Zafirlukast (Zafirlukastum)

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

Prostaglandins, thromboxanes, leukotrienes and their antagonists

Included in the formulation
  • Acolat®
    pills inwards 
    AstraZeneca UK Ltd     United Kingdom
    • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    VED

    ONLS

    АТХ:

    R.03.D.C.01   Zafirlukast

    Pharmacodynamics:

    Competitively blocks LTC leukotriene receptors4, LTD4 and LTE4, as a result of which it prevents contractions of the smooth muscles of the bronchi.

    Reduces the risk of edema of the respiratory tract, reduces the severity of clinical manifestations of bronchial asthma at night and daytime.

    Has no effect on histamine, thromboxane, prostaglandin and cholinergic receptors.

    Pharmacokinetics:

    After oral administration, up to 70% is absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is achieved after 3 hours. The connection with plasma proteins is 99%.

    Therapeutic effect develops after the reception. Metabolism in the liver. Penetrates into breast milk.

    The elimination half-life is 10 hours. Elimination with feces and kidneys in the form of metabolites.

    Indications:

    It is used for the treatment of bronchial asthma of mild and moderate severity (for the prevention of seizures and maintenance therapy).

    ICD-10

    X.J40-J47.J45   Asthma

    Contraindications:

    Age up to 5 years, individual intolerance.

    Carefully:

    Pregnancy and lactation, hypersensitivity.

    Pregnancy and lactation:

    Recommendations for FDA - Category B. Applicable with caution, in cases where the expected effect exceeds the risk to the fetus and newborn.

    Dosing and Administration:

    Use in children

    Inside, 1 hour before meals, children 5-11 years - 10 mg 2 times a day.

    Adults and children from the age of 12

    Inside, 1 hour before meals, 20 mg twice a day. When the need for a dose is doubled - 40 mg twice a day.

    The highest daily dose: 80 mg.

    The highest single dose: 40 mg.

    Side effects:

    Central and peripheral nervous system: headache, weakness, insomnia.

    The cardiovascular system: thrombocytopenia, rarely - agranulocytosis.

    Digestive system: nausea, vomiting, rarely - bilirubinemia, hepatitis.

    Reproductive system: metrorrhagia.

    Allergic reactions.

    Overdose:

    Cases of overdose are not described.

    Treatment is symptomatic.

    Interaction:

    Simultaneous use with anticoagulants increases the risk of bleeding.

    Acetylsalicylic acid increases the concentration of zafirlukast.

    Erythromycin and theophylline reduce the concentration of the drug in the blood plasma.

    Special instructions:

    The drug is not intended for arresting bronchospasm.

    Instructions
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