lemborexant (Rx)

Brand and Other Names:Dayvigo
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Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

tablet

  • 5mg
  • 10mg

Insomnia

Indicated for insomnia characterized by difficulties with sleep onset and/or sleep maintenance

5 mg PO no more than once per night, immediately before going to bed, with at least 7 hr remaining before planned time of awakening

May increase dose to maximum of 10 mg based on clinical response and tolerability

Dosage Modifications

Coadministration with CYP3A inhibitors

  • Strong or moderate CYP3A inhibitors: Avoid concomitant use
  • Weak CYP3A inhibitors: Not to exceed 5 mg/night

Coadministration with CYP3A inducers

  • Strong or moderate CYP3A inducers: Avoid concomitant use

Renal impairment

  • Mild, moderate, or severe: No dose adjustment recommended
  • Severe: AUC increased; patients may experience increased risk of somnolence

Hepatic impairment

  • Mild (Child-Pugh A): No dose adjustment recommended; however, patients may experience an increased risk of somnolence; AUC increased
  • Moderate (Child-Pugh B): Not to exceed 5 mg/night; AUC, peak plasma concentration, and half-life increased
  • Severe (Child-Pugh C): Not recommended (not studied)

Safety and efficacy not established

Insomnia

Indicated for insomnia characterized by difficulties with sleep onset and/or sleep maintenance

5 mg PO no more than once per night, immediately before going to bed, with at least 7 hr remaining before planned time of awakening

May increase dose to maximum of 10 mg based on clinical response and tolerability

Dosage Modifications

Coadministration with CYP3A inhibitors

  • Strong or moderate CYP3A inhibitors: Avoid concomitant use
  • Weak CYP3A inhibitors: Not to exceed 5 mg/night

Coadministration with CYP3A inducers

  • Strong or moderate CYP3A inducers: Avoid concomitant use

Renal impairment

  • Mild, moderate, or severe: No dose adjustment recommended
  • Severe: AUC increased; patients may experience increased risk of somnolence

Hepatic impairment

  • Mild (Child-Pugh A): No dose adjustment recommended; however, patients may experience an increased risk of somnolence; AUC increased
  • Moderate (Child-Pugh B): Not to exceed 5 mg/night; AUC, peak plasma concentration, and half-life increased
  • Severe (Child-Pugh C): Not recommended (not studied)

Dosing Considerations

Somnolence incidence in patients aged ≥65 yr with 10 mg was higher (9.8%) compared with 7.7% in patients <65 yr

Somnolence incidence with 5 mg was similar in patients aged ≥65 yr (4.9%) and <65 yr (5.1%)

Somnolence incidence in patients treated with placebo was ≤2% regardless of age

Exercise caution when using doses >5 mg in patients aged ≥65 yr who may be at higher risk of falls

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Interactions

Interaction Checker

and lemborexant

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            Adverse Effects

            1-10%

            5 mg/night

            • Somnolence or fatigue (6.9%)
            • Headache (5.9%)
            • Sleep paralysis (1.3%)

            10 mg/night

            • Somnolence or fatigue (9.6%)
            • Headache (4.5%)
            • Nightmare or abnormal dreams (2.2%)
            • Sleep paralysis (1.6%)

            <1%

            5 mg/night

            • Nightmare or abnormal dreams (0.9%)
            • Hypnagogic hallucinations (0.1%)

            10 mg/night

            • Hypnagogic hallucinations (0.7%)
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            Warnings

            Contraindications

            Narcolepsy

            Cautions

            CNS depressant that can impair daytime wakefulness even when used as prescribed; CNS depression may persist and affect next-day tasks (eg, driving ability); CNS depression may persist in some patients for several days after discontinuing; coadministration with other CNS depressants may increase risk

            Sleep paralysis, an inability to move or speak for up to several minutes during sleep-wake transitions, and hypnagogic/hypnopompic hallucinations, including vivid and disturbing perceptions, can occur; mild cataplexy can occur, with symptoms that include periods of leg weakness lasting from seconds to a few minutes

            Complex sleep behaviors, including sleep-walking, sleep-driving, and engaging in other activities while not fully awake (eg, preparing and eating food, making phone calls, having sex), reported with hypnotic use

            Consider effect on respiratory function if prescribed to patients with compromised respiratory function; has not been studied with moderate-to-severe obstructive sleep apnea or COPD

            In primarily depressed patients treated with hypnotics, worsening of depression and suicidal thoughts and actions (including completed suicides) have been reported; monitor for new behavioral signs or symptoms

            Evaluate for comorbid diagnoses where insomnia may be presenting manifestation of a medial and/or psychiatric disorder

            Drug interaction overview

            • CNS depressants
              • Coadministration with other CNS depressants (eg, benzodiazepines, opioids, tricyclic antidepressants, alcohol) increases the risk of CNS depression, which can cause daytime impairment
            • CYP3A inhibitors
              • Coadministration with a strong, moderate, or weak CYP3A inhibitor increases lemborexant AUC and peak plasma concentration which may increase the risk of lemborexant adverse reactions
            • CYP3A inducers
              • Concomitant use with a strong or moderate CYP3A inducer decreases lemborexant exposure, which may reduce lemborexant efficacy
            • CYP2B6 substrates
              • Coadministration decreases AUC of CYP2B6 substrates
              • Check prescribing information for CYP2B6 substrate for dosage recommendations if coadministered
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            Pregnancy & Lactation

            Pregnancy

            Data are not available on use in pregnant women to evaluate for drug-associated risks of major birth defects, miscarriage, or adverse maternal or fetal outcomes

            Clinicians are encouraged to register patients in the Dayvigo pregnancy registry by calling 1-888-274-2378

            Animal studies

            • Rats
              • Lemborexant was administered orally to pregnant rats during organogenesis in 2 studies at doses of 60, 200, and 600 mg/kg/day or 20, 60, and 200 mg/kg/day, which are approximately 6 to >300 times the maximum recommended human dose (MRHD) based on AUC

              • Lemborexant caused maternal toxicity, manifested by decreased body weight and food consumption, decreased mean fetal body weight, an increased number of dead fetuses, and skeletal, external, and visceral malformations (omphalocele, cleft palate, and membranous ventricular septal defect) at >300 times the MRHD based on AUC

              • Lemborexant was administered orally to pregnant rats during pregnancy and lactation at doses of 30, 100, and 300 mg/kg/day, which are approximately 15-206 times the MRHD based on AUC

              • Lemborexant caused maternal toxicity that consisted of decreased body weight and food consumption and toxicity to offspring consisting of decreased pup body weights, decreased femur length, and decreased acoustic startle responses at 206 times the MRHD based on AUC
            • Rabbits
              • Lemborexant was administered orally to pregnant rabbits during the period of organogenesis at doses of 10, 30, and 100 mg/kg/day, which are approximately 7-139 times the MRHD based on AUC

              • Lemborexant caused maternal toxicity that consisted of decreased body weight and food consumption and a higher incidence of skeletal variations (presence of cervical ribs and supernumerary lung lobes) at approximately 139 times the MRHD based on AUC

            Lactation

            Data are not available on the presence of lemborexant in human milk, effects on breastfed infants, or effects on milk production

            Lemborexant and its metabolites are present in the milk of lactating rats; when a drug is present in animal milk, it is likely that the drug will be present in human milk

            Monitor infants exposed through breastmilk for excessive sedation

            Consider the developmental and health benefits of breastfeeding along with the mother’s clinical need for the drug and any potential adverse effects on the breastfed infant from the drug or from the underlying maternal condition

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.

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            Pharmacology

            Mechanism of Action

            Dual orexin antagonist (DORA)

            Orexins are neuropeptides that regulate the sleep-wake cycle; orexins promote wakefulness by binding G-protein-coupled receptors, OX1R and OX2R

            A major metabolite of lemborexant, M10, binds with comparable affinity as the parent drug to orexin receptors OX1R and OX2R

            Absorption

            Peak plasma concentration: 1-3 hr

            Food (high-fat, high-calorie meal) decreases peak plasma concentration by 23%, AUC by 18%, and delays peak plasma time by 2 hr

            Distribution

            Protein bound: ~94%

            Vd: 1970 L

            Blood-plasma ratio: 0.65

            Metabolism

            CYP3A4 (primary); CYP3A5 (less extent)

            Major circulating metabolite: M10

            Elimination

            Half-life: 17 hr (5 mg); 19 hr (10 mg)

            Excretion: Feces 29.1%; urine <1%

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            Administration

            Oral Administration

            Time to sleep onset may be delayed if taken with or soon after a meal

            Take at least 7 hr before planned awakening

            Do not take more than 1 dose/night

            Avoid alcohol consumption

            Storage

            Store at controlled room temperature of 20-25ºC (68-77ºF); excursions permitted to 15-30ºC (59-86ºF)

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            Formulary

            FormularyPatient Discounts

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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
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            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
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            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.