国家: 美国
语言: 英文
来源: NLM (National Library of Medicine)
mercaptopurine (UNII: E7WED276I5) (MERCAPTOPURINE ANHYDROUS - UNII:PKK6MUZ20G)
Physicians Total Care, Inc.
mercaptopurine
mercaptopurine 50 mg
ORAL
PRESCRIPTION DRUG
Mercaptopurine tablets are indicated for maintenance therapy of acute lymphatic (lymphocytic, lymphoblastic) leukemia as part of a combination regimen. The response to this agent depends upon the particular subclassification of acute lymphatic leukemia and the age of the patient (pediatric or adult). Mercaptopurine is not effective for prophylaxis or treatment of central nervous system leukemia. Mercaptopurine is not effective in acute myelogenous leukemia, chronic lymphatic leukemia, the lymphomas (including Hodgkins Disease), or solid tumors. Mercaptopurine tablets should not be used in patients whose disease has demonstrated prior resistance to this drug. In animals and humans, there is usually complete cross-resistance between mercaptopurine and thioguanine. Mercaptopurine should not be used in patients who have a hypersensitivity to mercaptopurine or any component of the formulation.
Light yellow to off white, diamond shaped, scored tablets containing 50 mg mercaptopurine, debossed with “P02 ”; Store at 20° to 25°C (68°to 77°F) in a dry place. See USP controlled room temperature.
Abbreviated New Drug Application
MERCAPTOPURINE - MERCAPTOPURINE TABLET PHYSICIANS TOTAL CARE, INC. ---------- 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 MERCATOPURINE 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 1,7-dihydro-6_H_-purine-6-thione 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 microcrystalline cellulose NF, lactose monohydrate NF, stearic acid NF, and colloidal silicon dioxide NF. Mercaptopurine Tablets USP meet USP Dissolution Test 2. CLINICAL PHARMACOLOGY MECHANISM OF ACTION: Mercaptopurine (6-MP) competes with hypoxanthine and guanine for the enzyme hypoxanthine-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 action of inosinate (IMP) dehydrogenase and xanthylate (XMP) aminase, converting TIMP to thiogua 阅读完整的文件