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Cited by 87Anesthesia and Pain ManagementDental Anxiety and Anesthesia TechniquesVeterinary Pharmacology and Anesthesia

The Quaternary Lidocaine Derivative, QX-314, Produces Long-lasting Local Anesthesia in Animal Models In Vivo

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Lim, Tony K. Y., MacLeod, Bernard A., Ries, Craig R., Schwarz, Stephan K. W.·2007·Anesthesiology
DOI 10.1097/01.anes.0000270758.77314.b4
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Abstract

Background: QX-314 is a quaternary lidocaine derivative considered to be devoid of clinically useful local anesthetic activity. However, several reports document that extracellular QX-314 application affects action potentials. Hence, the authors tested the hypothesis that QX-314 could produce local anesthesia in animal models in vivo. Methods: The authors tested QX-314 (10, 30, and 70 mM) in three standard in vivo local anesthetic animal models, using a randomized, blinded experimental design with negative (placebo) and positive (70 mM lidocaine) controls. The guinea pig intradermal wheal assay (n = 29) was used to test for peripheral inhibition of the cutaneous trunci muscle reflex, the mouse tail-flick test (n = 30) was used to test for sensory blockade, and the mouse sciatic nerve blockade model (n = 45) was used to test for motor blockade. Results: In all three animal models, QX-314 concentration-dependently and reversibly produced local anesthesia of long duration, at concentrations equivalent to those clinically relevant for lidocaine. In the guinea pig intradermal wheal assay, QX-314 produced peripheral nociceptive blockade up to 6 times longer than lidocaine (650 +/- 171 vs. 100 +/- 24 min [mean +/- SD]; n = 6 per group; P < 0.0001). In the mouse tail-flick test, QX-314 produced sensory blockade up to 10 times longer than lidocaine (540 +/- 134 vs. 50 +/- 11 min; n = 6 per group; P < 0.0001). Finally, in the mouse sciatic nerve model, QX-314 produced motor blockade up to 12 times longer compared with lidocaine (282 +/- 113 vs. 23 +/- 10 min; n = 9 or 10 per group; P < 0.0001). The onset of QX-314-mediated blockade was consistently slower compared with lidocaine. Animals injected with saline exhibited no local anesthetic effects in any of the three models. Conclusion: In a randomized, controlled laboratory study, the quaternary lidocaine derivative, QX-314, concentration-dependently and reversibly produced long-lasting local anesthesia with a slow onset in animal models in vivo. The authors' results raise the possibility that quaternary ammonium compounds may produce clinically useful local anesthesia of long duration in humans and challenge the conventional notion that these agents are ineffective when applied extracellularly.

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  1. Herr F, Na ´dor K, Pataky G, Borsi J: Untersuchungen u ¨ber die lokalana ¨s- thetische Wirkung von quaterna ¨ren Ammoniumbasen. Arch Exper Path Pharma- kol 1953; 217:447-55
  2. Hille B: Ion Channels of Excitable Membranes, 3rd edition. Sunderland, Sinauer Associates, 2001, p 518
  3. de Jong RH: Local Anesthetics. St. Louis, Mosby, 1994, pp 306 -8

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Authors
Lim, T. K. Y., MacLeod, B. A., Ries, C. R., & Schwarz, S. K. W.
Affiliations
  • Pharmacology Student.
  • Associate Professor and Jean Templeton Hugill Chair in Anesthesia.
  • University of British Columbia (CA)
ORCID
Venue
Anesthesiology
Publisher
Ovid Technologies (Wolters Kluwer Health)
Published
2007-08-01
Volume
107
Issue
2
Pages
305-311
ISSN
0003-3022 (ISSN-L)
DOI
10.1097/01.anes.0000270758.77314.b4
OpenAlex
W2058672163
Cited by
87
References
34
Citations by year
2026: 1 · 2025: 3 · 2024: 3 · 2023: 6 · 2022: 5 · 2021: 5 · 2020: 6 · 2019: 5 · 2018: 3 · 2017: 5 · 2016: 5 · 2015: 4 · 2014: 4 · 2013: 6 · 2012: 3
FWCI
5.65
Type
journal article
Language
en
Open access
Locations
  • Anesthesiology (publishedVersion)
  • PubMed (publishedVersion)
Funders
University of British Columbia
Topics
  • Health Sciences › Medicine › Surgery › Anesthesia and Pain Management
  • Health Sciences › Dentistry › Oral Surgery › Dental Anxiety and Anesthesia Techniques
  • Health Sciences › Veterinary › Small Animals › Veterinary Pharmacology and Anesthesia
Keywords
QX-314, local anesthesia, lidocaine, sensory block, motor block, tail-flick test, sciatic nerve block, anesthesia duration, local anesthetic pharmacology
MeSH terms
Action Potentials, Quaternary Ammonium Compounds, Anesthesia, Local, Anesthetics, Local, Animals, Disease Models, Animal, Dose-Response Relationship, Drug, Guinea Pigs, Intradermal Tests, Lidocaine, Nerve Block, Pain, Pain Measurement, Random Allocation, Sciatic Nerve, Sodium Chloride, Time Factors, Survival Analysis, Sciatic Neuropathy, Mice

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