Tapentadol: An initial analysis

Eric E. Prommer, MD

doi:10.5055/jom.2010.0020

Authors

Eric E. Prommer, MD

DOI:

https://doi.org/10.5055/jom.2010.0020

Keywords:

tapentadol, affinity, neuropathic

Abstract

Tapentadol hydrochloride (17(—)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol) is a newly released analgesic that works at two levels: by acting as a μ-opioid agonist and as a modulator of descending inhibitory pathways through its effects on neurotransmitters involved in these pathways. The theoretical advantage is the provision of synergistic analgesic activities, which may lessen the need for opioid escalation. The advantage is its potential as a possible new agent in neuropathic pain. Preclinical models confirm analgesic properties in acute pain and neuropathic pain models, but with less potency than morphine. Tapentadol has minimal CYP 450 interactions limiting potential for drug interactions. Human clinical trial data in nonmalignant pain suggest less potency than a step-3 opioid, and the drug remains to be tested in patients with cancer pain and neuropathic pain.

Author Biography

Eric E. Prommer, MD

Department of Hematology/Oncology/Palliative Care, Mayo Clinic, Phoenix, Arizona.

References

Tzschentke TM, Christoph T, Kogel B, et al.: (−)-(1R,2R)-3-(3-Dimethylamino-1-ethyl-2-methyl-propyl)-phenol hydrochloride (Tapentadol HCl): A novel mu-opioid receptor agonist/norepinephrine reuptake inhibitor with broad-spectrum analgesic properties. J Pharmacol Exp Ther. 2007; 323(1): 265-276.

Tapentadol (Nucynta)—A new analgesic. Med Lett Drugs Ther. 2009; 51(1318): 61-62.

Terlinden R, Ossig J, Fliegert F, et al.: Absorption, metabolism, and excretion of 14C-labeled tapentadol HCl in healthy male subjects. Eur J Drug Metab Pharmacokinet. 2007; 32(3): 163-169.

Prommer EE: Tramadol: Does it have a role in cancer pain management? J Opioid Manag. 2005; 1(3): 131.

Kneip C, Terlinden R, Beier H, et al.: Investigations into the drug-drug interaction potential of tapentadol in human liver microsomes and fresh human hepatocytes. Drug Metab Lett. 2008; 2(1): 67-75.

Hartrick C, Van Hove I, Stegmann JU, et al.: Efficacy and tolerability of tapentadol immediate release and oxycodone HCl immediate release in patients awaiting primary joint replacement surgery for end-stage joint disease: A 10-day, phase III, randomized, double-blind, active- and placebo-controlled study. Clin Ther. 2009; 31(2): 260-271.

Hale M, Upmalis D, Okamoto A, et al.: Tolerability of tapentadol immediate release in patients with lower back pain or osteoarthritis of the hip or knee over 90 days: A randomized, double-blind study. Curr Med Res Opin. 2009; 25(5): 1095-1104.

Daniels S, Casson E, Stegmann JU, et al.: A randomized, double-blind, placebo-controlled phase 3 study of the relative efficacy and tolerability of tapentadol IR and oxycodone IR for acute pain. Curr Med Res Opin. 2009; 25(6): 1551-1561.

Kleinert R, Lange C, Steup A, et al.: Single dose analgesic efficacy of tapentadol in postsurgical dental pain: The results of a randomized, double-blind, placebo-controlled study. Anesth Analg. 2008; 107(6): 2048-2055.

Grond S, Sablotzki A: Clinical pharmacology of tramadol. Clin Pharmacokinet. 2004; 43(13): 879-923.