• David R P Guay.
• Department of Experimental and Clinical Pharmacology, College of Pharmacy, University of Minnesota, Minneapolis, MN 55455, USA. guayx001@umn.edu
• Consult Pharm. 2009 Nov 1;24(11):833-40.

ObjectiveTo review the pharmacodynamics, pharmacokinetics, clinical efficacy, tolerability, dosing, and administration of tapentadol, a combination mu-opioid-receptor agonist and monoamine-reuptake inhibitor, and compare it with tramadol, the first drug in this class.Data SourcesMEDLINE/PUBMED and EMBASE searches (1986 through March 2009) were conducted to identify pertinent English-language papers. In addition, meeting abstracts from multiple pain specialty organizations were searched (2000 through 2008).Study Selection And Data ExtractionAll papers/abstracts evaluating any aspect of tapentadol.Data SynthesisOral tapentadol hydrochloride (HCl) is the second combination mu-opioid-receptor agonist and monoamine-reuptake inhibitor to be approved by the Food and Drug Administration (approved for treatment of moderate-to-severe acute pain in adults). It was active in a wide variety of pain states in animals and humans. It behaved in a similar fashion to morphine and hydromorphone in animal and human models of physical/psychological dependence. Oral tapentadol HCI is administered in doses of 50 to 100 mg every four to six hours (dose and dosing interval being selected on the basis of pain intensity). No specific recommendations have been made for elders.ConclusionTapentadol overcomes some of the liabilities of tramadol. However, it still has some liabilities: its potential to contribute to/precipitate serotonin syndrome and anticholinergic/5-HT3 antagonist effects and to induce physical/psychological dependence (similar to schedule II opioids). There is also a dearth of information in terms of efficacy/tolerability in chronic pain states, clinical data in frail elders, and details of drug-drug interaction potential vis-à-vis glucuronidation and quantitation of the risk of serotonin syndrome.

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