Eszopiclone

Indications
Oral
Insomnia
Adult: Initial: 2 mg immediately before bedtime. If clinically indicated, may initiate treatment at or increase dosage to 3 mg immediately before bedtime.
Elderly: Difficulty falling asleep: Initial: 1 mg immediately before bedtime; may increase to 2 mg at bedtime if clinically indicated. Difficulty staying asleep: 2 mg immediately before bedtime. Dosages exceeding 2 mg daily are not recommended.
Hepatic impairment: Severe hepatic impairment: Initial: 1 mg immediately before bedtime. Dosages exceeding 2 mg daily are not recommended.
Warnings / Precautions
Initiate treatment only after careful evaluation of patients; failure of insomnia to remit after 7-10 days of treatment may indicate presence of primary psychiatric and/or medical illness requiring evaluation. May be associated with abnormal thoughts and behaviour changes e.g. bizarre behavior, agitation, hallucinations, depersonalization, decreased inhibition. Complex sleep-related behaviours with no memory of the incident such as "sleep-driving", preparing and eating food, making phone calls, having sex while not fully awake have been reported. Caution in patients with history of drug or alcohol dependence and/or abuse. Worsening of depression, emergence of suicidality have been reported. Eszopiclone has rapid onset of action and must be taken immediately before bedtime or after experiencing difficulty sleeping. May impair ability to drive or operate machinery. Hypersensitivity reaction including angioedema involving the tongue, glottis or larynx, and symptoms suggestive of anaphylaxis have been reported. Abrupt discontinuance or rapid dose reduction may cause withdrawal symptoms. Caution in hepatic impairment; elderly/debilitated patients. Safety and efficacy have not been established in children <18 yr. Pregnancy and lactation.
Adverse Reactions
Headache, dizziness, somnolence, nervousness, depression, confusion, hallucination, anxiety, abnormal dreams, pain, migraine, neuralgia, rash, pruritus, dry mouth, unpleasant taste, nausea, vomiting, diarrhoea, dyspepsia, peripheral oedema, chest pain, urinary tract infection, viral infection, dysmenorrhoea, gynecomastia, decreased libido, dyspnoea, agitation, and memory impairment.
Potentially Fatal: Anaphylaxis reactions, angioedema involving the tongue, glottis or larynx.
Overdose Reactions
Symptoms: Impairment of consciousness (somnolence, coma) has been described. Overdose may cause exaggeration of its pharmacological effects. Management: Usefulness of dialysis in the management of Eszopiclone overdose has not been evaluated. Provide immediate gastric lavage where appropriate along with symptomatic and supportive treatment. Flumazenil may be useful. Monitor for hypotension and CNS depression and provide appropriate medical intervention.
Drug Interactions
Concurrent use of CYP3A4 inhibitors (e.g. ketoconazole, itraconazole, clarithromycin, nefazodone, troleandomycin, ritonavir, nelfinavir) may decrease metabolism and increase plasma concentrations of Eszopiclone; dosage reduction of Eszopiclone may be needed. Concurrent use with CYP3A4 inducers (e.g. rifampicin) may reduce concentrations of Eszopiclone. May enhance adverse CNS effects when used with alcohol, anticonvulsants, antihistamines, or other psychotropic drugs. Concurrent use with flumazenil may diminish the sedative effect of nonbenzodiazepine hypnotics.
See Below for More eszopiclone Drug Interactions
Food Interactions
Avoid alcohol and St. John's wort. Sleep onset may be delayed if administered with or immediately after a high-fat meal.
Mechanism of Actions
Eszopiclone is an S-enantiomer of zopiclone; a nonbenzodiazepine hypnotic of the cyclopyrrolone class. It is structurally unrelated to pyrazolopyrimidines, imidazopyridines, benzodiazepines, barbiturates, or other known drugs with similar hypnotic activity. The exact mechanism of action is unknown, its effect is associated with the interaction with gamma-aminobutyric acid (GABA)-receptor complex at binding domains found near to or allosterically coupled to benzodiazepine receptors.
Absorption: Rapidly absorbed from GI tract following oral admin. Tmax: About 1 hr.
Distribution: Protein binding: About 52-59%.
Metabolism: Extensively metabolised by oxidation and demethylation via CYP3A4 and CYP2E1 enzymes.
Excretion: About 75% of an oral dose of racemic zopiclone is excreted in urine. <10% of oral Eszopiclone is excreted as parent drug. Terminal elimination half-life: About 6 hr.
Administration
Should be taken on an empty stomach. (Take immediately before going to bed. Avoid taking after a heavy meal.)
Storage Conditions
Oral: Store at 25°C (77°F); excursions permitted to 15-30°C (59-86°F).
ATC Classification
N05CF04 - eszopiclone ; Belongs to the class of benzodiazepine related drugs. Used as hypnotics and sedatives.
Storage
Oral: Store at 25°C (77°F); excursions permitted to 15-30°C (59-86°F).
Available As
  • Eszopiclone 1 mg
  • Eszopiclone 2 mg
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