Home Drug Guide Lemborexant

Drug Guide

Generic Name

Lemborexant

Brand Names Dayvigo

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/A

Drug-Herb Interactions

N/A

Nursing 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.