival, it suppresses hypersensitivities of the cell-mediated type and causes variable alterations in antibody production. Immuno-inflammatory response mechanisms not established; suppresses disease manifestation and underlying pathology in autoimmune disease.
Absorption: Well-absorbed; Tmax=1-2 hrs. Distribution: Plasma protein binding (30%); crosses placenta, found in breast milk. Metabolism: Liver and erythrocytes (extensive); 6-MP activated to 6-thioguanine nucleotides (major metabolites); 6-MP inactivated via thiol methylation by TPMT and oxidation by xanthine oxidase. Elimination: Urine; T1/2=5 hrs (decay rate of S-containing metabolites of azathioprine).
Assess for drug hypersensitivity, renal/hepatic dysfunction, previous treatment of RA with alkylating agents, pregnancy/nursing status, and for possible drug interactions. Conduct TPMT genotyping/phenotyping to identify absent or reduced TPMT activity.
Monitor for signs/symptoms of cytopenias, malignancies, infections, GI hypersensitivity reactions, and other adverse reactions. Monitor CBCs, including platelet counts, weekly during the 1st month, twice monthly for the 2nd and 3rd months of therapy, then monthly or more frequently if dose/therapy changes are necessary. Periodically monitor serum transaminases, alkaline phosphatase, and bilirubin levels. Consider TPMT testing in patients with abnormal CBC results unresponsive to dose reduction.
Inform about necessity of periodic blood counts while on therapy and risks of malignancy and infection. Instruct to report to physician any unusual bleeding/bruising or signs/symptoms of infections. Educate about proper dosage instructions, especially with impaired renal function or concomitant use with allopurinol. Inform of the potential risks during pregnancy and nursing; advise to notify physician if pregnant or nursing. Instruct patients with increased risk for skin cancer to limit exposure to sunlight and UV light (eg, wearing protective clothing, using a sunscreen).
20-25°C (68-77°F). Protect from light.
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