How zopiclone works
Zopiclone is a drug from the group of so-called Z-substances. It has a sedative (calming) and sleep-inducing effect.
The human nervous system has various messenger substances (neurotransmitters) that can have an activating or inhibiting effect. Normally, they are present in a balanced equilibrium and enable the change between waking and sleeping states.
One of these messengers, GABA (gammaaminobutyric acid), has an inhibitory effect on the nervous system as soon as it binds to its docking sites (receptors). Zopiclone increases the effect of the neurotransmitter GABA, resulting in sedation. This makes it easier to fall asleep and stay asleep.
Z-substances such as zopiclone bind preferentially to the alpha-1 subunit of the GABA receptor, which is why other effects (anxiety-relieving effect, relaxation of the muscles, antiepileptic effect) recede into the background.
Absorption, degradation and excretion
After ingestion by mouth (oral administration), zopiclone is absorbed from the intestine into the blood at a rate of about 80 percent. The maximum effect occurs relatively quickly and lasts for five to ten hours. Zopiclone is then partially metabolized in the liver and subsequently excreted primarily by the kidneys.
Eszopiclone
The two enantiomers that make up zopiclone are S-zopiclone (or eszopiclone) and R-zopiclone. S-zopiclone is responsible for the drug’s sleep-inducing and sedative effects. It is also included in some sleeping pills as the active ingredient alone. You can read more about this in the article Eszopiclone.
When is zopiclone used?
The sleeping pill zopiclone is used for short-term treatment of sleep onset and sleep maintenance disorders in adults.
How zopiclone is used
The active ingredient is taken in the form of tablets. The zopiclone dosage is generally 7.5 milligrams daily (adults). Elderly patients and patients with kidney or liver dysfunction receive a lower dosage.
The tablets are taken immediately before bedtime with sufficient liquid – for a maximum of four weeks. This is because the active ingredient can be addictive, especially after prolonged use and at high doses.
In addition, the sleeping pill should not be stopped suddenly, otherwise withdrawal symptoms may occur. Instead, the dosage should be gradually reduced over a period of about a week (“tapering”).
What are the side effects of zopiclone?
Often (i.e., in about ten percent of those treated), a bitter metallic taste in the mouth, dry mouth mucosa and impaired coordination occur after taking the sleeping pill. Occasionally, zopiclone also causes side effects such as headache, dizziness, anxiety, nausea, and confusion.
With sudden discontinuation, withdrawal symptoms may include muscle pain, headache, anxiety, tremors, nightmares, confusion, and mild irritability. Especially in elderly patients, prolonged use of sleeping pills poses a risk of falls.
What should be considered when taking zopiclone?
Contraindications
Zopiclone is contraindicated in the following cases:
- pathological muscle weakness (myasthenia gravis)
- severe respiratory distress
- severe liver dysfunction
- hypersensitivity to the active substance or other components of the tablets
- Lactation
Drug interactions
When taken at the same time, zopiclone increases the effect of other centrally acting medicines such as painkillers, anti-depressants (antidepressants) and epilepsy (antiepileptics), allergy medicines (antihistamines) and muscle relaxants (muscle relaxants).
Avoid alcohol during treatment with zopiclone – it can increase side effects and increases the risk of dependence.
In contrast, drugs that promote degradation reduce the effect of zopiclone. This applies, for example, to rifampicin (antibiotic), carbamazepine, phenytoin and phenobarbital (for epilepsy and seizures) and St. John’s wort (herbal antidepressant).
If the concomitant use of such agents cannot be avoided, the dose must be adjusted accordingly by the treating physician.
Trafficability and operation of machines
Due to the evening intake of zopiclone, the main effect is limited to the night. Nevertheless, the ability to react may also be impaired during the day.
Anyone using zopiclone should therefore refrain from active participation in road traffic and from operating dangerous machinery. This is especially true when consuming alcohol at the same time.
Age restrictions
Children and adolescents under 18 years of age suffering from sleep onset and sleep maintenance disorders should not be treated with zopiclone.
Pregnancy and lactation
The level of experience regarding the short-term use of zopiclone during pregnancy is relatively high. Experts do not suspect any late effects on the newborn. However, adjustment disorders of the newborn may occur in the first days after birth (especially if the sleeping pill is used in the last third of pregnancy).
Zopiclone passes into breast milk only to a very small extent. Nevertheless, the sleeping pill must not be used during breastfeeding.
Overdose
Symptoms of poisoning with the active ingredient zopiclone are drowsiness, drowsiness and muscle weakness up to unconsciousness and breathing problems. A zopiclone overdose is generally not life-threatening. However, when the drug is combined with other centrally-acting medications or alcohol, the effects can be life-threatening.
How to obtain medications containing zopiclone
Zopiclone requires a prescription in Germany, Austria and Switzerland and is therefore only available from pharmacies with a prescription from a doctor.
No preparations containing the active ingredient zopiclone are currently sold in Austria.
Other interesting facts about zopiclone
The active ingredient zopiclone was officially approved in Germany in 1990. The market launch took place one year later.
