Pharmacological action – H1-antihistamine, antiallergic, antipruritic.

Pharmacodynamics

Non-sedating long-acting antihistamine. It is the primary active metabolite of loratadine. Suppresses the release of histamine from mast cells. Inhibits the cascade of allergic inflammation reactions, incl. release of pro-inflammatory cytokines, including IL-4, IL-6, IL-8, IL-13, release of adhesion molecules such as P-selectin. Thus, it prevents the development and facilitates the course of allergic reactions, has antipruritic and antiexudative effects, reduces capillary permeability, prevents the development of tissue edema, spasm of smooth muscles.

The drug does not affect the central nervous system, does not cause drowsiness (the use of desloratadine at the recommended dose of 5 mg / day is not accompanied by an increase in the incidence of drowsiness compared with the placebo group) and does not affect the speed of psychomotor reactions. In clinical and pharmacological studies of the use of desloratadine at the recommended therapeutic dose, there was no prolongation of the QT interval.

The action of the drug Erius® begins within 30 minutes after ingestion and lasts for 24 hours.

Pharmacokinetics

Desloratadine is well absorbed from the gastrointestinal tract. It is determined in blood plasma 30 minutes after ingestion. Tmax – an average of 3 hours. Does not penetrate the BBB. Communication with plasma proteins is 83-87%. When used in adults and adolescents for 14 days at a dose of 5 to 20 mg 1 time per day, clinically significant cumulation of the drug is not observed. Simultaneous ingestion of food or grapefruit juice does not affect the distribution of desloratadine when used at a dose of 7.5 mg 1 time per day. Desloratadine is not an inhibitor of CYP3A4 and CYP2D6, a substrate or an inhibitor of P-gp. It is extensively metabolized in the liver by hydroxylation to form 3-OH-desloratadine combined with glucuronide. Only a small part of the oral dose is excreted by the kidneys (<2%) and through the intestines (<7%) unchanged. T1 / 2 on average 27 hours.

Indications

allergic rhinitis (elimination or relief of sneezing, nasal congestion, discharge of mucus from the nose, itching in the nose, itching of the palate, itching and redness of the eyes, watery eyes);

urticaria (reduction or elimination of skin itching, rash).

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