Zopicon

Zopicone has sedative and hypnotic activity.

Indications Zopicona

It is used for symptomatic short-term treatment of insomnia, during which there are problems with falling asleep and frequent awakenings at night (or too early).

Release form

The medicine is released in tablet form, 10 pieces per blister pack. A box contains 1 or 2 packages of medicine.

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Pharmacodynamics

Zopicon is a fast-acting hypnotic drug. It is a member of the group of psychotropic substances, cyclopyrolone derivatives. The latter differ in structure from the newest hypnotic drugs, but are similar in medicinal effect to benzodiazepines. The hypnotic effect is provided by the specific ability to synthesize benzodiazepines with the brain endings, resulting in a slowdown in the functional activity of CNS cells.

The drug is not synthesized with peripheral benzodiazepine endings, and is also weakly synthesized with GABA and serotonin endings, α1, α2 adrenergic endings and dopamine receptors.

The drug reduces the period required to fall asleep, prolongs sleep time and reduces the number of awakenings at night. After taking the drug, sleep occurs quite quickly (while it has a normal structure of stages and duration; the period of the REM stage is not reduced). Due to the absence of aftereffects, it ensures stable working capacity during the day.

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Pharmacokinetics

Zopicon is well and rapidly absorbed. The bioavailability level is 75%. When using a single dose (7.5 mg), plasma Cmax values of 60 ng/ml are determined in less than 120 minutes. With repeated use of 7.5 mg over a 14-day period, this value reaches an average of 5 hours (3.8-6.5 hours). Intraplasmic protein synthesis is quite low (45% with plasma values of 25-100 ng/ml).

Approximately 4-5% of the drug is registered in the urine in an unchanged state. The main metabolic products (N-oxide derivative (12%), which has weak medicinal activity, as well as an inactive N-desmethyl component (16%)) are excreted by the kidneys. Over 90% of the used portion of the drug is completely excreted from the body over a 5-day period: with urine (75%) and feces (16%).

In elderly people, the bioavailability values of the drug are increased to 94%, as is the half-life (approximately 7 hours); accumulation of the drug after repeated use does not occur.

In individuals with liver problems, the half-life is significantly increased (11.9 hours), and the period for reaching plasma Cmax is extended to 3.5 hours.

The medication can pass into breast milk (its levels there are equal to 50% of the dose of the substance taken by the woman).

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Dosing and administration

Zopicon is used only with the doctor's prescription. Tablets should be taken orally, at night.

An adult should take 1 tablet (7.5 mg) before bedtime. Often the treatment cycle lasts 7-10 days in a row. On doctor's recommendation the course can be extended to 2-3 weeks, but it should be done under close medical supervision.

Elderly people or people with weak intellectual abilities should initially take 3.75 mg of the substance. Later, taking into account the tolerance of the drug and its effectiveness, the dosage can be increased to 7.5 mg.

People with liver problems or chronic respiratory failure should use 3.75 mg of the drug. If necessary, in some situations, the dosage can be increased to 7.5 mg.

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Use Zopicona during pregnancy

Do not use while breastfeeding or pregnant.

Contraindications

Main contraindications:

• severe intolerance associated with the drug or its components;
• severe respiratory disorders;
• sleep apnea;
• the presence in the patient's medical history of paradoxical reactions to sedatives and alcoholic beverages.

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Side effects Zopicona

When used in the required doses, the drug is tolerated without complications and, with short-term therapy, does not affect memory, respiratory or other functions of the body; it usually does not cause addiction, withdrawal syndrome or dependence of a physical or mental nature. Sometimes the following side effects may appear:

• CNS disorders: weakness or drowsiness, nightmares, dizziness, nervousness or euphoria, clouding of consciousness, and coordination disorder. In addition, anterograde amnesia or other memory disorders, decreased libido, depressed mood, decreased blood pressure, and a tendency to aggression. Tremor, paresthesia, muscle spasm, and speech disorder may also occur. If severe motor coordination disorder or dizziness is noted, this means that the patient has an overdose or intolerance to the drug;
• dysfunction of the cardiovascular system: increased heart rate;
• problems with digestive activity: vomiting, dry mouth with a bitter taste, constipation, tongue congestion, symptoms of dyspepsia, as well as increased or decreased appetite;
• respiratory disorders: dyspnea;
• symptoms related to the epidermis: the appearance of spots or redness, hyperhidrosis. Redness may be a manifestation of hypersensitivity to the drug - if such a problem occurs, the use should be discontinued;
• Others: headaches, chills, weight loss, blurred vision and a feeling of heaviness in the legs.

Overdose

The introduction of the drug in a dose of 0.37 g can cause prolonged sleep and clouding of consciousness, as well as a state of coma with depression or complete disappearance of reflexes.

Symptomatic procedures are prescribed. In acute intoxication, immediate gastric lavage, intravenous fluid injection and respiratory support with the help of a device are performed. Flumazenil acts as an antidote to the drug.

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Interactions with other drugs

The drug potentiates the depressant effect on the central nervous system caused by alcoholic beverages and the sedative effect of psychotropic drugs and anticonvulsants.

Medicines that inhibit individual liver enzymes (erythrocine with cimetidine) can potentiate the properties of Zopicon.

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Storage conditions

Zopicon should be stored in a dark and dry place, out of reach of children. Temperature indicators are in the range of 15-25°C.

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Shelf life

Zopicon can be used within a 3-year period from the date of manufacture of the therapeutic agent.

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Application for children

Should not be prescribed in pediatrics (under 18 years of age).

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Analogues

The analogs of the drug are Rofen, Zolsana, Sanval and Andante with Nitrest, and also Gipnogen, Selofen, Piklon with Zopiclone and Dobroson with Normason. The list also includes Healthy Sleep, Sonovan, Ivadal and Sonnat with Somnol.

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