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
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
Interaction
Special Instructions
Contraindications
Side effects
Overdose
Pregnancy use
The use of the drug BLOGIR-3® Syrup during pregnancy is contraindicated due to the lack of clinical data on the safety of its use during this period.
Desloratadine is excreted with breast milk, so the use of the drug during breast-feeding is contraindicated.
Similarities
Weight | 0.145 kg |
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Shelf life | 3 years. |
Conditions of storage | Store at a temperature not exceeding 25 °C. Store out of the reach of children! |
Manufacturer | Bayer Bitterfeld GmbH, Germany |
Medication form | oral solution |
Brand | Bayer Bitterfeld GmbH |
Other forms…
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