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Dayvigo (Lemborexant): Uses, Dose, MOA, Side Effects

Dayvigo (Lemborexant)

Drug Name: Lemborexant

Brand Name: Dayvigo

FDA Approval Date: 23rd December 2019 [Ref]

Manufacturer: Eisai and Imbrium Therapeutics.

Primary Indication: Insomnia

Lemborexant (Dayvigo) is a drug that induces sleep via mechanisms different from benzodiazepines. It acts by inhibiting the Orexin receptor pathway. Other medications in the same class of drugs include:

Lemborexant (Dayvigo) Uses:

Lemborexant is a sleeping pill, a hypnotic drug, that is indicated for the treatment of adults with sleeping problems such as difficulty falling asleep or maintaining a sound sleep overnight.

It shouldn’t be prescribed to children, those with advanced liver disease, and in combination with other sleeping pills, or even for daytime siesta.

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Lemborexant (Dayvigo) Dose:

The usual dose of Lemborexant is 5 mg at bedtime or within 30 minutes of going to bed. The dose may be increased to 10 mg if no effect is seen with 5 mg.

It is recommended to take the drug only once every night. Taking Lemborexant with meals may delay its onset of action, hence, it is best to take it 2 hours after the night meal.

Dayvigo dose adjustment in various conditions:

Lemborexant is metabolized by hepatic CYP3A4 enzymes which also metabolize other drugs. Thus, the concentration of Lemborexant may be altered when it is used in combination with other medications which are also metabolized by the CYP3A4 pathway.

Avoid Lemborexant with strong or moderate CYP3A4 inducers or inhibitors:

Avoid with Strong CYP3A4 inhibitors

Avoid with Strong CYP3A4 inducers

  • Ketoconazole
  • Itraconazole
  • Clarithromycin
  • Telithromycin
  • Ritonavir
  • Indinavir
  • Nelfinavir
  • Atazanavir
  • Conivaptan
  • Grapefruit juice
  • Rifampin
  • Carbamazepine
  • Phenobarbital
  • Phenytoin
  • Modafinil
  • Nevirapine
  • Efavirenz

Avoid with Moderate CYP3A4 inhibitors

Avoid with Moderate CYP3A4 inducers

  • Fluconazole
  • Erythromycin
  • Diltiazem
  • Verapamil
  • Amiodarone
  • Bosentan
  • Rifabutin
  • Efavirenz
  • St. John’s wort

Use with weak CYP3 inhibitors:

Use lower doses of 5 mg per day in patients on concomitant weak CYP3A4 inhibitors such as:

  • Fluoxetine
  • Sertraline
  • Cimetidine
  • Ranitidine
  • Diphenhydramine
  • Chlorpheniramine

Dose adjustment in liver disease:

Lemborexant is not recommended for use in patients with severe hepatic impairment. In moderate hepatic impairment, a lower dose of 5 mg may be used.

Dose adjustment in kidney disease:

No adjustment in the dose is necessary.

Use in pregnancy and breastfeeding:

Data is limited in pregnant and lactating mothers. Any exposure to Lemborexant during pregnancy should be reported.

If Lemborexant is used in breastfeeding women, the child should be monitored for excessive sleepiness.

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Lemborexant (Dayvigo) Contraindications and Warnings:

It should not be used in individuals with Narcolepsy, a  condition characterized by daytime sleepiness.

  • CNS depressant effects:

Daytime sleepiness is a side effect of Dayvigo. Patients may develop drowsiness while at work. It is recommended that patients should be advised to avoid performing tasks that require mental alertness such as operating heavy machinery or driving.

Daytime sleepiness may be more marked in patients who are on other concomitant medications such as benzodiazepines or are taking alcohol. The concomitant use of Lemborexant with other CNS depressants should be avoided.

  • Suicidal thoughts and Depression:

Orexin inhibitors including Dayvigo block centers in the brain responsible for mood and excitation. It has been noted that patients using Dayvigo may develop worsening symptoms of depression or develop a new onset of depression.

Sometimes, depression is severe and associated with suicidal thoughts and ideas in which case, the drug should be stopped.

  • Paralysis and cataplexy:

Cataplexy is a sudden onset of brief muscular weakness. It may occur with Dayvigo treatment at any point in time and may not be predictable.

The cataplexy and transient paralysis have also been observed with other medications belonging to Orexin inhibitors.

  • Complex sleeping behaviors:

Dayvigo use may result in complex sleeping behaviors such as walking, making phone calls, or having sex while asleep. There have been reports of gambling and criminal activities too in patients with complex sleeping behaviors.

Patients usually do not recall these behaviors. In addition, some patients may develop these complex sleep behaviors after one or two doses while others may develop these after prolonged use.

The treatment should be stopped if a person is suspected to have developed these behaviors.

  • Sleep apnea:

Hypnotics and drugs that induce sleep including Dayvigo should be avoided in patients who have chronic lung-related comorbid conditions such as ILD, uncontrolled asthma, and sleep apnea.

There is an increased risk of respiratory depression with these drugs.

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Dayvigo Side Effects:

In clinical trials, the following side effects were commonly observed:

CNS-related side effects:

  • Somnolence or excessive daytime sleepiness
  • Headache
  • Fatigue, sluggishness, and lethargy
  • Sleepiness and sedation
  • Dizziness
  • Hallucinations
  • Nightmares
  • Abnormal dreams

GI side effects:

  • Nausea and vomiting

Other rare side effects included sleepwalking and complex sleep behaviors.

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Lemborexant (Dayvigo) Mechanism of Action (MOA):

Lemborexant blocks the neuronal signals executed by the Orexin neuropeptides. It blocks the binding of Orexin A and Orexin B to its receptors, OX1R and OX2R.

The Orexin Neuronal pathways mediate multiple processes, including:

  • Sleep-awake cycles
  • Reward
  • Mood
  • Energy consumption, and
  • Feeding Behaviors [Ref]

By blocking Orexin receptors, Dayvigo induces sleep, apart from other effects which may include weight gain.

Effect on QT interval: It has no effect on the QT interval when used in the recommended doses.

Co-administration with Alcohol: Alcohol may exacerbate daytime sleepiness, falls, posture instability, and memory impairment when given with hypnotics including Dayvigo.

Maximum Plasma Concentration: 1 – 3 hours of administration

Protein binding: 94%

Effect of high-calorie and high-fat food on its absorption: Absorption of Dayvigo is delayed by about 2 hours.

Metabolism: Extensively metabolized by CYP3A4 and to some extent by CYP3A5 enzyme pathways.

Excretion: 57.4% via feces, 29.1% via urine

Half-life elimination: 17 and 19 hours for 5 mg and 10 mg respectively

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Written by Dr. Ahmed

I am Dr. Ahmed (MBBS; FCPS Medicine), an Internist and a practicing physician. I am in the medical field for over fifteen years working in one of the busiest hospitals and writing medical posts for over 5 years.

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