No more sedatives! How do new-generation sleeping pills gently regulate sleep rhythms?

March 18, 2025

1. Why are traditional sleeping pills addictive and affect sleep quality?

Have you ever tried traditional sleeping pills (such as diazepam, zopiclone, zolpidem) and found them to be effective at first, but as time went on, the dosage became higher and higher, and after stopping the medication, it was even harder to fall asleep than before? This phenomenon is not uncommon, because the mechanism of action of traditional sleeping pills determines their addictiveness and side effects .

📌 The main problems with traditional sleeping pills :

❌ Forced sedation of the brain leads to dependence - this type of drug enhances the inhibitory effect of GABA ( γ- aminobutyric acid) receptors , forcing the brain's neural activity to decrease , thereby quickly falling asleep ( Lader, 2011 ). However, the brain will gradually adapt to this external intervention and develop tolerance, resulting in the need for higher doses to achieve the same effect.

❌ Disruption of normal sleep structure - Studies have found that benzodiazepines (such as diazepam) may reduce REM (rapid eye movement) sleep , affecting memory consolidation, emotion regulation and brain health ( Kuriyama & Endo, 2018 ).

❌ Feeling sleepy when waking up in the morning affects daytime performance - Traditional sleeping pills have a long half-life and may still remain in the body the next morning, causing daytime sleepiness and decreased concentration , affecting work and quality of life ( Billioti de Gage et al., 2014 ). ❌ Rebound insomnia after discontinuation of medication - Since the brain adapts to the inhibitory effects of the GABA system after long-term medication , sudden discontinuation of medication may lead to rebound insomnia, increased anxiety, and even withdrawal symptoms ( Lader, 2011 ).

So, is there a gentler and safer way to help you sleep that is not addictive and does not damage your sleep quality? The answer is a new generation of sleeping pills .

2. How do the new generation of sleeping aids help the brain fall asleep naturally?

Unlike traditional sleeping pills, Suvorexant , Lemborexant , and Daridorexant are orexin receptor antagonists ( ORAs ), and their mechanism of action is more in line with the body's natural sleep regulation .

📌 What is orexin and how does it affect sleep?

Orexin is a neurotransmitter secreted by the hypothalamus of the brain . Its main function is to maintain wakefulness and prevent the brain from entering sleep mode.

✅ High orexin levels → daytime wakefulness (brain activity, concentration).

✅ Low orexin levels → sleep at night (reduced wakefulness signals, the body enters a resting state).

Common questions for people with insomnia :

❌ High levels of orexin in the brain make it difficult to fall asleep even when tired ( Mahlios et al., 2013 ).

❌ Orexin remains active at night, causing waking up easily in the middle of the night and shallow sleep ( Sun et al., 2021 ).

📌 How do orexin receptor antagonists improve sleep?

The new generation of sleeping pills do not forcibly calm the nervous system, but instead block orexin receptors ( Orexin Receptors OX1R and OX2R ), reducing wakefulness signals and allowing the body to naturally enter a sleep state.

3. Suvorexant, Lebrexant, and Darilexant: Comparison of the mechanisms of action of three new sleeping aids

The three orexin receptor antagonists ( ORAs ) currently approved worldwide - suvorexant, lebrexant and dalisant - are optimized for different types of insomnia.

drug	Main Function	Target Group	Mechanism of action
Suvorexant	Reduce nighttime awakenings and maintain stable sleep throughout the night	People who wake up easily at night and have sleep maintenance disorders	Acts on OX1R & OX2R to reduce wakefulness signals and help sleep more consistently.
Lemborexant	Speed up the time to fall asleep and reduce difficulty falling asleep	Anxiety-type insomnia, difficulty falling asleep	It mainly acts on OX2R , reduces wakefulness signals, and allows the brain to quickly enter a sleep state.
Daridorexant	Improve the proportion of deep sleep and reduce morning fatigue	Those who have light sleep and feel sleepy in the morning	It acts on OX1R & OX2R , optimizes sleep structure, increases the proportion of deep sleep, and makes you more energetic when you wake up in the morning.

📌 Research data supports :

• Clinical studies on Lebrexan have shown that taking it can shorten the time it takes to fall asleep by 52% , helping people to enter a sleep state quickly ( Ueno et al., 2022 ).

• Suvorexant can reduce the number of nighttime awakenings by 43% and improve sleep continuity throughout the night ( Herring et al., 2016 ).

• Dauvilliers can increase the proportion of deep sleep without affecting daytime wakefulness ( Dauvilliers et al., 2022 ).

4. Why are orexin receptor antagonists safer than traditional sleeping pills?

Features	Traditional sleeping pills (eg, diazepam, zopiclone)	Orexin receptor antagonists (suvorexant, lebrexant, darilexant)
Mechanism of action	Directly enhances GABA inhibition, forcing sedation	Block wake-up signals and let the body fall asleep naturally
Does it affect deep sleep?	May reduce REM sleep and affect memory consolidation	Does not affect deep sleep and improves sleep quality
Is it addictive?	Long-term use can lead to addiction and increased tolerance	No dependency, can be used for a long time
Morning state	Feeling sleepy in the morning and having decreased concentration	Wake up the next day, no effect

📌 Why do doctors recommend orexin receptor antagonists?

✅ It is non-addictive and can be used for a long time .

✅ Does not affect deep sleep and improves overall sleep quality .

✅ It will not cause drowsiness the next day and your mental state will be good during the day .

5. Conclusion: How to choose a safer sleep aid plan?

📌 Core summary :

• Traditional sleeping pills help people fall asleep by calming the nervous system, but they are addictive and may affect deep sleep ( Lader, 2011 ).

• The new generation of sleeping aids (such as suvorexant, lebrexant, and darilexant) reduce wakefulness signals rather than forced sedation, allowing the brain to fall asleep naturally and without dependence ( Sun et al., 2021 ).

• Studies have shown that these new sleeping aids can be used for a long time and sleep will not rebound after discontinuation , making them a safer choice for sleeping aids ( Ueno et al., 2022 ).

📌 Recommended for symptoms :

✅ Difficulty falling asleep ➝ Lebron (helps you fall asleep quickly) .

✅ Waking up easily at night ➝ Suvorexant (reduces nighttime awakenings) .

✅ Light sleep, tiredness in the morning ➝ Daryl Leydig (Improve deep sleep) .

If you’re looking for a safer, non-addictive sleep aid, orexin receptor antagonists may be your best choice !

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