Mezapamum

General characteristics. Structure:

Active ingredient: 10 mg of Medazepamum.

Excipients: lactoses monohydrate (sugar milk); potato starch; calcium stearate (calcium stearate).

The drug of a number of tranquilizers having the calming effect, removing emotional pressure, reducing alarm, fear possesses vegetostabiliziruyushchy action. To a lesser extent shows miorelaksantny and gipnosedativny properties in this connection is among "day" tranquilizers.

Pharmacological properties:

Pharmacodynamics. Anxiolytic means (tranquilizer) derivative of benzodiazepine. Has anxiolytic, myorelaxation and antiepileptic effect, has slightly expressed timoleptichesky effect. Sedative and somnolent action is expressed to a lesser extent, than at typical benzodiazepine tranquilizers therefore Medazepamum is carried to group of so-called "day" tranquilizers.

Interacts with benzodiazepine receptors of limbic system and the ascending activating brain trunk formation, promotes opening of chloric channels that leads to strengthening of brake influence of GABA in TsNS.

Eliminates a condition of alarm, sensation of fear, psychoneurotic tension, the general motive excitement, excess fussiness, recovers an affective behavior and exerts the stabilizing impact on the autonomic nervous system. Recovers critical evaluation of own disease. Antiepileptic, central myorelaxation, sedative and somnolent action is expressed to a lesser extent, than at typical anxiolytic means of derivatives of benzodiazepine.

Pharmacokinetics. After intake it is quickly soaked up. Absorption makes 49-75%. Cmax is reached in 1-2 h. Linkng with proteins of plasma - 99.8%. It is metabolized by a hydroxylation, N-demethylation, oxidation with formation of active metabolites: to desmetilmedazepa (nordiazepa), diazepam, to desmetildiazepa, oxazepam (7.1% of a dose).

Nordiazepam has long T1/2, collects in an organism and has the expressed sedative effect. The metabolites connected with glucuronic acid are removed by kidneys (63-85%) and through intestines (15-37%). T1/2 is 20-176 h. After completion of reception within 3-14 days significant concentration of metabolites in plasma are defined (have long T1/2).

Indications to use:

Neurosises, psychopathia with alarm, excitement, nervous tension, irritability, neurocirculatory dystonia, migraine (prevention of attacks), a menopausal syndrome, an alcoholism (abstinence syndrome). "School" neurosises, mental lability and hyperexcitability at children.

Route of administration and doses:

Accept inside. The adult in an initiation of treatment - on 5 mg of 2-3 times/days, then the dose is gradually raised to 30 mg/days. In out-patient conditions doses on 5 mg in the morning and in the afternoon and 10 mg are recommended in the evening. If necessary it is possible to increase a dose to 40 mg/days. To elderly people and teenagers - on 10-20 mg/days; children are 10 years old and are more senior - in a dose of 2 mg/kg/days. Duration of use depends on indications and individual reaction of the patient to treatment.

Maximum daily doses: for adults at out-patient treatment - 40 mg, in the conditions of a hospital - 60 mg.

Features of use:

With care apply at a renal and/or liver failure, a spinal and cerebellar ataxy, intraocular hypertensia, organic lesions of TsNS, at respiratory insufficiency, at patients of advanced age, at a serious general condition, at pregnancy.

Medazepamum should be applied whenever possible quickly since at prolonged use, especially in high doses, there is a danger of formation of medicinal dependence. Physical dependence comes seldom, however at excessive exceeding of a dose development of tolerance and mental dependence was observed. For prevention of development of an abstinence syndrome Medazepamum should be cancelled gradually.

At treatment benzodiazepines established existence of braking of ability to training, storing processes.

During treatment not to allow alcohol intake.

At children Medazepamum is applied according to strict indications.

Influence on ability to driving of motor transport and to control of mechanisms

During use of Medazepamum it is not recommended to be engaged in potentially dangerous types of activity demanding bystry psychomotor reactions.

Use in II and III trimesters of pregnancy is possible only according to strict indications.

Side effects:

From TsNS and peripheral nervous system: drowsiness, feeling of easy fatigue, a headache (the first reaction to reception disappearing after a dose decline), weakness, dizziness, an oglushennost, an ecmnesia, a depression, confusion of consciousness, a dysarthtia, accommodation paresis are possible.

At elderly patients and children orientation loss, lack of braking, aggression, the increased muscular fatigue are more probable. At elderly patients and mentally retarded patients the ataxy is possible.

From endocrine system: decrease in a libido, decrease in a potentiality, disturbance of a menstrual cycle.

From respiratory system: oppression of a respiratory center (at obstruction of respiratory tracts or injury of a brain), alveolar hypoventilation (at patients with HOBL at reception in high doses).

From cardiovascular system: tachycardia, decrease in the ABP.

From the alimentary system: dryness in a mouth, dyspepsia.

Others: an ischuria, a spasm of phonatory bands, thorax pains, a withdrawal, paradoxical reactions, medicinal dependence (especially at prolonged use), allergic reactions.

Interaction with other medicines:

At simultaneous use with opioid analgetics, anesthetics, muscle relaxants, ethanol strengthening of the oppressing influence on TsNS is possible.

At simultaneous use with antihypertensives of the central action, beta adrenoblockers, anticoagulants results of medicinal interaction are unpredictable.

At simultaneous use with Cimetidinum increase in intensity and duration of action of Medazepamum is possible, barbiturates and Phenytoinum can reduce its efficiency.

Oral contraceptives can inhibit metabolism of Medazepamum that leads to strengthening of intensity and duration of its action.

Reduces efficiency of a levodopa, strengthens action of Phenytoinum.

Contraindications:

Myasthenia, acute diseases of a liver and kidneys, night an apnoea, alcohol and drug addiction, the I trimester of pregnancy, the lactation period, children's age up to 10 years, hypersensitivity to Medazepamum.

Overdose:

Symptoms: long confusion of consciousness, drowsiness, feeling of fatigue, ataxy, tachycardia, arterial hypotension, decrease in a tone of muscles; in hard cases — a coma, spasms, respiratory depression, up to a full apnoea and heart.

Treatment: gastric lavage; reception of absorbent carbon and laxatives; control and correction of breath, ChSS, ABP, body temperature and blood circulation; symptomatic therapy. The artificial diuresis and a hemodialysis are a little effective. For elimination of the oppressing action on TsNS the specific antagonist of benzodiazepines can be used — flumazenit.

Storage conditions:

The list III of the list of the drugs, psychotropic substances and their precursors which are subject to control in the Russian Federation. To store in the unavailable to children, protected from light place at a temperature not above 30 °C.

Issue conditions:

According to the recipe

Packaging:

On 50 pieces of tablets - bottles from dark glass in packs cardboard.