pharmachologic effect
Sonnat is a hypnotic drug that is a representative of the third generation of hypnotics. The drug Sonnat contains the active substance - zopiclone - a drug from the cyclopyrrolone group. The drug has a hypnotic effect and, due to its short half-life, does not cause post-somnia disorders. The drug Sonnat helps to make it easier to fall asleep and increase the duration of sleep. Patients receiving therapy with Sonnat experienced improved sleep quality, prolongation of deep sleep (third and fourth stages of sleep), as well as the second stage of sleep. In addition, zopiclone significantly reduces the number of night awakenings and does not affect the apnea index. The mechanism of action of the drug is based on its ability to bind to the receptors of the GABA complex, while zopiclone selectively stimulates the omega-1 and omega-2 subtypes of benzodiazepine receptors of the macromolecular GABA-benzodiazepine-chlorionophore complex, without affecting the benzodiazepine receptors of the omega-5 subtype. Due to the binding of the drug to omega receptors, the opening of neuronal ionoform channels for chlorine is noted, the sensitivity of GABA receptors to the mediator increases and the inhibitory effect of GABA on the central nervous system increases. Due to the selective effect of the drug on omega-1 and omega-2 receptor subtypes, Sonnat has no side effects characteristic of benzodiazepine hypnotics. When administered orally, zopiclone is well absorbed from the gastrointestinal tract. The bioavailability of the drug is about 70%. Zopiclone is characterized by a high degree of binding to plasma proteins (up to 92%). The peak concentration of the active substance in the blood plasma is observed 1-3 hours after oral administration, the maximum plasma concentration of zopiclone is about 75.9 ng/ml. The therapeutic effect of the drug is observed 30 minutes after use and lasts for 6-8 hours. Metabolized in the liver, as a result of metabolism, N-oxide is formed, which has pharmacological activity that is significantly inferior to the pharmacological activity of unchanged zopiclone. In addition, as a result of metabolism, two pharmacologically inactive metabolites are formed. The drug penetrates well through the blood-brain and hematoplacentral barriers and is excreted in breast milk. The half-life is approximately 5.5-6 hours. It is excreted mainly by the kidneys and to a small extent with carbon dioxide during respiration. The drug does not accumulate in the body. In patients with impaired renal function, the half-life of zopiclone is prolonged. In elderly patients with normal renal function, the pharmacokinetics of the drug does not change.
Indications for use
The drug is used to treat patients with various sleep disorders, including the treatment of patients with the following conditions: - difficulty falling asleep;
- shallow sleep, state of weakness and fatigue after sleep; - frequent awakenings during night sleep; - insomnia, including situational, short-term, intermittent and chronic insomnia; — the drug is also used to treat patients with mental disorders that are accompanied by secondary sleep disorders; - the drug can be prescribed in the complex treatment of patients with bronchial asthma who suffer from nocturnal asthmatic attacks. Method of administration The drug is taken orally. It is recommended to swallow the tablet whole, without chewing or crushing, with a sufficient amount of liquid. The duration of the course of treatment and the dose of the drug are determined by the attending physician individually for each patient, depending on the nature of the disease and the patient’s personal characteristics. Adults are usually prescribed 7.5 mg of zopiclone (1 tablet of Sonnat) once in the evening before bed. If necessary, the dose of the drug can be increased to 15 mg of zopiclone (2 tablets of the drug Sonnat). Elderly patients (over 65 years of age), as well as patients suffering from impaired liver function and respiratory failure, are usually prescribed 3.75 mg of zopiclone (0.5 tablets of the drug Sonnat). Depending on the tolerability of the drug, the dose can be gradually increased to 7.5 mg of zopiclone (1 tablet of Sonnat). It is not recommended to take the drug for more than 4 weeks in a row.
Side effects
The drug is usually well tolerated by patients, however, in isolated cases, patients using the drug Sonnat have developed the following side effects: From the central and peripheral nervous system: drowsiness, fatigue, irritability, weakness, headache, dizziness, confusion, emotional lability , memory impairment. In addition, when using zopiclone, paradoxical reactions may develop, including nightmares, nervousness, aggressiveness, fits of anger and hallucinations. From the digestive system: nausea, vomiting, dry mouth, changes in taste and a metallic or bitter taste in the mouth. Allergic reactions: skin rash, itching, urticaria. Others: anterograde amnesia, decreased libido. With prolonged use of the drug, drug dependence and withdrawal syndrome may develop.
Contraindications
Increased individual sensitivity to the components of the drug.
The drug is contraindicated in patients suffering from severe respiratory failure. The drug is not prescribed to women during pregnancy and breastfeeding, as well as to children under the age of 15 years. The drug should not be prescribed to patients whose work involves operating potentially dangerous machinery or driving a car. Pregnancy The drug is contraindicated for use during pregnancy. Use of the drug during pregnancy can lead to developmental disorders of the central nervous system in the child. If the drug was taken in the third trimester, especially immediately before the onset of labor, constant medical monitoring of the newborn is necessary, since withdrawal syndrome and disorders of the central nervous system in the newborn are possible. If it is necessary to use the drug during lactation, it is necessary to resolve the issue of interrupting breastfeeding.
Drug interactions The drug enhances the pharmacological effects of drugs that depress the central nervous system, including antiepileptic drugs, ethanol, antipsychotics and other hypnotics. With simultaneous use, the drug helps to reduce plasma concentrations of trimipramine.
Overdose
When using excessive doses of the drug, patients experience the development of symptoms of depression of the central nervous system, the severity of which depends on the dose of zopiclone taken. In case of an overdose of the drug, gastric lavage, intake of enterosorbents and symptomatic therapy are indicated. The specific antidote for zopiclone is flumazenil, a drug from the group of benzodiazepine receptor antagonists; the use of a specific antidote for the treatment of zopiclone poisoning is possible only in a hospital setting
Release form
Film-coated tablets, 10 pieces in a blister, 1 or 3 blisters in a cardboard package.
Storage conditions
It is recommended to store the drug in a dry place away from direct sunlight at a temperature not exceeding 25 degrees Celsius. Shelf life – 3 years. Attention! The description of the drug on this page is simplified. Before purchasing and using the drug, consult your doctor or pharmacist, and also read the instructions approved by the manufacturer. Information about the drug is provided for informational purposes only and should not be used as a guide to self-medication. ATTENTION! This section is provided for informational purposes only and is not a catalog or price list of our company. To obtain information about the availability of drugs, call + 99871 202 0999 Pharmacy Network Helpline 999.
Sonnat tablets p/o 7.5 mg No. 10x3
Name
Sonnat tablet 7.5 mg No. 30
Description
Film-coated tablets are light yellow in color with an orange tint, round in shape with a biconvex surface, with the inscription “KMP” on one side of the tablet. A white core is visible on the transverse fault.
Main active ingredient
Zopiclone
Release form
10 tablets in blister packs, 1 or 3 blister packs along with instructions for use are placed in a pack.
Dosage
7.5 mg No. 30
Pharmacodynamics
Zopiclone is a member of a new class of psychotropic drugs, the cyclopyrrolones, which are structurally different from benzodiazepines and barbiturates. The sedative-hypnotic effect of zopiclone is due to its high affinity for binding sites on the GABA receptor complex in the central nervous system. Zopiclone prolongs sleep duration, improves sleep quality and reduces the number of night awakenings, while maintaining normal sleep phase structure and without reducing the proportion of REM sleep.
Pharmacokinetics
Absorption Zopiclone is rapidly absorbed: peak plasma concentrations are reached after 1.5-2 hours and are 30, 60 and 1.15 ng/ml after administration of 3.75 mg, 7.5 mg and 15 mg, respectively. Bioavailability is about 80%. Absorption is not affected by repeated administration, weight or gender of the patient. Distribution Zopiclone is very quickly distributed from the vascular bed. Plasma protein binding is low (about 45%) and far from saturation. The risk of drug interactions due to substitution at the protein binding site is very low. Decrease in plasma concentration: between 3.75 mg and 15 mg, and this process is not dose dependent. The half-life is approximately 5 hours. Benzodiazepines and related compounds cross the blood-brain barrier and placenta and are excreted into breast milk. During breastfeeding, the pharmacokinetic profiles of zopiclone in maternal milk and plasma are similar. The estimated percentage of the dose consumed by the infant does not exceed 0.2% of the dose received by the mother in 24 hours. Metabolism Zopiclone is extensively metabolized in the liver. The two main metabolites are the N-oxide (pharmacologically active in animals) and the N-demethylated derivative (pharmacologically inactive in animals). Their apparent half-lives, determined from urinary excretion studies, are approximately 4.5 and 7.5 hours, respectively. This is consistent with the fact that after repeated doses (15 mg) for 14 days there is no significant accumulation. During the studies, there was no increase in enzymatic activity in animals, even when administered in high doses. Elimination The low renal clearance of unchanged zopiclone (average 8.4 ml/min), compared with plasma clearance (232 ml/min), indicates that zopiclone is excreted from the body mainly in the form of metabolites. Approximately 80% of the substance is excreted by the kidneys in the form of free metabolites (N-oxide and N-demethylated derivative), and about 16% in feces. Particular risk groups: Elderly patients: Although hepatic metabolism is slightly reduced and the half-life is 7 hours, multiple studies have not shown that zopiclone accumulates in plasma after repeated dosing. Patients with renal failure: with long-term use of the drug, no accumulation of zopiclone and its metabolites was observed. Zopiclone penetrates dialysis membranes. When treating overdose, hemodialysis is not appropriate because zopiclone has a large volume of distribution. Patients with liver cirrhosis: The clearance of zopiclone is significantly reduced due to delayed demethylation, so dose adjustment is necessary in these patients.
Indications for use
For the treatment of short-term insomnia in adults (including difficulty falling asleep, waking up at night and early). For maintenance treatment of chronic insomnia, using for a limited period of time. Zopiclone is prescribed only in cases where sleep disturbances are severe and limit the patient's activity or cause extreme distress.
Directions for use and doses
Use internally. Treatment should begin with the minimum effective dose. Depending on the effectiveness and tolerability of the drug, the dose may be increased in the future. The daily dose of Sonnat should not exceed 7.5 mg (1 tablet). The drug should be taken immediately before bedtime. Recommended daily dose of Sonnat: adults under 65 years of age - 1 tablet. The Sonnat tablet cannot be divided into two halves, therefore, if it is necessary to reduce the dose to 3.75 mg (adults over 65 years of age and in other exceptional cases), it is necessary to use zopiclone preparations from other manufacturers. The duration of therapy for situational insomnia is 2-5 days, temporary - 2-3 weeks. The duration of treatment may be increased according to the doctor's decision, but should not exceed 4 weeks (including the period of gradual dose reduction). 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 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. Use in special categories of patients: Patients over 65 years of age: the drug is not recommended to be used at this dosage (see section “Contraindications”), Patients with renal, hepatic and respiratory failure: the drug is not recommended to be used at this dosage (see section “Contraindications” ). Children: Zopiclone is contraindicated. If you miss another dose of the drug, do not use a double dose to replace the missed dose. Continue taking as recommended by your doctor.
Use 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. Children. Zopiclone is not used in children.
Precautionary measures
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. 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: exceeding the recommended dose of zopiclone (7.5 mg); 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 suddenly stopping the drug can 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 the drug lasts no more than 4 weeks, the likelihood of developing withdrawal symptoms is minimal. It is recommended to discontinue the drug gradually. Rebound insomnia. As an exacerbation of insomnia, which was tried to be treated with benzodiazepines or their derivatives, transient rebound insomnia may develop. Amnesia and altered psychomotor function. “For several hours after taking the pill, anterograde amnesia and changes in psychomotor function may occur. To reduce the risk of their development, the patient should take the tablet immediately before bedtime 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) and memory and behavior disorders: exacerbation of insomnia, nightmares, agitation, nervousness, delusions, hallucinations, oneiric state, confusion, psychosis-like symptoms, euphoria, irritability , anterograde amnesia, suggestibility. These symptoms may be accompanied by disorders that are potentially harmful to the patient or others: abnormal behavior, auto-aggression or aggression towards others, especially if family members or friends try to prevent the patient from doing what he wants, automatic behavior with subsequent amnesia. The appearance of these symptoms requires cessation of treatment. Somnambulism and related behavior. Patients who took zopiclone and did not fully wake up experienced somnambulism and other types of similar behavior, when the patient, while sleeping, drives a car, prepares and eats food, makes phone calls, has sexual intercourse, after which he does not remember anything. The use of alcohol and other CNS depressants with zopiclone increases the risk of behavioral disorders that occur when zopiclone is used in doses that exceed the maximum recommended dose. For patients who develop such behavioral disturbances, it is strongly recommended that they stop taking zopiclone. Risk of drug accumulation. Benzodiazepines and their derivatives (just like any other drug) remain in the body for a certain time, which is approximately 5 half-lives. In elderly patients and patients with impaired liver function, the half-life may be significantly longer. After repeated doses, 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. During clinical studies in patients with renal failure, no accumulation of zopiclone was observed. 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 should be reduced by 2 times. 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 who have a history of alcoholism or other types of dependence on drugs or other substances. 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 clearly established and 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 or 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. Other psychiatric and paradoxical reactions: During treatment with zopiclone, paradoxical reactions have been reported in some patients, mostly elderly: increased insomnia, nightmares, anxiety, agitation, irritability, aggressiveness, attacks of anger, delirium, hallucinations, oneiric delirium, confusion, psychotic symptoms, inappropriate behavior and other behavioral disorders. If such reactions occur, Sonnat is discontinued.
Interaction with other drugs
Undesirable combinations. Alcohol potentiates the sedative effect of benzodiazepines and related substances. Due to reduced concentration, driving a vehicle and operating machinery can be dangerous. Patients should avoid drinking alcoholic beverages or taking medications that contain alcohol. Combinations that require precautions. Rifampicin. A decrease in plasma concentrations and a decrease in the effectiveness of zopiclone due to increased metabolism in the liver. Monitoring of the patient's clinical condition is necessary. If necessary, another sleeping pill may be prescribed. Combinations to consider. Other drugs that depress the activity of the central nervous system: morphine derivatives (analgesics, antitussives and drugs for substitution therapy in the treatment of drug addiction, except buprenorphine), antipsychotics, barbiturates, anxiolytics, other hypnotics, sedative antidepressants, sedative H1-antihistamines, antihypertensives central action, baclofen, thalidomide, pizotifen. Increased inhibition of central nervous system activity. Due to reduced concentration, driving a vehicle and operating machinery can be dangerous. In addition, with simultaneous use of zopiclone with morphine derivatives (analgesics, antitussives and drugs for substitution therapy in the treatment of drug addiction) and barbiturates, the risk of respiratory depression increases, which can be fatal in case of overdose. Buprenorphine. When buprenorphine is used as replacement therapy for drug addiction, there is an increased risk of respiratory depression, which can potentially be fatal. The risk/benefit of using this combination must be carefully weighed. Patients should be warned to strictly adhere to the doses prescribed by the doctor. Clozapine. Increased risk of collapse with respiratory arrest and/or cardiac arrest. Clarithromycin, erythromycin, telithromycin. Slight increase in the sedative effects of zopiclone. Ketoconazole, itraconazole, voriconazole. Slight increase in the sedative effects of zopiclone. Nelfinavir, ritonavir. Slight increase in the sedative effects of zopiclone.
Contraindications
Hypersensitivity to any component of the drug. Liver failure (risk of developing encephalopathy), renal and respiratory failure. Sleep apnea syndrome. Myasthenia. Childhood. Age over 65 years. Congenital galactosemia; glucose/galactose malabsorption syndrome or lactase deficiency. Pregnancy and breastfeeding.
Compound
1 tablet contains: Active ingredient: zopiclone - 7.5 mg; Excipients: povidone, talc, lactose monohydrate (tablettose-80), microcrystalline cellulose, calcium stearate, coating mixture “Opadry II Yellow” 33G22507 (triacetin, hypromellose, lactose monohydrate, titanium dioxide (E 171), polyethylene glycol, yellow iron oxide (E 172)).
Overdose
Symptoms: confusion, lethargy, drowsiness, ataxia, muscle weakness, hypotension, respiratory depression, coma. Overdose can be fatal, especially in cases of simultaneous overdose of multiple central nervous system depressants (including alcohol). Treatment: induce vomiting (if the overdose occurred no more than 1 hour ago), gastric lavage with respiratory protection, then take activated charcoal. Hemodialysis is ineffective. Careful monitoring of cardiac and respiratory functions is necessary. Administration of flumazenil, which has the opposite effect of zopiclone and may cause neurological disorders (seizures), may be helpful.
Side effect
The most common side effect when using the drug 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
Storage conditions
In original packaging to protect from light and moisture at temperatures not exceeding 25 °C. Keep out of the reach of children.
