MERCAPTOPURINE tablet

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

mercaptopurine (UNII: E7WED276I5) (MERCAPTOPURINE ANHYDROUS - UNII:PKK6MUZ20G)

Available from:

Physicians Total Care, Inc.

INN (International Name):

mercaptopurine

Composition:

mercaptopurine 50 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

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.

Product summary:

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.

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

MERCAPTOPURINE - MERCAPTOPURINE TABLET
PHYSICIANS TOTAL CARE, INC.
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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