Lemborexant (Dayvigo) - Eisai's Insomnia Drug - has recently been approved for the treatment of insomnia. It is indicated in patients having difficulty falling asleep or maintaining sleep at night.
Lemborexant (Dayvigo) Dose in Adults
Lemborexant (Dayvigo) Dose in the treatment of Insomnia:
- 5 mg orally once a day at bedtime with at least seven hours of sleep (before the planned time of awakening).
- The dose may be increased as indicated to a maximum dose of 10 mg/day.
Dosage adjustment for concomitant therapy:
- When taken with Weak CYP3A inhibitors such as chlorzoxazone or ranitidine, the maximum dose should not exceed 5 mg/day.
Lemborexant (Dayvigo) Dose in Childrens:
It is not recommended for use in children.
Pregnancy Risk Factor: Undetermined
- It has not yet been tested in pregnant women.
- In some animal studies, adverse fetal outcomes have been observed.
Use while breastfeeding
- It is unknown if the drug will be excreted into breastmilk.
- Manufacturer recommends that you monitor your infant for sedation, and weigh the benefits and risks of treatment.
Lemborexant (Dayvigo) Dosage in Renal disease:
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Mild to moderate renal impairment
- Dose adjustment is not important.
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Grave renal impairment
- It is not necessary to adjust the dose.
- Patients with significant renal impairment are more likely to have somnolence as a result of increased medication exposure.
Lemborexant (Dayvigo) dosage in liver disease:
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Mild impairment
- Dose adjustment is not important.
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Moderate impairment
- Maximum daily intake should not exceed 5mg.
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Severe impairment
- It should not be used if you have severe hepatic impairment.
- It has not been tested in severe liver disease.
Side Effects of Lemborexant (Dayvigo):
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Central nervous system:
- Drowsiness
- Fatigue
- Headache
- Abnormal dreams
- Nightmares
- Sleep paralysis
Uncommon side effects of Lemborexant (dayvigo):
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Cardiovascular:
- Palpitations
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Central nervous system:
- Cataplexy
- Central nervous system depression
Contraindication to Lemborexant (Dayvigo) Include:
- Narcolepsy.
Warnings and precautions
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Depression in the CNS:
- It can cause CNS depression, which may lead to impairment of day-to-day physical activities.
- Before initiating treatment, individuals who engage in activities that require mental alertness (e.g. driving or operating heavy machinery) must be warned.
- Some patients may experience somnolence the next day or continue to feel the effects for several days.
- You should administer it to people who can stay in bed for at most seven hours following its intake.
- Avoid using alcohol and other CNS depressant medication together.
- Concomitant CNS depressions can increase the risk of daytime sleepiness. Patients may be given a higher dose or slept for less than seven hours.
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Falls
- It can cause sleepiness and increase the risk of falling, particularly in older patients.
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Rapid eye movement (REM), sleep effects
- Some patients may experience sleep paralysis, mild cataplexy, or hypnagogic/hypnopompic hallucinations.
- Cataplexy refers to the short episodes of weakness in the legs that last from seconds to a few moments.
- It can happen at night as well as during the day and may be associated with an event like laughter or surprise.
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Activities that are sleep-related:
- It has been linked to sleep-related dangerous activities.
- These dangerous activities include sleepingwalking, driving, sleeping, cooking, eating and making phone calls.
- These events are often forgotten by patients.
- They may also occur in the recommended dosages, with or without the concomitant use alcohol or other CNS-depressant drugs.
- Patients who have such symptoms should stop taking the drug.
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Depression
- Patients suffering from depression should be cautious.
- Monitor patients for depressive symptoms and suicidal thoughts.
- Depressed patients are at high risk for drug overdose.
- These patients should only receive the minimum dose.
- Prescriptions for these patients should be limited to the lowest amount possible, consistent with good patient care.
-
Use of drugs:
- Patients who have a history or addiction to drugs should be cautious when using the drug.
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Hepatic impairment
- This drug has not been tested in patients suffering from liver disease.
-
Respiratory disease
- Patients suffering from chronic respiratory conditions should be cautious when taking the drug.
- Patients suffering from sleep apnea or COPD and other chronic lung conditions can develop respiratory failure.
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Alizapride |
May enhance the CNS depressant effect of CNS Depressants. |
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Brimonidine (Topical) |
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Bromopride |
May enhance the CNS depressant effect of CNS Depressants. |
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Cannabidiol |
May enhance the CNS depressant effect of CNS Depressants. |
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Cannabis |
May enhance the CNS depressant effect of CNS Depressants. |
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Chlorphenesin Carbamate |
May enhance the adverse/toxic effect of CNS Depressants. |
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Clofazimine |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
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Deferasirox |
May lower the serum level of CYP3A4 substrates (High risk with Inducers). |
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Dimethindene (Topical) |
CNS depressants may have an enhanced CNS depressant impact. |
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Dronabinol |
May enhance the CNS depressant effect of CNS Depressants. |
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Erdafitinib |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
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Erdafitinib |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
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Ivosidenib |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
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Kava Kava |
May enhance the adverse/toxic effect of CNS Depressants. |
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Lofexidine |
CNS depressants may have an enhanced CNS depressant impact. Management: Separate drug interaction monographs go into further detail about the medications indicated as exceptions to this book. |
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Magnesium Sulfate |
CNS depressants may have an enhanced CNS depressant impact. |
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Melatonin |
May intensify hypnotics' sedative effects (Nonbenzodiazepine). |
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MetyroSINE |
CNS depressants may have an enhanced CNS depressant impact. |
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Minocycline (Systemic) |
CNS depressants may have an enhanced CNS depressant impact. |
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Nabilone |
CNS depressants may have an enhanced CNS depressant impact. |
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Piribedil |
CNS depressants may have an enhanced CNS depressant impact. |
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Pramipexole |
CNS depressants may have an enhanced CNS depressant impact. |
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ROPINIRole |
CNS Depressants may enhance the sedative effect of ROPINIRole. |
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Rotigotine |
CNS Depressants may enhance the sedative effect of Rotigotine. |
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Rufinamide |
May enhance the adverse/toxic effect of CNS Depressants. Specifically, sleepiness and dizziness may be enhanced. |
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Sarilumab |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
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Selective Serotonin Reuptake Inhibitors |
CNS Depressants may enhance the adverse/toxic effect of Selective Serotonin Reuptake Inhibitors. Specifically, the risk of psychomotor impairment may be enhanced. |
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Siltuximab |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
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Simeprevir |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
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Tetrahydrocannabinol |
May enhance the CNS depressant effect of CNS Depressants. |
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Tetrahydrocannabinol and Cannabidiol |
May enhance the CNS depressant effect of CNS Depressants. |
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Tocilizumab |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
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Risk Factor D (Consider therapy modification) |
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Blonanserin |
CNS Depressants may enhance the CNS depressant effect of Blonanserin. |
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Buprenorphine |
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Chlormethiazole |
May enhance the CNS depressant effect 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. |
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CNS Depressants |
Lemborexant may make CNS depressants more effective at lowering blood pressure. Management: Due to the possibility of additive CNS depressant effects when lemborexant and concurrent CNS depressants are administered concurrently, dosage modifications may be required. Effects of CNS depressants must be closely monitored. |
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CYP3A4 Inhibitors (Weak) |
Lemborexant serum concentration can rise. Management: When used in conjunction with weak CYP3A4 inhibitors, a maximum daily dose of 5 mg of lemborexant is advised. |
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Droperidol |
May enhance the CNS depressant effect of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (eg, opioids, barbiturates) with concomitant use. Exceptions to this monograph are discussed in further detail in separate drug interaction monographs. |
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Flunitrazepam |
CNS Depressants may enhance the CNS depressant effect of Flunitrazepam. |
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HYDROcodone |
The CNS depressive action of HYDROcodone may be enhanced by CNS depressants. Management: Whenever feasible, refrain from using hydrocodone and benzodiazepines or other CNS depressants concurrently. Only in the event that other treatment choices are insufficient should these medications be combined. Limit the duration and dosage of each medicine when used together. |
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Methotrimeprazine |
The CNS depressing action of methotrimeprazine may be enhanced by CNS depressants. The CNS depressant action of CNS Depressants may be strengthened by methotrimeprazine. Management: Start concurrent methotrimeprazine therapy while reducing the adult dose of CNS depressants by 50%. Only once a clinically effective dose of methotrimeprazine has been established should additional CNS depressant dosage modifications be made. |
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OxyCODONE |
CNS Depressants may enhance the CNS depressant effect 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. |
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Perampanel |
May enhance the CNS depressant effect of CNS Depressants. Management: Patients taking perampanel with any other drug that has CNS depressant activities should avoid complex and high-risk activities, particularly those such as driving that require alertness and coordination, until they have experience using the combination. |
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Stiripentol |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Use of stiripentol with CYP3A4 substrates that are considered to have a narrow therapeutic index should be avoided due to the increased risk for adverse effects and toxicity. Any CYP3A4 substrate used with stiripentol requires closer monitoring. |
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Suvorexant |
CNS Depressants may enhance the CNS depressant effect 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. |
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Tapentadol |
May enhance the CNS depressant effect of CNS Depressants. Management: Avoid concomitant use of tapentadol 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. |
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Zolpidem |
CNS Depressants may enhance the CNS depressant effect 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. |
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Risk Factor X (Avoid combination) |
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Alcohol (Ethyl) |
May enhance the CNS depressant effect of Lemborexant. Alcohol (Ethyl) may increase the serum concentration of Lemborexant. |
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Azelastine (Nasal) |
CNS Depressants may enhance the CNS depressant effect of Azelastine (Nasal). |
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Bromperidol |
May enhance the CNS depressant effect of CNS Depressants. |
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Conivaptan |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
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CYP3A4 Inducers (Moderate) |
Lemborexant's serum concentration can drop. |
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CYP3A4 Inducers (Strong) |
Lemborexant's serum concentration can drop. |
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CYP3A4 Inhibitors (Moderate) |
Lemborexant's serum concentration can drop. |
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CYP3A4 Inhibitors (Strong) |
Lemborexant's serum concentration can drop. |
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Fusidic Acid (Systemic) |
May elevate CYP3A4 substrates' serum concentration (High risk with Inhibitors). |
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Idelalisib |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
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Orphenadrine |
CNS Depressants may enhance the CNS depressant effect of Orphenadrine. |
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Oxomemazine |
May enhance the CNS depressant effect of CNS Depressants. |
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Paraldehyde |
CNS Depressants may enhance the CNS depressant effect of Paraldehyde. |
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Sodium Oxybate |
Hypnotics (Nonbenzodiazepine) may intensify Sodium Oxybate's CNS depressive effects. |
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Thalidomide |
The CNS depressing effect of thalidomide may be enhanced by CNS depressants. |
Monitor:
- Liver and renal functions at baseline and as clinically indicated.
- Monitor for depression and suicidal thoughts and suicidal tendencies.
How to administer Lemborexant (Dayvigo)?
- You should take it orally at bedtime, at least seven hours before your planned time of awakening.
- If the drug is taken immediately after or with a meal, it may delay the onset of action and sleep onset.
Mechanism of action of Lemborexant (Dayvigo):
It prevents the binding of wake-promoting neuropeptides, orexin A orexin B to receptors OX1R or OX2R. This is believed to suppress wake drive.
It has beenThe beginning of actionAbout 15 to 20 minutesAbsorptionThe drug's absorption is delayed by 2 hours due to high fat meals. About 94% is from the drug.Protein-bound. It is primarilyMetabolizedCYP3A4 and, to a lesser degree, CYP3A5 to the major circulating active metabolite of M10. It has been aEliminating half-lifeIt takes between 17 and 19 hours. Time taken to get therePeak serum concentrationIt takes between 1 and 3 hours. It isExcretedIt is found primarily in the feces (57%), and urine (29%).
Lemborexant Brand Name (International):
- Dayvigo
Lemborexant Brand Names in Pakistan:
It is not available in Pakistan.
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