Absorption: well absorbed. Protein binding: ~30%. Metabolism: hepatic. Half-life elimination: Azathioprine and mercaptopurine: Variable: ~2 hours. Time to peak: 1 to 2 hours. Excretion: Urine.
禁忌症
Hypersensitivity to azathioprine or any component of the formulation; pregnancy; patients with rheumatoid arthritis and a history of treatment with alkylating agents may have a prohibitive risk of malignancy with azathioprine treatment.
Renal Allotransplantation: Initial dose: 3-5 mg/kg/day on the day of transplantation; Maintenance dose: 1-3 mg/kg/day. Systemic lupus erythematosus: 2 to 3 mg/kg/day orally in 2 to 3 divided doses. In patients in remission, consider tapering to less than 2 mg/kg/day. Maintenance of improvement of lupus nephritis: 2 mg/kg/day orally with or without a low-dose daily glucocorticoid. Rheumatoid Arthritis: initially, 1 mg/kg/day; increased by 0.5 mg/kg/day at 4-wk intervals; MAX: 2.5 mg/kg/day.
小兒調整劑量
腎功能調整劑量
CrCl (10 to <30 mL/minute): Initial: Administer 75% to 100% of the usual indication-specific dose. CrCl (<10 mL/minute): Initial: Administer 50% to 100% of the usual indication-specific dose.