Tapentadol in Pain Management A μ-Opioid Receptor Agonist and Noradrenaline Reuptake Inhibitor

• Published in: CNS drugs Vol. 25; no. 5; pp. 359 - 370
• Main Authors: Hartrick, Craig T., Rozek, Richard J.
• Format: Journal Article
• Language: English
• Published: Cham Springer International Publishing 01.05.2011; Adis International; Wolters Kluwer Health, Inc
• Subjects: Adrenergic alpha-2 Receptor Agonists - administration & dosage; Adrenergic alpha-2 Receptor Agonists - adverse effects; Adrenergic alpha-2 Receptor Agonists - therapeutic use; Analgesics; Analgesics, Opioid - administration & dosage; Analgesics, Opioid - adverse effects; Analgesics, Opioid - therapeutic use; Biological and medical sciences; Care and treatment; Delayed-Action Preparations; Drug Interactions; Gastrointestinal diseases; Humans; Leading Article; Medical sciences; Medicine; Medicine & Public Health; Neuralgia - drug therapy; Neurology; Neuropharmacology; Neurosciences; Pain; Pain - drug therapy; Pharmacology. Drug treatments; Pharmacotherapy; Phenols - administration & dosage; Phenols - adverse effects; Phenols - therapeutic use; Psychiatry; Psychopharmacology; Receptors, Opioid, mu - agonists; Risk factors; United States; Neuropathic Pain; Numerical Rating Scale; Immediate Release; Oxycodone; Diabetic Peripheral Neuropathy; Human; Drug; Agonist; Indication; Toxicity; Treatment efficiency; μ Opioid receptor; Chemical structure; Pharmacotherapy; Review; Catecholamine; Reuptake inhibitor; Tapentadol; Analgesic; Pain; Treatment; Neurotransmitter; Secondary effect; Norepinephrine; Mechanism of action
• ISSN: 1172-7047; 1179-1934; 1179-1934
• DOI: 10.2165/11589080-000000000-00000

Several mechanisms can be proposed to explain an apparent synergistic analgesic action between μ-opioid and α 2 -adrenergic receptor agonists. Combining both effects in a single molecule eliminates the potential for drug-drug interactions inherent in multiple drug therapy. Tapentadol is the first US FDA-approved centrally acting analgesic having both μ-opioid receptor agonist and noradrenaline (norepinephrine) reuptake inhibition activity with minimal serotonin reuptake inhibition. This dual mode of action may make tapentadol particularly useful in the treatment of neuropathic pain. Having limited protein binding, no active metabolites and no significant microsomal enzyme induction or inhibition, tapentadol has a limited potential for drug-drug interactions. Clinical trial evidence in acute and chronic non-cancer pain and neuropathic pain supports an opioid-sparing effect that reduces some of the typical opioid-related adverse effects. Specifically, the reduction in treatment-emergent gastrointestinal adverse effects for tapentadol compared with equianalgesic pure μ-opioid receptor agonists results in improved tolerability and adherence to therapy for both the immediate- and extended-release formulations of tapentadol.