Edem (desloratadine) syrup 0.5 mg/ml. 60 ml.

Description

Edem syrup Composition
active substance: desloratadine;

1 ml of syrup contains desloratadine in terms of 100% substance, 0.5 mg;

Edem syrup excipients: sorbitol (E 420); sucrose; sodium hydrogen phosphate dodecahydrate; sodium benzoate (E 211); disodium edetate; propylene glycol; citric acid, monohydrate; sunset yellow FCF (E 110); purified water.

Edem syrup Dosage form
Syrup.

Basic physical and chemical properties: transparent, viscous liquid, orange.

Pharmacotherapeutic group
Antihistamines for systemic use.

ATX code R06A X27

Pharmacodynamics
Desloratadine is a potent selective peripheral histamine H1 receptor blocker that is non-sedating. Desloratadine is the primary active metabolite of loratadine.

After oral administration, Edem selectively blocks peripheral H1-histamine receptors, since the drug almost does not penetrate the blood-brain barrier.

Numerous studies have shown that in addition to antihistamine activity, Eden has demonstrated its anti-allergic and anti-inflammatory properties. It was found that Eden suppresses a cascade of various reactions underlying allergic inflammation, namely:

release of pro-inflammatory cytokines, including IL-4, IL-6, IL-8, IL-13;
the release of pro-inflammatory chemokines such as RANTES;
superoxide anion production by activated polymorphonuclear neutrophils;
eosinophil adhesion and chemotaxis;
the expression of adhesion molecules such as P-selectin;
IgE-dependent release of histamine, prostaglandin D2 and leukotriene C4;
acute allergic bronchospasm and allergic cough in animal studies.
The safety of using Edem for children has been demonstrated in 3 clinical studies. The drug was prescribed to children from 6 months to 11 years old who needed antihistamine therapy, in a daily dose of 1 mg (age group – from 6 to 11 months), 1.25 mg (age group – from 1 to 5 years) or 2, 5 mg (age group 6 to 11 years old). The treatment was well tolerated, which was confirmed by the results of clinical laboratory studies, the state of vital functions of the body and ECG data (including the length of the QT interval).

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

Desloratadine hardly crosses the blood-brain barrier. At the recommended dose of 5 mg, the frequency of drowsiness did not exceed that in the placebo group. In clinical trials, Edem did not affect psychomotor functions when taken up to 7.5 mg.

In addition to the accepted division of allergic rhinitis into seasonal and perennial, allergic rhinitis can also be alternatively classified into intermittent and persistent by the duration of symptoms. Intermittent allergic rhinitis is defined as having symptoms for less than 4 days a week or less than 4 weeks. In the case of persistent allergic rhinitis, symptoms persist for 4 days or more per week or for a period longer than 4 weeks.

The clinical efficacy of Edem in the treatment of seasonal allergic rhinitis has been demonstrated in four multiple dose, placebo-controlled clinical trials.

In patients with allergic rhinitis, Eden effectively eliminated the following symptoms: sneezing, nasal discharge and itching, as well as eye irritation, watery eyes and redness, itching of the palate.

Pharmacokinetics
Desloratadine begins to be detected in plasma within 30 minutes after taking the drug. Edem effectively controls symptoms within 24 hours. Desloratadine is well absorbed. The maximum concentration of desloratadine in plasma Cmax is achieved on average after 3 hours, the half-life is on average 27 hours. The degree of cumulation of desloratadine corresponds to its half-life (approximately 27 hours) and the 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 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 drug were detected.

A low metabolic rate of desloratadine was observed in about 8% of subjects, in which there was a significant increase in plasma levels of the drug and a lengthening half-life. The prevalence of metabolic slowdowns may be due to race. This fact is still considered clinically irrelevant.

When conducting cross-comparative studies with the same dose of the drug, bioequivalence of the drug in the form of tablets and syrup was found.

When conducting

Pharmacokinetic studies in pediatric practice revealed that AUC and Cmax of desloratadine (when used in recommended doses) can be equated to those 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 CYP3A4 or CYP2D6 and is neither a substrate nor an inhibitor of P-glycoprotein.

Edem syrup Indications
For the relief of symptoms associated with allergic rhinitis, such as sneezing, nasal discharge, itching, swelling and nasal congestion, as well as itchy and red eyes, watery eyes, itchy palate and coughing.

For the relief of symptoms associated with hives, such as itching and rashes.

Contraindications
Hypersensitivity to desloratadine, to any auxiliary component of the drug, or to loratadine.