Eszopiclone
Pronouncation: (es-zoe-PIK-lone)Class: Sedative and hypnotic, nonbarbiturate
Trade Names:
Lunesta
- Tablets 1 mg
- Tablets 2 mg
- Tablets 3 mg
Pharmacology
Precise mechanism is unknown; however, binding with GABA-receptor complexes located close to or allosterically coupled to benzodiazepine receptors is suspected.
Pharmacokinetics
Absorption
Rapidly absorbed after oral administration, reaching C max within about 1 h.
Distribution
Weakly bound to plasma protein (52% to 59%).
Metabolism
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.
Elimination
Mean elimination t ½ 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.
Indications and Usage
Treatment of insomnia.
Contraindications
Standard considerations.
Dosage and Administration
AdultsPO Recommended starting dose is 2 mg immediately before bedtime. Swallow tablet whole and do not crush, chew, or break. Dosing can be initiated at or raised to 3 mg if clinically indicated.
ElderlyPO 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.
Severe Hepatic Function ImpairmentAdults
PO Recommended starting dose is 1 mg (max, 2 mg).
Coadministration with Potent CYP3A4 InhibitorAdults
PO Recommended starting dose is 1 mg. If needed, increase dose to 2 mg.
General Advice
Administer on an empty stomach. Administer with a snack if GI upset occurs. Administration after a high-fat meal may reduce effects on sleep.
Storage/Stability
Store tablets at controlled room temperature (59° to 86°F).
Drug Interactions
Drugs that induce CYP3A4 (eg, rifampin)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 and adverse reactions.
EthanolAdditive effects of psychomotor performance.
OlanzapinePharmacodynamic interaction may result a decrease in digit symbol substitutional test (DSST) scores.
Laboratory Test Interactions
None well documented.
Adverse Reactions
CNS
Headache (21%); somnolence (10%); dizziness (7%); nervousness (5%); depression (4%); anxiety, confusion, hallucinations, decreased libido, abnormal dreams, neuralgia (3%); migraine (at least 1%).
Dermatologic
Rash, pruritus (4%).
GI
Unpleasant taste (34%); dry mouth (7%); dyspepsia, nausea (5%); diarrhea (4%); vomiting (3%).
Genitourinary
Dysmenorrhea, gynecomastia, UTI (3%).
Respiratory
Respiratory infection (10%).
Miscellaneous
Pain (5%); accidental injury, viral infection (3%); chest pain, peripheral edema (at least 1%).
Precautions
MonitorBaseline symptomsIdentify baseline symptoms (difficulty falling asleep, nocturnal awakening, and/or early morning awakening) and monitor patient's response to therapy. Notify health care provider if symptoms do not improve or worsen. |
Pregnancy
Category C .
Lactation
Undetermined.
Children
Safety and efficacy not established.
Elderly
Subjects 65 yr of age and older had a 41% increase in total exposure (AUC) to and a slightly prolonged elimination of eszopiclone (t ½ about 9 h). In elderly patient, dose should be decreased to 1 mg (max, 2 mg).
Special Risk Patients
Use with caution in patients with compromised respiratory function, diseases, or conditions that could affect metabolism or hemodynamic responses.
Duration of therapy
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, ensure patient is periodically reevaluated to determine whether there is a continuing need for the medication.
Psychiatric or physical disorders
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.
Suicide
Supervise depressed patients at risk during therapy. Prescribe the smallest quantity consistent with good patient management in order to reduce the risk of overdose.
Withdrawal
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, tremor, muscle or abdominal cramps, sweating). If significant withdrawal symptoms develop, reinstitute previous dosing schedule and attempt a less rapid tapering regimen after patient has stabilized.
Overdosage
Symptoms
Exaggeration of pharmacologic effects, impairment of consciousness ranging from somnolence to coma and death.
Patient Information
- Advise patient to read the patient information leaflet before starting therapy and with each refill.
- Review lifestyle changes that may improve sleep (eg, quiet and dark environment, avoidance of caffeine and nicotine, warm water bath, relaxation techniques).
- Advise patient that medication is usually started at a low dose and then gradually increased until maximum benefit is obtained.
- Advise patient to take prescribed dose immediately before going to bed to reduce the risk of falling.
- Advise patient to take prescribed dose with a full glass of water and to swallow tablet whole and not to crush, chew, or break the tablet.
- Advise patient to take on an empty stomach but to take with food if stomach upset occurs. Caution patient not to take after a high-fat meal, because medication may not work as well.
- Caution patient not to take eszopiclone unless they will be able to get 8 h or more of sleep before being active again. Advise patient that taking eszopiclone with less than 8 h sleep may result in daytime amnesia or memory loss.
- Review safety precautions with regard to falls, especially for elderly and debilitated patients.
- Caution patient that medication may be habit forming and to take as prescribed and not to stop taking or change the dose unless advised by health care provider.
- Advise patient sleep may be disturbed for 1 or 2 nights following discontinuation of eszopiclone therapy.
- Advise patient that if medication needs to be discontinued after long-term use it will be slowly withdrawn unless safety concerns (eg, rash) require a more rapid withdrawal.
- Instruct patient to avoid alcoholic beverages and other depressants while taking this medication.
- Instruct patient to contact health care provider if symptoms do not appear to be getting better, worsen, or if bothersome adverse reactions (eg, daytime drowsiness, dizziness, incoordination, memory problems, changes in thinking or behavior) occur. Caution patient not to increase the dose on their own if symptoms do not appear to be improving.
- Advise patient to take sips of water, suck on ice chips or sugarless hard candy, or chew sugarless gum if dry mouth occurs.
- Advise patient that drug may cause drowsiness or impair judgment, thinking, or reflexes and to use caution while driving or performing other tasks requiring mental alertness until tolerance is determined.
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More Eszopiclone resources:
Eszopiclone - Includes detailed dosage instructions.
