Stalevo, 50 mg+12, 5 mg+200 mg 30 pcs

Stalevo is a combined antiparkinsonian drug that is a combination of levodopa, a metabolic precursor of dopamine, carbidopa, an inhibitor of aromatic amino acid decarboxylase, and entacapone, an inhibitor of catechol-O-methyltransferase (COMT).

Levodopa increases dopamine in the brain.

Dopamine is formed directly from levodopa with the participation of aromatic amino acid decarboxylase.

The anti-Parkinsonian effect of levodopa is due to its conversion to dopamine directly in the CNS.

Levodopa is rapidly decarboxylated in peripheral tissues, converting to dopamine, which, however, does not penetrate the BBB.

Carbidopa inhibits the process of decarboxylation of levodopa and formation of dopamine in peripheral tissues, which indirectly leads to an increase in the amount of levodopa delivered to the CNS.

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

Entacapone is a reversible, specific COMT inhibitor of mainly peripheral action.

Entacapone slows the clearance of levodopa from the bloodstream, resulting in increased bioavailability of levodopa, prolonging its therapeutic effect.

Indications

Parkinson’s disease and Parkinsonism (except drug-induced) where the use of levodopa + carbidopa combination is ineffective.

Composition

One coated tablet contains:

Levodopa 50 mg,

carbidopa in monohydrate form 12.5 mg,

entacapone 200 mg.

Auxiliary substances:

Corn starch,

Mannitol,

/p>

croscarmellose sodium,

povidone,

Magnesium stearate.

Composition of the shell:

hypromellose,

sucrose,

titanium dioxide,

iron oxide yellow,

iron oxide red,

magnesium stearate,

polysorbate 80,

glycerin 85%.

How to take, the dosage

The drug is taken orally, regardless of meals, without dividing the tablet into parts. The optimal daily dose is determined by careful individual selection.

One of three current dosages is recommended (50/12.5/200 mg, 100/25/200 mg, or 150/37.5/200 mg levodopa/carbidopa/entacapone).

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

If more levodopa is needed, reduce the interval between doses and/or transfer the patient to Stalevo treatment at a higher dosage (necessarily within the recommended dosage).

If less levodopa is needed, increase the intervals between doses and/or transfer the patient to Stalevo treatment at a lower dosage.

If other medications containing levodopa are used concomitantly with Stalevo, the recommendations for the total daily dose of the medication should be carefully followed.

Interaction

The therapeutic effect of Stalevo is reduced when concomitantly administered with dopamine receptor antagonists (some neuroleptics and antiemetics), phenytoin, papaverine.

Concomitant administration with iron preparations may decrease efficacy of Stalevo because levodopa and entacapone form chelated complexes with iron ions in the gastrointestinal tract.

There should be a time interval of 2-3 h between doses of Stalevo and iron-containing drugs.

The therapeutic effect of Stalevo may decrease in patients receiving a high-protein diet due to the competing effects of levodopa and some amino acids.

Stalevo is compatible with imisin and moclobemide, pyridoxine hydrochloride, diazepam, and ibuprofen.

Special Instructions

Stalevo is not intended to eliminate extrapyramidal reactions caused by medication. Before the planned general anesthesia the drug may be taken as long as the patient is allowed to take it orally. In case of long-term therapy Stalevo requires periodic monitoring of functions of the liver, hematopoiesis system, kidneys, cardiovascular system.

Control of the cardiovascular system function is required during the whole period of initial dose adjustment of the drug. Use of the drug in open-angle glaucoma is possible only with careful control of intraocular pressure. When replacing Stalevo with levodopa + carbidopa therapy (without entacapone) an increase in levodopa dose will be required.

Stalevo should be withdrawn slowly, increasing the levodopa dose if necessary. Therapy with Stalevo does not prevent the use of other anti-Parkinsonian drugs. The daily dose of seleginine in concurrent use with the drug Stalevo should not exceed 10 mg.

Effects on driving and operating machinery:

entacapone in combination with levodopa causes drowsiness and occasional momentary falling asleep. It is necessary to refrain from driving and working with machines and mechanisms while taking the drug Stalevo.

Contraindications

• Veeping liver dysfunction.
• Open angle glaucoma.
• Pheochromocytoma.
• Combined use with non-selective MAO type A and B inhibitors (e.g., phenelzine, tranylcypromine).
• Combined use with selective MAO type A and B inhibitors.
• Malignant neuroleptic syndrome and/or atraumatic acute rhabdomyolysis (including history).
• Child and adolescent age below 18 years.
• Pregnancy.
• Period of lactation (breastfeeding).
• High sensitivity to the components of the drug.

The drug should be used with caution when:

• Developed cardiovascular and pulmonary insufficiency.
• Bronchial asthma.
• Hepatic disease.
• Kidney disease.
• Diabetes mellitus and other decompensated endocrine disorders.
• Gastrointestinal erosive lesions.
• Convulsions (in anamnesis).
• A history of myocardial infarction (with persistent cardiac rhythm disturbances).
• Psychosis in history and/or during treatment.
• Depression with suicidal tendencies.
• Associative behavior.
• Open-angle glaucoma.

Cautions should be taken when using Stalevo concomitantly with:

• Drugs that can cause orthostatic hypotension.
• With dopamine-blocking neuroleptics (especially dopamine D2-receptor antagonists).
• With tricyclic antidepressants, desipramine, maprolitin, venlafaxine.
• With warfarin and drugs metabolized by Comt (paroxetine).
  

Side effects

• nausea, vomiting, lack of appetite, abdominal pain;
• development of peptic ulcer;
• lower blood pressure;
cardiac arrhythmias;
• spontaneous movements;
• disorders of sleep, dizziness;
• weakness, fatigue.

.

Overdose

Symptoms: increased severity of side effects, except for allergic reactions, which are dose-dependent.

Treatment: hospitalization, gastric lavage, repeated administration of activated charcoal.

Control of respiratory, cardiovascular and urinary system functions; ECG-monitoring, antiarrhythmic therapy if necessary.

Pyridoxine is ineffective in Stalevo overdose.

Pregnancy use

The drug is contraindicated in pregnancy (except when the potential positive effect of taking the drug exceeds the possible risk to the fetus) and during lactation.