levorphanol

Levorphanol is a potent synthetic opioid analgesic used for the management of moderate to severe pain, particularly when other pain medications are ineffective or not tolerated. It is the levorotatory enantiomer of racemorphan and was first described in 1946 and marketed as Levo-Dromoran in 1953. Levorphanol acts primarily as an agonist at the μ-opioid receptor (MOR), but also activates δ-opioid (DOR) and κ-opioid (KOR) receptors, as well as the nociceptin receptor (NOP). Additionally, it functions as an NMDA receptor antagonist and inhibits reuptake of serotonin and norepinephrine, contributing to its efficacy in neuropathic pain. Compared to morphine, it is approximately eight times more potent at MOR with a longer duration of action. Its metabolism occurs via glucuronidation in the liver without involvement of CYP450 enzymes. The drug has been used both for acute severe pain and chronic pain conditions[1][3][5][6].

Brand names

Levo-Dromoran

Other names

levorphanollevorphanol tartrate