Clinical Overview
Zopiclone is a nonbenzodiazepine hypnotic indicated for the short-term treatment of insomnia. It is the racemic mixture of eszopiclone and is widely available internationally, though not approved in the United States. It provides effective sleep initiation and maintenance with less disruption of sleep architecture compared to benzodiazepines.
Primary Clinical Applications
Zopiclone is indicated for short-term treatment of insomnia, including difficulty falling asleep, frequent nocturnal awakenings, and early morning awakening. It is effective for both sleep onset and sleep maintenance insomnia, providing 7-8 hours of sleep with minimal next-day impairment when used appropriately.
Mechanism and Clinical Benefits
Zopiclone acts as a positive allosteric modulator of GABA-A receptors, particularly those containing alpha-1 subunits. This selective binding promotes sleep while preserving normal sleep stages and reducing rebound insomnia compared to traditional sedative-hypnotics. It has a half-life of approximately 5 hours, minimizing next-day sedation.
Clinical Considerations
The medication should be taken immediately before bedtime with at least 7-8 hours available for sleep. A characteristic metallic taste is common and may affect compliance. Like other Z-drugs, zopiclone has potential for tolerance, dependence, and complex sleep behaviors, requiring careful patient selection and monitoring.
Prescribing Information
Dosing & Administration
Insomnia – Adults:
- Recommended dose: 7.5 mg immediately before bedtime
- Range: 3.75-7.5 mg once daily
- Duration: Usually 2-4 weeks maximum
Elderly (≥65 years):
- Initial and usual dose: 3.75 mg immediately before bedtime
- Maximum: 7.5 mg if 3.75 mg insufficient
Hepatic Impairment:
- Mild-moderate: 3.75 mg immediately before bedtime
- Severe: Contraindicated
Administration:
- Take immediately before bedtime
- Ensure 7-8 hours available for sleep
- Do not take with or after a high-fat meal
- Swallow tablet whole with water
Indications
- Short-term treatment of insomnia
- Difficulty with sleep initiation and/or maintenance
Contraindications
- Hypersensitivity to zopiclone
- Severe hepatic insufficiency
- Respiratory failure
- Sleep apnea syndrome
- Myasthenia gravis
Warnings & Precautions
- Complex sleep behaviors: Sleep-driving, sleep-eating, and other activities while not fully awake may occur without alcohol or other CNS depressants; discontinue immediately if these occur
- CNS depression: Risk increased with alcohol and other CNS depressants
- Next-day impairment: Dose-dependent risk, especially at ≥2–3 mg; use caution with activities requiring alertness the next day
- Dependence and tolerance: Risk with prolonged use
- Withdrawal symptoms: May occur with abrupt discontinuation
- Respiratory depression: Risk in patients with compromised respiratory function
Drug Interactions
- CNS depressants: Enhanced sedation and respiratory depression
- Alcohol: Contraindicated – dangerous potentiation
- CYP3A4 inhibitors: May increase zopiclone levels
- CYP3A4 inducers: May reduce zopiclone effectiveness
Adverse Reactions
Common (≥1%):
- Metallic taste (very common), dry mouth, drowsiness
- Dizziness, headache, nausea
Serious:
- Complex sleep behaviors, severe allergic reactions
- Respiratory depression, dependence
Special Populations
- Elderly: Increased sensitivity, start with 3.75 mg
- Hepatic Impairment: Reduce dose for mild-moderate, contraindicated in severe
- Pregnancy: Category C – avoid during pregnancy
- Metallic taste: Very common, may affect compliance
Medical Disclaimer: This information is for educational purposes only and is not intended as medical advice. Always consult with qualified healthcare professionals before making any treatment decisions. Individual patient circumstances may vary significantly.
