Levodopa + Benserazide (Levodopum + Benserazidum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Anti-Parkinsonics

Dopaminomimetics

Included in the formulation
  • Levodopa + Benserazide
    capsules inwards 
    IZVARINO PHARMA, LLC     Russia
  • Levodopa / Benserazid-Teva
    pills inwards 
    Teva Pharmaceutical Enterprises Co., Ltd.     Israel
  • Madopar® "125"
    capsules inwards 
    Hoffmann-La Roche Ltd.     Switzerland
  • Madopar® "250"
    pillscapsules inwards 
    Hoffmann-La Roche Ltd.     Switzerland
  • Madopar®GSS "125"
    capsules inwards 
    Hoffmann-La Roche Ltd.     Switzerland
    • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    VED

    ONLS

    АТХ:

    N.04.B.A   Dopa and dopa derivatives

    N.04.B.A.02   Levodopa and a decarboxylase inhibitor

    Pharmacodynamics:

    Combined anti-Parkinsonics.

    Levodopa

    Replenishes the deficiency of dopamine. The precursor of the dopamine mediator penetrates the blood-brain barrier and is converted to dopamine in the central nervous system.

    Benserazide

    Inhibits peripheral DOPA decarboxylase, increasing the concentration of levodopa in the central nervous system and reducing side effects: hypokinesia, dysphagia, tremor, rigidity of muscles, salivation.

    The optimal combination of levodopa and benserazide is 4: 1. The therapeutic effect develops after 6-8 days, reaches a maximum - after 25-30 days

    Pharmacokinetics:

    Levodopa

    Absorbed in the gastrointestinal tract in an amount of 20-30% of the dose. The maximum concentration in blood plasma is achieved after 2-3 hours. It binds to plasma proteins by 10-30%.

    Metabolized by the action of catechol-O-methyltransferase and dopa decarboxylase in all tissues to dopamine, norepinephrine, epinephrine and 3-O-methyldopa.

    The elimination half-life is 0.6-1.3 hours. Elimination by the kidneys, partly with feces.

    Benserazide

    Absorbed in the gastrointestinal tract up to 30%. The maximum concentration in the blood plasma is reached after 2-3 hours. It does not penetrate the blood-brain barrier, accumulates in the lungs, small intestine, kidneys, liver. Penetrates through the placental barrier. Metabolised in the liver.

    Half-life 1.5 hours Elimination by the kidneys (64%) and the intestine (26%).

    Cumulation

    Levodopa in combination with benserazidom is cumulated at 74-120%.

    Indications:

    It is used for the treatment of Parkinson's disease, as well as for the treatment of the restless legs syndrome.

    ICD-10

    VI.G20-G26.G21   Secondary Parkinsonism

    VI.G20-G26.G20   Parkinson's disease

    Contraindications:
    • Liver failure.
    • Pheochromocytoma.
    • Closed-angle glaucoma.
    • Atraumatic acute rhabdomyolysis (including in the anamnesis).
    • Malignant neuroleptic syndrome.
    • Individual intolerance.
    Carefully:

    Cardiovascular and pulmonary insufficiency,bronchial asthma, endocrine diseases in the stage of decompensation, erosive-ulcerative lesions of the gastrointestinal tract, convulsions (including in the anamnesis), psychoses, open-angle glaucoma, depressive states with suicidal tendencies.

    Pregnancy and lactation:Recommendations for FDA - Category C. During pregnancy and lactation, the drug is contraindicated. Benserazide can cause bone disease in the fetus.
    Dosing and Administration:

    Inside regardless of the time of meal. The dose is selected individually. The initial dose: 50 mg of levodopa and 12.5 mg of benserazide 3-4 times a day, with a gradual increase to the optimum amount: 300-800 mg of levodopa and 75-200 mg of benserazide for 4-6 receptions.

    The highest daily dose: 1000-1200 mg of levodopa and 250-300 mg of benserazide.

    The highest single dose: 1 tablet.

    Side effects:

    Central and peripheral nervous system: headache, insomnia, nightmares, hallucinations, euphoria, paranoid thinking, cognitive dysfunction, ataxia, trismus, blepharospasm, bruxism.

    The cardiovascular system: orthostatic hypotension, arrhythmia, arterial hypertension, phlebitis.

    Respiratory system: dyspnea, pain in the chest.

    The system of hematopoiesis: anemia, agranulocytosis, thrombocytopenia.

    Digestive system: dryness, bitter aftertaste, burning sensation in the mouth, nausea, salivation, vomiting, hiccough, dysphagia, diarrhea, constipation, flatulence, hepatitis, duodenal ulcer development.

    Sense organs: oculogic crises, diplopia, mydriasis, blurred vision.

    Urinary system: urinary retention, priapism, change in urine color, urinary incontinence.

    Dermatological reactions: hyperemia, hot flushes, hyperhidrosis, hair loss, hives.

    Allergic reactions.

    Overdose:

    Symptoms: increased side effects.

    Treatment: symptomatic.

    Interaction:

    Contraindicated simultaneous use with nonselective and selective MAO inhibitors types A and B.

    Compatible with other antiparkinsonian drugs, antidepressants (imizin, moclobemide).

    Antagonists of dopamine receptors, phenytoin, papaverine reduce the therapeutic effect of levodopa.

    It is recommended to take iron preparations with a 2-3 hour interval, since levodopa is combined with iron ions, forming chelate complexes.

    Compatible with vitamin B6, ibuprofen, diazepam.

    Special instructions:

    Not effective against extrapyramidal disorders caused by medication.

    Causes drowsiness and short-term sudden falling asleep. When taking the drug, patients are forbidden to drive a car and work with moving machinery.

    Instructions
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