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Levorphanol


Mechanism of action:

Levorphanol is an opioid and belongs to the morphinan derivatives. Levorphanol activates the μ-opioid receptor, which inhibits neuronal adenylate cyclase and reduces cAMP production. It also inhibits presynaptic voltage-gated Ca2+ channels, preventing calcium influx and reducing the release of pain-related neurotransmitters such as glutamate and substance P. At the same time, it activates postsynaptic K+ channels, promoting potassium efflux and leading to neuronal hyperpolarization.

Reference(s):

1. Allen RM et al. (2003). The competitive N-methyl-D-aspartate receptor antagonist (-)-6-phosphonomethyl-deca-hydroisoquinoline-3-carboxylic acid (LY235959) potentiates the antinociceptive effects of opioids that vary in efficacy at the mu-opioid receptor. J Pharmacol Exp Ther. 


2. Prommer E et al. (2007). Levorphanol: the forgotten opioid. Support Care Cancer.

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