Dextromethorphan shows efficacy in experimental pain (nociception) and opioid tolerance

K J Elliott1, M Brodsky, A Hyanansky

  • 1Department of Neurology, Memorial Sloan-Kettering Cancer Center, New York, NY 10021, USA.

Neurology
|December 1, 1995
PubMed

Insights

Dextromethorphan, an N-methyl-D-aspartate receptor antagonist, shows promise for pain relief. It has demonstrated analgesic effects and can prevent tolerance to other pain medications, suggesting its potential for treating zoster-associated neuralgia.

Area of Science:

  • Neuroscience
  • Pharmacology
  • Pain Research

Background:

  • Dextromethorphan is an oral antitussive and a clinically available N-methyl-D-aspartate (NMDA) receptor antagonist.
  • NMDA receptors play a role in pain signaling and the development of analgesic tolerance.

Purpose of the Study:

  • To evaluate the potential analgesic efficacy of dextromethorphan in zoster-associated neuralgia.
  • To explore dextromethorphan's effects on pain pathways and opiate tolerance.

Main Methods:

  • Review of existing experimental data on dextromethorphan's pharmacological actions.
  • Analysis of dextromethorphan's effects in the formalin test for pain.
  • Examination of dextromethorphan's impact on c-fos proto-oncogene expression.
  • Assessment of dextromethorphan's role in opiate analgesic tolerance models.

Main Results:

  • Dextromethorphan exhibits analgesic efficacy in experimental pain models.
  • It blocks nociceptive activation of the c-fos proto-oncogene.
  • Dextromethorphan prevents and reverses opiate analgesic tolerance in experimental settings.

Conclusions:

  • Experimental data suggest dextromethorphan possesses analgesic properties relevant to neuropathic pain.
  • Further investigation in controlled clinical trials is warranted to confirm its efficacy for zoster-associated neuralgia.

Related Concept Videos

Opioid Analgesics: Synthetic and Semisynthetic Opioids01:15

Opioid Analgesics: Synthetic and Semisynthetic Opioids

Synthetic and semisynthetic opioids are pivotal in pain management and tackling opioid addiction. Semisynthetic opioids, including morphinans (morphine derivatives), oxycodone, oxymorphone, hydrocodone, and hydromorphone, have improved pharmacokinetic profiles compared to morphine. Additionally, heroin and 6-MAM (6-Monoacetylmorphine) show better CNS penetration than morphine due to heightened lipid solubility. Hydromorphone, a potent opioid, undergoes hepatic metabolism to form the active...
Analgesia and Pain Management01:25

Analgesia and Pain Management

Pain is critical to various clinical pathologies, provoking an urgent need for effective management. Pain, whether acute or chronic, is a complex neurochemical process. Its alleviation depends on the type, with nonopioid analgesics effective for mild to moderate pain, such as musculoskeletal or inflammatory pain, while neuropathic pain responds best to anticonvulsants, tricyclic antidepressants, or serotonin/norepinephrine reuptake inhibitors. For severe acute or chronic pain, opioids may be...
Opioid Receptors: Overview01:22

Opioid Receptors: Overview

Opioid receptors, including the mu (μ, MOR), delta (δ, DOR), and kappa (κ, KOR) types, belong to the rhodopsin family of G protein-coupled receptors. These receptors are located throughout the central and peripheral nervous systems and in non-neuronal tissues such as macrophages and astrocytes. Opioid receptor ligands can be categorized into agonists or antagonists. Highly selective agonists include [d-Ala2, MePhe4, Gly(ol)5]-enkephalin or DAMGO for MOR, [D-Pen2, D-Pen5]-enkephalin or DPDPE for...
Opioid Analgesics: Morphine and Other Natural Cogeners01:20

Opioid Analgesics: Morphine and Other Natural Cogeners

Opioids are a class of drugs that mimic endogenous opioid peptides and act on opioid receptors, and help in pain relief. These compounds are classified as natural, synthetic, or semi-synthetic. Natural opioids, like morphine, codeine, and thebaine, are derived from the opium poppy plant (Papaver somniferum or Papaver album) and are termed opiates. Synthetic opioids are artificial, while semi-synthetic opioids combine natural and synthetic compounds. Morphine, a prototypical opioid, possesses a...
Chemotherapy-Induced Nausea and Vomiting: Cannabinoids01:21

Chemotherapy-Induced Nausea and Vomiting: Cannabinoids

Tetrahydrocannabinol (THC) is a phytocannabinoid that primarily interacts with the CB1 receptor, a type of G protein-coupled receptor (GPCR) predominantly in and around the chemoreceptor trigger zone (CTZ) and emetic center. THC also blocks the serotonin receptor activity in the dorsal vagal complex (DVC) by inhibiting serotonin release. THC exerts its anti-emetic effects through these interactions, which are beneficial for patients undergoing chemotherapy.
Two synthetic agonists of THC,...
Upper Respiratory Drugs: Antitussives, Expectorants, and Mucolytics01:23

Upper Respiratory Drugs: Antitussives, Expectorants, and Mucolytics

Respiratory symptoms, such as congestion and cough, commonly accompany respiratory tract conditions. Various medications, such as antitussives, expectorants, and mucolytics, play crucial roles in providing relief.
Antitussives include codeine, dextromethorphan (Robitussin), and benzonatate (Tessalon). Codeine and dextromethorphan exert their effects centrally by suppressing the cough reflex center in the medulla.  Benzonatate operates peripherally within the respiratory tract by anesthetizing...