Anesthesiology, V 120 • No 4 976 April 2014
E
FFECTIVE management of acute postoperative pain
is important for promoting recovery of patients after
surgery and for improving postoperative outcomes. Regional
anesthesia, especially peripheral nerve blockade, is enjoying
wider popularity, thanks in large part to the use of ultra-
sound guidance. Some studies suggest that major morbid-
ity, including persistent pain after surgery, as well as patient
mortality, is reduced by the use of regional anesthesia peri-
operatively. Key problems in regional anesthesia include the
relatively brief duration of action of clinically available local
anesthetics, necessitating cumbersome and expensive cath-
eter infusions, and nonselective blockade, leading to numb-
ness, motor weakness, and hypotension. As a result, sustained
release preparations and other approaches are under develop-
ment to produce prolonged nociceptor-selective nerve block.
A recent strategy is to open membrane channels selectively
expressed on nociceptors to allow entry of local anesthet-
ics.
1–4
Te transient receptor potential vanilloid 1 (TRPV1)
channel, important in the transduction of nociceptive or
painful stimuli,
5
is such a large pore channel and is expressed
not only on terminals of C and Aδ sensory fbers but also
on their axons, the site of perineural injection. Initial stud-
ies by Binshtok et al.
1
used perisciatic administration of the
What We Already Know about This Topic
• The transient receptor potential vanilloid 1 channel on noci-
ceptive neurons provides a route of intracellular entry for local
anesthetics
• The combination of capsaicin, which opens the transient re-
ceptor potential vanilloid 1 channel, and local anesthetics re-
sults in prolonged nociceptor-selective nerve blockade in rats
What This Article Tells Us That Is New
• After incisional hind paw surgery in rats, administration of li-
docaine and QX-314 followed by capsaicin initially attenuated
mechanical hypersensitivity, but led to a delayed onset of me-
chanical hypersensitivity and neurotoxicity
Copyright © 2013, the American Society of Anesthesiologists, Inc. Lippincott Williams & Wilkins. Anesthesiology 2014; 120:976-86
ABSTRACT
Background: Long-lasting, sensory-specifc peripheral nerve blockade would advance perioperative analgesia. Perineural
injection of a combination of transient receptor potential vanilloid 1 channel agonists and lidocaine or its hydrophilic deriva-
tive, QX-314, produces prolonged sensory or nociceptor-selective nerve block in rodents. In this study, the authors tested the
efcacy of these combinations in peripheral nerve block after incisional surgery in rats.
Methods: Te authors administered perisciatic lidocaine (2%), QX-314 (0.2%) followed by dilute capsaicin (0.05%, 10 min
later), or vehicle in rats and the duration of motor and sensory block to thermal and mechanical stimuli assessed in normal
animals and those after incisional surgery to the hind paw. Other animals receiving these injections were evaluated 7 weeks
later by behavior and histology for potential neurotoxicity.
Results: Perineural injection of the combination not only attenuated mechanical hypersensitivity for 72 h after incision but
also resulted in delayed onset mechanical hypersensitivity several weeks later, accompanied by degeneration of central termi-
nals of isolectin B4 (nonpeptidergic) and calcitonin gene–related peptide–containing (peptidergic) aferents in the ipsilateral
spinal cord. Dorsal root ganglia ipsilateral to injection of the combination showed increased expression of activating transcrip-
tion factor-3 and satellite cell activation.
Conclusions: Combined administration of local anesthetics with the transient receptor potential vanilloid 1 agonist capsaicin
induced a near complete blockade of incision-induced hypersensitivity for several days. However, the same combination induced
delayed mechanical hypersensitivity and neurotoxicity in naïve rats. Combination of these drugs in these concentrations is likely
to result in neurotoxicity, and the safety of other concentrations warrants further study. (ANESTHESIOLOGY 2014; 120:976-86)
Portions of this research were previously presented at Neuroscience 2011 on November 15, 2011, in Washington, D.C. Steven L. Shafer, M.D.,
served as Handling Editor for this article.
Submitted for publication May 6, 2013. Accepted for publication October 23, 2013. From the Department of Anesthesiology, Wake Forest
University School of Medicine, Winston-Salem, North Carolina (C.M.P., T.T.H., and C.A.A.); Department of Anesthesiology-Pediatric Anesthe-
sia, Wake Forest University School of Medicine, Winston-Salem, North Carolina (D.R.); and Department of Anesthesiology and Physiology
and Pharmacology, Wake Forest University School of Medicine, Winston-Salem, North Carolina (J.C.E.).
Nociceptor-selective Peripheral Nerve Block Induces
Delayed Mechanical Hypersensitivity and Neurotoxicity
in Rats
Christopher M. Peters, Ph.D., Douglas Ririe, M.D., Ph.D., Timothy T. Houle, Ph.D.,
Carol A. Aschenbrenner, M.A., James C. Eisenach, M.D.
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