Critical and persistent pain is a critical problem with repercussions in our nation, occurring in harm to the quality of life of sufferers as well as socioeconomic fatalities, due to work absenteeism. This article aspires to examine the use of tapentadol, an anesthetic with a double mechanism of action, in the handling of acute and continuous pain disorders.

Drug Description

Tapentadol dosage is worthwhile in the treatment of acute and chronic affliction, with power equal to the opioids presently used. In advancement, it formulated less sufferance, limited adverse impacts, and a nicely remedial comeback in chronic neuropathic trouble when correlated to pure μ-opioid receptor agonists.

Pain - A major Problem

Pain is a circumstance of immense probability, about 20 to 25% of the population with an increasing incidence. Despite the enormous advancements in anatomy, physiology, diagnosis, and pain supervision, more than 50% of patients report inadequate assistance.

This can be connected to the neuroplasticity procedure of the discomfort pathways, ascertaining a persistent “memory” of the antagonistic event and neuronal hyperexcitability. Understanding chronic pain Neurobiology is necessary to target the medication.

Accordingly, the use of pharmaceuticals that behave on more than one pathophysiologic mechanism, such as tapentadol, can be a fresh pike in the therapeutic armamentarium against sharp discomfort and particularly chronic ones.


How is tapentadol beneficial?

Tapentadol is an exclusive non-racemic molecule with an identical major mode of action, accessible in the United States of America (USA) and Europe for the medication of acute and lasting pain.

It has been handy in the U.S. since 2008 for the process of reasonable acute to severe discomfort, in its sudden release (IR) formulation, and since 2011 for the handling of moderate chronic to intense pain in its extended-release (ER) formulation, after approval by the Food and Drug Administration (FDA).

In the European market, the IR and ER formulations of the pharmaceutical were authorized by the European Medicines Agency (EMA) in 20107.

Pharmacological Properties of Tapentadol

● Tapentadol behaves as both a MOR agonist and a noradrenaline reuptake inhibitor (NRI).

● Continuous with its twofold mechanism, tapentadol displayed anesthetic influences in several preclinical categories of pain and was similarly effective in curing numerous aspects of chronic suffering in clinical assessments.

● Tapentadol’s major metabolite (tapentadol-O-glucuronide) is not useful at opioid receptors, synaptosomal reuptake procedures, or other compelling sites.

Tapentadol extended release: clinical concerns in chronic pain

● Functions via μ-opioid receptor agonism and noradrenaline reuptake inhibition
● Decreases favorable to urgent chronic suffering of fluctuating aetiologies, including neuropathic discomfort
● At least as effective as conventional influential opioids, but more acceptable GI tolerability
● Advantageous and typically well withstood over up to 2 years’ therapy, without an inkling of tolerance

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