Synergistic interaction between trazodone and gabapentin in rodent models of neuropathic pain

PLoS One. 2021 Jan 4;16(1):e0244649. doi: 10.1371/journal.pone.0244649. eCollection 2021.

Abstract

Neuropathic pain is a chronic debilitating condition caused by injury or disease of the nerves of the somatosensory system. Although several therapeutic approaches are recommended, none has emerged as an optimal treatment leaving a need for developing more effective therapies. Given the small number of approved drugs and their limited clinical efficacy, combining drugs with different mechanisms of action is frequently used to yield greater efficacy. We demonstrate that the combination of trazodone, a multifunctional drug for the treatment of major depressive disorders, and gabapentin, a GABA analogue approved for neuropathic pain relief, results in a synergistic antinociceptive effect in the mice writhing test. To explore the potential relevance of this finding in chronic neuropathic pain, pharmacodynamic interactions between low doses of trazodone (0.3 mg/kg) and gabapentin (3 mg/kg) were evaluated in the chronic constriction injury (CCI) rat model, measuring the effects of the two drugs both on evoked and spontaneous nociception and on general well being components. Two innate behaviors, burrowing and nest building, were used to assess these aspects. Besides exerting a significant antinociceptive effect on hyperalgesia and on spontaneous pain, combined inactive doses of trazodone and gabapentin restored in CCI rats innate behaviors that are strongly reduced or even abolished during persistent nociception, suggesting that the combination may have an impact also on pain components different from somatosensory perception. Our results support the development of a trazodone and gabapentin low doses combination product for optimal multimodal analgesia treatment.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Analgesics / pharmacology
  • Analgesics / therapeutic use*
  • Animals
  • Anti-Anxiety Agents / pharmacology
  • Anti-Anxiety Agents / therapeutic use*
  • Depressive Disorder, Major / drug therapy
  • Disease Models, Animal
  • Drug Synergism
  • Gabapentin / pharmacology
  • Gabapentin / therapeutic use*
  • Male
  • Mice
  • Neuralgia / drug therapy*
  • Nociception / drug effects
  • Trazodone / pharmacology
  • Trazodone / therapeutic use*

Substances

  • Analgesics
  • Anti-Anxiety Agents
  • Gabapentin
  • Trazodone

Grants and funding

This work was funded by Angelini S.p.A. Angelini S.p.A. provided support in the form of salaries for BG, AdM, AA, LP, LD, CM, FPDG and ST. The specific roles of these authors are articulated in the “author contributions” section. The funder had a role in the study design, data collection and analysis, decision to publish and preparation of the manuscript through the provision of expert decision-making input from the preclinical and management teams.