Tapentadol, a novel analgesic: Review of recent trends in synthesis, related substances, analytical methods, pharmacodynamics and pharmacokinetics

Abstract

This write-up describes the comprehensive facts of tapentadol, on recent trends in synthesis, related substances, analytical methods, pharmacodynamics, pharmacokinetics, adverse effect and drug interaction. Chemically, tapentadol is 3-[(1R,2R)-3-(dimethylamino)-1-ethyl-2-methylpropyl] phenol hydrochloride. Tapentadol is a centrally-acting synthetic novel analgesic which acts as μ-opioid receptor agonist as well as norepinephrine re-uptake inhibitor. Nausea and vomiting are common side effects and tapentadol glucuronide conjugate is a major metabolite excreted in urine. It is synthesized by three different schemes while nine related substances were reported. Tapentadol and its metabolites were determined in plasma matrix by chromatographic methods using spectrofluorometric detection.

Keywords

• Analysis
• Chemistry
• Pharmacodynamics
• Pharmacokinetics
• Tapentadol