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Lemborexant powder

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Lemborexant powder is a hypnotics that use to treat adult patients with insomnia characterized by difficulties with sleep onset and/or sleep maintenance, works by slowing activity in the brain to allow sleep.

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Product Description

Lemborexant Powder Basic Characteristics

Product Name Lemborexant powder
CAS Number 1369764-02-2
Molecular Formula C22H20F2N4O2
Formula Weight 410.422
Synonyms (1R,2S)-2-[[(2,4-Dimethyl-5-pyrimidinyl)oxy]methyl]-2-(3-fluorophenyl)-N-(5-fluoro-2-pyridinyl)cyclopropanecarboxamide;
Appearance White to Off-White Solid powder
Storage and Handling 20°C, Inert atmosphere

 

What is Lemborexant Powder

Lemborexant powder is a hypnotics that use to treat adult patients with insomnia characterized by difficulties with sleep onset and/or sleep maintenance, works by slowing activity in the brain to allow sleep.  Lemborexant is a novel dual orexin receptor antagonist, belongs to the group of medicines called central nervous system (CNS) depressants, mainly appear at “tablet” form, sold under brand name with “Dayvigo”.

 

Lemborexant Powder Mechanism of Action

The mechanism of action of lemborexant powder in the treatment of insomnia is presumed to be through antagonism of orexin receptors. The orexin neuropeptide signaling system is involved in many physiologic functions, including sleep/wake control. Orexin-A and orexin-B activate post-synaptic G-protein coupled2 orexin-1 receptors (OX1R) and orexin-2 receptors (OX2R), which are found on neurons in the hypothalamus that project to numerous wake-controlling nuclei. Each receptor carries slightly different activity – activation of OX1R appears to suppress the onset of rapid eye movement (REM) sleep, whereas activation of OX2R appears to suppress non-REM sleep. The orexin neuropeptide signaling system plays a role in wakefulness. Blocking the binding of wake-promoting neuropeptides orexin A and orexin B to orexin receptors OX1R and OX2R is thought to suppress wake drive. Lemborexant powder binds to orexin receptors OX1R and OX2R and acts as a competitive antagonist with stronger inhibition effect to OX2R*.

It has been proposed that lemborexant powder take advantage of this unique mechanism may come with fewer side effects than more commonly prescribed drugs to treat insomnia, like: benzodiazepines.At present, this kind of medications used to treat insomnia include benzodiazepines and “z-drugs,” which act on the GABA receptor, antihistamines that disrupt the wakeful effects of histamine, and trazodone, which exerts its effects on both the serotonergic system and histamine receptors. Benzodiazepines present with a high potential for misuse and physical and psychological dependence. While lemborexant powder still a relatively novel drug, evidence suggests lemborexant powder may be at least more effective with less potential for dependence than zolpidem, a non-benzodiazepine GABA receptor agonist. Lemborexant powder effectively reduces sleep latency and increases maintenance compared to controls. Lemborexant powder appears to be more effective at improving sleep maintenance than zolpidem in patients with insomnia.

 

Lemborexant Powder Benefit &Side Effect

Lemborexant 5 mg and 10 mg improved sleep onset and sleep maintenance over 6 months and was well-tolerated. Treatment with lemborexant resulted in significantly greater increases from baseline in total sleep time compared with both placebo and zolpidem. REM sleep was significantly increased with lemborexant compared to baseline, and latency and REM sleep were significantly decreased from baseline.

Daytime sleepiness or fatigue occur in some people who take Lemborexant Powder. Side effects can be more likely to occur if Lemborexant powder is taken in a high dose, in combination with other CNS depressants, or after a night of poor sleep.

Around 1 in 20 people taking 5 mg of Lemborexant Powder experience daytime sleepiness or similar side effects, while 1 in 10 people taking 10 mg of Lemborexant Powder experience them.

There is a dose-dependent decrease in balance, memory, and attention for the four hours after taking Lemborexant Powder. Therefore, it should only be taken right before going to sleep. The impacts on balance and memory are increased if alcohol and Lemborexant Powder are taken together, and this is discouraged.

Less common side effects on Lemborexant powder include:

▪ Somnolence

▪ Drowsiness

▪ CNS depressant effects/daytime impairment

▪ Sleep paralysis

▪ Hypnagogic/hypnopompic hallucinations

▪ Cataplexy-like symptoms

▪ Complex sleep behaviors

▪ Worsening of depression/suicidal ideation

 

How Do You Take Lemborexant Powder

Take lemborexant powder only once per night right before you get into bed and get enough 7hours to sleep will get more better effect. You may have trouble speaking or moving while you are falling asleep. It may take longer for you to wake up, speak, or move around when you wake up. You may feel like you are still dreaming for several minutes after waking. Do not take it with or soon after a meal, will tale longer to work. In meanwhile, your reactions may be impaired the morning after you take lemborexant powder. Do not drive or do anything that requires you to be alert. Drowsiness can cause falls, accidents, or severe injuries. Do not increase your dose without talking to your healthcare provider first. Call your healthcare provider if your insomnia (sleep problem) worsens or is not improved within 7 to 10 days.



What Drugs Will Affect Lemborexant Powder?

Using lemborexant with other drugs that make you drowsy can worsen this effect. Ask your doctor before using opioid medication, a sleeping pill, a muscle relaxer, or medicine for anxiety or seizures.

Sometimes it is not safe to use certain medications at the same time. Some drugs can affect your blood levels of other drugs you take, which may increase side effects or make the medications less effective.

Other drugs may affect lemborexant, including prescription and over-the-counter medicines, vitamins, and herbal products. Tell your doctor about all your current medicines and any medicine you start or stop using.

 

Reference

[1]. 2021 Dec 20. Drugs and Lactation Database (LactMed) [Internet]. Bethesda (MD): National Library of Medicine (US); 2006–. PMID: 33104322

[2]. BMJ Open. 2021 Nov 26;11(11):e054885. doi: 10.1136/bmjopen-2021-054885.PMID: 34836909

[3]. Regul Toxicol Pharmacol. 2021 Dec;127:105053. doi: 10.1016/j.yrtph.2021.105053. Epub 2021 Oct 4. PMID: 34619288

 

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