ESZOPICLONE
| Eszopiclone (es-zo'pi-clone) Lunesta Classifications: sedative-hypnotic; anxiolytic; Therapeutic:sedative-hypnotic Pregnancy Category: C Controlled Substance: Schedule IV |
Availability
1 mg, 2 mg, 3 mg tablets
Action
Eszopiclone is a nonbenzodiazepine sedative-hypnotic agent. The precise mechanism of action is unknown but believed to result from its interaction with GABA-receptor complexes at binding sites close to or coupled to benzodiazepine receptors in the brain.
Therapeutic Effect
Improves sleep maintenance in transient insomnia.
Uses
Treatment of insomnia.
Contraindications
Hypersensitivity to eszopiclone; concurrent administration with CYP3A4 inhibitor drugs; alcohol intoxication; alcoholism; children <18 y; suicidal tendencies or ideation; pregnancy (category C).
Cautious Use
Hepatic impairment; elderly or debilitated patients; concurrent administration of CNS DEPRESSANTS; signs and symptoms of depression; COPD; lactation.
Route & Dosage
| Insomnia Adult: PO 2–3 mg h.s. Geriatric: PO 1–2 mg h.s. Severe Hepatic Impairment PO ≤2 mg |
Administration
Oral- Give immediately prior to bedtime.
- Store at 15°–30° C (59°– 86° F).
Adverse Effects (≥1%)
CNS: Anxiety, confusion, depression, dizziness, hallucinations, headache, irritability, decreased libido, nervousness, somnolence. CV: Tachycardia, pericardial infusion, left ventricular systolic dysfunction (LVSD). GI: Dry mouth, dyspepsia, nausea, vomiting. GU: Dysmenorrhea, gynecomastia. Respiratory: Infection. Skin: Rash, pruritus. Special Senses: Unpleasant taste.Interactions
Drug: Inhibitors of CYP3A4, including (but not limited to) amiodarone, antiretroviral protease inhibitors, aprepitant, clarithromycin, dalfopristin/quinupristin, delavirdine, diltiazem, efavirenz (inducer or inhibitor), erythromycin, fluconazole, fluoxetine, fluvoxamine, itraconazole, ketoconazole, mifepristone, nefazodone, norfloxacin, other systemic azole antifungals (miconazole and voriconazole), troleandomycin, and zafirlukast increase eszopiclone levels. Ethanol and other cns depressant agents can produce additive effects in combination with eszopiclone. Herbal: St. John's wort can increase eszopiclone levels.Pharmacokinetics
Absorption: Rapidly absorbed from GI tract. Distribution: 52–59% protein bound. Peak: 1 h. Metabolism: Extensive hepatic metabolism. Elimination: Primarily in the urine. Half-Life: 5–6 h.Nursing Implications
Assessment & Drug Effects
- Monitor for and report worsening insomnia and cognitive or behavioral changes.
- Monitor for suicidal ideation in depressive patients.
- Monitor for S&S of CNS depression when other CNS DEPRESSANTS are used concurrently.
- Supervise ambulation if patient is out of bed after taking eszopiclone.
Patient & Family Education
- Follow directions for taking the drug (see Administration).
- Do not take this drug unless you can get at least 8 h of sleep.
- Do not consume alcohol while taking this drug.
- Do not take with or immediately after a high fat meal.
- Do not drive or engage in potentially hazardous activities until response to drug is known.
- Report any of the following to a health care provider: worsening insomnia, cognitive or behavioral changes, problem with reproductive function.
Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; 
Canadian drug name; 
Prototype drug