Composition, form of production and packaging
The tablets covered with a film membrane of white color, round, biconcave.
Zopiclone 7.5 mg
[PRING] microcrystalline cellulose, silicon dioxide colloid (aerosil), lactose (milk sugar), sodium carboxymethyl starch (primogel), potato starch, magnesium stearate, povidone (polyvinylpyrrolidone), methyloxypropylcellulose, talc, macrogol 4000 (polyethylene glycol 4000), titanium dioxide.
10 pieces. - packings cellular planimetric (2) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2008.
Zopiclone is a hypnotic from 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 are associated with its effect on the CNS receptors related to the macromolecular complex of GABA, modulating the opening of the channels for chloride ions, resulting in an increase in the inhibitory effect of GABA and the inhibition of interneuronal transmission in various parts of the central nervous system.
Zopiclone has the property of shortening the time to sleep and reducing the frequency of nocturnal awakenings, increasing the duration of sleep and improving the quality of sleep and awakening. Virtually does not cause post-somnolent disorders: there is no feeling of weakness and drowsiness on the morning of the next day.
Adapting to the hypnotic effect of the drug is absent for a long period of treatment, up to 17 weeks.
Zopiclone is rapidly absorbed. C max in blood plasma are achieved within 1.5-2 h and are approximately 30 and 60 ng / ml after ingestion of 3.75 mg and 7.5 mg respectively. Absorption of the drug does not depend on sex, nor on food intake.
The connection with plasma proteins is approximately 45%.
After repeated administration of cumulation zopiclone and its metabolites do not occur. Individual differences are insignificant.
The main metabolites are the N-oxide derivative and the N-desmethyl metabolite. T 1/2 is approximately 4.5 and 7.4 hours, respectively.
In recommended doses, T 1/2 of unchanged zopiclone is approximately 5 hours. In the urine, zopiclone is excreted (approximately 80%), mainly in the form of metabolites, with a caloric mass of about 16%.
Individual groups of patients
In elderly patients, despite a slight decrease in metabolism in the liver and an elongation of T 1/2 to about 7 hours, no cumulation of the drug in the plasma was detected even after repeated administration.
In patients with renal insufficiency, cumulation of zopiclone or its metabolites was not detected even after prolonged use.
In patients with liver cirrhosis, the zopiclone clearance decreases by approximately 40%, in accordance with the decrease in the demethylation process.
- treatment of transient, situational and chronic insomnia in adults of different etiology (including difficulties with falling asleep, night and early awakenings).
Treatment should be as short as possible and not exceed four weeks. Elongation of treatment periods above the maximum allowable is performed after a second assessment of the patient's condition. The drug is taken before bedtime.
Duration of treatment.
Transient insomnia: 2 to 5 days.
Situational insomnia: 2 to 3 weeks.
Chronic insomnia: the duration of the course treatment is determined after consultation with a specialist.
The recommended adult dose is 7.5 mg (1 tab). The maximum dose is 15 mg.
Treatment of elderly patients and patients with impaired liver function or chronic pulmonary insufficiency begin with a dose of 3.75 mg (1/2 table) and, if necessary, increase to 7.5 mg.
Although in cases of renal failure cumulation of zopiclone and its metabolites was not found, in such patients it is recommended to start treatment with a dose of 3.75 mg.
The most frequent side effect observed when zopiclone is prescribed is a bitter taste in the mouth, can also be:
From the side of the central nervous system : dizziness, headache, residual drowsiness after waking up;
From the digestive system: digestive disorders: indigestion, nausea, dry mouth.
Allergic skin reactions such as pruritus and rash, extremely rare are angioedema and anaphylactic reactions.
Mental and paradoxical reactions: rarely - nightmares, irritability, confusion, hallucinations, aggressiveness, confusion, depressed mood, impaired coordination of movements, depressive state, inadequate behavior with possible development of amnesia.
After cessation of treatment in rare cases, there may be a "cancellation" syndrome and ricochet insomnia.
Single cases of a slight increase in serum transaminases and / or alkaline phosphatase were noted.
- hypersensitivity to zopiclone or other components of the drug;
- Myasthenia gravis;
- severe respiratory failure;
severe hepatic impairment;
- a syndrome of "nocturnal" apnea;
- Pregnancy and the period of breastfeeding;
- age to 18 years.
PREGNANCY AND LACTATION
It is not recommended to use the drug during pregnancy and prescribe to nursing mothers.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindications: severe hepatic impairment.
APPLICATION FOR CHILDREN
Contraindication: age to 18 years .
In patients with nocturnal seizures of bronchial asthma in combination with preparations of the methylxanthine series (theophylline), zopiclone reduces asthma attacks in the early pre-dawn hours, reduces their intensity and duration. When zopiclone is prescribed, it must be remembered that although the risk is minimal, it is impossible to completely exclude the development of addiction and abuse of the drug. The risk of dependence or abuse arises in the following cases:
- dose and duration of treatment;
- abuse of alcohol and / or drugs;
- sharing with alcohol or other psychotropic drugs.
Ricochet insomnia and withdrawal syndrome
The risk of such events after a sharp cessation of zopiclone can not be ruled out, especially after long-term treatment. Therefore, it is recommended to gradually reduce the dosage and notify the patient about it.
Anterograde amnesia can occur, especially with interruption of sleep or after a considerable time between taking the drug and going to sleep. To reduce the risk of anterograde amnesia:
- take the pill just before bedtime;
- to ensure a sleep duration of at least 6 hours.
The drug is not indicated for the treatment of depression, and can even mask its symptoms.
Use in children
A safe and effective dose of zopiclone has not been established in children and young people under the age of 18 years .
Influence on ability to driving and management of transport
Because of its pharmacological properties, zopiclone can adversely affect the ability to drive and control transport, as well as to engage in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions, so during the period of treatment, one must be extremely cautious or refrain from activities of this kind.
Overdose 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.
The first help consists in washing the stomach, taking activated charcoal. If necessary, symptomatic and supportive therapy in a hospital is recommended. Particular attention should be given to respiratory and cardiovascular functions.
Hemodialysis is of low significance because of the large volume distribution of zopiclone. Flumazenil can be used as an antidote.
It is not recommended simultaneous reception with alcohol, since the sedative effect of zopiclone may intensify.
Strengthening the oppressive effect on the central nervous system can occur in cases of simultaneous appointment with neuroleptics, hypnotics, tranquilizers, sedatives, antidepressants, narcotic analgesics, antiepileptic drugs, anesthetics, antihistamines with sedative effect, and erythromycin. Taking the drug reduces the concentration of trimipramine in the plasma.
TERMS OF RELEASE FROM PHARMACY
According to doctor's prescription.
TERMS AND CONDITIONS OF STORAGE
List B. In a dry, protected from light and inaccessible to children place. Shelf life: 3 years. Do not use the product after the expiry date printed on the package.