AZATHIOPRINE

Immunosuppressive medicine

Dosage Forms

Tablet

50 mg

Powder for injection

100 mg

Uses

  • Rheumatoid arthritis
  • Psoriatic arthritis
  • Suppression of transplant rejection
  • Inflammatory bowel disease
  • Severe refractory eczema
  • Generalised myasthenia gravis
  • Autoimmune diseases
  • Systemic lupus erythematosus (SLE)

Dose and Duration

Only use the IV route if oral route is not possible. Give IV injection over 1 minute followed by 50 ml sodium chloride intravenous infusion
Suppression of transplant rejection
Adult:by mouth or IV injection, up to 5 mg/kg on the day of surgery, then reduced according to response to a maintenance dose of 1–4 mg/kg per day or by IV infusion, 1–2.5 mg/kg/day adjusted according to response. Maintain therapy indefinitely
Child 1 month–18 years: by mouth or IV infusion maintenance dose of 1–3 mg/kg given 1–2 times a day, adjusted according to response
Severe refractory eczema
Adult: by mouth, normal or high thiopurine methyl transferase (TPMT) activity, 1–3 mg/kg per day: intermediate TPMT activity, 0.5–1.5 mg/kg per day
Generalised myasthenia gravis (in conjunction with a steroid)
Adult: 0.5–1 mg/kg/day increased over 3–4 weeks to 2.0 - 2.5 mg/kg/day
Child 1 month–18 years:by mouth, 1 mg/kg once a day, adjusted according to response (max 3 mg/kg) Consider withdrawal if there is no improvement within 3 months
Other conditions
Adult: by mouth or IV infusion, 1–3 mg/kg/day adjusted according to response
Child 1 month–18 years:by mouth, 1 mg/kg once a day, adjusted according to response (max 3 mg/kg) Consider withdrawal if there is no improvement within 3 months

Preparation

  • Reconstitute powder according to manufacturer’s instructions

Contraindications

  • Hypersensitivity to azathioprine or mercaptopurine

Side Effects

  • Viral, fungal and bacterial infections
  • Bone marrow suppression, leucopoenia, thrombocytopenia
  • Hepatotoxicity
  • Nausea, anorexia
  • Stevens-Johnson syndrome

Interactions

  • Allopurinol (increased effects and toxicity of azathioprine)
  • Cotrimoxazole, trimethoprim (increased risk of haematological toxicity)
  • Live vaccines (reduced immune response to vaccine)
  • Warfarin (anticoagulant effect possibly reduced)

Patient Instructions

  • Swallow your tablets at least 1 hour before or 3 hours af ter food or milk
  • Report any signs of bone marrow suppression such as unexplained bruising or bleeding, purpura, infection or sore throat to your doctor
  • Take with plenty of fluid
  • Report immediately to health worker if jaundice occurs

Pregnancy

  • Can be used

Breastfeeding

  • Do not use

⚠️ Caution

  • Monitor full blood counts every week, or more frequently in high doses, in renal and hepatic failure for the first 4 weeks and at least every 3 months thereafter
  • Reduce dose in the elderly, when given with allopurinol and in renal and hepatic impairment
  • Withdraw treatment immediately if interstitial nephritis occurs
  • Intravenous injection is alkaline and very irritant, only use this route if oral route is not possible
  • Transplant patients who become pregnant should continue with azathioprine under close supervision. It can cause premature birth, spontaneous abortion and low birth weight and teratogenicity
  • Only use in breast feeding if likely benefit outweighs risk