Tapentadol: A Comprehensive Review of Its Role in Pain Management

Abstract

Pain is a prevalent issue among patients, requiring effective management to prevent the transition of acute pain into chronic pain and to mitigate significant clinical and socioeconomic impacts, such as increased morbidity, mortality, prolonged recovery, unplanned readmissions, and diminished quality of life. Despite advancements in pain management guidelines, achieving consistent pain relief remains challenging due to individual differences in pain thresholds, the nature of surgical procedures, patient age, and existing comorbidities. Tapentadol, an opioid that acts as both a μ-opioid receptor agonist and a noradrenaline reuptake inhibitor, presents a promising option for pain management. Approved by the FDA in 2008 for immediate release and in 2011 for extended release, tapentadol effectively addresses both nociceptive and neuropathic pain, offering a more favorable efficacy-safety profile compared to traditional opioids such as tramadol. Additionally, tapentadol is gaining recognition as a preferred option for managing significant pain in cancer patients due to its effectiveness and reduced side effects. This review evaluates tapentadol's clinical and pharmacological attributes, systematically analyzing literature on its efficacy, safety, pharmacokinetics, and comparative effectiveness, suggesting that tapentadol is a viable option for effective pain management with potential for broader clinical applications.

Keywords: analgesia; cancer; oncology pain; opioids; pain management; tapentadol.

Figure 1. Visual representation of countries that include tapentadol in opioid class drugs for pain management

Image Credit: Authors. Data visualization based on information from [12]

Figure 2. PRISMA flowchart

PRISMA: Preferred Reporting Items for Systematic Reviews and Meta-Analyses Image Credit: Authors

Figure 3. Tapentadol mechanism of action. Employing its effect on MOR and as a noradrenaline reuptake inhibitor. Also acting on A2-AR, SPR, and GLR

SP: substance P; GL: glutamate; MOR: µ-opioid receptor; SPR: substance P receptor; GLR: glutamate receptor; A2-AR: alpha 2-adrenoreceptor; NA: noradrenaline; NAT: noradrenaline transporter Image Credit: Alshehri [42]. Originally published by, adapted, and used with permission from Dove Medical Press Ltd.