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Pharmacodynamics. Desloratadine is a selective peripheral histamine h1 receptor blocker that does not induce sedation. desloratadine is the primary active metabolite of loratadine. after oral administration, it selectively blocks peripheral h1-histamine receptors.

In addition to antihistamine activity, desloratadine has anti-allergic and anti-inflammatory effects. It was found that desloratadine inhibits a cascade of various reactions underlying the development of allergic inflammation, namely:

The safety of using desloratadine in children has been demonstrated in three clinical studies. The preparation was prescribed to children aged 6 months to 11 years who needed antihistamine therapy in a daily dose of 1 mg (age group 6 to 11 months), 1.25 mg (from 1 to 5 years) or 2.5 mg ( from 6 to 11 years old). The treatment was well tolerated, which was confirmed by the results of clinical laboratory tests, the state of vital functions of the body and ECG data (including the duration of the Q – T interval).

During clinical studies, the daily use of desloratadine at a dose of up to 20 mg for 14 days was not accompanied by statistically significant clinical changes in the cardiovascular system. In the course of a clinical and pharmacological study, the use of desloratadine 45 mg / day (9 times higher than the therapeutic dose) for 10 days did not cause an extension of the Q – T interval.

Desloratadine does not penetrate the BBB. With the recommended dose of 5 mg, the frequency of sleepiness did not exceed that in the placebo group. In clinical trials, desloratadine did not affect psychomotor function at doses up to 7.5 mg.

Pharmacokinetics. Desloratadine begins to be determined in blood plasma within 30 minutes after application. Eden effectively controls symptoms within 24 hours. Cmax of desloratadine in blood plasma is achieved on average after 3 hours, T½ is an average of 27 hours. The degree of desloratadine cumulation corresponds to its T½ (≈27 hours) and frequency of use (1 time per day). The bioavailability of desloratadine was dose proportional, ranging from 5 to 20 mg.

Desloratadine moderately (83–87%) binds to blood plasma proteins. When using desloratadine in a dose of 5 to 20 mg once a day for 14 days, no signs of clinically significant cumulation of the preparation were detected.

When conducting pharmacokinetic studies in pediatric practice, it was found that the AUC and Cmax of desloratadine (when used in recommended doses) can be equated to the same indicators in adults who took desloratadine in the form of a syrup at a dose of 5 mg.

Research results have shown that desloratadine does not inhibit CYP 3A4 or CYP 2D6 and is neither a substrate nor an inhibitor of P-glycoprotein.

Food (high-fat, high-calorie breakfast) or grapefruit juice does not affect the distribution of desloratadine.

For the elimination of symptoms associated with allergic rhinitis, such as sneezing, nasal discharge, itching, swelling and nasal congestion, as well as itching and redness of the eyes, watery eyes, itchy palate and cough; to relieve symptoms associated with hives, such as itching and rashes.

The preparationis taken orally, regardless of food intake.

Children: from 6 to 11 months: 2 ml of syrup (1 mg of desloratadine) 1 time per day;

from 1 to 5 years: 2.5 ml of syrup (1.25 mg of desloratadine) once a day;

from 6 to 11 years: 5 ml of syrup (2.5 mg of desloratadine) 1 time per day.

Adults and adolescents from 12 years old: 10 ml of syrup (5 mg desloratadine) 1 time per day.

For dosing the preparation, it is recommended to use a dosing spoon or a dosing cup with appropriate divisions.

The duration of treatment depends on the severity and course of the disease.

Treatment of intermittent allergic rhinitis (the presence of symptoms less than 4 days a week or less than 4 weeks) should be carried out taking into account the history data: stop after the disappearance of symptoms and resume after their recurrence. With persistent allergic rhinitis (the presence of symptoms more than 4 days a week or more than 4 weeks), it is necessary to continue treatment throughout the entire period of contact with the allergen.

Hypersensitivity to desloratadine or any other component of the preparation.

Desloratadine is generally well tolerated, but side effects are sometimes possible.

From the side of the psyche: hallucinations.

From the nervous system: headache, dizziness, drowsiness, insomnia, psychomotor hyperactivity, convulsions.