Tapentadol: A Review of Experimental Pharmacology Studies, Clinical Trials, and Recent Findings

Abstract

Tapentadol is an analgesic compound that acts centrally to attenuate pain. Previous studies have shown that tapentadol has dual mechanisms of action as a mu-opioid receptor agonist and noradrenaline re-uptake inhibition. Therefore, tapentadol provides a great advantage over classic opioids in pain management from nociceptive to neuropathic. Cumulative evidence from in vitro data suggests that tapentadol effect of norepinephrine re-uptake could be a new target that overcomes other classic opioids in chronic neuropathic pain. Compared to tramadol and other opioids, tapentadol is associated with fewer adverse effects than tramadol. Tapentadol is a new alternative to treat acute, chronic, and neuropathic pain. Thus, this review article was focused on understanding the studies that led to the development of tapentadol as a novel analgesic drug and its advantages over conventional opioids. Thus, tapentadol is a good alternative with fewer adverse effects and is available for human use.

Keywords: chronic pain; clinical trials; neuropathic pain; opioids.

Figure 1

Suggested tapentadol analgesic mechanism of action. A dual-function on the mu-opioids receptor (MOR) and norepinephrine reuptake transporter (NET). Alpha 2- adrenoreceptor (A2-AR), substance P receptor (SPR), and Glutamate receptor (GLR).