Lemborexant (Dayvigo)

Primer

Lemborexant (Trade name: Dayvigo) is a dual orexin receptor antagonist (DORA) used in the treatment of insomnia.

Pharmacokinetics

See also article: Introduction to Pharmacology

Pharmacokinetics of Lemborexant

Absorption
Distribution
Metabolism
Elimination
Half-life

See also article: Cytochrome (CYP) P450 Metabolism

Lemborexant: Cytochrome P450 Metabolism

Substrate of (Metabolized by)
Induces
Inhibits

Pharmacodynamics

Mechanism of Action

Lemborexant is a dual orexin receptor antagonist
- It is a reversible, competitive antagonist that binds rapidly to both orexin receptors 1 and 2, with greater affinity for orexin receptor 2.^[1]
- It thus blocks binding of orexin A and B to orexin receptors 1 and 2 respectively.
Increases NREM and REM sleep
Reduces wakefulness

Toxicity

Indications

Insomnia disorder

Dosing

Dosing for Lemborexant

Starting	5 mg PO qHS
Titration	Increased by 5 mg PO qHS
Maximum	10 mg PO qHS
Taper

Formulations

Lemborexant comes in

Monitoring

Contraindications

Absolute

Relative

Drug-Drug Interactions

Side Effects

Headaches, sedation, vivid dreaming

Adverse Events

Clinical Pearls

Lemborexant, like all DORAs, have a theoretical risk for abuse.^[2]
- Patients with a history of abuse or addiction may be at increased risk for abuse and addiction to DORAs and should be followed carefully

Special Populations

Geriatric

See main article: Geriatric Pharmacology

Pediatric

See main article: Pediatric Pharmacology

Obstetric and Fetal

See main article: Obstetric and Fetal Pharmacology

Medically Ill

See main article: Psychotropic Dosing in the Medically Ill

Resources

¹⁾ Rosenberg, R., Murphy, P., Zammit, G., Mayleben, D., Kumar, D., Dhadda, S., ... & Moline, M. (2019). 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 network open, 2(12), e1918254-e1918254.

²⁾ FDA Review, Lemborexant, Department of Health and Human Services Food and Drug Administration Center for Drug Evaluation and Research | Office of Surveillance and Epidemiology (OSE) Epidemiology

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