Description of Zopiclone
Zopiclone is a cyclopyrrolone with actions similar to benzodiazepines namely hypnotic, sedative, anxiolytic, anticonvulsant and muscle relaxant. It shortens sleep onset latency and causes minimal residual effects the following morning – it does not accumulate significantly on repeated dosing and has short apparent half-life. The site of action, as with other cyclopyrrolones, is however different from that of benzodiazepines
Uses of Zopiclone
Zopiclone is used for short term treatment of insomnia, including difficulties in falling asleep, nocturnal awakening and early awakening, transient, situational or chronic insomnia, and insomnia secondary to psychiatric disturbances, in situations where the insomnia is debilitating or is causing severe distress for the patient.
Dosage of Zopiclone
For short-term treatment of insomnia:
Initially, 3.75 mg is taken at bedtime; but the dose may be increased up to a maximum daily dose of 7.5 mg as needed or depending on response to the initial dose if 3.75 mg.
In the elderly, patients with hepatic and renal insufficiency, an initial dose of 3.75 mg is given at bedtime. Their dose may be increased up to a maximum 5 mg daily depending on response and tolerance.
In all cases, ensure to use the lowest effective dose. On no account should there be repeat dose during the same night. That’s to say that it should be administered only as a single dose.
As with all hypnotics, zopiclone is not recommended for long term use (i.e. periods of more than 4 weeks). If physical dependence is suspected treatment should be withdrawn gradually.
Zopiclone us not recommended for children below 18 years of age.
How to Use Zopiclone
Because Zopiclone causes drowsiness, it is only taken at bed time. The only time it may be taken during the day is if patient is an inpatient. It is taken by mouth (orally). It may be taken with or without meals prior to bedtime. Swallow whole without sucking, chewing or breaking.
It should not be taken with any other sleep medicines, including those that can be bought over-the-counter if any. Don’t drink alcohol before or while taking these medicines. Together they may be more likely to cause side effects. Someone who takes zopiclone may still feel drowsy the day after taking one of these drugs. Keep in mind that all medicines taken for insomnia can impair one’s ability to drive and activities that require alertness the morning after use.
When not to take Zopiclone
Zopiclone should not be taken in severe sleep apnoea syndrome and by patients with severe hepatic impairment.
Other disease conditions where Zopiclone should not be taken are in myasthenia gravis, history of complex sleep behaviour and respiratory failure.
It should not be taken in pregnancy, and lactation and by children.
Precautions to observe While Taking Zopiclone
Observe precaution in any of these conditions or situations:
- In psychiatric disorders
- History of drug abuse.
- In the elderly, hepatic & renal insufficiency (reduce dose);
- When you want to drive or operate machinery.
- Limit treatment duration to <4 week to minimise risk of dependence and tolerance.
- Avoid abrupt discontinuation of therapy
Drug Interactions with Zopiclone
- Zopiclone may enhance CNS depressant effects of alcohol, hypnotics, opioid analgesics, TCAS.
- Its hypnotic effect is reduced hypnotic when used together with CYP3A4 inducers such as rifampicin, phenytoin and carbamazepine.
- Its hypnotic effect is increased when used together with CYP3A4 inhibitors e.g. erythromycin, clarithromycin, ketoconazole, itraconazole, ritonavir
- The most common side effects of Zopiclone is metallic or bitter after-taste.
- Less common side effects include Gl disturbances including nausea & vomiting; headache, dizziness, drowsiness, dry mouth.
- Especially in the elderly, it causes irritability, confusion, depressed mood, aggressiveness, incoordination, anterograde amnesia may occur.
- Rare side effects of Zopiclone are mild increase in liver enzymes, allergic-type reactions such as rash, urticaria.
How to Store
Store in a cool, dry place and away from direct sunlight. Keep away from the reach of children.