About
Mercaptopurine (6-MP) is an antimetabolite and purine analogue primarily used in the treatment of acute lymphoblastic leukemia (ALL) and certain autoimmune diseases. It exerts its therapeutic effects by acting as a false metabolite, thereby interfering with crucial nucleic acid synthesis pathways. Specifically, 6-MP inhibits de novo purine synthesis and its incorporation into DNA and RNA, which is vital for cell proliferation. This disruption is particularly detrimental to rapidly dividing cells, such as those found in cancers. Administered orally, 6-MP is a prodrug that requires intracellular activation by hypoxanthine-guanine phosphoribosyltransferase (HGPRT) to its active thioguanine nucleotide metabolites. Its complex metabolism involves several enzymes, notably thiopurine methyltransferase (TPMT), which plays a significant role in determining drug efficacy and potential toxicity. Genetic testing for TPMT deficiency is often recommended prior to treatment to guide appropriate dosing and mitigate the risk of severe myelosuppression, ensuring safer and more effective therapy.
Uses
- Acute lymphoblastic leukemia (ALL)
- Acute myeloid leukemia (AML) (less common)
- Crohn's disease (off-label)
- Ulcerative colitis (off-label)
Directions For Use
Take orally as directed by your doctor. Dosage is individualized and may require regular blood tests.
Benefits
- Key component in ALL maintenance therapy.
- Effective in inducing and maintaining remission in ALL.
- Oral administration for convenience.
- Can be used in combination chemotherapy regimens.
- Long-standing clinical use and established efficacy.
- Helps prevent relapse in certain leukemias.
Side Effects
- Myelosuppression (leukopenia, thrombocytopenia, anemia)
- Nausea and vomiting
- Diarrhea
- Hepatotoxicity (liver damage)
- Mucositis
- Anorexia
- Skin rash
- Fever
- Pancreatitis (rare)
- Increased risk of infections
- Alopecia (mild)
- Hyperuricemia
Safety Measures
- Alcohol - Avoid alcohol due to potential for increased hepatotoxicity and gastrointestinal irritation.
- Pregnancy - Contraindicated in pregnancy due to teratogenic effects. Use effective contraception.
- Breastfeeding - Not recommended during breastfeeding as it may be excreted in breast milk and harm the infant.
- Liver - Use with extreme caution in patients with liver impairment; monitor liver function closely.
- Kidney - Dose adjustment may be necessary in patients with renal impairment.
- Lung - Rarely associated with interstitial pneumonitis; monitor for respiratory symptoms.
Disclaimer
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