Lemborexant (Dayvigo)

Primer

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

Pharmacokinetics

Pharmacokinetics of Lemborexant

Absorption
Distribution
Metabolism
Elimination
Half-life

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

Pediatric

Obstetric and Fetal

Medically Ill

Resources

References

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