Stalevo, pills 100mg+25mg+200mg 30pcs

Composition

1 coated tablet contains:

levodopa 100 mg,

carbidopa monohydrate 12.5 mg, entacapone 200 mg.

Auxiliary substances:

corn starch,

mannitol,

sodium croscarmellose,

povidone,

magnesium stearate.

Shell composition:

hypromellose, sucrose, titanium dioxide, iron oxide yellow, iron oxide red, magnesium stearate, polysorbate 80, glycerin 85%.

Pharmacological action

Stalevo is a combined antiparkinsonian drug that combines levodopa, a metabolic precursor of dopamine, carbidopa, an aromatic amino acid decarboxylase inhibitor, and entacapone, a catechol-O-methyltransferase (COMT) inhibitor. Levodopa increases dopamine levels in the brain.

Dopamine is formed directly from levodopa with the participation of aromatic amino acid decarboxylase. The antiparkinsonian effect of levodopa is due to its conversion to dopamine directly in the central nervous system. Levodopa is rapidly decarboxylated in peripheral tissues, turning into dopamine, which, however, does not penetrate the BBB.

Carbidopa inhibits the decarboxylation of levodopa and the formation of dopamine in peripheral tissues, which indirectly leads to an increase in the amount of levodopa entering the central nervous system.

As a result of inhibition of dopa-decarboxylase, levodopa is biotransformed with the participation of catechol-O-methyltransferase (COMT) into the potentially dangerous metabolite 3-O-methyldopa (3-OMD).

Entacapone is a reversible, specific COMT inhibitor, mainly of peripheral action. Entacapone slows the clearance of levodopa from the bloodstream, which leads to an increase in the bioavailability of levodopa, prolonging its therapeutic effect.

Indications

Parkinson’s disease and Parkinsonism (with the exception of medication) in cases where the use of a combination of levodopa + carbidopa is ineffective.

Use during pregnancy and lactation

The drug is contraindicated for use during pregnancy (except in cases where the potential positive effect of taking the drug exceeds the possible risk for fetal development) and during lactation.

Contraindications

-Severe liver function disorders. – Angle-closure glaucoma. – Pheochromocytoma. – Combined use with non-selective MAO inhibitors of types A and B (for example, phenelzine, tranylcypromine). – Combined use with selective MAO inhibitors of types A and B. -neuroleptic malignant syndrome and/or atraumatic acute rhabdomyolysis (including in the anamnesis). – Children and teenagers under 18 years of age. – Pregnancy. – The period of lactation (breastfeeding). – Hypersensitivity to the components of the drug. The drug should be used with caution in patients with: – Severe cardiovascular and pulmonary insufficiency. – Bronchial asthma. – Liver diseases. – Kidney diseases. – Diabetes mellitus and other decompensated endocrine diseases. – Erosive and ulcerative lesions of the gastrointestinal tract. – Convulsions (in the anamnesis). – With a history of myocardial infarction (with persistent cardiac arrhythmias). – Psychosis in the anamnesis and / or during treatment. – Depression with suicidal tendencies. – Antisocial behavior. – Open-angle glaucoma. Caution should be exercised when using Stalevo concomitantly with: – Drugs that can cause orthostatic hypotension. – With antipsychotics that block dopamine (especially dopamine D2-receptor antagonists). – With tricyclic antidepressants, desipramine, maprolitin, venlafaxine. – With warfarin and drugs metabolized by COMT (paroxetine).

Interaction

The therapeutic effect of Stalevo decreases when taken simultaneously with dopamine receptor antagonists (some antipsychotics and antiemetics), phenytoin, papaverine.

When taken concomitantly with iron preparations, the effectiveness of Stalevo may decrease, since levodopa and entacapone form chelate complexes with iron ions in the gastrointestinal tract.

It is necessary to observe a time interval of 2-3 hours between doses of Steel and iron-containing preparations.

The therapeutic effect of Stalevo may be reduced in patients receiving a high-protein diet, due to the competing action of levodopa and certain amino acids. Stalevo is compatible with imizine and moclobemide, pyridoxine hydrochloride, diazepam, ibuprofen.

How to take, course of use and dosage

The drug is taken orally, regardless of food intake, without dividing the tablet into parts. The optimal daily dose is determined by careful individual selection. It is recommended to use one of the three existing dosage types of the drug (50/12.5/200 mg,100/25/200 mg or 150/37.5/200 mg of levodopa / carbidopa / entacapone).

As a single dose, only 1 tablet of any dosage should be taken. The maximum daily dose is 1.5 g of levodopa,2 g of entacapone,375 mg of carbidopa (corresponds to 10 tablets of Stalevo 150/37.5/200 mg).

If it is necessary to introduce a larger amount of levodopa, reduce the interval between doses of the drug and / or transfer the patient to treatment with Stalevo in a larger dosage (always within the recommended dose). If a smaller amount of levodopa is required, then the intervals between doses of the drug are increased and/or the patient is transferred to the treatment of Stalevo in a lower dosage.

If other drugs containing levodopa are used simultaneously with Stalevo, then the recommendations for the total daily dose of the drug should be carefully followed.

Overdose

Symptoms: increased severity of side effects, with the exception of allergic reactions, which are dose-independent.

Treatment: hospitalization, gastric lavage, repeated use of activated charcoal. Monitoring of the functions of the respiratory, cardiovascular and urinary systems; ECG monitoring, if necessary – antiarrhythmic therapy.

Pyridoxine is ineffective in an overdose of Stalevo.

Special instructions

Stalevo is not intended to eliminate extrapyramidal reactions caused by taking medications. Before the planned general anesthesia, the drug can be taken as long as the patient is allowed to take it orally.

In the case of long-term therapy with Stalevo, periodic monitoring of the functions of the liver, hematopoiesis system, kidneys, and cardiovascular system is required. Monitoring of the function of the cardiovascular system is required during the entire period of initial dose adjustment of the drug.

The use of the drug in open-angle glaucoma is possible only with careful monitoring of intraocular pressure. When replacing Stalevo with levodopa + carbidopa therapy (without entacapone), an increase in the dose of levodopa will be required. Cancellation of Stalevo is carried out slowly, if necessary, increasing the dose of levodopa. Therapy with Stalevo does not interfere with the use of other Antiparkinsonian drugs. The daily dose of seleginin when taken concomitantly with Stalevo should not exceed 10 mg.

Effects on the ability to drive motor vehicles and manage mechanisms: entacapone in combination with levodopa causes drowsiness and occasional instantaneous falling asleep. It is necessary to give up driving a car and working with machines and mechanisms during the period of taking the drug Stalevo.

Form of production

Film-coated tablets.

Storage conditions

At a temperature of 15-25 °C

Shelf life

3 years

Active ingredient

Levodopa, Entacapone, Carbidopa

Conditions of release from pharmacies

By prescription

Dosage form

Tablets