Cyclodolum

General characteristics. Structure:

Active ingredient: trigeksifenidit; 1 tablet contains a trigeksifenidil of a hydrochloride of 2 mg; excipients: lactoses monohydrate, talc, calcium stearate. Main physical and chemical properties: tablets of a round form, white color, with a flat surface, with slanted edges.

Pharmacological properties:

Pharmacodynamics. Cyclodolum - anticholinergic drug of the central action, breaks bonds between a dopamine and acetylcholine in the central nervous system.
In the central nervous system thanks to a trigeksifenidil the cholinergic effects caused by deficit of a dopamine are weakened. Drug renders expressed central N-holinoblokiruyushchee, and also peripheral M-holinoblokiruyushchee action.
At parkinsonism Cyclodolum, as well as other holinoblokiruyushchy drugs, reduces a tremor. In a smaller measure drug influences rigidity of muscles and a bradykinesia. Owing to holinoblokiruyushchy effect of drug the sialosis, a potovydeleniye and greasiness of skin decreases. Spasmolytic effect of drug is also connected with anticholinergic activity and direct myotropic impact.

Pharmacokinetics. After intake drug is quickly soaked up, gets through a blood-brain barrier. The elimination half-life averages 6-10 hours. There are no data on distribution, linkng with proteins of a blood plasma, metabolism and clearance of a trigeksifenidil, change of removal of drug at abnormal liver functions and kidneys (including at a hemodialysis), about penetration through a placenta and in maternal milk.

Indications to use:

Monotherapy and combination therapy (with a levodopa) parkinsonism of various origin.

Route of administration and doses:

The dose of drug needs to be selected individually, starting with the lowest, raising it to the minimum effective.
At parkinsonism syndromes: the initial dose makes 1 mg of a trigeksifenidil of a hydrochloride a day. Each 3-5 days gradually raise this dose on 1-2 mg a day to obtaining optimum medical effect. The maintenance dose makes 6-16 mg a day, distributed on 3-5 receptions. The maximum daily dose - 20 mg.
For treatment of the extrapyramidal frustration connected with reception of medicines: appoint 2-16 mg of a trigeksifenidil of a hydrochloride a day, depending on weight of symptoms. The maximum daily dose - 20 mg.
Anticholinergic therapy of other extrapyramidal frustration: the dose of drug needs to be regulated gradually, raising every day an initial dose of 2 mg of a trigeksifenidil of a hydrochloride to minimum effective maintenance dose which can exceed that maximum quantity which is appointed at other indications. The maximum daily dose makes 50 mg.
Cyclodolum is intended to children and teenagers from 5 to 17 years only for treatment of extrapyramidal dystonias. The maximum daily dose - 40 mg of a trigeksifenidil of a hydrochloride.
Administration of drug does not depend on time of the use of food. The tablet is recommended to be washed down with enough liquid (150-200 ml). At hypersalivation if it was observed prior to treatment, trigeksifenidit it is necessary to accept after food. At development in the course of treatment of a xerostomia Cyclodolum is appointed to food (if at the same time there is no nausea).
It is necessary to complete treatment gradually, reducing a dose of a trigeksifenidil for 1-2 weeks, to its full cancellation. Sharp drug withdrawal can lead to a sudden aggravation of symptoms of the patient at the expense of an aggravation of symptoms of a disease.
Duration of treatment is determined by the doctor individually in each case.

Features of use:

Cyclodolum is applied with care at a prostatauxe (adenoma) without existence of a residual urine, at arterial hypertension, at heart diseases, kidneys and a liver.
Throughout treatment it is necessary to control intraocular pressure regularly.
At patients 60 years are more senior selection of a dose is carried out with special care (there is a high risk of hypersensitivity). Use twice of a smaller dose is sufficient for obtaining the expected effect.
At use of Cyclodolum it is not necessary to take alcohol.
At long treatment intensity of the undesirable reactions caused by anticholinergic activity of a trigeksifenidil considerably decreases.
It must be kept in mind that to drug there can be a medicinal dependence.

Ability to influence speed of response at control of motor transport or other mechanisms.
During treatment it is necessary to abstain from control of vehicles and work with potentially dangerous mechanisms as ability to concentration of attention decreases and time of psychomotor reaction is extended.

Use during pregnancy or feeding by a breast.
Considering that there are no data on use of a trigeksifenidil by pregnant women, drug is not used during pregnancy.
As there are no data on excretion of a trigeksifenidil with maternal milk, in case of drug use by the women nursing feeding should be stopped.

Children.
To children and teenagers (except cases of extrapyramidal dystonias) Cyclodolum is not appointed as sufficient experience about use of a trigeksifenidil in these age categories is not accumulated.

Side effects:

From the central nervous system: headache, accommodation disturbance, drowsiness, irritability, nausea and vomiting. Seldom (at the raised doses or hypersensitivity) the concern, disturbance of consciousness, memory and dream can be observed. Very seldom - the involuntary movements in the form of diskineziya (especially at patients who accept levodopa drugs).
The effects caused by anticholinergic activity: dryness of a mucous membrane of an oral cavity, reduced potovydeleniye, lock, disturbance of an urination, tachycardia; seldom – a mydriasis, a vision disorder; very seldom – bradycardia.
Allergic reactions: enanthesis.
The majority of these symptoms pass during treatment or are eliminated due to reduction of a dose or increase in intervals between administrations of drug.

Interaction with other medicines:

Simultaneous use of Cyclodolum with difengidraminy or isopromethazine can lead to manifestations of the undesirable reactions connected with strengthening of anticholinergic action.
At simultaneous use of quinidine and Cyclodolum anticholinergic influence on cordial activity (braking of atrioventricular conductivity) amplifies.
Under the influence of Reserpinum protivoparkinsonichesky action of a trigeksifenidil decreases that leads to strengthening of a syndrome of parkinsonism.
Under the influence of MAO inhibitors strengthening of anticholinergic action M-holinoblokatorov, applied at parkinsonism is possible.
If Cyclodolum is applied in a combination with other protivoparkinsonichesky drugs (for example, a levodopa), its dose has to be considerably reduced as such combination can strengthen dyskinesia, especially in an initiation of treatment.
The dyskinesia caused by use of tranquilizers also amplifies at a concomitant use of Cyclodolum.
At simultaneous use Cyclodolum weakens effect of Metoclopramidum and Chlorpromazinum.
Interaction of Cyclodolum with alcohol strengthens effect of alcohol.

Contraindications:

• Hypersensitivity to a trigeksifenidil or to other components of drug;
• glaucoma;
• urination delay;
• a prostatauxe (adenoma) with existence of a residual urine;
• obstructive diseases of digestive tract;
• fibrillation of auricles;
• pregnancy;
• children's age up to 5 years.

Overdose:

Use of a trigeksifenidil in high doses can lead to dangerous poisonings.
Symptoms: the hyperemia of the person, a xeroderma and mucous membranes, swallowing disturbance, fervescence and expansion of pupils can be the first displays of intoxication. Displays of heavy intoxication are the general muscular weakness, disturbance of a mochevyvedeniye, decrease in a vermicular movement of intestines, a condition of excitement or a spasm, consciousness disturbance, sometimes a loss of consciousness, an apnoea and heavy disturbances of cordial activity (tachycardia, disturbances of a rhythm).
Treatment needs to be begun as soon as possible. The hemodialysis and hemoperfusion are shown only for the first hours after poisoning. Use of bicarbonate or sodium lactate is necessary for elimination of complications from cardiovascular system.
Physostigmine is applied to therapy of various symptoms of intoxication (a delirium, a coma, extrapyramidal frustration); tachyarrhythmias, frequent ventricular extrasystoles, various blockade. Infusionally enter 2-8 mg of physostigmine under ECG monitoring. In case of physostigmine overdose (time of semi-removal of 20-40 minutes) drug of the choice is atropine which 0,5 mg are capable to counteract 1 mg of physostigmine.

Storage conditions:

To store in dry, isolated, protected from light, the place, unavailable to children, at a temperature not above 25ºС.

Period of validity - 5 years.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in the blister, on 4 blisters in a pack.