What is the main mechanism of tramadol?

Abstract

Tramadol is an analgesic that is used worldwide for pain, but its mechanisms of action have not been fully elucidated. The majority of studies to date have focused on activation of the μ-opioid receptor (μOR) and inhibition of monoamine reuptake as mechanisms of tramadol. Although it has been speculated that tramadol acts primarily through activation of the μOR, no evidence has revealed whether tramadol directly activates the μOR. During the past decade, major advances have been made in our understanding of the physiology and pharmacology of ion channels and G protein-coupled receptor (GPCR) signaling. Several studies have shown that GPCRs and ion channels are targets for tramadol. In particular, tramadol has been shown to affect GPCRs. Here, the effects of tramadol on GPCRs, monoamine transporters, and ion channels are presented with a discussion of recent research on the mechanisms of tramadol.

• Authors: Kouichiro Minami, Junichi Ogata, Yasuhito Uezono
• Journal: Naunyn-Schmiedeberg's archives of pharmacology (Naunyn Schmiedebergs Arch Pharmacol) Vol. 388 Issue 10 Pg. 999-1007 (Oct 2015) ISSN: 1432-1912 [Electronic] Germany
• PMID: 26292636 (Publication Type: Journal Article, Review)

Chemical References

• Analgesics, Opioid
• Ion Channels
• Receptors, G-Protein-Coupled
• Receptors, Opioid, mu
• Vesicular Monoamine Transport Proteins
• Tramadol

Topics

• Analgesics, Opioid (pharmacology)
• Animals
• Humans
• Ion Channels (metabolism)
• Pain (drug therapy)
• Receptors, G-Protein-Coupled (metabolism)
• Receptors, Opioid, mu (agonists)
• Tramadol (pharmacology)
• Vesicular Monoamine Transport Proteins (metabolism)