Mercaptopurine

Indications
 Oral
Acute lymphatic leukaemia
Adult: Usual maintenance dose: Initially, 1.5-2.5 mg/kg daily as a single dose, usually used in combination with methotrexate. Dose may vary individually based on response and tolerance. Monitor blood counts at least once wkly. Withdraw treatment immedietely if there is a sharp drop in the white cell count or severe bone-marrow depression. May resume treatment slowly and carefully if white cell count remains constant for 2-3 days or rises. Reduce dose when used with allopurinol.
Child: Usual maintenance dose: Initially, 1.5-2.5 mg/kg daily as a single dose, usually used in combination with methotrexate. Dose may vary individually based on response and tolerance. Monitor blood counts at least once wkly. Withdraw treatment immedietely if there is a sharp drop in the white cell count or severe bone-marrow depression. May resume treatment slowly and carefully if white cell count remains constant for 2-3 days or rises. Reduce dose when used with allopurinol.
Renal impairment: Dosage may need to be reduced.
Hepatic impairment: Dosage may need to be reduced
Oral
Crohn's disease
Adult: Initially 1-1.5 mg/kg daily, may increase to 125 mg daily.
Child: Initially 1-1.5 mg/kg daily increased to a max of 75 mg daily
Renal impairment: Dosage may need to be reduced.
Hepatic impairment: Dosage may need to be reduced.
Contraindications
 Pregnancy and lactation. Prior resistance to mercaptopurine or thioguanine; severe liver disease; severe bone marrow suppression.
Warnings / Precautions
 Hepatic or renal dysfunction; monitor hepatic function periodically. Mercaptopurine is potentially carcinogenic. Thiopurine S-methyl transferase (TPMT) deficiency; porphyria.
Adverse Reactions
 Hyperuricaemia, bone marrow toxicity, hypoplasia, anorexia, diarrhoea, leukopenia, thrombocytopenia, intestinal ulceration, crystalluria with haematuria, immunosuppression, interstitial pneumonitis. Cutaneous hyperpigmentation, alopecia.
Potentially Fatal: Myelosuppression; hepatotoxicity, cholestatic jaundice.
Drug Interactions
 Anticoagulant action of warfarin may be inhibited by mercaptopurine. Enhanced toxicity with myelosuppressive drugs.
Potentially Fatal: Effects enhanced by allopurinol (reduce dose of mercaptopurine). Other hepatotoxic drugs (e.g. doxorubicin) potentiate toxicity.
See Below for More mercaptopurine Drug Interactions
Mechanism of Actions
 Mercaptopurine is a purine antagonist which is converted intracellularly into its active nucleotides, including thioinosinic acid. The nucleotides inhibit several reactions which ultimately interferes with nucleic acid synthesis and prevents the formation of RNA and DNA.
Absorption: Variable and incomplete; peak plasma concentrations within 2 hr (oral).
Distribution: Widely distributed; crosses the blood-brain barrier and CSF.
Metabolism: Hepatic by methylation, oxidation and formation of inorganic sulfates.
Excretion: Urine (as metabolites and unchanged drug).
Administration
 Should be taken on an empty stomach. (Best taken on an empty stomach 1 hr before or 2 hr after meals. Ensure adequate fluid intake.)
Storage Conditions
 Oral: Store at 20-25°C
ATC Classification
 L01BB02 - mercaptopurine ; Belongs to the class of antimetabolites, purine analogues. Used in the treatment of cancer.
Storage
 Oral: Store at 20-25°C
Available As
  • Mercaptopurine 200 mg
  • Mercaptopurine 50 mg

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