"Zopiclone": analogues, comparison of drugs, composition, instructions and reviews

Zopiclone (like other similar drugs based on it, Imovan, Somnol, Piclodorm, Relaxone, etc.) is a derivative of cyclopyrrolone, a precursor to exzopiclone, characterized by the highest likelihood of adverse reactions (such as a metallic taste in the mouth) among all new sleeping pills. Therefore, it is currently not used in many countries around the world.

Its properties are very similar to benzodiazepines, but it is safer (the risk of drug dependence is small). The antagonist of Zopiclone is Flumazenil.

Compound

Zopiclone capsules, milky in color with a creamy tint, are packaged in contour cells of ten pieces. There are two blisters in total in the package.

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One tablet contains one active ingredient - zopiclone. Additional microelements are the following components:

• lactose monohydrate;
• magnesium stearate;
• hypromellose;
• titanium dioxide;
• potato starch;
• calcium dihydrogen phosphate.

Contraindications

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Like any other drug, Zopiclone has a number of prohibitions on its use, for example:

What analogues exist for Zopiclone?

Pharmacokinetics of the drug

The drug is well absorbed from the gastrointestinal tract, has a short-term effect (therefore, there is no morning drowsiness after its use) and does not have a cumulative effect. Metabolism occurs in the liver (oxidation and hydroxylation) with a half-life (t1/2) of about 6 hours.

The maximum concentration in plasma is observed after 70-75 minutes. About 5% of the drug is excreted unchanged, 75% by the kidneys, and 20% with feces. Some data from recent years indicate a small amount of the drug secreted by the salivary glands.

Inducers and blockers of cytochrome P450, respectively, accelerate or slow down the clearance of substances. Adjustment (reduction) of the drug is required for liver diseases and when prescribing the drug for elderly patients.

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The drug is capable of passing through the histohematic, blood-brain and placental barriers. When passing through the placenta, it is able to penetrate into mother’s milk (the amount of the drug is 2 times less than in plasma). Metabolism occurs in the liver with the formation of three metabolites: two inactive and a low-active amine oxide.

Instructions for use

Zopiclone is taken orally once shortly before bedtime. The recommended daily dose for an adult patient is seven and a half milligrams.

In the presence of severe or persistent insomnia, the dosage can be doubled. For elderly people, it is recommended to start treatment with a small dose - 3.75 milligrams (half a tablet); if there is no result and adverse reactions occur, it can be increased.

Patients with impaired renal function do not need to adjust the dosage regimen. In case of severe liver failure, the drug should be consumed no more than 3.75 milligrams per day.

Cases of overdose

If the dosage was intentionally or accidentally violated, the following disorders may occur:

• from the gastrointestinal tract : a feeling of bitterness in the mouth, a metallic taste, dryness of the mucous membranes of the oral cavity and dyspeptic disorders;
• from the central nervous system : severe headache, dizziness and loss of consciousness, memory loss (anterograde form), hallucinations, nightmares and confusion;
• from dermatological manifestations : skin rash of various localization, pinpoint and spotty forms.

The amount of the drug required for the occurrence of adverse reactions is purely individual and depends on the compensatory capabilities of the body.

Peculiarities

During the treatment period, it is not recommended to consume alcoholic beverages and psychotropic medications. Immediate termination of the course does not provoke withdrawal syndrome.

When using Zopiclone for myasthenia gravis, due to a possible increase in muscle weakness, it is necessary to establish certain control over the patient's condition.

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The duration of therapy should not be more than one month. Due to the risk of dizziness and impaired coordination of movement, the next day after taking the tablet, driving a car and performing other dangerous work must be done with extreme caution.

Zopiclone for sleep and insomnia

Zopiclone is a new drug with a hypnotic effect, which is aimed at combating sleep problems. It differs from other drugs in a sufficient number of side reactions. The medicine is absolutely safe, since the likelihood of addiction is reduced to zero.

Description of the drug

Zopiclone is a sleeping pill from the cyclopyrrolone group. The medication is characterized by the following actions:

• sedative;
• hypnotic;
• tranquilizing;
• anticonvulsant;
• muscle relaxant.

Sleeping pills are related to a new class of psychotropic drugs. The drug quickly induces sleep in the patient, and at the same time does not reduce the part of REM sleep in its structure.

The drug is characterized by rapid half-life from the body. Usually cleared within 3-6 hours. The drug differs from other drugs with a similar effect in that it does not cause a feeling of weakness and severe drowsiness.

Taking the medication allows you to shorten the period of falling asleep and reduces the number of night awakenings. The quality of sleep improves significantly. Shows a special result for situational insomnia, which is accompanied by psycho-emotional stress. Sleep comes within 20 minutes after taking it.

Manufacturers

The manufacturer of Zopiclone for insomnia is Slovakofarma (Slovakia).

Contraindications and special instructions

Do not take Zopiclone if:

• hypersensitivity to the components in the composition;
• respiratory failure;
• sleep apnea syndrome;
• acute or chronic liver failure;
• myasthenia gravis;
• allergies to foods that contain wheat;
• carrying a baby in the 1st and 3rd trimesters;
• breastfeeding;
• children under 15 years old.

When using the medicine, you must pay attention to the following instructions:

1. Stopping the medication must be done in several stages. The dosage is reduced gradually. In this case, the likelihood of recurrent insomnia is significantly reduced. Also, the patient will not experience headaches, severe excitability, or nervous reactions.
2. If a person suffers from bronchial asthma, the number of attacks, their duration and intensity will be reduced.

The drug should not be taken with alcoholic beverages.

Side effects

Taking Zopiclone can provoke:

• metallic or bitter taste in the mouth;
• gastrointestinal disorders;
• confusion;
• mental disorders;
• irritability;
• allergic reactions.

If during therapy the patient experiences any extraneous symptoms, immediately consult a doctor for advice.

Benefits and harms of use

Zopiclone is considered one of the safest drugs that is beneficial for sleep. The medication helps normalize sleep and wakefulness, relieves depression, stress, anxiety, and feelings of fear. With long-term use it is not addictive. Partially strengthens the immune system and generally has a good effect on well-being.

Negative aspects include the presence of contraindications. The medicine can also cause negative reactions such as confusion, allergic reactions, and gastrointestinal disorders.

Instructions for use and dosage

The medication is taken orally. Adults and children over 15 years of age take 7.5 mg of the substance once before bedtime. If severe disturbances are observed, the dose can be increased by 2 times.

In old age, the dosage is reduced. The maximum possible dose is 3.75 mg. This is associated with metabolic disorders and toxic effects on the body. If there are kidney problems, then no dosage change is required.

During the study of the drug, no teratogenic effects were noted.

But the use of the drug in high doses in the second and third trimesters can reduce motor activity and have a detrimental effect on the fetal heart rate.

Therefore, it is important to consult a doctor who will assess the advisability of taking it. If during breastfeeding it is impossible to do without medication, then it is necessary to stop feeding for a while.

Analogues, substitutes and generics

If for some reason it is impossible to take Zopiclone, then there are effective analogues:

• Relaxon;
• Thorson;
• Somnol;
• Imovan;
• Piclodorm.

All medications have identical effects. But before taking and replacing the product, be sure to consult a doctor.

Customer Reviews

Patient reviews of sleeping pills are mostly positive.

Anna, 32 years old

“I work at a school, so everyone understands what it means to constantly spend time with children, even small ones.

Lately I have become very tired, my strength has left me, I have become irritable and nervous. Other health problems also appeared, so I consulted a doctor. He recommended Zopiclone to me.

After the first doses, the fatigue disappeared and my mood improved. I began to sleep more soundly at night.”

Irina, 56 years old

“I work as a pharmacist on the night shift, which is why my schedule is completely out of whack. I know how harmful it is not to sleep at night, but people don’t choose work. As a specialized specialist, I chose Zopiclone. My health has improved significantly, my sleep has returned to normal.”

Prices in pharmacies

The cost of Zopiclone is from 160 to 180 rubles.

Helpful Links

Zopiclone on otzovik.com and irecommend.ru.

Source: https://www.ObzorMatrasov.ru/narusheniya-sna/zopiklon-dlya-sna-pri-bessonnitse.html

Generics

According to the instructions and reviews, a number of the following drugs are analogues of Zopiclone (synonym), for example:

Terms and conditions of storage: store in a dark place inaccessible to children. Shelf life - twenty-four months. The tablets are dispensed from the pharmacy strictly according to the prescription.

"Imovan"

The active microelement is zopiclone, a hypnotic substance of the cyclopyrrolon group. The drug has a sedative, tranquilizing and muscle relaxant effect.

When using Imovan, it is important to remember that, despite the insignificant probability, there is a risk of addiction to the active substance and abuse of it.

The likelihood of addiction appears when dosages are violated and treatment is too long.

The risk of withdrawal syndrome and rebound insomnia after stopping the course should not be ruled out, especially after long-term use of Imovan. As a result, the dosage of the drug must be reduced gradually.

"Relakson"

A medicine that is used for chronic insomnia of various origins.

During night attacks of bronchial asthma in people who receive methylxanthine drugs, Relaxon weakens asthma attacks in the early hours and reduces their duration.

After completing a course of therapy, especially a long one, there is a risk of rebound insomnia and drug withdrawal syndrome, so it is not recommended to discontinue Relaxon quickly; it is important to gradually reduce the dose.

During therapy, you need to avoid alcoholic beverages, as they enhance the sedative effect.

Scope of application and contraindications

The sleeping pill Zopiclone is used for the following purposes:

• primary/secondary sleep disorders : difficulty falling asleep, waking up at night; early awakening, dissatisfaction with the quality of sleep, neuroses at night, sleep disorders, jet lag;
• insomnia : transient-periodic (episodic), situational (single-stage) and chronic;
• mental illnesses and disorders manifested by dissomnia : loss of a loved one, depressive states, anxiety disorders, chronic alcoholism, history of panic disorder;
• existing bronchial asthma, which manifests itself with night attacks - Zopiclone in this case is used in combination with a single use of Theophyllini.

Contraindications for use:

• severe respiratory failure (for example, with chronic obstructive pulmonary disease, bronchial asthma);
• hypersensitivity to the components of the drug ;
• pregnancy - use is contraindicated in all trimesters, which is associated with teratogenic and toxic effects on the fetus in certain doses or during certain periods of pregnancy;
• lactation period - due to the possibility of active substances getting into breast milk, medication intake is limited for the entire period of breastfeeding;
• age up to 15 years (according to Vidal 2020 recommendations);
• bulbar-spinal asthenia.

"Zolinox"

The medication is indicated for use in the presence of the following sleep disorders:

• difficulty falling asleep;
• night awakenings;
• early awakening;
• insomnia.

When using Zolinox, sleep occurs within thirty minutes and lasts six to eight hours. Eliminates headaches. Eliminates asthma attacks in the morning, reduces their intensity and duration.

Long-term use is not recommended; the course of therapy should not exceed twenty-eight days. The next day after using the medicine, patients should drive with caution and work with complex mechanisms.

"Somnol"

The drug is, according to reviews, an analogue of Zopiclone. A photo of the drug is presented above. The medication is available in the form of tablets for oral administration. The capsules are film-coated, biconvex round in shape, milky in color, with a line on one side of the surface.

"Somnol" is recommended for use by adult patients to eliminate situational and transient insomnia, including difficulty going to bed, as well as night awakenings.

The tablets are intended to be taken orally in the evening, usually before bedtime. It is recommended to use the drug for no longer than four weeks, including periods of dose reduction.

The decision to increase the dose and extend the course beyond the prescribed period is made only by doctors. Therapy begins with a minimum dosage. It is contraindicated to use the medicine in doses that exceed the maximum.

General information about the drug

Compared to other sleeping pills, Zopiclone is not addictive. It is absolutely safe and does not have a negative effect on internal organs or systems. This medicine helps to maintain good sleep.

When using this product, the period of falling asleep is significantly reduced and the quality of rest is improved. It is also characterized by soothing and relaxing properties. The components of the medication do not lead to post-somnia disorders. This means that the next day a person does not feel tired or weak.

Drug group, INN, scope of application

The drug belongs to medications that have a hypnotic effect. INN – Zopiclone. This drug is the first representative of the third class of psychotropic drugs. It is structurally different from barbiturates and benzodiazepines.

The drug is prescribed for chronic, situational or episodic insomnia. Experts also recommend taking the drug for bronchial asthma if it is accompanied by sleep disturbances.

Release forms and prices for the drug, average in Russia

The medicine goes on sale in the form of white tablets with a light cream tint, coated with a special coating. One cardboard package contains 2 blisters (10 tablets each).

Since the drug can only be purchased with a prescription from a specialist, it is not available for free sale in online pharmacies. The average price of Zopiclone in Moscow is 280 rubles. It depends on the number of tablets in one package (10 or 2 pieces).

Composition of Zopiclone

The manufacturers of the drug used zopiclone (7.5 mg) as the main active ingredient. The substance belongs to the sleeping pills. Characterized by a non-benzodiazepine structure. Zopiclone is a benzodiazepine receptor antagonist.

Penetrating inside the body, it comes into contact with central receptors. Helps increase the sensitivity of GABA receptors to the mediator, causing an increase in the frequency of opening of channels in the cytoplasmic membrane through which chlorine ions pass.

Features of the drug

Also, during the production of tablets, additional substances are used that improve the tolerability of the drug and improve the binding of the components to each other. The list of auxiliary components includes:

• lactose monohydrate;
• potato starch;
• microcrystalline cellulose;
• magnesium stearate;
• povidone;
• Aerosil;
• colloidal anhydrous silicon dioxide.

If you are allergic to one of the components, you should stop taking this medicine.

Pharmacodynamics and pharmacokinetics

The drug belongs to the group of cyclopyrrolone derivatives. It has anxiolytic, sedative, relaxant, amnestic and anticonvulsant properties.

The tablets significantly improve the quality of sleep, reduce the period of falling asleep and the number of awakenings. Under the influence of drugs, the structure of sleep does not change. There are no negative consequences after taking the drug. There is also no cumulation observed with repeated doses.

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Mechanism of action of Zopiclone

The drug is characterized by a high degree of absorption, which does not depend on the gender of the patient, time of administration or dosage. After about 2 hours, the peak amount of the active substance in the plasma is recorded. The level of bioavailability reaches 80%.

No more than 45% binds to plasma proteins. The half-life from the body is 5-7 hours. The metabolic process takes place in the liver. The substance leaves the body with urine (about 80%). Approximately 16% is excreted in feces.

"Piklodorm"

It is an analogue of Zopiclone. The drug has a hypnotic and sedative effect. Instantly and completely absorbed in the gastrointestinal tract. The maximum content is reached one to three hours after taking the medicine. It quite easily passes through physiological filters and spreads throughout organs and systems, including the brain. Reduces bedtime, does not change the phase structure of dreams, and enhances sleep cycles.

Does not provoke unnecessary symptoms after insomnia. No feeling of sleepiness the next morning. Reduces the number of night awakenings.

Falling asleep occurs within thirty minutes, sleep continues for eight hours. Eliminates headaches. In people with nocturnal manifestations of bronchial asthma, when used together with theophylline, asthma attacks occur less frequently in the early hours. The medicine weakens their intensity and duration.

Source

Practical application experience

The opinion of ordinary people and reviews of doctors who practice prescribing Zopiclone to their patients.

The sleeping pill Zopiclone is an excellent remedy for combating insomnia. Personally, I have been prescribing it to patients with sleep disorders of various etiologies for the past 3 years.

Of great importance is the possibility of taking the drug for a sufficiently long time without the risk of drug dependence (up to 2-3 weeks). I often advise students to take it on the eve of a session, since Zopiclone allows you to fall asleep quickly enough and wake up after 4-5 hours without feeling drowsy.

Depressive and anxiety states are another indication for use, since in such patients all phases of sleep are disturbed.

Psychiatrist, Gorustovich Elena Pavlovna

An excellent drug that was recommended to me by our local therapist. Problems with sleep arose immediately after the death of my husband; due to stress, I could not sleep for about 2 months.

I went to the doctor with blood pressure problems and talked about my sleep problems. She advised me to take Zopiclone at a dosage of 3.75 mg before bed.

I drank it for 12 days, in the morning I felt great, no drowsiness. After a ten-day course, sleep more or less returned to normal, but after 5-6 months, sleep problems and anxiety (also stress) reappeared. Now I am repeating the course of taking the medication again, I sleep perfectly, and I feel comfortable during the day.

Marko Tamara Ivanovna, 69 years old, pensioner

Pros: effectiveness, price, availability and good tolerability.

Disadvantages: cannot be taken for more than 3 weeks, possibility of drug dependence, effect on internal organs.