Eszopiclone (Lunesta) is a non-benzodiazepine hypnotic drug. It is a prescription sleeping pill that is used to fall asleep faster, increase the sleep time, and reduce sleep interruptions.

Eszopiclone (Lunesta) Uses:

• Insomnia:

  • It is indicated for the treatment of insomnia.

Eszopiclone (Lunesta) Dose in Adults

Eszopiclone (Lunesta) Dose in the treatment of Insomnia: Oral:

Note: Use the lowest effective dose.

• Initial dose:
  • 1 mg administered orally immediately before bedtime.
  • The dose may be increased to 2 mg or 3 mg if indicated/ required to a maximum dose of 3 mg daily.

• Debilitated patients:

  • Initial dose: 1 mg administered immediately before bedtime to a maximum dose of 2 mg.

• Concurrent use with strong CYP3A4 inhibitor:

  • Initial dose: 1 mg administered immediately before bedtime to a maximum dose of 2 mg.

Dose in Children:

Not indicated.

Eszopiclone (Lunesta) Pregnancy Risk Category: C

• Es-zopiclone, the S-isomer for the racemic derivative of zopiclone, is called Es-zopiclone.
• Although data is not available, it is possible that similar drugs may cause preterm births, low birth weights, and/or small gestational ages in infants who have been exposed to hypnotic drugs by their mothers.
• Pregnancy should not be prolonged and the drug should be stopped immediately to prevent rebound insomnia.

Use of eszopiclone during breastfeeding

• It is unknown if the drug will be excreted into breast milk.
• Zopiclone can be excreted from breastmilk.
• Manufacturers recommend weighing the risks to the infant's health and the benefits for the mother when treating them.

Lunesta Dose in Kidney Disease:

Adjustment in the dose is not necessary.

Lunesta Dose in Liver disease:

• Mild to moderate impairment:

  • Adjustment in the dose is not necessary.

• Severe impairment:

  • 1 mg immediately before bedtime initially to a maximum dose of 2 mg.
  • Since systemic exposure is increased in severe hepatic impairment, it should be used with caution.

Common Side Effects of Eszopiclone (Lunesta):

• Central Nervous System:

  • Headache

• Gastrointestinal:

  • Dysgeusia

Less Common Side Effects Of Eszopiclone (Lunesta):

• Cardiovascular:

  • Chest Pain
  • Peripheral Edema

• Central Nervous System:

  • Drowsiness
  • Dizziness
  • Pain
  • Nervousness
  • Depression
  • Confusion
  • Neuralgia
  • Abnormal Dreams
  • Anxiety
  • Hallucination
  • Migraine

• Dermatologic:

  • Skin Rash
  • Pruritus

• Endocrine & Metabolic:

  • Decreased Libido
  • Gynecomastia

• Gastrointestinal:

  • Xerostomia
  • Dyspepsia
  • Nausea
  • Diarrhea
  • Vomiting

• Genitourinary:

  • Dysmenorrhea
  • Urinary Tract Infection

• Infection:

  • Infection
  • Viral Infection

• Miscellaneous:

  • Accidental Injury

Contraindications to Eszopiclone (Lunesta):

Allergy reactions to eszopiclone and any component of the formulation

Warnings and precautions

• Abnormal thinking and behavior changes:

  • The unpredictable behavior changes caused by hypnotics or sedatives include abnormal thinking, inhibition, bizarre behavior and aggression.
  • These changes could indicate undiagnosed psychiatric disorders that should be assessed.

• Depression in the CNS:

  • Patients on high doses, such as over 2 mg, may experience impairments in daytime activities.
  • Patients taking 3 mg or more of the medication should be warned about activities that require mental alertness, such as heavy machinery operation.
  • If the patient took the drug, but got less than a full night of sleep (7 to 8 hours), there may be a risk of daytime psychomotor impairment.
  • Daytime psychomotor impairment can also be caused by a higher dose or co-administration of the drug with another CNS depressant drug or drugs that could raise its serum concentration.
  • If a CNS depressant drug has been used concurrently, it may be necessary to adjust the dosage.
  • Avoid using sedatives and hypnotics together.

• Hypersensitivity reactions

  • Anaphylaxis, angioedema and other allergic reactions may occur.
  • As fatal hypersensitivity reactions can occur, patients who have suffered severe allergic reactions should not be given the drug again.

• Activities that are sleep-related:

  • It is associated with an increased risk of sleeping-related hazardous activities like sleep walking, driving, cooking, making calls, and amnesia.
  • Concomitant alcohol consumption or use of other drugs that increase arousal could increase the likelihood of these activities.
  • Patients who report such activities must stop receiving treatment.

• Depression

  • Patients suffering from depression should be aware that the drug can cause serious side effects. Apnea may result from drug overdose.
  • This may lead to depression worsening and even suicidal thoughts being heightened.
  • To avoid overdose and dependence, doctors must prescribe the lowest effective dose for the least time.

• Use of drugs:

  • Patients who have a history or drug dependence should be closely monitored.

• Hepatic impairment

  • Patients with liver disease should not use it as it is metabolized by the liver.
  • Patients with severe hepatic impairment may need to adjust their dose.

• Respiratory disease

  • Patients with COPD, sleep apnea, or other chronic lung diseases should not use it.

Eszopiclone: Drug Interaction

Note: Drug Interaction Categories:

• Risk Factor C: Monitor When Using Combination
• Risk Factor D: Consider Treatment Modification
• Risk Factor X: Avoid Concomitant Use

Monitoring parameters:

None mentioned.

How to administer Eszopiclone (Lunesta)?

• The drug should not be taken following a high fat meal.
• Because of its rapid onset of action, it should be taken immediately before going to bed or it should be administered after the patient has been in the bed and is having difficulty falling asleep.

Mechanism of action of Eszopiclone (Lunesta):

Although the mechanism of action is still not known, it likely interacts with GABA receptors in the binding domains close to the benzodiazepine receptors.

Absorption:

• It is rapidly absorbed, however, fatty meals and heavy meals may delay its absorption.

Protein binding:

• 52% to 59% of the drug is protein-bound.

Metabolism:

• It is metabolized in the liver via oxidation and demethylation (CYP2E1, 3A4); .
• The (S)-N-desmethyl zopiclone metabolite is less potent than the parent compound

Half-life elimination:

• About 6 hours;
• In elderly (≥65 years), the half-life is prolonged to about 9 hours.

Time to peak, plasma:

• 1 hour

Excretion:

• Upt o75% is excreted in urine primarily as metabolites;
• <10% is excreted as parent drug

International Brands of Eszopiclone:

• Lunesta
• Eszop
• Fresom
• Fulnite
• Inductal
• Isoklon
• Lunesta
• Lunox 2
• Magicpiclone
• Nefor
• Neogaival
• Night Calm
• Noptic
• Orizon
• Sleepez
• Sleepil
• Sominex 1
• Sominex 2
• Sono
• Valnoc
• Wen Fei
• Zolnite

Eszopiclone Brand Names in Pakistan: