Cyclodol

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

Exposure to trihexyphenidil 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-anticholinergic, and in addition peripheral m-anticholinergic drug effect.[1]

Indications Cyclodol

It is used for mono- and complex treatment (together with levodopa) for parkinsonism , which has a different nature.

In tablets with a volume of 5 mg, it can be used for such disorders:

• extrapyramidal signs associated with the use of antipsychotics 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 with pyramidal paresis.

Release form

The release of a therapeutic substance is made in tablets with a volume of 2 and 5 mg - 10 pieces inside a cell package; inside the box - 4 such packages.

Pharmacodynamics

In the case of parkinsonism, Cyclodol, like other anticholinergics, weakens the tremor. Less active drug affects muscle stiffness with bradykinesia.

The anticholinergic effect of the medication weakens sweating, salivation and sebum. [2]

The antispasmodic activity of drugs is also associated with anticholinergic effects and direct myotropic effects. [3]

Pharmacokinetics

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

Dosing and administration

The drug dosage is selected individually, starting with the minimum and increasing to the lowest effective one.

In the case of Parkinson's syndrome, the size of the initial portion is equal to 1 mg of trihexyphenidil hydrochloride per day (for a dosage of 1 mg, Cyclodol is not used). At 3–5 day intervals, this portion is gradually increased by 1–2 mg per day until the optimal therapeutic effect is achieved. The maintenance dosage is in the range of 6-16 mg per day (divided into 3-5 applications). A maximum of 20 mg of medication can be taken per day.

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

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

For children aged 5-17 years, the drug is prescribed only for the treatment of extrapyramidal dystonia. At the same time, they can take no more than 40 mg of medicine per day.

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

It is necessary to cancel therapy gradually, reducing the dosage of trihexyphenidil in the period of 1-2 weeks, until it is completely discontinued. In the case of a sharp withdrawal of drugs, the patient's condition may worsen - an aggravation of the symptoms of the disease will begin.

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

• Application for children

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

Use Cyclodol during pregnancy

Cyclodol should not be used during pregnancy.

Due to the lack of information regarding the elimination of trihexyphenidil with breast milk, if you need to take medication, you must stop breastfeeding.

Contraindications

The main contraindications:

• severe intolerance to trihexyphenidil or other elements of the drug;
• delay in urination;
• glaucoma;
• hypertrophy of the prostate, in which there is a violation of urinary outflow, and prostate adenoma;
• stenosing forms of diseases affecting the gastrointestinal tract (achalasia, pyloroduodenal stenosis, etc.);
• intestinal atony, intestinal obstruction of a paralytic or mechanical type, atonic forms of constipation and megacolon;
• tachyarrhythmia, including atrial fibrillation;
• decompensated cardiopathy.

Side effects Cyclodol

Mental and NS related problems: headaches, irritability, weakness and sleep disturbances (including drowsiness), as well as dizziness, vomiting and nausea. There may be an exacerbation of the course of myasthenia gravis.

In the case of taking too high dosages or severe drug intolerance, nervousness, cognitive dysfunction (disorder of short-term and instant memory, confusion), anxiety, euphoria and agitation, and in addition, delirium, insomnia, hallucinations and paranoid signs may be noted (especially in the elderly and individuals with atherosclerosis).

There is information about the development of dyskinesia in the form of involuntary movements of the body, lips, face and extremities (especially in people using levodopa) that have a chorea-like character. If mental disorders appear, it may be necessary to cancel Cyclodol. There are reports of trihexyphenidil abuse associated with its hallucinogenic and euphoric activity.

Impact associated with anticholinergic effect: dryness of the mucous membranes and epidermis (also the development of xerostomia with the possible appearance of dysphagia), hypohidrosis, thirst, hot flashes and hyperthermia; in addition, weakening of bronchial secretion, tachycardia, urinary disorder (urinary retention and difficulty at the beginning of the process) and constipation. Accommodation disorder (this includes cycloplegia), visual blurriness, mydriasis, an increase in IOP, photophobia, and the development of angle-closure glaucoma (sometimes with blindness) can be observed.

There is evidence of the occurrence of paradoxical sinus bradycardia, isolated cases of the development of a purulent form of parotitis, which is secondary to excessive xerostomia, and, in addition, the appearance of intestinal obstruction and dilatation of the large intestine.

Immune disorders: signs of intolerance, including an epidermal rash.

In the case of abrupt withdrawal of the drug, there is an exacerbation of the manifestations of parkinsonism and the onset of ZNS.

The children showed psychosis, chorea, hyperkinesia, weight loss, memory and sleep disorders, and anxiety.

Most of the described signs disappear during therapy or disappear after a dosage reduction or an increase in the interval between drug applications.

Overdose

The use of excessively large portions of trihexyphenidil can provoke dangerous intoxication.

Among the signs of poisoning with anticholinergics are dryness of the mucous membranes and epidermis, facial hyperemia, accommodative paralysis, mydriasis, and in addition, an increase in blood pressure and temperature, swallowing and heart rate disorders (among them tachycardia), vomiting, rapid breathing and nausea. A rash on the upper torso and on the face is possible. In severe poisoning, urinary disorders, muscle weakness and weakening of intestinal peristalsis appear.

Signs of irritation of the central nervous system are: disorientation, confusion, delirium, agitation, hallucinations and hyperactivity; in addition, there is anxiety, ataxia, incoherence, aggressiveness and paranoid disorders; sometimes convulsions appear. Progression may develop, reaching depression of the central nervous system, respiratory and cardiovascular failure, as well as coma and death.

Therapy must be started very quickly, ensuring the patency of the respiratory tract. Hemodialysis hemoperfusion can be performed exclusively in the first few hours after intoxication. Antiarrhythmic substances should not be prescribed for the development of arrhythmias. Diazepam can be used to control seizures and agitation, but the risk of CNS depression must be taken into account. It is necessary to compensate for acidosis with hypoxia. The use of lactate or sodium bicarbonate is required to eliminate complications affecting the CVS.

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

Interactions with other drugs

Cannabinoid barbiturates, alcohol, opiates and other CNS depressants can lead to the development of an additive effect when used in conjunction with trihexyphenidil, as well as to an increase in sedation. There is a risk of abuse.

Clozapine, nefopam, phenothiazines (among them chlorpromazine), disopyramide, antihistamines (this includes diprazine with diphenhydramine) and amantadine can potentiate cholinolytic side effects.

Tricyclics with anticholinergic effects and MAOIs can lead to potentiation of the anticholinergic effect of the drug due to the development of an additive effect. Among the manifestations of this effect are constipation, xerostomia, urinary retention, active glaucoma, blurred vision, difficulty at the onset of the urinary process and paralytic intestinal obstruction (especially in the elderly). Anticholinergics are used very carefully in combination with MAOIs or tricyclics. When using antidepressants, you need to start taking trihexyphenidil with a reduced dosage; in this case, you need to constantly monitor the patient's condition.

When administered with tranquilizers, the likelihood of a late form of dyskinesia increases, which is why the use of Cyclodol to prevent drug-induced parkinsonism during treatment with tranquilizers is prohibited. Dyskinesia associated with the use of tranquilizers is potentiated when they are administered in combination with trihexyphenidyl.

The drug reduces the effect of domperidone with metoclopramide in relation to the gastrointestinal tract.

The use of the drug in combination with levodopa weakens its absorption and reduces systemic parameters; in this regard, a correction of its portion is required. Due to the fact that this combination is capable of potentiating drug-induced dyskinesia (especially at the beginning of therapy), the standard dosage of trihexyphenidil or levodopa must be reduced when they are combined.

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

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

Reserpine reduces the antiparkinsonian activity of trihexyphenidil, which is why Parkinson's syndrome is potentiated.

Storage conditions

Cyclodol must be kept out of the reach of small children. Temperature indicators - no higher than 25 ° С.

Shelf life

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

Analogs

The analogues of the drug are Romparkin, Parkopan with Tryfen and Trihexyphenidil.