Tapentadol: Can It Kill Two Birds with One Stone without Breaking Windows?

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Chang EJ, Choi EJ, Kim KH

Tapentadol: Can It Kill Two Birds with One Stone without Breaking Windows?

Korean J Pain. 2016 Jul;29(3):153-7. doi: 10.3344/kjp.2016.29.3.153. Epub 2016 Jul 1.

PubMed ID

27413479 [ View in PubMed

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Abstract

Tapentadol is a novel oral analgesic with a dual mode of action as an agonist of the micro-opioid receptor (MOR), and as a norepinephrine reuptake inhibitor (NRI) all in a single molecule. Immediate release (IR) tapentadol shows its analgesic effect quickly, at around 30 minutes. Its MOR agonistic action produces acute nociceptive pain relief; its role as an NRI brings about chronic neuropathic pain relief. Absorption is rapid, with a mean maximal serum concentration at 1.25-1.5 h after oral intake. It is present primarily in the form of conjugated metabolites after glucuronidation, and excretes rapidly and completely via the kidneys. The most common adverse reactions are nausea, dizziness, vomiting, and somnolence. Constipation is more common in use of the ER formulation. Precautions against concomitant use of central nervous system depressants, including sedatives, hypnotics, tranquilizers, general anesthetics, phenothiazines, other opioids, and alcohol, or use of tapentadol within 14 days of the cessation of monoamine oxidase inhibitors, are advised. The safety and efficacy have not been established for use during pregnancy, labor, and delivery, or for nursing mothers, pediatric patients less than 18 years of age, and cases of severe renal impairment and severe hepatic impairment. The major concerns for tapentadol are abuse, addiction, seeking behavior, withdrawal, and physical dependence. The presumed problem for use of tapentadol is to control the ratio of MOR agonist and NRI. In conclusion, tapentadol produces both nociceptive and neuropathic pain relief, but with worries about abuse and dependence.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Tapentadol	Delta-type opioid receptor	Protein	Humans	Unknown	Agonist	Details
Tapentadol	Kappa-type opioid receptor	Protein	Humans	Unknown	Agonist	Details
Tapentadol	Mu-type opioid receptor	Protein	Humans	Unknown	Agonist	Details
Tapentadol	Sodium-dependent noradrenaline transporter	Protein	Humans	Unknown	Inhibitor	Details