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One tablet dispersible contains: active substances: levodopa 100 mg benserazide 25 mg (as benserazide hydrochloride 28.5 mg) Excipients: . Citric acid anhydrous, maize starch pregelatinised, microcrystalline cellulose, magnesium stearate One capsule contains: active substances: levodopa 100 mg benserazide 25 mg (as benserazide hydrochloride 28.5 mg) excipients:microcrystalline cellulose, talc, povidone, magnesium stearate sheath: cap capsules andriol cycle – indigo dye, titanium dioxide, gelatin; . capsule enclosure – colorant iron red oxide, titanium dioxide, gelatin One tablet contains: active substance: Levodopa 200 mg benserazide 50 mg (as benserazide hydrochloride, 57 mg) Excipients: mannitol, dicalcium phosphate, microcrystalline cellulose, corn starch, pregelatinized starch, crospovidone ., ethyl cellulose, colorant red iron oxide, silicon dioxide colloidal (anhydrous), sodium docusate, magnesium stearate One capsule modified release (GSS capsule – hydrodynamically balanced system) contains: active substance: levodopa 100 mg benserazide 25 mg (as benserazide hydrochloride 28.5 mg) excipients: hypromellose, hydrogenated vegetable oil, calcium hydrogen phosphate, mannitol, povidone, talc, magnesium stearate sheath: cap capsules – indigo dye, a dye yellow iron oxide, titanium dioxide, gelatin; capsule body – indigo dye, titanium dioxide, gelatin.

Description Tablets dispersible: cylindrical, flat on both sides of the tablet with a beveled edge, white or almost white, odorless or with a faint odor, slightly marble, engraved with «ROCHE 125″ on one side of the tablet and a fault line on the other side. The diameter of the tablets of approximately 11 mm; . thickness of about 4.2 mm Capsule: hard gelatine capsule; body pinkish flesh-colored, opaque; cap light blue, opaque; on the capsule there is an inscription «ROCHE» black. The contents of capsules – a fine granular powder, sometimes skomkovavshiysya, light beige color with a subtle scent. Tablets:cylindrical, flat tablets with bevelled edge, pale red with small patches, with barely perceptible odor; on one side of the risk of a cruciform tablets, engraved «ROCHE» and hexagon; tablet on the other side – the risk of the cruciform. Tablet diameter 12.6-13.4 mm; thickness of 3.4 mm. Capsules modified release: hard gelatin capsule; body light blue, opaque; lid dark green, opaque; on the capsule is marked «ROCHE» ink rusty-red. The contents of capsules – a fine granular powder, sometimes skomkovavshiysya, white or slightly yellowish color, with a subtle fragrance.

Pharmacotherapeutic group
antiparkinsonian agent (dopamine precursor to + peripheral decarboxylase inhibitor)

ATX Code [N04BA]

Pharmacological properties Pharmacodynamics The combined agent for treating Parkinson’s disease and syndrome “Restless legs” Parkinson’s Disease Dopamine, which is a neurotransmitter in the brain of patients with Parkinson formed in the basal ganglia in insufficient quantities. L-dopa or L-DOPA (3,4 – digidrofenilalanin) is the metabolic precursor of dopamine. Unlike dopamine Levodopa penetrates well through the blood brain barrier. After Levodopa penetrates the central nervous system, it is converted into dopamine via the aromatic amino acid decarboxylase. After oral levodopa rapidly decarboxylated to dopamine in the cerebral and in extracerebral tissues. As a result, most of the levodopa reaches the basal ganglia, and peripheral dopamine often causes side effects. Therefore, you must block extracerebral decarboxylation of levodopa. What is achieved by the simultaneous administration of levodopa and benserazide, a peripheral decarboxylase inhibitor. Madopar is a combination of these substances in an optimum ratio of 4: 1, and is as effective as higher doses of levodopa.

Syndrome “Restless legs”
The exact mechanism of action is not known, but the dopaminergic system plays an important role in the pathogenesis syndrome “Restless Legs.”

Pharmacokinetics Absorption Capsules Madopar ‘125’ and tablets Madopar “250” Levodopa is mainly absorbed in the upper small intestine. The time to reach maximum concentration of levodopa is 1 hour after taking the capsules or tablets. Capsules Madopar “125” and tablets Madopar “250” bioequivalent. Maximum concentrations of levodopa in the plasma and extent of absorption of levodopa (AUC) increased proportionally with dose (in a range of doses of levodopa of from 50 to 200 mg). food intake reduces the rate and extent of absorption of levodopa. When assigning capsules or tablets postprandial maximum concentration of levodopa is reduced by 30% in the plasma and later achieved. The extent of absorption of levodopa is reduced by 15%. The absolute bioavailability of levodopa capsules Madopar ‘125’ and tablets Madopar ‘250’ is 98% (from 74% to 112%). Madopar fast tablet / dispersible / “125” The pharmacokinetic profiles of levodopa after administration of dispersible tablets are similar to those after taking Madopar capsules “125” or Madopar “250” tablets, but the time to reach maximum concentration tends to decrease. Suction Parameters dispersible tablets in patients less variable. Madopar GSS ‘125’, the capsule with the modified release Madopar GSS “125” has a different pharmacokinetic properties than the aforementioned release form. The active substances are released slowly into the stomach.The maximum plasma concentration by 20-30% smaller than capsules Madopar “125” and tablets Madopar “250” and is achieved through 3 hours after administration. Dynamics plasma concentration is characterized by more prolonged period of “half-life” (the time interval during which the plasma concentration is greater than or equal to half of the maximum) than the capsules Madopar “125” and tablets Madopar “250”, indicating that the continuously modified release. The bioavailability of the drug Madopar GSS “125” is 50-70% of the bioavailability of the capsules Madopar ‘125’ and tablets Madopar ‘250’ and is independent of food intake. Food intake and no effect on the maximum concentration of levodopa, which is achieved by 5 hours after administration Madopar GSS “125”.

Levodopa passes the blood-brain barrier by a saturable transport system and does not bind to plasma proteins. The volume of distribution is 57 liters. The area under the curve “concentration-time» (AUC) for levodopa CSF is 12% of that in plasma.
Benserazide at therapeutic doses do not penetrate the blood-brain barrier. It accumulates mainly in the kidneys, lungs, small intestine and liver.

Levodopa is metabolized by two main (decarboxylation and O-methylation) and two side paths (transamination and oxidation).
Decarboxylase of aromatic amino acids converts levodopa into dopamine. The major end products of this pathway are exchange dihydroxyphenylacetic acid and homovanillic.
Catechol-o-methyl transferase methylates levodopa to form a 3-O-methyldopa. The half-life of the main metabolite in plasma is 15-17 hours, and in patients receiving therapeutic doses of Madopar, there is its accumulation.
The decrease in the peripheral decarboxylation of levodopa, with a joint appointment with benserazide, resulting in higher plasma concentrations of levodopa and 3-O- methyldopa and lower plasma concentrations of catecholamines (dopamine, norepinephrine) and fenolkarboksilnyh acid (homovanillic acid digidrofeniluksusnoy acid).
In the liver and intestinal mucosa benserazide hydroxylated to form trihydroxy benzylhydrazine. This metabolite is a potent inhibitor of aromatic amino acid decarboxylase.

of peripheral decarboxylase inhibition of levodopa half-life is 1.5 hours. The clearance of levodopa from plasma is about 430 ml / min.
Benserazide almost entirely eliminated by metabolism. Metabolites are mainly in the urine (64%) and, to a lesser extent in the feces (24%).

Pharmacokinetics in specific patient populations Patients with renal and hepatic insufficiency Data on the pharmacokinetics of levodopa in patients with renal and hepatic insufficiency are absent. Elderly patients (65-78 years) in elderly patients (65 – 78 years) with Parkinson’s disease elimination half-life and AUC levodopa is increased by 25%, which is not clinically significant change and does not affect the dosing regimen.

Indications Parkinson’s disease:
Madopar is indicated for the treatment of Parkinson’s disease.
Madopar fast tablet / dispersible / “125” – a special formulation for patients with dysphagia or akinesia in the early morning and in the afternoon, or the phenomena of “exhaustion of a single dose effect” or . “increase the latent period before the onset of the clinical effect of the drug”
Madopar GSS “125” is shown in all types of action of levodopa fluctuations (namely “peak dose dyskinesia” and “end of dose phenomenon”, for example, in the stillness of the night).

The syndrome of “restless legs”:
Madopar is indicated for the treatment of “restless legs” syndrome, including:


  • idiopathic syndrome of “restless legs”
  • syndrome of “restless legs” in patients with chronic renal failure who are on dialysis.Contraindications:
    Hypersensitivity to levodopa, benserazide or to any other component of the drug.
    Decompensated dysfunction of the endocrine organs, liver or kidney problems (with the exception of patients with the syndrome of “restless legs” on dialysis), diseases of the cardiovascular system in the stage of decompensation, mental illness with psychotic component , angle-closure glaucoma.
    Madopar should not be used in combination with non-selective monoamine oxidase inhibitors (MAOIs), or with a combination of MAO-a inhibitors and MAO-B.
    age younger than 25 years.
    Pregnancy and lactation. Madopar is contraindicated in women of childbearing potential not using reliable methods of contraception (see. “Pregnancy and lactation”).

    Pregnancy and lactation
    Madopar absolutely contraindicated during pregnancy and women of childbearing age who are not using reliable methods of contraception because of a possible breach of skeletal development in the fetus.
    If during treatment arises pregnancy, the drug should be canceled in accordance with the recommendations of the attending physician.
    If necessary, Madopar taking the drug during lactation, breast-feeding should be discontinued due to lack of reliable data on the penetration of benserazide passes into breast milk. We can not exclude the risk of improper skeletal development in the newborn.

    Dosage and administration
    Capsules (Madopar ‘125’ or GSS Madopar ‘125’) should be swallowed whole without chewing. The capsules Madopar GSS “125” can not be opened before use, otherwise the effect of the modified release of the active substance is lost.
    Tablets (Madopar ‘250’) can crush to facilitate swallowing.
    Tablets dispersible (Madopar fast tablet / dispersible / “125”) to be dissolved in a quarter cup water (25-50 ml); the tablet is completely dissolved within a few minutes to produce a suspension of a milky white color, which should be no later than half an hour after the dissolution of the tablet. As can be quickly formed precipitate, before receiving the recommended mix the solution.

    inside is not less than 30 minutes before or 1 hour after a meal.

    The standard dosing regimen
    Treatment should be started gradually, individually selecting dose to optimum effect.

    Initial therapy
    at an early stage of Parkinson’s disease, it is recommended to start treatment with Madopar receiving 62.3 mg (50 mg levodopa + 12.5 mg benserazide) 3-4 times a day. When portability scheme initial metering dose should be slowly increased depending on the response of the patient.
    The optimum effect is usually achieved at a daily dose of 300-800 mg of levodopa + 75-200 mg benserazide received at three or more steps. To achieve optimal effect may take 4 to 6 weeks. If necessary, the daily dose further increase this should be done at intervals of 1 month.

    Maintenance therapy
    The average maintenance dose -. 125 mg (100 mg of levodopa + 25 mg benserazide) 3-6 times a day
    . The number of receptions (at least three) and their distribution throughout the day must provide optimum effect
    capsule Madopar can be replaced to optimize the effect of ” 125 “and the tablet Madopar ‘250’ on the fast Madopar tablets / dispersible /” 125 “or capsules Madopar GSS” 125 “.

    The syndrome of “restless legs”
    maximum permissible dose a day -. 500 mg of Madopar (400 mg levodopa + 100 mg benserazide)
    . 1 hour before sleep, with a small amount of food idiopathic syndrome of “restless legs” violations of sleep is recommended to assign the capsule Madopar ‘125 . “or tablets Madopar ‘250’ Initial dose: 62.5 mg (50 mg levodopa + 12.5 mg benserazide) -125 mg (100 mg of levodopa + 25 mg benserazide) Madopar. With little effect should increase the dose to 250 mg (200 mg of levodopa + 50 mg benserazide) Madopar. Idiopathic syndrome of “restless legs” with impaired sleep and sleep initial dose: 1 capsule of Madopar GSS “125” and 1 capsule of Madopar ‘125’ 1 an hour before bedtime. With little effect it is recommended to increase the dose of Madopar GSS “125” to 250 mg (2 capsules). Idiopathic syndrome of “restless legs” with impaired sleep and sleep, as well as violations during the day Extras: 1 tablet dispersible or 1 capsule of Madopar ‘125’ , the maximum daily dose – 500 mg (400 mg of levodopa + 100 mg benserazide) Madopar. The syndrome of “restless legs” in patents with chronic renal failure receiving dialysis 125 mg of Madopar (1 tablet dispersible or 1 capsule of Madopar ‘125’) 30 minutes before dialysis.


    Special dosage instructions

    Parkinson’s disease
    Madopar may be combined with other antiparkinsonian agents, as further treatment may be necessary to reduce the dose of other medications or their gradual abolition.
    Madopar fast tablet / dispersible / “125” – a special formulation for patients with dysphagia or akinesia andriol cycle in the early morning hours and in the afternoon, or the phenomena of “exhaustion of the effect of a single dose” or “increase in the latent period before the onset of the clinical effect of the drug.”
    If the patient during the day, there are marked motor fluctuations (the phenomenon of “exhaustion of a single dose effect,” a phenomenon “vklyucheniya- off “), recommended a more frequent reception of correspondingly lower individual doses, or – what is preferable -. use Madopar GSS” 125 ”
    Go to Madopar GSS” 125 “is better to start with a morning dose, while maintaining daily dose and dosage regimen of Madopar ‘125’ or Madopar ‘250’.
    After 2-3 days, gradually increase the dose by approximately 50%. Patients should be warned that his condition may temporarily deteriorate. Because of its properties farmakokinetichesih Madopar GSS “125” begins to act a little bit later. Clinical effect can be achieved more quickly by appointing Madopar GSS “125” together with capsules Madopar ‘125’ or dispersible tablets. This may be particularly useful in the case of the first morning dose, which should be slightly higher than the next. Individual dose of Madopar GSS “125” must be chosen carefully and slowly, between changes in the dose interval should be not less than 2-3 days.
    In patients with nocturnal symptoms positive effect could be achieved by gradually increasing the evening dose GSS Madopar ‘125’ and 250 mg (2 capsules) at bedtime.
    to eliminate the pronounced effect of Madopar GSS “125” (dyskinesia) more effectively increase the interval between doses, than the reduction of a single dose.
    If Madopar GSS “125” is not sufficiently effective, it is recommended vernugsya to continue treatment preparations Madopar ‘125’ , Madopar ‘250’ and Madopar fast tablet / dispersible / “125”.
    In patients with renal insufficiency, mild to moderate dose adjustment is required.
    Madopar is well tolerated in patients receiving hemodialysis.
    In the long-term treatment may cause “hardening” episodes, “depletion phenomenon”, the phenomenon of “on-off”. When episodes “pour” and “depletion phenomenon” resort to crushing dose (single dose reduction or a reduction of the dosing interval of the drug), and the appearance of the phenomenon of “on-off” – single dose to increase with a decrease in the number of receptions. Later, you can try again to increase the dose to enhance the effect of the treatment.

    The syndrome of “restless legs”
    To eliminate the growth of symptoms “restless legs” syndrome (early appearance during the day, increasing the severity and the involvement of other body parts) daily dose should not exceed the recommended maximum dose – 500 mg (400 mg levodopa benserazide 100 mg) Madopar.
    With an increase in clinical symptoms of levodopa dose should be reduced or phased out levodopa therapy and appoint another.

    Side effects Blood system: rare cases of hemolytic anemia, transient leukopenia, thrombocytopenia. In patients for a long time taking levodopa is recommended to periodically monitor blood count, liver and kidney function. On the part of the gastrointestinal tract: nausea, vomiting, diarrhea, some cases of loss of or changes in taste, dryness of the oral mucosa. On the part of the skin appendages: rarely – pruritus, rash. cardio-vascular system: arrhythmia, orthostatic hypotension (weakened after reducing the dose of Madopar), arterial hypertension. from the nervous system and psychiatric: agitation, anxiety, insomnia, hallucinations, delusions, temporary disorientation (especially in the elderly patients and in patients who have observed these symptoms in the disease), depression, headache, dizziness, in the later stages of treatment occasionally – spontaneous movements (such as chorea or athetosis), episodes of “hardening” the weakening effect of the end of the period, the dose of action ( the phenomenon of “exhaustion”), the phenomenon of “on-off”, pronounced sleepiness, episodes of sudden sleepiness, increased manifestations of the syndrome of “restless legs.” On the part of the body to flail: febrile infection, rhinitis, bronchitis, Laboratory findings: sometimes – transient increase in liver transaminases and alkaline phosphatase, increased gamma-glutamiltranspepgidazy, increased blood urea nitrogen, changes in urine color to red, darkening on standing. On the part of the body as a whole: anorexia

    Overdose Symptoms mentioned in section “Adverse reactions”, but in a more pronounced form: the part of the cardiovascular system (arrhythmias), psychiatric (mental confusion, insomnia), gastro-intestinal tract (nausea and vomiting), abnormal involuntary . motion When taking capsules with modified release (GSS Madopar ‘125’) the occurrence of overdose symptoms may occur later due to delayed absorption of the active substance in the stomach. Therapy: it is necessary to control the vital functions. Symptomatic therapy:. A respiratory analeptic, antiarrhythmics, where appropriate, – neuroleptics When using capsules with modified release of the active substances (GSS Madopar ‘125’) should prevent further absorption of the drug.

    Interaction with other medicinal products The pharmacokinetic interactions Trihexyphenidyl (anticholinergic medication) reduces the rate but not the extent of absorption of levodopa. Purpose trihexyphenidyl with Madopar GSS “125” did not affect the pharmacokinetics of levodopa. Antacids reduce the extent of absorption of levodopa by 32% in the appointment with Madopar GSS “125”. Ferric sulfate reduces AUC and maximal concentrations of levodopa in the plasma of 30-50%, which is clinically significant changes in some, but not all patients. Metoclopramide increases the rate of absorption of levodopa. levodopa does not enter into the pharmacokinetic interaction with bromocriptine, amantadine, selegiline and domperidone.

    Pharmacodynamic interactions Neuroleptics, opioids and antigipertentvnye medications containing reserpine inhibit the action of Madopar. MAO inhibitors If Madopar is prescribed to patients receiving irreversible non-selective MAO inhibitors, that of discontinuation of MAO inhibitor before you start taking Madopar must be at least two weeks (see. Section “Contraindications”). However, selective MAO-B inhibitors (eg, selegiline or rasagiline) and selective inhibitors of MAO-A (such as moclobemide) can be administered to patients receiving Madopar. It is recommended to adjust the dose of levodopa depending on the individual patient’s needs in terms of efficacy and tolerability. The combination of MAO-A inhibitors and MAO-B is equivalent to receiving non-selective MAO inhibitors, therefore this combination should not be given concurrently with Madopar.


    Sympathomimetics (epinephrine, norepinephrine, isoproterenol, amphetamine). Madopar should not be administered concurrently with sympathomimetics as levodopa may potentiate their action. If concomitant use is still required, it is very important the careful monitoring of the state of the cardiovascular system and, if necessary, dose reduction of sympathomimetics.

    Antiparkinsonian agent. Possibly a combined use of the drug with other antiparkinsonian agents (anticholinergics, amantadine, dopamine agonists), but it may enhance the desirable and undesirable effects.You may need to reduce the dose of Madopar or the other drug. If the inhibitor is added to the treatment of catechol-o-methyl transferase / COMT /, you may need to reduce the dose of Madopar. At the start of Madopar therapy, anticholinergic drugs should not be stopped abruptly, because levodopa begins to act immediately.

    Levodopa may affect the results of laboratory determination of catecholamines, creatinine, uric acid and glucose, possible false positive Coombs test.
    In patients treated with Madopar, the drug simultaneously with the high-protein diet may impair the absorption of levodopa from the gastrointestinal tract. General anesthesia with halothane. Receiving Madopar must be canceled for 12 – 48 hours before the surgery, since the patient receiving Madopar during halothane anesthesia may be fluctuations in blood pressure and arrhythmia.

    In patients with hypersensitivity to the drug can develop appropriate responses.
    In patients with open-angle glaucoma is recommended to regularly measure the intraocular pressure, because theoretically levodopa may increase intraocular pressure.
    Side effects from the gastrointestinal tract, possible in the initial stages of treatment, can significantly extent eliminated if taking Madopar with a small amount of food or liquid, as well as if you increase the dose slowly.
    in the course of treatment is necessary to monitor liver and kidney function, blood count.
    Patients with diabetes need to frequently monitor blood glucose levels and correct dose of hypoglycemic drugs.
    When the need for surgery with anesthesia sheathe Madopar therapy should be continued up to the operation, with the exception of general anesthesia with halothane. As a patient receiving Madopar during halothane anesthesia may cause fluctuations in blood pressure and arrhythmia, taking Madopar should be discontinued for 12-48 hours prior to surgery. Mosley operations resume andriol cycle treatment, gradually increasing the dose to the previous level.
    Madopar can not cancel sharply. Abrupt withdrawal of the drug may lead to a “neuroleptic malignant syndrome” (fever, muscle stiffness, and possible mental changes and an increase in serum creatine phosphokinase), which may take the form of a life-threatening. If you have any of these symptoms the patient should be under medical supervision (if need to be hospitalized) and receive appropriate symptomatic treatment. This may include the re-appointment of Madopar after appropriate patient assessment.
    Depression can be a clinical manifestation of underlying disease (Parkinsonism, a syndrome of “restless legs”), and may occur on the background of Madopar therapy. The patient should be closely monitored in terms of the possible appearance of psychiatric side effects. The ability of drug abuse addiction and Some patients with observed appearance of Parkinson’s disease and cognitive disorders resulting from uncontrolled application of increasing doses of the drug, despite a doctor’s recommendation and a significant excess of therapeutic doses.

    Effect on driving vehicles and working with machines and mechanisms
    In the event of drowsiness, sudden episodes of drowsiness should avoid driving or using machinery. When these symptoms should consider dose reduction or discontinuation.

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