国家: 美国
语言: 英文
来源: NLM (National Library of Medicine)
MERCAPTOPURINE (UNII: E7WED276I5) (MERCAPTOPURINE ANHYDROUS - UNII:PKK6MUZ20G)
Avera McKennan Hospital
MERCAPTOPURINE
MERCAPTOPURINE 50 mg
PRESCRIPTION DRUG
Abbreviated New Drug Application
MERCAPTOPURINE- MERCAPTOPURINE TABLET AVERA MCKENNAN HOSPITAL ---------- MERCAPTOPURINE TABLETS USP, 50 MG RX ONLY CAUTION MERCAPTOPURINE IS A POTENT DRUG. IT SHOULD NOT BE USED UNLESS A DIAGNOSIS OF ACUTE LYMPHATIC LEUKEMIA HAS BEEN ADEQUATELY ESTABLISHED AND THE RESPONSIBLE PHYSICIAN IS EXPERIENCED WITH THE RISKS OF MERCAPTOPURINE AND KNOWLEDGEABLE IN ASSESSING RESPONSE TO CHEMOTHERAPY. DESCRIPTION Mercaptopurine was synthesized and developed by Hitchings, Elion, and associates at the Wellcome Research Laboratories. Mercaptopurine, known chemically as 6_H_-purine-6-thione, 1,7-dihydro-, monohydrate, is an analogue of the purine bases adenine and hypoxanthine. Its structural formula is: Mercaptopurine is available in tablet form for oral administration. Each scored tablet contains 50 mg mercaptopurine and the inactive ingredients hypromellose, lactose (anhydrous), lactose (monohydrate), magnesium stearate, potato starch, sodium starch glycolate, starch and stearic acid. Each tablet meets the requirements of Test 2 for Dissolution in the USP monograph for Mercaptopurine Tablets, USP. CLINICAL PHARMACOLOGY MECHANISM OF ACTION Mercaptopurine (6-MP) competes with hypoxanthine and guanine for the enzyme hyphoxanthine-guanine phosphoribosyltransferase (HGPRTase) and is itself converted to thioinosinic acid (TIMP). This intracellular nucleotide inhibits several reactions involving inosinic acid (IMP), including the conversion of IMP to xanthylic acid (XMP) and the conversion of IMP to adenylic acid (AMP) via adenylosuccinate (SAMP). In addition, 6-methylthioinosinate (MTIMP) is formed by the methylation of TIMP. Both TIMP and MTIMP have been reported to inhibit glutamine-5-phosphoribosylpyrophosphate amidotransferase, the first enzyme unique to the de novo pathway for purine ribonucleotide synthesis. Experiments indicate that radiolabeled mercaptopurine may be recovered from the DNA in the form of deoxythioguanosine. Some mercaptopurine is converted to nucleotide derivatives of 6-thioguanine (6- TG) by the sequential a 阅读完整的文件