Nurses Compass
Drug Guide
Lemborexant
Classification
Therapeutic: Hypnotic for sleep disorder (Insomnia)
Pharmacological: Dual orexin receptor antagonist (DORA)
FDA Approved Indications
- Sleep onset and sleep maintenance insomnia in adults
Mechanism of Action
Lemborexant selectively antagonizes orexin receptors (OX1R and OX2R), which play a role in wakefulness, thereby promoting sleep by inhibiting the orexin neuropeptide signaling system.
Dosage and Administration
Adult: Initial dose is 5 mg orally at bedtime; can be increased to 10 mg or decreased to 5 mg based on response and tolerability.
Pediatric: Not approved for use in pediatric patients.
Geriatric: Use with caution; start at lower dose (5 mg) due to increased sensitivity to hypnotics.
Renal Impairment: No specific adjustment recommended, but caution advised.
Hepatic Impairment: Use only if clearly needed; no specific dose adjustment recommended.
Pharmacokinetics
Absorption: Rapidly absorbed with peak plasma concentrations in approximately 1.3 hours.
Distribution: Extensively bound to plasma proteins.
Metabolism: Primarily metabolized in the liver via CYP3A enzymes; minor contribution from CYP2B6.
Excretion: Metabolites excreted mainly in feces (67%) and urine (23%).
Half Life: Approximately 12 hours, suitable for once-per-night dosing.
Contraindications
- Hypersensitivity to lemborexant or any component of the formulation.
Precautions
- Risk of sleep paralysis, cataplexy, hallucinations, and complex sleep behaviors (e.g., sleep driving).
- Caution in patients with suicidal ideation or behavior.
- Use with caution in patients with hepatic impairment.
Adverse Reactions - Common
- Somnolence (Very common)
- Headache (Common)
- Fatigue (Common)
Adverse Reactions - Serious
- Sleep paralysis, hallucinations, complex sleep behaviors (Uncommon)
- Daytime drowsiness leading to falls or accidents (Uncommon)
- Potential worsening of depression or suicidal thoughts (Rare)
Drug-Drug Interactions
- CYP3A inhibitors (e.g., ketoconazole, itraconazole) may increase lemborexant levels.
- CYP3A inducers (e.g., rifampin) may decrease efficacy.
Drug-Food Interactions
N/ADrug-Herb Interactions
N/ANursing Implications
Assessment: Monitor sleep patterns, mental status, and safety, especially in elderly patients.
Diagnoses:
- Risk for injury due to sedation or impaired cognition.
Implementation: Administer at bedtime, ensure patient understands the importance of safety measures.
Evaluation: Assess sleep quality and duration, monitor for adverse effects.
Patient/Family Teaching
- Take medication exactly as prescribed, at the same time each night.
- Do not drive or operate machinery after taking lemborexant until alertness returns.
- Avoid alcohol and other CNS depressants.
- Report any unusual behaviors or side effects.
Special Considerations
Black Box Warnings:
- Complex sleep behaviors including sleep driving, sleep eating, and sleep talking have been reported.
- Risk of adverse effects is increased in older adults.
Genetic Factors: No specific genetic factors identified affecting response.
Lab Test Interference: No known interference.
Overdose Management
Signs/Symptoms: Excessive sedation, hypotension, impaired consciousness.
Treatment: Supportive care, airway management, monitoring vital signs. Activated charcoal may be considered if ingestion is recent and the patient is alert.
Storage and Handling
Storage: Store at room temperature, 20°C to 25°C (68°F to 77°F).
Stability: Stable for the duration of the labeled shelf life when stored properly.