Levodopa + Benserazide capsules 200 + 50mg, No. 100

According to the instructions, Levodopa / Benserazide is prescribed for the treatment of Parkinson's disease.

Inside , if possible, at least 30 minutes before or 1 hour after meals.

Treatment begins with a small dose, gradually increasing the dose for each patient individually, until a therapeutic effect is achieved. It is necessary to avoid high doses for the simultaneous administration of the drug.

The dosing guidelines given below should be considered as general guidelines.

For patients who have not previously taken levodopa, an initial dose of 50 mg of levodopa / 12.5 mg of benserazide is prescribed 2Ц4 times a day (from 100Ц200 mg of levodopa / 25Ц50 mg of benserazide per day). If well tolerated, the dose is increased by 50Ц100 mg of levodopa / 12.5Ц25 mg of benserazide every 3 days until a therapeutic effect is achieved.

Further (after the initial) dose selection is carried out with a frequency of 1 time per month. Usually, the therapeutic effect is noted already when taking 200-400 mg of levodopa / 50-100 mg of benserazide per day.

The maximum daily dose is 800 mg levodopa / 200 mg benserazide.

The daily dose should be divided into 4 or more doses. The frequency of reception should be distributed so as to ensure the optimal therapeutic effect.

If undesirable reactions occur, it is necessary to either stop increasing the dose or reduce the daily dose.

The optimal therapeutic effect is usually achieved when taking 300-800 mg of levodopa / 100-200 mg of benserazide.

Patients who have previously taken levodopa should start taking Levodopa / Benserazide-Teva 12 hours after stopping levodopa.

The dose of the drug should be approximately 20% of the previous dose of levodopa in order to maintain the already achieved therapeutic effect. If necessary, the dose is increased according to the scheme described for patients who have not previously taken levodopa.

Patients who have previously taken levodopa in combination with an aromatic L-amino acid decarboxylase inhibitor should start taking Levodopa / Benserazide-Teva 12 hours after discontinuing levodopa in combination with an aromatic L-amino acid decarboxylase inhibitor. To minimize the decrease in the already achieved therapeutic efficacy, it is necessary to discontinue the previous therapy at night and start taking the drug Levodopa / Benserazide-Teva the next morning. If necessary, the dose is increased according to the scheme described for patients who have not previously taken levodopa.

For patients who have previously taken other antiparkinsonian drugs, the drug Levodopa / Benserazide-Teva is possible. As soon as the therapeutic effect of the drug Levodopa / Benserazide-Teva becomes obvious, it is necessary to reconsider the treatment regimen and reduce or cancel the alternative drug.

Dosing regimens in special cases

Patients who experience severe motor fluctuations are advised to take the daily dose more than 4 times a day without changing the daily dose itself.

In old age, dose increases should be slower.

Experience with children and adolescents is limited.

With renal and hepatic insufficiency of mild and moderate severity, dose adjustment is not required.

If spontaneous movements such as chorea or athetosis appear in the later stages of treatment, it is necessary to reduce the dose.

With long-term use of the drug, the appearance of episodes of 'freezing', weakening of the effect by the end of the dose period and the phenomenon of 'on-off' can be eliminated or significantly reduced by lowering the dose or using the drug at a lower dose, but more often. Subsequently, you can increase the dose again to enhance the effect of the treatment.

If undesirable reactions from CVS appear, it is necessary to reduce the dose.

Active ingredients:

levodopa - 200 mg

benserazide hydrochloride - 57 mg, which corresponds to the content of benserazide - 50 mg

Excipients: mannitol - 178.3 mg, microcrystalline cellulose - 9.9 mg, pregelatinized corn starch - 37.4 mg, calcium hydrogen phosphate (anhydrous) - 15.94 mg, povidone K25 - 22 mg, crospovidone (type A) - 16.5 mg, colloidal silicon dioxide - 1.42 mg, iron dye red oxide (E172) - 0.54 mg, magnesium stearate - 11 mg.

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

• severe dysfunction of the organs of the endocrine system;

• glaucoma;

• severe liver dysfunction;

• severe renal impairment;

• severe dysfunction of the CVS;

• endogenous and exogenous psychoses;

• simultaneous reception with non-selective MAO inhibitors, a combination of MAO type A and MAO type B inhibitors (which is equivalent to non-selective MAO inhibition);

• women of childbearing age who do not use reliable methods of contraception;

• pregnancy;

• breastfeeding period;

• age up to 25 years.

Levodopa / Benserazide is a drug used for Parkinson's disease.

The tablets are pink in color with slight marbling, round, flat, with a bevel, on both sides of the tablet there is a cruciform mark, on one side there is an engraving 'B' and 'L' in two sections of a cruciform mark.

Clinical pharmacology

Levodopa / benserazide is a combined antiparkinsonian drug containing a dopamine precursor and an inhibitor of peripheral decarboxylase of aromatic L-amino acids.

In parkinsonism, the neurotransmitter dopamine is produced in the basal nuclei in insufficient quantities.

Replacement therapy is carried out by using levodopa, a direct metabolic precursor of dopamine.

Most of levodopa is converted to dopamine in peripheral tissues (intestines, liver, kidneys, heart, stomach), which is not involved in the implementation of the antiparkinsonian effect, since peripheral dopamine poorly penetrates the BBB, and is also responsible for most of its unwanted reactions.

Blocking the extracerebral decarboxylation of levodopa is highly desirable.

This is achieved by the simultaneous administration of levodopa and benserazide - an inhibitor of peripheral decarboxylase of aromatic L-amino acids, which reduces the formation of dopamine in peripheral tissues, which indirectly leads to an increase in the amount of levodopa entering the central nervous system - on the one hand and to a decrease in the manifestations of undesirable reactions of levodopa - with other.

The combination of these substances in a 4: 1 ratio is as effective as high doses of levodopa.

Interaction

Pharmacokinetic interactions

With the simultaneous use of trihexyphenidil (m-anticholinergic), there is a decrease in the rate, but not the degree of absorption of levodopa.

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

With simultaneous use with antacids, the degree of absorption of levodopa / benserazide is reduced by 32%.

Metoclopramide increases the rate of absorption of levodopa.

Pharmacodynamic interactions

Antipsychotics, opioids and antihypertensive drugs containing reserpine suppress the effect of levodopa / benserazide. The lowest doses of these drugs are used if necessary.

With simultaneous use, pyridoxine can reduce the antiparkinsonian effect of levodopa / benserazide.

Levodopa / benserazide should not be used with non-selective MAO inhibitors. If it is necessary to use levodopa / benserazide in patients receiving irreversible nonselective MAO inhibitors, at least 2 weeks should elapse from the moment the MAO inhibitor is discontinued until the start of admission. Premature (within 2 weeks after discontinuation) use of levodopa / benserazide for a non-selective MAO inhibitor (for example, tranylcypromine) can cause a hypertensive crisis.

Selective type B MAO inhibitors (including selegiline, rasagiline) and type A selective MAO inhibitors (moclobemide) can be used during treatment with levodopa / benserazide. In certain cases, selegiline can increase the effect of levodopa / benserazide without causing dangerous interactions. At the same time, it is recommended to adjust the dose of levodopa / benserazide, depending on the individual needs of the patient in terms of therapeutic efficacy and tolerability.

The combination of selective MAO inhibitors type B and selective MAO inhibitors type A is equivalent to taking a non-selective MAO inhibitor, therefore such a combination should not be used with levodopa / benserazide.

If it is necessary to use antihypertensive drugs during treatment with levodopa / benserazide, it is necessary to take into account the possibility of developing orthostatic hypotension.

Levodopa / benserazide potentiates the action of sympathomimetics (epinephrine, norepinephrine, isoproterenol, amphetamine), therefore, such a combination of drugs should not be used. If the simultaneous reception is still required, then the state of the CVS should be carefully monitored and, if necessary, the dose of sympathomimetics should be reduced.

It is possible to use levodopa / benserazide with other antiparkinsonian drugs (anticholinergic drugs, amantadine, dopamine receptor agonists), while not only desirable, but also undesirable effects may increase. It may be necessary to reduce the dose of levodopa / benserazide or another drug. With the simultaneous use of levodopa / benserazide with a catechol-O-methyltransferase inhibitor, it may be necessary to reduce the dose of levodopa / benserazide.

Since a patient receiving levodopa / benserazide may experience fluctuations in blood pressure and arrhythmias during halothane anesthesia, it is necessary to stop taking the drug 12Ц48 hours before surgery.

Protein-rich foods may decrease the therapeutic effect of levodopa / benserazide.

Levodopa / benserazide can affect the results of laboratory tests of catecholamines, creatinine, uric acid, glucose, alkaline phosphatase, bilirubin. An increase in the concentration of urea and creatinine in the blood, a false negative reaction to glucose in the urine using the glucose oxidase method, and a false positive result of the Coombs test can be determined.

Indications for use:

According to the instructions, Levodopa / Benserazide is prescribed for the treatment of Parkinson's disease.

Method of administration and dosage:

Inside , if possible, at least 30 minutes before or 1 hour after meals.

Treatment begins with a small dose, gradually increasing the dose for each patient individually, until a therapeutic effect is achieved. It is necessary to avoid high doses for the simultaneous administration of the drug.

The dosing guidelines given below should be considered as general guidelines.

For patients who have not previously taken levodopa, an initial dose of 50 mg of levodopa / 12.5 mg of benserazide is prescribed 2Ц4 times a day (from 100Ц200 mg of levodopa / 25Ц50 mg of benserazide per day). If well tolerated, the dose is increased by 50Ц100 mg of levodopa / 12.5Ц25 mg of benserazide every 3 days until a therapeutic effect is achieved.

Further (after the initial) dose selection is carried out with a frequency of 1 time per month. Usually, the therapeutic effect is noted already when taking 200-400 mg of levodopa / 50-100 mg of benserazide per day.

The maximum daily dose is 800 mg levodopa / 200 mg benserazide.

The daily dose should be divided into 4 or more doses. The frequency of reception should be distributed so as to ensure the optimal therapeutic effect.

If undesirable reactions occur, it is necessary to either stop increasing the dose or reduce the daily dose.

The optimal therapeutic effect is usually achieved when taking 300-800 mg of levodopa / 100-200 mg of benserazide.

Patients who have previously taken levodopa should start taking Levodopa / Benserazide 12 hours after stopping levodopa.

The dose of the drug should be approximately 20% of the previous dose of levodopa in order to maintain the already achieved therapeutic effect. If necessary, the dose is increased according to the scheme described for patients who have not previously taken levodopa.

Patients who have previously taken levodopa in combination with an aromatic L-amino acid decarboxylase inhibitor should start taking Levodopa / Benserazide 12 hours after discontinuing levodopa in combination with an aromatic L-amino acid decarboxylase inhibitor. To minimize the decrease in the already achieved therapeutic efficacy, it is necessary to discontinue the previous therapy at night and start taking the drug Levodopa / Benserazide-Teva the next morning. If necessary, the dose is increased according to the scheme described for patients who have not previously taken levodopa.

Patients who have previously taken other antiparkinsonian drugs may take Levodopa / Benserazide. As soon as the therapeutic effect of the drug Levodopa / Benserazide becomes obvious, it is necessary to reconsider the treatment regimen and reduce or cancel the alternative drug.

Dosing regimens in special cases

Patients who experience severe motor fluctuations are advised to take the daily dose more than 4 times a day without changing the daily dose itself.

In old age, dose increases should be slower.

Experience with children and adolescents is limited.

With renal and hepatic insufficiency of mild and moderate severity, dose adjustment is not required.

If spontaneous movements such as chorea or athetosis appear in the later stages of treatment, it is necessary to reduce the dose.

With long-term use of the drug, the appearance of episodes of 'freezing', weakening of the effect by the end of the dose period and the phenomenon of 'on-off' can be eliminated or significantly reduced by lowering the dose or using the drug at a lower dose, but more often. Subsequently, you can increase the dose again to enhance the effect of the treatment.

If undesirable reactions from CVS appear, it is necessary to reduce the dose.

Contraindications

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

• severe dysfunction of the organs of the endocrine system;

• glaucoma;

• severe liver dysfunction;

• severe renal impairment;

• severe dysfunction of the CVS;

• endogenous and exogenous psychoses;

• simultaneous reception with non-selective MAO inhibitors, a combination of MAO type A and MAO type B inhibitors (which is equivalent to non-selective MAO inhibition);

• women of childbearing age who do not use reliable methods of contraception;

• pregnancy;

• breastfeeding period;

• age up to 25 years.

special instructions

Adverse reactions from the gastrointestinal tract, which are possible at the initial stage of treatment, are largely eliminated if Levodopa / Benserazide is taken with a small amount of food or liquid, as well as a slower increase in the dose. The use of the drug Levodopa / Benserazide is not recommended for the treatment of iatrogenic extrapyramidal syndrome and Huntington's chorea.

In patients with a history of gastrointestinal ulcers, seizures and osteomalacia, it is necessary to regularly monitor the corresponding indicators. In the course of treatment, the indicators of liver, kidney function, blood count should be monitored. In patients with a history of ischemic heart disease, myocardial infarction, cardiac arrhythmias, it is necessary to regularly monitor the ECG.

Patients with a history of orthostatic hypotension should be monitored by a physician, especially at the beginning of treatment.

In patients with diabetes mellitus, blood glucose levels should be monitored frequently and the dose of oral hypoglycemic drugs should be adjusted.

When using the drug Levodopa / Benserazide, cases of sudden onset of sleep have been reported. Patients should be advised of the possibility of sudden falling asleep.

When using the drug Levodopa / Benserazide, the risk of developing malignant melanoma increases, and therefore the use of the drug in patients with malignant melanoma, incl. history is not recommended. The use of the drug Levodopa / Benserazide, especially in high doses, increases the risk of developing compulsive disorders.

Before general anesthesia, Levodopa / Benserazide should be taken for as long as possible. An exception is halothane anesthesia. Since the patient receiving the drug may experience fluctuations in blood pressure and arrhythmias during halothane anesthesia, the drug should be discontinued 12-24 hours before surgery. After surgery, treatment is resumed, gradually increasing the dose.

ѕрепарат Ћеводопа/Ѕенсеразид нельз¤ отмен¤ть резко. –езка¤ отмена препарата может привести к синдрому отмены (повышение температуры тела, ригидность мышц, а также возможные психические изменени¤ и повышение активности  ‘  в сыворотке крови) или акинетическим кризам, которые могут прин¤ть угрожающую жизни форму. ѕри возникновении таких симптомов пациент должен находитьс¤ под наблюдением врача (при необходимости должен быть госпитализирован) и получать соответствующую терапию, котора¤ может включать повторное применение препарата Ћеводопа/Ѕенсеразид

?епресси¤ может быть клиническим про¤влением основного заболевани¤ (паркинсонизм) и также может возникнуть на фоне лечени¤ препаратом Ћеводопа/Ѕенсеразид. “акие пациенты должны быть под наблюдением врача дл¤ своевременного вы¤влени¤ психических нежелательных реакций.

In some patients with Parkinson's disease, the appearance of behavioral and cognitive disorders was noted as a result of the uncontrolled use of increasing doses of the drug, despite the doctor's recommendations and a significant increase in therapeutic doses.

Experience with Levodopa / Benserazide under the age of 25 is limited.

Influence on the ability to drive vehicles and work with equipment.

Patients who experience excessive daytime sleepiness or sudden episodes of sleep should refuse to drive or work with equipment. If these symptoms appear during treatment with Levodopa / Benserazide, the possibility of reducing the dose or discontinuing therapy should be considered.

Storage conditions

In a place protected from moisture, at a temperature not exceeding 25 ? C.

Shelf life

2 years