Zopiclone

Zopiclone has hypnotic and sedative activity. It is a drug from the pyrrolopyrazinamide category.

Indications Zopiclone

It is used in connection with the following sleep disorders:

• problems with the process of falling asleep;
• regular awakenings in the morning or at night;
• insomnia (this includes its short-term, chronic or situational forms);
• restless sleep process;
• sleep disorders caused by various forms of mental disorders.

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Release form

The substance is released in tablet form, in the amount of 10 pieces inside a cell plate. In a box - 1, 2 or 3 plates.

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Pharmacodynamics

Because the drug is a hypnotic, a derivative of the element cyclopyrrolone, it is considered an effective agonist of benzodiazepine endings. The drug has a powerful anxiolytic and sedative effect. Along with this, Zopiclone demonstrates anticonvulsant, amnestic and muscle relaxant activity.

The chemical parameters of zopiclone, which is the active component of the drug, contribute to the potentiation of GABA-ergic brain processes, as a result of which the sensitivity threshold relative to the conductor of GABA-endings increases - during the interaction of medicinal active elements and benzodiazepine endings. The use of the drug leads to a decrease in the number of awakenings during night sleep.

In addition, Zopiclone has a positive effect on falling asleep and significantly increases the duration of sleep. It should be taken into account that the drug does not have a negative effect on the sleep structure itself (does not change its phases, does not reduce the duration of the REM phase, etc.).

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Pharmacokinetics

The medication dissolves in the stomach at a fairly high speed; its Cmax values are recorded after several hours from the moment of administration.

The medicine easily passes through the histohematic barrier, then evenly distributed inside the organs with tissues, and in addition inside the brain. In case of repeated therapeutic cycle Zopiclone does not accumulate. After 0.5 hours from the administration of the drug, a deep sleep begins with a duration of no more than 8 hours.

It is necessary to take into account that the combined use of the drug and drugs containing theophylline in people with asthma leads to a significant reduction in the intensity of attacks and their duration during the pre-morning period.

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Dosing and administration

The average dosage of the drug is 7.5 mg (1 tablet of the drug). The drug is taken before bedtime. If insomnia is severe, the dosage can be doubled.

However, elderly people and people with liver problems should use a maximum of 3.75 mg of the substance per day.

Use Zopiclone during pregnancy

The medicine should not be used if you are pregnant or breastfeeding.

Contraindications

Among the contraindications:

• the presence of severe intolerance to medicinal components;
• respiratory failure.

At the same time, the drug should be prescribed with great caution to people with liver failure, apnea syndrome, congenital galactosemia, glucose-galactose malabsorption, as well as lactase deficiency or myasthenia.

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Side effects Zopiclone

If the medication is used in recommended doses, side effects often do not develop. But in case of significant excess of doses, the following disorders may be observed:

• behavioral disturbances, amnesia, somnambulism, aggressive state, altered or confused consciousness, and at the same time rebound insomnia, dependence of a psychological or physical nature, coordination disorder, speech problems, depression, hallucinations with headaches and ataxia. Dizziness and a feeling of euphoria are also possible;
• epidermal rash, Quincke's edema, urticaria and other allergic symptoms;
• asthenia, vomiting, diarrhea, dispersion with anorexia and weight loss;
• diplopia, decreased libido and hypotension.

It is necessary to clarify that in case of overdose the patient develops a bitter taste, and in addition, dryness of the oral mucosa. At times, potentiation of liver enzyme activity occurs.

Overdose

Zopiclone intoxication can cause life-threatening disorders. CNS suppression is often observed during poisoning. Symptoms of overdose include drowsiness and lethargy, confusion, ataxia, decreased or increased blood pressure, and respiratory depression.

If up to 1 hour has passed since the drug was administered, vomiting should be induced in the victim. In other circumstances, gastric lavage is performed immediately, with special attention to protecting the respiratory organs. To reduce the absorption of the active drug component, activated carbon is prescribed.

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Interactions with other drugs

Zopiclone should not be used in combination with alcohol or alcohol-containing medications.

At the same time, the drug weakens the effectiveness of trimipramine and potentiates the suppressive effect on the nervous system of drugs that have antidepressant, sedative, anxiolytic, and also anticonvulsant, antipsychotic and antihistamine effects.

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Storage conditions

Zopiclone should be kept in a place closed to small children. Temperature indicators - in the range up to 25°C.

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Shelf life

Zopiclone can be used within a 2-year period from the date of manufacture of the medicinal substance.

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Application for children

It is prohibited to prescribe in pediatrics (children under 18 years of age).

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Analogues

The drug's analogues are Imovan, Somnol, Relaxon with Torson, Zopiclone 7.5-SL and Piclodorm.

Reviews

Zopiclone receives a large number of different reviews. Many of them note the high effectiveness of the drug. But its disadvantages are also discussed - a large list of negative symptoms, as well as the fact that it cannot be used for long-term therapy of sleep disorders.