Colchicine may interfere with cyclosporin pharmacokinetics by increasing cyclosporin plasma levels either by enhancing cyclosporin absorption or by reducing its hepatic metabolism. 7.7 Main adverse effects Gastrointestinal symptoms are a common complication of chronic colchicine therapy. Thus the dose of colchicine is usually limited by gastrointestinal toxicity. Binding of colchicine and thiocolchicoside to human serum proteins and blood cells. Sabouraud A(1), Chappey O, Dupin T, Scherrmann JM. Author information: (1)INSERM U26, Hôpital F. Widal, Paris, France. Colchicine reference guide for safe and effective use from the American Society of Health-System Pharmacists (AHFS DI). INDICATIONS. Colchicine capsules are indicated for prophylaxis of gout flares in adults. Limitations Of Use. The safety and effectiveness of colchicine capsules for acute treatment of gout flares during prophylaxis has not been studied. To review the literature and provide an updates on the mechanisms of action and therapeutic uses of oral colchicine in arthritis and inflammatory conditions. The primary mechanism of action of colchicine is tubulin disruption. This leads to subsequent down regulation of multiple inflammatory Colchicine disposition involves both active biliary and renal excretion of parent drug, and at least in mammals a substantial fraction undergoes hepatic demethylation prior to excretion. 2 About 10-20% of colchicine is excreted unchanged in urine; between 5 and 50% of an intravenous dose is eliminated in the bile within 48 h [3]. Metabolism. A published in vitro human liver microsome study showed that about 16% of Colchicine is metabolized to 2-O-demethylColchicine and 3-O-demethylColchicine (2- and 3-DMC, respectively) by CYP3A4. Glucuronidation is also believed to be a metabolic pathway for Colchicine. Excretion. In a published study in healthy volunteers, 40 to 65% of the total absorbed dose of Colchicine (1 mg. P450-mediated biotransformation pathway of colchicine with the CYP3A4, while colchicine inhibits the expression of this enzyme. Colchicine is a medication used to treat gout and Behçet's disease. In gout it is less preferred to NSAIDs or steroids. Other uses include the prevention of pericarditis and familial Mediterranean fever.