dextilidine

Dextilidine is the (1S,2R)-enantiomer of the synthetic opioid analgesic tilidine. It functions as a prodrug that undergoes rapid first-pass metabolism in the liver, primarily via N-demethylation by CYP3A4 and CYP2C19 enzymes, to form its active metabolite, nortilidine. Nortilidine is a potent agonist of the μ-opioid receptor and is responsible for the moderate to strong analgesic effects associated with tilidine administration. In clinical practice, dextilidine is typically administered as part of the racemic mixture tilidine, which is often formulated in combination with naloxone to prevent parenteral abuse.

Brand names

ValoronValoron N

Other names

(+)-tilidine(1S,2R)-tilidinedextilidina