The Role of Orexins In Sleep-Wake Regulation1
Rethinking the treatment of insomnia
Excessive wakefulness is common underlying cause of insomnia
NORMAL SLEEP-AWAKE REGULATION
Daytime
In the daytime,
orexins help us
stay awake
Night
At night,
orexin activity is very low
letting us sleep
INSOMNIA
Insomnia
In insomnia,
excess orexins prevent
us from sleeping
DAYVIGO
DAYVIGO blocks
orexin activity, helping
patients fall asleep
and stay asleep
Normal sleep-wake regulation occurs when the wake-promoting pathway predominates during the day, and the sleep-promoting pathway predominates at night.
In insomnia, patients have difficulty falling asleep or staying asleep as a result of an imbalance and conflict between these two pathways.
These pathways are controlled by wake-promoting and sleep-promoting neurotransmitters. The orexin neuropeptide signaling system is thought to play a critical role in wakefulness in the brain.2
What is DAYVIGO®
- A dual orexin receptor antagonist (DORA). The Orexin neuropeptide
signaling system is a central promoter of wakefulness.3 - Blocking the binding of wake-promoting neuropeptides orexin A and
orexin B to receptors OX1R and OX2R is thought to suppress wake drive.4
DAYVIGO works differently from sedatives which enhance sleep-promoting
effects through increased GABA activity2
DAYVIGO® blocks orexin activity at night, encouraging normal sleep
DAYVIGO prevents orexins from keeping the "wake switch" on.
• DAYVIGO suppresses wakefulness and can normalize sleep-wake patterns.
References:
-
Wang, Chunmei et al., 2018. The Orexin/Receptor System: Molecular Mechanism and Therapeutic Potential
for Neurological Diseases. Frontiers in molecular neuroscience, 11, p.220. -
Rosenberg, Russell et al., 2019. Comparison of Lemborexant With Placebo and Zolpidem Tartrate Extended Release for the
Treatment of Older Adults With Insomnia Disorder: A Phase 3 Randomized Clinical Trial. JAMA network open, 2(12), p.e1918254. -
Sakurai, Takeshi, 2007. The neural circuit of orexin (hypocretin): maintaining sleep and wakefulness.
Nature reviews. Neuroscience, 8(3), pp.171–181. -
Kärppä, Mikko et al., 2020. Long-term efficacy and tolerability of lemborexant compared with placebo in adults with insomnia
disorder: results from the phase 3 randomized clinical trial SUNRISE 2. Sleep (New York, N.Y.), 43(9), pp.Sleep (New York, N.Y.),
2020–09-14, Vol.43 (9). -
DAYVIGO (lemborexant) [Prescribing Information]. Eisai (HK) Co. Ltd; 2021.