Normazidol

General characteristics. Structure:

Active ingredient - пирлиндол 25 mg or 50 mg;

Excipients - lactose, potato starch, sodium carboxymethylcellulose, calcium stearate.

Pharmacological properties:

Pharmacodynamics. Pirlindol - derivative an indole, having elements of structural similarity to serotonin, and also with Reserpinum. Pirlindol has the expressed antidepressive activity, feature of his action is existence at it timoleptichesky effect with the balanced action (the activating action at patients with apathetic, anergic depressions, is combined with sedative and anxiolytic action at patients with the agitated states). Selectively inhibits monoamine oxidase (MAO) of A type (quickly and completely reversibly); blocks deamination of serotonin and noradrenaline, to a lesser extent - tyramine (that creates less premises for development of a tiraminovy ("cheese") syndrome); partially inhibits the return capture of monoamines. Activates processes of synoptic transfer of nervous excitement to TsNS. Weakens depressive effects of Reserpinum, strengthens action of the predecessor of Norepinephrinum - dioxyphenylalanine (L-dofa), stimulates adrenergic structures; exponentiates effects of the predecessor of serotonin - 5 oxytryptophanes (stimulates serotonergic structures). Unlike tricyclic antidepressants, does not possess anticholinergic action. Has also nootropic effect, improves cognitive (cognitive) functions. Pirlindol does not kumulirutsya in an organism, has no tolerance, does not cause dependence or a withdrawal.

Pharmacokinetics. Pirlindol is almost completely soaked up from digestive tract. After reception of a single dose the maximum concentration of active ingredient in a blood plasma is reached in 2-8 hours. Pirlindol is subject to enterogepatichesky circulation. Elimination from a blood plasma is carried out trekhfazno. Absolute bioavailability makes 20-30% as the expressed metabolism at the first passing through a liver takes place. Pirlindol strongly contacts proteins of a blood plasma (95%) therefore the terminal period of its semi-removal is long - 185 hours. Pirlindol is almost completely metabolized and only his very insignificant quantity is removed with urine in not changed look. About 50-70% of metabolites are brought out of an organism with urine, 25-45% - with bile through intestines.

Indications to use:

Depressions of various genesis, it is preferential with psychomotor block and asthenic frustration, with alarming and depressive or an alarming and crazy component. Involutional depression. An alcoholic abstinence syndrome, Alzheimer's disease (as a part of complex therapy).

Route of administration and doses:

Inside on 50-75 mg (0,05 - 0,075 g) a day in two steps, gradually increasing a dose by 25 - 50 mg to 150 - 300 mg (0,15 - 0,30) a day. The maximum daily dose - 400 mg divided into 2-3 receptions. After achievement of therapeutic effect treatment is continued by individually picked up dose within 2-4 weeks then the dose is gradually reduced.

Features of use:

After use of MAO inhibitors therapy is begun not earlier than in 14 days. Lack of holinoblokiruyushchy action allows to use at patients with glaucoma and adenoma of a prostate

Influence on ability of control of vehicles: it is necessary to be careful as speed of reaction can be reduced.

Side effects:

Dryness in a mouth, perspiration, a tremor of hands, tachycardia, nausea, dizziness, allergic reactions.

Interaction with other medicines:

Normazidol do not appoint along with other MAO inhibitors, furasolidone, Procarbazinum, selegiliny. Increases efficiency of Epinephrinum (in connection with antimonoaminoksidazny activity). Let's combine with antipsychotic means, anxiolytics. During therapy it is impossible to take alcohol.

Contraindications:

Individual hypersensitivity to drug, an acute hepatitis, diseases of the hemopoietic system, a concomitant use with MAO inhibitors (see. "Special instructions").

Use of drug at pregnancy and during feeding by a breast
It is not recommended. There are no adequate and well controlled clinical trials of use of drug during pregnancy and during feeding by a breast. It is known that use of tricyclic antidepressants and similar drugs in the third trimester of pregnancy can cause in the newborn tachycardia, a hyperexcitability, muscular spasms. Use of drug is admissible only if the advantage for mother exceeds possible risk for a fruit.

Overdose:

Pirlindol малотоксичен. Overdose cases at people are not described. At long repeated introduction of a pirlindol the experimental animal in the doses considerably exceeding therapeutic noted pathological disturbances of the major bodies and their systems. Very high doses of drug cause spasms which can be stopped diazepam in animals.

Storage conditions:

In dry, protected from light and the place, unavailable to children, at a temperature not above 30 °C.

Issue conditions:

According to the recipe

Packaging:

Tablets on 25 and 50 mg. On 10 tablets in a blister strip packaging from a film of polyvinyl chloride light-protective and aluminum foil. On 5 planimetric packagings together with the application instruction place in a pack from a cardboard.