Clinical and pharmacological group: & nbsp

H1-antihistamines

Included in the formulation
  • Kestin®
    pills inwards 
    Almiral S.A.     Spain
  • Kestin®
    pills inwards 
    Almiral S.A.     Spain
  • Kestin®
    syrup inwards 
    Nycomed Denmark APS     Denmark
  • Kestin®
    pills inwards 
    Almiral S.A.     Spain
  • Ebastin
    pills inwards 
  • Espa-Bastin®
    pills inwards 
    Esparma GmbH     Germany
  • АТХ:

    R.06.A.X.22   Ebastin

    Pharmacodynamics:

    Histamine H blocker1-receptors from the piperidine derivative group. Has anti-allergic effect. Characterized by a prolonged action (up to 48 hours), which is due to the formation of active metabolites. Unlike many histamine H blockers1-receptors ebastine practically does not possess m-holinoblocking activity, and also penetrates poorly into the central nervous system and does not exert a pronounced sedative effect.

    Pharmacokinetics:

    Absorption is 90-95%. Metabolized in the liver, turning into an active metabolite carerebastine. Fatty food accelerates absorption (concentration in the blood increases by 1.5 times) and presystemic metabolism (formation of weightoblastin). Maximum concentration after a single dose of 10 mg is achieved after 2.6-4 hours and is 80-100 ng / ml. The equilibrium concentration is achieved in 3-5 days and is 130-160 ng / ml. Relationship with plasma proteins ebastin and weightoblastin 95%.The half-life of the weight regimen is 15-19 hours, it is excreted by the kidneys 60-70% in the form of conjugates. With renal failure, the elimination half-life increases to 23-26 hours, with liver failure - up to 27 hours.

    Indications:

    Allergic rhinitis (seasonal, perennial), idiopathic chronic urticaria, allergic diseases and conditions caused by an increased release of histamine.

    VII.H10-H13.H10.1   Acute atopic conjunctivitis

    X.J30-J39.J30   Vasomotor and allergic rhinitis

    XII.L50-L54.L50   Hives

    XIX.T66-T78.T78.4   Allergy, unspecified

    Contraindications:

    Pregnancy, lactation, hypersensitivity to piperidine derivatives.

    Carefully:

    Kidney and / or liver failure, lengthening the interval QT, hypokalemia, child (aged 2 - syrup, aged 6 - for tablets).

    Pregnancy and lactation:

    Category by FDA not determined. The safety of use in pregnant and lactating women has not been studied. Not recommended.

    Dosing and Administration:

    Inside regardless of food intake. Adults and children over 12 years of age - 10-20 mg once a day (depending on the severity of the symptoms).

    Side effects:

    Possible: headache, dry mouth, drowsiness.

    Rarely: abdominal pain, dyspepsia, nausea, asthenic syndrome, drowsiness, insomnia, rhinitis, sinusitis.

    Overdose:

    Anticholinergic effects: clumsiness or instability, dryness in the oral cavity, nose or throat, flush of blood to the face, shortness of breath. Anticholinergic effects are less likely compared with diphenhydramine or promethazine.

    CNS depression (drowsiness) or CNS stimulation (hallucinations, convulsions, restless sleep).

    Hypotension.

    Treatment is symptomatic. Do not use respiratory analeptics due to the threat of seizures!

    Interaction:

    It is not recommended simultaneous application with ketoconazole and erythromycin (QT interval prolongation is possible).

    Alcohol and drugs that depress the central nervous system (barbiturates, hypnotics, narcotic analgesics, sedatives, anxiolytics and antipsychotics) -increase CNS depression.

    Allergens used for carrying out skin tests - to cancel antihistamines before carrying out skin tests due to the possibility of false negative results.

    Anticholinergics or other drugs with anticholinergic activity - increased anticholinergic effects, the development of paralytic intestinal obstruction.

    MAO inhibitors, including furazolidone and procarbazine - prolongation and intensification of the inhibitory effect on the central nervous system and the anticholinergic effects of ebastin.

    Means that have ototoxic effect - masking symptoms of ototoxic action, such as tinnitus or dizziness.

    Photosensitizing agents - enhanced photosensitization.

    Special instructions:

    In case of an overdose, do not use respiratory analeptics due to the threat of seizures!

    The drug in therapeutic doses does not affect the ability to drive vehicles and mechanisms.

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