Adult: For short-term management: Initially, 1 mg immediately before bedtime, may increase to 2 mg or 3 mg if clinically indicated. Use the lowest effective dose. Max: 3 mg immediately before bedtime. Elderly: Initially, 1 mg immediately before bedtime, may increase to 2 mg if clinically indicated. Use the lowest effective dose. Max: 2 mg immediately before bedtime.
Should be taken on an empty stomach. Take immediately before going to bed. Avoid taking after a heavy meal.
Contraindications
History of drug-induced complex sleep behaviours. Recommendations for contraindication may vary among countries and individual products (refer to specific product guidelines).
Special Precautions
Patient with concomitant disease or condition that may affect metabolism or haemodynamic responses; compromised respiratory function, COPD, or sleep apnoea; history of psychiatric disorder, alcohol or drug abuse; depression. Patients taking strong CYP3A4 inhibitors. Avoid abrupt withdrawal. Severe hepatic impairment. Elderly and debilitated patient. Pregnancy and lactation.
Adverse Reactions
Significant: Withdrawal symptoms (after abrupt discontinuation or rapid dose reduction), rebound insomnia (following discontinuation); anterograde amnesia; next-day psychomotor impairment (particularly in patients taking higher doses [2 mg or 3 mg] or higher than recommended dose, or with inadequate sleep [less than 7-8 hours]); abnormal thinking and behavioural changes (including decreased inhibition, bizarre behaviour, agitation, depersonalisation, hallucinations); increased risk of physical and psychological dependence or abuse. Cardiac disorders: Chest pain. Gastrointestinal disorders: Dysgeusia, dry mouth, diarrhoea, nausea, vomiting, dyspepsia. General disorders and administration site conditions: Pain. Infections and infestations: Viral infection. Metabolism and nutrition disorders: Peripheral oedema. Nervous system disorders: Headache, dizziness, drowsiness, migraine, neuralgia. Psychiatric disorders: Anxiety, nervousness, abnormal dreams. Renal and urinary disorders: UTI. Reproductive system and breast disorders: Decreased libido, dysmenorrhoea, gynaecomastia. Respiratory, thoracic and mediastinal disorders: Respiratory infection. Skin and subcutaneous tissue disorders: Rash, pruritus. Potentially Fatal: Complex sleep behaviours (e.g. sleepwalking, sleep-driving), worsening depression (including suicidal ideation and completed suicides). Rarely, anaphylaxis and angioedema (involving the tongue, glottis or larynx).
This drug may cause drowsiness, amnesia, impaired coordination and muscle function, if affected, do not drive or operate machinery.
Monitoring Parameters
Assess the potential causes of insomnia before starting treatment. Observe for excessive CNS depression, abnormal thinking, and behavioural changes. Re-evaluate patient if insomnia persists after 7-10 days of treatment.
Overdosage
Symptoms: CNS depression ranging from drowsiness to coma; methaemoglobinaemia. Management: Symptomatic and supportive treatment. Perform gastric lavage soon after ingestion. May use flumazenil as an antidote. Administer IV fluids as needed. Monitor respiration, pulse, blood pressure and other appropriate vital signs. Monitor and manage hypotension and CNS depression with appropriate medical intervention. Monitoring of methaemoglobin may be considered in cases of high dose overdosage.
Drug Interactions
Additive CNS depression with other CNS depressants (e.g. benzodiazepines, TCAs, sedatives and hypnotics). Increased exposure with strong CYP3A4 inhibitors (e.g. ketoconazole, itraconazole, clarithromycin, troleandomycin, nefazodone, ritonavir, nelfinavir). May decrease exposure with strong CYP3A4 inducers (e.g. rifampicin, carbamazepine, phenytoin). Potentially Fatal: Concomitant use with opioids may result in sedation, respiratory depression and coma.
Food Interaction
May delay onset of action with or immediately following a heavy, high-fat meal. May enhance sedative effect with alcohol; avoid concomitant use. May decrease exposure with St. John's wort.
Action
Description: Mechanism of Action: Eszopiclone, a non-benzodiazepine hypnotic agent, is the S-enantiomer of zopiclone. The exact mechanism of action is unknown; however, it is believed to affect the modulation of gamma-aminobutyric acid (GABA)-A receptor macromolecular complexes at binding domains located near or allosterically coupled to benzodiazepine receptors. Pharmacokinetics: Absorption: Rapidly absorbed from the gastrointestinal tract. Food may delay the onset of action, particularly with heavy, high-fat meals. Time to peak plasma concentration: Approx 1 hour. Distribution: Plasma protein binding: 52-59%. Metabolism: Extensively metabolised in the liver by CYP3A4 and CYP2E1 isoenzymes via oxidation and demethylation to primary plasma metabolites, (S)-zopiclone-N-oxide and (S)-N-desmethyl zopiclone, that have little or no activity. Excretion: Via urine (up to 75%, mainly as metabolites; <10% as unchanged drug). Elimination half-life: Approx 6 hours.
Chemical Structure
Eszopiclone Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 969472, Eszopiclone. https://pubchem.ncbi.nlm.nih.gov/compound/Eszopiclone. Accessed Mar. 22, 2024.
N05CF04 - eszopiclone ; Belongs to the class of benzodiazepine related drugs. Used as hypnotics and sedatives.
References
Anon. Eszopiclone. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 04/03/2024.Anon. Eszopiclone. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 04/03/2024.Buckingham R (ed). Eszopiclone. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/03/2024.Eszopiclone. Gold Standard Drug Database in ClinicalKey [online]. Elsevier Inc. https://www.clinicalkey.com. Accessed 04/03/2024.Lunesta Tablet, Coated (Sumitomo Pharma America, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 04/03/2024.Lunesta Tablets (Sunovion Pharmaceuticals, Inc.). U.S. FDA. https://www.fda.gov. Accessed 04/03/2024.Lunivia 3 mg Film-coated Tablets (Axunio Pharma GmbH). MHRA. https://products.mhra.gov.uk. Accessed 04/03/2024.
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