Azathioprine

This antimetabolite of the purine synthesis represents the classic drug in autoimmune and rheumatologic disorders to be combined with glucocorticosteroids. Monotherapy may take 2-8 weeks to show clinical response (Abu-Shakra et al. 2001, Ashinoff et al. 1988, Callen et al. 1991, Tan et al. 1997, Tsokos et al. 1985). Before initiation of the therapy, activity of the metabolizing enzyme thiomethyltransferase should be evaluated to individually adapt the dosage of azathioprine and lower the incidence of side effects. With normal enzyme levels, doses of 2 mg/kg body weight and greater are recommended. Side effects include disturbances in blood cell counts and liver enzyme levels. Initially, these laboratory parameters should be checked at weeks 2, 4, and 8, and thereafter every 3 months. The incidence of infections seems to be only slightly increased in contrast to a distinct increase of tumors on long-term treatment. This, however, seems to apply to almost any immunosuppressive and most immunomodulatory drugs.

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