Lemborexant
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Omid Afkhami-Ardakani
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Overview
Lemborexant is a Dual Orexin Receptor Antagonist (DORA) that is FDA approved for the treatment of adult patients with insomnia. Common adverse reactions include Somnolence, Fatigue, Headache, Abnormal dreams, Sleep paralysis, and Hypnagogic hallucinations..
Adult Indications and Dosage
FDA-Labeled Indications and Dosage (Adult)
Recommended starting dose: 5 mg taken no more than once per night, immediately before going to bed, with at least 7 hours remaining before the planned time of awakening.
Dose may be increased to 10 mg based on clinical response and tolerability.
Maximum recommended dose: 10 mg once daily.
Off-Label Use and Dosage (Adult)
Guideline-Supported Use
There is limited information regarding Off-Label Guideline-Supported Use of Lemborexant in adult patients.
Non–Guideline-Supported Use
There is limited information regarding Off-Label Non–Guideline-Supported Use of Lemborexant in adult patients.
Pediatric Indications and Dosage
FDA-Labeled Indications and Dosage (Pediatric)
Safety and effectiveness in pediatric patients have not been established.
Off-Label Use and Dosage (Pediatric)
Guideline-Supported Use
There is limited information regarding Off-Label Guideline-Supported Use of Lemborexant in pediatric patients.
Non–Guideline-Supported Use
There is limited information regarding Off-Label Non–Guideline-Supported Use of Lemborexant in pediatric patients.
Contraindications
Patients with narcolepsy.
Warnings
CNS Depressant Effects and Daytime Impairment: May impair alertness and motor coordination, including morning impairment.
Sleep Paralysis, Hypnagogic/Hypnopompic Hallucinations, and Cataplexy-like Symptoms: May occur with use.
Complex Sleep Behaviors: Behaviors such as sleep-walking, sleep-driving, and engaging in other activities while not fully awake may occur. Discontinue immediately if a complex sleep behavior occurs.
Compromised Respiratory Function: Effects on respiratory function should be considered.
Worsening of Depression/Suicidal Ideation: May occur. Prescribe the lowest number of tablets feasible to avoid intentional overdosage.
Need to Evaluate for Co-morbid Diagnoses: Reevaluate if insomnia persists after 7 to 10 days of treatment.
Adverse Reactions
Clinical Trials Experience
Somnolence
Fatigue
Headache
Abnormal dreams
Sleep paralysis
Hypnagogic hallucinations
Postmarketing Experience
There is limited information regarding Lemborexant Postmarketing Experience in the drug label.
Drug Interactions
CYP3A Inhibitors: Avoid concomitant use with strong or moderate CYP3A inhibitors.
CYP3A Inducers: Avoid concomitant use with strong or moderate CYP3A inducers.
Alcohol: Avoid concomitant use; may increase the risk of CNS depression.
Other CNS Depressants: Concomitant use may increase the risk of CNS depression.
Use in Specific Populations
Pregnancy
Pregnancy Category (FDA):
There is no FDA guidance on usage of Lemborexant in women who are pregnant.
Pregnancy Category (AUS): B3
There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Lemborexant in women who are pregnant.
Labor and Delivery
There is no FDA guidance on use of Lemborexant during labor and delivery.
Nursing Mothers
Unknown if excreted in human milk; caution advised.
Pediatric Use
There is no FDA guidance on the use of Lemborexant in pediatric settings.
Geriatic Use
There is no FDA guidance on the use of Lemborexant in geriatric settings.
Gender
There is no FDA guidance on the use of Lemborexant with respect to specific gender populations.
Race
There is no FDA guidance on the use of Lemborexant with respect to specific racial populations.
Renal Impairment
There is no FDA guidance on the use of Lemborexant in patients with renal impairment.
Hepatic Impairment
Moderate impairment: Maximum dose of 5 mg.
Severe impairment: Not recommended.
Females of Reproductive Potential and Males
There is no FDA guidance on the use of Lemborexant in women of reproductive potentials and males.
Immunocompromised Patients
There is no FDA guidance one the use of Lemborexant in patients who are immunocompromised.
Administration and Monitoring
Administration
Take orally within 30 minutes before going to bed.
Ensure at least 7 hours remain before planned awakening.
Do not take with or immediately after a meal, as this may delay onset of action.
Monitoring
Monitor for signs of CNS depression.
Assess for complex sleep behaviors.
Evaluate for worsening depression or suicidal thoughts.
IV Compatibility
Not applicable.
Overdosage
Symptoms: Excessive sedation.
Impaired psychomotor performance.
Potential respiratory depression.
Pharmacology
There is limited information regarding Lemborexant Pharmacology in the drug label.
Mechanism of Action
Lemborexant is a dual orexin receptor antagonist (DORA) that blocks orexin receptors OX1R and OX2R, which are involved in wakefulness, thereby promoting sleep.
Structure
There is limited information regarding Lemborexant Structure in the drug label.
Pharmacodynamics
Binds to OX1R and OX2R with IC₅₀ values of 6.1 nM and 2.6 nM, respectively.
No significant effect on QTc interval at doses up to 5 times the recommended dose.
Pharmacokinetics
Absorption: Tmax approximately 1–3 hours.
Bioavailability: ≥87%.
Distribution: Volume of distribution ~1970 L; 94% protein bound.
Metabolism: Primarily via CYP3A4.
Elimination: Half-life ~17–19 hours; excreted in feces (57.4%) and urine (29.1%).
Nonclinical Toxicology
There is limited information regarding Lemborexant Nonclinical Toxicology in the drug label.
Clinical Studies
There is limited information regarding Lemborexant Clinical Studies in the drug label.
How Supplied
Form: Film-coated tablets.
Strengths:
5 mg: Pale yellow, round, debossed with "5" on one side and "LЄM" on the other.
10 mg: Orange, round, debossed with "10" on one side and "LЄM" on the other.
Packaging: Bottles of 30 tablets.
Storage
Storage Conditions: Store at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C and 30°C (59°F and 86°F).
Images
Drug Images
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Package and Label Display Panel
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Patient Counseling Information
Advise patients to take Dayvigo only when they can stay in bed for at least 7 hours.
Caution against next-day impairment, Worsening Depression or Suicidal Thoughts.
Precautions with Alcohol
Patients should be advised of the following precautions regarding alcohol consumption while taking Dayvigo:
Increased Sedative Effects: Combining Dayvigo with alcohol can enhance sedative effects, leading to increased drowsiness, dizziness, and impaired cognitive and motor functions.
Risk of Next-Day Impairment: Alcohol can increase the blood levels of Dayvigo, potentially leading to next-day impairment in activities requiring mental alertness. Recommendation: Patients should avoid consuming alcohol while taking Dayvigo to minimize the risk of adverse effects.
Brand Names
Dayvigo®
Manufacturered by Eisai Inc.
Look-Alike Drug Names
There is limited information regarding Lemborexant Look-Alike Drug Names in the drug label.
Drug Shortage Status
Price
References
The contents of this FDA label are provided by the National Library of Medicine.