Stalevo (Stalevo)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceLevodopa + Entacapone + [Carbidopa]Levodopa + Entacapone + [Carbidopa]
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  • Stalevo
    pills inwards 
    Orion Corporation Orion Pharma     Finland
  • Stalevo®
       
    • Dosage form: & nbsp
    Film-coated tablets.

    Composition:

    active substances

    coated tablets

    50 mg / 12.5 mg / 200 mg

    100 mg / 25 mg / 200 mg

    150 mg / 37.5 mg / 200 mg

    levodopa

    50 mg

    100 mg

    150 mg

    carbidopa monohydrate, (corresponds to carbidopa)

    13.5 mg (12.5 mg)

    27.0 mg (25.0 mg)

    40.5 mg (37.5 mg)

    entacapone

    200 mg

    200 mg

    200 mg

    Excipients:

    Corn starch

    65.00 mg

    85.00 mg

    105.0 mg

    Mannitol

    59.5 mg

    86.10 mg

    113.0 mg

    Sodium croscarmellose

    17.70 mg

    23.70 mg

    28.5 mg

    Povidone

    31.90 mg

    39.70 mg

    46.6 mg

    Magnesium stearate

    6.50 mg

    8.50 mg

    10.5 mg

    Shell

    Hypromellose

    8.27 mg

    10.82 mg

    13.36 mg

    Sucrose

    1.18 mg

    1.55 mg

    1.91 mg

    Titanium dioxide

    1.65 mg

    2.16 mg

    2.67 mg

    Iron oxide yellow

    0.12 mg

    0.15 mg

    0.19 mg

    Iron oxide red

    0.35 mg

    0.46 mg

    0.57 mg

    Magnesium stearate

    0.59 mg

    0.77 mg

    0.96 mg

    Polysorbate 80

    0.24 mg

    0.31 mg

    0.38 mg

    Glycerin 85%

    0.59 mg

    0.77 mg

    0.96 mg
    Description:
    Tablets are brownish-red or grayish-red, oblong-ellipsoidal, biconvex, without risks, coated.
    For dosage of 50 mg / 12.5 mg / 200 mg:
    on one side there is code LCE 50.
    For a dosage of 100 mg / 25 mg / 200 mg:
    on one side there is code LCE 100.
    For a dosage of 150 mg / 37.5 mg / 200 mg:
    on one side there is code LCE 150.
    Pharmacotherapeutic group:An antiparkinsonian agent (dopamine precursor + decarboxylase peripheral inhibitor + COMT inhibitor)
    ATX: & nbsp

    N.04.B.A.03   Levodopa, a decarboxylase inhibitor and a catechol-o-methyltransferase inhibitor

    Pharmacodynamics:Levodopa - the precursor of the dopamine mediator, penetrates the blood-brain barrier, reducing the symptoms of dopamine deficiency. The antiparkinsonian effect of levodopa is due to the transformation into dopamine directly in the central nervous system (CNS), which leads to the replenishment of its deficiency. Carbidopa, an inhibitor of peripheral Dopa-decarboxylase, reduces the formation of dopamine in peripheral tissues, which indirectly leads to an increase in the amount of levodopa entering the central nervous system (CNS). With the inhibition of Dopha- decarboxylase levodopa mainly metabolized into a potentially dangerous metabolite of 3-O-methyldopa (3-OMD) catechol-O-methyltransferase. Entacapone is a reversible, specific inhibitor of catechol-O-methyltransferase (COMT), mainly peripheral. Entacapone slows the clearance of levodopa from the bloodstream, which increases the bioavailability of levodopa, prolonging its therapeutic effect.
    Pharmacokinetics:
    Absorption and distribution.
    Levodopa quickly absorbed from the gastrointestinal tract (GIT). Eating foods rich in large amounts of neutral amino acids can delay and reduce absorption. Slightly associated with blood plasma proteins (10-30%), absorption is 20-30% of the dose. At oral reception the maximum concentration in a blood plasma is reached in 2-3 hours. Individual bioavailability is 15-33%. The volume of distribution is 1.6 l / kg.
    Carbidopa compared with levodopa absorbed and absorbed somewhat more slowly. Data on pharmacokinetics are limited. It binds to plasma proteins by about 36%. Individual bioavailability of carbidopa is 40-70%.
    Entacapon quickly absorbed from the gastrointestinal tract. It binds to plasma proteins by 98%, mainly with albumin; in therapeutic concentrations does not displace other drugs with a high degree of complex formation from the bond with proteins (warfarin, salicylic acid, phenylbutazone, diazepam and etc.). Individual bioavailability is 35% (with a single oral intake of 200 mg). The maximum concentration with a single oral intake is achieved after 1 hour.The volume of distribution is 0.27 l / kg.
    Metabolism and excretion.
    Levodopa It is actively metabolized in all tissues with Dofa decarboxylase and catechol-O-methyltransferase to dopamine, norepinephrine, epinephrine and 3-O-methyldopa. 75% of the accepted dose is excreted by the kidneys in the form of metabolites for 8 hours. In unchanged form it is excreted by the kidneys (35% for 7 hours) and the intestine. The total clearance of levodopa is 0.55-1.38 l / kg / h. The half-life is 0.6-1.3 hours.
    Carbidopa metabolized to two major metabolites that are excreted in the urine as glucuronides and unbound structures. Unchanged carbidopa by 30% is excreted by the kidneys with urine. Among the metabolites excreted in urine, the main ones are: alpha-methyl-3-methoxy-4-hydroxyphenylpropionic acid and alpha-methyl-3,4-dihydroxyphenylpropionic acid. The half-life is 2-3 hours.
    Entacapon almost completely metabolized. Has the effect of a "first pass" through the liver, a small amount of entacapone being an (E) -isomer, turns into a (Z) -isomer (about 5% of the total entacapone in the blood plasma). It is excreted by the kidneys by 10-20% and through the intestine (with feces and bile) by 80-90%. The main way of metabolism of entacapone and its active metabolite is conjugation with glucuronic acid.The total clearance is about 0.7 l / kg / h. The half-life is 0.4-0.7 hours.
    Due to the short half-life of the repeated application, there is no true accumulation of levodopa or entacapone.
    Age groups of patients. Pharmacokinetic parameters in patients younger (45-64 years) and older (65-75 years) age are the same.
    Floor. Bioavailability of levodopa is significantly higher in women. The bioavailability of carbidopa and entacapone does not depend on the sex of the patients.
    Violation of the function of the liver. Metabolism of entacapone is slowed in patients with mild and moderate liver function abnormalities (classes A and B according to the Child-Pugh classification), which leads to an increase in entacapone concentration in the blood plasma both in the absorption phase and in the elimination phase.
    Impaired renal function. Does not affect the pharmacokinetics of entacapone. Studies of the pharmacokinetics of levodopa and carbidopa in patients with impaired renal function have not been performed.
    Indications:Parkinson's disease and parkinsonism (with the exception of drug) in cases where the use of combination levodopa + carbidopa ineffective.
    Contraindications:
    - hypersensitivity to the active components or to any of the excipients (excipients);
    - severe liver dysfunction;
    - narrow-angle glaucoma;
    - pheochromocytoma;
    - combined use with nonselective monoamine oxidase (MAO) inhibitors of types A and B (eg, phenelzine, tranylcypromine);
    - joint application with selective MAO-A and MAO-B inhibitors;
    - malignant neuroleptic syndrome and / or atraumatic acute rhabdomyolysis (including in anamnesis).
    - age to 18 years;
    - the period of breastfeeding;
    - pregnancy, except for those individual situations when the potential positive effect of taking CTIJIEBO exceeds the possible risk for fetal development;
    - deficiency of sugar / isomaltase, intolerance to fructose, glucose-galactose malabsorption.
    Carefully:
    Severe cardiovascular and pulmonary, insufficiency, bronchial asthma, liver, kidney disease; diabetes mellitus and other decompensated endocrine diseases, erosive and ulcerative lesions of the gastrointestinal tract; convulsions (in the anamnesis); Myocardial infarction in anamnesis (with residual atrial nodular or ventricular arrhythmias) - control of cardiac function induring the entire period of initial regulation of the dosing regimen; Psychosis in the history and / or in the process of treatment, depression with suicidal tendencies, antisocial behavior;
    Wide-angle glaucoma - with careful monitoring of intraocular pressure; Patients receiving on the background of treatment STALVO drugs that can cause orthostatic hypotension;
    With the concomitant administration of neuroleptics blocking dopamine receptors (especially D2 receptors), STALVE treatment should be performed under close observation of the patient to stop the antiparkinsonian effect of the drug or enhance the symptoms of the disease;
    Simultaneous reception of STEELOVO and three cyclic antidepressants, desipramine, maprolitin, venlafaxine.
    Simultaneous reception with warfarin and drugs metabolized by COMT (paroxetine).
    Dosing and Administration:
    Inside, regardless of food intake; tablets can not be divided into parts or broken. The optimal daily dose is determined by careful selection of the dose of levodopa for each patient individually. The daily dose is preferably optimized using one of the three existing dosage types of STEEL (50 / 12.5 / 200 mg, 100/25/200 mg or 150/37.5 / 200 mg levodopa / carbidopa / entacapone).As a single dose, only one 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 STEVE 150/37.5 / 200 mg). The frequency of dosing is determined by the attending physician. Dose regulation during treatment.
    If more Levodopa is needed, the interval between doses is reduced and / or the patient is transferred to STALVE treatment at a higher dosage (mandatory within the recommended dose!).
    If less Levodopa is required, the intervals between doses of the drug are increased and / or the patient is transferred to STEVEVO treatment at a lower dosage.
    If other drugs containing levodopa are used concomitantly with STEVE, then recommendations for the total daily dose of the drug should be carefully followed.
    Side effects:Nervous system disorders: ataxia, numbness, trismus, activation of latent Gorner syndrome, dyskinesia (including choreiramic, dystonic and other involuntary movements), hyperkinesia, bradykinesia (inclusion-exclusion phenomenon), worsening of parkinsonism symptoms, blepharospasm, bruxism; drowsiness, dizziness, anorexia.
    Mental disorders: - confusion, insomnia, paronial, nightmares, hallucinations, agitation, anxiety, euphoria; changes in thinking (including paranoid thinking and transient psychoses); Depression with or without development of suicidal tendencies; cognitive dysfunction;
    The cardiovascular system: arrhythmia, orthostatic hypotension, increased blood pressure, phlebitis.
    Organs of vision: diplopia, blurred vision, dilated pupils, oculogic crises.
    Digestive system disorders: xerostomia, bitter taste in the mouth, nausea, vomiting, salivation, dysphagia, hiccough, pain and discomfort in the abdomen, constipation, diarrhea, flatulence, burning sensation in the tongue, gastrointestinal bleeding, development of duodenal ulcer; hepatitis.
    Skin reactions: hyperemia of the skin, a sensation of "hot flashes" of blood, hyperhidrosis, sweating (darkening), hair loss, erythematous or macular rash, urticaria.
    Disorders of the urinary system: urine retention, urinary incontinence, change in urine color, priapism.
    Respiratory system: pain in the chest, shortness of breath.
    Hemopoietic system: hemolytic and non-hemolytic anemia, thrombocytopenia, agranulocytosis.
    Other: weakness, fatigue, headache, dysphonia, malignant melanoma.
    Overdose:
    Symptoms: increased severity of side effects, except for allergic reactions that are dose-independent.
    Treatment: hospitalization, gastric lavage, repeated receptions of activated charcoal. Control of the functions of the respiratory, cardiovascular and urinary systems; ECG monitoring, if necessary - antiarrhythmic therapy. Pyridoxine Ineffective in overdose STEELOVO.
    Interaction:
    Other anti-Parkinsonics. Therapy STEELOVO does not prevent the use of other antiparkinsonian drugs. The daily dose of seleghinin with simultaneous admission with the drug STEVELO should not exceed 10 mg.
    Antidepressants. STEELA is compatible with imipramine and moclobemide. The therapeutic effect of STEELVO decreases with simultaneous reception with antagonists of dopamine receptors (some neuroleptic and antiemetics), phenytoin, papaverine.
    The therapeutic effect of STEEL can decrease in patients receiving a high-protein diet, due to the competing effect of levodopa and some amino acids.
    At simultaneous reception with preparations of iron it is necessary to observe a time interval in 2-3 h between receptions of STEEL and iron-containing preparations (levodopa and entacapon form chelate complexes in the gastrointestinal tract with iron ions).
    STEELO is compatible with preparations of vitamin B6 (pyridoxine), diazepam, ibuprofen.
    Special instructions:
    When STALEVO is replaced with therapy levodopa + carbidopa (without entacapone) - an increase in the dose of levodopa is required.
    Entacapone in combination with levodopa causes drowsiness and episodic instantaneous falling asleep. It is necessary to refuse to drive a car and work with machines and mechanisms.
    STEELO is not prescribed for the elimination of extrapyramidal reactions caused by medication.
    Before the planned general anesthesia, the drug can be taken as long as the patient is allowed oral intake.
    In the case of long-term STEELOVO therapy, periodic monitoring of liver function, hematopoiesis system, kidneys, cardiovascular system is required.
    Cancel STALEVO slowly, if necessary, increasing the dose of levodopa.
    Form release / dosage:
    Tablets, film-coated 50 mg / 12.5 mg / 200 mg; _100 mg / 25 mg / 200 mg; 150 mg / 37.5 mg / 200 mg.
    Packaging:
    Primary packaging: 10, 30, 100 and 250 tablets in a bottle of high-density polyethylene (HDPE) with a polypropylene stopper, equipped with a protective mechanism against accidental opening. The neck of the vial is sealed with foil (control of the primary autopsy).
    Secondary packaging: 1 bottle together with instructions for medical use in a pack of cardboard.
    Storage conditions:Store at a temperature of 15 to 25 ° C. Keep out of the reach of children.
    Shelf life:Do not use after the expiration date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:LS-000759
    Date of registration:18.05.2011
    The owner of the registration certificate:Orion Corporation Orion Pharma Orion Corporation Orion Pharma Finland
    Manufacturer: & nbsp
    Representation: & nbspORION CORPORATION ORION PHARMA ORION CORPORATION ORION PHARMA Finland
    Information update date: & nbsp22.08.2015
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