莱博雷生(lemborexant)的半衰期、服用最佳时间及治疗效果？

Author: Medicalhalo

Release time: 2025-10-19 11:44:20

The effective half-lives of lemborexant 5mg and 10mg are 17 hours and 19 hours respectively. The best time to take it is before bedtime. It has good efficacy in treating insomnia in adults.

The new anti-insomnia drug lemborexant

is a new dual orexin receptor antagonist, developed by Japan's Eisai Company. It was approved by the U.S. Food and Drug Administration on December 20, 2019 for the treatment of insomnia in adults. This medicine comes in tablets, each containing 5mg or 10mg of Leborexen.

Effects and effects

Lemborexant can competitively antagonize orexin receptor 1 and orexin receptor 2 at the same time, inhibiting the wake-promoting effect of orexin, thereby inhibiting the occurrence of wakefulness and playing a role in treating insomnia. Lemborexant has good efficacy in treating insomnia in adults. By weakening the arousal signal, it can shorten the time to fall asleep and extend the duration of sleep. It is used to treat difficulty falling asleep or maintaining sleep. It is less likely to cause adverse reactions such as falls and hangovers.

Half-life of lemborexant

The drug instructions for lemborexant clearly state that after administration, the recovery rates of the prototype drug in feces and urine are 57.4% and 29.1% respectively (prototype drug < 1%). The effective half-lives of 5mg and 10mg are 17 hours and 19 hours respectively.

Treatment Effectiveness

Importance: Insomnia disorders are common among older adults and are associated with health risks. However, issues with the effectiveness and safety of existing treatments create significant unmet needs in this patient population.

Objective: To compare the efficacy of the orexin receptor antagonist lemborexant with placebo and zolpidem tartrate sustained-release in the treatment of insomnia.

Design, setting, and participants: The SUNRISE 1 (SUNRISE 1) clinical trial of lemborexant in patients with insomnia aged 55 years and older is a global, randomized, double-blind, parallel-group, placebo-controlled, active-controlled Phase 3 study. Data analysis was conducted from January 31, 2018 to September 10, 2018. Participants were aged 55 years and older and had insomnia, characterized by difficulty maintaining sleep and confirmed by sleep history, sleep diary, and polysomnography. Participants may also have difficulty falling asleep.

Intervention: Participants received placebo, zolpidem tartrate extended-release (6.25 mg), or leborexan (5 mg or 10 mg) at bedtime for 1 month.

Main results and measurements: Paired polysomnograms were collected at baseline, the first two nights, and the last two nights of treatment. The primary endpoint was change in latency from baseline to sustained sleep with lemborexant treatment compared with placebo. The primary secondary endpoints were sleep effectiveness and change from baseline in post-sleep arousal events compared with placebo, and post-sleep arousal events in the second half of the night compared with zolpidem.

Results: Of 1006 randomized participants, 869 (86.4%) were female, with a mean age of 63 years (range, 55-88 years). Both doses of lemborexant treatment demonstrated statistically significant greater changes from baseline to objective sleep onset compared with placebo.

As assessed by latency to sustained sleep (log-transformed) measured using polysomnography at the end of 1 month of treatment (nights 29 and 30) (least squares geometric mean treatment ratio vs. Primary endpoints for placebo: 0.77, 95% for lemborexant 5 mg and 0.72, 95% for lemborexant 10 mg.For nights 29 and 30, mean change from baseline in sleep efficiency as measured using polysomnography (LSM treatment difference compared with placebo 5 mg lemborexant, 7.1%, 10 mg lemborexant, 8.0% and post-sleep awakening episodes leborexant) P< .001 was significantly higher. Additionally, for nights 29 and 30, post-sleep awakenings occurred in the second half of the night. The least squares mean treatment difference for lemborexant 5 mg was -6. .7 minutes for 10 mg of lemborexant - 8.0 minutes, significantly higher than zolpidem treatment measured using polysomnography

6 subjects (4 in the zolpidem group and 2 in the lemborexant group). 5mg group), none were treatment-related. Other adverse events were mostly mild or moderate in severity.

Conclusions and Relevance: In this randomized clinical trial, treatment with lemborexant improved sleep onset and sleep maintenance, including in the second half of the night, compared with placebo and zolpidem, as measured objectively using polysomnography.

The best time to take lemborexant

The best time to take lemborexant is before going to bed or when going to bed. If taken with or shortly after a meal, the effect of lemborexant may be delayed.

Taking lemborexant before bed can make the drug more effective and block the wake-promoting neuropeptide orexin. A And orexin B binds to the receptors OX1R and OX2R, thereby inhibiting the awakening drive, which can improve the patient's sleep disruption and relieve the symptoms of difficulty falling asleep.

In addition, the recommended dose of lemborexant is 5 mg per day. No more than once at night, before going to bed, with at least 7 hours remaining before the scheduled wake-up time. The dosage of lemborexant can be increased to 10 mg based on the patient's clinical response and tolerance.

Lemborexa. nt) Precautions

1. Avoid drinking:

During the use of lemborexant, patients should not drink alcohol and take this product at the same time to avoid alcohol affecting the therapeutic effect of the drug and reducing its efficacy.

2. Patients with depression should use with caution:

Depression worsening or suicidal thoughts have been reported during lemborexant treatment, so patients with depression should use it strictly under the guidance of a doctor.

3. Complex sleep behavior:

< p>Lemborexant may cause complex sleep behaviors, including sleepwalking, sleep driving, preparing and eating food, talking on the phone, or engaging in sexual intercourse while not fully awake. Inform patients that they should discontinue use of lemborexant and notify them immediately if any of the above symptoms occur. Medical staff

4. Daytime impairment:

Lemborexant may impair daytime awakening. If this product is used with less than a full night of sleep, or if the recommended dose is exceeded, the risk of daytime impairment will be increased. If leborexan is used under these conditions, patients should be warned not to drive or engage in any activity that requires a high level of alertness. Inform the patient that increased sleep may increase the risk of falling.

Summary

Lemborexan t) It can improve patients' insomnia and has good efficacy. The half-life of the drug varies depending on the drug specifications. It is recommended that patients only take this product when preparing or going to bed, and need to stay in bed for a full night (at least 7 hours) before moving again.