Madopar GSS 125, 100 mg+25 mg, modified release capsules, 100 pcs.

Composition and release form

Madopar® fast-acting tablets (dispersible) “125”

in dark glass bottles 30 or 100 pcs.; 1 bottle in a cardboard pack.

Madopar® "125"

in dark glass bottles 30 or 100 pcs.; 1 bottle in a cardboard pack.

Madopar® “250”

in dark glass bottles 30 or 100 pcs.; 1 bottle in a cardboard pack.

Madopar® GSS "125"

in dark glass bottles 30 or 100 pcs.; 1 bottle in a cardboard pack.

Description of the dosage form

Dispersible tablets: cylindrical, flat on both sides with a beveled edge, white or almost white, odorless or slightly odorless, slightly marbled, engraved “ROCHE 125” on one side of the tablet and a break line on the other side. Tablet diameter is about 11 mm; thickness - about 4.2 mm.

Capsules: hard gelatin; body - pinkish-flesh color, opaque; the lid is light blue, opaque; The capsule is marked “ROCHE” in black. The contents of the capsules are a fine granular powder, sometimes clumped, light beige in color, with a subtle odor.

Tablets: cylindrical, flat with a beveled edge, pale red in color with small inclusions, with a subtle odor; on one side of the tablet there is a cross-shaped line, engraving “ROCHE” and a hexagon; on the other there is a cross-shaped risk. Tablet diameter - 12.6–13.4 mm; thickness - 3–4 mm.

Modified release capsules: hard gelatin; body - light blue, opaque; the lid is dark green, opaque; The capsule is marked “ROCHE” in rusty red ink. The contents of the capsules are a fine granular powder, sometimes clumped, white or slightly yellowish in color, with a subtle odor.

Pharmacodynamics

Combined drug for the treatment of Parkinson's disease and restless legs syndrome.

Parkinson's disease. Dopamine, a neurotransmitter in the brain, is produced in insufficient quantities in the basal ganglia of patients with parkinsonism. Levodopa or L-DOPA (3,4-dihydrophenylalanine) is a metabolic precursor to dopamine. Unlike dopamine, levodopa penetrates well through the BBB. After levodopa enters the central nervous system, it is converted to dopamine by aromatic amino acid decarboxylase.

Replacement therapy is carried out by prescribing levodopa, the immediate metabolic precursor of dopamine, since the latter does not penetrate the BBB well.

Following oral administration, levodopa is rapidly decarboxylated to dopamine in both cerebral and extracerebral tissues. As a result, most of the administered levodopa does not reach the basal ganglia, and peripheral dopamine often causes side effects. Therefore, blocking extracerebral decarboxylation of levodopa is necessary. This is achieved by the simultaneous administration of levodopa and benserazide, a peripheral decarboxylase inhibitor.

Madopar® is a combination of these substances in an optimal ratio of 4:1 and is as effective as large doses of levodopa.

Restless legs syndrome. The exact mechanism of action is unknown, but the dopaminergic system plays an important role in the pathogenesis of this syndrome.

Pharmacokinetics

Suction

Madopar® “125” capsules and Madopar® “250” tablets

Levodopa is primarily absorbed in the upper small intestine. The time to reach Cmax of levodopa is 1 hour after taking capsules or tablets.

Capsules and tablets are bioequivalent.

Cmax of levodopa in plasma and the extent of levodopa absorption (AUC) increase proportionally to the dose (in the levodopa dose range from 50 to 200 mg).

Eating reduces the rate and extent of absorption of levodopa. When capsules or tablets are administered after meals, the Cmax of levodopa in plasma is reduced by 30% and is achieved later. The degree of absorption of levodopa is reduced by 15%. The absolute bioavailability of levodopa in Madopar® “125” capsules and Madopar® “250” tablets is 98% (from 74 to 112%).

Madopar® fast-acting tablets (dispersible) “125”

The pharmacokinetic profiles of levodopa after administration of dispersible tablets are similar to those after administration of Madopar® "125" capsules or Madopar® "250" tablets, but the time to reach Cmax tends to decrease. Patient absorption of dispersible tablets is less variable.

Madopar® GSS "125", capsules with modified release of the active substance

Madopar® GSS “125” has different pharmacokinetic properties than the above release forms. The active substances are released slowly in the stomach. Cmax in plasma is 20–30% less than that of conventional dosage forms and is achieved 3 hours after administration. The dynamics of plasma concentration is characterized by a longer half-life (the period of time during which the plasma concentration is greater than or equal to half the maximum) than that of Madopar® 125 capsules and Madopar® 250 tablets, which indicates a continuous modifiable release . The bioavailability of Madopar® GSS “125” is 50–70% of the bioavailability of Madopar® “125” capsules and Madopar® “250” tablets and does not depend on food intake. Food intake does not affect the Cmax of levodopa, which is achieved later, 5 hours after taking Madopar® GSS “125”.

Distribution

Levodopa crosses the BBB via a saturable transport system. It does not bind to plasma proteins. Distribution volume - 57 l. The AUC for levodopa in cerebrospinal fluid is 12% of that in plasma.

Benserazide in therapeutic doses does not penetrate the BBB. It accumulates mainly in the kidneys, lungs, small intestine and liver.

Metabolism

Levodopa is metabolized by two main pathways (decarboxylation and o-methylation) and two additional pathways (transamination and oxidation).

Aromatic amino acid decarboxylase converts levodopa to dopamine. The main end products of this metabolic pathway are homovanillic and dihydroxyphenylacetic acids.

Catechol-o-methyl-transferase methylates levodopa to form 3-o-methyldopa. The half-life of this main metabolite from plasma is 15–17 hours, and its accumulation occurs in patients taking therapeutic doses of Madopar®.

Reduced peripheral decarboxylation of levodopa when coadministered with benserazide leads to higher plasma concentrations of levodopa and 3-o-methyldopa and lower plasma concentrations of catecholamines (dopamine, norepinephrine) and phenolcarboxylic acids (homovanillic acid, dihydrophenylacetic acid).

In the intestinal mucosa and liver, benserazide is hydroxylated to form trihydroxybenzylhydrazine. This metabolite is a potent inhibitor of aromatic amino acid decarboxylase.

Removal

With peripheral inhibition of T1/2 decarboxylase, levodopa - 1.5 hours. Plasma clearance of levodopa is approximately 430 ml/min.

Benserazide is almost completely eliminated by metabolism. Metabolites are excreted mainly in urine (64%) and to a lesser extent in feces (24%).

Pharmacokinetics in special groups of patients

Patients with renal and liver failure. There are no data on the pharmacokinetics of levodopa in patients with renal and hepatic impairment.

Elderly patients (65–78 years). In elderly patients (65–78 years) with Parkinson's disease, T1/2 and AUC of levodopa increase by 25%, which is not a clinically significant change and does not in any way affect the dosage regimen.

Madopar “125” dispersible tablets 100 mg+25 mg 100 pcs.

Capsules (Madopar “125” or Madopar GSS “125”) should be swallowed whole without chewing. Madopar GSS “125” capsules cannot be opened before use, otherwise the effect of the modified release of the active substance is lost. Parkinson's disease. Orally, at least 30 minutes before or 1 hour after meals. Standard dosage regimen. Treatment should be started gradually, with individual doses adjusted until the optimal effect is achieved. Initial therapy At the early stage of Parkinson's disease, it is recommended to begin treatment with Madopar by taking 62.5 mg (50 mg levodopa + 12.5 mg benserazide) 3-4 times a day. If the initial dosing schedule is tolerated, the dose should be increased slowly based on patient response. The optimal effect is usually achieved with a daily dose of 300-800 mg levodopa + 75-200 mg benserazide, taken in three or more divided doses. It may take 4 to 6 weeks to achieve optimal results. If it is necessary to further increase the daily dose, this should be done at intervals of 1 month. Maintenance therapy. The average maintenance dose is 125 mg (100 mg levodopa + 25 mg benserazide) 3-6 times a day. The number of doses (at least three) and their distribution throughout the day should ensure optimal effect. To optimize the effect, you can replace Madopar “125” capsules and Madopar “250” tablets with Madopar fast-acting tablets /dispersible/ “125” or Madopar GSS “125” capsules. Restless legs syndrome. The maximum permissible dose per day is 500 mg of Madopar (400 mg of levodopa + 100 mg of benserazide). 1 hour before bedtime with a small amount of food. Before using Madopar, you should refrain from eating foods rich in protein. Idiopathic restless legs syndrome with sleep disturbances It is recommended to prescribe Madopar “125” capsules or Madopar “250” tablets. Initial dose: 62.5 mg (50 mg levodopa + 12.5 mg benserazide) - 125 mg (100 mg levodopa + 25 mg benserazide) Madopara. If the effect is insufficient, the dose should be increased to 250 mg (200 mg levodopa + 50 mg benserazide) of Madopar. Idiopathic restless legs syndrome with sleep and sleep disorders Initial dose: 1 capsule of Madopar GSS “125” and 1 capsule of Madopar “125” 1 hour before bedtime. If the effect is insufficient, it is recommended to increase the dose of Madopar GSS “125” to 250 mg (2 capsules). Idiopathic restless legs syndrome with problems falling asleep and sleeping, as well as disturbances during the day. Additionally: 1 dispersible tablet or 1 capsule Madopar “125”, the maximum permissible daily dose is 500 mg (400 mg levodopa + 100 mg benserazide) Madopar. “Restless legs” syndrome in patients with chronic renal failure receiving dialysis 125 mg Madopar (1 dispersible tablet or 1 capsule Madopar “125”) 30 minutes before the start of dialysis. Dosing in special cases. Parkinson's disease. Madopar can be combined with other antiparkinsonian drugs; as treatment continues, it may be necessary to reduce the dose of other drugs or gradually discontinue them. Madopar fast-acting tablets /dispersible/ “125” is a special dosage form for patients with dysphagia or akinesia in the early morning hours and in the afternoon or with the phenomena of “depletion of the effect of a single dose” or “increase in the latent period before the onset of the clinical effect of the drug.” If during the day the patient experiences pronounced motor fluctuations (the phenomenon of “exhaustion of the effect of a single dose”, the phenomenon of “on-off”), it is recommended either more frequent administration of correspondingly smaller single doses, or, which is preferable, the use of Madopar GSS “125”. It is better to start the transition to Madopar GSS “125” with the morning dose, maintaining the daily dose and dosage regimen of Madopar “125” or Madopar “250”. After 2-3 days, the dose is gradually increased by approximately 50%. The patient should be warned that his condition may temporarily worsen. Due to its pharmacokinetic properties, Madopar GSS “125” begins to act somewhat later. The clinical effect can be achieved faster by prescribing Madopar GSS “125” together with Madopar “125” capsules or dispersible tablets. This may be especially useful in the case of the first morning dose, which should be slightly higher than subsequent doses. The individual dose of Madopar GSS “125” must be selected slowly and carefully, the interval between dose changes should be at least 2-3 days. In patients with nocturnal symptoms, a positive effect was achieved by gradually increasing the evening dose of Madopar GSS “125” to 250 mg (2 capsules) before going to bed. To eliminate the pronounced effect of Madopar GSS “125” (dyskinesia), increasing the intervals between doses is more effective than reducing the single dose. If Madopar GSS “125” is not effective enough, it is recommended to return to the previous treatment with Madopar “125”, Madopar “250” and Madopar fast-acting tablets / dispersible / “125”. No dose adjustment is required in patients with mild or moderate renal impairment. Madopar is well tolerated by patients on hemodialysis. With long-term treatment, fluctuations may occur - episodes of “freezing”, weakening of the effect towards the end of the dose period, the “on-off” phenomenon. To eliminate these symptoms or reduce their severity, dose adjustments should be made, possibly by prescribing smaller doses, but more often. Subsequently, you can try to increase the dose again to enhance the therapeutic effect. Restless legs syndrome. To avoid an increase in the symptoms of restless legs syndrome (early appearance during the day, increasing severity and involvement of other parts of the body), the daily dose should not exceed the recommended maximum dose of 500 mg (400 mg levodopa + 100 mg benserazide) of Madopar. If clinical symptoms increase, the dose of levodopa should be reduced or levodopa should be gradually discontinued and other therapy should be prescribed.

Indications of the drug Madopar® “125”

Parkinson's disease:

— Madopar® fast-acting tablets (dispersible) “125” — a special dosage form for patients with dysphagia and akinesia in the early morning hours and in the afternoon, or with the phenomena of “depletion of the effect of a single dose” or “increase in the latent period before the onset of the clinical effect of the drug ";

— Madopar® GSS “125” is indicated for any type of fluctuation in the effect of levodopa (namely: “peak dose dyskinesia” and “end dose phenomenon”, for example, immobility at night);

restless legs syndrome, including idiopathic and restless legs syndrome in patients with chronic renal failure on dialysis.

Madopar® gss "125" (Madopar® hbs "125")

Treatment should be started gradually, with individual doses adjusted until the optimal therapeutic effect is achieved.

Madopar® 125 capsules should be swallowed whole without chewing.

Madopar® GSS “125” capsules should be swallowed whole without chewing; they should not be opened before use to avoid loss of the modified release effect of the active substance.

Madopar® 250 tablets can be crushed to make them easier to swallow.

Madopar® "125" fast-acting tablets (dispersible) should be dissolved in 25-50 ml of water. The tablet completely dissolves in a few minutes to form a milky-white solution, which should be taken no later than 30 minutes after the tablet dissolves. Since a precipitate can quickly form, it is recommended to stir the solution before use.

Parkinson's disease

Standard dosage regimen

Orally, at least 30 minutes before or 1 hour after meals.

Initial therapy

At the early stage of Parkinson's disease, it is recommended to begin treatment with Madopar at a dose of 62.5 mg (50 mg levodopa + 12.5 mg benserazide 3-4 times a day). If well tolerated, the dose should be gradually increased, depending on the patient's response.

The optimal effect is achieved, as a rule, with a daily dose containing 300-800 mg of levodopa + 75-200 mg of benserazide, taken in 3 or more doses. It may take 4 to 6 weeks to achieve optimal results. Further increases in the daily dose, if necessary, should be carried out at intervals of 1 month.

Maintenance therapy

The average maintenance dose is 125 mg (100 mg levodopa + 25 mg benserazide) Madopar 3-6 times a day. The frequency of administration (at least 3 times) during the day should be distributed so as to ensure optimal effect. To optimize the effect, it may be necessary to replace Madopar "125" in the form of regular capsules and Madopar "250" in the form of regular tablets with Madopar® "125" fast-acting tablets (dispersible) or Madopar® GSS "125".

Restless legs syndrome

The drug should be taken 1 hour before bedtime, with a small amount of food. The maximum daily dose is 500 mg Madopar (400 mg levodopa + 100 mg benserazide).

Idiopathic restless legs syndrome with sleep disturbances

It is recommended to prescribe Madopar® “125” capsules or Madopar® “250” tablets.

The initial dose is 62.5-125 mg. If the effect is insufficient, the dose of Madopar should be increased to 250 mg (200 mg levodopa + 50 mg benserazide).

Idiopathic restless legs syndrome with sleep and sleep disorders

The initial dose is 1 capsule of Madopar® GSS “125” and 1 capsule of Madopar® “125” 1 hour before bedtime. If the effect is insufficient, the dose of Madopar GSS “125” should be increased to 250 mg (2 capsules).

Idiopathic restless legs syndrome with difficulty falling asleep and staying asleep, as well as disturbances during the day

Additionally: 1 dispersible tablet or 1 capsule of Madopar® “125”, the maximum daily dose of Madopar is 500 mg (400 mg of levodopa and 100 mg of benserazide).

Restless legs syndrome in patients with chronic renal failure receiving dialysis

The drug is prescribed in a dose of 125 mg (1 dispersible tablet or 1 capsule of Madopar® “125”) 30 minutes before the start of dialysis.

Dosage regimen in special cases

Parkinson's disease

Madopar® can be combined with other antiparkinsonian drugs. However, as treatment continues, it may be necessary to reduce the dose of other drugs or gradually discontinue them.

Madopar® "125" fast-acting tablets (dispersible) - a special dosage form for patients with dysphagia or akinesia in the early morning and afternoon or for patients with the phenomenon of "depletion of the effect of a single dose" or "increasing the latency period before the onset of clinical effect of the drug "

If during the day the patient experiences strong motor fluctuations (the phenomenon of “exhaustion of the effect of a single dose”, the phenomenon of “on-off”), it is recommended either more frequent administration of correspondingly smaller single doses, or, which is preferable, the use of Madopar GSS “125”.

It is best to switch to Madopar® GSS “125” from one day to the next, starting with the morning dose. You should keep the same daily dose and dosage regimen as when taking Madopar “125” and Madopar “250”.

After 2-3 days, the dose is gradually increased by approximately 50%. Patients should be warned that their condition may temporarily worsen. Due to the characteristics of the dosage form, Madopar® GSS “125” begins to act somewhat later.

The clinical effect can be achieved faster by prescribing Madopar® GSS “125” together with Madopar® “125” capsules or Madopar “125” fast-acting tablets (dispersible). This may be optimal as the first morning dose, which should be slightly higher than subsequent doses.

The dose of Madopar GSS "125" should be adjusted slowly and carefully, and the interval between dose changes should be at least 2-3 days.

In patients with symptoms of the disease that manifest themselves at night, a positive effect was achieved by gradually increasing the evening dose of Madopar GSS “125” to 250 mg (2 capsules) before bedtime.

If the effect of Madopar GSS “125” (dyskinesia) is pronounced, increasing the intervals between doses is more effective than reducing the single dose.

If Madopar® GSS "125" is not effective enough, it is recommended to return to the previously used treatment with Madopar "125", Madopar "250" or Madopar "125" fast-acting tablets (dispersible).

With long-term therapy, episodes of “freezing”, “exhaustion phenomenon” and the “on-off” phenomenon may occur. In case of episodes of “freezing”, “exhaustion phenomenon”, the dose of the drug is divided (reducing the single dose or shortening the interval between doses of the drug), and when the “on-off” phenomenon occurs, the single dose is increased with a decrease in the number of doses. Subsequently, you can try to increase the dose again to enhance the effectiveness of treatment.

In patients with mild or moderate renal impairment

no dose adjustment is required.
Madopar® is well tolerated by patients receiving hemodialysis sessions
.

Restless legs syndrome

To avoid an increase in the symptoms of restless legs syndrome (early appearance during the day, increasing severity and involvement of other parts of the body), the daily dose should not exceed the recommended maximum dose of Madopar - 500 mg (400 mg levodopa + 100 mg benserazide).

If clinical symptoms increase, the dose of levodopa should be reduced or levodopa should be gradually discontinued and other therapy should be prescribed.

Contraindications

hypersensitivity to levodopa, benserazide or any other component of the drug;

decompensated dysfunction of endocrine organs, liver or kidneys (except for patients with restless legs syndrome receiving dialysis);

diseases of the cardiovascular system in the stage of decompensation;

mental illness with a psychotic component;

angle-closure glaucoma;

in combination with non-selective MAO inhibitors or a combination of MAO-A and MAO-B inhibitors;

age under 25 years;

pregnancy;

breastfeeding period;

women of childbearing age who are not using reliable methods of contraception (see “Pregnancy and lactation”).

Use during pregnancy and breastfeeding

Madopar® is absolutely contraindicated during pregnancy and in women of childbearing age who do not use reliable methods of contraception, due to possible disruption of skeletal development in the fetus.

If pregnancy occurs during treatment, the drug should be discontinued in accordance with the recommendations of the attending physician.

If it is necessary to take Madopar® during breastfeeding, breastfeeding should be discontinued due to the lack of reliable data on the penetration of benserazide into breast milk. The risk of abnormal skeletal development in a newborn cannot be ruled out.

Side effects

From the blood system: rare cases of hemolytic anemia, transient leukopenia, thrombocytopenia. In patients taking levodopa for a long time, it is recommended to periodically monitor the blood count, liver and kidney function.

From the gastrointestinal tract: anorexia, nausea, vomiting, diarrhea, isolated cases of loss or change in taste, dryness of the oral mucosa.

On the skin: rarely - itching, rash.

From the cardiovascular system: arrhythmias, orthostatic hypotension (weakens after reducing the dose of Madopar®), arterial hypertension.

From the nervous system and mental sphere: agitation, anxiety, insomnia, hallucinations, delirium, temporary disorientation (especially in elderly patients and patients with a history of these symptoms), depression, headache, dizziness, sometimes in later stages of treatment - spontaneous movements (such as chorea or athetosis), episodes of “freezing”, weakening of the effect towards the end of the dose period (the “exhaustion” phenomenon), the “on-off” phenomenon, severe drowsiness, episodes of sudden drowsiness, increased manifestations of restless legs syndrome .

From the body as a whole: febrile infection, rhinitis, bronchitis.

Laboratory indicators: sometimes - a transient increase in the activity of liver transaminases and alkaline phosphatase, an increase in blood urea nitrogen, a change in the color of urine to red, darkening when standing.

Interaction

Pharmacokinetic interaction

Trihexyphenidyl (an anticholinergic drug) reduces the rate, but not the extent, of absorption of levodopa. The administration of trihexyphenidyl together with Madopar® GSS “125” does not affect other parameters of the pharmacokinetics of levodopa.

Antacids reduce the degree of absorption of levodopa by 32% when prescribed with Madopar® GSS "125".

Ferrous sulfate reduces the plasma levodopa Cmax and AUC by 30–50%, which is a clinically significant change in some patients.

Metoclopramide increases the rate of absorption of levodopa.

Levodopa does not interact pharmacokinetically with bromocriptine, amantadine, selegiline and domperidone.

Pharmacodynamic interaction

Neuroleptics, opiates and antihypertensive drugs containing reserpine suppress the effect of Madopar®.

MAO inhibitors. If Madopar® is prescribed to patients receiving irreversible non-selective MAO inhibitors, then at least 2 weeks must elapse from stopping the MAO inhibitor before starting Madopar® (see “Contraindications”). However, selective MAO-B inhibitors (such as selegiline or rasagiline) and selective MAO-A inhibitors (such as moclobemide) can be prescribed to patients taking Madopar®. It is recommended to adjust the dose of levodopa depending on the patient's individual needs in terms of effectiveness and tolerability. The combination of MAO-A and MAO-B inhibitors is equivalent to taking a non-selective MAO inhibitor, therefore such a combination should not be prescribed simultaneously with Madopar®.

Sympathomimetics (adrenaline, norepinephrine, isoproterenol, amphetamine). Madopar® should not be prescribed simultaneously with sympathomimetics, since levodopa may potentiate their effect. If concomitant use is still necessary, careful monitoring of the cardiovascular system and, if necessary, reducing the dose of sympathomimetics are very important.

Antiparkinsonian drugs. The combined use of the drug with other antiparkinsonian drugs (anticholinergics, amantadine, dopamine agonists) is possible, but this may enhance not only the desired, but also the undesirable effects. It may be necessary to reduce the dose of Madopar® or another drug. If a catechol-o-methyltransferase inhibitor (COMT) is added to treatment, a reduction in the dose of Madopar® may be required. When starting Madopar® therapy, anticholinergic drugs should not be discontinued abruptly, since levodopa does not begin to act immediately.

Levodopa may affect laboratory results of catecholamines, creatinine, uric acid and glucose, and a false-positive Coombs test result is possible.

In patients receiving Madopar®, taking the drug simultaneously with a protein-rich meal may interfere with the absorption of levodopa from the gastrointestinal tract.

General anesthesia with halothane. Taking Madopar® should be discontinued 12–48 hours before surgery, since a patient receiving Madopar® may experience blood pressure fluctuations and arrhythmia during halothane anesthesia.

Madopar® "125" (Madopar® "125")

Capsules (Madopar® “125” or Madopar® GSS “125”) should be swallowed whole without chewing. Capsules of the drug Madopar® GSS “125” cannot be opened before use, otherwise the effect of the modified release of the active substance is lost.

Tablets (Madopar® 250) can be crushed to make them easier to swallow. The drug Madopar® fast-acting tablets (dispersible) “125” should be dissolved in a quarter glass of water (25-50 ml); The tablet dissolves completely after a few minutes to form a milky-white suspension, which should be taken no later than half an hour after the tablet has dissolved. Since a precipitate can quickly form, it is recommended to stir the solution before use.

Parkinson's disease

Orally, at least 30 minutes before or 1 hour after meals. This method of administration will avoid the competitive influence on the absorption of levodopa from protein supplied with food (see section “Interaction with other drugs”), and will contribute to a more rapid onset of action of the drug.

Standard dosage regimen

Treatment should be started gradually, with individual doses adjusted until the optimal effect is achieved.

Initial therapy

In the early stages of Parkinson's disease, it is recommended to start treatment with 62.5 mg (50 mg levodopa + 12.5 mg benserazide) in the form of 1/2 tablet of Madopar® fast-acting tablets (dispersible) “125” or 1/4 tablet of Madopar® “250”, 3-4 times a day. If the initial dosing schedule is tolerated, the dose should be increased slowly based on patient response.

The optimal effect is usually achieved with a daily dose of 300-800 mg levodopa + 75-200 mg benserazide, taken in three or more divided doses. It may take 4 to 6 weeks to achieve optimal results. If it is necessary to further increase the daily dose, this should be done at intervals of 1 month.

Maintenance therapy

The average maintenance dose is 125 mg (100 mg levodopa + 25 mg benserazide) 3-6 times a day. The number of doses (at least three) and their distribution throughout the day should ensure optimal effect.

To optimize the effect, you can replace Madopar® “125” capsules with Madopar® GSS “125” capsules, Madopar® fast-acting tablets (dispersible) “125”, or Madopar® “250” tablets.

Restless legs syndrome

The maximum permissible dose per day is 500 mg of the appropriate form of Madopar® (400 mg levodopa + 100 mg benserazide).

1 hour before bedtime with low protein food. Before using the appropriate form of Madopar®, you should refrain from eating foods rich in protein.

Idiopathic restless legs syndrome with sleep disturbances

It is recommended to prescribe Madopar® “125” capsules or Madopar® “250” tablets.

Initial dose: 62.5 mg (50 mg levodopa + 12.5 mg benserazide) - 125 mg (100 mg levodopa + 25 mg benserazide) of the appropriate form of Madopar®. If the effect is insufficient, the dose should be increased to 250 mg (200 mg levodopa + 50 mg benserazide) of the drug.

Idiopathic restless legs syndrome with sleep and sleep disorders

Initial dose: 1 capsule of Madopar® GSS “125” and 1 capsule of Madopar® “125” 1 hour before bedtime. If the effect is insufficient, it is recommended to increase the dose of Madopar® GSS “125” to 250 mg (2 capsules).

Idiopathic restless legs syndrome with difficulty falling asleep and staying asleep, as well as disturbances during the day

Additionally: 1 tablet of the drug Madopar® fast-acting tablets (dispersible) “125” or 1 capsule of the drug Madopar® “125”, the maximum permissible daily dose is 500 mg (400 mg levodopa + 100 mg benserazide) of the drug.

Restless legs syndrome in patients with chronic renal failure receiving dialysis

125 mg of the appropriate form of Madopar® (1 tablet of Madopar® fast-acting tablets (dispersible) “125” or 1 capsule of Madopar® “125”) 30 minutes before the start of dialysis.

Dosage regimen in special cases

Parkinson's disease

The drug Madopar® "125" can be combined with other antiparkinsonian drugs; as treatment continues, it may be necessary to reduce the dose of other drugs or gradually discontinue them.

The drug Madopar® fast-acting tablets (dispersible) “125” is a special dosage form for patients with dysphagia or akinesia in the early morning hours and in the afternoon or with the phenomena of “depletion of the effect of a single dose” or “increase in the latent period before the onset of the clinical effect of the drug” .

If during the day the patient experiences pronounced motor fluctuations (the phenomenon of “exhaustion of the effect of a single dose”, the phenomenon of “on-off”), it is recommended either more frequent administration of correspondingly smaller single doses, or, which is preferable, the use of the drug Madopar® GSS “125” .

It is better to start the transition to the drug Madopar® GSS "125" with the morning dose, maintaining the daily dose and regimen of the drug Madopar® "125" or the drug Madopar® "250".

After 2-3 days, the dose is gradually increased by approximately 50%. The patient should be warned that his condition may temporarily worsen. Due to its pharmacokinetic properties, the drug Madopar® GSS “125” begins to act somewhat later.

The clinical effect can be achieved faster by prescribing the drug Madopar® GSS “125” together with capsules of the drug Madopar® “125” or dispersible tablets of the drug Madopar® fast-acting tablets (dispersible) “125”. This may be especially useful in the case of the first morning dose, which should be slightly higher than subsequent doses.

The individual dose of Madopar® GSS “125” should be selected slowly and carefully, the interval between dose changes should be at least 2-3 days.

In patients with nocturnal symptoms, a positive effect was achieved by gradually increasing the evening dose of Madopar® GSS “125” to 250 mg (2 capsules) before going to bed.

To eliminate the pronounced effect of the drug Madopar® GSS "125" (dyskinesia), increasing the intervals between doses is more effective than reducing the single dose.

If Madopar® GSS “125” is not effective enough, it is recommended to return to previous treatment with Madopar® “125”, Madopar® “250” and Madopar® fast-acting tablets (dispersible) “125”.

In patients with mild or moderate renal impairment

no dose adjustment is required.

In patients with liver failure

the efficacy and safety profile of Madopar® “125” has not been established (see section “Contraindications”).

The drug Madopar® "125" is well tolerated by patients on hemodialysis.

With long-term treatment, fluctuations may occur - episodes of “freezing”, weakening of the effect towards the end of the dose period, the “on-off” phenomenon. To eliminate these symptoms or reduce their severity, dose adjustments should be made, possibly by prescribing smaller doses, but more often. Subsequently, you can try to increase the dose again to enhance the therapeutic effect.

Restless legs syndrome

To avoid an increase in the symptoms of restless legs syndrome (early appearance during the day, increasing severity and involvement of other parts of the body), the daily dose should not exceed the recommended maximum dose of 500 mg (400 mg levodopa + 100 mg benserazide) of the drug.

If clinical symptoms increase, the dose of the drug should be reduced or the drug should be gradually discontinued and other therapy prescribed.

Directions for use and doses

Orally, at least 30 minutes before or 1 hour after meals.

Capsules (Madopar® “125” or Madopar® GSS “125”) should be swallowed whole without chewing. Madopar® GSS “125” capsules cannot be opened before use, otherwise the effect of the modified release of the active substance is lost.

Tablets (Madopar® 250) can be crushed to make them easier to swallow.

Dispersible tablets (Madopar® fast-acting tablets (dispersible) “125”) should be dissolved in 1/4 cup of water (25–50 ml); The tablet dissolves completely after a few minutes to form a milky-white suspension, which should be taken no later than 30 minutes after the tablet has dissolved. Since a precipitate can quickly form, it is recommended to stir the solution before use.

Parkinson's disease

Standard dosage regimen

Treatment should be started gradually, with individual doses adjusted until the optimal effect is achieved.

Initial therapy

At the early stage of Parkinson's disease, it is recommended to start treatment with Madopar® with 62.5 mg (50 mg levodopa + 12.5 mg benserazide) 3-4 times a day. If the initial dosing schedule is tolerated, the dose should be increased slowly based on patient response.

The optimal effect is usually achieved with a daily dose of 300–800 mg levodopa + 75–200 mg benserazide, taken in 3 or more divided 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.

Maintenance treatment

The average maintenance dose is 125 mg (100 mg levodopa + 25 mg benserazide) 3-6 times a day. The number of doses (at least 3) and their distribution throughout the day should ensure optimal effect.

To optimize the effect, you can replace Madopar® “125” capsules and Madopar® “250” tablets with Madopar® fast-acting tablets (dispersible) or Madopar® GSS “125” capsules.

Restless legs syndrome

The maximum permissible dose is 500 mg/day Madopar® (400 mg levodopa + 100 mg benserazide). 1 hour before bedtime, with a small amount of food.

Idiopathic restless legs syndrome with sleep disturbances

It is recommended to prescribe Madopar® “125” capsules or Madopar® “250” tablets.

Initial dose: 62.5 mg (50 mg levodopa + 12.5 mg benserazide)–125 mg (100 mg levodopa + 25 mg benserazide) Madopar®. If the effect is insufficient, the dose should be increased to 250 mg (200 mg levodopa + 50 mg benserazide) Madopar®.

Idiopathic restless legs syndrome with sleep and sleep disorders

Initial dose: 1 capsule. Madopar® GSS “125” and 1 caps. Madopar® “125” 1 hour before bedtime. If the effect is insufficient, it is recommended to increase the dose of Madopar® GSS “125” to 250 mg (2 capsules).

Idiopathic restless legs syndrome with difficulty falling asleep and staying asleep, as well as disturbances during the day

Additionally: 1 table. dispersible or 1 cap. Madopar® "125", the maximum permissible daily dose is 500 mg (400 mg levodopa + 100 mg benserazide).

Restless legs syndrome in patients with chronic renal failure receiving dialysis

125 mg Madopar® (1 dispersible tablet or 1 capsule Madopar® “125”) 30 minutes before the start of dialysis.

Dosing in special cases

Parkinson's disease

Madopar® can be combined with other antiparkinsonian drugs; as treatment continues, it may be necessary to reduce the dose of other drugs or gradually discontinue them.

Madopar® fast-acting tablets (dispersible) “125” is a special dosage form for patients with dysphagia or akinesia in the early morning and afternoon, or with the phenomena of “depletion of the effect of a single dose” or “increase in the latent period before the onset of the clinical effect of the drug” .

If during the day the patient experiences pronounced motor fluctuations (the phenomenon of “exhaustion of the effect of a single dose”, the phenomenon of “on-off”), it is recommended either more frequent administration of correspondingly smaller single doses, or, which is preferable, the use of Madopar® GSS “125”.

It is best to start the transition to Madopar® GSS "125" with the morning dose, maintaining the daily dose and dosage regimen of Madopar® "125" or Madopar® "250".

After 2–3 days, the dose is gradually increased by approximately 50%. The patient should be warned that his condition may temporarily worsen. Due to its pharmacological properties, Madopar® GSS “125” begins to act somewhat later. The clinical effect can be achieved faster by prescribing Madopar® GSS “125” together with Madopar® “125” capsules or dispersible tablets. This may be especially useful in the case of the first morning dose, which should be slightly higher than subsequent doses. The individual dose of Madopar® GSS “125” should be adjusted slowly and carefully, and the interval between dose changes should be at least 2–3 days.

In patients with nocturnal symptoms, a positive effect was achieved by gradually increasing the evening dose of Madopar® GSS “125” to 250 mg (2 capsules) before going to bed.

To eliminate the pronounced effect of Madopar® GSS “125” (dyskinesia), increasing the intervals between doses is more effective than reducing the single dose.

If Madopar® GSS "125" is not effective enough even at a daily dose corresponding to 1500 mg of levodopa, it is recommended to return to the previous treatment with Madopar® "125", Madopar® "250" and Madopar® fast-acting tablets (dispersible) "125".

No dose adjustment is required in patients with mild or moderate renal impairment.

Madopar® is well tolerated by patients receiving hemodialysis sessions.

With long-term therapy, episodes of “freezing”, “exhaustion phenomenon”, and “on-off” phenomena may occur. During episodes of “freezing” and the “exhaustion phenomenon,” they resort to splitting the dose of the drug (reducing the single dose or shortening the interval between doses of the drug), and when the “on-off” phenomenon occurs, increasing the single dose while reducing the number of doses. Subsequently, you can try to increase the dose again to enhance the effect of treatment.

Restless legs syndrome

To avoid an increase in the symptoms of restless legs syndrome (early appearance during the day, increasing severity and involvement of other parts of the body), the daily dose should not exceed the recommended maximum dose of 500 mg (400 mg levodopa + 100 mg benserazide) of Madopar®.

If clinical symptoms increase, the dose of levodopa should be reduced or levodopa should be gradually discontinued and other therapy should be prescribed.

Madopar GSS 125 100mg+25mg caps modif vysv No. 100

Capsules (Madopar® “125” or Madopar® GSS “125”) should be swallowed whole without chewing. Madopar® GSS “125” capsules cannot be opened before use, otherwise the effect of the modified release of the active substance is lost.

Tablets (Madopar® 250) can be crushed to make them easier to swallow.

Dispersible tablets (Madopar® fast-acting tablets /dispersible/ “125”) should be dissolved in a quarter glass of water (25–50 ml); The tablet dissolves completely after a few minutes to form a milky-white suspension, which should be taken no later than half an hour after the tablet has dissolved. Since a precipitate can quickly form, it is recommended to stir the solution before use.

Parkinson's disease

Orally, at least 30 minutes before or 1 hour after meals.

Standard dosage regimen

Treatment should be started gradually, with individual doses adjusted until the optimal effect is achieved.

Initial therapy

At the early stage of Parkinson's disease, it is recommended to start treatment with Madopar® with 62.5 mg (50 mg levodopa + 12.5 mg benserazide) 3-4 times a day. If the initial dosing schedule is tolerated, the dose should be increased slowly based on patient response. The optimal effect is usually achieved with a daily dose of 300–800 mg levodopa + 75–200 mg benserazide, taken in three or more divided doses. It may take 4 to 6 weeks to achieve optimal results. If it is necessary to further increase the daily dose, this should be done at intervals of 1 month.

Maintenance therapy

The average maintenance dose is 125 mg (100 mg levodopa + 25 mg benserazide) 3-6 times a day. The number of doses (at least three) and their distribution throughout the day should ensure optimal effect.

To optimize the effect, you can replace Madopar® “125” capsules and Madopar® “250” tablets with Madopar® fast-acting tablets /dispersible/ “125” or Madopar® GSS “125” capsules.

Restless legs syndrome

The maximum permissible dose per day is 500 mg Madopar® (400 mg levodopa + 100 mg benserazide).

1 hour before bedtime with a small amount of food. Before using Madopar®, you should refrain from eating foods rich in protein.

Idiopathic restless legs syndrome with sleep disturbances

It is recommended to prescribe Madopar® “125” capsules or Madopar® “250” tablets.

Initial dose: 62.5 mg (50 mg levodopa + 12.5 mg benserazide) - 125 mg (100 mg levodopa + 25 mg benserazide) Madopar®. If the effect is insufficient, the dose should be increased to 250 mg (200 mg levodopa + 50 mg benserazide) Madopar®.

Idiopathic restless legs syndrome with sleep and sleep disorders

Initial dose: 1 capsule of Madopar® GSS “125” and 1 capsule of Madopar® “125” 1 hour before bedtime. If the effect is insufficient, it is recommended to increase the dose of Madopar® GSS “125” to 250 mg (2 capsules).

Idiopathic restless legs syndrome with difficulty falling asleep and staying asleep, as well as disturbances during the day

Additionally: 1 dispersible tablet or 1 capsule Madopar® “125”, the maximum permissible daily dose is 500 mg (400 mg levodopa + 100 mg benserazide) Madopar®.

Restless legs syndrome in patients with chronic renal failure receiving dialysis

125 mg Madopar® (1 dispersible tablet or 1 capsule Madopar® “125”) 30 minutes before the start of dialysis.

Dosing in special cases

Parkinson's disease

Madopar® can be combined with other antiparkinsonian drugs; as treatment continues, it may be necessary to reduce the dose of other drugs or gradually discontinue them.

Madopar® fast-acting tablets /dispersible/ “125” is a special dosage form for patients with dysphagia or akinesia in the early morning hours and in the afternoon or with the phenomena of “depletion of the effect of a single dose” or “increase in the latent period before the onset of the clinical effect of the drug.”

If during the day the patient experiences pronounced motor fluctuations (the phenomenon of “exhaustion of the effect of a single dose”, the phenomenon of “on-off”), it is recommended either more frequent administration of correspondingly smaller single doses, or, which is preferable, the use of Madopar® GSS “125”.

It is better to start the transition to Madopar® GSS "125" with the morning dose, maintaining the daily dose and dosage regimen of Madopar® "125" or Madopar® "250".

After 2–3 days, the dose is gradually increased by approximately 50%. The patient should be warned that his condition may temporarily worsen. Due to its pharmacokinetic properties, Madopar® GSS “125” begins to act somewhat later. The clinical effect can be achieved faster by prescribing Madopar® GSS “125” together with Madopar® “125” capsules or dispersible tablets. This may be especially useful in the case of the first morning dose, which should be slightly higher than subsequent doses. The individual dose of Madopar® GSS "125" must be selected slowly and carefully, the interval between dose changes should be at least 2-3 days.

In patients with nocturnal symptoms, a positive effect was achieved by gradually increasing the evening dose of Madopar® GSS “125” to 250 mg (2 capsules) before going to bed.

To eliminate the pronounced effect of Madopar® GSS “125” (dyskinesia), increasing the intervals between doses is more effective than reducing the single dose.

If Madopar® GSS “125” is not effective enough, it is recommended to return to the previous treatment with Madopar® “125”, Madopar® “250” and Madopar® fast-acting tablets /dispersible/ “125”.

No dose adjustment is required in patients with mild or moderate renal impairment.

Madopar® is well tolerated by patients on hemodialysis.

With long-term treatment, fluctuations may occur - episodes of “freezing”, weakening of the effect towards the end of the dose period, the “on-off” phenomenon. To eliminate these symptoms or reduce their severity, dose adjustments should be made, possibly by prescribing smaller doses, but more often. Subsequently, you can try to increase the dose again to enhance the therapeutic effect.

Restless legs syndrome

To avoid an increase in the symptoms of restless legs syndrome (early appearance during the day, increasing severity and involvement of other parts of the body), the daily dose should not exceed the recommended maximum dose of 500 mg (400 mg levodopa + 100 mg benserazide) of Madopar®.

If clinical symptoms increase, the dose of levodopa should be reduced or levodopa should be gradually discontinued and other therapy should be prescribed.

Overdose

Symptoms: from the cardiovascular system - arrhythmias; mental sphere - confusion, insomnia; from the gastrointestinal tract - nausea and vomiting; pathological involuntary movements (mentioned in the “Side effects” section, but in a more pronounced form).

When taking modified-release capsules (Madopar® GSS "125"), the onset of overdose symptoms may occur later due to slow absorption of the active substances in the stomach.

Treatment: it is necessary to monitor vital functions; symptomatic therapy - the prescription of respiratory analeptics, antiarrhythmic drugs, and, in appropriate cases, neuroleptics.

When using a dosage form with a modified release of active substances (Madopar® GSS “125”), further absorption of the drug should be prevented.

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** The Drug Directory is intended for informational purposes only. For more complete information, please refer to the manufacturer's instructions. Do not self-medicate; Before starting to use the drug Madopar fast-acting tablets (dispersible) “125” you should consult a doctor. EUROLAB is not responsible for the consequences caused by the use of information posted on the portal. Any information on the site does not replace medical advice and cannot serve as a guarantee of the positive effect of the drug.

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special instructions

Persons with hypersensitivity to the drug may develop corresponding reactions.

In patients with open-angle glaucoma, it is recommended that intraocular pressure be measured regularly because levodopa may theoretically increase intraocular pressure.

Side effects from the gastrointestinal tract, which are possible at the initial stage of treatment, can be largely eliminated if Madopar® is taken with a small amount of food or liquid, and also if the dose is increased slowly.

During treatment, it is necessary to monitor liver and kidney function and blood count.

Patients with diabetes need to frequently monitor blood glucose levels and adjust the dose of hypoglycemic drugs.

If surgery with general anesthesia is necessary, Madopar® therapy should be continued until surgery, with the exception of general anesthesia with halothane. Since blood pressure fluctuations and arrhythmia may occur in a patient receiving Madopar® during halothane anesthesia, Madopar® should be discontinued 12–48 hours before surgery. After surgery, treatment is resumed, gradually increasing the dose to the previous level.

Madopar® should not be discontinued abruptly. Abrupt discontinuation of the drug may lead to “neuroleptic malignant syndrome” (fever, muscle stiffness, as well as possible mental changes and increased serum creatine phosphokinase), which can become life-threatening. If such symptoms occur, the patient should be under medical supervision (if necessary, hospitalized) and receive appropriate symptomatic therapy. This may include re-prescribing Madopar® after appropriate assessment of the patient's condition.

Depression can be either a clinical manifestation of the underlying disease (parkinsonism, restless legs syndrome) or occur during Madopar® therapy. The patient should be carefully monitored for the possible occurrence of psychiatric adverse reactions.

Possibility of drug dependence and abuse

Some patients with Parkinson's disease have experienced the appearance of behavioral and cognitive disorders as a result of uncontrolled use of increasing doses of the drug, despite the doctor's recommendations and significantly exceeding therapeutic doses of the drug.

Impact on driving vehicles and working with machines and mechanisms

If drowsiness occurs, incl. sudden episodes of drowsiness, you should avoid driving a car or working with machinery. If these symptoms occur, dose reduction or discontinuation of therapy should be considered.

Madopar fast-acting tablets (dispersible) “125” 100mg+25mg 100 pcs.

pharmachologic effect

Antiparkinsonian drug (dopamine precursor + peripheral decarboxylase inhibitor)

Composition and release form Madopar fast-acting tablets (dispersible) “125” 100 mg + 25 mg 100 pcs.

Dispersible tablets - 1 tablet:

• Active ingredients: levodopa - 100 mg; benserazide hydrochloride - 28.5 mg, which corresponds to the content of benserazide - 25 mg;
• Excipients: anhydrous citric acid - 20 mg, pregelatinized corn starch - 41.5 mg, microcrystalline cellulose - 303 mg, magnesium stearate - 7 mg.

30 pcs. - dark glass bottles (1) - cardboard packs. 100 pieces. - dark glass bottles (1) - cardboard packs.

Description of the dosage form

Dispersible tablets are white or almost white, cylindrical, flat on both sides, with a beveled edge, odorless or slightly odorless, slightly marbled, engraved “ROCHE 125” on one side and a break line on the other; tablet diameter is about 11 mm, thickness is about 4.2 mm.

Directions for use and doses

Treatment should be started gradually, with individual doses adjusted until the optimal therapeutic effect is achieved.

Madopar® 125 capsules should be swallowed whole without chewing.

Madopar® GSS “125” capsules should be swallowed whole without chewing; they should not be opened before use to avoid loss of the modified release effect of the active substance.

Madopar® 250 tablets can be crushed to make them easier to swallow.

Madopar® "125" fast-acting tablets (dispersible) should be dissolved in 25-50 ml of water. The tablet completely dissolves in a few minutes to form a milky-white solution, which should be taken no later than 30 minutes after the tablet dissolves. Since a precipitate can quickly form, it is recommended to stir the solution before use.

Parkinson's disease

Standard dosage regimen

Orally, at least 30 minutes before or 1 hour after meals.

Initial therapy

At the early stage of Parkinson's disease, it is recommended to begin treatment with Madopar at a dose of 62.5 mg (50 mg levodopa + 12.5 mg benserazide 3-4 times a day). If well tolerated, the dose should be gradually increased, depending on the patient's response.

The optimal effect is achieved, as a rule, with a daily dose containing 300-800 mg of levodopa + 75-200 mg of benserazide, taken in 3 or more doses. It may take 4 to 6 weeks to achieve optimal results. Further increases in the daily dose, if necessary, should be carried out at intervals of 1 month.

Maintenance therapy

The average maintenance dose is 125 mg (100 mg levodopa + 25 mg benserazide) Madopar 3-6 times a day. The frequency of administration (at least 3 times) during the day should be distributed so as to ensure optimal effect. To optimize the effect, it may be necessary to replace Madopar "125" in the form of regular capsules and Madopar "250" in the form of regular tablets with Madopar® "125" fast-acting tablets (dispersible) or Madopar® GSS "125".

Restless legs syndrome

The drug should be taken 1 hour before bedtime, with a small amount of food. The maximum daily dose is 500 mg Madopar (400 mg levodopa + 100 mg benserazide).

Idiopathic restless legs syndrome with sleep disturbances

It is recommended to prescribe Madopar® “125” capsules or Madopar® “250” tablets.

The initial dose is 62.5-125 mg. If the effect is insufficient, the dose of Madopar should be increased to 250 mg (200 mg levodopa + 50 mg benserazide).

Idiopathic restless legs syndrome with sleep and sleep disorders

The initial dose is 1 capsule of Madopar® GSS “125” and 1 capsule of Madopar® “125” 1 hour before bedtime. If the effect is insufficient, the dose of Madopar GSS “125” should be increased to 250 mg (2 capsules).

Idiopathic restless legs syndrome with difficulty falling asleep and staying asleep, as well as disturbances during the day

Additionally: 1 dispersible tablet or 1 capsule of Madopar® “125”, the maximum daily dose of Madopar is 500 mg (400 mg of levodopa and 100 mg of benserazide).

Restless legs syndrome in patients with chronic renal failure receiving dialysis

The drug is prescribed in a dose of 125 mg (1 dispersible tablet or 1 capsule of Madopar® “125”) 30 minutes before the start of dialysis.

Dosage regimen in special cases

Parkinson's disease

Madopar® can be combined with other antiparkinsonian drugs. However, as treatment continues, it may be necessary to reduce the dose of other drugs or gradually discontinue them.

Madopar® "125" fast-acting tablets (dispersible) - a special dosage form for patients with dysphagia or akinesia in the early morning and afternoon or for patients with the phenomenon of "depletion of the effect of a single dose" or "increasing the latency period before the onset of clinical effect of the drug "

If during the day the patient experiences strong motor fluctuations (the phenomenon of “exhaustion of the effect of a single dose”, the phenomenon of “on-off”), it is recommended either more frequent administration of correspondingly smaller single doses, or, which is preferable, the use of Madopar GSS “125”.

It is best to switch to Madopar® GSS “125” from one day to the next, starting with the morning dose. You should keep the same daily dose and dosage regimen as when taking Madopar “125” and Madopar “250”.

After 2-3 days, the dose is gradually increased by approximately 50%. Patients should be warned that their condition may temporarily worsen. Due to the characteristics of the dosage form, Madopar® GSS “125” begins to act somewhat later.

The clinical effect can be achieved faster by prescribing Madopar® GSS “125” together with Madopar® “125” capsules or Madopar “125” fast-acting tablets (dispersible). This may be optimal as the first morning dose, which should be slightly higher than subsequent doses.

The dose of Madopar GSS "125" should be adjusted slowly and carefully, and the interval between dose changes should be at least 2-3 days.

In patients with symptoms of the disease that manifest themselves at night, a positive effect was achieved by gradually increasing the evening dose of Madopar GSS “125” to 250 mg (2 capsules) before bedtime.

If the effect of Madopar GSS “125” (dyskinesia) is pronounced, increasing the intervals between doses is more effective than reducing the single dose.

If Madopar® GSS "125" is not effective enough, it is recommended to return to the previously used treatment with Madopar "125", Madopar "250" or Madopar "125" fast-acting tablets (dispersible).

With long-term therapy, episodes of “freezing”, “exhaustion phenomenon” and the “on-off” phenomenon may occur. In case of episodes of “freezing”, “exhaustion phenomenon”, the dose of the drug is divided (reducing the single dose or shortening the interval between doses of the drug), and when the “on-off” phenomenon occurs, the single dose is increased with a decrease in the number of doses. Subsequently, you can try to increase the dose again to enhance the effectiveness of treatment.

In patients with mild or moderate renal impairment, no dose adjustment is required. Madopar® is well tolerated by patients receiving hemodialysis sessions.

Restless legs syndrome

To avoid an increase in the symptoms of restless legs syndrome (early appearance during the day, increasing severity and involvement of other parts of the body), the daily dose should not exceed the recommended maximum dose of Madopar - 500 mg (400 mg levodopa + 100 mg benserazide).

If clinical symptoms increase, the dose of levodopa should be reduced or levodopa should be gradually discontinued and other therapy should be prescribed.

Pharmacodynamics

A combined antiparkinsonian drug containing a dopamine precursor and an inhibitor of peripheral decarboxylases.

In Parkinsonism, the brain neurotransmitter dopamine is produced in insufficient quantities in the basal ganglia. Levodopa, or L-DOPA - (3,4-dihydrophenylalanine), is a metabolic precursor of dopamine and, unlike the latter, penetrates well through the BBB. After levodopa enters the central nervous system, it is converted to dopamine by aromatic acid decarboxylase.

Parkinson's disease

Following oral administration, levodopa is rapidly decarboxylated to dopamine in both cerebral and extracerebral tissues. As a result, most of the administered levodopa does not reach the basal ganglia, and peripheral dopamine often causes adverse reactions. Therefore, blocking extracerebral decarboxylation of levodopa is necessary. This is achieved by simultaneous administration of levodopa and benserazide, a peripheral decarboxylase inhibitor.

Madopar® is a combination of these substances in a 4:1 ratio, which is optimal and has the same effectiveness as levodopa in high doses.

Fast-acting (dispersible) tablets are especially indicated for patients with dysphagia, as well as patients who need a faster onset of action of the drug.

GSS capsules are a special dosage form with a delayed release of active substances in the stomach. The maximum concentration in plasma is 20-30% less than when taking Madopar® “125” capsules and Madopar® “250” tablets, and is achieved 3 hours after administration.

Restless legs syndrome

The exact mechanism of restless legs syndrome is unknown, but the dopaminergic system plays an important role in the pathogenesis of this syndrome.

Pharmacokinetics

The pharmacokinetic profiles of levodopa after taking Madopar in this dosage form are similar to those after taking Madopar tablets and capsules, however, the time to reach Cmax tends to shorten. The absorption parameters of fast-acting tablets (dispersible) are less variable between patients than with conventional dosage forms.

Indications for use Madopar fast-acting tablets (dispersible) “125” 100mg+25mg 100 pcs.

Parkinson's disease, including:

• in patients with dysphagia, with akinesia in the early morning hours and in the afternoon, patients with the phenomena of “depletion of the effect of a single dose” or “increase in the latent period before the onset of the clinical effect of the drug” (Madopar® “125” fast-acting tablets (dispersible));
• in patients with any type of fluctuation in the effect of levodopa, namely, “peak dose dyskinesia” and “end dose phenomenon”, for example, immobility at night (Madopar® GSS “125”).

Restless legs syndrome:

• idiopathic restless legs syndrome;
• restless legs syndrome in patients with chronic renal failure on dialysis.

Contraindications

• decompensated dysfunction of the endocrine system organs;
• decompensated liver dysfunction;
• decompensated renal dysfunction (except for patients with restless legs syndrome receiving dialysis);
• diseases of the cardiovascular system in the stage of decompensation;
• mental illness with a psychotic component;
• angle-closure glaucoma;
• simultaneous use with non-selective MAO inhibitors, a combination of MAO type A and MAO type B inhibitors;
• age up to 25 years;
• women of childbearing age who do not use reliable methods of contraception;
• pregnancy;
• lactation period (breastfeeding);
• hypersensitivity to the components of the drug.

Application of Madopar fast-acting tablets (dispersible) “125” 100mg+25mg 100 pcs. during pregnancy and breastfeeding

Madopar® is contraindicated during pregnancy and in women of childbearing age who do not use reliable methods of contraception, due to possible disruption of skeletal development in the fetus.

If pregnancy occurs during treatment with Madopar, the drug should be discontinued immediately in accordance with the recommendations of the attending physician.

It is not known whether benserazide is excreted in breast milk. If it is necessary to use Madopar during lactation, breastfeeding should be stopped, since skeletal development disorders in the child cannot be ruled out.

Contraindication: age under 25 years.

special instructions

Persons with hypersensitivity to the drug may develop corresponding reactions.

Adverse reactions from the digestive system, possible at the initial stage of treatment, are largely eliminated if Madopar® is taken with a small amount of food or liquid, as well as by slowly increasing the dose.

Patients with open-angle glaucoma should have their intraocular pressure measured regularly because levodopa may theoretically increase intraocular pressure.

In patients taking levodopa, it is recommended to periodically monitor blood count, liver and kidney function.

Patients with diabetes mellitus should frequently monitor blood glucose levels and adjust the dose of hypoglycemic drugs.

If possible, Madopar should be continued for as long as possible before general anesthesia, with the exception of halothane anesthesia. Since fluctuations in blood pressure and arrhythmias may occur in a patient receiving Madopar® during halothane anesthesia, Madopar should be discontinued 12-48 hours before surgery. After surgery, treatment is resumed, gradually increasing the dose to the previous level.

Madopar® should not be discontinued abruptly. Abrupt discontinuation of the drug can lead to the development of neuroleptic malignant syndrome (fever, muscle rigidity, as well as possible mental changes and increased serum CPK), which can take a life-threatening form. If such symptoms occur, the patient should be under medical supervision (if necessary, hospitalization) and receive appropriate symptomatic therapy, which may include re-prescribing Madopar after an appropriate assessment of the patient's condition.

Depression can be a clinical manifestation of the underlying disease (parkinsonism, restless legs syndrome) and can also occur during Madopar therapy. Patients taking Madopar® should be carefully monitored for the possible occurrence of psychiatric adverse reactions.

Some patients with Parkinson's disease have experienced the appearance of behavioral and cognitive disorders as a result of uncontrolled use of increasing doses of the drug, despite the doctor's recommendations and significantly exceeding therapeutic doses of the drug.

Impact on the ability to drive vehicles and operate machinery

If drowsiness or sudden episodes of drowsiness occur, the patient should stop driving a car or working with machines and mechanisms. If these symptoms occur, dose reduction or discontinuation of therapy should be considered.

Overdose

Symptoms: increased side effects - arrhythmia, confusion, insomnia, nausea and vomiting, pathological involuntary movements. When taking a dosage form with a modified release of active substances (Madopar® GSS “125”) in the stomach, the onset of symptoms may be delayed.

Treatment: symptomatic therapy - respiratory analeptics, antiarrhythmic drugs, neuroleptics; it is necessary to monitor vital functions. When using a dosage form with a modified release of active substances (Madopar® GSS “125”), further absorption of the drug should be prevented.

Side effects of Madopar fast-acting tablets (dispersible) “125” 100mg+25mg 100 pcs.

From the central nervous system and peripheral nervous system: agitation, anxiety, insomnia, hallucinations, delirium, temporary disorientation (especially in elderly patients and in patients with a history of these symptoms), depression, headache, dizziness, in later stages of treatment sometimes - spontaneous movements (such as chorea or athetosis), episodes of “freezing”, weakening of the effect towards the end of the dose period (the “exhaustion” phenomenon), the “on-off” phenomenon, severe drowsiness, episodes of sudden drowsiness, increased manifestations of restless legs syndrome "

From the digestive system: nausea, vomiting, diarrhea; in some cases - loss or change in taste sensations, dryness of the oral mucosa.

From the cardiovascular system: arrhythmias, orthostatic hypotension (weakens after reducing the dose of Madopar), arterial hypertension.

From the respiratory system: rhinitis, bronchitis.

From the hematopoietic system: rarely - hemolytic anemia, transient leukopenia, thrombocytopenia.

Dermatological reactions: rarely - itching, rash.

From the laboratory parameters: sometimes - a transient increase in the activity of liver transaminases, alkaline phosphatase, an increase in gamma-glutamyl transpeptidase, an increase in blood urea nitrogen, a change in the color of urine to red, darkening when standing.

From the body as a whole: anorexia.

Other: febrile infection.

Drug interactions

Pharmacokinetic interaction

When used concomitantly, trihexyphenidyl (an anticholinergic drug) reduces the rate, but not the extent, of absorption of levodopa. The administration of trihexyphenidyl together with Madopar GSS “125” does not affect the pharmacokinetics of levodopa.

When antacids are used simultaneously with Madopar GSS, the degree of absorption of levodopa is reduced by 32%.

Ferrous sulfate reduces the plasma Cmax and AUC value of levodopa by 30-50%; these changes are in some cases clinically significant.

Metoclopramide increases the rate of absorption of levodopa.

Levodopa does not interact pharmacokinetically with bromocriptine, amantadine, selegiline and domperidone.

Pharmacodynamic interaction

Neuroleptics, opiates and antihypertensive drugs containing reserpine suppress the effect of Madopar.

If it is necessary to prescribe Madopar to patients receiving irreversible non-selective MAO inhibitors, at least 2 weeks must pass from the moment of stopping the MAO inhibitor before starting to take Madopar.

Selective MAO type B inhibitors (including selegiline, rasagiline) and selective MAO type A inhibitors (moclobemide) can be prescribed during treatment with Madopar. It is recommended to adjust the dose of levodopa depending on the patient's individual needs in terms of effectiveness and tolerability. The combination of MAO type A and MAO type B inhibitors is equivalent to taking a non-selective MAO inhibitor, therefore such a combination should not be prescribed simultaneously with Madopar.

Madopar® should not be prescribed simultaneously with sympathomimetics (adrenaline, norepinephrine, isoproterenol, amphetamine), since levodopa can potentiate their effect. If concomitant use is necessary, carefully monitor the cardiovascular system and, if necessary, reduce the dose of sympathomimetics.

The combined use of the drug with other antiparkinsonian drugs (anticholinergics, amantadine, dopamine agonists) is possible, and not only the desired but also the undesirable effects may be enhanced. It may be necessary to reduce the dose of Madopar or another drug.

When using Madopar simultaneously with a COMT inhibitor, it may be necessary to reduce the dose of Madopar. If treatment with Madopar is started, anticholinergic drugs should not be discontinued abruptly, since levodopa does not take effect immediately.

Since a patient receiving Madopar® may experience fluctuations in blood pressure and arrhythmias during halothane anesthesia, Madopar should be discontinued 12-48 hours before surgery.

Levodopa may affect laboratory results of catecholamines, creatinine, uric acid and glucose, and a false-positive Coombs test result is possible.

In patients receiving Madopar®, taking the drug simultaneously with a protein-rich meal may interfere with the absorption of levodopa from the gastrointestinal tract.