Classes
DEA Class; Rx
Common Brand Names; Azasan, Imuran
- DMARDs, Immunomodulators;
- Immunosuppressants
Description
Oral and parenteral thiopurine immunosuppressive agent; metabolized to 6-mercaptopurine
Commonly used in transplant patients but also is useful in RA, lupus nephritis, and psoriatic arthritis
In gastroenterology, used in the treatment of Crohn’s disease and ulcerative colitis
Indications
Indicated for kidney transplant rejection prophylaxis.
For kidney transplant rejection prophylaxis.
Contraindications
Documented hypersensitivity
Pregnancy, lactation
Rheumatoid arthritis: Patients previously treated with alkylating agents
Adverse Effects
- Leukopenia (28-50%)
- Infection (20%)
- Lymphoma
- Abdominal pain
- Alopecia
- Arthralgia
- Bacterial, fungal, protozoal, viral infections
- Bone marrow suppression
- Diarrhea
- Fever
- Hepatotoxicity
- Macrocytic anemia
- Myalgia
- Nausea or vomiting
- Rash
- Skin cancer
- Steatorrhea
- Sweet syndrome (acute febrile neutrophilic dermatosis)
- Thrombocytopenia
Warnings
Long-term use increases risk of neoplasia
Increased risk of infection and hepatotoxicity; monitor liver function periodically; hepatic sinudoidal obstruction syndrome reported; discontinue therapy if suspected
Cases of JC virus-associated infection resulting in progressive multifocal leukoencephalopathy (PML), sometimes fatal, reported in patients treated with immunosuppressants, including azathioprine
Severe leukopenia, thrombocytopenia, anemias including macrocytic anemia, and/or pancytopenia may occur; severe bone marrow suppression may also occur; patients with or nucleotide diphosphatase (NUDT15) deficiency may be at an increased risk of myelotoxicity if patient receiving conventional doses of drug; delayed hematologic suppression may occur; prompt reduction in dosage or temporary withdrawal of drug may be necessary if there is rapid fall in or persistently low leukocyte count, or other evidence of bone marrow depression; leukopenia does not correlate with therapeutic effect; therefore dose should not be increased intentionally to lower white blood cell count
Pregnancy and Lactation
Pregnancy category: D
Lactation: Drug excreted at low levels in breast milk; use not recommended
Maximum Dosage
2.5 mg/kg/day PO for RA; 3—5 mg/kg/day PO or IV for kidney transplant rejection prophylaxis.
2.5 mg/kg/day PO for RA; 3—5 mg/kg/day PO or IV for kidney transplant rejection prophylaxis.
Safety and efficacy have not been established. Doses of 1—2 mg/kg/day PO for kidney transplant rejection prophylaxis have been used.
Safety and efficacy have not been established. Doses of 1—2 mg/kg/day PO for kidney transplant rejection prophylaxis have been used.
How supplied
Azathioprine
tablet
- 50mg
- 75mg
- 100mg
powder for injection
- 100mg/vial