Instructions for use. Contraindications and release form.
INSTRUCTIONS
on the use of the drug
Zopiclone-FT
Dosage form and its description:
round, biconvex, white film-coated tablets with a score line on one side.
Compound:
Active substance: zopiclone 7.5 mg.
Excipients: corn starch, croscarmellose sodium, magnesium stearate, povidone, colloidal anhydrous silicon dioxide, microcrystalline cellulose, lactose monohydrate.
Shell composition: hypromellose, titanium dioxide, macrogol 400
Pharmacotherapeutic group:
Sleeping pills and sedatives. Benzodiazepine-like drugs.
ATX code: N05CF01
Pharmacodynamics
Zopiclone is a hypnotic that is a derivative of cyclopyrrolone. It quickly initiates and maintains sleep without reducing overall paradoxical sleep and preserves slow-wave sleep. There are minor residual effects the morning after taking zopiclone. Pharmacological properties of zopiclone include hypnotic, sedative, anxiolytic, anticonvulsant, and muscle relaxant effects. These effects are due to the high affinity and specific agonistic effect of the drug on the central receptors of the GABA macromolecular complex, which regulate the opening of chloride ion channels. however, compared to benzodiazepines, zopiclone and other cyclopyrrolones have been found to act at a different site in the receptor complex, including its different conformational changes.
Pharmacokinetics
Suction:
After oral administration at a dose of 7.5 mg, zopiclone is rapidly absorbed. Maximum plasma concentrations are reached within 1.5-2 hours and are approximately 30 ng/ml and 60 ng-ml after administration of 3.75 mg and 7.5 mg, respectively. Bioavailability is approximately 80%. Absorption is not affected by time of use, repeated doses or gender of the patient.
Distribution :
The drug is quickly distributed throughout the body. Plasma protein binding is weak (approximately 45%) and unsaturated. The risk of drug interactions due to the protein binding of zopiclone is very small. The volume of distribution is 91.8-104.6 liters. At recommended doses, the half-life of zopiclone is approximately 5 hours.
Repeated use of the drug does not cause accumulation; interindividual differences are insignificant.
Benzodiazepines and benzodiazepine-like drugs cross the blood-brain and placental barriers and are excreted into breast milk. During lactation, the pharmacokinetic properties of zopiclone in milk are the same as in plasma. It is calculated that with mother's milk the baby absorbs no more than 1% of the dose of the drug that the mother took within 24 hours.
Metabolism:
Zopiclone is metabolized primarily in the liver. In humans, the main metabolins of zopiclone are N-oxide (pharmacologically active in animals) and N-desmethylzopiclone (pharmacologically inactive in animals). In vitro studies indicate that cytochrome P450 (CYP)3A4 is the most important isoenzyme involved in the formation of both metabolites of zopiclone; CYP2C8 is also involved in the formation of N-desmethylzopiclone.
The apparent half-life (calculated from urine values) is 4.5 hours and 7.4 hours, respectively. Even when large doses are used in animals, no enzyme induction is observed.
Removal:
When comparing the low renal clearance of unchanged zopiclone (mean 8.4 ml/min) with its plasma clearance (232 ml/min), it is clear that zopiclone clearance is largely determined by metabolism. the drug is mainly excreted in the urine (approximately 80%) in the form of metabolites (N-oxide and N-demethylated derivatives) and in feces (approximately 16%).
High risk groups
In elderly patients, hepatic metabolism is significantly reduced and the half-life is approximately 7 hours. Various studies have not proven its accumulation in the body after repeated use of zopiclone.
In renal failure, the accumulation of zopiclone and its metabolites has not been established with long-term use of the drug. Hemodialysis is not used in the treatment of overdose due to the large volume of distribution of zopiclone.
In patients with liver cirrhosis, the plasma clearance of zopiclone is reduced (approximately 40%) due to a slower demethylation process, so dose adjustments should be made in these patients.
Indications for use
For the treatment of transient short-term insomnia in adults (including difficulty falling asleep, nighttime and early awakenings).
For maintenance treatment of chronic insomnia, using for a limited period of time.
Directions for use and doses
Orally, without chewing or dissolving, immediately before bedtime.
The dose should be adjusted depending on the patient's age, body weight, general health and type of insomnia.
Adults under 65 years of age: 1 tablet (7.5 mg) once daily.
In all cases, the daily dose of ZOPICLONE-FT should not exceed 7.5 mg.
Duration of treatment:
Treatment should be short-term if possible, ranging from a few days to 2-4 weeks (maximum), including a period of dose reduction:
Transient insomnia (for example, during travel) - 2-5 days;
Short-term insomnia - 2-3 weeks (for example, caused by stress).
How to stop treatment
Before starting to use the drug, patients should be explained that therapy should not be long-term and how to gradually stop it. Gradual cessation of treatment reduces the risk of recurrence of insomnia.
To reduce anxiety caused by possible symptoms of discontinuation of the drug, patients should be warned about the possibility of recurrence of insomnia after stopping treatment.
Side effect
The most common side effect when using ZOPICLONA-FT is a bitter or microtallic taste in the mouth.
The incidence of adverse reactions is indicated as: very often (≥1/10); often (from ≥1/100 to<1/10); нечасто (от ≥1/1000 до <1/100); редко (от ≥1/10000 до <1/1000); очень редко (<1/10000), частота неизвестна (невозможно определить частоту по имеющимся данным).
From the immune system: rarely - angioedema, anaphylactic reactions.
Mental disorders: infrequently - nightmares, agitation; rarely - confusion, decreased libido, irritability, aggressiveness, hallucinations; frequency unknown - anxiety, delirium, anger, depressed mood, inappropriate behavior (possibly associated with amnesia) and somnambulism, addiction, withdrawal syndrome.
From the nervous system: often - dysgeusia (bitter taste in the mouth), residual drowsiness; infrequently - dizziness, headache; rarely - antegrade amnesia (the risk increases with increasing dose; in some cases, behavioral disturbances can additionally be observed); frequency unknown - ataxia, paresthesia.
On the part of the organ of vision: frequency unknown - diplopia.
From the respiratory system, chest and mediastinum: rarely - shortness of breath, frequency unknown - respiratory depression.
From the gastrointestinal tract: often - dry mouth, infrequently - nausea, vomiting; frequency unknown - dyspepsia.
From the hepatobiliary system: very rarely - mild to moderate increase in the level of transaminases and/or alkaline phosphatase in plasma.
From the skin and subcutaneous tissue: rarely - urticaria or rash, itching.
From the musculoskeletal system and connective tissue: frequency unknown - muscle weakness.
General disorders and disorders at the injection site: frequency unknown - weakness.
Injuries, intoxications, complications of manipulations: rare - falls (mainly in elderly patients).
There are reports that after stopping zopiclone, withdrawal symptoms develop, the symptoms of which vary and can manifest as rebound insomnia, muscle pain, restlessness, tremors, sweating, agitation, confusion, headache, palpitations, tachycardia, delirium, hallucinations , nightmares, panic attacks, muscle cramps, gastrointestinal disorders and irritability. In severe cases, the following symptoms may occur: derealization, depersonalization, hyperacusis, numbness and tingling in the extremities, increased sensitivity to light and noise, tactile hyperesthesia, hallucinations. In very rare cases, seizures may occur.
Contraindications
Hypersensitivity to zopiclone or to any of the auxiliary components;
Myasthenia;
Severe respiratory failure;
Sleep apnea syndrome;
Severe liver failure;
Pregnancy;
Breastfeeding period;
Children under 18 years of age;
Congenital lactose intolerance, Lapp lactose deficiency, glucose-galactose malabsorption.
Overdose
Symptoms of overdose depend on the dose of ZOPICLONE-FT taken and are manifested by signs of depression of the central nervous system from drowsiness to the development of a coma. In mild cases, overdose is accompanied by drowsiness, confusion, and lethargy; in more severe cases, ataxia, hypotension, methemoglobinemia, respiratory depression and coma appear. An overdose does not pose a threat to life, except in combination with alcohol and drugs that depress the central nervous system.
The presence of concomitant diseases and the weakened condition of the patient can contribute to the severity of symptoms, which in rare cases can lead to death.
Treatment. Within an hour after an overdose of zopiclone, it is necessary to rinse the stomach and give activated charcoal. If necessary, symptomatic and supportive therapy in a hospital setting with monitoring of respiratory and cardiovascular activity is recommended.
In severe cases, the benzodiazepine receptor antagonist flumazenil can be used as an antidote. It has a short half-life (about an hour). Flumazenil should not be used in cases of mixed overdose or as a diagnostic agent. Hemodialysis in overdose is not effective due to the large volume of distribution of zopiclone.
Interaction with other drugs
Alcohol
When used simultaneously with alcohol, the sedative effect of benzodiazepines or benzodiazepine-like drugs increases. Inhibited attention may affect the patient's ability to drive or operate machinery. Avoid drinking alcoholic beverages and medications containing ethyl alcohol.
Morphine derivatives (painkillers, cough suppressants and replacement therapy), barbiturates
Increased risk of respiratory depression; An overdose can result in death.
Concomitant use of drugs that depress the central nervous system - morphine derivatives (painkillers, cough suppressants and replacement therapy), barbiturates, antidepressants and H1-antihistamines with sedative action, anti-anxiety drugs, antipsychotics, clonidine and its analogues, thalidomide
Strengthening the inhibitory effect of the central nervous system. Inhibited attention may affect the patient's ability to drive or operate machinery.
Clozatine
Increased risk of shock with respiratory arrest and/or cardiac arrest.
Erythromycin
The effect of erythromycin on the pharmacokinetics of zopiclone was studied in 10 healthy volunteers. In the presence of erythromycin, the AUC of zopiclone increases by 80%, indicating the ability of erythromycin to inhibit the metabolism of drugs that are metabolized by CYP3A4. As a result, the hypnotic effects of zopiclone may be enhanced.
Since zopiclone is metabolized by the cytochrome P450 system, plasma levels of zopiclone may increase when administered concomitantly with CYP3A4 inhibitors, such as erythromycin, clarithromycin, ketoconazole, itracolnazole and ritonavir. When used concomitantly with CYP3A4 inhibitors, a dose reduction of zopiclone may be necessary.
On the contrary, when used simultaneously with CYP3A4 inducers, such as rifampicin, phenobarbital, carbamazepine, phenytoin, St. John's wort, the plasma level of zopiclone may decrease. When used concomitantly with CYP3A4 inducers, an increase in the dose of zopiclone may be required.
special instructions
Whenever possible, the cause of insomnia should be determined and possible precipitating factors should be eliminated before prescribing a sleeping pill. Benzodiazepines and benzodiazepine-like drugs are not prescribed as the main drugs in the treatment of psychosis.
To reduce the risk of drug withdrawal symptoms, treatment with zopiclone should be short-term or intermittent.
High risk groups:
The greatest caution should be exercised in cases where there is a history of alcoholism or addiction/dependence on other substances;
Patients with impaired liver function, because benzodiazepines and benzodiazepine-like drugs in severe liver failure can accelerate the development of encephalopathy, so in this case they are contraindicated;
Patients with respiratory failure, because benzodiazepines and their derivatives have a depressing effect on the respiratory center (restlessness and anxiety can be harbingers of respiratory decompensation);
Elderly patients, because muscle relaxant and sedative effects may lead to injury due to falls.
Risk of addiction
Treatment with benzodiazepines and their derivatives, especially long-term, even in therapeutic doses, can lead to physical and mental dependence.
The risk of addiction increases if the following factors are present:
Increasing the duration of treatment (more than 4 weeks);
Alcohol abuse and/or taking other psychotropic medications;
Anxiety.
If the patient has developed a physical dependence, then sudden cessation of taking ZOPICLONA-FT can lead to the development of withdrawal syndrome: headache, muscle pain, anxiety, restlessness, tension, irritability, confusion. In more severe cases, symptoms may include derealization, depersonalization, numbness and tingling in the extremities, increased sensitivity to light, noise and touch, hallucinations or epileptic seizures.
After stopping treatment, withdrawal symptoms may appear within a few days. When treatment with ZOPICLONE-FT lasts no more than 4 weeks, the likelihood of developing withdrawal symptoms is minimal. It is recommended to discontinue the drug gradually.
Depression
Benzodiazepines and benzodiazepine-like drugs should not be used in the monotherapy of depression and the treatment of anxiety caused by depression, as they may induce suicide.
Tolerance
When benzodiazepines and their derivatives are used after repeated use over several weeks, some loss of effectiveness may occur. In patients taking zopiclone for no more than 4 weeks, cases of addiction were not observed. If tolerance develops, the dose of the drug cannot be increased.
The phenomenon of "recoil"
When therapy with benzodiazepines and their derivatives is stopped in an intensified form, insomnia may resume, anxiety, restlessness, and mood changes may appear. The appearance of the syndrome is facilitated by long-term treatment or abrupt cessation of treatment. In this regard, upon completion of treatment, it is recommended to reduce the dose of the drug gradually and inform the patient about this.
Rarely, antegrade amnesia may occur, especially when sleep is interrupted or after a long period of time between taking the pill and going to bed. To reduce the risk of antegrade amnesia, you should take ZOPICLONE-FT immediately before bedtime and ensure conditions for 7-8 hours of uninterrupted sleep.
Somnambulism and related behavior
Sleepwalking and sleep-related behaviors (eg, preparing and eating food, talking on the phone, driving) followed by amnesia have been reported in patients who have taken zopiclone and are not fully awake. Concomitant use of drugs that depress the central nervous system with zopiclone, alcohol consumption, or exceeding recommended doses increases the risk of developing this disorder. In patients who report such behavior disorder, the drug should be discontinued.
Other mental and paradoxical reactions:
During treatment with zopiclone, paradoxical reactions have been reported in some patients, mostly elderly: increased insomnia, nightmares, anxiety, agitation, irritability, aggressiveness, fits of anger, dilirium, hallucinations, oneiric delirium, confusion, psychotic symptoms, inappropriate behavior and others behavioral disorders. If such reactions occur, ZOPICLONE-FT is discontinued.
Risk of accumulation
Benzodiazepines and their analogues remain in the body for a time equal to 5 half-lives. In patients with impaired liver function and the elderly, T1/2 may increase significantly. With repeated doses, the concentration of zopiclone and its metabolites in the blood plasma is higher and the saturation stage is reached later. The effectiveness and safety of the drug can be assessed after reaching the saturation stage. Dose adjustment may be required.
Despite the fact that in patients with impaired renal function no accumulation of zopiclone was detected during long-term use, the dose of the drug is reduced by 2 times.
During treatment with ZOPICLONE-FT, you should not drink alcohol, and you should also avoid taking medications containing ethanol.
Use during pregnancy and lactation
Available data are insufficient to assess the safety of zopiclone during pregnancy and lactation.
Pregnancy:
Human experience with zopiclone during pregnancy is limited. Animal studies have not revealed any negative effects on pregnancy and fetal development. However, results obtained in animals do not always correlate with effects in humans. Therefore, the use of the drug during pregnancy is contraindicated.
If ZOPICLONE-FT is prescribed to women of reproductive age, they should be aware of the need to consult a doctor if pregnancy is suspected or planned to discontinue the drug.
When prescribing the drug in the third trimester of pregnancy or during childbirth, symptoms such as hypotemia, hypotension, drowsiness and respiratory depression should be expected in the newborn.
Newborns whose mothers took benzodiazepines or their analogues during the latter stages of pregnancy may develop physical dependence and are at risk of developing withdrawal symptoms in the postnatal period.
Lactation:
Although the concentration of zopiclone in breast milk is low, the drug should be avoided during breastfeeding.
Use in children.
Zopiclone is contraindicated in children and adolescents under 18 years of age, as the safety and effectiveness of zopiclone in this group of patients has not been established.
The ability to influence the reaction rate when driving a vehicle or working with other mechanisms.
ZOPICLONE-FT significantly affects the ability to drive vehicles and maintain machinery. as it causes sedation, decreased ability to concentrate, blurred vision and impaired muscle function. This risk increases when used concomitantly with alcohol. Therefore, it is not recommended to drive vehicles or operate machinery while using zopiclone and alcohol simultaneously. the risk of impaired attention increases if the patient's sleep duration was insufficient.
Release form:
Film-coated tablets in blister packs No. 10x1, No. 10x2, No. 10x3 and in jars No. 20 and No. 30 in package No. 1.
Every 1, 2 or 3 blisters or jars together with an insert are placed in a cardboard pack.
Storage conditions.
Store in a place protected from moisture and light at a temperature not exceeding 25°C.
Keep out of the reach of children!
Best before date:
2 years. The expiration date is indicated on the packaging.
The medicine cannot be used after the date indicated on the package.
Conditions for dispensing from pharmacies:
By doctor's prescription.
Manufacturer's name and address
Pharmtechnology LLC, 220024 Minsk, st. Korzhenevsky, 22.
Zopiclone is one of the most popular drugs used to achieve a hypnotic effect. The instructions for use describe in detail the indications and limitations for its use. One tablet contains 75 mg of the main active ingredient, which is Zopiclone. The auxiliary components include small amounts of starch, lactose and anhydrous silicon dioxide. The sleeping pill Zopiclone is produced in tablets with a protective coating.
Pharmacodynamics and pharmacokinetics
During treatment with the drug, a hypnotic and sedative effect develops. The substance is a derivative of cyclopyrollone. It is a benzodiazepine receptor agonist. As a result of its action, the time it takes to fall asleep is reduced. Getting up at night becomes less frequent, due to which the duration of sleep increases (see).
There are no changes in the structure of sleep; the fast phase retains its time of occurrence and duration. The clinic of incomplete awakening may not be clearly expressed. With subsequent rapid administration of the drug, no signs of accumulation are observed.
Zopiclone is characterized by rapid and complete absorption from the digestive tract. The maximum concentration of the drug is detected 1–2 hours after administration. After the substance enters the blood, binding to plasma proteins is observed. Elimination of the medication begins 3 hours after administration. The active components of the drug may pass into breast milk.
Instructions for use
Indications for the use of the drug Zopiclone include:
- Sleep disturbance with difficulty falling asleep and early awakening.
- , which has a transient, situational or chronic course.
- Mental illnesses accompanied by sleep disturbances.
- The presence of bronchial asthma, in which attacks bother the patient mainly at night. In this case, the drug is taken together with Theophylline.
The sleeping pill Zopiclone is taken orally, the tablets are swallowed with water. If necessary, the product can be pre-diluted in water at room temperature. Instructions for use of Zopiclone indicate that the average therapeutic dose is 7.5 mg. This amount should be used before bed in the evening.
In case of weak effect, repeat administration is acceptable. Elderly patients, as well as persons with insufficient functional activity of the liver and kidneys, are recommended to reduce the volume of the drug to 3.75 mg.
Side effects and contraindications
Prescribing the drug against the background of special individual sensitivity, as well as exceeding permissible concentrations, leads to the appearance of reactions such as:
- Changes in taste sensations with the appearance of an unpleasant metallic taste.
- Development of insufficient saliva production.
- Gag reflex and nausea.
- Pain in the head, hallucinations.
- Skin rashes.
Zopiclone tablets should not be used if the patient has:
- severe respiratory failure;
- hypersensitivity or intolerance to any component included in the composition.
The tablets should not be taken by pregnant women throughout their entire period and while breastfeeding (see). In childhood, use is possible only after reaching fifteen years of age. Use should be used with caution in patients who have liver and kidney dysfunction.
The development of dependence is rare. The chance increases with long-term use, which is at least a month. During treatment, it is prohibited to consume alcoholic beverages and drugs. Driving a car and working in enterprises that require attention should be limited.
Important! When Zopiclone is taken simultaneously with Trimipramine, a decrease in the concentration and therapeutic effect of the first drug is observed. When combined with drugs that depress the central nervous system, an increase in the effect of the drug is observed.
Analogs and price
The price of Zopiclone ranges from 550–900 rubles; the drug can only be purchased with a prescription from a specialist. Among analogues that have an identical composition or a similar mechanism of action, the most popular are:
- Imovan. It has a hypnotic, muscle relaxant and tranquilizing effect. Despite the fact that side effects are quite rare, the drug can be addictive. That is why dosage selection should only be carried out by the attending physician. It is necessary to avoid exceeding the therapeutic dose, as well as long-term use.
- Somnol. A drug that promotes the development of a hypnotic effect. Available in tablet form. The duration of use to prevent pathological reactions and addiction should not exceed a period of one month. Abrupt withdrawal of the drug should not be allowed, so discontinuation of use must be carried out gradually.
Zopiclone is the first representative of a new class of psychotropic drugs, the sedative and hypnotic effect is due to a high degree of affinity for binding sites on the GABA receptor complex in the central nervous system.
After taking the drug, sleep quickly sets in, characterized by a normal phase structure and duration. At the same time, the duration of the REM sleep phase does not decrease.
It is a hypnotic from the group of cyclopyrron derivatives, has a sedative, amnestic, anxiolytic and anticonvulsant effect. By interacting with benzodiazepine receptors, it enhances GABAergic processes in the brain, increasing the sensitivity of the receptors to the mediator.
After oral administration, it is quickly absorbed from the stomach, distributed throughout the body, including the brain. The maximum concentration of the active substance in the blood is achieved after 1-3 hours.
Indications for use
What does Zopiclone help with? According to the instructions, the drug is prescribed in the following cases:
- difficulty falling asleep;
- constant night or morning awakenings;
- insomnia, including chronic, short-term or situational types of ailment;
- restless sleep;
- sleep disorders associated with various types of mental disorders.
Instructions for use Zopiclone, dosage
The tablet is taken orally before bedtime (30 minutes before) with water.
Standard dosages according to the instructions are 1 tablet Zopiclone 7.5 mg per day. For severe forms of insomnia, the dosage can be doubled.
Maximum dosage – 15 mg \ 2 tablets.
For elderly patients and people suffering from liver dysfunction, the maximum dosage is 3.75 mg (half a tablet).
special instructions
Use should be avoided during pregnancy and breastfeeding. It is necessary to refrain from performing potentially hazardous activities that require increased attention.
Abrupt cessation of treatment does not cause the development of withdrawal syndrome.
During treatment, you should avoid drinking alcohol and taking depressant psychotropic drugs. In cases of use of Zopiclone for myasthenia gravis, strict neurological monitoring must be ensured due to a possible increase in muscle weakness.
Side effects
The instructions warn about the possibility of developing the following side effects when prescribing Zopiclone:
- From the gastrointestinal tract: metallic or bitter taste in the mouth, dry throat, vomiting, nausea.
- From the side of the central nervous system: drowsiness, headache, dizziness, hallucinations, confusion, anterograde amnesia, nightmares.
- Skin: rash, irritation.
Contraindications
Zopiclone is contraindicated in the following cases:
- hypersensitivity to the components of the drug;
- severe respiratory failure;
- pregnancy and lactation;
- children under 15 years old.
Patients with severe liver failure are prescribed with extreme caution.
Overdose
An overdose is manifested by deep, long sleep. Provide supportive and symptomatic treatment.
Zopiclone analogues, price in pharmacies
If necessary, you can replace Zopiclone with an analogue of the active substance - these are the following drugs:
- Imovan,
- Relaxon,
- Zolinox,
- Somnol,
- Piclodorm,
- Thorson.
When choosing analogues, it is important to understand that the instructions for use of Zopiclone, price and reviews do not apply to drugs with similar effects. It is important to consult a doctor and not change the drug yourself.
Price in Russian pharmacies: the medicine has been discontinued, with the same active ingredient you can buy 7.5 mg tablets, 20 pcs - from 245 to 302 rubles, according to 482 pharmacies.
Store in a place protected from light, out of reach of children, at room temperature. Shelf life – 2 years. Dispensing conditions from pharmacies are by prescription.
Zopiclone: instructions for use and reviews
Latin name: Zopiclone
ATX code: N05CF01
Active substance: zopiclone
Manufacturer: Calyx Chemicals & Pharmaceuticals Pvt. (India)
Updating the description and photo: 27.08.2019
Zopiclone is a sedative drug used to treat sleep disorders.
Release form and composition
The product is produced in the form of tablets: white with a creamy tint or white (10 pieces in blister packs, 2 packs in a cardboard box and instructions for use of Zopiclone).
1 tablet contains:
- Active substance: zopiclone – 7.5 mg;
- Auxiliary components: potato starch, tabletose 80, microcrystalline cellulose, talc, medical low molecular weight polyvinylpyrrolidone, aerosil, magnesium stearate.
Pharmacological properties
Pharmacodynamics
Zopiclone is a hypnotic from the group of cyclopyrrolone derivatives, a non-benzodiazepine benzodiazepine receptor agonist. It also has a sedative, anxiolytic, central muscle relaxant, anticonvulsant and amnestic effect.
Zopiclone, like benzodiazepine derivatives, enhances GABAergic processes in the brain (when interacting with benzodiazepine receptors). This leads to increased sensitivity of GABA receptors to the mediator. However, the substance is thought to interact with different sites on the benzodiazepine receptor than benzodiazepines.
Features of the effect of zopiclone on sleep: a decrease in the time it takes to fall asleep, a decrease in the number of night awakenings, an increase in the total duration of sleep. It has virtually no effect on sleep structure and does not significantly reduce the amount of REM sleep. The consequences of using the drug upon awakening are absent or only slightly expressed. Repeated doses of the drug are not accompanied by accumulation.
Pharmacokinetics
Zopiclone is quickly and completely absorbed from the gastrointestinal tract. Cmax (maximum concentration of the substance) is achieved in 1–3 hours. Easily penetrates histohematic barriers, including the blood-brain barrier, and spreads throughout organs and tissues, including the brain. The half-life ranges from 5.5 to 6 hours; does not accumulate.
Indications for use
- Primary sleep disorders: difficulty falling asleep, night and early awakenings, transient situational and chronic insomnia;
- Secondary sleep disorders associated with mental disorders, in cases where they significantly worsen the patient's condition.
Contraindications
- Decompensated respiratory failure;
- Age up to 15 years;
- Hypersensitivity to the components of the drug.
Nursing and pregnant women are not recommended to take sleeping pills.
In severe liver failure, the drug should be used with extreme caution.
Zopiclone, instructions for use: method and dosage
Zopiclone tablets are taken orally, in 1 dose, shortly before bedtime.
Patients with functional renal impairment do not require dosage adjustment. In case of severe liver failure, the drug should be taken in a daily dose of 3.75 mg.
Side effects
During treatment you may experience:
- Very common: mild metallic or bitter taste in the mouth;
- Rarely: gastrointestinal disorders (in the form of nausea, vomiting), mental disorders (in the form of irritability, confusion, depressed mood);
- Very rare: allergic reactions (in the form of urticaria, rash).
Upon awakening, drowsiness may develop, and occasionally dizziness and impaired coordination of movements.
Overdose
Main symptoms: depression of the central nervous system, manifested in varying degrees of severity (in the form of drowsiness, loss of consciousness and other disorders).
Therapy: gastric lavage, taking activated charcoal; symptomatic treatment (determined by the degree of poisoning). In hospital settings, flumazenil (a benzodiazepine receptor antagonist) is used. Hemodialysis is ineffective.
special instructions
During therapy, alcohol and depressant psychotropic drugs should be avoided.
Abrupt cessation of treatment does not cause withdrawal syndrome.
When using Zopiclone against the background of myasthenia gravis, due to a possible increase in muscle weakness, strict neurological control should be established over the patient's condition.
The duration of the course should not exceed 4 weeks.
Impact on the ability to drive vehicles and complex mechanisms
Due to the likelihood of developing dizziness and impaired coordination of movements the day after taking Zopiclone, you should drive a car and perform potentially dangerous work with caution.
Use during pregnancy and lactation
Zopiclone tablets are not prescribed during pregnancy/lactation.
Use in childhood
The drug is not prescribed to patients under 15 years of age.
For liver dysfunction
Zopiclone should be used with extreme caution in severe liver failure under medical supervision.
Drug interactions
When using certain medications simultaneously, the following effects may occur:
- Muscle relaxants and depressant psychotropic drugs: enhancing their effect;
- Trimipramine: decrease in its concentration (this should be taken into account when prescribing drugs together, as well as when using other tricyclic antidepressants).
Analogues
Analogues of Zopiclone are: Imovan, Relaxon, Zopiclone 7.5-SL, Zolinox, Somnol, Piclodorm, Thorson.
Terms and conditions of storage
Store in a place protected from light, out of reach of children, at room temperature.
Shelf life – 2 years.
Compound
Each film-coated tablet contains:
Active substance: zopiclone3.75 mg
Excipients: corn starch, croscarmellose sodium, magnesium stearate, povidone, colloidal anhydrous silicon dioxide, microcrystalline cellulose, lactose monohydrate.
Shell composition: hypromellose, titanium dioxide, macrogol 400.
Pharmacotherapeutic group
Sleeping pills and sedatives.
Benzodiazepine-like drugs.
Code ATX: N05 CF01
Pharmacological properties
Zopiclone is a member of the group of psychotropic drugs - cyclopyrrolones, related benzodiazepine derivatives. Pharmacological effects of zopiclone: hypnotic, sedative, anxiolytic, anticonvulsant, muscle relaxant. Under the influence of zopiclone, the time to fall asleep, the frequency of night and early awakenings decreases, the duration of sleep increases and the quality of sleep and awakening improves.
Indications for use
for the treatment of transient short-term insomnia in adults (including difficulty falling asleep, night and early awakenings). for maintenance treatment of chronic insomnia, using a limited period of time.
During a course of treatment, the lowest effective dose of the drug should always be used.
Directions for use and doses
Inside,without chewing or dissolving, immediately before bedtime.
The dose should be adjusted depending on the patient's age, body weight, general health and type of insomnia.
Adults under 65 years of age: 2 tablets (7.5 mg) once daily.
Patients with impaired liver function or respiratory failure:The recommended dose of the drug is 1 tablet (3.75 mg).
In all cases, the daily dose of ZOPICLONE should not exceed 2 tablets (7.5 mg).
Duration of treatment:
Treatment should be, if possible, short-term, ranging from a few days to 2-4 weeks (maximum), including a period of dose reduction:
Transient insomnia (for example, during travel) - 2 - 5 days; short-term insomnia - 2 - 3 weeks (for example, caused by stress).
How to stop treatment
Before starting to use the drug, patients should be explained that therapy should not be long-term and how to gradually stop it. Gradual cessation of treatment reduces the risk of recurrence of insomnia.
To reduce anxiety caused by possible symptoms of discontinuation of the drug, patients should be warned about the possibility of recurrence of insomnia after stopping treatment.
If you miss another dose of the drug, take it immediately. Do not use double dose insteadmissed. Continue taking the drug as recommended by your doctor.
Side effect
The most common side effect with Zopiclone is a bitter or metallic taste in the mouth.
The incidence of adverse reactions is indicated as: very often (≥1/10); often (from ≥1/100 to
From the immune system: very rarely - angioedema, anaphylactic reactions.
Mental disorders: infrequently - nightmares, agitation; rarely - confusion, decreased libido, irritability, aggressiveness, hallucinations; frequency unknown - anxiety, delirium, anger, depressed mood, inappropriate behavior (possibly associated with amnesia) and somnambulism, addiction, withdrawal syndrome.
From the nervous system: often - dysgeusia (bitter taste in the mouth), residual drowsiness; infrequently - dizziness, headache; rarely - antegrade amnesia (the risk increases with increasing dose; in some cases, behavioral disorders can additionally be observed); frequency unknown - ataxia, paresthesia.
On the part of the organ of vision: frequency unknown - diplopia.
From the respiratory system, chest and mediastinum:rarely - shortness of breath, frequency unknown - respiratory depression.
From the gastrointestinal tract: often - dry mouth, infrequently - nausea, vomiting; frequency unknown - dyspepsia.
From the hepatobiliary system: very rarely - mild to moderate increase in the level of transaminases and/or alkaline phosphatase in plasma.
From the skin and subcutaneous tissue:rarely - urticaria orrash, itching.
From the musculoskeletal system and connective tissue:frequency unknown - muscle weakness.
General disorders and disorders at the injection site:frequency unknown - weakness.
Injuries, intoxications, complications of manipulations: rare - falls (mainly in elderly patients).
There are reports that after stopping zopiclone, a withdrawal syndrome develops, the symptoms of which vary and can manifest as rebound insomnia, muscle pain, restlessness, tremors, sweating, agitation, confusion, headache, palpitations, tachycardia, delirium, hallucinations , nightmares, panic attacks, muscle cramps, gastrointestinal disorders and irritability. In severe cases, the following symptoms may occur: derealization, depersonalization, hyperacusis, numbness and tingling in the extremities, increased sensitivity to light and noise, tactile hyperesthesia, hallucinations. In very rare cases, seizures may occur.
If shi worsensl any side effect, whether described in this section or not, should beimmediately consult a doctor.
Contraindications
hypersensitivity to zopiclone or to any of the auxiliary components; myasthenia gravis; severe respiratory failure; sleep apnea syndrome; severe liver failure; pregnancy; breastfeeding period; children under 18 years of age; congenital lactose intolerance, Lapp lactase deficiency, glucose-galactose malabsorption.
Overdose
Symptoms of overdose depend on the dose of ZOPICLONE taken and are manifested by signs of depression of the central nervous system from drowsiness to the development of a coma. In mild cases, overdose is accompanied by drowsiness, confusion, and lethargy; in more severe cases, ataxia, hypotension, methemoglobinemia, respiratory depression and coma appear. An overdose does not pose a threat to life, except in combination with alcohol and drugs that depress the central nervous system.
The presence of concomitant diseases and the weakened condition of the patient can contribute to the severity of symptoms, which in rare cases can lead to death.
Treatment. Within an hour after an overdose of zopiclone, it is necessary to rinse the stomach and give activated charcoal. If necessary, symptomatic and supportive therapy in a hospital setting with monitoring of respiratory and cardiovascular activity is recommended.
In severe cases, the benzodiazepine receptor antagonist flumazenil can be used as an antidote. It has a short half-life (about an hour). Flumazenil should not be used in cases of mixed overdose or as a diagnostic agent. Hemodialysis in overdose is not effective due to the large volume of distribution of zopiclone.
Mutuallyaction with other drugs
Alcohol
When used simultaneously with alcohol, the sedative effect of benzodiazepines or benzodiazepine-like drugs increases. Inhibited attention may affect the patient's ability to drive or operate machinery. Avoid drinking alcoholic beverages and medications containing ethyl alcohol.
Morphine derivatives (painkillers, cough suppressants and replacement therapy), barbiturates
Increased risk of respiratory depression; An overdose can result in death. Concomitant use with drugs that depress the central nervous system - morphine derivatives (painkillers, cough suppressants and replacement therapy), barbiturates, antidepressants and Hi-antihistamines with sedative action, anti-anxiety drugs, antipsychotics, clonidine and its analogues, thalidomide
Strengthening the inhibitory effect on the central nervous system. Inhibited attention may affect the patient's ability to drive or operate machinery. Clozapine
Increased risk of shock with respiratory arrest and/or cardiac arrest. Erythromycin
The effect of erythromycin on the pharmacokinetics of zopiclone was studied in 10 healthy volunteers. In the presence of erythromycin, the AUC of zopiclone increases by 80%, indicating the ability of erythromycin to inhibit the metabolism of drugs that are metabolized by CYP3A4. As a result, the hypnotic effects of zopiclone may be enhanced.
Because zopiclone is metabolized by the cytochrome P450 system, plasma levels of zopiclone may increase when coadministered with CYP3A4 inhibitors such as erythromycin, clarithromycin, ketoconazole, itraconazole and ritonavir. When used concomitantly with CYP3A4 inhibitors, a dose reduction of zopiclone may be necessary.
On the contrary, when used simultaneously with CYP3A4 inducers, such as rifampicin, phenobarbital, carbamazepine, phenytoin, St. John's wort, the plasma level of zopiclone may decrease. When used concomitantly with CYP3A4 inducers, an increase in the dose of zopiclone may be required.
Precautionary measures
Whenever possible, the cause of insomnia should be determined and possible precipitating factors should be eliminated before prescribing a sleeping pill. Benzodiazepines and benzodiazepine-like drugs are not prescribed as the main drugs in the treatment of psychosis.
To reduce the risk of drug withdrawal symptoms, treatment with zopiclone should be short-term or intermittent.
High groupsrisk:
The greatest caution should be exercised in cases where there is a history of alcoholism or addiction/dependence on other substances; patients with impaired liver function, because benzodiazepines and benzodiazepine-like drugs in severe liver failure can accelerate the development of encephalopathy, so in this case they are contraindicated; patients with respiratory failure, because benzodiazepines and their derivatives have a depressing effect on the respiratory center (restlessness and anxiety can be harbingers of respiratory decompensation); elderly patients, because muscle relaxant and sedative effects may lead to injury due to falls.
Risk of addiction
Treatment with benzodiazepines and their derivatives, especially long-term, even in therapeutic doses, can lead to physical and mental dependence.
The risk of addiction increases if the following factors are present:
If the patient has developed a physical dependence, sudden cessation of taking ZOPICLONE may lead to the development of withdrawal symptoms: headache, muscle pain, anxiety, restlessness, tension, irritability, confusion. In more severe cases, symptoms may include derealization, depersonalization, numbness and tingling in the extremities, increased sensitivity to light, noise and touch, hallucinations or epileptic seizures.
After stopping treatment, withdrawal symptoms may appear within a few days. When treatment with ZOPICLONE lasts no more than 4 weeks, the likelihood of developing withdrawal symptoms is minimal. It is recommended to discontinue the drug gradually.
Depression
Benzodiazepines and benzodiazepine-like drugs should not be used in the monotherapy of depression and the treatment of anxiety caused by depression, as they may induce suicide.
Tolerance
When benzodiazepines and their derivatives are used after repeated use over several weeks, some loss of effectiveness may occur. In patients taking zopiclone for no more than 4 weeks, cases of addiction were not observed. If tolerance develops, the dose of the drug cannot be increased.
The phenomenon of "recoil"
When therapy with benzodiazepines and their derivatives is stopped in an intensified form, insomnia may resume, anxiety, restlessness, and mood changes may appear. The appearance of the syndrome is facilitated by long-term treatment or abrupt cessation of treatment. In this regard, upon completion of treatment, it is recommended to reduce the dose of the drug gradually and inform the patient about this.
Amnesia
Rarely, antegrade amnesia may occur, especially when sleep is interrupted or after a long period of time between taking the pill and going to bed. To reduce the risk of antegrade amnesia, you should take ZOPICLONE immediately before bedtime and ensure conditions for 7-8 hours of uninterrupted sleep. Somnambulism and related behavior
Sleepwalking and sleep-related behaviors (eg, preparing and eating food, talking on the phone, driving) followed by amnesia have been reported in patients who have taken zopiclone and are not fully awake. Concomitant use of drugs that depress the central nervous system with zopiclone, alcohol consumption, or exceeding recommended doses increases the risk of developing this disorder. In patients who report such behavior disorder, the drug should be discontinued.
Other mental andparadoxical reactions:
During treatment with zopiclone, paradoxical reactions have been reported in some patients, mostly elderly: increased insomnia, nightmares, anxiety, agitation, irritability, aggressiveness, fits of anger, delirium, hallucinations, oneiric delirium, confusion, psychotic symptoms, inappropriate behavior and others behavioral disorders. If such reactions occur, ZOPICLONE is discontinued.
Risk of accumulation
Benzodiazepines and their analogues remain in the body for a time equal to 5 half-lives. In patients with impaired liver function and the elderly, T/2 may increase significantly. With repeated doses, the concentration of zopiclone and its metabolites in the blood plasma is higher and the saturation stage is reached later. The effectiveness and safety of the drug can be assessed after reaching the saturation stage. Dose adjustment may be required.
Despite the fact that in patients with impaired renal function no accumulation of zopiclone was detected during long-term use, the dose of the drug is reduced by 2 times.
During treatment with ZOPICLONE, you should not drink alcohol, and you should also avoid taking medications containing ethanol.
Pregnancy and breastfeeding
Available data are insufficient to assess the safety of zopiclone during pregnancy and lactation.
Pregnancy
Human experience with zopiclone during pregnancy is limited. Animal studies have not revealed any negative effects on pregnancy and fetal development. However, results obtained in animals do not always correlate with effects in humans. Therefore, the use of the drug during pregnancy is contraindicated.
If ZOPICLONE is prescribed to women of reproductive age, they should be aware of the need to contact their doctor if they suspect or plan to become pregnant to discontinue the drug.
When prescribing the drug in the third trimester of pregnancy or during childbirth, symptoms such as hypothermia, hypotension, drowsiness and respiratory depression should be expected in the newborn.
Newborns whose mothers took benzodiazepines or their analogues during the latter stages of pregnancy may develop physical dependence and are at risk of developing withdrawal symptoms in the postnatal period.
Lactation
Although the concentration of zopiclone in breast milk is low, the drug should be avoided during breastfeeding.