Biotransformation Williamson RA, Karp LE. Recommendations for the safe handling of parenteral antineoplastic drugs. Patients receiving Azathioprine and allopurinol concomitantly should have a dose reduction of Azathioprine, to approximately 1/ 3 to 1/ 4 the usual dose. It is an imidazolyl derivative of 6-mercaptopurine and many of its biological effects are similar to those of the parent compound. Distribution. Following iv 6-MP administration, 6-MP levels were described by … >> Azathioprine works to suppress the immune system when it is attacking your pet’s own body. Clinical Oncological Society of Australia. After oral administration of [35 S]-azathioprine, the maximum plasma radioactivity occurs at 1-2 hours and decays with a half-life … The frequency and severity of adverse reactions depend on the dose and duration of Azathioprine tablets as well as on the patient’s underlying disease or concomitant therapies. Approximately 0.3% (1:300) of patients of European or African ancestry have two loss-of-function alleles of the TPMT gene and have little or no TPMT activity (homozygous deficient or poor metabolizers), and approximately 10% of patients have one loss-of-function TPMT allele leading to intermediate TPMT activity (heterozygous deficient or intermediate metabolizers). Information is available on the risk of malignancy with the use of Azathioprine in rheumatoid arthritis (see ADVERSE REACTIONS). It is used to treat disorders in dogs such as hemolytic anemia, thrombocytopenia, some chronic liver, kidney, and stomach / intestinal diseases, and arthritis and skin diseases caused by a … The half life of azathioprine is approximately 5 hours. 6. azathioprine and decays with a half-life of 5 hours. Renal clearance is probably not important in predicting biological effectiveness or toxicities, although dose reduction is practiced in patients with poor renal function. Hepatotoxicity has been uncommon (less than 1%) in rheumatoid arthritis patients. Azathioprine is an immunosupressant used in organ transplantation, autoimmune disease such as rheumatoid arthritis or inflammatory bowel disease such as Crohn's disease and ulcerative colitis. Recommendations for handling cytotoxic agents. Conversion to mercaptopurine also occurs in the presence of sulfhydryl compounds such as cysteine, glutathione, and hydrogen sulfide. The TPMT*2, TPMT*3A, and TPMT*3C alleles account for about 95% of individuals with reduced levels of TPMT activity. Dose reduction or temporary withdrawal may result in reversal of these toxicities. Common side effects include bone-marrow suppression and vomiting. Activation of 6-mercaptopurine occurs via hypoxanthine-guanine phosphoribosyltransferase (HGPRT) and a series of multi-enzymatic processes involving kinases to form 6-thioguanine nucleotides (6-TGNs) as major metabolites. Use with xanthine oxidase (XO) inhibitors, We comply with the HONcode standard for trustworthy health information -, ANALYSIS(68382-118, 68382-119, 68382-120), MANUFACTURE(68382-118, 68382-119, 68382-120). Adult Indications and Dosage FDA-Labeled Indications and Dosage (Adult) Renal Homotransplantation Guidelines and recommendations for safe handling of antineoplastic agents. Nausea and vomiting may occur within the first few months of therapy with Azathioprine tablets, and occurred in approximately 12% of 676 rheumatoid arthritis patients. Available for Android and iOS devices. Genetic polymorphisms influence TPMT and NUDT15 activity. 35. /SM 0.02 This is not an estimate of the half-life of azathioprine itself, but is the decay rate for all S-containing metabolites of the drug. One is thiol methylation, which is catalyzed by the enzyme thiopurine S-methyltransferase (TPMT), to form the inactive metabolite methyl-6-MP (6-MeMP). 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