Leukemias, a part from chronic lymphocytic leukemia, (as a component of various chemotherapeutic regimens); an adjunct for prevention of rejection in renal, cardiac, hepatic, and pancreatic transplantations; treatment of rheumatoid arthritis unresponsive to the classical medications; treatment of inflammatory bowel disease; systemic lupus erythematosus; nephrotic syndrome; management of other immunologic diseases including myasthenia gravis, pemphigoid and pemphigus; systemic dermatomyositis, glomerulonephritis, chronic active hepatitis among others.
Leukemia: Orally, 2.5 mg / kg / day in single or divided doses. In case of poor response after four weeks at this dosage, an increase in dosage to 5 mg / kg / day is tried. Maintenance-Dose: Orally, 1.5 - 2.5 mg/kg/ day. Inflammatory bowel disease: Orally, 1.5 mg /kg / day, adjusted accordingly. In case of poor response after 2-3months at this dosage, an increase in dosage to 2.5 mg / kg / day is tried.Usual dose in children: Orally, 2.5 mg / kg / day in single or divided doses. Consult specialist literature for further information.
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It competes with hypoxanthine and guanine for the enzyme hypoxanthine-guanine phosphoribosyltransferase. It is convert-ed to thioinosinic acid, which inhibits several reactions involving inosinic acid e.g. conversion of inosinic acid to xanthylic acid and the conversion of inosinic acid to adenylic acid] via adenylosuccinate. The end result is inhibition of DNA synthesis and RNA synthesis [though to a lesser effect].
GI hypersensitivity reaction can occur; periodic blood counts.
Hypersensitivity to the drug; treating rheumatoid arthritis in pregnant women
Leukopenia; thrombocytopenia; anaemia; neoplasia; hyperuricemia; uric acid nephropathy; nausea and vomiting; stomatitis; GI ulceration; darkening of skin; hepatotoxicity; infection; hypersensitivity reactions.
Drug interactions: Activity of warfarin may be decreased; due to its immunosuppressant effect, it may re-activate live attenuated vaccines and / or reduce immune response; immunosuppressants like cyclophosphamide; chlorambucil and corticosteroids accentuate its positive effects as well as its side effects; angiotensin-converting enzyme