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Thioguanine

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An anticancer medication.

Information about Thioguanine

Thioguanine (also referred to as 6-thioguanine and as tioguanine) is a purine analogue that is used in the therapy of acute and chronic myelogenous leukemias

Liver safety of Thioguanine

Thioguanine therapy is associated with minor, usually transient and asymptomatic elevations in serum aminotransferase levels and has also been linked to rare instances of cholestatic acute liver injury and to chronic liver injury, resulting in portal hypertension due to nodular regenerative hyperplasia. 

Mechanism of action of Thioguanine

Thioguanine (thye" oh gwa' neen) is a thiopurine, a purine analogue and antimetabolite.  It is a derivative of mercaptopurine (2-amino-6-mercaptopurine) and, like its parent molecule, inhibits purine metabolism, thus blocking DNA, RNA and subsequent protein synthesis.  Thioguanine also has antiinflammatory activity. 

FDA approval information for Thioguanine

Thioguanine was approved for use in the United States in 1966 and is commonly used in the therapy of acute and chronic myelogenous (nonlymphocytic) leukemias.  Thioguanine has also been used off-label to treat autoimmune diseases as a steroid sparing agent. 

Dosage and administration for Thioguanine

Thioguanine is available generically and under the brand name of Tabloid as tablets of 40 mg.  The usual dose is 1 to 3 mg per kilogram or 40 to 120 mg daily and it is typically given long term. 

Side effects of Thioguanine

Common side effects include nausea, abdominal upset, rash, aphthous ulcers and dose related bone marrow suppression.

 


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