Azathioprine

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Azathioprine 

• major cytotoxic used for immunosupression + widely used to control tissue rejection in transplant surgery.

Mechanism

• Metabolised to yield mercaptopurine (6-MP). 6-MP has no intrinsic activity but requires transformation to 6-thioguanine nucleotides which interfere with DNA synthesis.
• Inhibits lymphocyte clonal proliferation in the induction phase of immune reaction.
  • ↓ Cell mediated immune reaction (T lymphocytes) 
  • ↓ Ab mediated immune reaction (B lymphocytes) 
  • ↓ other inflammatory effects that depend on cell division

Pharmakokinetics

• Well absorbed orally
• 98% cleared by hepatic metabolism to 6-MP
• Further converted by xanthine oxidase (XO) and thiopurinemethyl-transferase
•  T_1/2 ~ 12 min. 

Interactions

• if given with XO inhibitor (allopurinol), accumulation and toxicity will occur unless dose ↓ ~30%.

Adverse Effects:

• Bone marrow suppression
• Diarrhoea
• Skin eruptions
• Mild hepatotoxicity

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