Azathioprine
- Atc Codes:L04AX01
- CAS Codes:446-86-6
- PHARMGKB ID:446-86-6
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
- Toxicological Effects
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Inhibits
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Azathioprin, Immunoprin, Imurek; Belgium: Azathioprine, Imuran; Bulgaria: Azathioprine, Imuran; Cyprus: Imuprin, Imuran; Czech Republic: Azaprine, Azathioprin, Immunoprin, Imuran; Denmark: Azathioprin, Imurel; Estonia: Imuran; Finland: Azamun, Azathioprin, Imurel; France: Azathioprine, Imurel; Germany: Aza-Q, Azaderm, Azafalk, Azaimun, Azamedac, Azathioprin, Azathioprine, Colinsan, Imurek, Imurel, Zytrim; Greece: Azathioprine; Hungary: Azathioprin, Imuran; Ireland: Azathioprine, Imuger, Imuran; Italy: Azafor, Azatioprina, Immunoprin; Latvia: Imuran; Lithuania: Imuran; Luxembourg: Imuran; Malta: Azathioprine; Netherlands: Azathioprine, Imuran; Poland: Azapharm, Azathioprine, Imuran; Portugal: Azatioprina, Imuran; Romania: Imuran; Slovakia: Imuran, Immunoprin; Slovenia: Imuran; Spain: Imurel; Sweden: Azathioprin, Imurel; UK: Imuran.
North America
Canada: Azathioprine, Imuran; USA: Azasan, Azathioprine, Imuran.
Latin America
Argentina: Azatioprina, Imurán; Brazil: Imunen, Imuran; Mexico: Azatrilem, Imurán.
Asia
Japan: Azanin, Imuran.
Drug combinations
Chemistry
Azathioprine: C~9~H~7~N~7~O~2~S. Mw: 277.26. (1) 1H-Purine, 6-[(1-methyl-4-nitro-1H-imidazol-5-yl)thio]; (2) 6-[(1-Methyl-4-nitroimidazol-5-yl)thio]purine. CAS-446-86-6 (1962).
Pharmacologic Category
Immunosuppressive Agents. Biologic Response Modifiers. Disease-modifying Antirheumatic Drugs. (ATC-Code: L04AX01).
Mechanism of action
Antagonizes purine metabolism and may inhibit synthesis of DNA, RNA, and proteins. May also interfere with cellular metabolism and inhibit mitosis.
Therapeutic use
Kidney transplants. Active rheumatoid arthritis.
Pregnancy and lactiation implications
Should not be used to treat arthritis during pregnancy. The potential benefit to the mother vs possible risk to the fetus should be considered when treating other disease states. Not recommended for use during lactation.
Unlabeled use
Solid organ (nonrenal) transplants. Corticosteroid-dependent Crohn’s disease. Ulcerative colitis.
Contraindications
Hypersensitivity to azathioprine or any component of the formulation. Pregnancy.
Warnings and precautions
Gastrointestinal toxicity (reversible) may occur within the first several weeks of therapy. Dose-related hematologic toxicities (pancytopenia, thrombocytopenia) may occur. Chronic immunosuppression increases the risk of serious infections and of neoplasia. Use with caution in hepatic or renal impairment. Patients with genetic deficiency of thiopurine methyltransferase, and patients on concurrent therapy with drugs which may inhibit TPMT (e.g. olsalazine) or xanthine oxidase (e.g. allopurinol) may be sensitive to myelosuppressive effects. Concomitant use with mercaptopurine may result in profound myelosuppression. Patients on concurrent therapy with drugs which may inhibit TPMT (e.g. olsalazine) or xanthine oxidase (e.g. allopurinol) may be sensitive to myelosuppressive effects.