Lemborexant is a dual orexin receptor antagonist (DORA) used for the treatment of adult insomnia characterized by difficulties with sleep onset, sleep maintenance, or both. The best known brand formulation is Dayvigo, which is approved and currently marketed in Canada in both 5mg and 10mg tablet strengths.
Unlike traditional sedative hypnotic medications that primarily enhance GABA mediated inhibition, lemborexant targets the brain’s orexin wakefulness system. Orexin A and orexin B are neuropeptides involved in promoting wakefulness and regulating the sleep wake cycle. Lemborexant blocks signaling at both orexin 1 (OX1R) and orexin 2 (OX2R) receptors, reducing the biological drive to remain awake and helping facilitate sleep.
By suppressing orexin mediated wakefulness rather than broadly depressing central nervous system activity, lemborexant can help improve both sleep onset and sleep maintenance. It is therefore used in adults who experience difficulty initially falling asleep, repeated nighttime awakenings, or difficulty remaining asleep through the night.
Lemborexant is an oral medication, and 10mg is the highest marketed tablet strength of Dayvigo. Health Canada lists Dayvigo 10mg as a marketed prescription pharmaceutical with DIN 02507374.
This product provides:
- Active Ingredient: Lemborexant
- Strength: 10mg per tablet
- Quantity: 30 Tablets
- Drug Class: Dual Orexin Receptor Antagonist (DORA)
- Dosage Form: Oral Tablet
- Common Brand: Dayvigo
- Primary Use: Treatment of Adult Insomnia
Lemborexant is metabolized primarily through the CYP3A pathway, making drug interactions an important consideration. Strong or moderate CYP3A inhibitors can substantially increase lemborexant exposure, while CYP3A inducers may reduce its effectiveness. Medication interactions should therefore be reviewed by a qualified healthcare professional.
As a sleep promoting medication, lemborexant can cause somnolence, fatigue, dizziness, and next day impairment. The risk of reduced alertness can be greater with the 10mg strength, particularly when adequate sleep time is not available. Alcohol and other central nervous system depressants can increase sedation and impairment.
Lemborexant has also been associated with sleep related effects including sleep paralysis, vivid hallucinations during transitions between sleep and wakefulness, and temporary muscle weakness resembling cataplexy. Complex sleep behaviors, such as performing activities while not fully awake, can also occur with sleep medications and warrant medical assessment.
Lemborexant should not be used in patients with narcolepsy, because blocking orexin signaling can worsen symptoms associated with the disorder. Additional caution may be appropriate in individuals with respiratory disorders, significant liver impairment, depression, or those taking other sedating medications.
Lemborexant is a prescription medication in Canada and should be used according to the directions of a qualified healthcare professional following appropriate evaluation of persistent sleep difficulties.
