Korean J Pain. 2016 Jul;29(3):153-7. doi: 10.3344/kjp.2016.29.3.153. Epub 2016 Jul 01.
Tapentadol: Can It Kill Two Birds with One Stone without Breaking Windows?.
The Korean journal of pain
Eun Jung Chang, Eun Ji Choi, Kyung Hoon Kim
Affiliations
Affiliations
- Department of Anesthesia and Pain Medicine, School of Medicine, Pusan National University, Yangsan, Korea.
PMID: 27413479
PMCID: PMC4942642 DOI: 10.3344/kjp.2016.29.3.153
Abstract
Tapentadol is a novel oral analgesic with a dual mode of action as an agonist of the µ-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.
Keywords: Acute pain; Addictive behavior; Adverse drug reactions; Alpha adrenergic receptors; Chronic pain; Hyperalgesia; Mode of action; Mu opioid receptor; N-desmethyltapentadol; Neuropathic pain; Nociceptive pain; Tapentadol
References
- J Pain. 2013 Feb;14(2):158-64 - PubMed
- Exp Clin Psychopharmacol. 2011 Apr;19(2):123-30 - PubMed
- J Chem Biol. 2009 Aug;2(3):131-51 - PubMed
- Eur J Pain. 2010 Sep;14(8):781-3 - PubMed
- Pain Med. 2015 Jan;16(1):131-40 - PubMed
- Clin Ther. 2009 Dec;31(12):2804-18 - PubMed
- Expert Opin Pharmacother. 2013 Nov;14(16):2297-304 - PubMed
- Clin Pharmacokinet. 2015 Aug;54(8):825-36 - PubMed
- Addiction. 2013 Jun;108(6):1095-106 - PubMed
- Saudi J Anaesth. 2013 Jul;7(3):322-6 - PubMed
- Korean J Pain. 2013 Jul;26(3):265-9 - PubMed
- J Pain. 2013 Oct;14(10):1227-41 - PubMed
- Clin Pharmacokinet. 2010 Oct;49(10):671-82 - PubMed
- Neurosci Lett. 2012 Jan 24;507(2):151-5 - PubMed
- Clin J Pain. 2014 Aug;30(8):685-92 - PubMed
- Clin Drug Investig. 2010;30(8):489-505 - PubMed
- Korean J Pain. 2014 Apr;27(2):103-11 - PubMed
- Korean J Pain. 2016 Jan;29(1):40-7 - PubMed
- Pain Med. 2016 Aug;17(8):1490-6 - PubMed
- Anaesthesia. 2015 May;70(5):518-22 - PubMed
- J Opioid Manag. 2012 Nov-Dec;8(6):395-402 - PubMed
- Pain Med. 2015 Jan;16(1):119-30 - PubMed
- Eur J Drug Metab Pharmacokinet. 2007 Jul-Sep;32(3):163-9 - PubMed
Publication Types