Ciclodol

Cyclodol is an antiparkinsonian drug; it contains the active ingredient trihexyphenidyl. The drug has a central anticholinergic effect, destroying the bonds that form between acetylcholine and dopamine within the central nervous system.

The effect of trihexyphenidyl leads to a weakening of cholinergic activity associated with a lack of dopamine within the central nervous system. The drug has a powerful central n-cholinergic blocking effect, and in addition, a peripheral m-cholinergic blocking medicinal effect. [ 1 ]

Indicações Ciclodol

It is used for mono- and complex treatment (together with levodopa) for Parkinsonism of various origins.

In tablets of 5 mg it can be used for the following disorders:

• extrapyramidal symptoms associated with the use of neuroleptics or drugs that have a similar effect;
• spastic diplegia;
• Parkinson's disease;
• spastic paralysis caused by disorders affecting the extrapyramidal system;
• sometimes helps to reduce tone and improve motor activity in cases of pyramidal paresis.

Forma de liberação

The therapeutic substance is released in tablets of 2 and 5 mg volume – 10 pieces inside a blister pack; inside a box – 4 such packs.

Farmacodinâmica

In case of Parkinsonism, Cyclodol, like other anticholinergics, weakens tremor. The drug has a less active effect on muscle rigidity with bradykinesia.

The anticholinergic effect of the drug reduces sweating, salivation and sebum production. [ 2 ]

The spasmolytic activity of the drug is also associated with anticholinergic effects and direct myotropic effects. [ 3 ]

Farmacocinética

When administered orally, the drug is absorbed at high speed; the active element overcomes the BBB. Average half-life values are within 6-10 hours.

Dosagem e administração

The medicinal dosage is selected individually, starting with the minimum and increasing to the least effective.

In case of Parkinsonism syndrome, the initial dose is 1 mg of trihexyphenidyl hydrochloride per day (Cyclodol is not used for a dosage of 1 mg). At 3-5-day intervals, this dose is gradually increased by 1-2 mg per day until the optimal therapeutic effect is achieved. The maintenance dose is within 6-16 mg per day (divided into 3-5 applications). A maximum of 20 mg of the drug can be taken per day.

To eliminate extrapyramidal disorders caused by the use of medications, 2-16 mg of the drug is used per day (the portion size depends on the severity of the manifestations). No more than 20 mg of the drug is allowed per day.

During anticholinergic treatment of other extrapyramidal disorders, the dosage of the drug is adjusted gradually, increasing the initial dose (2 mg) daily to the lowest effective maintenance dose (it may exceed the maximum volume used for other indications). A maximum of 50 mg is allowed per day.

Children aged 5-17 years are prescribed the drug only for the treatment of extrapyramidal dystonia. In this case, they can take no more than 40 mg of the drug per day.

The use of the medicine is not tied to food intake. The tablet should be washed down with plain water (0.15-0.2 l). In case of hypersalivation noted before the start of therapy, the medicine is taken after eating. If xerostomia develops during treatment, the medicine is used before meals (provided there is no nausea).

The therapy should be discontinued gradually, reducing the dosage of trihexyphenidyl over a period of 1-2 weeks, until the drug is completely discontinued. In case of abrupt discontinuation of the drug, the patient's condition may worsen - the symptoms of the disease will begin to worsen.

The duration of the therapeutic course is selected by the doctor individually.

• Application for children

The drug is used in pediatrics in children over 5 years of age and only for the treatment of extrapyramidal dystonia.

Uso Ciclodol durante a gravidez

Cyclodol should not be used during pregnancy.

Due to the lack of information regarding the excretion of trihexyphenidyl in breast milk, if you need to take the drug, you should stop breastfeeding.

Contra-indicações

Main contraindications:

• severe intolerance to trihexyphenidyl or other components of the drug;
• urinary retention;
• glaucoma;
• prostate hypertrophy, which is characterized by a violation of urinary outflow, and prostate adenoma;
• stenotic forms of diseases affecting the gastrointestinal tract (achalasia, pyloroduodenal stenosis, etc.);
• intestinal atony, intestinal obstruction of paralytic or mechanical type, atonic forms of obstipation and megacolon;
• tachyarrhythmia, including atrial fibrillation;
• decompensated cardiopathies.

Efeitos colaterais Ciclodol

Mental and nervous system problems: headaches, irritability, weakness and sleep disorders (including drowsiness), as well as dizziness, vomiting and nausea. Exacerbation of myasthenia may occur.

In case of taking too large doses or severe intolerance to the drug, nervousness, cognitive dysfunction (short-term and immediate memory impairment, confusion), anxiety, euphoria and excitement may occur, as well as delirium, insomnia, hallucinations and paranoid symptoms (especially in the elderly and people with atherosclerosis).

There are reports of dyskinesia in the form of chorea-like involuntary movements of the body, lips, face and limbs (especially in people using levodopa). If mental disorders occur, it may be necessary to discontinue Cyclodol. There are reports of trihexyphenidyl abuse due to its hallucinogenic and euphoric activity.

Effects associated with the anticholinergic effect: dryness of the mucous membranes and epidermis (also the development of xerostomia with possible dysphagia), hypohidrosis, thirst, hot flashes and hyperthermia; in addition, decreased bronchial secretion, tachycardia, urinary disorder (urination delay and difficulty in the beginning of the process) and obstipation. Accommodation disorder (including cycloplegia), blurred vision, mydriasis, increased intraocular pressure, photophobia and the development of closed-angle glaucoma (sometimes with blindness) may be observed.

There are data on the occurrence of paradoxical sinus bradycardia, isolated cases of the development of a purulent form of mumps, which is secondary to excessive xerostomia, and also on the occurrence of intestinal obstruction and dilation of the large intestine.

Immune disorders: signs of intolerance, including epidermal rash.

In case of abrupt discontinuation of the drug, an exacerbation of Parkinsonism manifestations and the development of NMS are observed.

Children experienced psychosis, chorea, hyperkinesia, weight loss, memory and sleep disorders, and anxiety.

Most of the described symptoms disappear during the course of therapy or go away after reducing the dosage or increasing the interval between drug administrations.

Overdose

Using excessively large doses of trihexyphenidyl can cause dangerous intoxication.

Signs of poisoning with anticholinergics include dry mucous membranes and epidermis, facial hyperemia, accommodative paralysis, mydriasis, and in addition, increased blood pressure and temperature, swallowing and heart rhythm disorders (including tachycardia), vomiting, rapid breathing, and nausea. A rash may develop on the upper body and face. In severe poisoning, urinary disorders, muscle weakness, and weakened intestinal peristalsis may occur.

Manifestations of CNS irritation include disorientation, confusion, delirium, agitation, hallucinations, and hyperactivity; in addition, anxiety, ataxia, incoherence, aggressiveness, and paranoid disorders occur; convulsions sometimes occur. Progression to CNS depression, respiratory and cardiovascular failure, coma, and death may occur.

Therapy should be initiated very quickly, ensuring patency of the respiratory tract. Hemoperfusion with hemodialysis can be performed only in the first few hours after intoxication. Antiarrhythmic agents should not be prescribed if arrhythmias develop. Diazepam can be used to control seizures and agitation, but the risk of CNS depression must be taken into account. Acidosis with hypoxia must be compensated. The use of lactate or sodium bicarbonate is required to eliminate complications affecting the cardiovascular system.

Physostigmine is administered to remove some signs of poisoning (comatose state, delirium, extrapyramidal disorders), frequent ventricular extrasystoles, tachyarrhythmia and various blockades. The substance is administered during ECG monitoring (2-8 mg, via infusion). In case of poisoning with physostigmine (half-life is 20-40 minutes), the drug of choice is atropine - 0.5 mg of atropine is required to counteract 1 mg of physostigmine.

Interações com outras drogas

Cannabinoid barbiturates, alcohol, opiates and other CNS depressants may cause additive effects when used with trihexyphenidyl, as well as increased sedative effects. There is a risk of abuse.

Clozapine, nefopam, phenothiazines (including chlorpromazine), disopyramide, antihistamines (including diphenhydramine and promethazine) and amantadine may potentiate anticholinergic side effects.

Tricyclics with anticholinergic effects and MAOIs may potentiate the anticholinergic effects of the drug due to the development of an additive effect. Manifestations of such effects include constipation, xerostomia, urinary retention, active glaucoma, blurred vision, difficulty initiating urination, and paralytic intestinal obstruction (especially in the elderly). Anticholinergics should be used with caution in combination with MAOIs or tricyclics. When using antidepressants, trihexyphenidyl should be started with a reduced dosage; the patient's condition should be constantly monitored.

When administered with tranquilizers, the likelihood of late dyskinesia increases, which is why Cyclodol is prohibited for the prevention of drug-induced parkinsonism during tranquilizer treatment. Tranquilizer-associated dyskinesia is potentiated when administered in combination with trihexyphenidyl.

The drug reduces the effect of domperidone and metoclopramide on the gastrointestinal tract.

The use of the drug in combination with levodopa weakens its absorption and reduces systemic indices; in this regard, its dosage must be adjusted. Due to the fact that this combination can potentiate drug-induced dyskinesia (especially at the beginning of therapy), the standard dosage of trihexyphenidyl or levodopa must be reduced when combined.

The therapeutic effect of the drug may be antagonistic to the activity exhibited by parasympathomimetics.

Antiarrhythmic anticholinergics (including quinidine) potentiate the anticholinergic effect on the heart (slowing of AV conduction).

Reserpine reduces the antiparkinsonian activity of trihexyphenidyl, which potentiates parkinsonism syndrome.

Condições de armazenamento

Cyclodol should be stored in a place inaccessible to small children. Temperature indicators - no higher than 25°C.

Validade

Cyclodol can be used within a 5-year period from the date of manufacture of the medicinal product.

Analogues

The analogs of the drug are Romparkin, Parkopan with Trifen and Trihexyphenidyl.