Clinical Information

Tapentadol, a centrally acting opioid analgesic, is used in the treatment of moderate to severe acute and chronic pain and for the management of neuropathic pain associated with diabetic peripheral neuropathy in adults (extended-release formulation only). Tapentadol acts as an opiate agonist through its binding to mu-opioid receptors and through the inhibition of norepinephrine reuptake. About 97% of the parent drug is metabolized. The major pathway of tapentadol metabolism is conjugation with glucuronic acid to produce glucuronides. Tapentadol and its metabolites (N-desmethyltapentadol and hydroxyl-tapentadol) are excreted almost exclusively via the kidneys, and approximately 70% of the drug is excreted in urine in the conjugated form. The metabolites of tapentadol have no analgesic activity. The half-life of tapentadol is approximately 4 hours.

Opioid analgesics have high abuse potential and the regular use of tapentadol may result in physical dependence and tolerance. Tapentadol is a schedule II-controlled substance with abuse liability similar to other opioid agonists.