Mercaptopurine
- Atc Codes:L01BB02
- CAS Codes:6112-76-1#50-44-2
- PHARMGKB ID:6112-76-1#50-44-2
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Unlabeled Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Puri-Nethol; Belgium: Puri-Nethol; Bulgaria: Puri-Nethol; Czech Republic: Puri-Nethol; Estonia: Puri-Nethol; France: Purinethol; Germany: Mercaptopurin, Purinethol, Puri-Nethol; Greece: Mercaptopurina, Purinethol; Ireland: Puri-Nethol; Italy: Purinethol; Latvia: Puri-Nethol; Lithuania: Puri-Nethol; Luxembourg: Puri-Nethol; Malta: Puri-Nethol; Netherlands: Puri-Nethol; Poland: Mercaptopurinum, Purinethol; Romania: Puri-Nethol; Slovakia: Puri-Nethol; Slovenia: Puri-Nethol; Spain: Mercaptopurina; Sweden: Puri-Nethol; UK: Puri-Nethol.
North America
Canada: Purinethol; USA: Mercaptopurine, Purinethol.
Latin America
Argentina: Mercaptopurina, Puri-Nethol, Varimer; Brazil: Puri-Nethol; Mexico: Purinethol.
Asia
Japan: Leukerin.
Drug combinations
Chemistry
Mercaptopurine: C~5~H~4~N~4~S H~2~O. Mw: 170.19. (1) 6H-Purine-6-thione, 1,7-dihydro-, monohydrate; (2) Purine-6-thiol monohydrate. CAS-6112-76-1; CAS-50-44-2 (anhydrous).
Pharmacologic Category
Antineoplastic Agents; Antimetabolites. Immunosuppressive Agents. (ATC-Code: L01BB02).
Mechanism of action
Acts as false metabolite and is incorporated into DNA and RNA, eventually inhibiting their synthesis.
Therapeutic use
Treatment (maintenance and induction) of acute lymphoblastic leukemia.
Pregnancy and lactiation implications
Might cause fetal harm. Use with particular caution during 1^st^ trimester of pregnancy (increased incidence of abortion). Avoid use in pregnant women unless benefits outweigh risks.
Unlabeled use
Steroid-sparing agent for corticosteroid-dependent Crohn’s disease and ulcerative colitis. Maintenance of remission in Crohn’s disease. Fistulizing Crohn’s disease.
Contraindications
Hypersensitivity to mercaptopurine or any component of the formulation. Patients whose disease showed prior resistance to mercaptopurine or thioguanine. Severe liver disease, severe bone marrow suppression. Pregnancy.
Warnings and precautions
Hazardous agent. Hepatotoxicity might occur (use with caution with other hepatotoxic drugs or in dosages >2.5 mg/kg/day). Lethargy and confusion may be more prominent signs of infection. Use with caution in prior bone marrow suppression. Patients with genetic deficiency of thiopurine methyltransferase may be sensitive to myelosuppressive effects. Concomitant use with azathioprine may result in profound myelosuppression. Patients on concurrent therapy with drugs which may inhibit thiopurine s-methyltransferase)(e.g. olsalazine) or xanthine oxidase (e.g. allopurinol) might be sensitive to myelosuppressive effects. Immune response to vaccines might be diminished.