Azathioprine - Pharmacology, Mechanism of Action, Side Effects

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Case description

Azathioprine is an immunosuppressant used in various inflammatory diseases including RA and is the preferred DMARD in SLE patient who are pregnancy. It is also used to prevent renal transplant rejection. Azathioprine is a prodrug of 6-mercaptopurine which is metabolised through different pathways. Metabolism into 6-thioguanine nucleotides is of benefit because this is where azathioprine exerts its immunosuppressive effects.

An alternative metabolic pathway of 6-Mercaptopurine is via xanthine oxidase which will form 6 thiouric acid which is non toxic and can be cleared by the body. Another alternate metabolic pathway of mercaptopurine is via thiopurine methyltransferase forming 6methyl mercaptopurine which is also non toxic and can be cleared by the body. Myelosuppression is the primary side effect and can lead to malignancy especially skin cancer and lymphoma.

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