Colchicine Pharmacokinetics and Mechanism of Action

Author(s): Christos Angelidis*, Zoi Kotsialou, Charalampos Kossyvakis, Agathi-Rosa Vrettou, Achilleas Zacharoulis, Fotios Kolokathis, Vasilios Kekeris, Georgios Giannopoulos.

Journal Name: Current Pharmaceutical Design

Volume 24 , Issue 6 , 2018

Abstract:

Colchicine is a tricyclic, lipid-soluble alkaloid derived from the plant of the Lily family Colchicum autumnale, sometimes called the “autumn crocus”. It is predominantly metabolized in the gastrointestinal tract. Two proteins, P-glycoprotein (P-gp) and CYP3A4 seem to play a pivotal role, governing its pharmacokinetic. The commonest side effects are gastrointestinal (nausea, vomiting and particularly dose-related-diarrhea) occurring in 5-10% of patients. Colchicine exerts its unique action mainly through inhibition of microtubule polymerization. Microtubule polymerization affects a variety of cellular processes including maintenance of shape, signaling, division, migration, and cellular transport. Colchicine interferes with several inflammatory pathways including adhesion and recruitment of neutrophils, superoxide production, inflammasome activation, the RhoA/Rho effector kinase (ROCK) pathway and the tumor necrosis factor alpha (TNF-α) -induced nuclear factor κΒ (NF-κΒ) pathway attenuating the inflammatory response. This concise paper attempts to give a brief review of its pharmacokinetic properties and its main mechanisms of action.

Keywords: Colchicine, inflammation, mechanism of action, microtubules, pharmacokinetics, toxicity.

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Article Details

VOLUME: 24
ISSUE: 6
Year: 2018
Page: [659 - 663]
Pages: 5
DOI: 10.2174/1381612824666180123110042
Price: $58

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