levallorphan

Levallorphan is a synthetic opioid modulator of the morphinan family that acts as both an opioid antagonist and partial agonist. It primarily functions as a competitive antagonist at the mu-opioid receptor (MOR), reversing or preventing effects such as respiratory depression, sedation, and hypotension induced by opioids like morphine. Unlike pure antagonists such as naloxone, levallorphan also exhibits agonist activity at the kappa-opioid receptor (KOR), which can provide mild analgesia but may cause psychotomimetic side effects at higher doses. Historically, it was used to reverse opioid-induced respiratory depression during anesthesia and in cases of narcotic overdose. It was also combined with other opioids (notably pethidine) to reduce their side effects in obstetrics. Its use has declined due to the availability of newer agents like naloxone[1][2][4][5].

Brand names

LorfanNaloxifanNaloxiphan

Other names

levallorphan tartrate