Drug Guide
Eszopiclone
Classification
Therapeutic: Sedative/hypnotic for insomnia
Pharmacological: Non-benzodiazepine hypnotic (Z-drug)
FDA Approved Indications
- Treatment of insomnia characterized by difficulty with sleep onset, sleep maintenance, or both.
Mechanism of Action
Eszopiclone works by binding to the GABA-A receptor complex, enhancing GABAergic inhibitory effects, which results in sedation and sleep induction.
Dosage and Administration
Adult: Initial dose: 2 mg at bedtime. Can be increased to 3 mg after 2 weeks if needed, up to a maximum of 3 mg.
Pediatric: Not approved for pediatric use.
Geriatric: Start with 1-2 mg at bedtime due to increased sensitivity; dose adjustments as needed.
Renal Impairment: Use with caution; consider starting at lower doses.
Hepatic Impairment: Use with caution; dose adjustment may be necessary.
Pharmacokinetics
Absorption: Well absorbed with peak plasma concentrations in approximately 1 hour.
Distribution: Widely distributed; protein binding approximately 45%.
Metabolism: Primarily metabolized by the liver via CYP3A4 enzyme, producing inactive metabolites.
Excretion: Excreted mostly via urine (around 70-80%), with some fecal excretion.
Half Life: Approximately 5-7 hours in healthy adults.
Contraindications
- Hypersensitivity to eszopiclone or any component of the formulation.
Precautions
- Use with caution in patients with a history of drug or alcohol dependence, psychiatric disorders, or sleep apnea. Avoid with concomitant use of other CNS depressants.
Adverse Reactions - Common
- Unpleasant taste (Common)
- Headache (Common)
- Dizziness (Common)
- Somnolence (Common)
Adverse Reactions - Serious
- Complex sleep behaviors (e.g., sleep walking, sleep driving, sleep eating) (Rare)
- Anaphylaxis or angioedema (Rare)
- Psychiatric and behavioral changes, including hallucinations (Rare)
Drug-Drug Interactions
- CNS depressants (additive sedative effects), CYP3A4 inhibitors (may increase eszopiclone levels), medications affecting sleep architecture.
Drug-Food Interactions
N/ADrug-Herb Interactions
N/ANursing Implications
Assessment: Assess for hepatic and renal function before initiating therapy. Monitor for emergence of adverse reactions.
Diagnoses:
- Risk for falls related to sedation and dizziness.
- Risk for impaired sleep pattern.
Implementation: Administer immediately before bedtime. Advise patients to avoid alcohol and other CNS depressants while taking this medication. Educate about potential sleep behaviors and side effects.
Evaluation: Evaluate the effectiveness of sleep improvement and monitor for adverse reactions, particularly complex sleep behaviors.
Patient/Family Teaching
- Take medication exactly as prescribed, at the same time each night.
- Avoid alcohol and operating machinery after taking eszopiclone.
- Report any unusual behaviors such as sleep walking or sleep eating.
- Do not drive or engage in hazardous activities until the effects are known.
Special Considerations
Black Box Warnings:
- Complex sleep-related behaviors such as sleep walking, sleep driving, and sleep eating have been reported with all Z-drugs, including eszopiclone.
- Caution patients about performing activities while not fully awake, with amnesia, confusion, or hallucinations.
Genetic Factors: No specific genetic markers needed for testing, but CYP3A4 genetic variability can affect metabolism.
Lab Test Interference: May interfere with certain sleep studies or CNS assessments.
Overdose Management
Signs/Symptoms: Excessive sedation, confusion, ataxia, coma.
Treatment: Supportive care, ensuring airway patency, monitoring vital signs. Activated charcoal may be used if ingestion was recent. Flumazenil has limited utility and is not routinely recommended.
Storage and Handling
Storage: Store at room temperature, 20-25°C (68-77°F), away from moisture and light.
Stability: Stable for the duration of the labeled shelf life when stored properly.