Pronoran - instructions for use, reviews, analogs and forms of release (tablets 50 mg) drugs for the treatment of Parkinson's disease, memory impairment and attention in the aging process in adults, children and pregnancy. Composition and side effects

In this article, you can read the instructions for using the drug Pronoran. There are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors specialists on the use of Pronoran in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Pronoran in the presence of existing structural analogues.Use to treat Parkinson's disease, memory impairment and attention in the aging process in adults, children, as well as during pregnancy and lactation. Composition of the preparation.

Pronoran - is an agonist of dopaminergic receptors. Penetrates into the bloodstream of the brain, where it binds to the dopaminergic receptors of the brain, showing high affinity and selectivity for dopaminergic receptors such as D2 and D3.

The mechanism of action of pyribedil (the active ingredient of the drug Pronoran) determines the main clinical properties of the drug for the treatment of Parkinson's disease both at the initial and later stages of the disease with exposure to all major motor symptoms. In addition to affecting dopaminergic receptors, pyribedil displays antagonist activity in two major alpha-adrenergic receptors of the central nervous system (alpha2A and alpha2C).

The synergistic effect of pyribedil, as an α2-receptor antagonist and a dopaminergic receptor agonist in the brain, has been demonstrated in various animal models with Parkinson's disease: prolonged use of pyribedil leads to less pronounced dyskinesia,than the use of levodopa, with similar efficacy in relation to reversible akinesia, concomitant Parkinson's disease.

During pharmacodynamic studies in humans have shown cortical arousal electrogenesis dopaminergic type as in waking and at bedtime to the manifestation of clinical activity in relation to the various functions controlled by dopamine. This activity was demonstrated using a behavioral or psychometric scale. It has been shown that in healthy volunteers, piribedil improves attention and vigilance associated with cognitive tasks.

Efficacy pronoran as monotherapy or in combination with levodopa in the treatment of Parkinson's disease was studied in three double-blind, placebo-controlled clinical studies (Study 2 compared with placebo and one study compared to bromocriptine). The study involved 1103 patients of the 1-3 stages on the scale of Hen and Jahr (Hoehn & Jahr), 543 of whom received Pronoran. It has been shown that in a dosage of 150-300 mg per day, Pronoran is effective in all motor symptoms with a 30% improvement in the Unified Assessment ScaleParkinson's disease (UPDRS) Part 3 (motor) for more than 7 months with monotherapy and 12 months in combination with levodopa. Improvement of the "activity in daily life" part on the UPDRS 2 scale was evaluated in the same values.

In monotherapy, the statistically significant ratio of patients requiring emergency treatment with levodopa receiving pyribedil (16.6%) was less than in the placebo group (40.2%).

The presence of dopaminergic receptors in the vessels of the lower limbs explains the vasodilating effect of pyribedil (increases blood flow in the vessels of the lower extremities).

Composition

Piribedil + auxiliary substances.

Pharmacokinetics

Pronoran is quickly and almost completely absorbed from the digestive tract and is intensively distributed. The maximum concentration (Cmax) of pyribedil in the blood plasma is achieved 3 to 6 hours after oral administration of the controlled-release dosage form. Binding to plasma proteins is average (unbound fraction is 20-30%). Due to the low connectivity of pyribedil with plasma proteins, the risk of drug interaction when used with other drugs is low. Piribedil is intensively metabolized in the liver and excreted mainly in the urine: 75% of absorbed pyribedil is excreted by the kidneys in the form of metabolites.The plasma elimination of piribedil is biphasic and consists of an initial phase and a second, slower phase, leading to a stable concentration of pyribedil in the blood plasma for more than 24 hours.

Indications

• as an auxiliary symptomatic therapy for chronic cognitive impairment and neurosensory deficit in the course of aging (attention, memory, etc.);
• Parkinson's disease in the form of monotherapy (in forms predominantly involving tremor) or in combination therapy with levodopa at both the initial and later stages of the disease, especially in forms involving tremor;
• as an auxiliary symptomatic therapy for intermittent claudication due to obliterating diseases of the arteries of the lower limbs (stage 2 according to the classification of Lerish and Fontaine);
• therapy of symptoms of ophthalmic diseases of ischemic origin (including reduction of visual acuity, narrowing of the field of view, decrease in contrast of colors).

Forms of release

Controlled-release tablets coated with 50 mg.

Instructions for use and dosing regimen

Inside.The tablet should be taken after a meal, washed down with half a glass of water, without chewing.

For all indications (except for Parkinson's disease), the drug is prescribed in a dose of 50 mg (1 tablet) once a day. In more severe cases, 50 mg twice a day.

With Parkinson's disease in the form of monotherapy, 150-250 mg per day (3-5 tablets per day) are divided into 3 divided doses per day. If you need to take the drug at a dose of 250 mg, it is recommended to take 2 tablets 50 mg in the morning and in the afternoon and 1 tablet 50 mg in the evening.

When used in combination with drugs levodopa daily dose is 150 mg (3 tablets): it is recommended to divide into 3 divided doses.

When choosing a dose in case of its increase, it is recommended to titrate the dose, gradually increasing by 1 tablet (50 mg) every 2 weeks.

Discontinuation of treatment

A sharp cessation of therapy with a dopaminergic receptor agonist is associated with a risk of malignant neuroleptic syndrome (CNS). To avoid this, you should reduce the dose of Pronoran gradually, until complete withdrawal.

Disorder of habits and drives

To avoid the risk of occurrence of disorders of habits and drives, the lowest effective dose of the drug should be given.If such symptoms occur, consider lowering the dose or gradually stopping therapy with the drug.

Patients with hepatic and / or renal insufficiency

Studies of the use of Pronoran in this group of patients have not been conducted. In patients with hepatic and / or renal insufficiency, Pronoran should be used with caution.

Side effect

• mental disorders, such as confusion, excitement, hallucinations (visual, auditory, mixed), disappearing when the drug is withdrawn;
• aggression, psychotic disorders (delirium, delirium), dizziness, disappearing when the drug is withdrawn;
• drowsiness;
• dyskinesia (movement disorders);
• hypotension;
• Orthostatic hypotension with loss of consciousness or malaise or lability of blood pressure;
• minor gastrointestinal disorders (nausea, vomiting, flatulence) that can occur, especially when selecting the appropriate individual dose;
• pathological propensity to gambling;
• increased libido;
• hypersexuality;
• obsessive desire to shop;
• overeating / compulsive overeating;
• peripheral edema;
• risk of developing allergic reactions to the dye crimson, which is part of the drug.

Contraindications

• increased individual sensitivity to pyribedil and / or excipients included in the preparation;
• collapse;
• acute myocardial infarction;
• joint reception with neuroleptics (except clozapine);
• Children under 18 years of age (due to lack of data).

Application in pregnancy and lactation

Fertility

Studies in animals have not revealed direct or indirect adverse effects of Pronoran on the development of the embryo and fetus, labor activity and postnatal development.

Pregnancy

It was shown that in mice, pyribedil penetrates the placental barrier and is distributed in the fetal organs.

Due to the lack of data, the drug is not recommended to use Pronoran during pregnancy and in women with preserved reproductive potential, who do not use reliable contraceptive measures.

Breastfeeding period

Due to the lack of data, the drug is not recommended for use during breastfeeding.

Use in children

Contraindicated in children and adolescents under 18 years.The efficacy and safety of the use of Pronoran in children and adolescents under the age of 18 years has not been studied, and at present there is no data on the use of piribedil in this population.

special instructions

It is released on prescription.

Due to the fact that the composition of the drug includes sucrose, patients with intolerance to fructose, glucose or galactose, as well as patients with a deficiency of sucrose isomaltase (a rare metabolic disorder), the drug is not recommended.

Sudden falling asleep

In some patients (especially in patients with Parkinson's disease) on the background of taking piribedil, a state of severe drowsiness sometimes suddenly occurs until sudden falling asleep. Sudden falling asleep during daily activity, in some cases unconscious or occurring without previous symptoms, is extremely rare, but, nevertheless, patients managing the car and / or working on equipment requiring a high degree of attention should be warned about this. If such reactions occur, patients should refuse to drive and / or work on equipment requiring a high degree of attention.In addition, consideration should be given to reducing the dose of piribedil or discontinuing therapy with this drug.

Orthostatic hypotension

It is known that dopamine agonists disrupt the systemic regulation of blood pressure, which can lead to the development of orthostatic hypotension.

It is recommended to monitor blood pressure, especially at the beginning of treatment, due to the general risk of developing orthostatic hypotension associated with dopaminergic drugs.

Given the age of the population receiving treatment with Pronoran, the risk of falls that can be caused by sudden falling asleep, hypotension or confusion is accounted for.

Disorder of habits and drives

Patients should be monitored to detect the development of a behavioral disorder.

Patients and their caregivers should be warned about possible symptoms of behavioral disorders and addictions (gambling addiction, increased libido and hypersexuality, obsessive desire to shop and overeating / compulsive overeating) when taking dopamine agonists, incl. piribedil. If such symptoms occur, consider lowering the dose or gradually stopping therapy with the drug.

Behavioral disorders

There were reported cases of behavioral disorders that were associated with such manifestations as confusion, agitation, aggression. If such symptoms occur, consider lowering the dose or gradually stopping therapy with the drug.

Psychotic disorders

Dopamine agonists can cause or exacerbate psychotic disorders such as delirium, delirium and hallucinations. If such symptoms occur, consider lowering the dose or gradually stopping therapy with the drug.

Dyskinesia (movement disorders)

In patients with advanced Parkinson's disease, levodopa preparations may cause dyskinesia at the beginning of titration of the dose of piribedil. In this case, reduce the dose of piribedil.

Malignant neuroleptic syndrome (CNS)

Symptoms similar to malignant neuroleptic syndrome, with a sharp abolition of dopaminergic drugs, have been reported.

Peripheral edema

There was reported the occurrence of peripheral edema on the background of therapy with dopamine agonists. This should be taken into account when prescribing piribedil.

Excipients

Dye crimson, which is part of the drug, in some patients increases the risk of allergic reactions.

Impact on the ability to drive vehicles and manage mechanisms

Patients with episodes of severe drowsiness and / or sudden falling asleep during piribedil therapy should refrain from managing vehicles and equipment requiring a high degree of attention until these reactions disappear.

Drug Interactions

In connection with the mutual antagonism between dopaminergic antiparkinsonian drugs and neuroleptics, simultaneous administration with neuroleptics (with the exception of clozapine) is contraindicated.

Patients with an extrapyramidal syndrome caused by taking antipsychotics should be treated with anticholinergic drugs and dopaminergic antiparkinsonian drugs should not be prescribed (due to the blocking of dopaminergic receptors by neuroleptics).

Dopaminergic receptor agonists can cause or exacerbate psychotic disorders.If you want the appointment of antipsychotic drugs in patients with Parkinson's disease receiving treatment with dopaminergic antiparkinsonian agents, the dose of the latter should be gradually reduced to the final abolition of (sudden cancellation of dopaminergic drugs linked to the risk of development of "neuroleptic malignant syndrome").

Antiemetic antipsychotics: antiemetic drugs should be used that do not cause extrapyramidal symptoms.

It is not suitable for the simultaneous use of these drugs in connection with the mutual antagonism between dopaminergic antiparkinsonian drugs and tetrabenazine.

It is not recommended simultaneous use of Pronoran with alcohol.

Care should be taken when using pyribedil with other drugs that have a sedative effect.

Analogues of the drug Pronoran

Structural analogs for the active substance:

• Piribedil.

Analogues on the curative effect (agents for the treatment of Parkinson's disease):

• Azilect;
• Benserazide;
• Bromocriptine;
• Duellin;
• Zimox;
• Izik;
• Cognitive;
• Creeded;
• Levodopa;
• Madopar;
• Mendileks;
• Midantan;
• Mirapex;
• On whom;
• Niar;
• Newpro;
• Pantogam;
• Pantogam is an asset;
• Pantokaltsin;
• Parcón;
• Permax;
• Mertz PC;
• Pramipexole;
• Rekvip Modabit;
• Rolprin SR;
• Segan;
• Selegiline;
• Sinemet;
• Stalevo;
• Tasmar;
• Tremonorm;
• Tropacin;
• Phenotropil;
• Cyclodol;
• Eldepril;
• Yumeks.

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