Tapentadol (trade names: Nucynta, Palexia, In India available as TAPAL by MSN Labs) is a centrally acting analgesic with a dual mode of action as an agonist of the μ-opioid receptor and as a norepinephrine reuptake inhibitor. It is also an agonist of the σ2 receptor, though the function of this orphan receptor remains controversial.
Similar to levorphanol—another opioid with serotonin–norepinephrine reuptake inhibitor (SNRI) effects—in its dual mechanism of action, tapentadol provides analgesia comparable to other opioid analgesics such as hydrocodone, oxycodone, and pethidine (meperidine) but with a more tolerable side effect profile. While its analgesic actions have been compared to tramadol and oxycodone, its general potency is somewhere between tramadol and morphine in effectiveness.
Tapentadol is approved by the United States Food and Drug Administration for the treatment of moderate to severe acute pain. Due to the dual mechanism of action as an opioid agonist and norepinephrine reuptake inhibitor, there is also potential for off-label use in chronic pain. Physicians use SNRIs in chronic pain management to increase the effectiveness of opioids and other analgesics such as NSAIDs against neuropathic pain and from certain specific contributing causes such as fibromyalgia and diabetic neuropathy. One SNRI often used as an adjunct, atypical & potentiator is duloxetine (Cymbalta).
Read more about Tapentadol: History, Clinical Trials, Indications, Availability and Dosage, Cost, Mechanism of Action, Adverse Effects, Contraindications, Abuse Potential, Overdose, See Also