Levodopa + benserazide tabs 250mg + 50mg #100

User manual for Levodopa + benserazide

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Composition

Levodopa, benserazide hydrochloride, microcrystalline cellulose talc, titanium dioxide, gelatin, povidone, dye.

Form of issue

    Levodopa + benserazide GSS 125 - capsules with modified release of active substance in dark vials in cardboard bundle No. 100.
    Levodopa + benserazide 125 - tablets of dispersible cylindrical form in dark bottles in a cardboard bundle No. 100.
    Levodopa + benserazide 250 - tablets of cylindrical form in a glass bottle in a pack of cardboard No. 30, 100.

pharmachologic effect

Antiparkinsonian.

Pharmacodynamics and pharmacokinetics

Pharmacodynamics

The drug with antiparkinsonian action. The left-handed isomer of DOPA (levodopa) is a precursor of dopamine. The mechanism of action of levodopa is based on its transformation into dopamine, which compensates for the lack of dopamine in the central nervous system. The part that is synthesized in dopamine in peripheral tissues in the antiparkinsonian action of levodopa is not involved, since the central nervous system does not penetrate and is responsible for its side effects. Eliminates tremor, hypokinesia, dysphagia, stiffness, drooling.
Benserazid, an inhibitor of dopa-decarboxylase, helps to reduce the synthesis of dopamine in peripheral tissues, which indirectly increases the amount of levodopa that enters the central nervous system. The pronounced therapeutic effect appears on the 6-8 day, and the maximum effect is observed after 25-30 days. The optimal ratio of levodopa and benserazide is 4: 1. The new dosage form (capsules GSS), allows in just a few hours to achieve an effective therapeutic drug concentration in the blood in the plasma, without significant fluctuations.

Pharmacokinetics

Levodopa + benserazide capsules and tablets are bioequivalent. Levodopa is absorbed mainly in the upper parts of the small intestine. Cmax levodopa in the blood after taking the drug is achieved after 1 hour, while the intake of food grade and rate of absorption of levodopa decreases. The substance with plasma proteins does not bind, penetrates through the BBB. Metabolism of levodopa occurs by o-methylation and decarboxylation with the formation of the main metabolite of 3-o-methyldopa. Under the action of decarboxylase, levodopa is transformed into dopamine.
Benserazide does not penetrate through the BBB (when administered in therapeutic doses), accumulates in the lungs, kidneys, liver and small intestine.
When co-administered with benserazid, the peripheral decarboxylation of levodopa decreases, which leads to an increase in the concentrations of levodopa and the metabolite of 3-o-methyldopa in the blood. The excretion of Benserazide occurs in the form of metabolites through the kidneys and intestines.
The drug in the form Levodopa + benserazide GSS 125 has other pharmacokinetic properties. The active substances in the stomach are released slowly. Cmax in the blood by 20-30% than, than in the previous dosage forms, and comes in 3 hours. The bioavailability of Levodopa + benserazide GSS 125 is lower and equal to 50-70% of the bioavailability of Levodopa + benserazide 250 and Levodopa + benserazide 125 tablets and does not depend on food intake.

Indications for use

Parkinson's disease, Parkinson's syndrome (other than caused by antipsychotics).

Contraindications

High sensitivity to the drug, violations of the endocrine and cardiovascular system, psychosis, liver disease, kidney, melanoma, pregnancy, lactation, age under 30 years.
Take with caution after suffering a myocardial infarction, with stomach ulcer, in the presence of arrhythmia, in patients with osteomalacia.

Side effects

Nausea, decreased appetite, vomiting, pain in the stomach, dysphagia, ulcerogenic effect; rarer - heart rhythm disturbances, orthostatic hypotension, hyperkinesia, depression, insomnia, increased excitability, constipation, tachycardia, mental disorders, leukopenia, hemolytic anemia, with prolonged use - weight gain.

Instructions for use Levodopa + benserazide (Method and dosage)

The dose of the drug is selected individually and depends on a number of factors: the patient's condition and the clinical picture of the disease. It is recommended that capsules and tablets be swallowed whole, taken during meals, washed down with water. Instructions for use Levodopa + benserazide 250 indicates the possibility of crushing the Levodopa + benserazide 250 tablet to facilitate swallowing.
The recommended initial dose is 0.125 g (1 capsule) 2 times a day. The dose rises weekly for 1 capsule per day. If any side effects occur, the dose increase stops. After the disappearance of adverse events, the dose is again increased by 1 capsule per day, every two weeks. The effective dose varies between 200-800 mg of levodopa per day and 50-200 mg of benserazide, which should be divided into 2-4 divided doses. Treatment is long.
If there are fluctuations in the effect during the day, you should switch to taking GSS capsules, while the dose should be increased 2-3 days after the bioavailability of this form of the drug is 50-60% lower. After reaching a maximum daily dose of 1.5 g and no effect should be returned to the usual forms of the drug.

Levodopa + benserazide is combined with other antiparkinsonian drugs, and as combined treatment can gradually cancel them or reduce the doses of other drugs.

Overdose

When an overdose occurs most often, insomnia, arrhythmia, nausea, involuntary movements, confusion, vomiting.

Interaction

Levodopa + benserazide, when taken together with sympathomimetics, enhances the effect of the latter, which may require a revision of their therapeutic doses. The drug should not be taken together with monoamine oxidase inhibitors.
Opioid analgesics, antipsychotics and antihypertensives containing reserpine reduce the effectiveness of Levodopa + benserazide. With the joint administration of Levodopa + benserazide with other antiparkinsonian drugs, it is possible to enhance its effect. During the treatment period, it is strictly forbidden to take pyridoxine (vitamin B6), which blocks the pharmacological action of levodopa.

Storage conditions

At a temperature of no higher than 25 ° C.
Shelf life - 4 years.

Reviews about Levodopa + benserazide

Reviews about Levodopa + benserazide are often diametrically different:
     "... My relative with Parkinson's disease was prescribed treatment with this drug. It takes 3 months, positive dynamics are evident - it began to regulate movements on its own, there was a shiver, convulsive movements, became a little more confident about moving around ";
     "... Levodopa + benserazide my grandfather takes a little more than a month, but we did not notice a marked improvement in the condition, in addition, motor activity decreased."