Update on colchicine, 2017

Abstract

Colchicine is an ancient medication that is currently approved for the treatment of gout and FMF. However, colchicine has a wide range of anti-inflammatory activities, and studies indicate that it may be beneficial in a variety of other conditions. This paper reviews the evidence for the well-established use of colchicine in gout, as well as several other rheumatic diseases. In addition, we highlight the potential benefit of colchicine in cardiac disease, including coronary artery disease in patients both with and without gout.

Keywords: cardiovascular disease; colchicine; gout; inflammation.

© The Author 2018. Published by Oxford University Press on behalf of the British Society for Rheumatology. All rights reserved. For Permissions, please email: journals.permissions@oup.com.

Figures

Fig. 1

Major mechanisms of colchicine metabolism and excretion Colchicine is initially absorbed in the jejunum and ileum. P-Glycoprotein (P-gp) on the apical surface of enterocytes secretes a fraction of unchanged colchicine back into the lumen, from which it can be excreted. The remainder enters the systemic circulation and passes through the kidneys, where unchanged colchicine is excreted through glomerular filtration as well as through direct renal P-gp secretion into the proximal tubule. Within hepatocytes, colchicine undergoes demethylation into three distinct metabolites through the action of CYP3A4. These metabolites, along with a portion of unchanged colchicine, are secreted into the bile via hepatic P-gp, and thence into the duodenum for potential excretion.