Clinical Gastroenterology Vol.22 No.12(1-1)

Theme Role of AZA/6-MP in the Treatment of Inflammatory Bowel Disease
Title The Pharmacokinetics of AZA/6-MP -- The General Remarks of Metabolism / Pharmacological Action, and the Gene Polymorphism of Metabolic Enzymes
Publish Date 2007/11
Author Kan Uchiyama Division of Gastroenterology and Hepatology, Department of Internal Medicine, The Jikei University School of Medicine (Kashiwa Hospital)
Author Makoto Nakamura Division of Gastroenterology and Hepatology, Department of Internal Medicine, The Jikei University School of Medicine (Kashiwa Hospital)
Author Takahiro Kubota Department of Drug Metabolism and Biopharmaceutics, Faculty of Pharmacy, Chiba Institute of Science
Author Tateki Yamane Division of Gastroenterology and Hepatology, Department of Internal Medicine, The Jikei University School of Medicine (Kashiwa Hospital)
Author Kiyotaka Fujise Division of Gastroenterology and Hepatology, Department of Internal Medicine, The Jikei University School of Medicine (Kashiwa Hospital)
Author Hisao Tajiri Department of Gastroenterology and Hepatology, The Jikei University School of Medicine
[ Summary ] Azathioprine (AZA)/6-mercaptopurine (6-MP) have recently become indispensable medicines for treatment of inflammatory bowel disease. However, several adverse drug reactions, such as pancreatitis, liver damage, nausea, alopecia and agranulocytosis due to myelosuppression, account for 15 - 28 % of the problems encountered. AZA/6-MP are metabolized immediately through xanthine oxidase (XO) and thiopurine S-methyltransferase (TPMT), and is then excreted. The polymorphism of TPMT or inosine triphosphate pyrophosphohydrolase (ITPase) influences the metabolism of these medicine. In addition, other medicines such as alloprinol, 5-aminosalicylic acid and folic acid have interactive effects.
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