Циклодол®

General characteristics. Structure:

Active ingredient: 2 mg of a trigeksifenidil of a hydrochloride.

Excipients: sucrose, potato starch, cellulose microcrystallic, calcium stearate.

The Protivoparkinsonichesky drug inhibiting cholinergic transfer to TsNS.

Pharmacological properties:

Pharmacodynamics. Cyclodolum of Grindeks is a sinteticheskimkholinoblokator which reduces characteristic of parkinsonism tremor, muscle tension and a bradykinesia. Cyclodolum of Grindeks possesses strong m-holinoblokiruyushchim and weak N-holinoblokiruyushchim action. The mechanism of action is based on its ability to compete with acetylcholine on a postsynaptic membrane.

Pharmacokinetics. At oral administration trigeksifenidit quickly and it is completely soaked up from a digestive tract. Binding by plasma sbelka about 90%. The effect is reached within an hour. Elimination half-life of 5-10 hours. Trigeksifenidil possesses a high lipotropnost, well passes through hematoencephalic and placental barriers. Trigeksifenidil is hydrolyzed in fabrics under the influence of nonspecific esterases on alcohol and organic acids, a small part trigeksifenidit выделяетсяв not changed look through kidneys.

Indications to use:

- parkinsonism, Parkinson's disease;

- the extrapyramidal disturbances caused by neuroleptics;

- the spastic paralyzes connected by sporazheniye of extrapyramidal system;

- Littl's disease.

Route of administration and doses:

The dosage is selected individually. Drug should be accepted to food.

Begin reception with a dosage – 1 mg a day. The dose is increased gradually by 2 mg every 3-5 days. A 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 makes – 10 mg, a daily dose – 20 mg of a trigeksifenidil. Duration of a course of treatment the opredelyaetlechashchy doctor for each patient individually depending on disease severity.

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

Elderly patients are more sensitive to this drug therefore they should use smaller doses.

In children's practice it is not used due to the lack of clinical data on use for children and teenagers aged up to 18 years.

Features of use:

Very carefully it is necessary to apply Tsiklodol Grindeks at elderly patients and at patients with cardiovascular diseases, with disturbances of functions of a liver and kidneys.

Care is necessary in the following cases: diseases which can lead to life-threatening tachycardia, a syndrome of senile dementia, a myasthenia, a prostatauxe with full bladder emptying.

Abuse cases trigeksifenidily, especially at psychiatric patients are known (in connection with gallyutsioniziruyushchy and eyforiziruyushchy action).

It is necessary to consider that development of medicinal dependence is possible. Treatment cannot be stopped suddenly.

Tablets Cyclodolum Grindekssoderzhat sucrose. This drug should not be used to patients with rare inborn intolerance of fructose, malabsorption of glucose galactose or insufficiency of invertase-isomaltase.

It is necessary to be careful since drug influences speed of response.

It is contraindicated at pregnancy, in the period of a lactation.

In pediatric practice do not apply.

Side effects:

Headache, irritability, nonsense, hallucinations, a mental disorientation (it is preferential at patients with atherosclerosis).

The effects caused by anticholinergic activity: dryness of a mucous membrane of an oral cavity, vision disorder, increase in intraocular pressure, lock, difficulty of an urination, tachycardia, skin rash, dermahemia.

Others: purulent parotitis (owing to a xerostomia).

Often: a mydriasis, accommodation disturbances, photophobia, dryness in a mouth, sweating reduction, a lock, stomach aches, nausea.

Infrequently: urination delay, tachycardia, hypersensitivity.

Seldom: closed-angle glaucoma that is connected with increase in intraocular pressure therefore it is regularly necessary to control the intraocular pressure, fatigue, drowsiness, dizziness, nervousness, sleeplessness, a memory impairment.

Very seldom: bradycardia.

At use of high doses or at treatment of patients with the contributing factors (atherosclerosis, old age or patients with an idiosyncrasy on any medicine) can arise: opacification of consciousness and other disturbances of mentality, unnatural increase in mood, excitement, irritation, vomiting.

In this case it is necessary to stop treatment. At reduction of a dosage or the termination of treatment side effects disappear.

Interaction with other medicines:

The Tsiklodola Grindeks action can amplify at use together with other holinoblokiruyushchy medicines with similar properties (for example, амантадин, some gistaminoblokator, derivatives of a fenotiazin, tricyclic antidepressants, etc.) and together with monoamine oxidase inhibitors (they inhibit the enzymes metabolizing medicines).

At use together with the called medicines there can be following side effects: dryness in a mouth, sight opacification, a delay of an urination and a lock.

Cyclodolum and parasympathomimetics work antagonistic.

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

Braking by Cyclodolum of motility of intestines can interfere with absorption of other medicines.

Cyclodolum weakens impact of Metoclopramidum and domperidon on a digestive tract.

Depressive effect of alcohol and other medicines (kannabioida, barbiturates and opiates) can amplify at use with Cyclodolum.

At use together with a levodopa the dosage of both drugs needs to be reduced. Usually in this case 3-6 mg of Cyclodolum a day divided into 2 receptions there are enough.

Contraindications:

— hypersensitivity to a trigeksifenidil and/or vspomogatelnymveshchestvo;

— not treated delay of an urination;

— a high-quality prostatauxe with an urination delay;

— closed-angle glaucoma;

— obstruction of a digestive tract;

— intestinal impassability;

— fluid lungs;

— tachyarrhythmias;

— acute intoxication alcohol, psychotropic medicines or opiates;

— acute delirium and mania;

— psychosis, dementia;

— late dyskinesia (tardive dyskinesia) – the pathological movements;

— side effect of prolonged use of antipsychotic medicines;

— serious illness of a liver and kidneys;

— pregnancy and period of a lactation;

— children's and teenage age up to 18 years.

Overdose:

Symptoms: high doses of Tsiklodola Grindeks cause blockade of the postganglionic terminations of a parasympathetic nervous system, the picture of poisoning corresponds, in principle, to poisoning with atropine (a mydriasis, dry mucous membranes, tachycardia, an atony of intestines and bilious ways, the increased body temperature, etc.).

Cyclodolum of Grindeks causes also disturbances from the central nervous system (irritability, consciousness disturbances, a derealization and other disturbances of mentality). At more serious poisoning there can be a coma or paralysis of a respiratory center.

Treatment – symptomatic: cold compresses, plentiful drink. It is possible to apply cholinesterase inhibitors (for example, physostigmine), for treatment of cordial complications were successfully used sodium bicarbonate or sodium a lactate, at spasms – diazepam, at deliriums – physostigmine.

The specific antidote is absent. It is necessary to carry out a gastric lavage and to use other possible ways for medicine absorption reduction (purpose of vomitives and a high enema).

Storage conditions:

To store in protected from light and the place, unavailable to children, at a temperature not above 25 °C.

Issue conditions:

According to the recipe

Packaging:

On 25 tablets in a blister strip packaging from a film of polyvinyl chloride and aluminum foil, on 2 planimetric packagings together with the application instruction in the state and Russian languages in a pack from a cardboard.