Zopiclone: uses, Mechanism Of Action And Adverse Reactions
In recent years, Z drugs have become popular, a type of hypnotics that rival benzodiazepines as the medical treatments of choice for cases of insomnia.
In this article we will analyze Pharmacological properties, uses and adverse reactions of zopiclone one of the most prominent anxiolytics within this group.
Zopiclone is a psychotropic drug in 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 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 cyclopyrrolones). These hypnotics, which increase the action of the neurotransmitter GABA in a manner similar to that of benzodiazepines, have become widely popular in recent years for the treatment of insomnia.
Although the relaxation caused by zopiclone occurs mainly in the central nervous system, it also affects the peripheral and muscles to a lesser extent. Consequently, it has mild muscle-relaxing and anticonvulsant effects that are added to the anxiolytic and hypnotic effects.
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 last 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 most. This is because the body easily develops pharmacological tolerance, so 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 some years, recent research suggests that the intensity of their therapeutic effects is very similar. Additionally, zopiclone could have an even greater addictive potential than benzodiazepines particularly if 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 occurring.
Mechanism of action and pharmacokinetics
Zopiclone has agonist (i.e. potentiating) effects on benzodiazepine BZ1 receptors, associated with GABA release 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 used anxiolytics for many decades. Both types of drugs bind to the same classes of GABAergic receptor, 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. Besides prolongs slow wave stages and phase II which can be positive or in any case not too disruptive.
It is a rapidly absorbed psychotropic drug whose maximum potency occurs around 2 hours after administration, although the effects begin to be noticeable after 1 hour. The average life time ranges between 4 and a half and 7 and a half hours, approximately; that is why It is effective in treating early awakenings
Among the most frequent side effects of zopiclone consumption that are related to the central nervous system are excessive feelings of drowsiness, decreased cognitive performance (leading to impairments in memory, especially in anterograde memory), anxiety, depression, muscle problems and coordination problems.
Other common symptoms include dry mouth, increased and decreased appetite, dyspepsia (a 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, unpleasant taste in the mouth
Headaches, chills, palpitations, psychomotor agitation, hostility, aggressiveness, nightmares, nausea, vomiting, diarrhea, weight loss, hives, muscle spasms, paresthesias, breathing difficulties (dyspnea) and decreased sexual desire may also occur. However, these adverse reactions are less common than the previous ones.
Excessive consumption of zopiclone can cause coma since, if the dose is high, the depressant effects that this drug exerts on the central nervous system are very significant. However, if another depressant substance, such as alcohol, is not consumed simultaneously, an overdose is unlikely to lead to death.
