Trigeksifenidil

General characteristics. Structure:

Active ingredient: 2 mg of a trigeksifenidil of a hydrochloride in 1 tablet.

Excipients: sucrose (sugar), potato starch, povidone, (polyvinylpirrolidone low-molecular medical), stearate calcium monohydrate, кросповидон (полипласдон XL-10).

Pharmacological properties:

Pharmacodynamics. Protivoparkinsonichesky means. Renders the central and peripheral holinoblokiruyushchy, and also myorelaxation action. The mechanism of action is based on the competition to acetylcholine on a postsynaptic membrane. Reduces a tremor, to a lesser extent influences rigidity and a hypokinesia.

Possesses peripheral M-holinoblokiruyushchim action: reduces a sialosis, to a lesser extent sweating and secretion of sebaceous glands.

Pharmacokinetics. At oral administration trigeksifenidit quickly and it is completely soaked up from a digestive tract. Elimination half-life of 5-10 hours. Trigeksifenidil possesses a high lipotropnost, well passes through hematoencephalic and placental barriers. It is allocated with breast milk. It is hydrolyzed in fabrics under the influence of nonspecific esterases.

It is removed by kidneys: a small amount in not changed look, and the main part - in the form of metabolites.

Indications to use:

Parkinsonism of various etiology; the motive disturbances connected with defeat of extrapyramidal system.

Route of administration and doses:

Inside, to food or during food. An initial dose - 0,5 - 1 mg/days. The dose is increased gradually by 1 - 2 mg every 3 - 5 days.

Usual maintenance dose - 6 - 10 mg a day, divided into 3 - 4 receptions. In hard cases there can be a need to increase a dose to 12 - 16 mg divided into 3 - 4 receptions. The maximum single dose - 10 mg3 daily - 16 mg.

Features of use:

During treatment it is necessary to abstain from driving of motor transport and occupations potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions. Treatment cannot be stopped suddenly. If at administration of drug there is a dryness in a mouth, it is desirable to accept it to food, otherwise nausea can develop.

Upon termination of treatment or in case of the beginning of alternative treatment of a dose of a trigeksifenidil it is necessary to reduce gradually.

To patients 60 years are more senior appoint with extra care because of the sensitivity increased to drug possibilities of a memory impairment and thinking. At use of high doses of drug or at treatment of patients with the contributing factors (atherosclerosis, old age or patients who had an idiosyncrasy on any medicine earlier) mental disturbances (unnatural increase in mood, excitement, an acrimony), vomiting or nausea can appear. In these cases it is necessary to stop treatment.

During prolonged treatment expressiveness of the side effects caused by anticholinergic action decreases. It is necessary to control eye pressure periodically.

Side effects:

From a nervous system: headache, dizziness, irritability, nonsense, hallucinations, increased fatigue, decrease in concentration of attention, psychoses.

The effects caused by anticholinergic activity: dryness of a mucous oral cavity, accommodation paresis, increase in intraocular pressure, a lock, an ischuria (including at prostate adenoma), tachycardia, decrease in sweating.

From the alimentary system: nausea, vomiting. Allergic reactions: skin rash.

Others: purulent parotitis (owing to a xerostomia), a dermahemia, decrease in a muscle tone, development of medicinal dependence is possible.

Interaction with other medicines:

At combined use with HI-gistaminoblokator, derivatives of a fenotiazin, tricyclic antidepressants expressiveness of peripheral holinoblokiruyushchy effects amplifies, with Chlorpromazinum - reduction of its concentration in plasma is possible.

Under the influence of Reserpinum protivoparkinsonichesky action of a trigeksifenidil decreases (exhaustion of reserves of a dopamine in the central nervous system, activation of cholinergic neurons).

The levodopa increases protivoparkinsonichesky activity of a trigeksifenidil. At use together with a levodopa the dosage of both drugs needs to be reduced. Usually in this case 3 - 6 mg of a trigeksifenidil a day divided into two receptions there are enough.

Under the influence of inhibitors of a monoaminooxidase strengthening of anticholinergic action of the holinoblokator applied at parkinsonism is possible.

At simultaneous use of a trigeksifenidil effect of the nitrates applied sublingual decreases (owing to dryness in a mouth).

Depressive effect of alcohol and the medicines exerting impact on the central nervous system can amplify at use with trigeksifenidily.

Contraindications:

Hypersensitivity to any of drug components, mechanical stenoses of digestive tract, megacolon, closed-angle glaucoma, an ischuria, a prostate hyperplasia (with existence of a residual urine), a fluid lungs, dementia, children's age (up to 12 years), pregnancy, the lactation period.

With care. Dekompensirovanny heart diseases, kidneys or liver, tachycardia, tachyarrhythmia, arterial hypertension, psychosis, acute myocardial infarction, advanced age.

Overdose:

High doses of a trigeksifenidil cause blockade of the postganglionic terminations of a parasympathetic nervous system, the picture of poisoning corresponds to poisoning with atropine (a mydriasis, dryness of mucous membranes of an oral cavity, tachycardia, an atony of intestines and bilious ways, fervescence). Disturbances from the central nervous system are expressed by symptoms of mental and motive excitement, the coma or paralysis of a respiratory center can develop.

Treatment of poisonings: the specific antidote is absent. First aid: gastric lavage, reception of absorbent carbon, symptomatic treatment.

Storage conditions:

According to rules of storage of strong substances. In the place protected from light at a temperature not above 25 °C. To store in the places unavailable to children. A period of validity - 5 years. Not to use after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets of 2 mg. Packaging: on 10 tablets in a blister strip packaging. 1, 2, 3, 4 or 5 blister strip packagings together with the application instruction in a pack from a cardboard.