Description
Release form
Film-coated tablets.
Packing
In a package of 30 pieces.
Pharmacological action
Stalevo – a combined antiparkinsonian drug, which 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 the content of 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 central nervous system. Levodopa quickly decarboxylates 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 the inhibition of dopa-decarboxylase, levodopa is biotransformed with the participation of catechol-O-methyltransferase (COMT) into a potentially dangerous metabolite of 3-O-methyldopa (3-OMD). Entacapone is a reversible, specific inhibitor of COMT, 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 the drug) in cases where the use of the combination of levodopa + carbidopa is ineffective.
Contraindications
– Severe impairment of liver function.
– Angle-closure glaucoma.
– Pheochromocytoma.
– Co-administration with non-selective MAO type A and B inhibitors (e.g. phenelzine, tranylcypromine).
– Co-administration with selective MAO inhibitors of types A and B.
– Malignant antipsychotic syndrome and / or atraumatic acute rhabdomyolysis (including history).
– Children and teens under 18 years of age.
– Pregnancy.
– Lactation (breastfeeding).
– Hypersensitivity to the drug.
Caution is advised to use the drug in:
– Severe cardiovascular and pulmonary failure.
– Bronchial asthma.
– Liver disease.
– Kidney Disease.
– Diabetes mellitus and other decompensated endocrine diseases.
– Erosive-ulcerative lesions of the gastrointestinal tract.
– Convulsions (history).
– With a history of myocardial infarction (with persistent cardiac arrhythmias).
– A history of psychosis and / or treatment.
– Depression with suicidal tendencies.
– Asocial Behavior.
– Open-angle glaucoma.
Caution should be exercised while using Stalevo with:
– Drugs that can cause orthostatic hypotension.
– With dopamine blocking antipsychotics (especially dopamine D2 receptor antagonists).
– With tricyclic antidepressants, desipramine, maprolitin, venlafaxine.
– With warfarin and drugs metabolized by COMT (paroxetine).
Use during pregnancy and lactation
The drug is contraindicated in pregnancy (except in cases where the potential positive effect of taking the drug exceeds the possible risk for the development of the fetus) and during lactation.
Composition
In 1 coated tablet, it contains: levodopa 100 mg, carbidopa in the form of monohydrate 12.5 mg, entacapone 200 mg.
Excipients: corn starch, mannitol, croscarmellose sodium, povidone, magnesium stearate.
Shell composition: hypromellose, sucrose, titanium dioxide, iron oxide yellow, iron oxide red, magnesium stearate, polysorbate 80, glycerol 85%.
Dosage and administration
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 forms 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 (corresponding to 10 tablets of Stalevo 150 / 37.5 / 200 mg).
If it is necessary to administer more levodopa, the interval between doses of the drug is reduced and / or the patient is transferred to the Stalevo treatment in a larger dosage (necessarily within the recommended dose). If less levodopa is required, then the intervals between doses of the drug are increased and / or the patient is transferred to Stalevo treatment in a lower dosage. If other drugs containing levodopa are used simultaneously with Stalevo, then you should carefully follow the recommendations for the total daily dose of the drug.
Drug interactions
Therapeutic effect Steel decreases while taking dopamine receptor antagonists (some antipsychotics and antiemetics), phenytoin, papaverine. With simultaneous administration with iron preparations, the effectiveness of Stalevo may decrease, because 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 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 certain amino acids. Steel compatible with imizine and moclobemide, pyridoxine hydrochloride, diazepam, ibuprofen.
Overdose
Symptoms: increased severity of side effects, except for allergic reactions that are dose-independent.
Treatment: hospitalization, gastric lavage, repeated activated charcoal. Control of functions of respiratory, cardiovascular and urinary systems of ECG – monitoring, if necessary – antiarrhythmic therapy.
Pyridoxine is ineffective in overdosing on Stalevo.
Storage conditions
Keep out of the reach and sight of children at temperatures between 15 ° and 25 ° C.
Shelf life
3 years.
Terms and conditions
prescription
dosage form
tablets
Possible product names
STEEL 0.1 / 0.025 / 0.2 N30 TABLE P / O
Steel 100mg + 25mg + 200mg Tab. n / a X30 /! until 11.10g /
Stalevo 100mg + 25mg + 200mg Tab. p / pl / rev X30
STEEL TAB P / O 100 MG + 25 MG + 200 MG No. 30
Steel tablets 100 mg, 30 pcs.
Orion Corporation, Finland
