lemborexant is a medication used for the treatment of insomnia. It belongs to orexin receptor antagonists. lemborexant works by blocking the action of orexin, a neuropeptide that plays a role in regulating wakefulness and sleep. By inhibiting the orexin signalling, lemborexant helps promote sleep and improve the overall quality and duration of sleep.
The spectrum of lemborexant’s action is primarily focused on insomnia, including difficulty falling asleep and staying asleep. It is used to treat insomnia and sleep maintenance. lemborexant can be used in adults for both short-term and long-term treatment of insomnia.
5 mg orally not more than once each night, just before going back to bed, with a minimum of 7 hours before the scheduled time of awakening remaining
Based on the clinical response and tolerability, the dosage can be increased upto 10 mg.
5 mg orally not more than once each night, just before going back to bed, with a minimum of 7 hours before the scheduled time of awakening remaining
Based on the clinical response and tolerability, the dosage can be increased up to 10 mg
Dosage Forms & Strengths
Schedule IV tablet:
10mg
5mg
Frequency defined
1-10%
10 mg /night
Headache (4.5%)
Sleep paralysis (1.6%)
fatigue or Somnolence (9.6%)
abnormal dreams or Nightmare (2.2%)
5 mg /night
fatigue or Somnolence (6.9)
Sleep paralysis (1.3%)
Headache (5.9%)
<1%
10 mg /night
Hypnagogic hallucinations (0.7%)
5 mg /night
Hypnagogic hallucinations (0.1%)
abnormal dreams or Nightmare (0.9%)
Black Box Warning:
There were no black box warnings specifically associated with lemborexant.
Contraindication/Caution:
Contraindication:
Hypersensitivity: lemborexant should not be used in patients with known allergic or hypersensitivity to the drug.
Severe hepatic impairment: lemborexant is contraindicated in individuals with severe hepatic impairment as it may lead to increased exposure to the drug.
Concomitant use with strong CYP3A4 inhibitors: lemborexant should not be used concomitantly with strong inhibitors of the enzyme CYP3A4, as this may increase the levels of lemborexant and its potential side effects.
Caution:
CNS depressant Effects: lemborexant may cause central nervous system (CNS) depressant effects, including drowsiness and impaired coordination. Caution should be exercised when operating machinery, driving, or engaging in activities that require alertness until the individual’s response to the medication is known.
Drug Interactions: lemborexant may interact with other medications, including those that are metabolized by the CYP3A4 enzyme system. Caution should be exercised when using lemborexant concomitantly with other drugs, and potential interactions should be evaluated.
Sleep Disorders: lemborexant is indicated for the treatment of insomnia. However, it is important to assess the underlying cause of sleep disturbances before initiating treatment. Caution should be exercised in individuals with other sleep disorders or conditions that may contribute to sleep disturbances.
Respiratory Impairment: lemborexant may cause respiratory depression or exacerbate respiratory conditions. It should be used under caution in patients with compromised respiratory function, such as chronic obstructive pulmonary disease (COPD) or sleep apnea.
Comorbidities:
Hepatic Impairment: lemborexant is primarily metabolized by the liver, so individuals with hepatic impairment may experience altered drug metabolism and clearance. Dose adjustments may be necessary in individuals with moderate to severe hepatic impairment.
Renal Impairment: lemborexant does not undergo significant renal excretion, so no dose adjustment is required in individuals with renal impairment. However, caution should still be exercised in this population, and individual response to the medication should be monitored.
Psychiatric Disorders: lemborexant should be used with caution in individuals with a history of psychiatric disorders, such as depression or anxiety, as it may worsen these conditions or lead to mood changes. Regular monitoring is important in individuals with pre-existing psychiatric conditions.
Pregnancy consideration: N/A
Lactation: unknown
Pregnancy category:
Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.
Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.
Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.
Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.
Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.
Category N: There is no data available for the drug under this category.
Pharmacology:
lemborexant is a dual orexin receptor antagonist (DORA) that acts by selectively blocking the binding of orexins (hypocretins) to their receptors. Orexins are neuropeptides that play a role in promoting wakefulness and regulating the sleep-wake cycle.
The pharmacological effects of lemborexant are mediated through its antagonism of the orexin receptors, specifically orexin receptor 1 (OX1R) and orexin receptor 2 (OX2R). By blocking the action of orexins, lemborexant inhibits wake-promoting signals and promotes sleep.
lemborexant exhibits high selectivity for OX1R and OX2R, with greater affinity for OX2R. By selectively targeting these receptors, lemborexant helps regulate the sleep-wake cycle without affecting other neurotransmitter systems involved in sedation or hypnotic effects.
The exact mechanism by which lemborexant promotes sleep is fully not known, but it is believed to involve the inhibition of wakefulness-promoting centers in the brain, the reduction of orexin-mediated arousal signals, and the promotion of sleep-inducing processes.
Pharmacodynamics:
Orexins, also known as hypocretins, are neuropeptides that play a major role in regulating the sleep-wake cycle and promoting wakefulness. They are primarily produced in the lateral hypothalamus and act on orexin receptors in various brain regions, including the arousal-promoting centers.
By blocking the orexin receptors, lemborexant inhibits the wake-promoting effects of orexins, resulting in a decrease in wakefulness and an increase in sleep propensity. This mechanism helps to regulate the sleep-wake cycle and promote consolidated and restful sleep.
Additionally, lemborexant has a high selectivity for the OX2R subtype, which is believed to be the primary mediator of the hypnotic effects. The inhibition of OX2R by lemborexant further contributes to its sleep-promoting properties.
The precise pharmacodynamic effects of lemborexant on other neurotransmitter systems or brain regions are not fully understood.
Pharmacokinetics:
Absorption
lemborexant is orally administered and is well-absorbed from the gastrointestinal tract. The maximum plasma concentration (Cmax) is reached within 1-3 hours after administration. The bioavailability of lemborexant is approximately 76%.
Distribution
lemborexant has a moderate volume of distribution, indicating that it distributes well into body tissues. It is extensively bound to plasma proteins, to albumin.
Metabolism
lemborexant is primarily metabolized in the liver by cytochrome P450 enzymes, specifically CYP3A4 and CYP3A5. The major metabolic pathway involves oxidation and subsequent glucuronidation. The metabolites formed are pharmacologically inactive.
Elimination and excretion
The elimination of lemborexant occurs primarily through the feces (approximately 88%) and to a lesser extent through urine (approximately 5%). The elimination half-life of lemborexant is approximately 17 hours.
Administration:
lemborexant is available as an oral tablet and should be taken by mouth.
Dosage: The specific dosage of lemborexant will depend on the individual’s response and condition to treatment.
Timing: lemborexant should be taken orally once daily, within 30 minutes before going to sleep, and with at least 7 hours before the planned time of waking up remaining.
Swallowing: The tablet should be swallowed whole with water and should not be crushed, chewed, or split.
Food: lemborexant can be taken with or without food, as food does not significantly affect its absorption.
Consistency: It is important to take lemborexant consistently daily at the same time to achieve optimal results.
Avoidance of Activities: After taking lemborexant, individuals should avoid engaging activities that require mental alertness or coordination, such as driving, operating machinery, or performing tasks that require full attention.
Patient information leaflet
Generic Name: lemborexant
Pronounced: (lem-boh-REX-ant)
Why do we use lemborexant?
lemborexant is a medication primarily used to treat insomnia. It belongs to orexin receptor antagonists, which work by blocking the action of orexin, a neurotransmitter involved in promoting wakefulness.
The main use of lemborexant is to help improve sleep onset and sleep maintenance in adults with insomnia. Lemborexant is typically prescribed for short-term use, usually 1 to 4 weeks.
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5 mg orally not more than once each night, just before going back to bed, with a minimum of 7 hours before the scheduled time of awakening remaining
Based on the clinical response and tolerability, the dosage can be increased upto 10 mg.
5 mg orally not more than once each night, just before going back to bed, with a minimum of 7 hours before the scheduled time of awakening remaining
Based on the clinical response and tolerability, the dosage can be increased up to 10 mg
