Mercaptopurine Generic Name & Formulations
Legal Class
General Description
Pharmacological Class
How Supplied
Manufacturer
Mercaptopurine Indications
Indications
Mercaptopurine Dosage and Administration
Adults and Children
Renal Impairment
For patients with renal impairment (CrCl<50mL/min), use the lowest recommended starting dosage or increase the dosing interval to every 36 to 48 hours. Adjust based on ANC and adverse reactions.
Hepatic Impairment
For patients with hepatic impairment, use the lowest recommended starting dosage and adjust based on ANC and adverse reactions.
Other Modifications
Males with female partners of reproductive age: use effective contraception during treatment and for 3 months after the last dose.
Dose reduction may be required for patients with heterozygous or homozygous TPMT or NUDT15 deficiency. Consider all clinical information when interpreting results from phenotypic testing used to determine the level of thiopurine nucleotides or TPMT activity in erythrocytes, since some coadministered drugs can influence measurement of TPMT activity in blood and blood from recent transfusions will misrepresent a patient’s actual TPMT activity.
Mercaptopurine Contraindications
Contraindications
Mercaptopurine Boxed Warnings
Not Applicable
Mercaptopurine Warnings/Precautions
Warnings/Precautions
Not effective in CNS leukemia, acute myelogenous leukemia, chronic lymphocytic leukemia, the lymphomas (including Hodgkin's disease), or solid tumors. Myelosuppression; monitor CBCs weekly and adjust dose for severe cytopenias. Consider testing for TPMT and NUDT15 deficiency in patients who experience severe bone marrow toxicities or repeated myelosuppression. Monitor serum transaminase, alkaline phosphatase, and bilirubin levels at weekly intervals when starting therapy, then monthly thereafter; interrupt treatment if evidence of hepatotoxicity occurs. Concomitant other hepatotoxic drugs or with pre-existing liver disease; monitor LFTs more frequently. Immunosuppression. Inflammatory bowel disease. Renal or hepatic impairment. Elderly. Pregnancy, nursing mothers: not recommended.
Mercaptopurine Pharmacokinetics
Absorption
Food has been shown to decrease the exposure of mercaptopurine.
Distribution
Plasma protein binding averages 19%.
Elimination
Half-life is less than 2 hours following a single oral dose.
46% of dose recovered in the urine (as parent drug and metabolites) in the first 24 hours.
Mercaptopurine Interactions
Interactions
Mercaptopurine Adverse Reactions
Adverse Reactions
Mercaptopurine Clinical Trials
See Literature
Mercaptopurine Note
Notes
Formerly known under the brand name Purinethol.