DAYVIGO

Dayvigo Generic Name & Formulations

Legal Class

CIV

General Description

Lemborexant 5mg, 10mg; tabs.

Pharmacological Class

Orexin receptor antagonist.

How Supplied

Tabs—30, 90

Manufacturer

Eisai Pharmaceuticals

Generic Availability

Mechanism of Action

Lemborexant exerts its therapeutic effects in insomnia is presumed to be through antagonism of orexin receptors. The orexin neuropeptide signaling system is a central promoter of wakefulness. Blocking the binding of wake-promoting neuropeptides orexin A and orexin B to receptors OX1R and OX2R is thought to suppress wake drive.

Dayvigo Indications

Indications

Treatment of insomnia characterized by difficulties with sleep onset and/or sleep maintenance.

Dayvigo Dosage and Administration

Adult

Take immediately before bedtime, with (≥7hrs) remaining before the planned time of awakening. 5mg once per night; may increase to max 10mg once daily based on clinical response and tolerability. Concomitant weak CYP3A inhibitors or moderate hepatic impairment: max 5mg once daily. Effect may be delayed if taken with or soon after a meal.

Children

Not established.

Dayvigo Contraindications

Contraindications

Narcolepsy.

Dayvigo Boxed Warnings

Not Applicable

Dayvigo Warnings/Precautions

Warnings/Precautions

CNS depression. Daytime impairment (including impaired driving w. 10mg dose). Monitor for somnolence. Discontinue immediately if any complex sleep behaviors develop. Compromised respiratory function (eg, moderate to severe COPD, mild to severe obstructive sleep apnea). Suicidal ideation or behavior. Depression. Monitor for worsening insomnia or new cognitive/behavioral abnormalities. Reevaluate if unresponsive after 7–10 days of treatment. Severe renal or mild hepatic impairment: possible increased risk of somnolence. Severe hepatic impairment: not recommended. Drug or alcohol abusers. Elderly. Pregnancy. Nursing mothers.

Dayvigo Pharmacokinetics

Absorption

The time to peak concentration (tmax) of lemborexant is ~1 to 3 hours. Lemborexant C_max decreased by 23%, AUC_0-inf increased by 18%, and t_max was delayed by 2 hours following administration of a high-fat and high-calorie meal (containing approximately 150, 250, and 500 to 600 calories from protein, carbohydrate, and fat, respectively).

Distribution

The volume of distribution of lemborexant is 1970 L. Plasma protein binding of lemborexant is ~88% in vitro and 94% in clinical samples.

Metabolism

Primarily metabolized by CYP3A4, and to a lesser extent by CYP3A5. The major circulating metabolite is M10.

Elimination

Following administration of an oral dose, 57.4% of the dose was recovered in the feces and 29.1% in the urine (<1% as unchanged). The effective half-life for lemborexant 5 mg and 10 mg is 17 and 19 hours, respectively.

Dayvigo Interactions

Interactions

Avoid alcohol. Potentiates CNS depression with other CNS depressants (eg, benzodiazepines, opioids, tricyclic antidepressants, alcohol); may need to adjust doses. Concomitant strong or moderate CYP3A inhibitors (eg, itraconazole, clarithromycin, fluconazole, verapamil); avoid. Concomitant weak CYP3A inhibitors (eg, chlorzoxazone, ranitidine); reduce dose (see Adults). Antagonized by strong or moderate CYP3A inducers (eg, rifampin, carbamazepine, St. John's wort, bosentan, efavirenz, etravirine, modafinil); avoid. Antagonizes CYP2B6 substrates (eg, bupropion, methadone); consider increasing dose of substrates.

Dayvigo Adverse Reactions

Adverse Reactions

Somnolence/fatigue, headache, nightmare/abnormal dreams; complex sleep-related behaviors (eg, sleep-walking, sleep-driving), sleep paralysis, hypnagogic hallucinations, cataplexy-like symptoms.

Dayvigo Clinical Trials

See Literature

Dayvigo Note