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NERVOUS SYSTEM › PSYCHOLEPTICS › HYPNOTICS AND SEDATIVES › Orexin receptor antagonists
lemborexant
N05CJ02
Forms & Strengths
- Oral tablets: 5 mg
- Oral tablets: 10 mg
Adult Dosing
- Recommended dose: 5 mg once nightly immediately before bedtime
- Maximum dose: 10 mg once nightly
- Must allow for at least 7 hours remaining before planned awakening
- Take with or immediately after food, preferably avoiding high-fat meals
Pediatric Dosing
- Safety and effectiveness in pediatric patients have not been established
Indications
- Treatment of adult patients with insomnia, characterized by difficulties with sleep onset and/or sleep maintenance
Mechanism of Action
- Dual orexin receptor antagonist (DORA)
- Antagonizes orexin receptors OX1R and OX2R, suppressing wakefulness-promoting drive
Contraindications
- Narcolepsy
- Known hypersensitivity to lemborexant or any excipients
Adverse Reactions
- Somnolence
- Nasopharyngitis
- Headache
- Abnormal dreams
- Sleep paralysis
- Complex sleep behaviors (e.g., sleep-walking, sleep-driving)
Drug Interactions
- Strong or moderate CYP3A inhibitors increase exposure; limit maximum dose to 5 mg
- Strong or moderate CYP3A inducers decrease efficacy; avoid coadministration
- Additive CNS depression with alcohol, CNS depressants, and sedatives
Curated Content: Needs Vetting Before Put to Clinical Use