Producer: JSC VEROPHARM Russia
Code of automatic telephone exchange: N05CF01
Release form: Firm dosage forms. Tablets.
General characteristics. Structure:
Active agent: 0,0075 g of a zopiklon. Excipients: cellulose microcrystallic, silicon dioxide colloid (aerosil), lactose (sugar milk), примогель (sodium carboxymethylstarch), potato starch or starch corn, magnesium stearate, oksipropilmetiltsellyuloz or oksipropiltsellyuloza, talc, polyvinylpirrolidone (povidone), polyethyleneglycol 4000, titanium dioxide.
Zopiklon is a hypnagogue from group of the tsiklopirrolon structurally different from benzodiazepines and barbiturates. It has the following pharmacological properties: somnolent, sedative, tranquilizing, anticonvulsant and myorelaxation. These effects are connected with its action on TsNS receptors relating to the GAMK macromolecular complex, modulating opening of channels for chlorine ions therefore there is strengthening of brake influence of GAMK and braking of interneural transfer in various departments of TsNS. Zopiklon has property to shorten time before backfilling and to urezhat the frequency of night awakenings, to increase duration of a dream and to improve quality of a dream and awakening. Practically does not cause postsomnichesky disturbances: there are no feelings of weakness and drowsiness for morning of the next day. Accustoming to somnolent effect of drug is absent during the long period of treatment, up to 17 weeks.
Absorption Zopiklon is quickly soaked up. The maximum concentration in a blood plasma are reached within 1,5–2 hours and make about 30 and 60 ng/ml after intake of 3,75 mg and 7,5 mg respectively. Absorption of drug does not depend on a floor, and also meal. Communication with proteins of a blood plasma makes about 45%.
Metabolism After repeated purposes of cumulation of a zopiklon and its metabolites does not happen. Interindividual differences insignificant. The main metabolites are derivative N-oxide and N-desmetilovy a metabolite. The elimination half-life makes about 4,5 and 7,4 hours respectively. In the recommended doses the elimination half-life of not changed zopiklon makes about 5 hours. With urine зопиклон it is removed (about 80%), mainly, in the form of metabolites, with a fecal masses about 16% are removed. Separate groups of patients 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 drug in plasma was not revealed even at repeated appointment. Patients with a renal failure have cumulation of a zopiklon or its metabolites it was not revealed even after long reception. At patients with cirrhosis the clearance of a zopiklon decreases approximately by 40% according to demethylation process reduction.
Indications to use:
Treatment of passing, situational and chronic sleeplessness at adults of various etiology (including difficulties with backfilling, night and early awakenings).
Route of administration and doses:
Treatment has to be whenever possible short and not exceed four weeks. Lengthening of terms of treatment from above the most admissible is carried out after repeated assessment of a condition of the patient. Drug is accepted before going to bed.
Passing sleeplessness: from 2 to 5 days.
Situational sleeplessness: from 2 to 3 weeks.
Chronic sleeplessness: duration of course treatment is defined after consultation with the specialist.
The recommended dose for adults — 7,5 mg (1 tablet). The maximum dose makes 15 mg. Treatment of elderly patients and patients with the broken function of a liver or chronic pulmonary insufficiency begin 3,75 mg (½ tablets) with a dose and, if necessary, increase up to 7,5 mg. Though in cases of a renal failure of cumulation of a zopiklon and its metabolites it was not revealed, at such patients recommend to begin treatment with a dose of 3,75 mg.
Features of use:
At patients with night attacks of bronchial asthma in combination with drugs of a metilksantinovy row (theophylline) зопиклон urezhat asthma attacks in early hours at dawn, reduces their intensity and duration. At purpose of a zopiklon it is necessary to remember that though the risk and is minimum, but it is absolutely impossible to exclude development of accustoming to drug and abuse of Risk of dependence or abuse arises in cases: disturbances of a dose and duration of treatment; alcohol abuses and/or ekarstvenny means; sharing with alcohol or other psychotropic drugs. Ricochet sleeplessness and a syndrome of "cancellation" Risk of such phenomena after the sharp termination of a zopiklon cannot be excluded, especially after prolonged treatment. Therefore recommend to reduce gradually a dosage and to notify on it the patient.
Amnesia. The ecmnesia can meet, especially at interruption of a dream or after a considerable period between administration of drug and withdrawal to a dream. It is necessary for decrease in risk of manifestation of an ecmnesia: to take a pill just before a dream; to provide dream duration not less than 6 hours.
Depression. Drug is not shown for treatment of a depression, and can even mask its symptoms.
Use at children. The safe and effective dose of a zopiklon was not established at children and young people to 18 years.
Influence on ability to driving and management of transport. Because of the pharmacological properties зопиклон can exert adverse impact on ability to driving and management of transport, and also on occupations of other potentially dangerous types of activity requiring special attention and speed of psychomotor reactions therefore during treatment it is necessary to be extremely careful or to abstain from activity of this sort.
The most frequent side effect observed at purpose of a zopiklon — bitter taste in a mouth, can also be: dizziness, a headache, residual drowsiness after awakening; digestive disturbances: dyspepsia, nausea, dryness in a mouth; allergic skin reactions like an itch and rashes, extremely seldom meet angioneurotic and anaphylactic reactions. Mental and paradoxical reactions Seldom: nightmares, irritability, confusion, hallucinations, aggression, confusion of consciousness, the suppressed mood, a lack of coordination of movements, a depression, inadequate behavior with possible development of amnesia (see. "Special instructions"). After the treatment termination the syndrome of "cancellation" and ricochet sleeplessness in rare instances can be observed (see. "Special instructions"). Isolated cases of slight increase in blood serum of transaminases and/or an alkaline phosphatase were celebrated.
Interaction with other medicines:
The concomitant use with alcohol as sedation of a zopiklon can amplify is not recommended. Strengthening of the oppressing influence on the central nervous system can meet in co-administration cases neuroleptics, hypnagogues, tranquilizers, sedatives, antidepressants, narcotic analgetics, antiepileptic drugs, anesthetics, antihistaminic drugs with sedation, and also erythromycin. Administration of drug reduces concentration of a trimipramin in plasma.
Hypersensitivity to a zopiklon or other components of drug; heavy myasthenia; the expressed respiratory insufficiency; heavy liver failure; syndrome of a "night" apnoea; pregnancy and period of breastfeeding; age up to 18 years. Pregnancy and a lactation is not recommended to use drug during pregnancy and to appoint to nursing mothers.
The overdose is usually shown in the form of symptoms of various extent of oppression of the central nervous system from drowsiness to a coma, depending on amount of the accepted drug. First aid consists in a gastric lavage, reception of absorbent carbon. If necessary the symptomatic and maintenance therapy in the conditions of a hospital is recommended. Special attention should be paid to respiratory and cardiovascular functions. The hemodialysis has the small importance because of the large volume of distribution of a zopiklon. Flumazenil can be used as an antidote.
Period of validity 3 years. Not to use drug after the expiry date specified on packaging. List B. In dry, protected from light and the place, unavailable to children.
According to the recipe
On 5 or 10 tablets in a blister strip packaging. On 5 or 20 tablets in bank of orange glass. Each can or on 1 or 2, either 3, or 4 blister strip packagings together with the application instruction place in a pack from a cardboard.