Classics in Chemical Neuroscience: Dextromethorphan (DXM)

ACS Chem Neurosci. 2023 Jun 21;14(12):2256-2270. doi: 10.1021/acschemneuro.3c00088. Epub 2023 Jun 8.

Abstract

Dextromethorphan (DXM) was introduced in 1958 as the first non-opioid cough suppressant and is indicated for multiple psychiatric disorders. It has been the most used over-the-counter cough suppressant since its emergence. However, individuals quickly noticed an intoxicating and psychedelic effect if they ingested large doses. DXM's antagonism at N-methyl-d-aspartate receptors (NMDAr) is thought to underly its efficacy in treating acute cough, but supratherapeutic doses mimic the activity of dissociative hallucinogens, such as phencyclidine and ketamine. In this Review we will discuss DXM's synthesis, manufacturing information, drug metabolism, pharmacology, adverse effects, recreational use, abuse potential, and its history and importance in therapy to present DXM as a true classic in chemical neuroscience.

Keywords: Dextromethorphan; NMDA receptor antagonist; cough; dextrorphan; dissociative hallucinogen; pseudobulbar affect.

Publication types

  • Review

MeSH terms

  • Antitussive Agents* / pharmacology
  • Antitussive Agents* / therapeutic use
  • Dextromethorphan / pharmacology
  • Dextromethorphan / therapeutic use
  • Hallucinogens* / pharmacology
  • Hallucinogens* / therapeutic use
  • Humans
  • Ketamine* / pharmacology
  • Ketamine* / therapeutic use
  • Phencyclidine
  • Receptors, N-Methyl-D-Aspartate

Substances

  • Antitussive Agents
  • Dextromethorphan
  • Hallucinogens
  • Phencyclidine
  • Ketamine
  • Receptors, N-Methyl-D-Aspartate