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:

  • The therapy of insomnia is advised.

Eszopiclone (Lunesta) Dose in Adults

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

Note: Use the lowest effective dose.

• Initial dose:
  • 1 mg taken orally just before going to bed.
  • If necessary or recommended, the dose may be increased to 2 mg or 3 mg, with a daily maximum of 3 mg.

• Debilitated patients:

  • Initial dose: A dose of 1 mg given right before night, up to a maximum of 2 mg.

• Concurrent use with strong CYP3A4 inhibitor:

  • Initial dose: A dose of 1 mg given right before night, up to a maximum 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.
• Due to its quick onset of action, it should be consumed right before bedtime or given to a patient who is already in bed but is having trouble 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 undergoes oxidation and demethylation in the liver (CYP2E1, 3A4) to be broken down.
• The (S)-N-desmethyl metabolite of zopiclone is less powerful than the original substance.

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: