Azathioprine

DEA Class;  Rx

Common Brand Names; Azasan, Imuran

  • DMARDs, Immunomodulators; 
  • Immunosuppressants

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

Indicated for kidney transplant rejection prophylaxis.

For kidney transplant rejection prophylaxis.

For the treatment of Behcet’s syndrome.
For the treatment of Crohn’s disease.
For the treatment of ulcerative colitis.
For the treatment of myasthenia gravis in patients who are poorly controlled with cholinesterase inhibitor therapy.
For the treatment of psoriasis.

Documented hypersensitivity

Pregnancy, lactation

Rheumatoid arthritis: Patients previously treated with alkylating agents

  • 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

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 category: D

Lactation: Drug excreted at low levels in breast milk; use not recommended

Adults

2.5 mg/kg/day PO for RA; 3—5 mg/kg/day PO or IV for kidney transplant rejection prophylaxis.

Elderly

2.5 mg/kg/day PO for RA; 3—5 mg/kg/day PO or IV for kidney transplant rejection prophylaxis.

Adolescents

Safety and efficacy have not been established. Doses of 1—2 mg/kg/day PO for kidney transplant rejection prophylaxis have been used.

Children

Safety and efficacy have not been established. Doses of 1—2 mg/kg/day PO for kidney transplant rejection prophylaxis have been used.

Azathioprine

tablet

  • 50mg
  • 75mg
  • 100mg

powder for injection

  • 100mg/vial

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