How Zopiclone Is Beneficial For Insomniac People
Zopiclone is a benzodiazepine analog drug, that is, it behaves and acts like a benzodiazepine, but its chemical structure is a little different, these drugs are also known as Z Drugs.
Instead of a pyridine ring, it is a cyclopyrrone, which mimics this structure, and which allows the rest of the molecule to bind to the GABA-complex Through a different site than benzodiazepines.
Zopiclone is a sleep-inducing agent. It has been shown to shorten the time to sleep and reduce the incidence of nocturnal awakenings, thereby increasing the quality of sleep and morning awakening.
Likewise, zopiclone is a drug with sedative, anxiety-reducing properties, with the ability to combat seizures and with muscle-relaxing effects. However, one of its main uses is in the short-term treatment of insomnia in adults.
What is Insomnia?
is an issue that comprises the capability to nod off or to keep it. It can also manifest itself through multiple awakenings throughout the night or an early morning awakening. The outcome is low quality of rest and inadequate rest.
This disorder significantly affects the quality of life and its most immediate consequences are daytime sleepiness, low concentration and the inability to maintain an active life. In the long term it can favor the development of various diseases. In fact, it is estimated that the risk of mortality increases significantly in those who sleep less than 6 hours a day.
Insomnia symptoms are not difficult to distinguish, as the patient himself sees troubles in nodding off or gets up right away. Lack of rest manifests itself throughout the day causing fatigue, weakness and, in extreme cases, even slowness when processing information, irritability
Causes of insomnia
A sleeping disorder might be the fundamental issue or it could be related to different conditions. Chronic insomnia is often caused by stress, life events, or habits that disrupt sleep. The absolute most continuous causes are the accompanying:
Main Uses of Zopiclone
Specialists endorse zopiclone for rest rhythm issues and for all types of a sleeping disorder, particularly when there are troubles nodding off, either initially or after a premature awakening.
Zopiclone is mainly prescribed in cases of insomnia, not only with conciliation but also with maintenance, since it reduces sleep latency and its sedative effects are maintained for several hours. In contrast to different hypnotics, zopiclone doesn’t essentially change sleep architecture.
In general, zopiclone treatment is limited to one to two weeks, or a maximum of one month. This is because of the way that the organism creates pharmacological resistance easily, subsequently, to acquire similar impacts, the dose should be progressively expanded.
Background and history
Zopiclone is a non-benzodiazepine sedative derived from cyclopyrrolone, which produces varying degrees of central nervous system depression and is dose dependent. Although not structurally related to benzodiazepines, its pharmacological profile is similar, particularly with nitrazepam.
The Z drugs emerged in the late 1980s and early 1990s. Zopiclone was approved by the British National Health Service early 1989, followed by zolpidem developed by Sanofi.
Zopiclone was created and developed by Rhône-Poulenc SA in 1986, a company that currently belongs to one of the most important pharmaceutical companies in the world, Sanofi-Aventis. At first, it was touted as the evolution of benzodiazepines.
However, recent studies have not shown any improvement over benzodiazepines in any respect. In April 2005, the DEA (Drug Enforcement Administration) warned that evidence was found that the drug can be as addictive as benzodiazepines, classifying it under schedule IV
Zopiclone, as customarily sold around the world, is a racemic combination of two stereoisomers , just one of which is active. In 2005, a pharmaceutical company in Massachusetts, called Sepracor, began an advertising campaign in the United States for a drug called Lunesta, it was the active stereoisomer, eszopiclone.
This had the result of putting what is a generic medication in most of the world under patent control in the United States. Generic forms of Lunesta have since opened up in the United States. Zopiclone is right now accessible off-patent in various European nations, just as Brazil, Canada, and Hong Kong.
The eszopiclone / zopiclone contrast is in the dose — the strongest eszopiclone measurements contains 3 mg of the active stereoisomer, while the most elevated zopiclone dose (10 mg) contains 5 mg of the therapeutic stereoisomer. The two agents have not been studied in clinical trials to decide the presence of any likely clinical contrasts (viability, efficacy, creating dependence on the medication, safety, and so forth)
Characteristics of Zopiclone
Zopiclone has agonistic on the benzodiazepine receptors BZ1, related to the release of GABA or gamma-aminobutyric acid. GABA, which reduces the excitability of neurons, is the main inhibitory neurotransmitter in the central nervous system; it also favors 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 receptor, producing very similar therapeutic effects and adverse reactions.
Nonetheless, zopiclone affects brain waves during rest, not as much as benzodiazepines. This medication abbreviates stage I sleep (which clarifies why it diminishes sleep latency), however does not alter REM phase. It also prolongs the slow wave stages and phase II, which can be positive or in any case not too disruptive.
It is a rapidly absorbing psychotropic drug whose maximum potency occurs within 2 hours of administration, although the effects begin to be noticeable after 1 hour. The half-life time ranges between 4 and a half hours and 7 and a half hours, approximately; This is why it is effective in treating early awakenings.
Generally, zopiclone is available as 7.5 milligram tablets for oral administration following the dosages listed below:
Adults: the usual dose is 7.5 mg taken before bedtime.
Elderly and / or debilitated patients: the recommended starting dose is 3.75 mg, which can be increased if necessary, to 7.5 mg before bedtime.
Treatment with zopiclone should not exceed 7-10 consecutive days. Use for more than 2-3 weeks should require a complete re-evaluation of the patient.
Since sleep disorders can be the first manifestation of physical or psychiatric problems, the symptomatic treatment of insomnia should be started only after a careful evaluation of the patient by the specialist.
Farmacos Z vs. Benzodiazepines
When comparing zaleplon, zolpidem and zopiclone with each other and with the benzodiazepines, it was concluded that the two pharmacological groups appear to be equally safe and effective in the treatment of insomnia.
Regarding the efficacy and safety of treatments for insomnia, benzodiazepine hypnotics and z-drugs are just as effective, although the former have a higher risk of unwanted effects.
A recent study showed that there is no significant difference in the efficacy and appearance of side effects according to the perspective of the participants who took benzodiazepines compared to those who took z-drugs. There are also no differences of interest in terms of dependence or the appearance of withdrawal symptoms.
The comparison of benzodiazepines with drugs “z” in the treatment of insomnia does not leave clear and conclusive results to decline the pharmacological balance for one or the other. The two groups of drugs appear to be equally effective and safe, although there may be small differences in relation to adverse effects in favor of the new hypnotics (z-drugs).
The search for new drugs that are equally effective as benzodiazepines but with fewer side effects led to the development of a new generation of hypnotics called Z compounds: zaleplon, zolpidem, zopiclone, and the most recent member of the group, eszopiclone (active enantiomer of zopiclone ).
Initially, the Z compounds were presented as promising hypnotics that will revolutionize the treatment of insomnia, due to their effectiveness, low incidence of adverse effects, and their reduced potential for dependence and abuse. However, with the boom in its use worldwide, reports of adverse effects increased, leading to the restriction of its use, prescription and disposal.
Indeed, some studies claim that these hypnotics are effective against insomnia and that they have a safer clinical profile when compared to their predecessors, while other studies show that there is not enough evidence to assert their safety
In a broad sense, Z drugs are characterized by being rapidly absorbed orally and by having a short plasma half-life, which makes them ideal for reducing sleep latency and reducing residual effects.
Of the group, Zopiclone is the one with the highest latency and half-life with potential for residual effects, only being surpassed by Eszopiclone, which has an active metabolite that prolongs its half-life, followed by Zolpidem with a half-life of 2. 5 hours approximately and its onset of action is faster than that of Zopiclone.
Finally, Zaleplon is the compound Z with the shortest latency and half-life, which makes it a hypnotic with no residual effects.
Zopiclone Vs Eszopiclone
Like zopiclone, eszopiclone is a manufactured compound demonstrated to be powerful in treating sleep deprivation. The selectivity of cyclopyrrolones gives more noteworthy advantages contrasted with benzodiazepines, as the previous supports the mesmerizing impact without creating critical anxiolytic and/or muscle unwinding impacts.
Eszopiclone is viable in the treatment of sleep deprivation, improving the seriousness of a sleeping disorder and showing an ideal security safety profile. Treatment with eszopiclone also resulted in longer total rest time and more prominent rest efficiency by polysomnography than zopiclone. Be that as it may, further examinations might be needed to approve the polysomnographic results.
The adverse effects of zopiclone are, in general, frequent and moderately important. The toxicological profile of this drug is similar to that of anxiolytic benzodiazepines. In most cases, adverse reactions are a prolongation of pharmacological action and mainly affect the central nervous system. The most characteristic adverse reactions are:
Frequently (10-25%): drowsiness, confusion and ataxia, especially in the elderly and debilitated, and if these symptoms persist, the dose should be reduced; dizziness, sedation, headache, depression, disorientation, dysphasia or dysarthria, reduced concentration, tremor, changes in libido, urinary incontinence, urinary retention, nausea, vomiting, diarrhea, constipation, taste disturbances (bitter or metallic taste), dry mouth, hypersalivation, epigastric pain.
Occasionally (1-9%): hepatitis, jaundice, dermatitis, urticaria, pruritus, leukopenia, agranulocytosis, anemia, thrombocytopenia, eosinophilia, behavioral disturbances, anterograde amnesia, paradoxical excitement, psychosis, vision disturbances, diplopia, nystagmus, disturbances audition.
Rarely (<1%): respiratory depression, hypotension, hypertension, bradycardia, tachycardia, palpitations.
With prolonged use, dependence develops. The abrupt interruption of a treatment at usual doses can cause withdrawal syndrome (anxiety, agitation, aggressiveness, insomnia, tremor, muscle spasm). If the treatment is with high doses, the withdrawal syndrome can be severe (delirium and seizures). The treatment will not be interrupted abruptly, nor will the doses be modified, without consulting the doctor (the interruption will be done gradually over 4-8 weeks).
Animal studies have not recorded embryotoxic or teratogenic effects. There are no adequate and well-controlled studies in humans. The use of this medicine is only accepted in the absence of safer therapeutic alternatives.
Zopiclone is excreted in human milk in small amounts. The possible effects on the nursing infant are unknown. It is recommended to stop breastfeeding or avoid the administration of this medicine.
The safety and efficacy of the use of zopiclone in children under 18 years of age have not been established. Use is not recommended in children under 18 years of age.
The elderly and / or debilitated patients show greater sensitivity to impaired motor and / or cognitive function after repeated exposure to hypnotic or sedative drugs.
These patients may also be more sensitive to the adverse effects of these drugs. It is recommended to use a reduced starting dose in order to reduce the incidence of adverse effects. Precautionary use, recommending monitoring.
Effects on the ability to drive
Benzodiazepines tend to cause decreased reflexes, small disturbances in psychomotor coordination and alertness. Therefore, patients treated with these drugs should avoid driving or operating complex machinery as much as possible, especially during the early hours of the morning if they have taken the drug at night (due to residual drowsiness). Do not drink alcoholic beverages.
Symptoms: As with other benzodiazepines, overdose is not life threatening unless its administration is combined with other central depressants (including alcohol). Benzodiazepine overdose is generally manifested by varying degrees of central nervous system depression, which can range from drowsiness to coma.
In moderate cases, symptoms include drowsiness, confusion, and lethargy. In more serious cases, ataxia, hypotonia, hypotension, respiratory depression, rarely coma and very rarely death may appear.
Treatment: Take into account the possibility that the patient has ingested multiple products. Vomiting should be induced (within an hour) if the patient remains unconscious or a gastric lavage should be performed with preservation of the airway if the patient is unconscious.
If gastric emptying is of no benefit, activated charcoal should be given to reduce absorption. Particular attention should be paid to respiratory and cardiovascular functions if the patient requires admission to an intensive care unit.
Antidote: Flumazenil can be used.
Can I take Zopiclone if I am pregnant?
The use of zopiclone is not suggested for pregnant women. If zopiclone is used during the last 3 months of pregnancy or during delivery, the newborn may be affected.
Symptoms may include decreased body temperature, decreased muscle tone, respiratory disorders, withdrawal symptoms. Therefore during this period, if possible, the use of zopiclone should be avoided.
Can I take Zopiclone if I am breastfeeding?
Zopiclone is excreted in human milk. Although the concentration of the drug in milk is low, lactating women should avoid taking this drug.
How quickly does treatment work?
Its hypnotic effect occurs 15 to 30 min after oral administration. However, your sleeping problems should improve considerably within 7 to 10 days after you start taking this medicine. If after a week of using it, you do not notice improvement, you should consult your doctor.
Is it safe to take Zopiclone?
Zopiclone is considered a safe drug as long as it is consumed by people over 18 years of age, as a treatment for short-term insomnia, that is, if it is consumed for two weeks or less.
Prescribing guidelines typically limit the use of these types of medications to two weeks, due to tolerance and dependency issues.
How long does a dose of Zopiclone last?
In general, the effect of Zopiclone (Sedorm) lasts about 6 hours depending on the function of the liver and kidneys. If there is a failure in your metabolism, you may experience drowsiness during the day, since the survival of the drug will be lengthened.
Are there any side effects of the treatment?
Yes, the most frequent side effects of Zopiclone, are the following:
Do I require a prescription for taking Zopiclone?
Zopiclone is a drug listed under schedule IV by the DEA for its addictive potential, for this reason, the only way to acquire it is through a medical prescription.
Why is it not safe to buy Zopiclone online?
Buying drugs online may be dangerous. First, for using Zopiclone, you need a prescription, it means that a doctor should examine you before prescribing any drugs, because not everybody is able to use this drug.
On the other hand, there is the risk of buying drugs from an unknown origin when you are buying medication online. We recommend not to take unnecessary risks.
Is this treatment option safe for children and elderly?
In accordance with the current state of knowledge regarding this drug, its use in children under 15 years of age is not recommended.
In people over 65 it should be used with great care, it is possible that the doctor indicates lower doses, due to a slowdown in its elimination.
How long do I have to take Zopiclone for?
All in all, zopiclone treatment is restricted to seven to about fourteen days, or a limit of one month. This is because of the way that the organism develops pharmacological resistance easily, along these lines, to get similar impacts, the portion should be progressively increased.
Can I take Zopiclone with other medications?
You should avoid taking zolpidem at the same time as any of the following medications:
Does Zopiclone create tolerance?
No significant tolerance is observed in patients treated with Zopiclone Qualigen for less than 4 weeks. After continued use for a few weeks, a certain degree of loss of efficacy with respect to hypnotic effects can be detected.
Who shouldn’t take Zopiclone?
You should not take Zopiclone if you have a severe liver problem if you have a problem where you temporarily stop breathing while you are sleeping (sleep apnea syndrome) if you have myasthenia gravis (fluctuating muscle weakness) if you are a child under the age of 18 years.
Does Zopiclone cause dependence?
Treatment with benzodiazepines and related compounds can lead to the development of physical and mental dependence. The risk of dependence increases with the dose and duration of treatment and is also higher in patients with a history of drug abuse or alcohol
I cannot swallow tablets, what should I take?
Zopiclone comes as a tablet. It also comes as a liquid for individuals who think that it’s difficult to swallow tablets, however this must be requested exceptionally by your primary care physician.