ColchicineColchicine Update: 2008
Section snippets
Methods
Using relevant pertinent English and non-English articles with English abstracts or English translations, found by a MEDLINE® (Medical Literature Analysis and Retrieval System Online) search and published up to July 2008 as a primary source of information, the existing literature regarding colchicines was reviewed. The focus was on colchicine pharmacology, toxicology, mechanisms of action, and clinical applications in gout and other medical conditions. Initial MEDLINE searches used the keywords
Update on Clinical Pharmacology of Colchicine
Colchicine is readily bioavailable after oral administration via uptake in the jejunum and ileum, and the lipophilic nature of colchicine allows it to be absorbed readily by multiple cell types and to bind to its primary target, tubulin (discussed below), serving as a reservoir of the drug (4). Absolute colchicine bioavailability is less than 50% (6, 7). A schematic for colchicine disposition is provided in Figure 1. In brief, colchicine is predominantly eliminated by biliary excretion and
Discussion
Despite approximately 2000 years of use, the broad effects of colchicine are only beginning to be explored for therapeutic uses beyond gout and certain other rheumatic diseases, including certain forms of pericarditis. The results of ongoing and future clinical trials for optimization of colchicine-dosing regimens should allow for safer utilization of the drug without undue loss of clinical efficacy. For example, guidelines for colchicine dosing for acute gout are being refined, with lower
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The author has received support from VA Research Service, National Institutes of Health and is a consultant for AR Scientific, Regeneron, ARDEA, Novartis, Pfizer, TAP, Savient, BioCryst.