What drug should I switch to after becoming resistant to leborexan?

Leborexan is a drug used to treat insomnia. After drug resistance develops, non-benzodiazepine drugs or benzodiazepine drugs can be replaced under the guidance of a doctor, both of which can have a therapeutic effect.

1. Non-benzodiazepine drugs: such as eszopiclone, eszopiclone tablets, zolpidem, zolpidem controlled-release agent, zopiclone, etc. The exact mechanism of action of hypnotics as hypnotics is not clear, and it is usually believed to be due to its action on the GABA receptor complex coupled to the benzodiazepine receptor.

2. Benzodiazepines: such as estazolam, flurazepam, quazepam, etc. However, due to the possibility of dependence on these drugs, long-term use is generally not recommended. Among them, estazolam can act on benzodiazepine receptors, inhibit different parts of the central nervous system, and has anxiolytic, sedative, and hypnotic effects.

3. Other drugs: Commonly used drugs include paroxetine, fluoxetine, citalopram, diazepam, clonazepam, prazosin, etc.

LeBron

It is an oral orexin receptor antagonist that exhibits reversible competitive antagonism against OXR1 and OXR2. It plays a role in treating insomnia through the antagonism of orexin receptors and can improve difficulty in falling asleep or staying asleep.

Lebraxant was developed by Eisai Inc for the treatment of adult patients with insomnia. In December 2019, lemborexant was first approved in the United States for the treatment of adult patients with insomnia, and in January 2020, it was also approved in Japan.

Clinical clinical use of leborexan in the treatment of insomnia

Purpose of the study: To compare the efficacy of the orexin receptor antagonist leborexan with placebo and zolpidem tartrate extended-release in the treatment of insomnia.

Research process: In a global randomized double-blind parallel group placebo-controlled active-controlled phase 3 study, a total of 1006 randomized participants were included in placebo (n=208), zolpidem tartrate extended-release (n=263), leborexan 5mg (n=266), and leborexan 10mg (n=269).

Study Results: Both doses of Leborexan treatment demonstrated statistically significant greater changes from baseline to objective sleep onset, with significantly higher mean changes from baseline in sleep efficiency and post-sleep awakening episodes compared with placebo. Treatment with leborexan significantly improved sleep onset and sleep maintenance, including in the second half of the night, and leborexan treatment was highly efficacious and well tolerated.

Lebraxen has significant benefits in sleep initiation and sleep maintenance, and more importantly, Lebraxen's effectiveness lasts for 12 months, providing long-term benefits for subjects suffering from insomnia.

Leborex side effects

Common side effects are drowsiness, nightmares, and palpitations. Serious adverse reactions include central nervous system depression and daytime impairment, sleep paralysis, hypnotic hallucinations, impaired respiratory function, exacerbation of depression, and suicidal ideation.

References:

Rosenberg R, Murphy P, Zammit G, Mayleben D, Kumar D, Dhadda S, Filippov G, LoPresti A, Moline M. 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 Netw Open. 2019 Dec 2;2(12):e1918254. doi: 10.1001/jamanetworkopen.2019.18254. Erratum in: JAMA Netw Open. 2020 Apr 1;3(4):e206497. 31880796; PMCID: PMC6991236.

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