Directions for use and doses
Use internally immediately before bedtime.
Dosage
Treatment should always begin with the minimum effective dose and the maximum dose should not be exceeded.
Usual doses:
Adults under 65 years of age: 7.5 mg is prescribed, i.e. 1 tablet.
Elderly patients over 65 years of age: 3.75 mg per day, a dose of 7.5 mg can only be used in exceptional cases.
Patients with impaired liver function or chronic pulmonary failure: the recommended dose is 3.75 mg.
Patients with renal failure: Treatment should begin with a dose of 3.75 mg per day.
In all cases, the daily dose of Sonex® should not exceed 7.5 mg.
Duration of treatment
Treatment should be as short-term as possible. The duration of treatment should not exceed 4 weeks, including the period of gradual cessation of treatment.
The duration of treatment for situational insomnia is 2-5 days; temporary insomnia - 2-3 weeks.
In some cases, it may be necessary to increase the duration of treatment. Long-term treatment is prescribed after consultation with a specialist.
Side effect
Side effects depend on the dose and individual sensitivity of the patient.
The most commonly observed side effect is a bitter taste in the mouth.
Adverse neurological and mental effects:
- anterograde amnesia, which can occur when taking therapeutic doses. The risk increases proportionally to the dose;
behavioral disorders, changes in consciousness, irritability, aggressiveness, restless behavior, somnambulism;
physical and psychological dependence, even when taking therapeutic doses, with withdrawal symptoms or rebound insomnia after cessation of treatment;
- feeling of intoxication, euphoria, speech disorders, coordination problems, depressive moods;
dizziness, headache, severe ataxia;
confusion, hallucinations, decreased attention or even drowsiness (especially in elderly patients), insomnia, nightmares, tension;
changes in sexual desire.
From the respiratory system:
- shortness of breath.
Skin: rash, itching, which may be symptoms of hypersensitivity.
Stop using the drug if symptoms occur.
From the organ of vision: diplopia.
Systemic side effects: muscle hypotension, asthenia, anaphylactic reactions, urticaria, angioedema.
From the gastrointestinal tract: dyspepsia, nausea, dry mouth, vomiting, diarrhea, constipation, anorexia or increased appetite.
Metabolism: weight loss.
From the musculoskeletal system: muscle hypotension.
From the liver: increased activity of liver enzymes.
Abnormal laboratory test results: very rarely - increased levels of transaminases and/or alkaline phosphatase, in rare cases can cause a clinical picture of liver damage.
Withdrawal syndrome has been reported when treatment with zopiclone is discontinued.
Sonex tablets p/o 7.5 mg No. 10x3
Name
Sonex tablet p/o 7.5 mg in container pack No. 10x3
Description
Film-coated tablets are white, round, biconvex, scored on one side.
Main active ingredient
Zopiclone
Release form
Pills
Dosage
7.5 mg
special instructions
Habituation: After taking benzodiazepines or their derivatives for several weeks, the sedative or hypnotic effect of the same dose may gradually weaken. In patients whose treatment period with Sonex® did not exceed 4 weeks, there was no pronounced addiction to the drug. Addiction. Treatment with benzodiazepines and their derivatives, especially long-term, can lead to physical and psychological pharmacodependence. Several factors contribute to the development of addiction: duration of treatment, dose, history of dependence on medications or other substances, including alcohol, and anxiety. Dependence may develop at therapeutic doses and/or in patients without specific risk factors. In very rare cases, dependence on zopiclone has been observed when receiving therapeutic doses. Once treatment is stopped, addiction may lead to withdrawal symptoms. Some of these symptoms occur frequently but are mild: insomnia, headache, anxiety, myalgia, muscle tension and irritability. Other symptoms that occur very rarely: restlessness or even confusion, paresthesia of the limbs, increased sensitivity to light, noise and physical contact, depersonalization, derealization, hallucinations and seizures. Withdrawal symptoms may develop several days after stopping treatment. When using short-acting benzodiazepines, especially at high doses, withdrawal symptoms may occur between two doses. The risk of dependence may increase when multiple benzodiazepines are used concomitantly as anxiolytics or hypnotics. There are also isolated cases of drug abuse. Rebound insomnia. As an exacerbation of insomnia that was tried to be treated with benzodiazepines or their derivatives, transient rebound insomnia may develop. Amnesia and changes in psychomotor function. Anterograde amnesia and changes in psychomotor function may occur within a few hours after taking the tablet. To reduce the risk of their development, the patient should take the tablet immediately before bedtime (see “Dosage and Administration”) and make sure that the conditions are as favorable as possible for several hours of uninterrupted sleep. Behavioral disorders: In some patients, benzodiazepines and their derivatives can cause a syndrome of altered consciousness (of varying degrees) with memory and behavioral disturbances. The following symptoms may develop: exacerbation of insomnia, nightmares, agitation, nervousness; delusional thoughts, hallucinations, confusion, psycho-like symptoms; mental retardation, mild excitability; euphoria, irritability; anterograde amnesia; suggestibility (naivety). These symptoms may be accompanied by disorders that are potentially harmful to the patient or others: abnormal behavior; self-aggression or aggression towards other persons, especially if family members or friends try to prevent the patient from doing what he wants; automatic behavior followed by amnesia. The appearance of these symptoms requires cessation of treatment. Somnambulism and related behavior: in patients who took zopiclone and did not fully wake up, somnambulism and other types of similar behavior were observed, when the patient, while sleeping, drives a car, prepares and consumes food, makes phone calls, sexual contacts, after which he does not remember anything . Use of alcohol and other CNS depressants with zopiclone increases the risk of the same behavioral disturbances that occur when zopiclone is used in doses exceeding the maximum recommended dose. For patients who develop such behavior disorders, it is strongly recommended to stop taking zopiclone (see section "Interactions with other drugs and other types of interactions" and section "Adverse reactions"). Risk of drug accumulation. Benzodiazepines and their derivatives (just like any other drug) remain in the body for a period of time equal to approximately 5 half-lives. In elderly patients and patients with impaired liver function, the half-life may be significantly longer. After repeated dosing, zopiclone or its metabolites reach steady state much later and at higher levels. The effectiveness and safety of the drug can only be assessed when a steady state is achieved. Dose adjustment may be necessary (see "Dosage and Administration"). During clinical studies in patients with renal failure, accumulation of zopiclone was not observed. Elderly patients. When prescribing benzodiazepines or their derivatives to elderly patients, one should be aware of their sedative and/or muscle relaxant effects, which can cause falls, which often have serious consequences for this group of patients.
Indications for use
Severe sleep disorders: situational and/or temporary insomnia.
Directions for use and doses
Use internally immediately before bedtime. Dosage Treatment should always begin with the minimum effective dose and the maximum dose should not be exceeded. Usual doses: Adults under 65 years of age: 7.5 mg is prescribed, i.e. 1 tablet. Elderly patients over 65 years of age: 3.75 mg per day, a dose of 7.5 mg can only be used in exceptional cases. Patients with impaired liver function or chronic pulmonary failure: the recommended dose is 3.75 mg. Patients with renal failure: Treatment should begin with a dose of 3.75 mg per day. In all cases, the daily dose of Sonex® should not exceed 7.5 mg.
Duration of treatment
Treatment should be as short-term as possible. The duration of treatment should not exceed 4 weeks, including the period of gradual cessation of treatment. The duration of treatment for situational insomnia is 2-5 days; temporary insomnia - 2-3 weeks. In some cases, it may be necessary to increase the duration of treatment. Long-term treatment is prescribed after consultation with a specialist. Duration of treatment The duration of treatment should be determined strictly according to indications, depending on the type of insomnia the patient has (see section “Method of administration and dosage”). Patients with major depressive episode. Benzodiazepines and their derivatives should not be prescribed as monotherapy, since in this case depression continues to develop and is accompanied by an unchanged or increased risk of suicide. The process of gradually stopping treatment. Patients should be clearly explained how to stop the treatment process, the need for a gradual dosage reduction, and also be warned about the risk of rebound insomnia. This will minimize any insomnia that may occur due to withdrawal symptoms caused by stopping treatment, even gradually. Patients should be informed of the potential for discomfort during the taper period. Patients with respiratory failure. When prescribing benzodiazepines and their derivatives to patients with respiratory failure, one should be aware of their depressant effect on the respiratory center (especially since anxiety and restlessness may be warning signs of respiratory decompensation, which requires transfer of the patient to the intensive care unit). Patients with renal failure and elderly patients. Although no accumulation of zopiclone has been detected after long-term use, it is recommended that this group of patients be prescribed half the usual recommended dose as a precautionary measure (see "Dosage and Administration" and the "Peculiarities of Use" section). Patients should be warned not to take the drug at the same time as other sedatives (see section "Interaction with other drugs and other types of interactions").
Use during pregnancy and lactation
Pregnancy. Animal studies have shown that zopiclone is not teratogenic. Today there is insufficient clinical data regarding the effect in the first trimester of pregnancy. By analogy with related products (benzodiazepines): a decrease in active movements and variability in fetal heart rate may be observed when taking high doses of zopiclone in the second and/or third trimester of pregnancy; Treatment with benzodiazepines during pregnancy, even in low doses, can cause signs of absorption, such as axial hypotonia and impaired sucking, and consequently poor weight gain. These signs are reversible but may persist for 1 to 3 weeks depending on the half-life of the prescribed benzodiazepine. At high doses, neonates may experience reversible respiratory depression or apnea and hypothermia. In addition, newborns may develop withdrawal symptoms, even in the absence of signs of absorption. It is characterized, in particular, by symptoms in newborns such as excessive excitability, restlessness and tremors, observed some time after birth. The timing of their appearance depends on the half-life of the drug and may increase the half-life. Therefore, the use of zopiclone should be avoided during pregnancy (regardless of its duration). If there is a need to initiate treatment with zopiclone during pregnancy, high doses should be avoided and the above-mentioned effects should be kept in mind when monitoring the newborn. Breastfeeding period. Zopiclone is not recommended for use during breastfeeding.
The ability to influence the reaction rate when driving a vehicle or working with other mechanisms
You should refrain from driving vehicles and operating machinery. Patients who drive vehicles and operate machinery should be warned about the risk of drowsiness. The risk of deterioration in attention increases even more if the duration of sleep is insufficient.
Precautionary measures
Particular caution is recommended when prescribing to patients with a history of alcoholism and other types of dependence on drugs or other substances (see section “Interaction with other drugs and other types of interactions”). Insomnia can be a sign of a physical or mental disorder. If insomnia persists or worsens after a short period of treatment, the clinical diagnosis should be re-evaluated. Children The use of Sonex® in children has not been studied, so it is not recommended for this group of patients.
Interaction with other drugs
Undesirable combination: Alcohol The sedative effect of benzodiazepines and their derivatives is enhanced if they are used in combination with alcohol. During treatment, it is prohibited to consume alcohol and drugs containing it. Combinations that should be taken into account: CNS depressants should not be prescribed simultaneously with Sonex®: morphine derivatives (analgesics, antitussives and substitution therapy for the treatment of drug addiction other than buprenorphine), sedatives, antidepressants (amitriptyline, doxepin, mianserin, mirtazapine, trimipramine), antipsychotics, barbiturates, anxiolytics, other hypnotics, sedative H1-antihistamines, central antihypertensives, baclofen; thalidomide; pizotifen, as this may lead to increased depression. Concomitant use with morphine derivatives (analgesics, antitussives and substitution therapy for the treatment of drug addiction other than buprenorphine) increases the risk of respiratory arrest, which can be fatal in case of overdose. Buprenorphine There is an increased risk of respiratory arrest, which can be fatal. The risk/benefit of this combination must be carefully weighed. The patient should be warned about the need to strictly adhere to the dosage prescribed by the doctor. Because zopiclone is metabolized by the cytochrome P450 (CYP) 3A4 isoenzyme, plasma levels of zopiclone may be increased when coadministered with CYP 3A4 inhibitors such as erythromycin, clarithromycin, ketoconazole, itraconazole and ritonavir. A dose reduction of zopiclone may be required when administered with CYP3A4 inhibitors. In contrast, plasma levels of zopiclone may be decreased when coadministered with CYP3A4 inducers such as rifampicin, carbamazepine, phenobarbital, phenytoin and St. John's wort (St. John's wort). It may be necessary to increase the dose of zopiclone when prescribed with SUR 3A4 inducers.
Contraindications
Hypersensitivity to zopiclone or to the components of the drug, severe acute or severe chronic liver failure (due to the risk of encephalopathy), acute respiratory failure, severe sleep apnea syndrome; myasthenia gravis, lactase deficiency (due to the lactose content in the drug). Children under 18 years of age, pregnancy and lactation.
Compound
Each tablet contains: active ingredient: zopiclone 7.5 mg; excipients: microcrystalline cellulose, talc, calcium stearate, sodium starch glycolate (type A), lactose monohydrate; shell: polyvinyl alcohol, titanium dioxide, polyethylene glycol, talc.
Overdose
Overdose can be life-threatening, especially in cases of simultaneous overdose of several central nervous system depressants (including alcohol). When taking a large amount of zopiclone, an overdose manifests itself mainly in depression of the central nervous system, which leads to a state ranging from drowsiness to coma, depending on the dose received. Mild overdose is manifested by symptoms of confusion and lethargy. In more serious cases, ataxia, hypotension, arterial hypotension, respiratory depression, and sometimes death were observed. If an oral overdose occurred earlier than an hour ago, the patient can be induced to vomit; in other cases, gastric lavage should be performed with respiratory protection. Following this, administration of activated charcoal may be helpful to reduce drug absorption. Close monitoring of cardiac and respiratory function in a specialized department is recommended. When treating overdose, hemodialysis is not appropriate because zopiclone has a large volume of distribution. For the diagnosis and/or treatment of accidental or intentional overdose of benzodiazepines, the administration of flumazenil may be useful. Flumazenil has the opposite effect of benzodiazepines, and therefore can cause neurological disorders (convulsions), especially in patients with epilepsy.
Side effect
Side effects depend on the dose and individual sensitivity of the patient. The most commonly observed side effect is a bitter taste in the mouth. Side neurological and mental effects: - anterograde amnesia, which can occur when taking therapeutic doses. The risk increases proportionally to the dose; behavioral disorders, changes in consciousness, irritability, aggressiveness, restless behavior, somnambulism; physical and psychological dependence, even when taking therapeutic doses, with withdrawal symptoms or rebound insomnia after cessation of treatment; - feeling of intoxication, euphoria, speech disorders, coordination problems, depressive moods; dizziness, headache, severe ataxia; confusion, hallucinations, decreased attention or even drowsiness (especially in elderly patients), insomnia, nightmares, tension; changes in sexual desire. From the respiratory system: - shortness of breath. Skin: rash, itching, which may be symptoms of hypersensitivity. Stop using the drug if symptoms occur. From the organ of vision: diplopia. Systemic side effects: muscle hypotension, asthenia, anaphylactic reactions, urticaria, angioedema. From the gastrointestinal tract: dyspepsia, nausea, dry mouth, vomiting, diarrhea, constipation, anorexia or increased appetite. Metabolism: weight loss. From the musculoskeletal system: muscle hypotension. From the liver: increased activity of liver enzymes. Abnormal laboratory test results: very rarely - increased levels of transaminases and/or alkaline phosphatase, in rare cases can cause a clinical picture of liver damage. Withdrawal syndrome has been reported when treatment with zopiclone is discontinued.
Storage conditions
Store in a place protected from light and moisture, at a temperature not exceeding 25 °C. Keep out of the reach of children!
Overdose
Overdose can be life-threatening, especially in cases of simultaneous overdose of several central nervous system depressants (including alcohol).
When taking a large amount of zopiclone, an overdose manifests itself mainly in depression of the central nervous system, which leads to a state ranging from drowsiness to coma, depending on the dose received. Mild overdose is manifested by symptoms of confusion and lethargy.
In more serious cases, ataxia, hypotension, arterial hypotension, respiratory depression, and sometimes death were observed.
If an oral overdose occurred earlier than an hour ago, the patient can be induced to vomit; in other cases, gastric lavage should be performed with respiratory protection. Following this, administration of activated charcoal may be helpful to reduce drug absorption.
Close monitoring of cardiac and respiratory function in a specialized department is recommended.
When treating overdose, hemodialysis is not appropriate because zopiclone has a large volume of distribution.
For the diagnosis and/or treatment of accidental or intentional overdose of benzodiazepines, the administration of flumazenil may be useful.
Flumazenil has the opposite effect of benzodiazepines, and therefore can cause neurological disorders (convulsions), especially in patients with epilepsy.
Use during pregnancy or breastfeeding
Pregnancy.
Animal studies have shown that zopiclone is not teratogenic. Today there is insufficient clinical data regarding the effect in the first trimester of pregnancy. By analogy with related products (benzodiazepines):
a decrease in active movements and variability in fetal heart rate may be observed when taking high doses of zopiclone in the second and/or third trimester of pregnancy;
Treatment with benzodiazepines during pregnancy, even in low doses, can cause signs of absorption, such as axial hypotonia and impaired sucking, and consequently poor weight gain. These signs are reversible but may persist for 1 to 3 weeks depending on the half-life of the prescribed benzodiazepine. At high doses, neonates may experience reversible respiratory depression or apnea and hypothermia. In addition, newborns may develop withdrawal symptoms, even in the absence of signs of absorption. It is characterized, in particular, by symptoms in newborns such as excessive excitability, restlessness and tremors, observed some time after birth. The timing of their appearance depends on the half-life of the drug and may increase the half-life.
Therefore, the use of zopiclone should be avoided during pregnancy (regardless of its duration).
If there is a need to initiate treatment with zopiclone during pregnancy, high doses should be avoided and the above-mentioned effects should be kept in mind when monitoring the newborn.
Breastfeeding period.
Zopiclone is not recommended for use during breastfeeding.
Children
The use of Sonex® in children has not been studied, so it is not recommended for this group of patients.
Features of application
addictive
After taking benzodiazepines or their derivatives for several weeks, the sedative or hypnotic effects of the same dose may gradually weaken.
In patients whose treatment period with Sonex® did not exceed 4 weeks, there was no pronounced addiction to the drug.
Addiction.
Treatment with benzodiazepines and their derivatives, especially long-term, can lead to physical and psychological pharmacodependence.
Several factors contribute to the development of addiction: duration of treatment, dose, history of dependence on medications or other substances, including alcohol, and anxiety.
Dependence may develop at therapeutic doses and/or in patients without specific risk factors.
In very rare cases, dependence on zopiclone has been observed when receiving therapeutic doses.
Once treatment is stopped, addiction may lead to withdrawal symptoms. Some of these symptoms occur frequently but are mild: insomnia, headache, anxiety, myalgia, muscle tension and irritability.
Other symptoms that occur very rarely: restlessness or even confusion, paresthesia of the limbs, increased sensitivity to light, noise and physical contact, depersonalization, derealization, hallucinations and seizures.
Withdrawal symptoms may develop several days after stopping treatment. When using short-acting benzodiazepines, especially at high doses, withdrawal symptoms may occur between two doses.
The risk of dependence may increase when multiple benzodiazepines are used concomitantly as anxiolytics or hypnotics.
There are also isolated cases of drug abuse.
Rebound insomnia.
As an exacerbation of insomnia that was tried to be treated with benzodiazepines or their derivatives, transient rebound insomnia may develop.
Amnesia and changes in psychomotor function,
Anterograde amnesia and changes in psychomotor function may occur within a few hours after taking the tablet. To reduce the risk of their development, the patient should take the tablet immediately before bedtime (see “Dosage and Administration”) and make sure that the conditions are as favorable as possible for several hours of uninterrupted sleep.
Behavioral disorders
In some patients, benzodiazepines and their derivatives can cause a syndrome of altered consciousness (of varying degrees) with memory and behavioral disturbances.
The following symptoms may develop:
exacerbation of insomnia, nightmares, agitation, nervousness;
delusional thoughts, hallucinations, confusion, psycho-like symptoms;
mental retardation, mild excitability;
euphoria, irritability;
anterograde amnesia;
suggestibility (naivety).
These symptoms may be accompanied by disorders that are potentially harmful to the patient or others:
abnormal behavior;
self-aggression or aggression towards other persons, especially if family members or friends try to prevent the patient from doing what he wants;
automatic behavior followed by amnesia.
The appearance of these symptoms requires cessation of treatment.
Somnambulism and related behavior:
In patients who took zopiclone and did not fully wake up, somnambulism and other types of similar behavior were observed, when the patient, while sleeping, drives a car, prepares and consumes food, makes phone calls, sexual contacts, after which he does not remember anything.
Use of alcohol and other CNS depressants with zopiclone increases the risk of the same behavioral disturbances that occur when zopiclone is used in doses exceeding the maximum recommended dose.
For patients who develop such behavior disorders, it is strongly recommended to stop taking zopiclone (see section "Interactions with other drugs and other types of interactions" and section "Adverse reactions").
Risk of drug accumulation.
Benzodiazepines and their derivatives (just like any other drug) remain in the body for a period of time equal to approximately 5 half-lives.
In elderly patients and patients with impaired liver function, the half-life may be significantly longer.
After repeated dosing, zopiclone or its metabolites reach steady state much later and at higher levels.
The effectiveness and safety of the drug can only be assessed when a steady state is achieved.
Dose adjustment may be necessary (see "Dosage and Administration").
During clinical studies in patients with renal failure, accumulation of zopiclone was not observed.
Elderly patients .
When prescribing benzodiazepines or their derivatives to elderly patients, one should be aware of their sedative and/or muscle relaxant effects, which can cause falls, which often have serious consequences for this group of patients.
Precautions for use
Particular caution is recommended when prescribing to patients with a history of alcoholism and other types of dependence on drugs or other substances (see section “Interaction with other drugs and other types of interactions”). Insomnia can be a sign of a physical or mental disorder. If insomnia persists or worsens after a short period of treatment, the clinical diagnosis should be re-evaluated.
Duration of treatment
The duration of treatment should be determined strictly according to indications, depending on the type of insomnia the patient has (see section “Method of administration and dosage”).
Patients with major depressive episode.
Benzodiazepines and their derivatives should not be prescribed as monotherapy, since in this case depression continues to develop and is accompanied by an unchanged or increased risk of suicide.
The process of gradually stopping treatment.
Patients should be clearly explained how to stop the treatment process, the need for a gradual dosage reduction, and also be warned about the risk of rebound insomnia. This will minimize any insomnia that may occur due to withdrawal symptoms caused by stopping treatment, even gradually.
Patients should be informed of the potential for discomfort during the taper period.
Patients with respiratory failure.
When prescribing benzodiazepines and their derivatives to patients with respiratory failure, one should be aware of their depressant effect on the respiratory center (especially since anxiety and restlessness may be warning signs of respiratory decompensation, which requires transfer of the patient to the intensive care unit).
Patients with renal failure and elderly patients.
Although no accumulation of zopiclone has been detected after long-term use, it is recommended that this group of patients be prescribed half the usual recommended dose as a precautionary measure (see "Dosage and Administration" and the "Peculiarities of Use" section).
Patients should be warned not to take the drug at the same time as other sedatives (see section "Interaction with other drugs and other types of interactions").
The ability to influence reaction speed when driving vehicles or other mechanisms
You should refrain from driving vehicles and operating machinery. Patients who drive vehicles and operate machinery should be warned about the risk of drowsiness.
The risk of deterioration in attention increases even more if the duration of sleep is insufficient.
Interaction with other drugs and other types of interactions
Undesirable combination :
Alcohol
The sedative effect of benzodiazepines and their derivatives is enhanced if they are used in combination with alcohol. During treatment, it is prohibited to consume alcohol and drugs containing it.
Plants that should be taken into account:
CNS depressants should not be prescribed simultaneously with Sonex®: morphine derivatives (analgesics, antitussives and substitution therapy for the treatment of drug addiction other than buprenorphine), sedatives, antidepressants (amitriptyline, doxepin, mianserin, mirtazapine, trimipramine), antipsychotics , barbiturates, anxiolytics, other hypnotics, sedative H1-antihistamines, central antihypertensives, baclofen; thalidomide; pizotifen, as this may lead to increased depression.
Concomitant use with morphine derivatives (analgesics, antitussives and substitution therapy for the treatment of drug addiction other than buprenorphine) increases the risk of respiratory arrest, which can be fatal in case of overdose.
Buprenorphine
There is an increased risk of respiratory arrest, which can be fatal.
The risk/benefit of this combination must be carefully weighed. The patient should be warned about the need to strictly adhere to the dosage prescribed by the doctor.
Because zopiclone is metabolized by the cytochrome P450 (CYP) 3A4 isoenzyme, plasma levels of zopiclone may be increased when coadministered with CYP 3A4 inhibitors such as erythromycin, clarithromycin, ketoconazole, itraconazole and ritonavir. A dose reduction of zopiclone may be required when administered with CYP3A4 inhibitors.
In contrast, plasma levels of zopiclone may be decreased when coadministered with CYP3A4 inducers such as rifampicin, carbamazepine, phenobarbital, phenytoin and St. John's wort (St. John's wort). It may be necessary to increase the dose of zopiclone when prescribed with SUR 3A4 inducers.
Psychological help. Consultations with a psychologist in Minsk. Psychotherapy.
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Zopicloni (SONEX, SOMNOL SONNAT-KMP)
Zopiclone is the first representative of a new class of psychotropic drugs, the cyclopyrrolones, which are structurally different from benzodiazepines and barbiturates.
Tablets are white or white with a creamy tint, flat-cylindrical in shape, scored and chamfered; composition: 1 tablet contains 7.5 mg of zopiclone; excipients: lactose monohydrate, microcrystalline cellulose, potato starch, povidone, aerosil, talc, magnesium stearate.
The pharmacodynamic effects of Zopiclone are similar in nature to similar compounds of this class, i.e. muscle relaxant, anxiolytic, sedative, hypnotic, anticonvulsant, causing amnesia. These effects are associated with a special agonistic effect on central receptors belonging to the macromolecular GABA-OMEGA complex, also called B31 and B32, which regulate the opening of chloride ion channels. Zopiclone has been found to prolong a person's sleep, improve sleep quality, and reduce the frequency of both nighttime and early awakenings. Zopiclone quickly induces sleep without reducing the portion of REM sleep in its structure, and then maintains sleep while maintaining normal phase composition. The absence of fatigue or drowsiness in the morning distinguishes Zopiclone from benzodiazepine and barbiturate drugs.
Pharmacokinetics: Zopiclone is rapidly absorbed. Maximum plasma concentrations are reached after 1.5-2 hours and are approximately 30 and 60 ng/ml after oral administration of 3.75 mg and 7.5 mg, respectively. Bioavailability is about 80%. Time of administration, repeated dosing and gender of the patient do not affect absorption. Zopiclone leaves the vascular bed very quickly. Plasma protein binding is low (about 45%) and unsaturated. The likelihood of drug interactions due to protein binding is very low. When using doses of 3.75 - 15 mg, clearance is independent of dose. The half-life is about 5 hours. Benzodiazepines and related compounds cross the blood-brain barrier, the placenta and into breast milk. During breastfeeding, the pharmacokinetic profile of zopiclone in breast milk approaches that in plasma. The estimated amount absorbed by a breastfeeding baby does not exceed 0.2% of the dose taken by the mother in 24 hours. There is no significant accumulation when taking the drug at a dose of 15 mg for 14 days.
Special risk groups: Elderly patients. Patients with renal failure. Patients with liver cirrhosis.
Indications for use: Treatment of primary sleep disorders: difficulty falling asleep, night and early awakenings, transient situational and chronic insomnia; as well as secondary sleep disorders in mental disorders in situations that significantly worsen the condition of patients. Indications are limited to serious sleep disorders in the following cases: - temporary insomnia; - short-term insomnia.
Contraindications:
Hypersensitivity to Zopiclone or other components of the drug, sleep apnea syndrome, decompensated respiratory failure, severe, acute or chronic liver failure (due to the risk of developing encephalopathy), myasthenia gravis, pregnancy, lactation, children under 18 years of age. The use of Zopiclone should be avoided during pregnancy, regardless of stage of pregnancy. Use during lactation is not recommended. Breastfeeding should be stopped during treatment (zopiclone passes into breast milk).
Directions for use and doses
Treatment should always begin with the lowest effective dose and should never exceed the maximum dose. Zopiclone should be taken immediately before bed. Treatment of elderly people should begin with the lowest dose - 3.75 mg. Depending on the effectiveness and tolerability, the dose may be increased in the future.
The usual doses are as follows:
- for adults under 65 years of age: 7.5 mg per day; — for elderly patients over 65 years of age, the recommended dose is 3.75 mg per day; only in exceptional cases can 7.5 mg per day be used; - for patients with severe liver failure, the recommended dose of Zopiclone is 3.75 mg; - for patients with moderate respiratory failure, the recommended dose is 3.75 mg per day; - for patients with renal failure, treatment should begin with a dose of 3.75 mg per day.
In all cases, the daily dose of Zopiclone should not exceed 7.5 mg.
Duration of treatment:
Treatment should be as short as possible, lasting from several days to 4 weeks, including a period of dose reduction.
It is necessary to indicate to patients what the duration of treatment is:
- from 2 to 5 days in case of temporary insomnia (for example, caused by a change of place when traveling); - from 2 to 3 weeks in case of short-term insomnia (for example, caused by some serious event in life).
In some cases, longer treatment may be required beyond the recommended period. In such cases, a repeated and thorough assessment of the patient's condition is mandatory.
Side effect
At recommended doses, the drug is well tolerated and has a low incidence of post-somnia disorders. The most common side effect of Zopiclone treatment is a mild bitter or metallic taste in the mouth. - anterograde amnesia, which can occur at therapeutic doses, the risk increases in proportion to the dose; - behavioral disturbances, changes in consciousness, irritability, depressed mood, aggressiveness, anxiety, sleepwalking; - physical and mental dependence, even at therapeutic doses, with withdrawal symptoms or rebound insomnia upon cessation of treatment; - dizziness, headache, in exceptional cases - ataxia; - confusion, hallucinations, decreased attention or even drowsiness (especially in old age), insomnia, nightmares, tension; - change in libido; - rash, itching; - diplopia; - muscle hypotension, asthenia, anaphylactic reactions, urticaria, angioedema; - gastrointestinal disorders: nausea, vomiting, dyspepsia, dryness and metallic taste in the mouth; - increased levels of liver enzymes; - very rarely the levels of transaminase and (or) alkaline phosphatase increase, which in some cases can lead to a clinical picture of liver damage. When waking up, you may experience drowsiness, and occasionally dizziness and poor coordination of movements.
Overdose
An overdose can be life-threatening, particularly when overdosing on multiple drugs, including other central nervous system depressants (eg, alcohol).
In case of taking a large amount of Zopiclone, signs of overdose appear in the form of inhibition of the central nervous system from drowsiness to coma, depending on the amount taken. In cases of minor overdose, symptoms include confusion and lethargy. In more severe cases, ataxia, hypotension, hypotension, and respiratory depression occur, sometimes with death.
If less than 1 hour has passed since the oral overdose, vomiting should be induced in a conscious patient; in other cases, it is necessary to perform gastric lavage, taking care of the airway. Following this, administration of activated carbon may be helpful to reduce absorption. Special monitoring of cardiac and respiratory activity is recommended to be carried out in a specialized department.
When managing a patient with an overdose, hemodialysis is ineffective due to the large volume of distribution of Zopiclone.
For the diagnosis and/or treatment of accidental or intentional overdose of benzodiazepines, the administration of flumazenil may be useful.
The antagonistic effect of flumazenil on the effects of benzodiazepines may contribute to the development of neurological symptoms (seizures), especially in patients with epilepsy. In cases of severe CNS depression, flumazenil may be required. It has a short half-life (about an hour). Flumazenil should not be used in cases of simultaneous overdose of several drugs and as a diagnostic tool.
Interaction with other drugs
The sedative effect of benzodiazepines and their derivatives increases when they are used in combination with alcohol. You should avoid taking alcoholic beverages and medications containing alcohol.
Zopiclone enhances the effect of muscle relaxants and depressant psychotropic drugs. The drug slightly reduces the concentration of trimipramine, which must be taken into account when prescribing them simultaneously, as well as when used with other tricyclic antidepressants.
Combinations to Consider
Other central nervous system depressants: morphine derivatives; sedative antidepressants (amitriptyline, doxepin, mianserin, mirtazapine, trimipramine), antipsychotics; barbiturates; anxiolytics; other sleeping pills; sedative H1-antihistamines; central antihypertensive agents; baclofen; thalidomide; Pizotifen.
When used concomitantly with morphine derivatives or barbiturates, the risk of respiratory depression increases, which can be fatal in case of overdose. Buprenorphine Increased risk of respiratory depression, which can be fatal. The balance of benefits and harms of this combination should be carefully weighed. The patient should be warned about the need to strictly adhere to the prescribed dose.
Medicines that inhibit certain liver enzymes (in particular cytochrome P 450) can enhance the activity of benzodiazepines and their derivatives. Plasma levels of zopiclone may be increased when coadministered with CYP3A4 inhibitors (eg, erythromycin, clarithromycin, ketoconazole, itraconazole, and ritonavir). A dose reduction of zopiclone may be necessary when coadministered with CYP3A4 inhibitors. Plasma levels of zopiclone may be reduced when co-administered with CYP3A4 inducers (rifampicin, carbamazepine, phenobarbital, phenytoin, and St. John's wort). An increased dose of zopiclone may be required when coadministered with CYP3A4 inducers.
Features of use The drug contains lactose and is therefore contraindicated in patients with congenital galactosemia, glucose or galactose malabsorption syndrome, as well as lactase deficiency. During treatment with the drug, alcohol and depressant psychotropic drugs should be avoided. In cases of use of the drug for myasthenia gravis, strict neurological monitoring should be ensured due to a possible increase in muscle weakness.
TOLERANCE If benzodiazepines and their derivatives are prescribed for several weeks, the sedative or hypnotic effect may gradually decrease, despite the use of the same dose. No significant tolerance was observed in patients treated with Zopiclone for periods of up to 4 weeks.
DEPENDENCE Any treatment with benzodiazepines and their derivatives, especially long-term treatment, can lead to the development of pharmacological dependence, physical and mental. Several factors contribute to the development of addiction: - duration of treatment (over 4 weeks) - dose (exceeding the recommended daily dose of 7.5 mg) - a history of a tendency to excessive use of medications or other substances, including alcohol - anxiety.
Dependence can develop at therapeutic doses and/or in patients without specific risk factors. Very rare cases of dependence due to Zopiclone have been reported when administered at therapeutic doses. Addiction can lead to withdrawal symptoms when treatment is stopped.
Some of these symptoms are common and mild: insomnia, headache, severe anxiety, myalgia, muscle tension and irritability.
Other symptoms observed less frequently include restlessness or even episodes of confusion, paresthesia of the limbs, increased sensitivity to noise, light and/or touch, depersonalization, derealization, hallucinations and seizures. After stopping treatment, withdrawal symptoms may develop within a few days. If short-acting benzodiazepines are used, especially if they are used in large doses, withdrawal symptoms may develop between two consecutive doses. Concomitant use of several benzodiazepines for anxiety or as a sleep aid may increase the likelihood of developing dependence.
INSOMNIA REABOUT Withdrawal syndrome is possible as an exacerbation of insomnia, indicating treatment with benzodiazepines or their derivatives.
AMNESIA AND CHANGES IN PSYCHOMOTOR FUNCTIONS
The development of anterograde amnesia and changes in psychomotor function is possible in the hours following after taking the pill. To reduce their risk, the tablet should be taken immediately after the patient goes to bed for the night, and care should be taken to ensure conditions that allow continuous sleep for several hours.
CONDUCT DISORDERS
In some patients, benzodiazepines and their derivatives can cause a syndrome that occurs with varying degrees of impairment of consciousness, memory and behavior disorders. The following symptoms are possible:
- exacerbation of insomnia, nightmares, anxiety, nervousness; - delirious stupefaction, hallucinations, oneiric disorder of consciousness (confused consciousness), symptoms resembling psychotic ones; - loss of self-control with impulsiveness; - euphoria, irritability; - anterograde amnesia; - suggestibility.
These symptoms may be accompanied by agitation, which can be harmful to the patient or others, for example:
- abnormal behavior; - aggressiveness towards oneself or other people, in particular if family or friends try to prevent the patient from doing what he wants; - automatism followed by amnesia. If these symptoms develop, treatment should be stopped.
SLEEPWALKING AND RELATED BEHAVIOR
Sleepwalking and related behaviors such as driving, cooking, making telephone calls, and sleep-related sexual intercourse followed by amnesia have been reported in patients who took Zopiclone and were not fully awake. Drinking alcohol and using other CNS depressants with Zopiclone increases the risk of developing this behavior, as does using Zopiclone in doses exceeding the maximum recommended dose. In the case of patients who exhibit this behavior, it is absolutely necessary to discontinue Zopiclone.
HAZARD OF DRUG ACCUMULATION
Benzodiazepines and their derivatives (like any other drug) remain in the body for a period of time equal to approximately 5 half-lives. In elderly patients and patients with impaired hepatic function, the half-life may increase significantly. With repeated dosing of Zopiclone, its metabolites reach the saturation stage much later, and their levels are higher. The effectiveness and safety of the drug can be judged only after the saturation stage has been reached. Dose adjustment may be required.
In clinical studies in patients with renal failure using Zopiclone, no accumulation was detected.
ELDERLY PATIENTS
Caution must be exercised when prescribing treatment with benzodiazepines or their derivatives to elderly patients, due to the risk of sedation and (or) muscle relaxant effects, which can cause falls, which often have serious consequences for patients in this group.
Precautionary measures
Extreme caution should be exercised when prescribing the drug to patients with a history of alcoholism or other addiction, addiction to medications or other substances. Insomnia can be a manifestation of an underlying mental or physical illness. If, after a short treatment period, insomnia does not improve or worsens, the diagnosis must be reconsidered.
DURATION OF TREATMENT
It is necessary to draw the patient's attention to the duration of treatment depending on the type of insomnia. The duration of the course of taking the drug should not exceed 4 weeks.
PATIENTS WITH EPISODES OF MAJOR DEPRESSION: Benzodiazepines or their derivatives alone should not be prescribed, since in this case the depression will not be treated and the risk of suicide will persist or even increase.
PROCESS OF GRADUAL DOSE REDUCTION
Patients should be given clear instructions on how to gradually discontinue treatment. In addition to the need for a gradual dose reduction, they should be aware of the danger of rebound insomnia in order to minimize any insomnia that may develop as a result of withdrawal symptoms due to discontinuation of treatment, even if it is gradual. Patients should be aware of the possible discomfort during a period of gradual dose reduction.
Effect on the ability to drive vehicles and moving equipment Due to the development of drowsiness, Zopiclone may have an adverse effect on the ability to drive vehicles and moving equipment, therefore, during the treatment period it is necessary to refrain from these types of activities. Also, due to possible dizziness and loss of coordination of movement, the day after taking the drug, you should drive a car and operate machinery with caution.
Release form: No. 10 x 1, No. 10 x 2, No. 10 × 3 in blisters; in cardboard packs. Store in a place protected from light and moisture at a temperature not exceeding 25 °C. Keep out of the reach of children! Shelf life: 2 years.
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