Interaction of Local Anesthetics with Biomembranes Consisting of Phospholipids and Cholesterol : Mechanistic and Clinical Implications for Anesthetic and Cardiotoxic Effects
Joint Authors
Mizogami, Maki
Tsuchiya, Hironori
Source
Anesthesiology Research and Practice
Issue
Vol. 2013, Issue 2013 (31 Dec. 2013), pp.1-18, 18 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2013-09-23
Country of Publication
Egypt
No. of Pages
18
Main Subjects
Abstract EN
Despite a long history in medical and dental application, the molecular mechanism and precise site of action are still arguable for local anesthetics.
Their effects are considered to be induced by acting on functional proteins, on membrane lipids, or on both.
Local anesthetics primarily interact with sodium channels embedded in cell membranes to reduce the excitability of nerve cells and cardiomyocytes or produce a malfunction of the cardiovascular system.
However, the membrane protein-interacting theory cannot explain all of the pharmacological and toxicological features of local anesthetics.
The administered drug molecules must diffuse through the lipid barriers of nerve sheaths and penetrate into or across the lipid bilayers of cell membranes to reach the acting site on transmembrane proteins.
Amphiphilic local anesthetics interact hydrophobically and electrostatically with lipid bilayers and modify their physicochemical property, with the direct inhibition of membrane functions, and with the resultant alteration of the membrane lipid environments surrounding transmembrane proteins and the subsequent protein conformational change, leading to the inhibition of channel functions.
We review recent studies on the interaction of local anesthetics with biomembranes consisting of phospholipids and cholesterol.
Understanding the membrane interactivity of local anesthetics would provide novel insights into their anesthetic and cardiotoxic effects.
American Psychological Association (APA)
Tsuchiya, Hironori& Mizogami, Maki. 2013. Interaction of Local Anesthetics with Biomembranes Consisting of Phospholipids and Cholesterol : Mechanistic and Clinical Implications for Anesthetic and Cardiotoxic Effects. Anesthesiology Research and Practice،Vol. 2013, no. 2013, pp.1-18.
https://search.emarefa.net/detail/BIM-461389
Modern Language Association (MLA)
Tsuchiya, Hironori& Mizogami, Maki. Interaction of Local Anesthetics with Biomembranes Consisting of Phospholipids and Cholesterol : Mechanistic and Clinical Implications for Anesthetic and Cardiotoxic Effects. Anesthesiology Research and Practice No. 2013 (2013), pp.1-18.
https://search.emarefa.net/detail/BIM-461389
American Medical Association (AMA)
Tsuchiya, Hironori& Mizogami, Maki. Interaction of Local Anesthetics with Biomembranes Consisting of Phospholipids and Cholesterol : Mechanistic and Clinical Implications for Anesthetic and Cardiotoxic Effects. Anesthesiology Research and Practice. 2013. Vol. 2013, no. 2013, pp.1-18.
https://search.emarefa.net/detail/BIM-461389
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-461389