Сомнол®
Producer: AS Grindex (JSC Grindeks) Latvia
Code of automatic telephone exchange: N05CF01
Release form: Firm dosage forms. Tablets.
General characteristics. Structure:
Active ingredient: 7,5 mg of a zopiklon.
Excipients: calcium hydrophosphate the anhydrous, potato starch which is dried up of magnesium stearate, sodium starch glikolit, silicon dioxide, dye 33G 28707 Opadry.
Pharmacological properties:
Pharmacodynamics. Somnolent drug, derivative tsiklopirrolona. Possesses somnolent, sedative, tranquilizing, anticonvulsant and myorelaxation action. This action spectrum is connected with influence of a zopiklon on TsNS receptors relating to the macromolecular GABA complex and modulation of opening of channels for chlorine ions.
Zopiklon has ability to reduce time of backfilling and frequency of night and early awakenings, increases dream duration, promotes improvement of quality of a dream and awakening.
These effects are combined with a characteristic elektroentsefalografichesky profile which differs from that, registered at reception benzodiazepines. At sleeplessness зопиклон reduces the I phase, prolongs the II phase of a dream and keeps or prolongs stages of a deep sleep (III and V) and a paradoxical (bystry) dream. The dream comes within 30 min. and proceeds 6-8 h.
Use of a zopiklon within 4 weeks does not cause significant ricochet sleeplessness, and also an uskolzaniye of somnolent effect (at reception during up to 17 weeks).
Drug belongs to the list No. 1 of strong substances PKKN.
Pharmacokinetics. After intake зопиклон it is quickly and completely soaked up from a GIT. The maximum concentration in a blood plasma are reached within 1,5-2 h and make about 30 ng/ml and 60 ng/ml after intake of 3,75 mg and 7,5 mg respectively. Absorption of a zopiklon does not depend on a floor, and also on meal.
Linkng with proteins of a blood plasma is weak (makes about 45%) and not saturable. The risk of interaction with other drugs at the level of communication with protein is very low. Zopiklon is quickly distributed from a system blood-groove. The volume of distribution makes 91,8-10,4 liters. Zopiklon easily passes through GEB.
Concentration of a zopiklon in breast milk are similar to that in plasma. Receipt of a zopiklon in the child's organism together with breast milk does not exceed 1% of the dose accepted by mother during 24 h.
After repeated uses cumulation of a zopiklon and its metabolites does not happen. Interindividual differences insignificant.
The main metabolites are derivative N - oxide (pharmacological active) and N-demetilovy a metabolite (pharmacological inactive). The elimination half-life makes about 4,5 and 7,4 hours respectively. Removal
In the recommended doses the elimination half-life of not changed zopiklon makes about 5 hours. Low values of renal clearance of not changed zopiklon (8,4 ml/min.) in comparison with its plasma clearance (232 ml/min.) indicate that the clearance of a zopiklon is preferential metabolic.
With urine зопиклон it is removed (about 80%) mainly in the form of metabolites, with a fecal masses about 16% are removed.
At elderly patients: despite small decrease in metabolism in a liver and lengthening of an elimination half-life approximately till 7 o'clock, cumulation of a zopiklon in plasma was not revealed even at repeated use.
At patients with a renal failure: cumulation of a zopiklon or its metabolites was not revealed even after long reception.
At patients with cirrhosis: in connection with demethylation process reduction approximately the plasma clearance of a zopiklon therefore dose adaptation is necessary decreases by 40%
Indications to use:
– treatment of passing or situational sleeplessness;
– short-term treatment of chronic sleeplessness (including as a result of mental disturbances).
Route of administration and doses:
Somnol accept inside.
The adult appoint 7,5 mg (1 таб.) shortly before a dream.
To patients with a renal failure treatment is recommended to begin 3,75 mg with a dose though cumulation of drug at this category of patients is noted.
To patients with an abnormal liver function treatment is recommended to begin 3,75 mg as removal of drug at this group of patients is reduced with a dose. In case of need it is possible to increase a dose carefully to 7,5 mg taking into account sensitivity of the patient.
To patients of advanced age at the beginning drug appoint 3,75 mg in a dose. In case of need the dose can be increased gradually taking into account sensitivity of the patient.
Features of use:
At use Somnola, as well as at purpose of other hypnagogues with sedation (including derivatives of benzodiazepine, barbiturates), development of mental and physical (somatic) dependence is possible. The risk of development of dependence is minimum if duration of treatment does not exceed 4 weeks, but increases at increase in a dose and duration of administration of drug.
At purpose of drug to patients with changes of the personality, existence in the anamnesis of instructions on the excessive use of alcoholic drinks and/or dependence on medicines, it must be kept in mind that the risk of development of dependence at them is increased.
At the termination of reception of Somnol passing, quite often heavy sleeplessness in combination with one of the cancellation symptoms mentioned above can renew. Therefore it is necessary to avoid the sudden termination of administration of drug.
To carry out cancellation gradually.
If according to recommendations drug is used by no more than 4 weeks, development of accustoming is improbable.
If after reception of a tablet of Somnol before going to bed the patient cannot fall asleep or wakes up at night, development of an ecmnesia is possible.
During treatment it is necessary to avoid alcohol intake.
Somnol has sedative effect and causes drowsiness. Therefore after administration of drug it is impossible to manage vehicles or to perform work of the operator of various devices and mechanisms.
Drug is not shown for treatment of a depression and can even mask its symptoms.
The safe and effective dose of a zopiklon was not established at children and young people to 18 years.
It is not recommended to use drug during pregnancy and to appoint to nursing mothers.
Side effects:
From the alimentary system: very often - bitter or metal taste in a mouth; perhaps - digestive disturbances (dyspepsia, nausea, dryness in a mouth), slight increase in blood serum of activity of transaminases and/or ShchF.
From a nervous system: perhaps when awakening - drowsiness, dizziness, a headache, a depression, aggression, an ecmnesia, euphoria and a lack of coordination of movements. Mental and paradoxical reactions - dreadful dreams, confusion, hallucinations and behavioural changes, for example, irritability, confusion of consciousness, the suppressed mood, inadequate behavior which, perhaps, is connected with amnesia noctambulation (lunacy), disturbance of a libido (these by-effects are more often observed at elderly people, but are heavy seldom).
Allergic reactions: skin itch, rash, anaphylactic reactions and/or Quincke's disease.
At the therapy termination: developing of ricochet sleeplessness (frequent awakening, resuming of sleeplessness or its strengthening) or emergence of medicinal dependence is possible, but usually it happens after prolonged use; very seldom - spasms.
Interaction with other medicines:
The concomitant use with alcohol since alcohol strengthens sedative action of Somnol is not recommended.
Strengthening of the oppressing influence on TsNS can meet in co-administration cases antipsychotic (antipsychotic) means, hypnotic drugs, tranquilizers, sedatives, antidepressants, narcotic analgetics, anticonvulsants, anesthetics, and also blockers histamine H1 receptors, possessing sedation. Before combined use of Somnol with these drugs it is necessary to weigh carefully expected advantage and risk of the carried-out therapy.
Somnol reduces concentration of a trimipramin in plasma and its effect.
Combined use of the drugs similar to benzodiazepine derivatives, and narcotic analgetics, including opiates and derivatives of morphine (analgeziruyushchy means, antitussives and therapy of replacement), can lead to strengthening of euphoria and increase in risk of development of medicinal dependence.
At simultaneous use with clozapine increase in risk of shock with an apnoea and/or hearts is possible.
Combined use of Somnol with narcotic analgetics and barbiturates can cause risk of respiratory depression. In case of overdose the lethal outcome is possible.
Effect of medicines, similar to derivatives of benzodiazepine, amplifies if they are applied in combination with inhibitors of liver enzymes, especially P450 cytochrome (for example, with an antibiotic erythromycin, antifungal drugs itrakonazoly, ketokonazoly).
However simultaneous use of carbamazepine, Phenytoinum or rifampicin (increase activity of liver enzymes) reduces therapeutic effect of Somnol.
Contraindications:
– heavy myasthenia (myasthenia gravis);
– heavy insufficiency of function of a liver;
– expressed to an apnoea during sleep;
– respiratory insufficiency;
– hypersensitivity to drug.
Somnol to children is not recommended to appoint.
Overdose:
Symptoms of various extent of oppression of TsNS from drowsiness to a coma, depending on amount of the accepted drug. In mild cases - drowsiness, confusion of consciousness, apathy; in more serious cases - an ataxy, a lethargy, hypotonia, respiratory depression and a coma. Seldom - AV blockade. Usually such oppression of TsNS does not threaten the patient's life.
However at combined use of Somnol with the alcohol or other means having the oppressing effect on TsNS, the overdose can be the heavy and life-threatening patient.
Other risk factors, such as associated disease and the weakened condition of the patient, can strengthen symptoms and even (very seldom) to lead to a lethal outcome.
Treatment: reception of absorbent carbon, a gastric lavage during 1 h after overdose. In case of the expressed oppression of TsNS flumazenit it is possible to apply as an antidote (not to use in case of the combined overdose with other medicines and as diagnostic means at overdose of unknown medicines for statement or an exception of the diagnosis of intoxication benzodiazepines). If necessary the symptomatic and maintenance therapy in the conditions of a hospital is recommended. Control of the vital functions of an organism is necessary (respiratory, cardiovascular). The hemodialysis is a little effective because of big Vd of a zopiklon.
Storage conditions:
Drug should be stored in the dry dark place at the room temperature, to keep in dry place and children.
Issue conditions:
According to the recipe
Packaging:
On 10 tablets in a blister strip packaging from PVC and aluminum. On 1 or 2 strip packaging in a cardboard box.
