Zopicon

Zopicon has sedative and hypnotic activity.

Indications Zopicon

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

Release form

The release of the drug is carried out in tablet form, 10 pieces inside the cell packaging. In the box - 1 or 2 packs of medicine.

[1], [2]

Pharmacodynamics

Zopicone is a fast-acting sleeping medicine. Included in the group of psychotropic substances, derivatives of cyclopyrolone. The latter are structurally different from the newest sleeping pills, but are similar in drug effect to benzodiazepines. The hypnotic effect is provided by the specific ability of the synthesis with cerebral endings of benzodiazepines, as a result of which the functional activity of the CNS cells slows down.

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

The drug reduces the period required for falling asleep, prolongs sleep time and reduces the number of awakenings at night. After the use of drugs sleep occurs fairly quickly (while it has a normal structure of stages and duration; the period of the stage of REM sleep is not reduced). Due to the absence of aftereffect, it allows to ensure stable working capacity during the day.

[3], [4], [5], [6],

Pharmacokinetics

Zopicon is well absorbed at high speed. The bioavailability level is 75%. When consumed in 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 figure reaches an average of 5 hours (3.8-6.5 hours). Intlasma protein synthesis is quite low (45% at plasma values of 25-100 ng / ml).

Approximately 4-5% of the drug is recorded inside the urine in an unchanged condition. The main metabolic products (N-oxide derivative (12%), which has weak drug activity, as well as 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 older people, the bioavailability values of drugs are increased to 94%, as well as the half-life (about 7 hours); accumulation of the drug after repeated use does not occur.

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

The drug is able to pass into the mother's milk (its performance there equals 50% of the portion of the substance that the woman took).

[7], [8], [9], [10], [11]

Dosing and administration

Zopicon is used exclusively with the appointment of a doctor. Take the pill orally, at night.

An adult needs to use 1-well pill (7.5 mg) before bedtime. Often the treatment cycle lasts 7-10 days in a row. According to the medical recommendation, the course can be extended up to 2-3 weeks, but it should be held under close medical supervision.

Elderly people or persons with weak intellectual abilities should first use 3.75 mg of the substance. Later, taking into account the tolerance of the drug and its effectiveness, the dosage may increase to 7.5 mg.

Persons with liver problems or chronic respiratory failure are required to use 3.75 mg each. With the need in some situations, the dosage can be increased to 7.5 mg.

[14], [15], [16], [17]

Use Zopicon during pregnancy

It is forbidden to use when breastfeeding or pregnancy.

Contraindications

Main contraindications:

• severe intolerance associated with the drug or its elements;
• respiratory distress in severe;
• sleep apnea;
• the patient has a history of paradoxical reactions to sedatives and alcoholic beverages.

[12], [13],

Side effects Zopicon

When used in the required portions, the drug is transferred without complications and with short-term therapy does not affect the memory, respiratory and other activities of the body; usually not addictive, withdrawal syndrome, and addictions of a physical or mental nature. The following side signs may sometimes appear:

• lesions affecting the central nervous system: a feeling of weakness or drowsiness, nightmares, dizziness, a feeling of nervousness or euphoria, confusion of consciousness, as well as coordination disorder. In addition, anterograde form of amnesia or other memory disorders, weakening of libido, depressed mood, reduced pressure and a tendency to show aggression. Tremor, paresthesia, muscle spasm and speech disorder may also occur. If there is a severe disorder of motor coordination or dizziness, this means that the patient has an overdose or drug intolerance;
• cardiovascular dysfunction: increased heart rate rhythm;
• problems with digestive activity: vomiting, dry mucous membranes of the mouth with a bitter taste, constipation, language congestion, dyspepsia symptoms, as well as increased or worse appetite;
• disorders of respiratory processes: dyspnea;
• symptoms associated with the epidermis: the appearance of spots or redness, hyperhidrosis. Redness may be a manifestation of hypersensitivity with respect to the drug - with such a problem, the use should be discontinued;
• others: headaches, chills, weight loss, blurred vision and feeling of heaviness in the legs.

Overdose

The introduction of the drug in portions of 0.37 g can cause prolonged sleep and blurring of consciousness, and in addition, a state of coma with depression or complete disappearance of reflexes.

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

[18], [19], [20],

Interactions with other drugs

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

Drugs that inhibit certain liver enzymes (erythromycin with cimetidine) are able to potentiate the properties of Zopicone.

[21], [22], [23], [24]

Storage conditions

Zopicon is required to be stored in a dark and dry place, closed from the penetration of children. Temperature indicators - in the range of marks 15-25 ° C.

[25], [26], [27], [28], [29]

Shelf life

Zopicon can be used within a 3-year period from the time the therapeutic agent is manufactured.

[30], [31], [32], [33], [34]

Application for children

You can not assign in pediatrics (up to 18 years of age).

[35], [36]

Analogs

Analogues of the drug are the substances Rofen, Zolsana, Sanval and Andante with Nitrest, and besides this Gipnogen, Selofen, Peaclon with Zopiclon and Dobroson with Normason. The list also includes Healthy Sleep, Sonovan, Ivadal and Sonnat with Somnom.

[37], [38], [39], [40], [41], [42]