Communication to plasma proteins is approximately 45%.Metabolism After reappointments accumulation of zopiclone and its metabolites occurs. Interindividual differences are insignificant. The main metabolites are the N-oxide derivative (pharmacologically active) and N-desmetilovy metabolite (pharmacologically inactive). The half-life of approximately 4.5 and 7.4 hours, respectively. At the recommended doses, the half-life of unchanged zopiclone is approximately 5 hours. The urine zopiclone displays (approximately 80%), mainly as metabolites, with stool output of approximately 16%. Specific groups of patients in elderly patients, despite the slight decrease in hepatic metabolism and lengthening half-life of approximately 7 hours equipoise only cycle drug accumulation plasma was not detected even with multiple assignment. in patients with renal insufficiency cumulation zopiclone or its metabolites were detected even after prolonged use. in patients with liver cirrhosis the clearance of zopiclone is reduced by approximately 40% in accordance with the decrease dimethylation process.
Treatment of transient, situational or chronic insomnia in adults (including difficulty falling asleep, nighttime awakenings and early).
- hypersensitivity to zopiclone or any other components of the drug;
- myasthenia gravis;
- severe respiratory failure;
- severe hepatic impairment;
- syndrome “sleepy” apnea;
- Pregnancy and breast-feeding;
- age 18 years.Pregnancy and lactation
is not recommended to use the drug during pregnancy and prescribe nursing mothers.
Dosage and administration
Treatment should be as short as possible and not exceed four weeks.
Lengthening the duration of treatment in excess of the maximum allowable carried out after re-evaluation of the patient’s condition. The drug is taken before bedtime. The duration of treatment Transient insomnia: 2 to 5 days. Situational insomnia: 2 to 3 weeks. Chronic equipoise only cycle insomnia: duration of course of treatment is determined after consultation with a specialist. The recommended dose for adults – 7.5 mg. This dose must not be exceeded. Treatment of elderly patients and patients with impaired liver function, or chronic obstructive pulmonary disease begin with a dose of 3.75 mg and, if appropriate, increased to 7.5 mg. Although in cases of renal insufficiency cumulation zopiclone or its metabolites were not found in these patients recommend starting treatment with a dose of 3.75 mg.
The most common side effect observed in the appointment of zopiclone – a bitter taste in the mouth may also be:
- dizziness, headache, residual drowsiness after waking;
- Digestive Disorders: dyspepsia, nausea, dry mouth;
- Allergic skin reactions such as itching and rashes, are extremely rare angioedema and anaphylactic reactions. Can occur anterograde amnesia. Psychiatric and paradoxical reactions Rare: nightmares, irritability, confusion, hallucinations, aggressiveness, confusion, depressed mood, incoordination, depression, inappropriate behavior with the possible development of amnesia. “Cancellation” syndrome and rebound insomnia observed after cessation of treatment. There have been isolated cases marked a slight increase in serum transaminases blood and / or alkaline phosphatase.Overdosing
Overdosing it is usually manifested in the form of varying degrees of symptoms of central nervous system depression of somnolence to coma, depending upon the amount of drug received. First aid is gastric lavage, activated charcoal. If necessary, it is recommended symptomatic and supportive therapy in a hospital. Particular attention should be paid to equipoise only cycle respiratory and cardiovascular functions.
Haemodialysis has little significance because of the large volume of distribution of zopiclone.
Flumazenil can be used as an antidote.
Not recommended concomitant use of alcohol as a sedative effect of zopiclone may be enhanced.
Increased depressant effect on the central nervous system can occur in cases of co-administration with the antipsychotics, hypnotics, tranquilizers, sedatives, antidepressants, narcotic analgesics, antiepileptic drugs, anesthetics , antigistaminnmi drugs with a sedative effect, and erythromycin. The drug reduces the concentration of trimipramine in plasma and its effect.
In appointing zopiclone must be remembered that although the risk and minimal, but can not completely eliminate the development of addiction to the drug and its abuse.
The risk of dependence or abuse arises in the following cases:
- violations of the dose and duration of treatment;
- abuse of alcohol and / or drugs;
- Use of alcohol or other psychotropic drugs. rebound insomnia syndrome “cancel” The risk of such phenomena after abrupt discontinuation of zopiclone can not be ruled out, especially after long-term treatment. Therefore recommended to gradually equipoise only cycle reduce the dose and notify the patient. Amnesia may occur anterograde amnesia, especially when sleep is interrupted or after a significant period of time between taking the drug and going to sleep.