Zopiclone: ​​uses, mechanism of action and adverse reactions

In recent years, Z drugs, a class of hypnotics that rival benzodiazepines as the medical treatment of choice for insomnia, have become popular.

In this article we will analyze the pharmacological properties, uses and adverse reactions of zopiclone, one of the most prominent anxiolytics within this group.

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What is zopiclone?

Zopiclone is a psychoactive drug from the class of hypnotics and sedatives, substances that inhibit the activity of the central nervous system, favoring relaxation and sleep. It is a relatively recent medicine: it was launched on the market in 1986 by the French company Rhône-Poulenc.

Along with zolpidem, zaleplon and eszopiclone, zopiclone belongs to the group of “Z drugs”. (in addition to that of cyclopyrrolones). These hypnotics, which increase the action of the GABA neurotransmitter in a manner similar to that of benzodiazepines, have become popular in recent years for the treatment of insomnia.

Although zopiclone-induced relaxation occurs primarily in the central nervous system, it also affects the peripheral nervous system and muscles to a lesser extent. Consequently, it has mild muscle relaxant and anticonvulsant effects that are added to those of an anxiolytic and hypnotic type.

What is it for?

zopiclone It is mainly prescribed in cases of insomnia, not only for conciliation but also for maintenance, since it reduces sleep latency and its sedative effects are maintained for several hours. Unlike other hypnotics, zopiclone does not significantly alter sleep phases.

In general, treatment with zopiclone is limited to one or two weeks, or a month at the most. This is due to the fact that the organism easily develops pharmacological tolerance, therefore, to obtain the same effects, the dose must be increased progressively; this is the main factor that explains dependence or addiction to psychoactive substances.

Although zopiclone and the other Z drugs have been considered superior to benzodiazepines for few years, recent research suggests that the intensity of its therapeutic effects is very similar. In addition, zopiclone could have an addictive potential even greater than that of benzodiazepines, particularly if combined with alcohol.

In fact, the excessive consumption of zopiclone together with alcohol or other depressant psychoactive drugs is relatively common. In many cases these acts have recreational purposes or are related to self-medication, and significantly increase the risk of a traffic accident.

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Mechanism of action and pharmacokinetics

Zopiclone has agonist (i.e., potentiating) effects on BZ1 benzodiazepine receptors, associated with the release of GABA either gamma-aminobutyric acid. GABA, which reduces the excitability of neurons, is the main inhibitory neurotransmitter in the central nervous system; It also promotes muscle relaxation.

This mechanism of action is equivalent to that of benzodiazepines, which have been the most widely used anxiolytics for many decades. Both types of drug bind to the same classes of GABAergic receptor, producing very similar therapeutic effects and adverse reactions.

However, zopiclone affects brain waves during sleep less than benzodiazepines. This drug shortens stage I sleep (which explains why it reduces sleep latency), but does not alter REM sleep. Besides prolongs slow wave stages and phase II, which can be positive or in any case is not too disruptive.

It is a rapidly absorbed psychoactive drug whose maximum potency occurs around 2 hours after administration, although the effects begin to be noticeable after 1 hour. The average life time oscillates between 4 and a half hours and 7 and a half hours, approximately; that is why It is effective in treating early awakenings..

Adverse reactions and side effects

Among the most common side effects of zopiclone use that are related to the central nervous system are excessive feeling of drowsiness, decreased cognitive performance (leading to impaired memory, especially in forward memory), anxiety, depressive symptoms, muscle problems and those of coordination.

Other common symptoms include dry mouth, increased and decreased appetite, dyspepsia (digestive disorder characterized by burning, pain and flatulence), constipation and bad breath. A particularly common reaction to taking zopiclone is the perception of a bitter and unpleasant taste in the mouth.

Headaches, chills, palpitations, psychomotor agitation, hostility, aggressiveness, nightmares, nausea, vomiting, diarrhoea, weight loss, hives, muscle spasms, paresthesias, shortness of breath (dyspnea) and decreased desire sexual. However, these adverse reactions are less common than the previous ones.

Excessive consumption of zopiclone can lead to coma since, if the dose is high, the depressant effects that this drug exerts on the central nervous system are very significant. However, if some other depressant substance, such as alcohol, is not consumed simultaneously, the overdose is unlikely to result in death.