Colchicine Pharmacokinetics and Mechanism of Action

Title:Colchicine Pharmacokinetics and Mechanism of Action

Volume: 24 Issue: 6

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

Affiliation:

• 2nd Department of Cardiology, Medical School, Attikon Hospital, National and Kapodistrian University of Athens, Athens,Greece

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

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.

Cite this article as:

Angelidis Christos*, Kotsialou Zoi , Kossyvakis Charalampos , Vrettou Agathi-Rosa, Zacharoulis Achilleas, Kolokathis Fotios , Kekeris Vasilios and Giannopoulos Georgios, Colchicine Pharmacokinetics and Mechanism of Action, Current Pharmaceutical Design 2018; 24 (6) . https://dx.doi.org/10.2174/1381612824666180123110042