Пиклодорм®

General characteristics. Structure:

Active ingredient: 7,5 mg of a zopiklon in 1 tablet.

Excipients: as a part of a kernel - potato starch, phosphate calcium a dihydrate, sugar milk (lactose), povidone (polyvinylpirrolidone low-molecular medical or пласдон), refined sugar (sucrose), magnesium stearate.

Structure of a cover: gidroksipropilmetiltsellyuloz (gipromelloz), titanium dioxide, talc, polyethyleneglycol (macrogoal) 4000.

Pharmacological properties:

Pharmacodynamics. Zopiklon - a hypnagogue from group of the tsiklopirrolon structurally different from benzodiazepines and barbiturates. Has sedative and somnolent effect. These effects are caused by impact of a zopiklon on the receptors of the central nervous system (TsPS) relating to a macromolecular complex of piperidic acid (GAMK) and activation of channels for chlorine ions therefore there is strengthening of brake influence of GAMK and braking of interneural transfer in various departments of TsNS. Has property to shorten the backfilling period, to urezhat the frequency of night awakenings, to increase dream duration, and also to improve quality of a dream and awakening. Practically does not cause postsomnichesky disturbances: there are no feelings of weakness and drowsiness for morning of the next day.

Accustoming to somnolent effect of drug is absent during the long period of treatment, up to 17 weeks.

Pharmacokinetics. It is quickly soaked up in digestive tract. The maximum concentration in a blood plasma is reached during 0,5 - 1,5 h and make about 30 and 60 ng/ml after intake of 3,75 mg and 7,5 mg respectively. In 1 h after intake 95% of drug are soaked up. Absorption of drug does not depend on reception write. Communication with proteins of a blood plasma makes about 45%. Easily gets through gistogematichesky barriers; does not kumulirut.

The main metabolites are N-oxide (active) and N-desmetilovy a metabolite. The elimination half-life (Т½) makes about 4,5 and 7,4 h respectively. In the recommended doses Т½ of not changed zopiklon makes about 5 h. With urine it is removed (about 80%), mainly, in the form of metabolites, and also with expired air, fecal masses.

Separate groups of patients. An easy and moderate renal failure do not cause essential changes of kinetics of a zopiklon, at the expressed renal failure increase in the area under a curve "concentration time" of drug in plasma (AUC), time of achievement of the maximum concentration and Т½ is possible.

Т½ increases as well at patients of advanced age a little.

At patients with cirrhosis the clearance of a zopiklon decreases approximately by 40% according to demethylation process reduction.

Indications to use:

Treatment of passing, situational and chronic sleeplessness at adults of various etiology (including the complicated backfilling, night and early awakenings).

Route of administration and doses:

Inside in 30-40 min. prior to an estimated dream. The recommended dose - 7,5 mg (1 tablet) a day. The maximum daily dose makes 15 mg. Treatment has to be whenever possible short and not exceed four weeks. Lengthening of terms of treatment from above the most admissible is carried out after repeated assessment of a condition of the patient.

Treatment of elderly patients and patients with the broken function of a liver begin 3,75 mg (1/2 tablets) with a dose and, if necessary, increase up to 7,5 mg a day.

Though in cases of a renal failure of cumulation of a zopiklon and its metabolites it was not revealed, at such patients recommend to begin treatment with a dose of 3,75 mg.

Features of use:

At purpose of drug it is necessary to remember that though the risk and is minimum, but it is impossible to exclude dependence development absolutely. The risk of development of dependence increases in cases:

• excesses of the recommended doses and duration of treatment;
• simultaneous use with alcohol or other psychotropic drugs;
• purposes of drug to patients with existence in the anamnesis the instruction on the excessive use of alcoholic drinks and/or dependence on medicines.

The risk of development of ricochet sleeplessness and syndrome of "cancellation" after the sharp termination of reception of Piklodorma® cannot be excluded, especially after prolonged treatment therefore it is necessary to avoid the sudden termination of treatment. It is necessary to carry out drug withdrawal gradually.

The ecmnesia can be observed, especially at interruption of a dream or at the long period of backfilling. For decrease in risk of manifestation of an ecmnesia it is necessary to take a pill just before a dream and to provide dream duration not less than 6 hours.

Drug is not shown for treatment of a depression, and can even mask its symptoms.

Influence on ability to manage vehicles and mechanisms. During treatment it is necessary to abstain from control of vehicles and occupation other potentially dangerous types of activity requiring special attention and speed of psychomotor reactions.

Side effects:

From the alimentary system: often - bitter or "metal" taste in a mouth; nausea, vomiting, dryness in a mouth.

From TsNS: a headache, dizziness, residual drowsiness after awakening; more often at patients of advanced age - aggression, confusion of consciousness, hypererethism, a depression, hallucinations, nightmares and an ecmnesia; seldom - euphoria, a lack of coordination of movements.

At the termination of administration of drug the syndrome of "cancellation" (frequent awakening, resuming of sleeplessness) is possible, and after prolonged use medicinal dependence can develop.

Allergic reactions: urticaria, skin rash.

Interaction with other medicines:

The concomitant use with alcohol as sedation of Piklodorm can amplify is not recommended.

Strengthening угнетающею influences on the central nervous system can meet in cases simultaneous appointments neuroleptics, hypnagogues, tranquilizers, sedatives, antidepressants, narcotic analgetics, antiepileptic drugs, anesthetics, antihistaminic drugs with sedation, and also erythromycin.

Administration of drug reduces concentration of a trimipramin in plasma.

Contraindications:

Hypersensitivity to a zopiklon, to other components of drug; heavy myasthenia; the expressed respiratory insufficiency; the expressed liver failure; syndrome of a "sleepy" apnoea; pregnancy; lactation period; age up to 18 years (efficiency and safety of use for children and teenagers are insufficiently studied).

Overdose:

Symptoms: oppression of TsNS of varying severity (from drowsiness to a coma), an ataxy, is rare - an atrioventricular block

Treatment: a gastric lavage if the diagnosis of overdose is established soon after administration of drug. A symptomatic and maintenance therapy in the conditions of a hospital. Special attention should be paid to respiratory and cardiovascular functions. As an antidote it is possible to apply the antagonist of benzodiazepine receptors - flumazenit. Carrying out a hemodialysis is inexpedient.

Storage conditions:

To store in the dry, protected from light place, at a temperature not above 25 °C. To store in the place, unavailable to children. A period of validity - 3 years. Not to use after the expiry date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets, film coated 7,5 mg. Packaging: on 10 tablets in a blister strip packaging from a film of polyvinyl chloride and aluminum foil. 1 or 2 blister strip packagings together with the application instruction place in a pack from a cardboard.