Review
Copyright ©The Author(s) 2015. Published by Baishideng Publishing Group Inc. All rights reserved.
World J Anesthesiol. Jul 27, 2015; 4(2): 17-29
Published online Jul 27, 2015. doi: 10.5313/wja.v4.i2.17
Pharmacokinetics and pharmacodynamics of lignocaine: A review
Laurence Weinberg, Benjamin Peake, Chong Tan, Mehrdad Nikfarjam
Laurence Weinberg, Anesthesia Perioperative Pain Unit, University of Melbourne, Victoria 3084, Australia
Laurence Weinberg, Benjamin Peake, Chong Tan, Department of Anesthesia, Austin Hospital, Victoria 3084, Australia
Laurence Weinberg, Mehrdad Nikfarjam, Department of Surgery, University of Melbourne, Victoria 3084, Australia
Mehrdad Nikfarjam, Department of Hepatobiliary Surgery, Austin Hospital, Victoria 3084, Australia
Author contributions: Weinberg L, Peake B, Tan C and Nikfarjam M contributed to this paper.
Conflict-of-interest statement: There are no conflicts of interests declared by any of the authors.
Open-Access: This article is an open-access article which was selected by an in-house editor and fully peer-reviewed by external reviewers. It is distributed in accordance with the Creative Commons Attribution Non Commercial (CC BY-NC 4.0) license, which permits others to distribute, remix, adapt, build upon this work non-commercially, and license their derivative works on different terms, provided the original work is properly cited and the use is non-commercial. See: http://creativecommons.org/licenses/by-nc/4.0/
Correspondence to: Laurence Weinberg, BSc, MD, MBBCh, MRCP, DipCritCareEcho, FANZCA, Department of Anesthesia, Austin Hospital, Studley Road, Victoria 3084, Australia. laurence.weinberg@austin.org.au
Telephone: +61-3-94965000 Fax: +61-3-94596421
Received: November 2, 2014
Peer-review started: November 4, 2014
First decision: November 27, 2014
Revised: March 20, 2015
Accepted: April 10, 2015
Article in press: April 14, 2015
Published online: July 27, 2015
Processing time: 266 Days and 16.9 Hours
Abstract

Lignocaine is an essential drug on World Health Organisation essential drug list, considered efficacious, safe and cost-effective for any health-care system. Despite its ubiquitous use in medicine and surgery, there are few detailed reviews of its pharmacokinetics and pharmacodynamics. Being an amide-type local anesthetic and Class 1b antiarrhythmic, lignocaine is most frequently used clinically for its anesthetic and antiarrhythmic benefits. However, lignocaine has important antinociceptive, immuno-modulating, and anti-inflammatory properties. Information pertaining to the pharmacokinetics and pharmacodynamics of lignocaine was examined by performing a literature search of PubMed, Embase and MEDLINE (via Ovid), pharmacology textbooks and online sources. We present a focused synopsis of lignocaine’s pharmacological composition, indications for use and mechanisms of action, focusing on its anti-inflammatory, immuno-modulating and analgesia effects. In addition we review the dosing regimes and infusion kinetics of lignocaine in the clinical setting. Finally, we review the evidence for ligocaine’s modulation of the inflammatory response during major surgery and its specific effects on cancer recurrence. These indirect effects of local anesthetics in tumor development may stem from the reduction of neuroendocrine responses to the stress response elicited by major surgery and tissue damage, enhanced preservation of immune-competence, in addition to opioid-sparing effects of modulating tumor growth.

Keywords: Lignocaine; Humans; Pharmacokinetics; Pharmacodynamics; Adult

Core tip: Lignocaine is a widely used amide-type local anesthetic and Class 1b antiarrhythmic. In addition to its anesthetic and antiarrhythmic effects, lignocaine has important analgesic, antinociceptive, immuno-modulating, and anti-inflammatory properties. Understanding the pharmacokinetics and pharmacodynamics of lignocaine will enable clinicians to safely prescribe lignocaine in a variety of clinical settings.