Lemborexant (Dayvigo)

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

Pharmacokinetics of Lemborexant

Lemborexant: Cytochrome P450 Metabolism

Substrate of (Metabolized by)
  • 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
  • Insomnia disorder

Dosing for Lemborexant

Starting 5 mg PO qHS
Titration Increased by 5 mg PO qHS
Maximum 10 mg PO qHS
  • Lemborexant comes in
  • Headaches, sedation, vivid dreaming
  • 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