Antinociceptive synergism upon the joint use of methadone and Phα1β in a model of cancer-related pain in C57BL/6J mice

Life Sci. 2021 Aug 1:278:119582. doi: 10.1016/j.lfs.2021.119582. Epub 2021 May 4.

Abstract

Opioids are the first-line treatment for cancer pain. Incomplete pain relief and the high rate of adverse effects of these compounds bring a need to combine them with other drugs acting on different targets.

Aims: We here evaluate the antinociceptive interaction and adverse events of methadone combined with recombinant Phα1β, an analgesic toxin from Phoneutria nigriventer.

Main methods: Melanoma was produced by intraplantar inoculation of B16-F10 cells into the right paw. von Frey filaments measured the paw-withdrawal threshold after administration of methadone, Phα1β, and their combination. The degree of interaction was evaluated using isobolographic analysis. Spontaneous performance and forced motor performance were assessed with the open-field and rotarod tests, respectively. Intestinal function was evaluated by the distance traveled by charcoal and opioid tolerance was induced by daily morphine injections.

Key findings: Co-administration of Phα1β with methadone synergistically reverses the melanoma-induced mechanical hypersensitivity. No motor alterations were observed but mild alterations on intestinal function after treatment with the combination that was also capable of restoring morphine analgesia in the tail-flick test after an opioid-induced tolerance.

Significance: Combinatorial treatment with Phα1β and methadone produces synergistic analgesic potentiation with potential implications to pain treatment even under opioid tolerance conditions.

Keywords: Cancer pain; Isobolographic analysis; Melanoma; Methadone; Phα1β; Synergism.

MeSH terms

  • Analgesics / pharmacology*
  • Analgesics, Opioid / pharmacology
  • Animals
  • Behavior, Animal
  • Calcium Channel Blockers / pharmacology
  • Cancer Pain / drug therapy*
  • Drug Synergism
  • Drug Therapy, Combination
  • Drug Tolerance
  • Gastrointestinal Tract / drug effects
  • Male
  • Melanoma, Experimental / metabolism
  • Methadone / administration & dosage*
  • Mice
  • Mice, Inbred C57BL
  • Neoplasm Transplantation
  • Neoplasms / complications
  • Pain Management / methods*
  • Spider Venoms / administration & dosage*
  • Time Factors

Substances

  • Analgesics
  • Analgesics, Opioid
  • Calcium Channel Blockers
  • Phalpha1beta toxin, Phoneutria nigriventer
  • Spider Venoms
  • Methadone