Version July 2025
Insomnia, sleep onset or sleep maintenance :
Note: In general, limit long-term use (>4 weeks) of insomnia medications to cases for which nonpharmacologic treatments are unavailable or ineffective and benefits are felt to outweigh risks (Ref). In one study, lemborexant was well tolerated and provided sustained efficacy over the course of 1 year (Ref).
Oral: 5 mg once daily, as needed, at bedtime with at least 7 hours before planned time of awakening; may increase to 10 mg based on response and tolerability; maximum dose: 10 mg/day.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Mild and moderate impairment: No dosage adjustment necessary.
Severe impairment: No dosage adjustment necessary; however, patients may have an increased risk of somnolence due to increased exposure to lemborexant.
Mild impairment: No dosage adjustment necessary.
Moderate impairment: Maximum dose: 5 mg/day.
Severe impairment: Use is not recommended (has not been studied).
Refer to adult dosing; use caution with doses >5 mg.
Lemborexant is frequently associated with central nervous system depression or next-day drowsiness, which may impair physical or mental abilities and increase the risk of falling, particularly in older adults. Balance impairment during the night has also been observed. Some patients experienced next-morning driving ability impairment with the 10 mg dose, indicating there is individual variation in sensitivity to CNS depressant effects (Ref).
Mechanism: Dose-related; related to the pharmacologic action via orexin receptor antagonism which is believed to suppress wake drive.
Onset: Rapid; sleep onset occurs within ~15 to 20 minutes; in older adults ≥55 years of age, onset of sleep occurs within 23 to 28 minutes (Ref). CNS depressant effects may persist for up to several days after discontinuing use.
Risk factors:
• Daytime impairment is increased with less than a full night of sleep (ie, <7 hours)
• Higher than recommended doses
• Concomitant use with other CNS depressants (eg, benzodiazepines, alcohol)
• Older adults (risk of falling)
Events associated with complex sleep-related disorder, including hazardous sleep-related activities such as sleep-walking, sleep-driving, cooking and eating food, making phone calls, or having sex while asleep have been observed rarely with lemborexant at therapeutic doses, with or without concomitant use of alcohol or other CNS depressants. Patients usually do not remember these events.
Onset: Varied; may occur at any time (following the first dose or any subsequent dose).
Lemborexant may cause abnormal dreams or nightmares infrequently and may lead to nonadherence or discontinuation. In addition, sleep paralysis (inability to move or speak for up to several minutes during sleep-wake transitions), hypnogenic hallucinations/hypnopompic hallucinations, or mild cataplexy may also occur. Cataplexy-like symptoms may occur during the night or day and are not always associated with a triggering event (eg, laughter, surprise).
Mechanism: Unknown whether these events are specifically related to antagonism of orexin receptors; however, orexin neuron loss is associated with the symptoms of narcolepsy which suggests orexin receptor antagonists can theoretically produce narcolepsy symptoms, particularly cataplexy (Ref).
Onset: Sleep paralysis events typically occurred following the first 1 or 2 doses and occurred around the time of sleep onset (within 1 hour of the dose). Two reports of cataplexy occurred ~14 hours postdose and lasted 3 to 4 minutes (Ref)
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
1% to 10%: Nervous system: Abnormal dreams (≤2%) (table 1), drowsiness (7% to 10%) (table 2), fatigue (7% to 10%) (table 3), headache (5% to 6%), nightmares (≤2%) (table 4), sleep paralysis (1% to 2%) (table 5)
|
Drug (Lemborexant) |
Placebo |
Dose |
Number of Patients (Lemborexant) |
Number of Patients (Placebo) |
|---|---|---|---|---|
|
2% |
0.9% |
10 mg |
582 |
528 |
|
0.9% |
0.9% |
5 mg |
580 |
528 |
|
Drug (Lemborexant) |
Placebo |
Dose |
Number of Patients (Lemborexant) |
Number of Patients (Placebo) |
|---|---|---|---|---|
|
10% |
1% |
10 mg |
582 |
528 |
|
7% |
1% |
5 mg |
580 |
528 |
|
Drug (Lemborexant) |
Placebo |
Dose |
Number of Patients (Lemborexant) |
Number of Patients (Placebo) |
|---|---|---|---|---|
|
10% |
1% |
10 mg |
582 |
528 |
|
7% |
1% |
5 mg |
580 |
528 |
|
Drug (Lemborexant) |
Placebo |
Dose |
Number of Patients (Lemborexant) |
Number of Patients (Placebo) |
|---|---|---|---|---|
|
2% |
0.9% |
10 mg |
582 |
528 |
|
0.9% |
0.9% |
5 mg |
580 |
528 |
|
Drug (Lemborexant) |
Placebo |
Dose |
Number of Patients (Lemborexant) |
Number of Patients (Placebo) |
|---|---|---|---|---|
|
2% |
0% |
10 mg |
582 |
528 |
|
1% |
0% |
5 mg |
580 |
528 |
<1%: Nervous system: Complex sleep-related disorder (Scott 2020), hypnogenic hallucinations (table 6)
|
Drug (Lemborexant) |
Placebo |
Dose |
Number of Patients (Lemborexant) |
Number of Patients (Placebo) |
|---|---|---|---|---|
|
0.7% |
0% |
10 mg |
582 |
528 |
|
0.1% |
0% |
5 mg |
580 |
528 |
Frequency not defined:
Cardiovascular: Palpitations
Nervous system: Cataplexy
Narcolepsy.
Canadian labeling: Additional contraindications (not in US labeling): Hypersensitivity to lemborexant or any component of the formulation.
Disease-related concerns:
• Depression: Use with caution in patients with depression; worsening of depression, including suicide or suicidal ideation, has been reported with the use of hypnotics. Intentional overdose may be an issue in this population. The minimum dose that will effectively treat the individual patient should be used. Prescriptions should be written for the smallest quantity consistent with good patient care.
• Drug abuse: Use with caution in patients with a history of drug abuse or dependence.
• Hepatic impairment: Use is not recommended in patients with severe hepatic impairment (has not been studied).
• Respiratory disease: Use with caution in patients with respiratory compromise, chronic obstructive pulmonary disease, or sleep apnea.
Other warnings/precautions:
• Appropriate use: Symptomatic treatment of insomnia should be initiated only after careful evaluation of potential causes of sleep disturbance. Failure of sleep disturbance to resolve after 7 to 10 days may indicate psychiatric and/or medical illness.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral:
DayVigo: 5 mg, 10 mg
No
Tablets (DayVigo Oral)
5 mg (per each): $14.10
10 mg (per each): $14.10
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral:
DayVigo: 5 mg, 10 mg
C-IV
Oral: Administer at bedtime with at least 7 hours before planned time of awakening. Time to sleep onset may be delayed if taken with or soon after a meal.
An FDA-approved patient medication guide, which is available with the product information and as follows, must be dispensed with this medication:
DayVigo: https://www.accessdata.fda.gov/drugsatfda_docs/label/2025/212028s011lbl.pdf#page=20
Insomnia, sleep onset or sleep maintenance: Treatment of insomnia characterized by difficulties with sleep onset and/or sleep maintenance in adults.
Dayvigo may be confused with Daypro, Daysee, or Daytrana.
Substrate of CYP3A4 (Major), P-glycoprotein (Minor); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential; Induces CYP2B6 (Weak);
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.
Alcohol (Ethyl): May increase CNS depressant effects of Lemborexant. Alcohol (Ethyl) may increase serum concentration of Lemborexant. Risk X: Avoid
Aldesleukin: May increase serum concentration of CYP Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor
Alizapride: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor
Amisulpride (Oral): May increase CNS depressant effects of CNS Depressants. Risk C: Monitor
Articaine: May increase CNS depressant effects of CNS Depressants. Management: Consider reducing the dose of articaine if possible when used in patients who are also receiving CNS depressants. Monitor for excessive CNS depressant effects with any combined use. Risk D: Consider Therapy Modification
Atazanavir: May increase serum concentration of CYP3A4 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk X: Avoid
Azelastine (Nasal): May increase CNS depressant effects of CNS Depressants. Risk X: Avoid
Benperidol: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor
Blonanserin: CNS Depressants may increase CNS depressant effects of Blonanserin. Management: Use caution if coadministering blonanserin and CNS depressants; dose reduction of the other CNS depressant may be required. Strong CNS depressants should not be coadministered with blonanserin. Risk D: Consider Therapy Modification
Brimonidine (Topical): May increase CNS depressant effects of CNS Depressants. Risk C: Monitor
Bromopride: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor
Bromperidol: May increase CNS depressant effects of CNS Depressants. Risk X: Avoid
Buclizine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor
Bulevirtide: May increase serum concentration of CYP3A4 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor
Buprenorphine: CNS Depressants may increase CNS depressant effects of Buprenorphine. Management: Consider reduced doses of other CNS depressants, and avoiding such drugs in patients at high risk of buprenorphine overuse/self-injection. Initiate buprenorphine at lower doses in patients already receiving CNS depressants. Risk D: Consider Therapy Modification
BuPROPion: CYP2B6 Inducers (Weak) may decrease serum concentration of BuPROPion. Risk C: Monitor
BusPIRone: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor
Cannabinoid-Containing Products: CNS Depressants may increase CNS depressant effects of Cannabinoid-Containing Products. Risk C: Monitor
Cetirizine (Systemic): May increase CNS depressant effects of CNS Depressants. Management: Consider avoiding this combination if possible. If required, monitor for excessive sedation or CNS depression, limit the dose and duration of combination therapy, and consider CNS depressant dose reductions. Risk D: Consider Therapy Modification
Chloral Hydrate/Chloral Betaine: CNS Depressants may increase CNS depressant effects of Chloral Hydrate/Chloral Betaine. Management: Consider alternatives to the use of chloral hydrate or chloral betaine and additional CNS depressants. If combined, consider a dose reduction of either agent and monitor closely for enhanced CNS depressive effects. Risk D: Consider Therapy Modification
Chlormethiazole: May increase CNS depressant effects of CNS Depressants. Management: Monitor closely for evidence of excessive CNS depression. The chlormethiazole labeling states that an appropriately reduced dose should be used if such a combination must be used. Risk D: Consider Therapy Modification
Chlorphenesin Carbamate: May increase adverse/toxic effects of CNS Depressants. Risk C: Monitor
Clofazimine: May increase serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor
CloZAPine: Lemborexant may increase CNS depressant effects of CloZAPine. Lemborexant may increase serum concentration of CloZAPine. Management: Dosage adjustments of lemborexant and clozapine may be necessary when administered together because of potentially additive CNS depressant effects. Close monitoring for CNS depressant effects is necessary. Consider monitoring clozapine concentrations. Risk D: Consider Therapy Modification
CNS Depressants: Lemborexant may increase CNS depressant effects of CNS Depressants. Management: Dosage adjustments of lemborexant and of concomitant CNS depressants may be necessary when administered together because of potentially additive CNS depressant effects. Close monitoring for CNS depressant effects is necessary. Risk D: Consider Therapy Modification
CYP3A4 Inducers (Moderate): May decrease serum concentration of Lemborexant. Risk X: Avoid
CYP3A4 Inducers (Strong): May decrease serum concentration of Lemborexant. Risk X: Avoid
CYP3A4 Inhibitors (Moderate): May increase serum concentration of Lemborexant. Risk X: Avoid
CYP3A4 Inhibitors (Strong): May increase serum concentration of Lemborexant. Risk X: Avoid
CYP3A4 Inhibitors (Weak): May increase serum concentration of Lemborexant. Management: The maximum recommended dosage of lemborexant is 5 mg, no more than once per night, when coadministered with weak CYP3A4 inhibitors. Risk D: Consider Therapy Modification
Daridorexant: May increase CNS depressant effects of CNS Depressants. Management: Dose reduction of daridorexant and/or any other CNS depressant may be necessary. Use of daridorexant with alcohol is not recommended, and the use of daridorexant with any other drug to treat insomnia is not recommended. Risk D: Consider Therapy Modification
DexmedeTOMIDine: CNS Depressants may increase CNS depressant effects of DexmedeTOMIDine. Management: Monitor for increased CNS depression during coadministration of dexmedetomidine and CNS depressants, and consider dose reductions of either agent to avoid excessive CNS depression. Risk D: Consider Therapy Modification
Difelikefalin: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor
Dihydralazine: CNS Depressants may increase hypotensive effects of Dihydralazine. Risk C: Monitor
Dimethindene (Topical): May increase CNS depressant effects of CNS Depressants. Risk C: Monitor
Dinutuximab Beta: May increase serum concentration of CYP Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor
Dothiepin: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor
DroPERidol: May increase CNS depressant effects of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (eg, opioids, barbiturates) with concomitant use. Risk D: Consider Therapy Modification
Elranatamab: May increase serum concentration of CYP Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor
Emedastine (Systemic): May increase CNS depressant effects of CNS Depressants. Management: Consider avoiding this combination if possible. If required, monitor for excessive sedation or CNS depression, limit the dose and duration of combination therapy, and consider CNS depressant dose reductions. Risk C: Monitor
Entacapone: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor
Epcoritamab: May increase serum concentration of CYP Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor
Flunarizine: CNS Depressants may increase CNS depressant effects of Flunarizine. Risk X: Avoid
Flunitrazepam: CNS Depressants may increase CNS depressant effects of Flunitrazepam. Management: Reduce the dose of CNS depressants when combined with flunitrazepam and monitor patients for evidence of CNS depression (eg, sedation, respiratory depression). Use non-CNS depressant alternatives when available. Risk D: Consider Therapy Modification
Fusidic Acid (Systemic): May increase serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Consider avoiding this combination if possible. If required, monitor patients closely for increased adverse effects of the CYP3A4 substrate. Risk D: Consider Therapy Modification
Gepotidacin: May increase serum concentration of CYP3A4 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk X: Avoid
Givinostat: May increase serum concentration of CYP3A4 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor
Glofitamab: May increase serum concentration of CYP Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor
Grapefruit Juice: May increase serum concentration of Lemborexant. Risk X: Avoid
HydrOXYzine: May increase CNS depressant effects of CNS Depressants. Management: Consider a decrease in the CNS depressant dose, as appropriate, when used together with hydroxyzine. Increase monitoring of signs/symptoms of CNS depression in any patient receiving hydroxyzine together with another CNS depressant. Risk D: Consider Therapy Modification
Ixabepilone: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor
Kava Kava: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor
Ketotifen (Systemic): May increase CNS depressant effects of CNS Depressants. Risk C: Monitor
Kratom: May increase CNS depressant effects of CNS Depressants. Risk X: Avoid
Levocetirizine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor
Lisuride: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor
Lofexidine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor
Loxapine: CNS Depressants may increase CNS depressant effects of Loxapine. Management: Consider reducing the dose of CNS depressants administered concomitantly with loxapine due to an increased risk of respiratory depression, sedation, hypotension, and syncope. Risk D: Consider Therapy Modification
Magnesium Sulfate: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor
Melatonin: May increase sedative effects of Hypnotics (Nonbenzodiazepine). Risk C: Monitor
Mequitazine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor
Metergoline: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor
Methotrimeprazine: CNS Depressants may increase CNS depressant effects of Methotrimeprazine. Methotrimeprazine may increase CNS depressant effects of CNS Depressants. Management: Reduce the usual dose of CNS depressants by 50% if starting methotrimeprazine until the dose of methotrimeprazine is stable. Monitor patient closely for evidence of CNS depression. Risk D: Consider Therapy Modification
Metoclopramide: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor
MetyroSINE: CNS Depressants may increase sedative effects of MetyroSINE. Risk C: Monitor
Minocycline (Systemic): May increase CNS depressant effects of CNS Depressants. Risk C: Monitor
Mosunetuzumab: May increase serum concentration of CYP Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor
Moxonidine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor
Nabilone: May increase CNS depressant effects of CNS Depressants. Risk X: Avoid
Noscapine: CNS Depressants may increase adverse/toxic effects of Noscapine. Risk X: Avoid
Olopatadine (Nasal): May increase CNS depressant effects of CNS Depressants. Risk X: Avoid
Opicapone: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor
Opioid Agonists: CNS Depressants may increase CNS depressant effects of Opioid Agonists. Management: Avoid concomitant use of opioid agonists and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. Risk D: Consider Therapy Modification
Opipramol: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor
Orphenadrine: CNS Depressants may increase CNS depressant effects of Orphenadrine. Risk X: Avoid
Oxomemazine: May increase CNS depressant effects of CNS Depressants. Risk X: Avoid
Oxybate Salt Products: Hypnotics (Nonbenzodiazepine) may increase CNS depressant effects of Oxybate Salt Products. Risk X: Avoid
OxyCODONE: CNS Depressants may increase CNS depressant effects of OxyCODONE. Management: Avoid concomitant use of oxycodone and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. Risk D: Consider Therapy Modification
Paraldehyde: CNS Depressants may increase CNS depressant effects of Paraldehyde. Risk X: Avoid
Periciazine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor
Pipamperone: May increase adverse/toxic effects of CNS Depressants. Risk C: Monitor
Piribedil: CNS Depressants may increase CNS depressant effects of Piribedil. Risk C: Monitor
Pramipexole: CNS Depressants may increase sedative effects of Pramipexole. Risk C: Monitor
Procarbazine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor
Rilmenidine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor
Ritlecitinib: May increase serum concentration of CYP3A4 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor
Ropeginterferon Alfa-2b: CNS Depressants may increase adverse/toxic effects of Ropeginterferon Alfa-2b. Specifically, the risk of neuropsychiatric adverse effects may be increased. Management: Avoid coadministration of ropeginterferon alfa-2b and other CNS depressants. If this combination cannot be avoided, monitor patients for neuropsychiatric adverse effects (eg, depression, suicidal ideation, aggression, mania). Risk D: Consider Therapy Modification
ROPINIRole: CNS Depressants may increase sedative effects of ROPINIRole. Risk C: Monitor
Rotigotine: CNS Depressants may increase sedative effects of Rotigotine. Risk C: Monitor
Spironolactone: May increase serum concentration of CYP3A4 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor
Suvorexant: CNS Depressants may increase CNS depressant effects of Suvorexant. Management: Dose reduction of suvorexant and/or any other CNS depressant may be necessary. Use of suvorexant with alcohol is not recommended, and the use of suvorexant with any other drug to treat insomnia is not recommended. Risk D: Consider Therapy Modification
Talquetamab: May increase serum concentration of CYP Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor
Tarlatamab: May increase serum concentration of CYP Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor
Teclistamab: May increase serum concentration of CYP Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor
Thalidomide: CNS Depressants may increase CNS depressant effects of Thalidomide. Risk X: Avoid
Treosulfan: May increase serum concentration of CYP3A4 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor
Trofinetide: May increase serum concentration of CYP3A4 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor
Valerian: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor
Xanomeline: May increase serum concentration of CYP3A4 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor
Zolpidem: CNS Depressants may increase CNS depressant effects of Zolpidem. Management: Reduce the Intermezzo brand sublingual zolpidem adult dose to 1.75 mg for men who are also receiving other CNS depressants. No such dose change is recommended for women. Avoid use with other CNS depressants at bedtime; avoid use with alcohol. Risk D: Consider Therapy Modification
Zuranolone: May increase CNS depressant effects of CNS Depressants. Management: Consider alternatives to the use of zuranolone with other CNS depressants or alcohol. If combined, consider a zuranolone dose reduction and monitor patients closely for increased CNS depressant effects. Risk D: Consider Therapy Modification
Concomitant alcohol use increases the risk of CNS depression, daytime impairment, postural instability, and memory impairment. Management: Avoid alcohol consumption with lemborexant.
Lemborexant crosses the placenta. Outcome data following maternal use during pregnancy are limited (Saito 2023).
Data collection to monitor pregnancy and infant outcomes following exposure to lemborexant is ongoing. Health care providers are encouraged to have patients exposed to lemborexant during pregnancy enroll in the National Pregnancy Registry for Psychiatric Medications, at 1-866-961-2388 or https://womensmentalhealth.org/research/pregnancyregistry.
Lemborexant is present in human milk.
Data related to the presence of lemborexant in human milk are available:
• Data are available from a case report following maternal use of lemborexant 10 mg daily beginning 12 weeks gestation. Breast milk was collected on postpartum day 2 from 8 to 19.6 hours after a dose. Breast milk concentrations of lemborexant ranged from 1.8 to 12.7 ng/mL. Using a milk concentration of 12.7 ng/mL, authors of the study calculated the estimated infant dose of lemborexant via human milk to be 0.00191 mg/kg/day providing a relative infant dose (RID) of 1.21% compared to the weight-adjusted maternal dose (Saito 2023).
• A study evaluating a new method of quantifying lemborexant milk concentrations provides data from 1 woman. The patient was taking lemborexant 5 mg prior to sleep on a regular basis. Maternal plasma and breast milk were sampled a few days after delivery following the maternal dose. Lemborexant concentrations 70 minutes after the dose were 4.69 ng/mL (breast milk) and 9.97 ng/mL (maternal plasma). When sampled 565 minutes after the dose, lemborexant concentrations were 5.12 ng/mL (breast milk) and 7.99 ng/mL (maternal plasma). Using the breast milk concentration taken 565 minutes after dosing, authors of the study calculated the RID of lemborexant to be 1.05% compared to the weight-adjusted maternal dose (Ishikawa 2024).
• Data related to the presence of lemborexant in human milk are available from a study conducted in 8 lactating women ≥5 weeks postpartum. Following an overnight fast, lemborexant was administered as a single 10 mg dose. Breast milk was sampled over a period of 10 days due to the long plasma half-life of lemborexant. The mean cumulative total concentration of lemborexant in breast milk was 0.0174 mg, providing an estimated infant dose via breast milk of 0.0029 mg/kg/day and a RID of 1.96% compared to the weight-adjusted maternal dose. Following the single dose, ~70% of the total amount present in breast milk was excreted within 24 hours. Expressed breast milk was not fed to the infants for ≥11 days after the maternal dose to avoid drug exposure (Rawal 2024).
• In general, breastfeeding is considered acceptable when the RID of a medication is <10% (Anderson 2016; Ito 2000).
According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and the benefits of treatment to the mother. Infants exposed to lemborexant via breast milk should be monitored for excessive sedation. Patients taking lemborexant may have decreased awareness and alertness.
Hepatic and renal function (baseline and as clinically indicated); worsening depression or suicidality; mental alertness.
Lemborexant blocks the binding of wake-promoting neuropeptides orexin A and orexin B to receptors OX1R and OX2R, which is thought to suppress wake drive.
Onset: ~15 to 20 minutes.
Absorption: High-fat and high-calorie meals decrease the Cmax by 23%, increase the AUC0-∞ by 18%, and delay the Tmax by 2 hours.
Distribution: Vd: 1,970 L.
Protein binding: ~94%.
Metabolism: Hepatic metabolism primarily by CYP3A4, and to a lesser extent by CYP3A5; the major circulating active metabolite is M10.
Half-life elimination: 17 to 19 hours.
Time to peak: ~1 to 3 hours.
Excretion: Feces: 57.4%; urine: 29.1% (<1% as unchanged drug).
Altered kidney function: Lemborexant exposure (AUC) was increased in patients with severe renal impairment (Child-Pugh class C).
Hepatic function impairment: Lemborexant exposure (AUC) was increased in patients with mild and moderate hepatic impairment (Child-Pugh class A and B), and the terminal half-life was increased in patients with moderate hepatic impairment (Child-Pugh class B).
