Mechanism of Action
BELSOMRA contains suvorexant, an orexin receptor antagonist.
- The therapeutic effect of BELSOMRA in insomnia is presumed to be through antagonism of orexin receptors
- What is orexin? Orexin is one of the neurotransmitters that play a role in wakefulness. It reinforces the activity of other wake-promoting neurotransmitters.1
- Blocking orexin receptors is thought to suppress wake drive.
- BELSOMRA has no appreciable binding affinity at acetylcholine, dopamine, gamma-aminobutyric acid (GABA), histamine, melatonin, noradrenaline, opiate, or serotonin receptors.2,3
- Antagonism of orexin receptors may also underlie potential adverse effects such as signs of narcolepsy/cataplexy. Genetic mutations in the orexin system in animals result in hereditary narcolepsy; loss of orexin neurons has been reported in humans with narcolepsy.