Review of drugs for the treatment of parkinson's disease. Parkinson's drugs prices List of parkinson's disease drugs

The group of drugs that stimulate the synthesis of dopamine include amantadine derivatives: amantadine (Midantan), Gludantan and PC Merz.

PC Merz

Stimulates dopaminergic transmission in the basal ganglia, as well as in other parts of the central nervous system due to the release of a transmitter and inhibition of its reverse neural uptake. It has a neuroprotective effect. By reducing the flow of calcium into the cell, it prevents its destruction. By reducing the excitability of the transmitter system, firstly, it optimizes the dopamine metabolism of the substantia nigra neurons and, secondly, improves the balance between the processes of inhibition and excitation in the striatum.
After oral administration, it is completely absorbed from the gastrointestinal tract. The maximum concentration in blood plasma is reached 5 hours after ingestion. Excreted in the urine. The initial dose is 100 mg per day for 3 days, and then from 4 to 7 days - 200 mg per day, during the second week - 300 mg per day. Depending on the patient's condition, from the third week of treatment, the dose can be increased to 400 mg per day. The maximum dose is 600 mg per day. The interval between morning and subsequent intake should be 6 hours. The last dose of the day is taken before dinner. During the course of treatment, the patient is recommended to drink at least two liters of fluid per day. The drug is also administered as an intravenous infusion of 200 mg 1-2 times a day for 3 hours. The duration of infusion therapy is 5-7 days. With an akinetic crisis, 2-3 infusions per day are prescribed for 7-14 days, followed by a switch to taking medications by mouth at 300-500 mg per day.
Side effects are possible in the form of headache, insomnia, anxiety, hallucinations, peripheral edema, and a decrease in blood pressure. During treatment, an increase in tremor may be observed, which is facilitated by the additional appointment of central anticholinergics. Drinking alcohol is prohibited. The drug is contraindicated in acute and chronic liver and kidney diseases, pregnancy. Restrictions on use: mental illness, epilepsy, thyrotoxicosis, congestive heart failure, orthostatic hypotension, allergic dermatitis. The drug PK Merz is available in tablets of 100 mg; in the form of a solution for infusion of 200 or 500 ml in a bottle.

Drugs for the treatment of Parkinson's disease: inhibiting the destruction of dopamine

The group of drugs that inhibit the destruction of dopamine includes inhibitors of COMT and MAO.
COMT (catechol-O-methyltransferase) is an enzyme that methylates levodopa and dopamine, converting them into inactive metabolites. Drugs in this group thereby increase the concentration of levodopa and dopamine in the blood and brain. Therefore, COMT inhibitors are advisable to be used in conjunction with levodopa drugs. This allows you to reduce the dosage of the latter, which is very important for the prevention and control of side effects that occur when taking levodopa-containing drugs.
There are peripheral COMT inhibitors - entacapone (Comtan), which do not enter the brain, and COMT inhibitors, which pass through the blood-brain barrier - tolcapone (Tasmar). These drugs have a mixed (central and peripheral) effect.
Peripheral COMT inhibitors prevent methylation of levodopa in the gastrointestinal tract and bloodstream. Due to this, a certain level of levodopa is maintained, which, after passing into the central nervous system, serves as a material for the synthesis of dopamine in the brain. COMT inhibitors that cross the blood-brain barrier act both in the periphery and in the central nervous system. COMT inhibitors are used as an adjunct therapy to dopamine-containing drugs in progressive parkinsonism complicated by motor fluctuations.

A drug for the treatment of Parkinson's disease: Tasmar

The effect of the drug manifests itself quite quickly, after the first dose. The maximum effect is observed at a dose of 100-200 mg. The initial dose is 100 mg 3 times a day. Each day, the first dose of Tasmar should be taken with the first dose of levodopa that day, with subsequent doses taken approximately 6 and 12 hours later. The dose of levodopa after the start of taking Tasmar is reduced (by about 30%). Then (after selecting the dose of levodopa), the dose of Tasmara is increased to 200 mg 3 times a day. Patients with moderate hepatic dysfunction should not increase the dose of Tasmar to 200 mg / day. In patients with mild to moderate liver dysfunction, there are no such restrictions. A side effect can manifest itself in the form of nausea, diarrhea (2-4 months after the start of admission), an increase in the level of liver enzymes (within 6-12 weeks), dizziness, the development of dyskinesias, insomnia. Contraindications are the simultaneous use of non-selective MAO inhibitors (selective MAO inhibitors are not contraindicated) or hypersensitivity to the drug. If Tasmar is discontinued, the daily dose of levodopa should be increased in order to prevent the development of neuroleptic malignant syndrome. When taking Tasmara, the urine may turn yellow, which should not be a cause for concern. Use with caution in severe renal and / or hepatic insufficiency. The drug Tasmar is available in tablets of 100 and 200 mg.
Dopamine in the brain is destroyed by monoamine oxidase (MAO). To suppress the destruction of dopamine and thereby increase its level, drugs are used that have a selective ability to inhibit the activity of the enzyme monoamine oxidase. These include selegiline and its derivatives: Cognitive, Selegos, Near.
The metabolites of these drugs also stimulate the release and inhibit the reuptake of dopamine. It has been established that the use of these agents at an early stage of parkinsonism inhibits the degeneration of dopamine-containing neurons in the substantia nigra and striatum, and, consequently, the progression of the disease. Prescribing drugs in this group allows you to reduce the dosage of levodopa drugs, reduce the severity of side effects and significantly reduce, and in some cases completely eliminate dyskinesias that developed while taking levodopa drugs.

Parkinson's disease drug: Cognitive

It has a selective ability to block monoamine oxidase, inhibits the metabolism of dopamine and increases its concentration in the extrapyramidal system. Thus, selegiline induces a therapeutic lengthening and enhancement of the effect of levodopa and, therefore, dopamine. It is completely absorbed in the gastrointestinal tract with a rapid achievement of maximum concentration in the blood. Easily penetrates into brain tissue, accumulates in lipid-rich tissues. The drug is taken orally without chewing, with a small amount of liquid. Cognitive in a dosage of 5 mg is taken 1-2 tablets in the morning after meals or 1 tablet after breakfast and 1 tablet after lunch. Cognitive in a dosage of 10 mg is taken 1 tablet in the morning after meals. The maximum dose is 10 mg. In combination therapy with levodopa, the dosage of the latter can be reduced by 10-30% in the first 2-3 days. Side effects: anxiety, depression, changes in consciousness, speech disturbances, double objects, lower blood pressure, dry mouth, exacerbation of bronchial asthma, skin rash. Contraindications: pregnancy, lactation, hypersensitivity. The drug is available in tablets of 5 or 10 mg.

A drug for the treatment of Parkinson's disease: Nair

MAO-B inhibitor, active ingredient - selegiline. The drug is used to treat parkinsonism and Parkinson's disease. In terms of therapeutic efficacy, conditions of admission, contraindications and possible side effects, it is identical to Cognitive. One Naira tablet contains 5 mg of selegiline.

Drug for the treatment of Parkinson's disease: Selegiline

Is an selective blocker of MAO-B. The drug increases the level of dopamine in the brain by reducing its biotransformation. It is used to treat Parkinson's disease and Parkinson's syndrome both as monotherapy and in combination with levodopa. The initial dose of the drug (5 mg) is taken in the morning. If necessary, it can be increased to 10 mg. Side effects: dry mouth, sleep disorders. Contraindications: hypersensitivity, extrapyramidal disorders not associated with dopamine metabolism disorders. Release form: 5 mg tablets.

Drug for the treatment of Parkinson's disease: Selegos

Active substance - selegiline... Is an selective inhibitor MAO-B, which prevents the breakdown of dopamine in the brain. In addition, the drug inhibits the reuptake of dopamine at the level of presynaptic dopaminergic receptors. Selegos has a neuroprotective effect and can slow down the development of age-related and degenerative changes in neurons. Long-term studies have shown that the addition of Selegos to levodopa in the early stages of Parkinson's disease slows the progression of the disease and reduces the need for levodopa, as well as slows down the onset of disability. In addition, combining the drug with levodopa helps to mitigate the side effects of levodopa. However, it is possible to use the drug as a monotherapy for Parkinson's disease and symptomatic parkinsonism. Selegos has been shown to be beneficial in the treatment of opiate withdrawal symptoms and narcolepsy. It improves cognitive, behavioral and psychomotor functions in patients with Alzheimer's disease and in HIV-infected patients. The use of the drug in Alzheimer's disease leads to a slowdown in the progression of the disease. Also, the drug has a beneficial effect on nervous tics and impaired concentration in children with Tourette's syndrome. Due to the sympatholytic action, the drug has a beneficial effect in patients with heart failure. The advantage of Selegos is its good tolerance, including in combination with other drugs. Available in tablets containing 5 mg of selegiline.

A drug for the treatment of Parkinson's disease: Yumex

Selectively blocks MAO-B, thereby increasing the level of dopamine in the damaged basal nuclei of the brain, especially during therapy with levodopa drugs. Yumex enhances the effect of levodopa, accelerates the onset and lengthens the time of its therapeutic effect. The drug does not interfere with the breakdown of other amines and therefore does not possess side effectcharacteristic of non-selective MAO inhibitors.
Yumex is prescribed for patients with Parkinson's disease and Parkinson's syndrome to increase the effectiveness of therapy with levodopa drugs (to reduce the dose of levodopa, remove resistance to therapy, reduce side effects and increase therapeutic efficacy). The drug is used in all stages of Parkinson's disease and, above all, in cases when the condition of patients changes during the day and is associated with the intake of levodopa, since the dopamine depot is completely depleted overnight, and in the morning it quickly recovers for a short time due to the intake of levodopa, and then it is again depleted until the next dose of levodopa, etc. This is reflected in the condition of patients, in whom a change in the period of akinesia with a period of improved motility and vice versa is clearly noted - the phenomenon of "on-off". The period of akinesia is significantly reduced by taking Yumex. The selection of the Yumex dose is carried out individually. Usually, the initial daily dose of Yumex is 5-10 mg (1-2 tablets). Patients take orally 1 tablet in the morning or 1 tablet in the morning and evening for several weeks, then the dose can be reduced by half. When combined treatment with levodopa drugs, the dose of the latter in some cases must be reduced accordingly. Taking Yumex with other antiparkinsonian drugs is also beneficial and does not affect each other. Side effects are associated with an overdose of levodopa. Insomnia, hallucinations, hyperkinesis, disorders of the gastrointestinal tract, nausea, vomiting, dry mouth may occur. The drug is contraindicated in case of extrapyramidal disorders (hereditary tremor, Hettington's chorea), not associated with a reduced dopamine content, with increased sensitivity to the drug. Release form: tablets of 5 or 10 mg.

Drugs for the treatment of Parkinson's disease: substitution therapy drugs

Group of medicines substitution therapy includes the following drugs: Madopar, Nakom, Sindopa, Sinemet, Tidomet, Duellin. These drugs are combinations of levodopa and peripheral decarboxylation inhibitors (carbidopa or benserazide) in different ratios. They do not stop the disease, but only lead to a known correction of dopamine deficiency.
Levodopa, as an active ingredient, is well absorbed; at oral administration the maximum concentration in the blood is reached after 1-2 hours. Most of levodopa in the liver, kidneys, intestines and other tissues is converted by decarboxylation to dopamine, which does not enter the brain from the peripheral blood. This forces an increase in the dosage of the drug so that the required amount gets into the central nervous system and is already converted into dopamine in it, thereby providing a therapeutic effect. Increasing the dose of the drug, in turn, leads to an increase in side effects. To eliminate this negative effect (destruction of the drug in other tissues before its penetration into the brain), combined drugs were created. The dosage and time of taking each of these funds are selected individually and depend on the therapeutic effect and the severity of side effects. The healing effect develops gradually.
When using levodopa, the following side effects may occur: nausea, vomiting, loss of appetite, decreased pressure when moving to an upright position, accompanied by darkening in the eyes, dizziness and loss of consciousness, heart rhythm disturbances, as well as a number of special phenomena (motor fluctuations and dyskinesias ), which are described below. Elderly patients may experience confusion, hallucinations, and psychosis. When there is side effects the dose of the drug is reduced or discontinued.
In case of nausea, vomiting and other disorders of the functions of the gastrointestinal tract, it is advisable to take the drug during or after meals or for more receptions, while accordingly reducing the single dose. For some time (at the beginning of treatment at the time of adaptation to the drug), these phenomena can be dealt with by taking Cerucal (10 mg 3 times a day) or Motilium (10 mg 3 times a day). This should be done with caution, since these drugs have a dopamine-blocking effect, which can lead to an increase in the phenomena of parkinsonism.
Contraindications to taking the drug are as follows: severe atherosclerosis, hypertension with a significant increase in blood pressure, decompensated diseases internal organs, narrow-angle glaucoma, blood diseases, melanoma, hypersensitivity to the drug. Vitamin B6 should not be taken during treatment with levodopa, as it reduces the effectiveness of its action.
Currently, for the treatment of Parkinson's syndrome, or Parkinson's disease, combined drugs are used in which the active substance levodopa is combined with a decarboxylase inhibitor benserazide (Madopar) or carbidopa (Nakom, Sindopa, Sinemet, Duellin).
It is preferable to use combined drugs with decarboxylase inhibitors drugs Sinemet and Nakom containing 0.25 g of levodopa and 0.025 g of carbidopa, or Madopar drug containing 50 (100 or 200) mg of levodopa and 12.5 (25 or 50) mg of benserazide. The decarboxylase inhibitor contained in them does not penetrate the blood-brain barrier, therefore, prevents the use of levodopa outside the brain and thereby allows you to reduce the dose of the drug.
The side effects of these drugs are less pronounced than that of levodopa. The drugs are of approximately equal effectiveness. Treatment begins with a small dose, then after 3 days it is increased until a clinical effect is achieved. If high doses (1000 mg / day) are ineffective, one should question the diagnosis of Parkinson's disease and think about symptomatic parkinsonism.
Levodopa drugs are most effective in the akinetic-rigid form of parkinsonism (reduce stiffness and eliminate slowness of movements) and are less effective in the trembling form.

Drug for the treatment of Parkinson's disease: Duellin

Antiparkinsonian combined agent - a combination of levodopa (a precursor of dopamine) and carbidopa (an inhibitor of aromatic amino acid decarboxylase). The drug is available in tablets of 100 mg / 10 mg; 100 mg / 25 mg; 250 mg / 25 mg levodopa and carbidopa, respectively. Eliminates hypokinesia, rigidity, tremor, dysphagia, salivation. The presence of the carbidopa enzyme in the preparation allows minimizing side effects from the gastrointestinal tract and the cardiovascular system. The drug is indicated for Parkinson's disease; Parkinson's syndrome (excluding those caused by antipsychotic drugs). Duellin, a combination drug of levodopa and carbidopa, is better tolerated than levodopa drugs. Sudden discontinuation of levodopa is unacceptable; with a sharp cancellation, it is possible to develop a symptom complex resembling a malignant neuroleptic syndrome, including muscle rigidity, increased body temperature, and mental abnormalities. When treating Duellin, activities that require high concentration of attention and speed of psychomotor reactions should be avoided. It is recommended to take the drug with meals or with a small amount of liquid, the capsules are swallowed whole. During long-term treatment, it is advisable to periodically monitor the functions of the liver, hematopoiesis, kidneys and cardiovascular system.

Drug for the treatment of Parkinson's disease: Madopar 125

It is a combination of levodopa and a decarboxylase inhibitor benserazide in a 4: 1 ratio (100 mg levodopa + 25 mg benserazide), which has shown itself to be optimal in clinical trials and in medical practice. It is as effective as high doses of levodopa. Levodopa and benserazide are absorbed mostly in the upper small intestine. The maximum plasma concentration of levodopa is reached approximately 1 hour after taking Madopar. Food intake decreases the rate and extent of absorption of levodopa. When the drug is prescribed after a normal meal, the maximum concentration of levodopa in the blood plasma is 30% less and is reached later. Treatment with Madopar should be started gradually, individually selecting doses and bringing their effect to the optimum. Patients should always swallow regular Madopar capsules without chewing. It should be taken, if possible, at least 30 minutes before or 1 hour after a meal. However, some patients tolerate Madopar better if taken with food. Patients at an early stage of Parkinson's disease are recommended to start treatment with Madopar with taking 1/2 tablet 3-4 times a day. As soon as the tolerance of the drug is confirmed, the dose should be slowly increased, achieving the maximum therapeutic effect, which is achieved, as a rule, with a daily dose of 5-10 Madopar tablets taken in three or more doses. It may take 4 to 6 weeks to achieve optimal effect. If it is necessary to further increase the daily dose, this should be done at intervals of 1 month. The average maintenance dose is 125 mg Madopar 3-6 times a day. The number of receptions (at least three) and their distribution throughout the day should be determined so as to ensure the optimal effect. Patients taking other antiparkinsonian drugs can also receive Madopar. However, as the treatment with Madopar continues and its therapeutic effect manifests itself, it may be necessary to reduce the dose of other drugs or to gradually cancel them. If during the day the patient has strong fluctuations in the action of the drug (the phenomenon of "on-off"), it is recommended either more frequent intake of correspondingly smaller single doses, or, which is preferable, the use of Madopar GSS. Contraindications: diseases of the endocrine system, kidneys, liver, heart, pregnancy, age up to 25 years, hypersensitivity to levodopa, benserazide, combined use of non-selective monoamine oxidase inhibitors is not recommended. Side effects: anorexia, nausea, vomiting and diarrhea, isolated cases of loss or change in taste. These side effects, which are possible at the initial stage of treatment, can be largely eliminated if Madopar is taken with meals or with a sufficient amount of food or liquid, as well as if the dose is increased slowly. In rare cases, skin reactions such as itching and rash. Sometimes - arrhythmias or orthostatic hypotension. Orthostatic abnormalities usually subside after dose reduction. With prolonged therapy with levodopa, it is necessary to periodically monitor the blood picture and the function of the liver and kidneys, since in rare cases it is possible to develop hemolytic anemia, as well as transient leukopenia and thrombocytopenia. In the later stages of treatment, spontaneous movements sometimes occur (for example, such as chorea or athetosis). They can usually be eliminated or reduced to an acceptable level by reducing the dose. In the future, to enhance the therapeutic effect, you can try to increase the dose, since these side reactions do not always occur. When long-term use the drug, its therapeutic efficacy may vary. This manifests itself in episodes of "freezing", weakening of the effect by the end of the dose period and the phenomenon of "on-off". Usually these phenomena can be eliminated or significantly reduced by dose reduction. Subsequently, you can try to increase the dose again to enhance the effect of the treatment, since all these adverse events do not necessarily appear again. In sick old age agitation, anxiety, insomnia, hallucinations, delusions, and temporary disorientation may occur. Release form: capsules of 125 mg (100 mg + 25 mg).

The drug for the treatment of Parkinson's disease: Madopar 250

Contains levodopa and benserazide in a 4: 1 ratio (200 mg levodopa and 50 mg benserazide). Refers to the standard form of Madopar and is available in capsule and tablet forms. Standard Madopar capsules and tablets are equivalent in terms of therapeutic efficacy. Release form: capsules of 250 mg (200 mg + 50 mg); tablets of 250 mg (200 mg + 50 mg).

Drug for the treatment of Parkinson's disease: Madopar fast-acting tablets (dispersible)

Fast Acting Madopar - Special dosage form for patients with dysphagia (swallowing disorders) and those cases when a faster onset of action is required, that is, for patients with akinesia in the early morning hours and in the afternoon, as well as for patients with the phenomenon of "lagging" or "shutdown". The rate of increase in the concentration of levodopa in the blood after taking the fast-acting Madopar is similar to that when taking the usual (standard) Madopar, but the time to reach the maximum concentration tends to be shortened. The absorption parameters of Madopar dispersible tablets in different patients are more uniform than in conventional dosage forms. Fast-acting tablets must be dissolved in a quarter glass of water (25-50 ml). The tablet dissolves completely in a few minutes to form a milky white solution. Since a precipitate can form quickly, it is recommended to stir the solution before taking. The tablets should be taken no later than half an hour after dissolution. Release form: dispersible tablets, 125 mg (100 mg + 25 mg).

The drug for the treatment of Parkinson's disease: Madopar GSS

GSS capsules (hydrodynamically balanced system) are a special dosage form that gives a sustained release of active substances in the stomach in order to achieve a more uniform release of levodopa and prevent symptoms that are associated with a shortening of the time of action of levodopa. The active substance is enclosed in a matrix consisting mainly of hydrocolloid, fats, moisturizing substances. The density of the capsule is less than that of the gastric juice, which allows it to float in the stomach. The interaction of gastric juice with the capsule matrix leads to the formation of a hydrated boundary layer through which the active substance can penetrate. The capsule remains in the stomach for 5-12 hours. This is important, since levodopa is absorbed only at the level of the upper third of the small intestine. Compared with traditional Madopar, the absorption of levodopa from Madopar GSS occurs more slowly. The maximum plasma concentration is 20-30% less than that of conventional dosage forms, and is reached approximately 2-3 hours after administration. The dynamics of plasma concentration is characterized by a longer elimination period than that of conventional dosage forms, which is convincing evidence of the continuous controlled release of active substances. Food intake does not affect the maximum concentration of levodopa, which is reached later, 5 hours after taking Madopar GSS.
The recommended initial dose of Madopar GSS is 1 capsule 3 times a day, and it should not exceed 600 mg per day. Madopar GSS is always taken whole with a small amount of water, regardless of the meal. If necessary, in addition to the morning dose of Madopar GSS, you can additionally take Madopar standard or dispersed to compensate for the delayed action of Madopar GSS. Contraindications and side effects are identical to those observed when taking standard Madopar. Release form: capsules of 125 mg (100 mg + 25 mg).

A drug for the treatment of Parkinson's disease: Nakom

A combination of carbidopa, an aromatic amino acid decarboxylase inhibitor, and levodopa, the metabolic precursor of dopamine. This combination leads to inhibition of the degradation of levodopa in the blood and peripheral tissues and an increase in its level in the brain tissues, where levodopa is converted to dopamine. In this regard, it is possible to use smaller doses of levodopa, while the therapeutic effect is observed faster and the severity of side effects decreases. Nakom is indicated for the treatment of Parkinson's syndrome and disease (except for drug parkinsonism syndrome). The drug primarily affects rigidity, slowness of movement and reduces postural disturbances, is less active in relation to tremor. When taking Nakoma, there is no need to avoid taking vitamin B6. Assign Nakom inside during or after meals. Doses are selected individually, taking into account the characteristics of the action of the main component (levodopa). Usually they start taking 0.5 tablets 1-2 times a day; if necessary, increase the daily dose, adding 0.5 tablets every 2-3 days until the optimal effect is achieved (usually up to 3-6 tablets per day, but not more than 8 tablets per day). Patients who previously received levodopa should stop taking levodopa before starting treatment with Nakom (at least 12 hours), and take Nakom in reduced doses (no more than 3 tablets per day) in the first days. The maintenance dose for most patients is 3-6 tablets per day (no more than 8 tablets per day). Contraindications: angle-closure glaucoma, taking MAO inhibitors and pregnancy. Side effects: hyperkinesis, headache, unsteadiness when walking, nausea, vomiting, depression, hallucinations, in some cases a change in the blood formula can be observed. Release form: tablets containing 250 mg of levodopa and 25 mg of carbidopa.

The drug for the treatment of Parkinson's disease: Sindopa

Combined drug, available in three versions, depending on the dose of levodopa and carbidopa: Sindopa 110, containing 100 mg levodopa and 10 mg carbidopa; Sindopa 275 containing 250 mg of levodopa and 25 mg of carbidopa; Sindopa Plus, containing 100 mg of levodopa and 25 mg of carbidopa. The selection of an individual dose is carried out gradually - taking into account the severity of clinical manifestations, drug tolerance and the presence of motor fluctuations and dyskinesias. The presence of drugs with different dosages of the active substance and carbidopa allows for a more differentiated influence on the manifestations of the disease, taking into account the development of complications of long-term administration of the drug. Contraindications: hypersensitivity, angle-closure glaucoma, melanomas, taking MAO inhibitors. Side effects: nausea, vomiting, cramps in the calf muscles, delirium, depression, insomnia, anxiety, dry mouth, disorders of the gastrointestinal tract, visual disturbances.

A drug for the treatment of Parkinson's disease: Sindopa 110

Contains 100 mg levodopa and 10 mg carbidopa. It is the main drug used to treat patients with Parkinson's syndrome or Parkinson's disease, who do not have complications that occur with prolonged use of levodopa: motor fluctuations or dyskinesias. Release form: tablets (100 mg + 10 mg).

The drug for the treatment of Parkinson's disease: Sindopa Plus

Contains 100 mg levodopa and 25 mg carbidopa. The increased content of carbidopa reduces the side effects that occur when taking levodopa, allows you to achieve an optimal therapeutic effect with a lower dose and delay the onset of complications associated with levodopa replacement therapy. Release form: tablets (100 mg + 25 mg).

A drug for the treatment of Parkinson's disease: Sindopa 275

The drug for the treatment of Parkinson's disease: Sinemet

Combined preparation containing an active ingredient levodopa and decarboxylase inhibitor carbidopa... It is used to treat Parkinson's disease and symptomatic parkinsonism. Sinemet provides a more effective and prolonged plasma concentration of levodopa than with levodopa alone. The drug reduces tremors, improves the function of swallowing, salivation, reduces postural instability, but is especially effective in relation to rigidity and bradykinesia. Sinemet is generally effective for motor fluctuations. It can be taken along with vitamin B6. The optimal daily dose of Sinemet is selected individually for each patient. For beginners in the treatment of parkinsonism with taking Sinemet, the initial dose is 1/2 tablet 1-2 times a day. If necessary, the daily dose can be gradually increased by 1/2 tablet until the optimal effect is achieved. The maximum daily dose is 8 tablets. Contraindications: hypersensitivity, angle-closure glaucoma, psychosis, hepatic and / or renal failure, heart failure, blood diseases, depression, melanoma and suspicion of it, diseases of the endocrine system, pregnancy, lactation, childhood (up to 12 years old). Side effects: violent movements, psychotic disturbances, depression, nausea, palpitations, arrhythmia, orthostatic hypotension, decreased appetite, dizziness, drowsiness, violation of the blood count. Release form: tablets (100 mg + 10 mg and 250 mg + 25 mg).

Drug for the treatment of Parkinson's disease: Sinemet CR

Antiparkinsonian combined agent - combination levodopa(the precursor of dopamine) and carbidopes (aromatic amino acid decarboxylase inhibitor). It is used to treat Parkinson's disease or Parkinson's syndrome. Eliminates hypokinesia, rigidity, tremor, dysphagia, salivation. It is effective in the treatment of patients with developing complications of prolonged use of Levodopa. Especially effective for reducing the "off" period. The optimal daily dose is set individually. The tablets are taken orally without chewing. The initial dose of the drug for patients who have not previously received levodopa is 1/2 tablet 2 times a day, followed by a gradual increase if necessary. If the patient previously took the usual Sinemet, then when switching to Sinemet CR the dose of the drug must be increased by 10-30%. In most cases, the optimal dose of the drug is 2 to 8 tablets, maximum 12 tablets. Side effects: dizziness, confusion, sleep disturbance, depression, dystonia, visual impairment, orthostatic hypotension, dyskinesia, palpitations, shortness of breath. Contraindications: simultaneous intake of MAO, melanoma, angle-closure glaucoma, hypersensitivity. Release form: tablets (200 mg + 50 mg).

Drug for the treatment of Parkinson's disease: Tidomet LS

Combined preparation containing levodopa (100 mg) and a decarboxylase inhibitor carbidopa (10mg). It is used to treat Parkinson's disease and Parkinson's syndrome. The presence of carbidopa in the drug inhibits the destruction of levodopa, prolonging its action and creating conditions for a more complete flow of levodopa into the brain tissue. Tidomet reduces many manifestations of parkinsonism, such as stiffness, slowness of movement, postural disturbances, and, to a lesser extent, tremors. The effective dose of the drug is selected individually, starting with a minimum (1/2 tablet) 1-2 times a day, followed by a gradual increase in 1/2 tablet until an optimal result is obtained, which is usually observed after 7-10 days. Contraindications: hypersensitivity to the drug, glaucoma, taking MAO inhibitors. Side effects: nausea, vomiting, loss of appetite, with prolonged use - involuntary violent movements, orthostatic hypotension. Release form: tablets (100 mg + 10 mg).

A drug for the treatment of Parkinson's disease: Tidomet Plus

Combined preparation containing 2.5 times more carbidopa than Tidomet LS ( levodopa - 100 mg and carbidopa - 25 mg). This ratio of the active substance levodopa and the decarboxylase inhibitor carbidopa (4: 1) allows achieving a therapeutic effect with a lower dose of levodopa, which is of particular importance in patients with motor fluctuations or dyskinesias. Contraindications and side effects are similar to those described in Tidomet LS. Release form: tablets (100 mg + 25 mg).

A drug for the treatment of Parkinson's disease: Tidomet Forte

Combined preparation containing a higher dose than Tidomet LS levodopa (250 mg) and carbidopa (25 mg)... Taking the drug with increased dose the active substance is necessary to obtain a faster therapeutic effect in patients with morning dose deficit, especially with impaired swallowing, and with evening intake - to exclude the occurrence of morning dose deficit. Release form: tablets (250 mg + 25 mg). With prolonged use of drugs containing levodopa, special phenomena of movement disorders develop. These include fluctuations in the patient's motor activity during the day (motor fluctuations) and the appearance of various violent movements (dyskinesias).
Their development is associated with a progressive decrease in the neurons of the substantia nigra and striatum, through which the action of levodopa is mediated, as well as with a number of other factors. It was found that these phenomena occur in all patients approximately 3-6 years after the start of treatment with levodopa drugs.
The following variants of motor fluctuations are distinguished: 1) the phenomenon of "depletion" of a single dose of levodopa, which manifests itself in the fact that the effect of the dose is reduced ("depleted") and the symptoms of the disease return before the next dose is taken; 2) the phenomenon of "delayed onset of effect" of the dose taken is characterized by the fact that the onset of action of the drug occurs later than usual (more than 60 minutes after administration); 3) the phenomenon of "on-off" is manifested by the fact that the beginning and end of the action of the drug come suddenly, and not smoothly, as it was before; these phenomena can occur after a certain time after administration or independently of it; 4) the phenomenon of "freezing" is manifested by a sudden, unpredictable in time blockade of the patient's movements, which occurs when walking, turning, passing through a doorway and other situations.
There are the following variants of dyskinesias: 1) biphasic dyskinesias that occur at the beginning and end of the drug; 2) dyskinesias appearing at the height (peak) of the dose; 3) dyskinesia that occurs during the termination of the next dose of the drug. Dyskinesias manifest themselves in different ways. These can be light, quick violent movements, sometimes invisible to the patient, in the area of \u200b\u200bthe face, trunk, legs, or heavy generalized movements like dystonia, which may be accompanied by painful muscle tension.
To combat motor fluctuations and dyskinesias, it is usually sufficient to increase the frequency of taking the drug (up to 5 times a day), respectively, reducing a single dose, or use drugs with prolonged action, while the daily dose of the drug should be increased by 20-30% due to its incomplete absorption from the intestine. These techniques are effective in the presence of dose-depletion, on-off, and some dyskinesias.
The use of prolonged forms of the drug is also advisable for dyskinesia that occurs at the height of the dose action, since this dosage form provides a more stable drug concentration in the blood without significant peaks. With the phenomenon of delayed onset of the dose, the drug should be taken 30-40 minutes before meals or Madopar soluble tablets should be used, which are rapidly absorbed from the gastrointestinal tract. If these techniques are unsuccessful, it is necessary to use drugs from other groups in combination with levodopa drugs or in monotherapy.
It should be emphasized that stopping the intake of levodopa drugs can lead to a sharp deterioration in the condition, up to the complete immobility of the patient with the development of disorders of swallowing and speech. This condition is called an akinetic crisis. It can lead to the development of hypostatic pneumonia, pressure ulcers, deep vein thrombosis, and other complications. With sudden withdrawal of levodopa drugs, neuroleptic malignant syndrome may also develop.

For citation:Shtok V.N., Fedorova N.V. MODERN PRINCIPLES OF TREATMENT OF PARKINSONISM // RMZH. 1998. No. 13. P. 4

Parkinsonism is a syndrome of lesion of the extrapyramidal system, the pathogenesis of which is associated with progressive degeneration of nigrostriatal neurons, as a result of which dopamine synthesis and the activity of dopaminergic systems decrease, while the activity of cholinergic systems is relatively or absolutely increased. As antiparkinsonian agents, anticholinergic drugs, aminoadamantane derivatives, DOPA-containing agents, monoamine oxidase type B inhibitors, catechol-O-methyltransferase inhibitors and dopamine receptor agonists are used. With a significant unilateral predominance of tremor and rigidity, which are not amenable to pharmacotherapy, as well as with pronounced adverse reactions against the background of the latter, they resort to stereotoxic destructive operations. Intracerebral transplantation of dopaminergic neurons in the mesencephalon of the human embryo opens up certain prospects.

Parkinsonism is a syndrome involving the extrapyramidal system, whose pathogenesis is associated with progressive degeneration of nigrostriatal neurons, leading to reductions in the synthesis of dopamine and in the activity of dopamine systems and to a relative or absolute increase in the activity of cholinergic systems. Cholinolytic drugs, aminoadamantane derivatives, DOPA-containing agents, monoamine oxidase B inhibitors, catechol-o-methyl-transferase inhibitors, and dopamine receptor agonists are used as antiparkinsonian agents. Stereotoxic destructive surgery should be resorted to if only drug-resistant tremor and rigidity are prevalent and if drug therapy causes significant adverse reactions. Intracerebral grafting of dopamine neurons of the human embryonal mesencephalon provides certain prospects.

V.N. Stock, N.V. Fedorova
Russian medical Academy postgraduate education, Center for Extrapyramidal Diseases of the Nervous System of the Ministry of Health of the Russian Federation, Clinical Hospital named after S.P. Botkin
V.N. Shtok, N.V. Fedorova
Russian Medical Academy of Postgraduate Training, Center for Exprapyramidal Diseases of the Nervous System, Ministry of Health of the Russian Federation, S.P. Botkin Clinical Hospital

P arkinsonism is a syndrome of lesions of the extrapyramidal nervous system, characterized by a combination of tremors, extrapyramidal muscle rigidity with a "cogwheel" symptom and akinesia. As the disease progresses, a fourth symptom appears - postural instability.
Distinguish between Parkinson's disease, secondary parkinsonism (vascular, medicinal, post-traumatic, post-encephalitic, etc.) and parkinsonism syndrome in degenerative and hereditary diseases of the central nervous system (strionigral degeneration, progressive supranuclear palsy, olivopontocerebellar atrophy, idiopathic disease, orthostatic hypothesis) chorea of \u200b\u200bHuntington, familial calcification of the basal ganglia, etc.). Despite the different etiology of these diseases, the pathogenesis of clinical symptoms is similar and is associated with progressive degeneration of nigrostriatal neurons, as a result of which dopamine synthesis and the activity of dopaminergic systems decrease, while the activity of cholinergic systems is relatively or absolutely increased. All major approaches to the pharmacotherapy of parkinsonism are aimed at correcting this imbalance of neurotransmitters that ensure the activity of the extrapyramidal nervous system.

Table 1. Anticholinergics and aminoadamantane derivatives

Antiparkinsonian drugs (PPA)

For the pharmacotherapy of parkinsonism, anticholinergic agents, aminoadamantane derivatives, DOPA-containing agents (DSS), monoamine oxidase (MAO) inhibitors of type B, catechol-O-methyltransferase (COMT) inhibitors, and dopamine receptor agonists (ADR) are used.
Individual sensitivity to PPP is variable. The threshold of the effect of PPS is determined by the minimum dose of one PPS that reduces the manifestations of parkinsonism. All PPPs can have side effects. The side effect threshold is determined by the dose of the drug causing the side effects. The “gap” between these thresholds defines the boundaries of the pharmacotherapeutic window, or the value of the optimal individual dose of each PPS.

The general rule when prescribing any PPS is to start treatment with a subeffective dose and then very slowly increase it (on average within 1 - 1.5 months) to select the dose that gives the minimum effect (threshold dose).
The need for this approach is explained by the fact that as the disease progresses, the dose of the threshold of effect increases, and the threshold of the dose causing adverse reactions decreases, that is, it narrows. the boundaries of the pharmacotherapeutic window.

Table 2. DOPA-containing preparations

Treatment with anticholinergic drugs

Cholinolytic drugs in parkinsonism arrest the relative or absolute increase in the activity of cholinergic systems. Despite the fact that various drugs in this group are analogs (Table 1) , in practice, the predominant individual sensitivity of patients to one of them is often noted. In order to identify individual sensitivity at the beginning of treatment, every 3-4 months one anticholinergic drug is replaced by another. In the future, the most effective drug prescribed for constant use with its replacement 1 - 2 times a year for a period of 1 month with another anticholinergic drug to avoid possible addiction. If there are doubts about the effectiveness of the anticholinergic drug, it is canceled. Worsening symptoms of parkinsonism after abrupt withdrawal indicates that the prescribed treatment was effective, and then the drug is resumed. Cholinolytic agents are contraindicated in glaucoma and prostate adenoma. Side effects in the form of dry mouth, blurred vision indicate an individual overdose and require correction of a single and daily dose.
Due to the adverse effect on cognitive functions, treatment with anticholinergic drugs is not started in old and senile age, as well as in patients with dementia.

Table 3. MAO type B inhibitors and COMT inhibitors

Table 4. Dopamine receptor agonists

Treatment with aminoadamantane derivatives

Drugs in this class have anticholinergic properties and improve the circulation of dopamine in dopaminergic synapses. Amantadine hydrochloride analogs (see table. 1) appoint 2 - 3 times a day, 1 tablet (0.1 g). More often, these drugs are added to anticholinergic drugs or DSS when their effect decreases, but they can also be used as a means initial therapy... As a rule, first a half dose (0.05 g) is prescribed 2 - 3 times a day, and then gradually over 3 - 4 weeks it is increased to an average daily dose (0.3 g). Side effects in the treatment with amantadine are anxiety, non-systemic dizziness, the appearance of a "marble" color of the skin of the distal extremities, swelling of the legs, visual illusions... Glucuronide of midantan - gludantan (0.2 g) is inferior in pharmacotherapeutic activity to amantadine hydrochloride, but less often gives side effects.

The daily dose of levodopa should not exceed 3 g, but even with prolonged treatment, this dose causes adverse reactions.
Up to 80% of levodopa taken orally undergoes "premature" decarboxylation, and only 1/5 of the dose taken reaches the brain and is metabolized by cerebral DDC with the formation of dopamine, as well as norepinephrine and adrenaline. If the level of catecholamines formed in the brain exceeds the threshold of side effects, then neurological (dystonia and dyskinesia) and mental (hallucinations, agitation, delirium, confusion) appear side reactions. These manifestations require dose reduction and sometimes drug withdrawal.

Treatment with levodopa drugs in combination with peripheral DDC inhibitors

Preparations containing levodopa with a peripheral DDC inhibitor - carbidopa or benserazide are presented in table. 2 ... Inhibitors of peripheral DDC inhibit premature decarboxylation of levodopa in the gastrointestinal tract and bloodstream(fig. 1) ... The ratio of the amount of levodopa and the DDC inhibitor in different drugs is different(see table 2 ). The higher the content of the inhibitor, the lower the risk of side effects from the gastrointestinal tract and cardiovascular system.
When taking levodopa drugs with a DDC inhibitor, the incidence of cardiovascular and gastroenterological complications is reduced to 4-6%. At the same time, inhibition of “premature” decarboxylation by 5 times increases the intake of the dose of levodopa taken through the BBB into the brain. Therefore, when replacing “pure” levodopa with drugs with a DDC inhibitor, a 5 times lower dose of levodopa is prescribed (in terms of “pure” levodopa. For example, if the patient took 3 g per day“pure ”levodopa, the amount of levodopa per day in the composition of drugs with a peripheral DDC inhibitor should be 5 times less (3000 mg: 5 \u003d 600 mg) and will be approximately 2.5 tablets of nakoma or bluemet (625 mg of levodopa), or 6 capsules madopara-125, or 3 capsules of madopar-250 (600 mg of levodopa).
If levodopa drugs with an inhibitor are prescribed as initial therapy, then treatment begins with subthreshold doses (for example, 1/4 tablet of bluemet or nakoma 2 times a day) with a gradual increase in the dose within 3 - 5 weeks.
Since the peripheral DDC inhibitor does not pass through the BBB and does not affect the formation of dopamine, norepinephrine and adrenaline in the brain, the risk of neurological and psychiatric side symptoms remains the same as when taking "pure" levodopa. Therefore, the daily dose of a drug with a DDC inhibitor in most cases should not exceed 750 mg of levodopa.
The use of vitamin B6 in combination with "pure" levodopa is impractical, at the same time, in the treatment of levodopa preparations containing a DDC inhibitor, the appointment of vitamin B6 is possible.

Clinical pathomorphosis of parkinsonism in the long-term course of the disease and the treatment of DSS

With a rational selection of the optimal individual dose, the expressed pharmacotherapeutic effect of DSS without the appearance of adverse reactions usually persists for 4 to 7 years, after which, even with the usual optimal dose, various side reactions and changes in the typical clinical picture of parkinsonism (clinical pathomorphosis) are noted with the appearance of a number of phenomena.
Effect depletion phenomenon single dose due to the shortening of the duration of action of drugs. The effect of the drugs is significantly reduced and even disappears after short periods of time after taking levodopa (for example, after 2 to 3 hours), as a result of which the symptoms of the disease return. These changes in motor activity are usually clearly associated with the timing of medication and are defined as simple motor fluctuations. The “on-off” phenomenon is that the effect of the next single dose of levodopa after a certain time after taking the medication (30-60 minutes) occurs very quickly - within 5-15 minutes (“on”) lasts 1-1.5 hours and disappears just as quickly (“off”). When turned on quickly, the state can change from almost complete immobility to almost complete relaxedness. Large fluctuations in physical activity during the day do not necessarily occur suddenly and are not always clearly associated with medication. The effect of a single dose becomes insufficient, delayed in time, and sometimes the next dose may not give a therapeutic effect at all. Such unpredictable fluctuations in motor activity are called “complex motor fluctuations”.
The phenomenon of "freezing" is manifested by a state of sudden paroxysmal akinesia. Allocate akinesia of the beginning of movement (starting difficulties of movement), “akinesia of turning”, “akinesia of the threshold”. Akinesia is often accompanied by stomping or postural instability.

Pharmacological approaches to correction of manifestations of motor fluctuations

If the manifestations of clinical pathomorphosis occur at a certain time after taking DSS, then their reduction can be achieved by changing the frequency of administration, the value of any single dose in the morning, afternoon or evening. However, the possibilities of this approach are limited.
Pharmacological correction with the help of long-acting DSS, MAO type B inhibitors, and dopamine receptor agonists turned out to be more effective.

Long-acting DSS (DSSPD)

The technology of manufacturing DSSPD provides a gradual release, and, consequently, the absorption of levodopa and the DDC inhibitor from an ingested tablet (Sinemet CR, nakom R) or capsule (Madopar HBS; see Table 2) ... When these drugs are taken, a more stable level of drug concentration in the blood and a more uniform synthesis of dopamine from drugs in the brain can reduce the severity of simple and complex motor fluctuations, reduce the frequency and degree of drug dyskinesias that occur when taking non-prolonged DSS.
The bioavailability of Sinemet CR and Madopar HBS is less than the bioavailability of traditional drugs (Sinemet and Madopar). Therefore, in the case of replacing traditional DSS with drugs of prolonged action, the dose of levodopa to obtain the same antiparkinsonian effect can be increased by 20-30%. When taking DSSPD, the frequency of admission during the day can be reduced. If these drugs are used at the beginning of treatment of patients with parkinsonism (at the initial stage), a uniform pharmacotherapeutic effect can sometimes be obtained by taking the drugs 1 - 2 times a day.

MAO type B inhibitors

MAO type B inhibitors (Table 3) prevent the metabolic degradation of available dopamine, which is formed during endogenous synthesis from the drug levodopa. Thanks to this, a higher and more stable level of available dopamine is maintained, the manifestations of the phenomenon of dose depletion, on-off and other manifestations of motor fluctuations are smoothed out.
In most cases, to achieve this effect, which, however, is never significantly pronounced, it is enough to take selegiline 5 mg 2 - 3 times a day. Some authors consider the necessary dose of 40 mg / day.

COMT inhibitors

COMT, as a result of natural metabolism, converts L-DOPA to 3-0-methyldopa, and dopamine to 3-0-methyldopamine. These products are not involved in the function of dopamine neurons. COMT inhibitors interfere with the metabolism of dopamine and its precursor. An inhibitor of COMT that does not pass the BBB and therefore metabolizes levodopa in the “periphery” is entacapone, and an inhibitor that passes through the BBB, that is, acting both “on the periphery” and in the brain, is tolcapone (Table 3) .
Adding tolcapone to DSS increases and prolongs stable plasma levodopa levels by 65%. The addition of COMT inhibitors increases the pharmacotherapeutic efficacy and corrects motor fluctuations in 83% of cases more often than the addition of ADR (69% of cases).

Dopamine receptor agonists

Unlike all the drugs mentioned above, ADR (Table 4) are able to act directly on postsynaptic dopamine receptors “bypassing” the degenerated dopaminergic neuron.
The corrective effect of ADR on the manifestations of clinical pathomorphosis is based on a combination of a stimulating effect on postsynaptic receptors and a modulating effect on the function of a presynaptic dopaminergic neuron(fig. 2) .
Piribedil (agonist as D 1 and D 2 -receptors) was more effective than bromocriptine (agonist D 2 receptors) when administered as monotherapy and when added to DSS.

The use of drugs correcting clinical pathomorphosis as a means of initial therapy

In recent years, drugs correcting pathomorphosis have been proposed to be used for the initial therapy of parkinsonism. The tactics for selecting an individual optimal dose is the same as for other ATS. Experience shows that in terms of efficiency, only PRSPs can be compared with traditional LTAs. Selegiline and ADR have a much lower antiparkinsonian potential. One of the reasons for the use of MAO type B inhibitors as initial pharmacotherapy is the assumption that the degeneration of nigrostriatal neurons in parkinsonism is promoted by increased lipid peroxidation. In the multicenter study “Antioxidant therapy with deprenyl and tocopherol for parkinsonism” (DATATOR), which used selegiline (10 mg per day) and tocopherol (2000 IU per day), it was shown that the progression of parkinsonism was slowed down. However, the hypothesis about the effectiveness of antioxidants in the treatment of parkinsonism cannot be considered proven.

Neurosurgical treatment of parkinsonism

One of the methods of treating parkinsonism is neurosurgical operations: stereotaxic methods (destruction or stimulation of certain structures of the basal nuclei) and intracerebral transplantation of embryonic tissue and human mesencephalon into subcortical structures.
Indications for stereotaxic destructive operations (ventrolateral thalamotomy, pallidotomy, thalamo-subthalamotomy, etc.) are clinical forms of parkinsonism with a significant unilateral predominance of tremor and rigidity (hemiparkinsonism), which are not amenable to pharmacotherapy in the presence of side effects.
Stereotactic stimulation - chronic electrical stimulation of subcortical structures through implanted electrodes - is performed to inhibit tremor and rigidity. It can be combined with a ventrolateral thalamotomy.
Intracerebral transplantation of dopaminergic neurons in the mesencephalon of the human embryo remains to this day a clinical and experimental operation, the effectiveness of which continues to be studied.
The implanted embryonic neurons of the mesencephalon either produce dopamine themselves or increase the synthesis of the neurotransmitter from levodopa taken by the patient. Intracerebral transplantation does not lead to the complete disappearance of the symptoms of the disease, but significantly improves the prospects for subsequent pharmacotherapy: in patients, the duration of action of a single dose of DSS increases, the severity of drug dyskinesias decreases, in some cases it is possible to reduce the daily dose of PPS.

Literature:

1. Hoehn M, Jahr MD. Parkinsonism: onset, progression and mortality. Neurology 1967; 17 (5): 427-42.
2. Koller WC. Classification of Parkinsonism. Handbook of Parkinsons disease (Ed. By W.C. Koller). Marsel Dekker. New York-Basel 1987; 99-126.
3. Marsden CD, Parkes JD, Quinn N. Fluctuation of disability in Parkinsons disease; clinical aspects. Movement disorders (Ed. C. D. Marsden, S. Fahn). London, Butterwoth 1982; 96-119.
4. Mouradian MM. Control-release oral levodopa therapy for Parkinson`s disease. Parkinsons disease review 1991; 1-7.
5. Obeso JA, Granadas F, Vaamonde J, et al. Motor complications associated with chronic levodopa therapy in Parkinsons disease. Neurology 1989; 39 (11; Suppl. 2): 11-8.
6. Olanow CW. Protective therapy for Parkinson`s disease. The scientific basis for the treatment of Parkinson's disease (Ed. By C.W. Olanow and A.N. Lieberman). The Parthenon Publishing Group 1992; 225-56.

Parkinson's disease or tremor palsy is a chronic progressive disease of the central nervous system, which is characterized by damage to the neurons of the substantia nigra of the brain. Parkinsonism is a syndrome, a set of neurological signs that occur in Parkinson's disease (80%) and in other diseases of the nervous system (20%). This fact must be taken into account, since the effectiveness of treatment depends on the correct diagnosis. Indeed, in addition to this ailment, there are a number of diseases that have similar symptoms:

• secondary parkinsonism after trauma and infectious diseases
• Alzheimer's (about signs)
• diffuse Lewy body disease
• gellervoarden-Spatz disease
• wilson-Konovalov disease
• normotensive hydrocephalus
• essential tremor
• progressive supranuclear palsy
• corticobasal degeneration

Therefore, high-quality differential diagnostics in this case is extremely important.

Diagnostic and Confirmation Methods

When is it necessary to suspect the development of Parkinson's disease and what manifestations should alert you? An urgent need to consult a neurologist if the following symptoms appear:

• increased muscle tone (rigidity)
• slowness of voluntary movements (hypokinesia)
• resting tremor - tremors that occur in the limbs and head and decrease as you perform activities
• instability when changing body position or walking (postural instability), which is not associated with disorders of the vestibular apparatus

At this stage, there are no specific laboratory tests that could reliably confirm the presence of Parkinson's disease. When performing magnetic resonance imaging and computed tomography brain changes in the substantia nigra are also not found.

In this case, the positron emission tomography and gamma tomography. The doctor can make a diagnosis based on these studies, complaints of the patient and his loved ones.

The situation is complicated by the fact that most often the onset of the disease is latent and the symptoms are weak, but the presence of at least one of them should be a reason for visiting a doctor. Learn more about symptoms.

At the reception, the specialist will prescribe the necessary examinations, diagnose and determine the form and stage of the disease.

Parkinson's disease forms are identified by the prevalence of symptoms:

1. Mixed form (increased tone, trembling limbs, slowness of voluntary movements)
2. Trembling form (tremor of the limbs and lower jaw)
3. Akinetic-rigid form (slowness of action and increased muscle tone)

Stages of the disease (according to Hoehn and Yarh)

1. Unilateral symptoms - tremor and muscle tone are expressed on one side
2. Bilateral symptoms - changes have spread to both arms or legs
3. Bilateral symptoms with mild unsteadiness when walking
4. Significant impairment of motor activity while maintaining the possibility of independent movement
5. The patient cannot move independently and is confined to a wheelchair

There are a number of signs that confirm that the patient does have this problem, and not one of the similar neurological conditions.

• The asymmetric onset of symptoms is unilateral tremor.
• Relatively slow development of the disease - about 5 years.
• Characteristic resting tremor - finger movements resemble coin counting
• Smell disorder
• Movement disorders
• Long lasting effect of levodopa - symptoms are reduced by 70-100%
• Duration of the disease 10 years or more
• Absent neurological disorders characteristic of other diseases (acute onset, impaired thinking, visual hallucinations, prolonged absence of symptoms)

Parkinson's disease treatments

There are several groups of drugs and medicines that are used to alleviate the condition of patients. They relieve the manifestations of the disease and prolong the active life of patients. But today it is not possible to stop the loss of dopaminergic cells and the disease remains incurable.

There are two main areas of treatment:

1. A therapy aimed at slowing the death of dopaminergic neurons and halting the development of the disease (Yumeks, Mirapex, Midantan, PK-Merz). Development in this area is ongoing, but 100% effectiveness of these drugs has not yet been proven.
2. Symptomatic therapy. It is designed to improve the quality of life of patients and eliminate symptoms.

The most common and widely used drug of the second group is levodopa... It helps to get rid of various movement disorders. The effectiveness of this drug reaches in some cases 100%, addiction to it does not occur within 4-6 years.

However, levodopa has many side effects (fluctuations in motor activity, involuntary movements). To minimize them, patients have to take special medications. Based on this, most doctors try to prescribe levodopa at a later stage in the development of the disease. On this basis, there is a debate between supporters and opponents of levodopa how to treat Parkinson's disease.

In the initial stages, patients under 50 years of age are advised to take dopamine antagonists (pramipexole, ropinirole). MAO-B inhibitors (selegiline, rasagiline) or amantadines (midantan) are often used.

Elderly patients are prescribed levodopa preparations regardless of the stage of the disease. Poorly amenable to drug treatment, posture instability. Tremor and increased muscle tone can be removed with a properly selected dose of the drug.

Patients with the third stage are combined levodopa and a dopamine antagonist.

If the patient's limb tremor prevails, then anticholinergic drugs (cyclodol, akineton) are prescribed, and for patients over 60 years old - obzidan.

Patients with parkinsonism also need to take tricyclic antidepressants.

About diet, special diet and physical activity.

Surgical treatments

In the case when drug therapy is not effective, deep stimulation of the brain (subthalamus) with weak electric currents or stereotaxic surgery is prescribed. As a result, it is possible to achieve the restoration of lost functions with the help of electrical stimulation of certain parts of the brain (intracerebral structures).

Another direction was the implantation of healthy cells that are designed to produce dopamine. It is the lack of this substance that causes the manifestations of parkinsonism.

Disease prognosis

Over time, despite treatment, symptoms increase. During the first 5 years of illness, 25% of patients receive disability in Parkinson's. Among patients who have been suffering from parkinsonism for 10 years, the disability reaches 65%. Among those who have been ill for 15 years, this number is already 90%.

With the use of levodopa, the mortality rate decreased and life expectancy increased. Continuous research in this area gives hope that soon it will be possible to completely cure the disease.

To summarize, correct diagnosis is very important, as many neurological diseases have similar symptoms. And treatment in each case must be prescribed individually. Many groups of drugs are used in Parkinson's disease. In each case, based on the results of the examination, its own scheme and dosage are prescribed. Therefore, it is unacceptable to take medications without consulting a doctor. It is extremely important to consult an experienced neurologist on time, who will prescribe effective treatment and will return the person to an active life.

- a disease with progressive death of brain cells that produce the active substance - dopamine.

Drug therapy for parkinsonism is aimed primarily at restoring the level of dopamine in the patient, increasing its amount.

Indeed, it is with the lack of dopamine that the emerging negative symptoms are associated - muscle stiffness, trembling of the limbs, dysfunction of the patient's locomotor system.

Secondary, but not unimportant, the task of drugs for becomes to increase the resistance of patients to pathology, eliminate sleep disorders, vitamin deficiency, pain inherent in Parkinson's pathology.

Dopamine control in patients with parkinsonism is carried out with the help of drugs based on levodopa, a substance that is synthesized into dopamine by the human body.

In the full course of therapy, doctors also include antioxidants, vitamin complexes, sleeping pills and pain relievers.

When describing the conditions for taking the drug, daily norms are indicated.

Antioxidants

The importance of antioxidants in the complex of treatment is due to the fact that they neutralize free radicals, molecules that are dangerous for the body and contribute to the death of nerve cells.

With parkinsonism, it is often prescribed:

1. Mexidol... In combination with antiparkinsonian drugs Mexidol for Parkinson's disease enhances their effect. Available in tablets. It is taken in a course of at least 2-6 weeks, starting from 125-250 mg (1-2 tablets) 1-2 times. The frequency of reception increases with time up to 3 times.
2. Glutathione(L-Glutathione). Glutathione in the treatment of Parkinson's disease restores drug-damaged liver cells. Available in solution and capsules. 1-2 capsules are taken orally on an empty stomach. The solution is injected with 0.9% sodium chloride at 0.6-2.4 g intramuscularly and intravenously.
3. Superoxide dismutase(SOD). Provides protection of the body from the generated free radicals. Available in capsules. Reception conditions: 1-2 capsules.

Mexidol is a prescription drug, Glutathione and Superoxide dismutase (SOD) can be bought without a prescription.

Hypnotics

Means that help improve sleep are necessary for patients with parkinsonism, as they are prone to problems with falling asleep, proper rest.

The doctor will first of all try to avoid unnecessary drug burden on the patient.

For those suffering from Parkinson's disease, herbal teas, sedatives and amino acids that restore the functioning of the nervous system are especially recommended for regulating sleep:

1. Phytosed... Available in tincture, capsule form. Composition - fruits, herbs and fruit, which have a hypnotic, sedative effect. Capsules take 1-2 pcs., And tincture - 5 ml 3-4 times.
2. Melatonin... This substance is called "sleep hormone". It evens out the daily biorhythms: during the day a person does not suffer from sleepiness, and at night he sleeps soundly and calmly. This is especially important for people with Parkinson's disease. They tend to have nightmares, leading to anxiety during the day and a reluctance to go to bed. The drug is taken 1-2 tablets before bedtime.

These drugs are sold by pharmacies without a prescription.

Also, in order to improve falling asleep, normalize sleep for those suffering from Parkinson's pathology, in the evening, warming procedures and relaxing massages are shown.

Levodopa

Levodopa is a substance that is converted into dopamine by the human body. Medicines based on levodopa are central to the management of painful symptoms in Parkinson's disease:

1. On whom... Sold in tablets. The dose of admission varies depending on the condition of the person, usually therapy is started with ½ tablet 1-2 times, increasing the amount until a positive shift in treatment.
2. Stalevo... Produced in tablets. It is taken in a dose of 50-200 mg, the total amount is determined by the attending physician.
3. Madopar... Available in 125 mg capsules and tablets and 250 mg tablets. Doses of admission vary: from 62.5 mg at the initial stage of therapy to 375 - 1000 mg in 3 or more doses.

These medicines are dispensed by pharmacies only with a doctor's prescription.

About the substance Levodopa in this video:

Vitamins

Taking vitamin complexes is necessary for people suffering from parkinsonism. They help restore the body's defenses and healthy organs to fight disease.

Available in pharmacies without a doctor's prescription.

When taking vitamin and mineral substances, it is necessary to take into account the peculiarities of their assimilation by the body. For convenience, you can take the combined vitamin complexes recommended by your doctor.

It is noted that those suffering from Parkinson's disease are prone to thinning and fragility of bones, problems with the gastrointestinal tract.

They often suffer from dehydration, sudden weight loss, and the side effects of numerous medications. Vitamin therapy and a balanced diet can help alleviate many of these problems.

Pain relievers

Parkinson's patients often complain of pain.

According to their descriptions, it is burning, pulling, tingling pain in the shoulder joints, lower back, neck, back, legs.

Often it is impossible to do without painkillers, at least somehow alleviating the condition of patients.

1. Ibufen... Ibufen in Parkinson's disease has anti-inflammatory, antipyretic, analgesic effects. Available in the form of tablets, capsules. Reception is calculated according to the formula: 5-10 mg per 1 kg of body weight 3-4 times (not exceeding a daily dose of 30 mg per 1 kg of body weight).
2. Ibufen's analogs- Ibuprofen, Nurofen. Available in tablets. Both drugs are taken 1 tablet 3-4 times, depending on the patient's condition.

These funds are dispensed by pharmacies without a doctor's prescription.

There is medical research that ibuprofen can prevent Parkinson's disease by reducing inflammation in the brain tissue.

List of new generation products and solutions for droppers

Among the drugs for Parkinson's disease last generation allocate Madopar GSS and Madopar fast-acting tablets (dispersible).

In comparison with the drug of the previous generation, they allow solving some of the problems arising in the treatment of patients with Parkinson's.

For example, many people with Parkinson's pathology suffer from bladder dysfunction, which leads to frequent trips to the toilet at night.

Madopar GSS significantly alleviates this symptom.

Fast-acting dispersible Madopar is absorbed 2 times faster, which facilitates the morning state of patients with parkinsonism.

The drugs are available in tablets and capsules. Admission rules:

• Madopar GSS is taken in the same way as regular Madopar, but the total daily dosage can be increased by 30-50%;
• fast-acting Madopar is dissolved with a small amount of water and the resulting suspension is taken orally.

Medicines are available with a prescription.

Amantadine is often prescribed to stimulate the release of dopamine.... It is effective in the early stages of the disease and allows you to delay the appointment of levodopa. It is also used when it is necessary to stop taking levodopa.

A popular amantadine-based drug is PC Merz for injection. It is prescribed by intravenous drip of 500 ml of solution 1-3 times.

About the creation of a new drug for the treatment of Parkinson's disease in this video:

How to get free pills

Beneficial categories of citizens of the Russian Federation can receive free medicines for treatment. The category of beneficiaries includes people with disabilities, participants in the Great Patriotic War who suffered during the disaster at the Chernobyl nuclear power plant.

They can get antiparkinsonian drugs free of charge in accordance with federal benefit laws.

Free medicines are dispensed according to a valid prescription from the attending physician. Dispensing is carried out only by pharmacies that have entered into an agreement for compensation of costs with a pension fund.

Drugs in the treatment of Parkinson's disease should first of all replenish the lack of dopamine in the patient's body.

But the severity of the disease requires prescription and auxiliary drugs - hypnotics to normalize sleep, pain relievers to alleviate severe conditions of patients.

The maximum effect of the treatment is achieved with the intake of vitamins and antioxidants.

Also, neurosurgical, physiotherapy exercises, the help of a psychologist, exposure to medical devices are used to treat the disease.

One of the most common organic diseases of the central nervous system, which occurs most often in people of older age groups. According to statistics, parkinsonism is observed in 1% of the population, and in age groups over 60 years of age, the incidence increases to 5%.

The disease is named after the English physician James Parkinson, who in 1817 described in detail its clinical manifestations. The disease is polyetiological. The etiological factors of parkinsonism are usually divided into 2 groups: Parkinson's disease (or primary idiopathic parkinsonism), which is a slowly progressive systemic degeneration of the extrapyramidal parts of the nervous system, and symptomatic (secondary) parkinsonism, including vascular (including atherosclerotic), post-encephallergic, toxic and other forms.

With parkinsonism, there is a lesion of the substantia nigra (degeneration of neurons, the disappearance of melanin pigment) and subcortical nodes (globus pallidus and, to a lesser extent, striatum).

The pathogenetic basis of parkinsonism is a violation of catecholamine metabolism in the brain - in patients, the level of dopamine in the subcortical nodes decreases sharply, the synthesis of melanin in the substantia nigra decreases, the complex balance of cholinergic, dopaminergic, serotonin- and histaminergic mediator systems is disturbed.

Of different types secondary parkinsonism most often occurs the so-called vascular parkinsonism, which can be caused by atherosclerosis of the cerebral vessels, hypertension and age-related changes in the vessels. These reasons are usually closely intertwined. It is often difficult to single out the leading role of one of them; therefore, it is more correct to talk about vascular parkinsonism in the collective sense of this term.

In recent years, the proportion of vascular parkinsonism (including atherosclerotic) has increased and, according to our data, is 40% among other major etiological forms of the disease. This is due to the “aging” of the population in different countries as a result of an increase in life expectancy and the proportion of cerebrovascular pathology in general. Vascular parkinsonism is more common among men (69.3%). The onset of the disease refers to old age (60-74 years), in contrast to idiopathic and postencephalitic parkinsonism, when the disease begins, as a rule, earlier (45-59 years for idiopathic, up to 45 years for postencephalitic parkinsonism). In families of patients with vascular parkinsonism, there is a clear predisposition to cardiovascular diseases and very rarely (in contrast to Parkinson's disease) such cases of the disease occur.

The disease begins most often gradually, without an apparent external cause, sometimes (34.72%) immediately after mental trauma. Even Charcot spoke out in favor of the etiological significance of "moral shock" in tremors. It is now known that a severe affective reaction is accompanied by vascular and humoral changes. In 20% of the cases of vascular parkinsonism observed by us, its direct cause was acute cerebral circulation disorders, more often in the basin of the middle cerebral artery, proceeding according to the ischemic type.

The main clinical manifestations of vascular parkinsonism include stiffness and trembling. Stiffness includes plastic muscle rigidity (increased muscle tone) and bradykinesia or akinesia (slower pace of movement), the most severe symptom of vascular parkinsonism. When the patient is lying down, muscle stiffness decreases. Vascular parkinsonism is characterized by the greatest increase in muscle tone in the legs, and this symptom is often the first manifestation of the disease, and stiffness occurs in both legs at once.

Bradykinesia is manifested by a sharp slowdown, depletion of active movements. The patient develops hypomimia; characteristic "mask-like, icy" facial expression that does not change in connection with the experienced emotions. Mimic emotional reactions are prone to "tonic fixation", and the patient, for example, continues to smile, although the reason for joy has long passed. Patients lose their individual characteristics of gait gestures, they become like a "wooden doll". Sometimes, under the influence of superstrong emotions, “paradoxical kinesia” appears; the ability to perform "motor feats", to talk animatedly, to run.

The slowness of movements is not accompanied by a noticeable violation of muscle strength; its peculiar dissociation is revealed: the force is great when the patient is asked to hold the limb in a given position, and is insignificant when the resistance is actively overcome. One of the earliest symptoms of bradykinesia is a peculiar change in handwriting in the form of micrography. Posture, posture and gait are also impaired. A patient with parkinsonism often stands, hunched over, bent forward, with lowered shoulders, bent at the elbows and arms pressed to the torso, slightly bent knees and head lowered to the chest. It is difficult for the patient to start moving. He treads in place before taking a step forward, walks slowly, in small steps, shuffling his feet. In vascular parkinsonism, extrapyramidal gait disturbances are often combined with cerebellar ataxia and spastic disorders associated with associated spinal circulatory failure (vascular myelopathy).

Tremors (tremors) are not a necessary symptom of vascular parkinsonism. The most common tremor is "rest" (static tremor). Trembling is most often localized in the distal extremities, mainly in the arms. The jitter amplitude is unstable; in vascular parkinsonism, the "pill rolling symptom" or "coin counting" characteristic of Parkinson's disease is rare. Head trembling can occur in the horizontal plane ("no-no"), less often in the vertical ("yes-yes").

Vegetative disorders (increased salivation, hyperhidrosis, greasiness of the skin of the face and scalp) with vascular parkinsonism are unsharp and more characteristic of postencephalitic parkinsonism.

In 44.19% of cases, vascular parkinsonism is combined with arterial hypertension. Essential hypertension can be the leading cause of vascular parkinsonism, regardless of whether it occurs with atherosclerosis or not. More often it is diagnosed long before the onset of parkinsonism, and the latter develops in these cases as a result of chronic hypertensive encephalopathy.

Rehabilitation measures for vascular parkinsonism should include a rational regimen, dietary nutrition (as in any vascular pathology), physical therapies, rational psychotherapy and autogenous training aimed at reducing tremors, muscle rigidity and bradykinesia, reducing cerebral and neurotic disorders, improving cerebral circulation and cardiac activity.

The patient should strive to maintain the habitual life stereotype as long as possible (stay in a work collective, continuation of professional activity). If this is not possible, feasible physical labor, sufficient physical activity are recommended. Patient self-care should be encouraged. Excessive help is harmful and contributes to faster disability. Thus, activity slows down, and inactivity accelerates the development of the disease.

In the complex of therapeutic measures for parkinsonism, drug treatment remains the main one. Given the complex pathophysiological mechanisms of the main symptoms of parkinsonism, the occurrence of which depends on damage to various levels of the nervous system: (cortex, subcortex, reticular formation of the brainstem, spinal cord and, possibly, peripheral parts of the nervous system), it is natural to conclude that any one pharmacological drug does not have a multifaceted corrective influence. Only the use of a complex of drugs that affect various links of the pathological process can be most effective.

To influence the main symptoms of parkinsonism (tremor, stiffness, bradykinesia), 3 main groups of drugs are currently used:

1. central anticholinergics, i.e. drugs that have the ability to reduce the sensitivity of organs and tissues to acetylcholine. These include tropacin, cyclodol (synonyms: artan, parkinzan, parkopan, romparkin), ridinol, norakin, bellazon, amedin, etc.
2. adamantans - midantan, viregit, symmetrel;
3. drugs from the L-DOPA group, compensating for the lack of dopamine in the subcortical nuclei: levopa, levodopa, dopaflex, dopar, as well as drugs synthesized on the basis of L-DOPA: madopar, nakom, cinemet.

Anticholinergic agents of central action in elderly and old people are usually effective in doses 2-3 times less than in young or middle-aged patients with parkinsonism. Treatment should be started with minimal doses (1 mg per dose, 1-2 times a day). Gradually, the dose is increased until a satisfactory therapeutic effect appears, continuing the treatment with the lowest effective doses for many months. The maximum daily dose of anticholinergics (otherwise, anticholinergic drugs) in the elderly, and therefore in patients with vascular parkinsonism, should not exceed 7.5 mg (2.5 mg 3 times a day). Large doses of anticholinergics are not only ineffective, but are also directly contraindicated due to pronounced side effects (dizziness, accommodation disturbances, intestinal paresis, etc.). Atropine-like drugs (anticholinergics) should be taken after meals. Of central anticholinergics, it gives fewer side effects and is better tolerated by patients with vascular parkinsonism Ridinol. In terms of chemical structure, it is close to cyclodol. Available in tablets of 1, 2 and 5 mg. The use of ridinol significantly reduces muscle tone, increases range of motion, reduces hypersalivation, improves sleep and pelvic organ function. Ridinol has a weaker effect on hyperkinesis.

Central anticholinergics are undesirable in glaucoma. In these cases, they are replaced with drugs of the phenothiazine series - dinesin (latibon, deparkin), parsidol (diparkol, antiparkin). These drugs, in contrast to atropine-like drugs, do not cause accommodation disturbances and are acceptable in patients with glaucoma.

In vascular parkinsonism caused by widespread atherosclerosis with atherosclerotic endarteritis of the extremities, mydocalm is useful. Its properties are close to the central muscle relaxants. There is evidence of the n-anticholinergic action of the drug. In addition, mydocalm has a beneficial effect on venous and arterial circulation in the extremities, has an antispasmodic effect. It is indicated in patients of any age. With parkinsonism, treatment should be started with a daily dose of 0.15 grams (0.05 grams 3 times a day), increasing it by 0.05 grams every 3 days. The maximum daily dose is 0.45 grams (0.15 grams every 8 hours). The maintenance dose usually does not exceed 0.05 grams 3 times a day. The course of treatment is 5-6 weeks. In especially severe cases in a hospital, intramuscular injections are advisable: 1 ml of 10% solution 1-2 times a day.

Midantan (amantadine hydrochloride) is one of the new, most effective antiparkinsonian drugs. It was proposed in the USA (Symmetrel) for the treatment of Asian influenza (A-2 virus). Its positive effect on parkinsonism was discovered by chance: several patients with parkinsonism got the flu and took amantadine-HCl, and there was a significant reduction in akinesia, stiffness and tremors. The domestic drug midantan has a positive effect on all the main symptoms of the disease: to a greater extent on rigidity and bradykinesia, to a lesser extent - on tremors. The drug is prescribed, as a rule, in a dose of 100 mg (0.1 gram) 2 times a day. The treatment takes several months. The best effect is provided by complex therapy with midantan in combination with central anticholinergics. Mindantan and other drugs from the adamantane group do not have a pronounced side effect, however, with prolonged use, increased irritability, insomnia are possible, therefore, it is undesirable to prescribe them at night. When side effects appear, it is possible to recommend combined treatment with minor tranquilizers (tazepam, nozepam, relanium, trioxazine, etc.).

The study of dopamine imbalance in parkinsonism led to the discovery of a fundamentally new effective treatment - L-DOPA. It should be remembered that the results of treatment with drugs from the L-DOPA group (L-DOPA, levopa, levodopa, dopaflex, dopar) become noticeable most often 2 months after the start of treatment. Most of all, the technique of careful slow increase of doses in accordance with the individual characteristics of the patient has justified itself. It is the only one possible with vascular parkinsonism. Drug treatmentL-DOPA, prescribing and changing dosages are carried out only under the supervision of a neuropathologist.In case of overdose and individual intolerance, there are pronounced side effects in the form of gastrointestinal disorders, cardiovascular disorders, and with prolonged use (as a rule, 2 years after the start of treatment) hyperkinesis of the extremities and oral muscles, resembling choreiform, as well as psychotic disturbances in the form of hypnagogic hallucinations, delusional statements.

New possibilities for the treatment of parkinsonism have opened up after the appearance of drugs that are a combination of L-DOPA and DOPA-decarboxylase inhibitors, which promote the rapid penetration of L-DOPA through the blood-brain barrier (nakom, madopar, bluemet). These drugs made it possible to reduce the daily dose of L-DOPA by 75-80%, significantly reduce the frequency and severity of its side effects. The effect when using nakoma and madopar occurs in most cases on the 7-15th day with a daily dose of 2-2.5 tablets. It is expressed in a significant decrease in muscle rigidity, a decrease in bradykinesia; the circle of self-care of patients expands, they begin to carry out subtle movements of the fingers. The best effect in vascular parkinsonism is provided by complex drug therapy, which includes, along with antiparkinsonian drugs, agents that directly affect the atherosclerotic process (diosponin, cetamifen, parmidin, miscleron, vitamin complexes, stugeron, cavinton), as well as drugs that improve cerebral circulation, reducing blood pressure with arterial hypertension.

A caring attitude, sensitivity to old, sick people, understanding their interests create a positive emotional background for them, contribute to the desire to remain useful to the family and society, and favor the best effect of drugs.