Eslotin (desloratadine) coated tablets 5 mg. № 30

Description

Eslotin Storage
active substance: desloratadine;

1 film-coated tablet contains desloratadine 5 mg;

excipients: calcium hydrogen phosphate, dihydrate; talc; corn starch; microcrystalline cellulose; magnesium stearate;

film coating: Opadry® II Blue 85F20400 (polyvinyl alcohol, polyethylene glycol (macrogol), titanium dioxide (E 171), talc, indigo carmine (E 132)).

Eslotin Dosage form
Film-coated tablets.

Main physical and chemical properties: round biconvex tablets, film-coated, blue with a dividing line on one side.

Pharmacotherapeutic group
Antihistamines for systemic use. ATX code R06A X27.

Pharmacological properties

Pharmacodynamics.

Desloratadine is a long-acting non-sedative antihistamine that has a selective antagonistic effect on peripheral H1 receptors. Following oral administration, desloratadine selectively blocks peripheral histamine H1 receptors and does not enter the central nervous system.

In in vitro studies, desloratadine has demonstrated its anti-allergic and anti-inflammatory properties on endothelial cells. This was manifested by inhibition of the secretion of pro-inflammatory cytokines, such as IL-4, IL-6, IL-8, and IL-13, from human mast cells / basophils, as well as inhibition of the expression of adhesion molecules, such as P-selectin. The clinical significance of these observations remains to be confirmed.

In high-dose studies in which desloratadine was administered daily at doses up to 20 mg for 14 days, no statistically significant changes in the cardiovascular system were observed.

Desloratadine does not enter the central nervous system and does not affect psychomotor function.

In patients with allergic rhinitis, desloratadine effectively relieves symptoms such as sneezing, runny nose and itching, as well as eye irritation, tearing and redness, and itchy palate. Desloratadine effectively controls symptoms for 24 hours.

Eslotin Pharmacokinetics.

Absorption.

The concentration of desloratadine in blood plasma can be determined 30 minutes after ingestion. Desloratadine is well absorbed, the maximum concentration is reached after about 3 hours; the half-life is approximately 27 hours. The degree of accumulation of desloratadine corresponded to its half-life (approximately 27 hours) and frequency of administration once daily. The bioavailability of desloratadine was dose proportional in the range of 5 to 20 mg.

In a pharmacokinetic study in which patient demographics were comparable to the general population with seasonal allergic rhinitis, higher concentrations of desloratadine were observed in 4% of participants. This number may vary depending on ethnicity. The maximum concentration of desloratadine was approximately 3 times higher after approximately 7 hours, the terminal half-life was approximately 89 hours. The safety profile of these patients did not differ from that in the general population.

Distribution.

Desloratadine is moderately bound to plasma proteins (83-87%). At a dose of desloratadine (5 to 20 mg) once a day for 14 days, no signs of clinically significant accumulation of the drug were detected.

Metabolism.

The enzyme responsible for desloratadine metabolism has not yet been identified, so some interactions with other drugs cannot be completely ruled out. Desloratadine does not inhibit CYP3A4 in vivo, in vitro studies have shown that it also does not inhibit CYP2D6, a substrate or inhibitor of P-glycoprotein.

Breeding.

In a study of a single dose of desloratadine at a dose of 7.5 mg meal (fatty high-calorie breakfast) does not affect its pharmacokinetics. It was also found that grapefruit juice also does not affect the pharmacokinetics of desloratadine.

Indication
Elimination of symptoms associated with:

allergic rhinitis (sneezing, runny nose, itching, swelling and nasal congestion, as well as itching and redness of the eyes, tearing, itchy palate and cough);
urticaria (itching, rash).
Contraindication
Hypersensitivity to desloratadine, loratadine or to any of the excipients.