Zopiclone - instructions for use, doses, side effects, contraindications

It is an agonist of benzodiazepine receptors. It interacts with the central receptors (subtypes of omega-1 and omega-2 benzodiazepine receptors) of the macromolecular GABA-benzodiazepine-chloronophore complex and does not interact with peripheral benzodiazepine receptors. Increases the sensitivity of GABA-receptors to the mediator (gamma-aminobutyric acid), which causes an increase in the opening frequency in the cytoplasmic membrane of the neurons of the channels for the incoming currents of chloride ions. As a result, there is an increase in the inhibitory effect of GABA and the inhibition of interneuronal transmission in various parts of the central nervous system.

Pharmacokinetics:

Quickly absorbed from the digestive tract. C_max is achieved after 1-1.5 h. Binding to plasma proteins is about 45%. Easily passes through the histohematological barriers, including blood-brain barrier, and is distributed to organs and tissues, including the brain.Passes through the placental barrier, penetrates into breast milk (in breast milk contains 2 times less concentrations than in blood plasma). Metabolised in the liver to form an N-oxide, which has little pharmacological activity, and two inactive metabolites. The half-life period is 3,5-6 h, with a pronounced insufficiency of liver function increases to 11 h. It is excreted mainly by kidneys in the form of metabolites (80%), and also through the intestine (16%). There are data on the excretion of small amounts of salivary glands. Repeated procedures are not accompanied by cumulation of zopiclone and its metabolites.

Shortens the period of falling asleep, reduces the number of nocturnal awakenings, improves the quality of sleep, does not change the phase structure of sleep. Effective in situational insomnia, associated with psychoemotional stress, changes in the usual rhythm of life (for example, when hospitalized), desynchronosis, including when changing time zones, shift mode. Sleep occurs within 20-30 minutes after ingestion and lasts 6-8 hours.

In patients with nocturnal manifestations of bronchial asthma in combination with preparations of the methylxanthine series (theophylline) reduces asthma attacks in the early pre-dawn hours, reduces their intensity and duration.

Indications:Sleep disorders (difficulty falling asleep, frequent nocturnal and / or early morning awakenings), including situational, short-term, chronic insomnia; secondary sleep disorders in mental disorders.

ICD-10

V.F00-F09.F07.2 Postcontasia syndrome

V.F50-F59.F51.0 Insomnia inorganic etiology

VI.G40-G47.G47.0 Disturbances of falling asleep and maintaining sleep [insomnia]

Contraindications:Hypersensitivity, severe respiratory failure, pregnancy (especially I and III trimester), breast-feeding, age to 18 years.

Carefully:

In connection with the possibility of developing drug dependence, an application for a long period of time can be prescribed by a doctor in exceptional cases. In the event that insomnia does not disappear within 4 weeks, you should inform your doctor. The likelihood of addiction, physical or psychological dependence increases when the prescribed dose is not met or the duration of treatment is more than 4 weeks.

Pregnancy and lactation:Contraindicated in pregnancy (especially in I and III trimester). When zopiclone is used by a woman in the third trimester of pregnancy, a newborn can have disorders from the nervous system, the appearance of withdrawal syndrome. In case the woman prescribed zopiclone immediately before the onset of labor and labor, constant medical supervision of the newborn is necessary. For the duration of treatment, breastfeeding should be discontinued (zopiclone penetrates into breast milk).

Dosing and Administration:Inside. The dose and duration of treatment is determined by the doctor strictly individually. The average dose is 7.5 mg once, at night, the maximum dose is 15 mg. Patients over 65 years of age, patients with liver disease or chronic respiratory failure, half the dose (3.75 mg) is recommended. The course of treatment: from several days to 4 weeks.

Side effects:

From the nervous system and sensory organs: drowsiness, fatigue, fatigue, headache, dizziness, irritability, confusion (more often in the elderly), depressed mood, muscle weakness, impaired coordination of movements, diplopia, memory impairment,paradoxical reactions (increased insomnia, nightmares, nervousness, agitation, aggressiveness, bouts of anger, hallucinations).

Other: bitter or metallic taste in the mouth, dry mouth, nausea, vomiting, skin allergic reactions, changes in libido, anterograde amnesia.

Overdose:

Symptoms: oppression of the central nervous system of varying degrees of severity (from drowsiness to loss of consciousness).

Treatment: gastric lavage, reception of activated charcoal; if necessary, symptomatic therapy. As a specific antidote, a benzodiazepine receptor antagonist flumazenil (in a hospital setting). Hemodialysis is ineffective.

Interaction:

With the joint use of zopiclone with other drugs that depress the central nervous system (including antipsychotics, other hypnotics, antiepileptic drugs, some antihistamines, alcohol), mutual enhancement of the effects is possible.

Zopiclone reduces the concentration of trimipramine in plasma.

Special instructions:

Cancellation of the drug should be carried out gradually, as with a sharp cessation of treatment, it is possible to resume insomnia, frequent awakenings, headache and muscle pain, anxiety, agitation, absent-mindedness, irritability.

Paradoxical reactions are more often observed in elderly patients. When there are paradoxical reactions zopiclone should be canceled.

The day after taking zopiclone, you should avoid driving the car and practicing potentially dangerous activities that require increased attention and quick response. During treatment with zopiclone, one should refrain from drinking alcoholic beverages or drugs containing alcohol.

Instructions

Zopiclone (Zopiclonum)