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Mercaptopurine

Class
Antimetabolites
Subclass
Purine analogs
Substance name
Mercaptopurine, 6-MP
Brand names
Purinethol®, Purixan®
Common formulations
Tablet, Oral suspension
Dosage and administration
Adults patients
Acute lymphoblastic leukemia • Maintenance therapy
•
1.5-2.5 mg/kg PO daily
Administered in combination with other chemotherapeutic agents.
Acute promyelocytic leukemia • Maintenance therapy • Off-label
•
60-70 mg/m² PO daily
Administered in combination with other chemotherapeutic agents.
Crohn's disease • Moderate-to-severe, maintenance of remission • Off-label
•
1.5 mg/kg PO daily
Crohn's disease • Moderate-to-severe, induction of remission • Off-label
•
0.75-1.5 mg/kg PO daily
Ulcerative colitis • Moderate-to-severe, maintenance of remission • Off-label
•
1.5 mg/kg PO daily
Other off-label uses
•
Treatment of Crohn's disease
•
Treatment of ulcerative colitis (moderate-to-severe, induction of remission)
•
Treatment of ulcerative colitis
Indications for use
Labeled indications
Adults
•
Treatment of acute lymphoblastic leukemia (maintenance therapy)
Off-label indications
Adults
•
Treatment of Crohn's disease (moderate-to-severe, induction of remission)
•
Treatment of Crohn's disease (moderate-to-severe, maintenance of remission)
•
Treatment of acute promyelocytic leukemia (maintenance therapy)
•
Treatment of ulcerative colitis (moderate-to-severe, induction of remission)
•
Treatment of ulcerative colitis (moderate-to-severe, maintenance of remission)
Children
•
Treatment of Crohn's disease
•
Treatment of ulcerative colitis
Safety risks
Contraindications
Hypersensitivity to mercaptopurine or its components
Warnings and precautions
Immunosuppression, hepatosplenic T-cell lymphoma, skin cancer, sarcomas, cervical cancer
•
Maintain a high level of suspicion, as mercaptopurine has been associated with an increased risk for these complications.
Macrophage activation syndrome
•
Use caution in patients with autoimmune conditions, particularly IBD. Monitor for and treat infections such as EBV and CMV that might trigger macrophage activation syndrome.
Myelosuppression
•
Maintain a high level of suspicion, as mercaptopurine has been associated with an increased risk of myelosuppression, including anemia, leukopenia, and thrombocytopenia. Monitor CBC and adjust mercaptopurine dose accordingly. Reduce mercaptopurine dose when coadministered with allopurinol. Consider testing for TPMT or NUDT15 deficiency in patients with severe myelosuppression. Reduce dose by 10% in patients with homozygous TPMT or NUDT15 deficiency.
Specific populations
Renal impairment
CrCl ≥ 50 mL/min
•
Use acceptable. No dose adjustment required.
CrCl < 50 mL/min
•
Reduce starting dose. Titrate slowly. Consider increasing the dosing interval to q36-48h instead of reducing the dose.
Renal replacement therapy
Continuous renal replacement
•
Dose as in CrCl < 50 mL/min. Maximal frequency of q48h. Titrate with caution.
Intermittent hemodialysis
•
Dose as in CrCl < 50 mL/min. Maximal frequency of q48h. Titrate with caution.
Peritoneal dialysis
•
Dose as in CrCl < 50 mL/min. Maximal frequency of q48h. Titrate with caution.
Hepatic impairment
Any severity
•
Reduce starting dose. Monitor serum aminotransferases. Monitor for toxicity.
Pregnancy and breastfeeding
Pregnancy
All trimesters • Australia Category: D
•
Do not use. Evidence of fetal harm in humans.
Breastfeeding
Do not use during breastfeeding.
Unknown amount excreted in breastmilk.
Undetectable levels in breastfed infants.
Unlikely to cause adverse effects in breastfed infants.
Adverse reactions
Very common > 10%
•
Myelosuppression, diarrhea, nausea, loss of appetite, vomiting, malaise, skin rash
Common 1-10%
•
Acute pancreatitis, skin cancer, cervical cancer, ↑ liver enzymes, ↑ serum TBIL, urticaria, ↑ serum uric acid, oral ulcers, hyperpigmentation
Unknown frequency
•
Hepatic encephalopathy, hepatic necrosis, jaundice, fever, macrophage activation syndrome, hepatosplenic T-cell lymphoma, hemolytic anemia, oligozoospermia, hair loss, ascites, photosensitivity of skin, ↓ blood glucose, pulmonary fibrosis, tumor lysis syndrome
Interactions
Drug(s)
Check Interactions
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