From the Guidelines
Zopiclone is a non-benzodiazepine sedative-hypnotic medication primarily used for the short-term treatment of insomnia. It belongs to the cyclopyrrolone class of drugs and works by enhancing the effect of the inhibitory neurotransmitter GABA in the brain, which helps to induce sleep 1. Zopiclone is typically available as tablets in strengths of 3.75mg and 7.5mg, with the usual adult dose being 7.5mg taken shortly before bedtime. The medication has a relatively short half-life of about 5 hours, which helps reduce morning drowsiness compared to some other sleep medications.
Key Points to Consider
- Zopiclone is generally recommended only for short-term use (2-4 weeks maximum) due to the risk of dependence and tolerance 1.
- Common side effects include a metallic taste in the mouth, dry mouth, and daytime drowsiness.
- Zopiclone is a controlled substance in many countries due to its potential for abuse and dependence.
- A systematic review found that nonbenzodiazepine BZRAs, including zopiclone, improved sleep efficiency and other important outcomes compared with placebo, but the benefits seemed to outweigh potential harms only when used at the lowest effective dose and for the shortest possible duration 1.
Important Considerations for Use
- The U.S. Food and Drug Administration recently released a safety announcement on the risk for serious injuries caused by sleep behaviors associated with nonbenzodiazepine BZRAs, including zopiclone 1.
- Patients should be counseled on the potential risks of zopiclone, including the risk of dependence, tolerance, and adverse events such as sleepwalking, sleep driving, and other activities while not fully awake.
From the Research
Definition of Zopiclone
- Zopiclone is a non-benzodiazepine hypnotic agent used for the treatment of insomnia 2, 3.
- It is chemically unrelated to benzodiazepines but potentiates gamma-aminobutyric acid-mediated neuronal inhibition 3.
- Zopiclone is indicated for short-term use and should not be prescribed for more than 4 weeks 3.
Pharmacological Properties
- Zopiclone has a relatively low propensity to cause residual clinical effects, such as difficulty in waking or reduced morning concentration 2.
- It has a rapid elimination half-life and is extensively metabolized by oxidation and demethylation 4.
- Zopiclone is excreted in the urine as racemic zopiclone at less than 10% of the orally administered dose 4.
Efficacy and Safety
- Zopiclone has demonstrated efficacy equivalent to or greater than that of benzodiazepines in the treatment of insomnia 2, 3.
- It is well-tolerated in both elderly and younger patients with insomnia, with a low incidence of adverse events such as bitter taste, dizziness, and dry mouth 2, 3, 4.
- Zopiclone does not have a high dependence potential, at least in those who are not regular drug abusers/addicts 2, 3.