Azathioprine(ay za thye’ oh preen)
Azasan, Imuran
PREGNANCY CATEGORY D
Drug class
Immunosuppressant
Therapeutic Actions
Suppresses cell-mediated hypersensitivities and alters antibody production; exact mechanisms of action in increasing homograft survival and affecting autoimmune diseases not clearly understood.
Indications
Renal homotransplantation: Adjunct for prevention of rejection
Rheumatoid arthritis: Use only with adults meeting criteria for classic rheumatoid arthritis and not responding to conventional management
Unlabeled uses: Treatment of chronic ulcerative colitis, myasthenia gravis, Behçet’s syndrome, Crohn’s disease, clinically definite MS (alone or in combination with other drugs), psoriasis
Contraindications and Cautions
Contraindicated with allergy to azathioprine; rheumatoid arthritis patients previously treated with alkylating agents, increasing their risk for neoplasia; pregnancy.
Use cautiously with bone marrow suppression, hepatic impairment, lactation, serious infection.
Available Forms
Tablets—25, 50, 75, 100 mg; injection—100 mg/vial
Dosages
Adults
Renal homotransplantation: Initially, 3–5 mg/kg/day PO or IV as a single dose on the day of transplant; for maintenance, use 1–3 mg/kg/day PO. Do not increase dose to decrease risk of rejection.
Rheumatoid arthritis: Usually given daily; initial dose is 1 mg/kg (50–100 mg) PO
given as a single dose or bid. Dose may be increased at 6–8 wk and thereafter by steps at 4-wk intervals. Dose increments should be 0.5 mg/kg/day up to a maximum dose of 2.5 mg/kg/day. Once patient is stabilized, dose should be decreased to lowest effective dose; decrease in 0.5-mg/kg increments. Patients who do not respond in 12 wk are probably refractory.
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