Zopiclone: uses, mechanism of action and adverse reactions.

This benzodiazepine-like drug is used in the treatment of insomnia, but is addictive.

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 discuss the pharmacological properties, uses and adverse reactions of zopiclone, one of the most popular anxiolytics for insomnia.one of the most prominent anxiolytics within this group.

What is zopiclone?

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

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

Although the relaxation caused by zopiclone occurs primarily in the central nervous system, it also affects the peripheral nervous system and muscles to a lesser extent. Consequently, it has mild myorelaxant and Anticonvulsant effects in addition to its anxiolytic and hypnotic effects.

What is it used for?

Zopiclone is prescribed mainly in cases of insomnia, not only of conciliation insomnianot only of conciliation insomnia but also of maintenance insomnia, 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 one month at the most. This is because the organism develops pharmacological tolerance easily, so to obtain the same effects the dose must be increased progressively; this is the main factor that explains the dependence or addiction to psychoactive substances.

Although zopiclone and the other Z-drugs have been considered superior to benzodiazepines for some years, recent research suggests that the intensity of their therapeutic effects is very similar. In addition, zopiclone may have even greater addictive potential than benzodiazepines, particularly when combined with alcohol.particularly when combined with alcohol.

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

Mechanism of action and pharmacokinetics.

Zopiclone has agonist (i.e., potentiating) effects on benzodiazepine BZ1 receptors, associated with the release of GABA or gamma-aminobutyric acid. GABA, which reduces the excitability of neurons, is the main inhibitory neurotransmitter of 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 drugs bind to the same classes of GABAergic receptors, producing very similar therapeutic effects and adverse reactions.

However, zopiclone affects brain waves during sleep to a lesser extent than benzodiazepines. This drug shortens stage I sleep (which explains why it reduces sleep latency), but does not alter the REM phase. In addition, prolongs the slow wave stages and stage II, which can be positive or negative.which may be positive or at least not too disruptive.

It is a rapidly absorbed psychotropic drug whose maximum potency is produced around 2 hours after administration, although the effects begin to be noticeable after 1 hour. The half-life is between 4.5 and 7.5 hours, approximately; this is why effective in treating early awakenings..

Adverse reactions and side effects

Among the most frequent side effects of zopiclone use related to the central nervous system are excessive drowsiness, decreased cognitive performance (leading to memory impairment, especially in anterograde memory), anxiety, depressive symptoms, muscle problems and coordination problems.

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. a bitter and unpleasant taste in the mouth..

Headaches, chills, palpitations, psychomotor agitation, hostility, aggressiveness, nightmares, nausea, vomiting, diarrhea, weight loss, urticaria, muscle spasms, paresthesias, breathing difficulties (dyspnea) and decreased sexual desire may also occur. However, these adverse reactions are less common than the above.

Excessive consumption of zopiclone can lead to coma since, if the dose is high, the depressant effects exerted by this drug on the central nervous system are very significant. However, if no other depressant, such as alcohol, is consumed at the same time, it is unlikely that the overdose will lead to death.