Azathioprine - Adverse Effects

Adverse Effects

Nausea and vomiting are common adverse effects, especially at the beginning of a treatment. Such cases are met with taking azathioprine after meals or transient intravenous administration. Side effects that are probably hypersensitivity reactions include dizziness, diarrhea, fatigue, and skin rashes. Hair loss is often seen in transplant patients receiving the drug, but rarely occurs under other indications. Because azathioprine suppresses the bone marrow, patients can develop anaemia and will be more susceptible to infection; regular monitoring of the blood count is recommended during treatment. Acute pancreatitis can also occur, especially in patients with Crohn's disease.

The enzyme thiopurine S-methyltransferase (TPMT) is responsible for various activation and deactivation steps in azathioprine's mechanism of action, and genetic polymorphisms of TPMT leads to decreased methylation and decreased inactivation of 6MP. This can result in dangerous bone marrow suppression, and an assay of TPMT in red blood cells or a TPMT gene test can avoid this complication. TMPT polymorphisms occur with a frequency of about 5%, meaning that 0.3% of patients have defects on both of their TMPT genes; they are homozygous.

Under FDA rules, like many other immunosuppressants, the use of this drug excludes eligibility for blood donation.

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