Transient Receptor Potential Vanilloid 1 Antagonists Prevent Anesthesia-induced Hypothermia and Decrease Postincisional Opioid Dose Requirements in Rodents

Anesthesiology. 2017 Nov;127(5):813-823. doi: 10.1097/ALN.0000000000001812.

Abstract

Background: Intraoperative hypothermia and postoperative pain control are two important clinical challenges in anesthesiology. Transient receptor potential vanilloid 1 has been implicated both in thermoregulation and pain. Transient receptor potential vanilloid 1 antagonists were not advanced as analgesics in humans in part due to a side effect of hyperthermia. This study tested the hypothesis that a single, preincision injection of a transient receptor potential vanilloid 1 antagonist could prevent anesthesia-induced hypothermia and decrease the opioid requirement for postsurgical hypersensitivity.

Methods: General anesthesia was induced in rats and mice with either isoflurane or ketamine, and animals were treated with transient receptor potential vanilloid 1 antagonists (AMG 517 or ABT-102). The core body temperature and oxygen consumption were monitored during anesthesia and the postanesthesia period. The effect of preincision AMG 517 on morphine-induced reversal of postincision hyperalgesia was evaluated in rats.

Results: AMG 517 and ABT-102 dose-dependently prevented general anesthesia-induced hypothermia (mean ± SD; from 1.5° ± 0.1°C to 0.1° ± 0.1°C decrease; P < 0.001) without causing hyperthermia in the postanesthesia phase. Isoflurane-induced hypothermia was prevented by AMG 517 in wild-type but not in transient receptor potential vanilloid 1 knockout mice (n = 7 to 11 per group). The prevention of anesthesia-induced hypothermia by AMG 517 involved activation of brown fat thermogenesis with a possible contribution from changes in vasomotor tone. A single preincision dose of AMG 517 decreased the morphine dose requirement for the reduction of postincision thermal (12.6 ± 3.0 vs. 15.6 ± 1.0 s) and mechanical (6.8 ± 3.0 vs. 9.5 ± 3.0 g) withdrawal latencies.

Conclusions: These studies demonstrate that transient receptor potential vanilloid 1 antagonists prevent anesthesia-induced hypothermia and decrease opioid dose requirements for the reduction of postincisional hypersensitivity in rodents.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Analgesics, Opioid / pharmacology
  • Analgesics, Opioid / therapeutic use*
  • Anesthesia / adverse effects*
  • Animals
  • Benzothiazoles / pharmacology
  • Benzothiazoles / therapeutic use
  • Dose-Response Relationship, Drug
  • Female
  • Hypothermia / chemically induced*
  • Hypothermia / pathology
  • Hypothermia / prevention & control*
  • Indazoles / pharmacology
  • Indazoles / therapeutic use
  • Male
  • Mice
  • Mice, Knockout
  • Pain Measurement / drug effects
  • Pain Measurement / methods
  • Pain, Postoperative / drug therapy*
  • Pain, Postoperative / pathology
  • Pyrimidines / pharmacology
  • Pyrimidines / therapeutic use
  • Rats
  • Rats, Sprague-Dawley
  • TRPV Cation Channels / antagonists & inhibitors*
  • Urea / analogs & derivatives
  • Urea / pharmacology
  • Urea / therapeutic use

Substances

  • ABT 102
  • Analgesics, Opioid
  • Benzothiazoles
  • Indazoles
  • N-(4-(6-(4-trifluoromethylphenyl)pyrimidin-4-yloxy)benzothiazol-2-yl)acetamide
  • Pyrimidines
  • TRPV Cation Channels
  • Trpv1 protein, rat
  • Urea