Eszopiclone

What is Eszopiclone?

• Eszopiclone (Lunesta), is a nonbenzodiazepine hypnotic agent that is a pyrrolopyrazine derivative of the cyclopyrrolone class.

Eszopiclone

What are the uses of this medicine?

• Eszopiclone (Lunesta), is a sedative-hypnotic (sleep) medicine.
• Eszopiclone tablets are used in adults for the treatment of a sleep problem called insomnia.

How does this medicine work?

• Eszopiclone (es zoe' pi klone) is a non-benzodiazepine, benzodiazepine receptor agonist of the cyclopyrrolone class that acts by binding to the benzodiazepine (BZ) site on the GABA receptor complex, causing neural inhibition and helping to induce sleep.
• Eszopiclone has selectivity for certain BZ receptor subtypes, and does not have the neuromuscular relaxation or anticonvulsant effects of the standard benzodiazepines.
• Eszopiclone has a relatively short half life and rapid onset of action.
• In multiple placebo controlled trials, eszopiclone was shown to decrease the latency to onset of sleep and improve perceived sleep quality, with few next day residual effects and minimal evidence of rebound insomnia after withdrawal.
• Eszopiclone is the S-isomer of zopiclone that has been available in other countries for more than 20 years.

Eszopiclone-3D-balls

Who Should Not Use this medicine ?

This medicine cannot be used in patients:

• who are allergic to anything in it.

What drug interactions can this medicine cause?

Eszopiclone-3D-vdW

• Tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take.

Be sure to mention any of the following:

• antidepressants
• certain antifungals such as itraconazole (Onmel, Sporanox) and ketoconazole (Nizoral)
• antihistamines
• clarithromycin (Biaxin)
• certain HIV protease inhibitors such as nelfinavir (Viracept) and ritonavir (Norvir)
• medications for anxiety, mental illness, or seizures
• nefazodone
• olanzapine (Zyprexa)
• rifampin (Rifadin, Rimactane)
• sedatives
• other sleeping pills
• tranquilizers
• troleandomycin (TAO) (not available in the US)

Is this medicine FDA approved?

• Eszopiclone was approved for use in the United States in 2004 for the treatment of insomnia and remains in common use.
• In 2020, it was the 232nd most commonly prescribed medication in the United States, with more than 1 million prescriptions.

How should this medicine be used?

Recommended dosage: Dosage in Adults:

• The recommended starting dose is 1 mg.
• Dosing can be raised to 2 mg or 3 mg if clinically indicated.
• The total dose of eszopiclone tablets should not exceed 3 mg, once daily immediately before bedtime.

Geriatric or Debilitated Patients:

• The total dose of eszopiclone tablets should not exceed 2 mg in elderly or debilitated patients.

• Patients with Severe Hepatic Impairment, or Taking Potent CYP3A4 Inhibitors:
• In patients with severe hepatic impairment, or in patients coadministered eszopiclone tablets with potent CYP3A4 inhibitors, the total dose of eszopiclone tablets should not exceed 2 mg.

• Dosage adjustments may be necessary when eszopiclone tablets are combined with other CNS depressant drugs because of the potentially additive effects.
• Taking eszopiclone tablets with or immediately after a heavy, high-fat meal results in slower absorption and would be expected to reduce the effect of eszopiclone tablets on sleep latency.

Administration:

• Take eszopiclone tablets exactly as prescribed. Do not take more eszopiclone tablets than prescribed for you.
• Take eszopiclone tablets right before you get into bed.
• Do not take eszopiclone tablets with or right after a meal.
• Do not take eszopiclone tablets unless you are able to get a full night’s sleep before you must be active again.
• Call your doctor if your insomnia worsens or is not better within 7 to 10 days. This may mean that there is another condition causing your sleep problems.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Tablets: 1 mg, 2 mg and 3 mg.

This medicine is available in fallowing brand namesː

• Lunesta

What side effects can this medication cause?

The most common side effects of this medicine may include:

• unpleasant taste in mouth, dry mouth
• drowsiness
• dizziness
• headache
• symptoms of the common cold
• You may still feel drowsy the next day after taking eszopiclone tablets.

Less common, but serious side effects may include:

• sleepiness during the day
• not thinking clearly
• act strangely, confused, or upset
• getting out of bed while not being fully awake and do an activity that you do not know you are doing.
• abnormal thoughts and behavior
• memory loss
• anxiety
• severe allergic reactions

"sleep-walking" or doing other activities when you are asleep like:

• eating
• talking
• having sex
• driving a car

What special precautions should I follow?

• Eszopiclone can cause next-day impairment even when used as prescribed, and that this risk is increased if dosing instructions are not carefully followed. Caution patients taking the 3 mg dose against driving and other activities requiring complete mental alertness the day after use. Inform patients that impairment can be present despite feeling fully awake.
• Inform patients that severe anaphylactic and anaphylactoid reactions have occurred with eszopiclone. Describe the signs/symptoms of these reactions and advise patients to seek medical attention immediately if any of them occur.
• Instruct patients and their families that sedative hypnotics can cause abnormal thinking and behavior change, including "sleep driving" and other complex behaviors while not being fully awake (preparing and eating food, making phone calls, or having sex). Tell patients to call you immediately if they develop any of these symptoms.
• Tell patients to immediately report any suicidal thoughts.
• Ask patients about alcohol consumption, medicines they are taking, and drugs they may be taking without a prescription. Advise patients not to use eszopiclone if they drank alcohol that evening or before bed.
• Patients should be counseled to take eszopiclone right before they get into bed and only when they are able to stay in bed a full night (7–8 hours) before being active again. Eszopiclone tablets should not be taken with or immediately after a meal. Advise patients NOT to take eszopiclone if they drank alcohol that evening.
• Following rapid dose decrease or abrupt discontinuation of the use of sedative/hypnotics, there have been reports of signs and symptoms similar to those associated with withdrawal from other CNS-depressant drugs
• Eszopiclone has not been implicated in causing serum enzyme elevations or clinically apparent liver injury.
• It is not known whether this drug is excreted in human milk.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• Signs and symptoms of overdose effects of CNS depressants can be expected.
• drowsiness
• Impairment of consciousness ranging from somnolence to coma.

Management of overdosage:

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.
• General symptomatic and supportive measures should be used along with immediate gastric lavage where appropriate.
• Intravenous fluids should be administered as needed.
• Flumazenil may be useful.
• As in all cases of drug overdose, respiration, pulse, blood pressure and other appropriate signs should be monitored and general supportive measures employed.
• Hypotension and CNS depression should be monitored and treated by appropriate medical intervention.
• The value of dialysis in the treatment of overdosage has not been determined.
• As with the management of all overdosage, the possibility of multiple drug ingestion should be considered.

Can this medicine be used in pregnancy?

• Pregnancy Category C.
• There are no adequate and well controlled studies in pregnant women.
• Eszopiclone should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Can this medicine be used in children?

• Safety and effectiveness have not been established in pediatric patients.

What are the active and inactive ingredients in this medicine?

• Active Ingredient: eszopiclone.
• Inactive Ingredients: black iron oxide, colloidal silicon dioxide, croscarmellose sodium type A, hypromellose, lactose monohydrate, magnesium stearate, microcrystalline cellulose, polyethylene glycol, red iron oxide, titanium dioxide and yellow iron oxide.

Who manufactures and distributes this medicine?

Manufactured for:

• Mylan Pharmaceuticals Inc.
• Morgantown, WV U.S.A.

Manufactured in Australia by:

• ALPHAPHARM PTY LTD
• 15 Garnet Street
• Carole Park QLD
• Australia

Marketed/ Packaged by:

• GSMS, Inc.
• Camarillo, CA USA

What should I know about storage and disposal of this medication?

• Store eszopiclone tablets at 20° to 25°C (68° to 77°F).
• Do not use eszopiclone tablets after the expiration date.
• Keep eszopiclone tablets and all medicines out of reach of children.

Sedatives and Hypnotics

• Antihistamines
• Diphenhydramine
• Doxylamine
• Hydroxyzine

• Barbiturates
  • Amobarbital
  • Butabarbital
  • Phenobarbital
  • Secobarbital

• Benzodiazepines
  • Diazepam
  • Estazolam
  • Flurazepam
  • Quazepam
  • Temazepam
  • Triazolam

• Benzodiazepine Receptor Agonists
  • Eszopiclone
  • Zaleplon
  • Zolpidem

• Herbals
  • Chamomile (Matricaria recutita)
  • Hops (Humulus lupulus)
  • Lavender (Lavandula angustifolia)
  • Passionflower (Passiflora incarnata)
  • Valerian (Valeriana officinalis)

• Melatonin and its Analogues
  • Melatonin
  • Ramelteon
  • Tasimelteon

Miscellaneous Agents

• • Buspirone
  • Chloral hydrate
  • Doxepin
  • Meprobamate
  • Sodium Oxybate (Narcolepsy Agent)
  • Suvorexant

 

• Dailymed label info on Eszopiclone
• FDA Eszopiclone