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

• Published in: Clinical pharmacology and therapeutics Vol. 90; no. 5; p. 662
• Main Authors: Mestres, J, Seifert, S A, Oprea, T I
• Format: Journal Article
• Language: English
• Published: United States 01.11.2011
• Subjects: 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
• ISSN: 1532-6535
• DOI: 10.1038/clpt.2011.177

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.