Relaxon - instructions for use, dose, side effects, contraindications

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Dosage form: & nbspFilm-coated tablets.

Composition:

Composition per one tablet

Active substance: Zopiclone 7.5 mg; Excipients: a sufficient amount to prepare a tablet weighing 165 mg (beta shell) [cellulose microcrystalline 8.2 mg, silicon dioxide colloid (aerosil) 1.6 mg, lactose monohydrate 90.7 mg, primogel (sodium carboxymethyl starch) 3.3 mg, potato starch 45.1 mg, magnesium stearate 1.6 mg, povidone (polyvinylpyrrolidone) 7.0 mg]

Excipients: sufficient amount to prepare a tablet weighing 170 mg (with a coat) [hypromellose (hydroxypropylmethyl cellulose) 2.085 mg, talc 0.565 mg, povidone (polyvinylpyrrolidone) 1.395 mg, macrogol (polyethylene glycol 4000) 0.51 mg, titanium dioxide 0.445 mg]

Description:

The tablets covered with a film membrane of white color, round, biconcave.

Pharmacotherapeutic group:Sleeping pills.

Pharmacodynamics:

Zopiclone is a hypnotic from a group of cyclopyrrolons structurally different from benzodiazepines and barbiturates. Has a sedative and hypnotic effect. These effects are due to the action of zopiclone on the central nervous system (CNS) receptors related to the macromolecular gamma-aminobutyric acid complex (GABA), and the activation of channels for chloride ions, resulting in an increase in the inhibitory effect of GABA and inhibition of interneuronal transmission in various parts of the central nervous system.

It has the ability to shorten the period of falling asleep, to reduce the frequency of nocturnal awakenings, to prolong the duration of sleep, and to improve the quality of sleep and awakening. Virtually does not cause post-somnolent disorders: there is no feeling of weakness and drowsiness on the morning of the next day.

Adapting to the hypnotic effect of the drug is absent for a long period of treatment, up to 17 weeks.

Pharmacokinetics:

Quickly absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is achieved within 1-3 hours and is about 60 ng / ml after ingestion of 7.5 mg. After 1 hour after ingestion, 95% of the drug is absorbed. Absorption of the drug is not dependent on food intake.

Easily penetrates through the histohematological barriers; Do not cumulate. The connection with plasma proteins is about 45%.

Metabolised in the liver. The main metabolites are N-oxide (active) and N-desmethyl metabolite. The half-life (T1 / 2) is about 4.5 and 7.4 hours, respectively. In recommended doses of T1 / 2 of unchanged zopiclone is 5.5 -6 hours. It is excreted in the urine (approximately 80%), mainly in the form of metabolites, as well as with exhaled air, caloric masses.

Individual groups of patients

In elderly patients, T1 / 2 slightly increases (up to 7 hours).

In patients with cirrhosis of the liver, zopiclone clearance decreases by approximately 40% in accordance with a decrease in the demethylation process.

Indications:

Treatment of transient, situational and chronic insomnia in adults of various etiologies (including difficulty falling asleep, night and early awakenings). Sleep disorders in mental disorders, bronchial asthma with night attacks (in combination with a one-time intake of a daily dose of theophylline).

Contraindications:

Hypersensitivity to zopiclone, other components of the drug; lactose intolerance, lactase deficiency or glucose-galactose malabsorption (the preparation contains lactose); severe myasthenia gravis; severe respiratory failure; severe hepatic impairment; syndrome of "nocturnal" apnea; pregnancy; lactation period; age to 18 years (efficacy and safety of use in children and adolescents have not been adequately studied).

Dosing and Administration:

Relaxone is prescribed inside, shortly before sleep.

The recommended dose is 7.5 mg (1 tablet) per day. The maximum daily dose is 15 mg.

Treatment should be as short as possible and not exceed four weeks. Elongation of treatment periods above the maximum allowable is performed after a second assessment of the patient's condition.

Treatment of elderly patients and patients with impaired liver function is recommended starting with 3.75 mg Zopiclone, if necessary, increase the dose to 7.5 mg per day.

Side effects:

On the part of the digestive system: often - a bitter or metallic taste in the mouth; nausea, vomiting, dry mouth.

From the side of the central nervous system: headache, dizziness, residual drowsiness after waking up; more often in elderly patients - aggressiveness, confusion, increased excitability, depression, hallucinations, nightmares and anterograde amnesia; rarely - euphoria, a violation of coordination of movements. When the drug is discontinued, the phenomenon of "cancellation" (frequent awakening, the resumption of insomnia) is possible, and after prolonged use, drug dependence may develop.

Allergic reactions: urticaria, skin rash.

Overdose:

Symptoms: oppression of the central nervous system of various degrees (from drowsiness to coma), ataxia, rarely - AV blockade.

Treatment: gastric lavage if the diagnosis of an overdose is established soon after taking the drug. Symptomatic and supportive therapy in a hospital. Particular attention should be given to respiratory and cardiovascular functions. As an antidote, a benzodiazepine receptor antagonist can be used - flumazenil. Carrying out of hemodialysis is inexpedient.

Interaction:

Drugs that have an inhibitory effect on the central nervous system (incl. ethanol), can enhance the sedative effect of Relaxon.

Reduces the concentration of trimipramine in plasma

Special instructions:

When prescribing the drug, it must be remembered that, although the risk is minimal, one can not completely exclude the development of addiction. The risk of dependence develops in the following cases:

exceeding recommended doses and duration of treatment;
simultaneous use with alcohol or other psychotropic drugs; -The purpose of the drug to patients with personality changes, the presence in the history of indications of excessive consumption of alcoholic beverages and / or dependence on medicines.

The risk of developing ricochet insomnia and the "cancellation" syndrome after the abrupt discontinuation of Relaxon's administration can not be ruled out,especially after long-term treatment. Therefore, sudden cessation of treatment should be avoided. It is necessary to implement the abolition of the drug gradually.

Anterograde amnesia can be observed, especially with interruption of sleep or with a long period of falling asleep. To reduce the risk of manifestations of anterograde amnesia, it is necessary to take the pill just before bedtime and provide a sleep duration of at least 6 hours.

The drug is not indicated for the treatment of depression, and can even mask its symptoms.

Effect on the ability to drive transp. cf. and fur:

During the period of treatment, it is necessary to be extremely cautious when driving vehicles and engaging in other potentially dangerous activities requiring increased attention and speed of psychomotor reactions, or refrain from activities of this kind.

Form release / dosage:Tablets, film-coated, 7.5 mg.

Packaging:

For 5 or 10 tablets in a contoured cell pack of a polyvinylchloride film and aluminum foil printed lacquered. For 5 or 20 tablets in a can of light-protective glass with a triangular aureole, capped with a lid tightened with a sealing element.

Each bank or 1, or 2 or 3, or 4 contour mesh packages together with instructions for use in a pack of cardboard.

Storage conditions:

At a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:P N001759 / 01

Date of registration:26.12.2007

The owner of the registration certificate:VEROPHARM SA VEROPHARM SA Russia

Manufacturer: & nbsp

VEROPHARM SA Russia

Information update date: & nbsp18.10.2015

Illustrated instructions

Instructions

Relaxon (Relaxon)