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

Article Details

Citation

Mestres J, Seifert SA, Oprea TI

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.

PubMed ID
21975349 [ View in PubMed
]
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.

DrugBank Data that Cites this Article

Drugs
Drug Targets
DrugTargetKindOrganismPharmacological ActionActions
Cyclobenzaprine5-hydroxytryptamine receptor 2AProteinHumans
Yes
Antagonist
Details
Cyclobenzaprine5-hydroxytryptamine receptor 2BProteinHumans
Unknown
Antagonist
Details
Cyclobenzaprine5-hydroxytryptamine receptor 2CProteinHumans
Unknown
Antagonist
Details
Cyclobenzaprine5-hydroxytryptamine receptor 6ProteinHumans
Unknown
Antagonist
Details
Cyclobenzaprine5-hydroxytryptamine receptor 7ProteinHumans
Unknown
Antagonist
Details
CyclobenzaprineSodium-dependent noradrenaline transporterProteinHumans
Unknown
Inhibitor
Details
CyclobenzaprineSodium-dependent serotonin transporterProteinHumans
Unknown
Inhibitor
Details
CyclobenzaprineToll-like receptor 4ProteinHumans
Unknown
Inhibitor
Details
Drug Interactions
DrugsInteraction
Isocarboxazid
Cyclobenzaprine
Cyclobenzaprine may increase the serotonergic activities of Isocarboxazid.
Linezolid
Cyclobenzaprine
Cyclobenzaprine may increase the serotonergic activities of Linezolid.
Minaprine
Cyclobenzaprine
Cyclobenzaprine may increase the serotonergic activities of Minaprine.
Moclobemide
Cyclobenzaprine
Cyclobenzaprine may increase the serotonergic activities of Moclobemide.
Nialamide
Cyclobenzaprine
Cyclobenzaprine may increase the serotonergic activities of Nialamide.