Difference between revisions of "Mercaptopurine (6-MP)"
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==General information== | ==General information== | ||
| − | Class/mechanism: Purine analog of adenine and hypoxanthine, antimetabolite that interferes with DNA synthesis. Mercaptopurine competes with hypoxanthine and guanine for the enzyme hypoxanthine-guanine phosphoribosyltransferase (HGPRTase) and is converted to thioinosinic acid (TIMP). TIMP inhibits reactions that typically involve inosinic acid (IMP), such as its conversion to xanthylic acid (XMP) and adenylic acid (AMP) via adenylosuccinate (SAMP). TIMP is also converted to 6-methylthioinosinate (MTIMP); TIMP and MTIMP have been observed to inhibit glutamine-5-phosphoribosylpyrophosphate amidotransferase, which is an enzyme involved in the de novo pathway of purine ribonucleotide synthesis.<ref name="insert">[http://www.accessdata.fda.gov/drugsatfda_docs/label/2011/009053s032lbl.pdf Mercaptopurine (Purinethol) package insert]</ref><ref>[http://hemonc.org/docs/packageinsert/mercaptopurine.pdf Mercaptopurine (Purinethol) package insert (locally hosted backup)]</ref> | + | Class/mechanism: Purine analog of adenine and hypoxanthine, antimetabolite that interferes with DNA synthesis. Mercaptopurine competes with hypoxanthine and guanine for the enzyme hypoxanthine-guanine phosphoribosyltransferase (HGPRTase) and is converted to thioinosinic acid (TIMP). TIMP inhibits reactions that typically involve inosinic acid (IMP), such as its conversion to xanthylic acid (XMP) and adenylic acid (AMP) via adenylosuccinate (SAMP). TIMP is also converted to 6-methylthioinosinate (MTIMP); TIMP and MTIMP have been observed to inhibit glutamine-5-phosphoribosylpyrophosphate amidotransferase, which is an enzyme involved in the de novo pathway of purine ribonucleotide synthesis. Structurally and functionally similar to [[Thioguanine (Tabloid)]].<ref name="insert">[http://www.accessdata.fda.gov/drugsatfda_docs/label/2011/009053s032lbl.pdf Mercaptopurine (Purinethol) package insert]</ref><ref>[http://hemonc.org/docs/packageinsert/mercaptopurine.pdf Mercaptopurine (Purinethol) package insert (locally hosted backup)]</ref> |
<br>Route: PO | <br>Route: PO | ||
<br>Extravasation: n/a | <br>Extravasation: n/a | ||
Revision as of 00:01, 25 February 2012
Also known as 6-MP or 6-Mercaptopurine.
General information
Class/mechanism: Purine analog of adenine and hypoxanthine, antimetabolite that interferes with DNA synthesis. Mercaptopurine competes with hypoxanthine and guanine for the enzyme hypoxanthine-guanine phosphoribosyltransferase (HGPRTase) and is converted to thioinosinic acid (TIMP). TIMP inhibits reactions that typically involve inosinic acid (IMP), such as its conversion to xanthylic acid (XMP) and adenylic acid (AMP) via adenylosuccinate (SAMP). TIMP is also converted to 6-methylthioinosinate (MTIMP); TIMP and MTIMP have been observed to inhibit glutamine-5-phosphoribosylpyrophosphate amidotransferase, which is an enzyme involved in the de novo pathway of purine ribonucleotide synthesis. Structurally and functionally similar to Thioguanine (Tabloid).[1][2]
Route: PO
Extravasation: n/a
For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the package insert[1].
Patient drug information
- Mercaptopurine (Purinethol) patient drug information (Chemocare)[3]
- Mercaptopurine (Purinethol) patient drug information (UpToDate)[4]