TDL Mechanism of Action

Pharmacology: Pharmacokinetics: Tramadol is readily absorbed following oral administration but is subject to first-pass metabolism. Tramadol is metabolized by N- and O- demethylation and glucuronidation or sulfation in the liver. The metabolite O-desmethyltramadol is pharmacologically active. Tramadol is excreted mainly in the urine predominantly as metabolites. Tramadol is widely distributed, crosses the placenta, and appears in small amounts in breast milk. The elimination half-life following oral administration is about 6 hours.
Metabolism: Production of the active metabolite O-desmethyltramadol is dependent on the cytochrome P450 isoenzyme CYP2D6, which exhibits genetic polymorphism. Concomitant administration with specific inhibitors of this enzyme, such as quinidine, may increase concentrations of tramadol and lower concentrations of its active metabolite but the clinical consequence of this effect is unclear.