TAPENTADOL: POTENTIAL NOVEL COMPLEMENTARY DUAL MECHANISMS OF ACTION1

Tapentadol, the active molecule in NUCYNTA®  ER , has been shown in preclinical and animal studies to activate the mu-opioid receptor (MOR) and inhibit reuptake of norepinephrine1*

Video animation depicting the unique mechanism of action of tapentadol

*Tapentadol is a centrally acting synthetic analgesic. The exact mechanism of action is unknown.

*Although the clinical relevance is unclear, preclinical studies have shown that tapentadol is an MOR agonist and a norepinephrine reuptake inhibitor (NRI). Analgesia in animal models is derived from both of these properties.

CONTRAINDICATIONS:

Significant respiratory depression; acute or severe bronchial asthma or hypercarbia in an unmonitored setting or in the absence of resuscitative equipment; known including paralytic ileus; hypersensitivity (e.g., anaphylaxis, angioedema) to tapentadol or to any other ingredients of the product; concurrent use of monoamine oxidase inhibitors (MAOIs) or use of MAOIs within the last 14 days.

References
  1. NUCYNTA® ER (package insert). Canton, MA: Collegium Pharmaceutical, Inc; 2018.
  2. Gourlay GK. Advances in opioid pharmacology. Support Care Cancer. 2005;13(3):153-159.
  3. Benarroch EE. Descending monoaminergic pain modulation. Neurology. 2008;71(3):217-221.