Blogir-3, 0.5 mg/ml 60 ml

Pharmacodynamics

A non-sedative long-acting antihistamine. It is the primary active metabolite of loratadine. It selectively blocks the activity of peripheral H1 histamine receptors. Suppresses the release of histamine from mast cells. Inhibits the cascade of allergic inflammatory reactions, including release of anti-inflammatory cytokines, including interleukins IL-4, IL-6, IL-8, IL-13, release of adhesion molecules, such as P-selectin. Thus it prevents and facilitates allergic reactions, has antipruritic and antiexudative effects, decreases capillary permeability, prevents development of edema, spasm of smooth muscles.

The drug has no effect on the central nervous system, practically does not have a sedative effect (does not cause drowsiness) and does not affect psychomotor reactions. It does not cause prolongation of QT interval on ECG.

Pharmacokinetics

Absorption
After oral administration desloratadine is well absorbed in the gastrointestinal tract, determined in blood plasma 30 min after oral administration. Maximal concentration Cmax is reached after about 3 hours.

Distribution

Binding of desloratadine to 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 no signs of clinically significant cumulation of desloratadine were found. Simultaneous intake of food or grapefruit juice has no effect on the distribution of desloratadine (when administered at a dose of 7.5 mg once daily). Does not penetrate through the blood-brain barrier.

Metabolism
Subjected to intensive metabolism in the liver by hydroxylation to form 3-ON-desloratadine combined with glucuronide. It is not an inhibitor of CYP3A4 and CYP2D6 isoenzymes and is not a substrate or inhibitor of P-glycoprotein.

Excretion
Desloratadine is excreted as glucuronide compound and in small amount (less than 2%) by kidneys and through intestine (less than 7%) in unchanged form. The elimination half-life T1/2 is on average 27 h.

Indications

– Allergic rhinitis (elimination or relief of sneezing, nasal congestion, nasal mucus secretion, nasal itching, palate itching, itching and red eyes, lacrimation);

– Urticaria (reduction or elimination of skin itching, rash).

Active ingredient

Desloratadine

Composition

1 ml of the syrup contains: active ingredient: desloratadine 0.5 mg.

Auxiliary substances: propylene glycol 150.0 mg, sorbitol 150.0 mg, hypromellose 3.5 mg, sucralose 2.0 mg, sodium citrate 1.26 mg, tutti-frutti flavoring (flavoring agents, propylene glycol E1520) 0.75 mg, citric acid 0.5 mg, water – q.s.

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How to take, the dosage

Orally, regardless of meals, with a small amount of water.

Children aged 1 to 5 years: 1.25 mg (2.5 ml syrup) once a day; children aged 6 to 11 years: 2.5 mg (5 ml syrup) once a day; adolescents and adults over 12 years: 5 mg (10 ml syrup) once a day.

In case of seasonal (intermittent) allergic rhinitis (with symptoms lasting less than 4 days per week or less than 4 weeks per year) it is necessary to evaluate the disease course. In case of symptoms disappearance the drug shall be stopped, in case of recurrent symptoms the drug administration shall be renewed.

In case of year-round (persistent) allergic rhinitis (in the presence of symptoms lasting for more than 4 days a week or more than 4 weeks a year) the drug shall be taken during the whole period of allergen exposure.

Interaction

No clinically significant changes in plasma concentrations of desloratadine were found during multiple co-administration of desloratadine with ketoconazole, erythromycin, azithromycin, fluoxetine and cimetidine. BLOGIR-3® does not increase the effect of alcohol on the central nervous system.

Food intake has no effect on the effectiveness of the drug.

Special Instructions

Use in pediatrics
The efficacy and safety of using BLOGIR-3® syrup in children under 1 year of age has not been established.
In most cases rhinitis in children under 2 years of age is of infectious nature. Studies of desloratadine efficacy in rhinitis of infectious etiology have not been conducted.

Differential diagnosis between allergic rhinitis and rhinitis of other origin in children under 2 years of age is very difficult. When making the differential diagnosis one should pay attention to the presence or absence of foci of infection or structural abnormalities of the upper airways, conduct a thorough history taking, examination as well as appropriate laboratory tests and skin tests.

Effect on the ability to drive vehicles and mechanisms
In the recommended dose the drug does not affect the ability to drive vehicles or mechanisms. Nevertheless, in very rare cases, some patients may experience somnolence while taking desloratadine, which may affect their ability to drive vehicles or operate mechanisms.

Contraindications

Hypersensitivity to the drug components; pregnancy and lactation; age less than 1 year; hereditary fructose intolerance (due to the presence of sorbitol in the drug).