About this Journal Submit a Manuscript Table of Contents
Journal of Biomedicine and Biotechnology
Volume 2012 (2012), Article ID 170958, 7 pages
http://dx.doi.org/10.1155/2012/170958
Research Article

Vasoconstriction Potency Induced by Aminoamide Local Anesthetics Correlates with Lipid Solubility

1Department of Anesthesiology and Pain Medicine, Gyeongsang National University Hospital, Jinju 660-702, Republic of Korea
2Department of Anesthesiology and Pain Medicine, Gyeongsang National University School of Medicine, Jinju 660-772, Republic of Korea
3Division of Chemistry, Gyeongnam Sciences High School, Jinju 660-851, Republic of Korea
4Department of Information Statistics and RINS, Gyeongsang National University, Jinju 660-701, Republic of Korea
5Department of Oral and Maxillofacial Surgery, Gyeongsang National University Hospital, Jinju 660-702, Republic of Korea
6Institute of Health Sciences, Gyeongsang National University School of Medicine, Jinju 660-772, Republic of Korea

Received 25 February 2012; Accepted 18 April 2012

Academic Editor: Dobromir Dobrev

Copyright © 2012 Hui-Jin Sung et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

Abstract

Aminoamide local anesthetics induce vasoconstriction in vivo and in vitro. The goals of this in vitro study were to investigate the potency of local anesthetic-induced vasoconstriction and to identify the physicochemical property (octanol/buffer partition coefficient, pKa, molecular weight, or potency) of local anesthetics that determines their potency in inducing isolated rat aortic ring contraction. Cumulative concentration-response curves to local anesthetics (levobupivacaine, ropivacaine, lidocaine, and mepivacaine) were obtained from isolated rat aorta. Regression analyses were performed to determine the relationship between the reported physicochemical properties of local anesthetics and the local anesthetic concentration that produced 50% (ED50) of the local anesthetic-induced maximum vasoconstriction. We determined the order of potency (ED50) of vasoconstriction among local anesthetics to be levobupivacaine > ropivacaine > lidocaine > mepivacaine. The relative importance of the independent variables that affect the vasoconstriction potency is octanol/buffer partition coefficient > potency > pKa > molecular weight. The ED50 in endothelium-denuded aorta negatively correlated with the octanol/buffer partition coefficient of local anesthetics ( ๐‘Ÿ 2 = 0 . 9 5 6 3 ; ๐‘ƒ < 0 . 0 0 1 ). The potency of the vasoconstriction in the endothelium-denuded aorta induced by local anesthetics is determined primarily by lipid solubility and, in part, by other physicochemical properties including potency and pKa.