Τίτλος:
Colchicine pharmacokinetics and mechanism of action
Γλώσσες Τεκμηρίου:
Αγγλικά
Περίληψη:
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. © 2017 Bentham Science Publishers.
Συγγραφείς:
Angelidis, C.
Kotsialou, Z.
Kossyvakis, C.
Vrettou, A.-R.
Zacharoulis, A.
Kolokathis, F.
Kekeris, V.
Giannopoulos, G.
Περιοδικό:
Current Pharmaceutical Design
Εκδότης:
Bentham Science Publishers B.V.
Λέξεις-κλειδιά:
antineoplastic agent; atorvastatin; calcium channel blocking agent; cimetidine; clarithromycin; colchicine; cyclosporine; endothelial leukocyte adhesion molecule 1; erythromycin; glucocorticoid; hydroxymethylglutaryl coenzyme A reductase inhibitor; immunoglobulin enhancer binding protein; inflammasome; L selectin; macrolide; mevinolin; proteinase inhibitor; pyrrole derivative; Rho kinase; simvastatin; superoxide; tolbutamide; tumor necrosis factor; antigout agent; colchicine; CYP3A4 protein, human; cytochrome P450 3A, acute kidney failure; acute liver failure; antiinflammatory activity; antioxidant activity; area under the curve; bone marrow suppression; cardiovascular disease; cell division; cell migration; cell transport; diarrhea; disseminated intravascular clotting; dose response; drug absorption; drug bioavailability; drug blood level; drug clearance; drug competition; drug distribution; drug dose reduction; drug dose titration; drug efficacy; drug elimination; drug half life; drug mechanism; drug metabolism; drug overdose; drug structure; drug withdrawal; food drug interaction; grapefruit juice; human; hypovolemia; maximum plasma concentration; microtubule assembly; nausea; peripheral neuropathy; priority journal; respiratory failure; Review; rhabdomyolysis; seizure; signal transduction; vomiting; drug effect; metabolism; microtubule, ATP Binding Cassette Transporter, Subfamily B, Member 1; Colchicine; Cytochrome P-450 CYP3A; Gout Suppressants; Humans; Microtubules
DOI:
10.2174/1381612824666180123110042
