Somnol - instructions for use, dose, side effects, contraindications

Active substanceZopicloneZopiclone

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Dosage form: & nbspFilm-coated tablets.

Composition:

One tablet contains:

active substance: zopiclone 7.5 mg;

Excipients: calcium hydrophosphate, anhydrous - 152.3 mg; potato starch, dried - 4.25 mg; Magnesium stearate - 1.7 mg, sodium carboxymethyl starch - 1.7 mg, silicon dioxide - 2.55 mg;

shell: Opaque white (hypromellose - 40,000%, lactose monohydrate - 24,000%, macrogol 3000 - 22,000%, titanium dioxide - 8,000%, triacetin - 6,000%) - 2,6 mg.

Description:

Round biconvex tablets covered with a white film membrane, with a risk on one side, on the cross section the nucleus is white.

Pharmacotherapeutic group:Sleeping pills.

ATX: & nbsp

N.05.C.F.01 Zopiclone

Pharmacodynamics:

Zopiclone is a hypnotic of a group of cyclopyrrolons structurally different from benzodiazepines and barbiturates. It has the following pharmacological properties: hypnotic, sedative, tranquilizing,

anticonvulsant and muscle relaxant. These effects of zopiclone are associated with a specific agonistic effect on the central nervous system (CNS) receptors,related to the macromolecular complex GABA-omega, modulating the opening of neuronal channels for chloride ions.

Zopiclone has the property of decreasing the time of falling asleep and the frequency of night and early awakenings, increasing the duration of sleep and improving the quality of sleep and awakening. These effects are combined with a characteristic electroencephalographic profile, which differs from that recorded when taking benzodiazepines. With insomnia zopiclone reduces the I phase, prolongs the II phase of sleep and preserves or prolongs the stages of deep sleep (III and V) and paradoxical (fast) sleep. Sleep occurs within 30 minutes and lasts 6-8 hours.

The use of zopiclone for 4 weeks does not cause significant ricochet insomnia, as well as the avoidance of hypnotic effect (with admission for up to 17 weeks).

Pharmacokinetics:

Absorption

After oral administration zopiclone quickly and completely absorbed in the gastrointestinal tract. The maximum plasma concentrations are achieved within 1.5-2 hours and are approximately 30 ng / ml and 60 ng / ml after ingestion of 3.75 mg and 7.5 mg, respectively. Absorption of zopiclone does not depend on sex, nor on food intake. Distribution

Linkage to blood plasma proteins is weak (about 45%) and unsaturated. The risk of interaction with other drugs at the level of communication with protein is very low. Zopiclone quickly distributed from the systemic blood flow. The volume of distribution is 91.8-10.4 liters. Zopiclone easily passes through the blood-brain barrier.

The concentrations of zopiclone in breast milk are similar to those in plasma. The intake of zopiclone in the baby's body, along with breast milk, does not exceed 1% of the dose taken by the mother within 24 hours.

Metabolism

After repeated applications, the cumulation of zopiclone and its metabolites does not occur. Individual differences are insignificant.

The main metabolites are the N-oxide derivative (pharmacologically active) and the N-demethyl metabolite (pharmacologically inactive). The half-life is approximately 4.5 and 7.4 hours, respectively.

Excretion

At recommended doses, the half-life of unchanged zopiclone is approximately 5 hours. Low values of renal clearance of unchanged zopiclone (8.4 ml / min) in comparison with its plasma clearance (232 ml / min) indicate that zopiclone clearance is predominantly metabolic.

With urine zopiclone is excreted (approximately 80%), mainly in the form of metabolites, approximately 16% is excreted with the feces.

Individual groups of patients

In elderly patients: despite a slight decrease in the metabolism in the liver and an elongation of the half-life to about 7 hours, the cumulation of zopiclone in plasma was not detected even after repeated use.

In patients with renal insufficiency: the cumulation of zopiclone or its metabolites was not detected even after long-term administration.

In patients with cirrhosis: in connection with the decrease in the demethylation process by about 40 % the plasma clearance of zopiclone decreases, so a dose adjustment is necessary.

Indications:

Treatment of transient, situational and chronic insomnia in adults (including difficulties with falling asleep, night and early awakenings).

Contraindications:

Hypersensitivity to zopiclone or to any component of the drug,
severe respiratory failure,
severe pseudo-paralytic myasthenia gravis (myasthenia gravis),
severe acute and chronic hepatic insufficiency,
syndrome of "sleepy" apnea,
congenital intolerance to galactose, deficiency of Lapp lactase, malabsorption of glucose-galactose,
period of lactation,
age to 18 years.

Carefully:

Persons with alcoholic, narcotic or drug dependence in history, patients who simultaneously take alcohol or other psychotropic drugs (increased risk of dependence or abuse).

Pregnancy and lactation:

Pregnancy

Because of the lack of clinical data and precaution in the first 3 months of pregnancy, zopiclone is not recommended. If you still need to apply zopiclone in the last 3 months of pregnancy, whenever possible, the minimum effective dose should be used. The use of zopiclone in the last trimester of pregnancy can cause newborn signs of hypothermia, hypotension, respiratory depression and drowsiness. During the first days of life, abstinence syndrome may manifest.

If zopiclone is prescribed for women of reproductive age, patients should be warned about the need to see a doctor to decide whether to stop using the medicine if pregnancy is suspected or planned.

Breastfeeding period

It is known that zopiclone excreted in breast milk.Its use by a nursing mother can cause sedation in the child (weakness, decreased tone). Therefore, during the period of breastfeeding, the use of Somolol should be discontinued.

Dosing and Administration:

Inside.

Treatment should be as short as possible and not exceed 4 weeks, including the period of dose reduction. Prolongation of the duration of treatment beyond the maximum allowable is carried out after a second assessment of the patient's condition. Treatment should always begin with the lowest effective dose and never exceed the maximum dose. The drug should be taken immediately before going to sleep at night.

Recommended doses

Adults under the age of 65 years - 1 tablet 7.5 mg once a day.

Patients with impaired renal function treatment is recommended to begin with a dose of 3.75 mg (½ tablets) once a day, although the cumulation of zopiclone or its metabolites in cases of renal failure is not noted.

Patients with impaired hepatic function treatment is started with a dose of 3.75 mg once a day, as the elimination of the drug in this group of patients is reduced. If necessary, the dose can be carefully increased to 7.5 mg once a day, taking into account the patient's sensitivity.

Patients with respiratory failure appoint 3.75 mg once a day. Treatment elderly patients over 65 years begin with a dose of 3.75 mg once a day. If necessary, the dose can be gradually increased, taking into account the individual sensitivity of the patient.

In all cases, the daily dose should not exceed 7.5 mg.

Duration of treatment

Transient insomnia: 2 to 5 days.

Situational insomnia: 2 to 3 weeks.

Chronic insomnia: the duration of the course of treatment is determined after consultation with a specialist.

Side effects:

The most frequent side effect observed with zopiclone administration is a bitter or metallic taste in the mouth. Also can be observed:

digestive disorders: indigestion, nausea, dry mouth,
on awakening: drowsiness, dizziness, headache, depression, aggressiveness, anterograde amnesia, euphoria and impaired coordination of movements,
psychic and paradoxical reactions: nightmares, confusion, hallucinations and behavioral changes, for example, irritability, confusion, depressed mood, inadequate behavior that may be associated with amnesia, somnambulism (sleeping), and libido.These side effects are more common in the elderly, but are rarely severe.
allergic skin reactions (itching, rashes), anaphylactic reactions and / or angioedema,
a slight increase in serum levels of transaminase and / or alkaline phosphatase activity.

When therapy is stopped, ricochet insomnia may arise (frequent awakening, the resumption of insomnia or its enhancement) or the emergence of drug dependence, but usually after a prolonged use. In very rare cases, cramps are possible.

Overdose:

Symptoms

Overdose of Somnol usually manifests itself in the form of symptoms of varying degrees of CNS depression from drowsiness to coma, depending on the amount of the drug taken. In mild cases, symptoms are expressed in drowsiness, confusion, apathy. In more serious cases, symptoms can be expressed in ataxia, lethargy, hypotension, respiratory depression and coma. Rarely, an atrioventricular block. Usually this CNS depression does not threaten the patient's life. However, with the simultaneous use of Somnol with alcohol or other agents that exert a depressing effect on the central nervous system, an overdose can be severe and life-threatening to the patient.Other risk factors, such as concomitant disease and a weakened patient, can exacerbate symptoms and even (very rarely) lead to death.

Treatment

Take activated charcoal, rinse stomach for 1 hour after an overdose. In the case of severe CNS depression flumazenil can be used as an antidote (not used in case of a combined overdose with other drugs and as a diagnostic tool in case of an overdose of unknown drugs for the formulation or elimination of the diagnosis of benzodiazepine intoxication). If necessary, symptomatic and supportive therapy in a hospital is recommended. It is necessary to control the vital functions of the body (respiratory, cardiovascular). Hemodialysis is of low significance because of the large volume distribution of zopiclone.

Interaction:

It is not recommended simultaneous reception with alcohol, since alcohol increases the sedative effect of Somnol.

Strengthening the oppressive effect on the central nervous system can occur in cases of concomitant administration with antipsychotic (neuroleptic) drugs, hypnotics,tranquilizers, sedatives, antidepressants, narcotic analgesics, anticonvulsants, anesthetics, as well as H1-histamine receptor blockers that have a sedative effect. Before the joint use of Somnol with these drugs should be carefully weighed the expected therapeutic effect.

Somnol reduces the concentration of trimipramine in the plasma and its effect.

Joint use of drugs similar to benzodiazepine derivatives and narcotic analgesics, including opiates and morphine derivatives (painkillers, cough suppressants and replacement therapy), can lead to increased euphoria and increased risk of drug dependence.

Clozapine may increase the risk of shock with stopping breathing and / or heart failure.

Joint use of Somnol with narcotic analgesics and barbiturates can cause the risk of respiratory depression. In case of an overdose, a lethal outcome is possible.

The action of drugs similar to benzodiazepine derivatives is enhanced if they are used in combination with inhibitors of hepatic enzymes, especially cytochrome P450 (for example, with antibiotic erythromycin, antifungals and itraconazole, ketoconazole).

However, the simultaneous use of carbamazepine, phenytoin or rifampicin (increase the activity of liver enzymes) reduces the therapeutic effect of Somnol.

Special instructions:

Capsules of Somolol tablets contain a dye, which includes lactose, so patients with a rare congenital intolerance to galactose, a deficit Lapp lactase or malabsorption of glucose-galactose, this medication can not be administered.

Patients with impaired liver or kidney function, as well as elderly people over 65 years of age and patients with respiratory failure, Somnol are used with caution (dose reduction is recommended) (see section Method of administration and dose). Always whenever possible, you should find out the cause of insomnia and before prescribing a hypnotic, you must eliminate the possible factors that cause it. Benzodiazepines and their analogs are not the first choice drugs in the treatment of psychoses.

The risk of dependence

To avoid possible development of drug dependence treatment course should not exceed 4 weeks.

Although the risk is minimal, it is impossible to completely exclude the development of addiction to the drug and its abuse.The risk of dependence or abuse arises in the following cases:

exceeding the dose and increasing the duration of treatment,
abuse of alcohol and / or other medicines,
application with alcohol or other psychotropic drugs,
presence of anxiety.

When prescribing a drug to patients with a history of excessive alcohol use and / or dependence on medicines and patients with personality changes, it should be borne in mind that the risk of dependence development is increased. These patients must be closely monitored.

The syndrome of "cancellation" and ricochet insomnia

The risk of such phenomena after a sharp cessation of zopiclone application can not be ruled out, especially after long-term treatment. Therefore, it is recommended to gradually reduce the dose and notify the patient about it.

If a patient becomes physically dependent on this drug, a sudden discontinuation of its use can lead to the development of the "withdrawal" syndrome, characterized by the following symptoms: insomnia, headache, muscle pain, anxiety, tension, agitation, impaired consciousness and irritability.

In more severe cases, the following symptoms can occur: impairment of perception of reality, depersonalization, loss of sensitivity and numbness of the limbs, increased sensitivity to noise, light and physical contact, hallucinations and epileptic seizures. If the duration of treatment does not exceed 4 weeks, the appearance of symptoms of "cancellation" when discontinuing the use of the drug is unlikely. Nevertheless, a gradual cessation of treatment is recommended.

When discontinuation of the drug may develop a transient syndrome of ricochet insomnia with increased resumption of symptoms, because of which treatment was started; often it is a severe insomnia in combination with one of the symptoms of "withdrawal" mentioned above. This syndrome is mainly manifested with sudden discontinuation of long-term therapy or with the use of doses exceeding the recommended doses. Therefore, sudden discontinuation of the drug should be avoided, its dose should be reduced gradually, informing the patient about the possible occurrence and measures to prevent the development of ricochet insomnia.

Amnesia

Anterograde amnesia can occur if, after taking the pill in the evening, the patient still wakes up at night or can not fall asleep, or in case a delay to bedtime is postponed. To reduce the risk of anterograde amnesia:

take the pill just before bedtime,
ensure a sleep duration of at least 7-8 hours.

Depression

The drug is not indicated for the treatment of depression and can even mask its symptoms. If insomnia is associated with depression, then before using Somnol it must be prevented. Somnol can not be used in monotherapy to treat depression and anxiety caused by it, as they can induce suicide.

Other psychic and paradoxical reactions

Some patients may experience paradoxical reactions during the use of benzodiazepines and their analogues:

increased insomnia and nightmares,
nervousness, irritability, agitation, aggressiveness and attacks of anger,
delirium, hallucinations, onyric delirium, psychotic symptoms, inadequate behavior and other behavioral disorders.

These symptoms are most likely to occur in the elderly. If this occurs, therapy should be discontinued.

Sleepwalking and related behavior

Patients who took zopiclone and did not fully awake, there was a note of drift and other similar behavior, for example, "driving a car", cooking and eating or talking on the phone followed by amnesia of such behavior. The use of alcohol and other drugs depressing the central nervous system simultaneously with zopiclone increases the risk of such behavior, as well as the use of zopiclone in doses exceeding the maximum recommended dose. Termination of therapy in patients who report such behavior should be strictly weighed.

Use in children

The effectiveness and safety of zopiclone in children under the age of 18 years have not been established.

Effect on the ability to drive transp. cf. and fur:

Since Somnol belongs to the group of sedatives that cause drowsiness, after taking the drug should refrain from driving vehicles or performing the work of the operator of various devices and mechanisms.

Form release / dosage:

Tablets, film-coated 7.5 mg.

Packaging:

For 10 tablets in a planar cell box made of aluminum foil and a polyvinylchloride film with a polyvinylidene chloride coating.

For 1 or 2 contour cell packs, along with the instructions for use are placed in a pack of cardboard.

Storage conditions:

List No. 1 of the strong BACC substances.

Store in a dry, dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N011747 / 01

Date of registration:12.07.2011

The owner of the registration certificate:GRINDEX, JSC GRINDEX, JSC Latvia

Manufacturer: & nbsp

Grindeks, JSC Latvia

Representation: & nbspGrindeks Rus, Open CompanyGrindeks Rus, Open CompanyRussia

Information update date: & nbsp16.10.2015

Illustrated instructions

Instructions

Somolol® (Somnol®)