lemborexant

Contraindicated in:

Narcolepsy;
Severe hepatic impairment.

Use Cautiously in:

History of substance abuse or addiction;
Severe renal impairment;
Mild or moderate hepatic impairment;
History of or concurrent psychiatric diagnoses;
Pulmonary disease or obstructive sleep apnea;
OB: Use during pregnancy only if potential maternal benefit justifies potential fetal risk;
Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant;
Pedi: Safety and effectiveness not established in children;
Geri: Older adults at ↑ risk for falls.

Adv. Reactions/Side Effects ⬆ ⬇

Neuro: cataplexy, depression, drowsiness, hallucinations (during sleep), headache, sleep driving, sleep paralysis, sleep walking, SUICIDAL BEHAVIOR/IDEATION

Interactions ⬆ ⬇

Drug-drug:

Strong CYP3A inhibitors, including clarithromycin or itraconazole, as well as moderate CYP3A inhibitors, including fluconazole or verapamil, may ↑ levels and risk of excessive sedation; avoid concurrent use.
Weak CYP3A inhibitors, including chlorzoxazone, may ↑ levels and risk of adverse reactions; do not exceed dose of 5 mg/day.
Strong CYP3A inducers, including carbamazepine or rifampin, as well as moderate CYP3A inducers, including bosentan, efavirenz, etravirine, or modafanil, may ↓ levels and risk of effectiveness; avoid concurrent use.
May ↓ levels and effectiveness of CYP2B6 substrates, including bupropion or methadone; dosage adjustments may be needed.
Risk of CNS depression, next-day impairment, "sleep-driving," and other complex behaviors while not fully awake ↑ with other CNS depressants, including alcohol, some antihistamines, opioids, other sedative/hypnotics (including benzodiazepines), and tricyclic antidepressants; dosage adjustments may be needed.

Drug-Natural Products:

St. John's wort may ↓ levels and risk of effectiveness; avoid concurrent use.

Drug-Food:

Grapefruit juicemay ↑ levels and risk of excessive sedation; avoid concurrent use.

Availability ⬆ ⬇

Tablets: 5 mg; 10 mg

Route/Dosage ⬆ ⬇

PO (Adults ): 5 mg immediately before going to bed; if well tolerated but not optimally effective, dose may be ↑ to 10 mg (max dose = 10 mg/night); do not repeat dose on a single night. Concurrent use of weak CYP3A inhibitor: Do not exceed dose of 5 mg/night.

Hepatic Impairment

PO (Adults ): Moderate hepatic impairment: Do not exceed dose of 5 mg/night.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Antagonizes the effects of orexins A and B, naturally occurring neuropeptides that promote wakefulness, by binding to their receptors.

Therapeutic effects:

Improved sleep.

Classifications ⬆ ⬇

Therapeutic Classification: sedative/hypnotics

Pharmacologic Classification: orexin receptor antagonists

Pharmacokinetics ⬆ ⬇

Absorption: High-fat, high-calorie meal delays absorption and sleep onset.

Distribution: Extensively distributed to extravascular tissues.

Protein Binding: 94%.

Metabolism/Excretion: Extensively metabolized by liver via CYP3A into active metabolite (M10). 57% excreted in feces, 29% in urine, mostly as metabolites.

Half-Life: 17–19 hr.

Contr. Subst. Schedule ⬆ ⬇

Time/Action Profile ⬆ ⬇

(sleep)

ROUTE	ONSET	PEAK	DURATION
PO	15–20 min	unknown	7 hr‡

‡Excess sedation may persist for several days after discontinuation.

Patient/Family Teaching ⬆ ⬇

Instruct patient to take lemborexant immediately before going to bed, as directed; do not increase dose. May result in short-term memory impairment, hallucinations, impaired coordination, and dizziness. Do not take lemborexant if consumed alcohol that evening. Advise patient to read Medication Guide before starting therapy and with each Rx refill in case of changes.
Advise patient to avoid grapefruit juice during therapy.
May cause daytime and next-day drowsiness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
Caution patient that balance during nighttime waking may be impaired with increased risk of falls. Nighttime attention and memory may also be impaired.
Inform patient and family of potential for signs and symptoms of sleep paralysis (inability to move or speak for up to several min during sleep-wake transitions and hallucinations, including vivid and disturbing perceptions) and mild cataplexy (leg weakness lasting from seconds to a few min, occurring at night or during the day.
Caution patient and family that lemborexant may cause complex sleep behaviors (sleep walking, sleep-driving, making and eating food, talking on the phone, having sex) while unaware. Patient may not remember anything done during the night; increased risk with alcohol or other CNS depressants. Discontinue lemborexant immediately and notify health care professional if complex sleep behaviors occur.
Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking any other Rx, OTC, or herbal products, especially St. John's wort.
Caution patient to avoid concurrent use of alcohol or other CNS depressants.
Encourage patient and family to be alert for emergence of worsening of depression and suicidal ideation. If these symptoms occur, notify health care professional immediately.
Rep: Advise patient to notify health care professional if pregnancy is planned or suspected or if breastfeeding. Infants exposed to lemborexant through breast milk should be monitored for excessive sedation. Inform pregnant patient of pregnancy exposure registry that monitors pregnancy outcomes in women who are exposed to lemborexant during pregnancy. Register patient by calling 1-888-274-2378.

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Indications ⬇

Contraind./Precautions ⬆ ⬇