What is the mechanism of action and clinical improvement effect of lemborexant?

Lemborexant is a reversible, competitive and orally active dual antagonist of orexin OX1 and OX2 receptors. It inhibits orexin by competitively binding to 2 subtypes of orexin receptors (orexin receptor 1 and receptor 2), thereby treating insomnia. According to existing clinical trials, leborexan has shown good results in improving insomnia symptoms.

lemborexant’s mechanism of action

The orexin system is a key regulator of the sleep-wake cycle and plays an important role in the regulation of sleep and wakefulness. It purposefully promotes the initiation and maintenance of sleep by interfering with orexinergic neurotransmission. In individuals with insomnia disorder, the orexin system, which regulates sleep and wakefulness, may not function properly.

Its mechanism of action is mainly by regulating melatonin receptors (MT1/MT2) and antagonizing orexin (orexin) receptors in the brain, thereby helping to improve sleep.

Melatonin receptors (MT1/MT2) play an important role in regulating the sleep-wake cycle, while orexin receptors are important in promoting wakefulness. By acting on these two receptors, leborexine helps prolong sleep time and improve sleep quality.

Clinical improvement with leborexan

According to existing clinical trials, leborexan has shown good effects in improving insomnia symptoms. It can significantly extend sleep time, improve sleep quality, reduce the number of nighttime awakenings, and shorten the time to fall asleep.

In a study involving 1,006 patients aged 55 years and older with insomnia disorders, the subjects took 5 mg and 10 mg of leborexine or placebo and 6.25 mg of zolpidem tartrate extended-release tablets. One month later, compared with placebo, taking 5 mg or 10 mg of leborexine before bed could significantly improve the symptoms of difficulty falling asleep, sleep efficiency was also significantly improved, and nighttime awakening time was significantly shortened.

At the same time, compared with zolpidem tartrate sustained-release tablets, Leborexen 5mg or 10mg significantly shortened the waking time in the second half of the night to -6.7 minutes and -8.0 minutes. These results indicate that Leborexen can effectively improve insomnia symptoms, including difficulty falling asleep, sleep efficiency, and nighttime awakenings.

It should be noted that Leborexan cannot treat the underlying causes of insomnia, such as depression, anxiety and other psychological diseases, or other physical diseases. When using leborexan to treat insomnia, it is recommended that patients also pay attention to adjustments to their living habits, such as maintaining a regular schedule, avoiding the use of electronic devices before going to bed, and reducing stress.

Labradorian

1. The recommended dose is 5 mg, taken before going to bed at night, with at least 7 hours remaining before the planned awakening time. The dose may be increased to 10 mg based on clinical response and tolerability.

2. The maximum recommended dose is 10mg, once a day.

3. The initial and maximum recommended dose for patients with moderate liver damage is 5 mg, taken once every night. This drug is not recommended for patients with severe liver damage.

Leborex medication

1. CNS depressant effects and daytime impairment: Impairment of alertness and motor coordination, including morning impairment, risk increases with dose and combined use with other central nervous system (CNS) depressants. For patients taking leborexine 10 mg, be reminded not to drive the next day and other activities that require complete mental alertness

2. Sleep paralysis, hypnotic/hypnotic hallucinations and cataplexy-like symptoms: may occur when using Lebraxen.

3. Complex sleep behaviors: Behaviors including sleepwalking, sleepwalking driving, and engaging in other activities while not fully awake may occur. If complex sleep behaviors occur, the drug should be discontinued immediately.

4. Impaired respiratory function: The impact on respiratory function should be considered.

5. Depressive exacerbation/suicidal ideation: Depressive exacerbation or suicidal ideation may occur. Prescribe the minimum number of tablets to avoid intentional overdose.

6. Diagnosis of comorbidities needs to be evaluated: Re-evaluate whether insomnia persists after 7-10 days of treatment.

Summary

As an orexin receptor antagonist, leborexan has certain efficacy in the treatment of insomnia. In addition, the efficacy of leborexan depends largely on factors such as the patient's age, gender, race, and body mass index. Clinical studies also show that leborexan has less impact on patients' daytime functions and has mild adverse reactions, such as headache, nausea, fatigue, etc.

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