Trade Names:Lunesta- Tablets 1 mg- Tablets 2 mg- Tablets 3 mg
Precise mechanism is unknown; however, binding with GABA-receptor complexes located close to or allosterically coupled to benzodiazepine receptors is suspected.
Rapidly absorbed after oral administration, reaching C max within about 1 h.
Weakly bound to plasma protein (52% to 59%).
Extensively metabolized by oxidation and demethylation. One metabolite, (S)-N-desmethyl zopiclone, binds to GABA receptors with substantially lower potency than the parent drug. The CYP2E1 and CYP3A4 isozymes are involved with eszopiclone metabolism.
Mean elimination half-life is 6 h. Up to 75% is excreted in the urine, mainly as metabolites, and less than 10% is excreted in the urine as the parent drug.
Because less than 10% of the orally administered dose is excreted in the urine, no dose adjustment is needed in patients with renal function impairment.Hepatic Function Impairment
Use with caution in patients with hepatic function impairment. No dosage adjustment is needed in patients with mild to moderate hepatic function impairment. The dose should not exceed 2 mg in patients with severe hepatic function impairment.Elderly
Subjects 65 yr of age and older had a 41% increase in total exposure (AUC) to and a slightly prolonged elimination of eszopiclone (half-life about 9 h).
Treatment of insomnia.
PO Recommended starting dose is 2 mg immediately before bedtime. Dosing can be initiated at or raised to 3 mg if clinically indicated.Elderly
PO For elderly patients whose primary complaint is difficulty falling asleep, the recommended starting dose is 1 mg immediately before bedtime. For elderly patients whose primary complaint is difficulty staying asleep, the recommended starting dose is 2 mg immediately before bedtime.Coadministration with CYP3A4 InhibitorAdults
PO Recommended starting dose is 1 mg. If needed, increase dose to 2 mg.Severe Hepatic Function ImpairmentAdults
PO Recommended starting dose is 1 mg (max, 2 mg).
Administer on an empty stomach. Administer with a snack if GI upset occurs. Administration after a high-fat meal may reduce effects on sleep. Administer immediately before bedtime.
Store tablets at 59° to 86°F.
Eszopiclone plasma concentrations may be reduced, decreasing the pharmacologic effects.Drugs that inhibit CYP3A4 (eg, clarithromycin, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir)
Eszopiclone plasma concentrations may be elevated, increasing the pharmacologic effects and adverse reactions.Ethanol
Additive effects on psychomotor performance.Olanzapine
Pharmacodynamic interaction may result in a decrease in digit symbol substitutional test scores.
None well documented.
Headache (21%); somnolence (10%); dizziness (7%); nervousness (5%); depression (4%); abnormal dreams, anxiety, confusion, decreased libido, hallucinations, neuralgia (3%); migraine (at least 1%).
Pruritus, rash (4%).
Unpleasant taste (34%); dry mouth (7%); dyspepsia (6%); nausea (5%); diarrhea (4%); vomiting (3%).
Dysmenorrhea, gynecomastia, UTI (3%).
Respiratory infection (10%).
Pain (5%); accidental injury, viral infection (3%); chest pain, peripheral edema (at least 1%).
Identify baseline symptoms (difficulty falling asleep, nocturnal awakening, and/or early morning awakening) and monitor patient's response to therapy.
Category C .
Safety and efficacy not established.
In elderly patients, decrease dose to 1 mg (max, 2 mg).
Use with caution in patients with concomitant illness, compromised respiratory function, signs and symptoms of depression, diseases, or conditions that could affect metabolism or hemodynamic responses.
Angioedema involving the tongue, glottis, or larynx have been reported.
Behavioral actions, including preparing and eating food, making phone calls, having sex, and sleep-driving, have been performed by patients who are not fully awake. Patients often have no memory of the event.
Eszopiclone is indicated for short-term (eg, 7 to 10 days) treatment of insomnia. If medication is used for more than 2 to 3 wk, periodically reevaluate patient determine whether there is a continuing need for the medication.
Worsening of insomnia or emergence of new thinking or behavior abnormalities may be the consequence of unrecognized psychiatric or physical disorders and requires immediate evaluation.
Supervise depressed patients at risk during therapy. Prescribe the smallest quantity consistent with good patient management in order to reduce the risk of overdose.
If treatment is to be discontinued or the dose reduced after long-term treatment, gradually taper the dose. Monitor patient for withdrawal symptoms (eg, increased anxiety, muscle or abdominal cramps, sweating, tremor). If withdrawal symptoms develop, reinstitute previous dosing schedule and attempt a less rapid tapering regimen after patient has stabilized.
Exaggeration of pharmacologic effects, impairment of consciousness ranging from somnolence to coma, and death.
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