Linking pharmacology to clinical reports: cyclobenzaprine and its possible association with serotonin syndrome

Clin Pharmacol Ther. 2011 Nov;90(5):662-5. doi: 10.1038/clpt.2011.177. Epub 2011 Oct 5.

Abstract

The link between cyclobenzaprine (Flexeril) administration and serotonin syndrome (SS) is subject to debate. Establishing such a connection is difficult because of the limited number of case reports available and the almost complete ignorance of its preclinical pharmacology. In this context, evidence is provided here that cyclobenzaprine blocks the serotonin and norepinephrine transporters and binds to another set of five serotonin receptors. SS should be considered when indicative signs occur in the context of cyclobenzaprine use.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amitriptyline / adverse effects
  • Amitriptyline / analogs & derivatives*
  • Amitriptyline / metabolism
  • Amitriptyline / pharmacology
  • Antidepressive Agents, Tricyclic / adverse effects*
  • Antidepressive Agents, Tricyclic / metabolism
  • Antidepressive Agents, Tricyclic / pharmacology
  • Humans
  • Norepinephrine Plasma Membrane Transport Proteins / antagonists & inhibitors
  • Protein Binding
  • Receptors, Serotonin / metabolism
  • Serotonin Plasma Membrane Transport Proteins / drug effects
  • Serotonin Plasma Membrane Transport Proteins / metabolism
  • Serotonin Syndrome / chemically induced*

Substances

  • Antidepressive Agents, Tricyclic
  • Norepinephrine Plasma Membrane Transport Proteins
  • Receptors, Serotonin
  • Serotonin Plasma Membrane Transport Proteins
  • Amitriptyline
  • cyclobenzaprine