Active substanceDesloratadineDesloratadine
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  • Dosage form: & nbspfilm-coated tablets
    Composition:

    1 tablet, film-coated, contains:

    active substance: desloratadine - 5,00 mg;

    Excipients: cellulose microcrystalline - 55.00 mg, corn pregelatinized corn starch - 15.00 mg, mannitol - 22.00 mg, talc - 2.50 mg, magnesium stearate - 0.50 mg;

    film jacket: Fall Light Blue 03F20404 (hypromellose 6sP - 1.90 mg, titanium dioxide (E 171) - 0.61 mg, macrogol 6000 - 0.34 mg, dye indigo carmine aluminum lacquer (E 132) - 0.14 mg) about 3.00 mg.

    Description:

    Round, biconvex tablets, covered with a film shell of blue color, with engraving "LT"on one side.

    Pharmacotherapeutic group:Antiallergic agent - H1-histamine receptor blocker
    ATX: & nbsp

    R.06.A.X   Other antihistamines for systemic use

    R.06.A.X.27   Desloratadine

    Pharmacodynamics:

    An antihistamine long-acting drug, a blocker of peripheral H1-gistaminovyh receptors. Desloratadine is the primary active metabolite of loratadine. Inhibits a cascade of reactions of allergic inflammation, incl. release of pro-inflammatory cytokines, including interleukins IL-4, IL-6.IL-8, IL-13, the release of pro-inflammatory chemokines, the production of superoxide anions by activated polymorphonuclear neutrophils, the adhesion and chemotaxis of eosinophils, the release of adhesion molecules such as P-selectin, IgE - mediated release of histamine, prostaglandin D2 and leukotriene C4. Thus, it prevents development and facilitates the course of allergic reactions, has antipruritic and antiexcudative action, reduces permeability of capillaries, prevents the development of edema of tissues, spasm of smooth muscles.

    The drug has no effect on the central nervous system, has almost no sedative effect (does not cause drowsiness) and does not affect the rate of psychomotor reactions when taking in the recommended doses. In clinicopharmacological studies using desloratadine in the recommended therapeutic dose there was no longer lengthening of the interval QT on an electrocardiogram.

    The action of desloratadine begins within 30 minutes after ingestion and lasts for 24 hours.

    Pharmacokinetics:

    Suction

    After taking the drug inside desloratadine well absorbed from the gastrointestinal tract.It is determined in the blood plasma after 30 minutes, and the maximum concentration in the blood plasma (CmOh) is reached after approximately 3 hours. The bioavailability of desloratadine is dose-proportional when taking a dose in the range from 5 mg to 20 mg.

    Distribution

    The connection with plasma proteins is 83-87%. When used in adults and adolescents for 14 days at a dose of 5 mg to 20 mg once a day, there are no signs of a clinically significant cumulation of desloratadine. The degree of accumulation of desloratadine is consistent with the value of the half-life and frequency of its application once a day. Simultaneous food intake (fatty foods, high-calorie food for breakfast) or grapefruit juice does not affect the distribution of desloratadine (when taken at a dose of 7.5 mg 1 time / day). Does not penetrate the blood-brain barrier.

    Metabolism

    Is not an inhibitor of isoenzymes CYP3A4 in vivo and CYP2D6 in vitro and is not a substrate or an inhibitor of P-glycoprotein. Intensively metabolized in the liver by hydroxylation to form 3-hydroxydeslorotadine, which is then glucuronized.

    Excretion

    The terminal phase of the half-life is about 27 hours.Only a small part of the dose taken internally is excreted by the kidneys (less than 2%) and through the intestine (less than 7%).

    Indications:

    To ease or eliminate symptoms:

    - allergic rhinitis (sneezing, nasal congestion, rhinorrhea, itching in the nose, itching of the palate, itching and redness of the eyes, lacrimation);

    - urticaria (skin itching, rash).

    Contraindications:

    - Phigh sensitivity to desloratadine, other components of the drug or loratadine;

    - pregnancy and the period of breastfeeding;

    - children under 12 years of age (efficacy and safety not established for this dosage form).

    Carefully:

    - Severe renal insufficiency;

    - simultaneous reception of alcohol.

    Pregnancy and lactation:

    The use of the drug in pregnancy is contraindicated due to the lack of clinical data on the safety of its use in this period.

    Desloratadine is excreted in breast milk, therefore its use during breastfeeding is contraindicated.

    Dosing and Administration:

    Inside, regardless of food intake.

    Adults and adolescents (12 years and older) - 1 tablet 5 mg once a day.

    Treatment of seasonal (intermittent) allergic rhinitis (the presence of symptoms lasting less than 4 days a week or less than 4 weeks per year) should be conducted in accordance with the patient's medical history, assessing the course of the disease. With the disappearance of symptoms, the drug should be stopped and resumed after they reappear.

    When year-round (persistent) allergic rhinitis (the presence of symptoms lasting more than 4 days a week or more than 4 weeks per year), long-term treatment is assumed during the entire period of exposure to the allergen.

    Side effects:

    In clinical studies, when taking desloratadine at a recommended dose of 5 mg per day, according to indications, including allergic rhinitis and chronic idiopathic urticaria, adverse reactions were reported in 3% of patients, which exceeded the same value in the placebo group.

    Undesirable reactions noted more often than others and exceeding the occurrence rate in the placebo group: increased fatigue (1.2%), dryness of the oral mucosa (0.8%), headache (0.6%).

    When using desloratadine in adults and adolescents at the recommended dose of 5 mg per day, the incidence of drowsiness is not higher than with placebo.

    Childhood

    In clinical studies involving 578 adolescents from 12 to 17 years, the most common reported headache. It occurred in 5.9% of patients receiving desloratadine and in 6.9% of patients taking placebo.

    The incidence of undesired reactions found during clinical study of desloratadine, which exceeded the frequency of occurrence in the placebo group, as well as other undesirable reactions reported during the post-detection period, are listed below.

    The incidence of adverse events was classified as follows: very often (≥1 / 10), often (≥1 / 100, <1/10), infrequently (≥1 / 1000, <1/100), rarely (≥1 / 10,000 , <1/1000), very rarely (<1/10000, including individual cases), the frequency is unknown (can not be estimated from the available data).

    Disorders of the psyche: very rarely - hallucinations.

    From the nervous system: often - headache; very rarely - dizziness, drowsiness, insomnia, psychomotor hyperactivity, convulsions.

    From the heart: very rarely - tachycardia, palpitation; frequency unknown - interval elongation QT.

    From the gastrointestinal tract: often - dryness of the oral mucosa; very rarely - abdominal pain, nausea, vomiting, indigestion, diarrhea.

    From the liver and bile ducts: very rarely - increased activity of liver enzymes, increased concentrations of bilirubin, hepatitis; frequency is unknown - jaundice.

    From the side of the rut and subcutaneous tissues: frequency unknown - photosensitivity.

    From the osteomuscular system and connective tissue: very rarely - myalgia.

    General disorders and disorders at the site of administration: often - increased fatigue; very rarely - hypersensitivity reactions (such as anaphylaxis, angioedema, dyspnea, pruritus, rash, urticaria); frequency unknown - asthenia.

    Postpayment period

    Childhood: frequency unknown - interval elongation QT, arrhythmia, bradycardia.

    If any of the side effects listed in the instruction are aggravated, or you notice any other side effects not listed in the instructions, inform the doctor about it.

    Overdose:

    Symptoms: taking a dose that exceeded the recommended dose 9 times (45 mg) did not lead to any clinically significant symptoms.

    Treatment: need gastric lavage, reception of activated charcoal; if necessary, symptomatic therapy. Desloratadine is not excreted in hemodialysis, the effectiveness of peritoneal dialysis is not established.

    In case of accidental ingestion of a large amount of the drug, you must immediately consult a doctor.

    Interaction:

    Clinically significant interaction with other drugs was not detected (including azithromycin, ketoconazole, fluoxetine, cimetidine and erythromycin).

    Simultaneous intake of food or grapefruit juice does not affect the effectiveness of the drug.

    Desloratadine does not increase the effect of ethanol on the central nervous system. Nevertheless, during the post-registration use cases of alcohol and alcohol intolerance were reported. therefore desloratadine Alcohol should be used with caution.

    Childhood

    Studies of the interaction of desloratadine were conducted only with the participation of adult patients.

    Special instructions:

    In the case of pronounced impairment of renal function, the drug Desal should be taken with caution (see section "Pharmacokinetics ").

    A study of the effectiveness of desloratadine in rhinitis of infectious etiology was not conducted.

    Effect on the ability to drive transp. cf. and fur:

    Consideration should be given to the potential for the development of side effects such as dizziness and drowsiness. When these undesirable phenomena appear, one should refrain from performing these activities.

    Form release / dosage:

    Tablets, film-coated, 5 mg.

    Packaging:

    10 tablets per blister Al / Al.

    For 1, 2 or 3 blisters together with instructions for medical use in a cardboard box.

    Storage conditions:

    In a dry, protected from light place, at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    2 years.

    Do not use after the expiration date printed on the package.

    Terms of leave from pharmacies:Without recipe
    Registration number:LP-002155
    Date of registration:25.07.2013
    Expiration Date:25.07.2018
    The owner of the registration certificate:Actavis PTS ehf GroupActavis PTS ehf Group Iceland
    Manufacturer: & nbsp
    Representation: & nbspAktavis, Open Company Aktavis, Open Company
    Information update date: & nbsp21.04.2017
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