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Do not crush, break, or open an extended-release tablet. Swallow it whole to avoid exposure to a potentially fatal dose. Tapentadol may be habit-forming, even at regular doses. Take this medicine exactly as prescribed by your doctor. Never share the medicine with another person. MISUSE OF NARCOTIC PAIN MEDICATION CAN CAUSE ADDICTION, OVERDOSE, OR DEATH, especially in a child or other person using the medicine without a prescription.
Tapentadol is an agonist of the μ-opioid receptor and a norepinephrine reuptake inhibitor (NRI).[1] Analgesia occurs within 32 minutes after oral administration, and lasts for 4–6 hours.[3] It is 18 times less potent than morphine in terms of binding to human mu-opioid receptors in in vitro research on human tissue.[16] In vivo, only 32% of an oral dose of tapentadol will survive first pass metabolism and proceed to the bloodstream to produce its effects on the central and peripheral nervous systems of the patient.[1]
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