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.

Atualização no manejo da dor musculoesquelética

“…5 Opioid classification per potency and mechanism of action. [35][36][37][38][39][40][41]49 Rev Bras Ortop Vol. 59 No.…”

“…Tem apresentações de liberação programada para uso de 12 em 12 horas, nas doses de 50 até 250 mg. A dose máxima em estudos é de 500 mg/dia. 39…”

Diabetic Neuropathic Pain: Directions for Exploring Treatments

“…Specifically, Tapentadol, a μ-opioid receptor agonist, could bind to the μ-opioid receptors in spinal cords to reduce the perception of pain. In addition, it also acts a noradrenaline re-uptake inhibitor [ 19 ]. Therefore, noradrenaline concentration in the synaptic cleft could be increased, further activating its descending inhibitory pain pathways.…”

Novel Opioids in the Setting of Acute Postoperative Pain: A Narrative Review

“…Tapentadol (brand name Nucynta) is a centrally acting opioid analgesic that demonstrates both MOR agonist activity as well as norepinephrine (NE) reuptake inhibition [ 52 , 53 , 54 ]. Its chemical structure is shown in Figure 2 .…”

“…Tapentadol was first approved by the FDA in 2008 as an immediate-release (IR) oral tablet to treat opioid-requiring moderate to severe pain when alternatives are inadequate. Its extended-release (ER) formulation was later approved in 2011, with its use expanded for the management of neuropathic pain associated with diabetic peripheral neuropathy [ 52 , 53 , 54 ]. The FDA recommends starting tapentadol at a low dosage to match the treatment goals of individual patients before titrating to higher doses.…”