Pharmacodynamics. Desloratadine is a long-acting non-sedative antihistamine that selectively antagonizes peripheral h1 receptors. After oral administration, desloratadine selectively blocks peripheral histamine h1 receptors.
In in vitro studies, desloratadine has demonstrated its anti-allergic properties on endothelial cells. This was manifested by inhibition of the release of anti-inflammatory cytokines, such as interleukin (IL) -4, -6, -8, and -13, from human mast cells / basophils, as well as inhibition of the expression of adhesion molecules such as P-selectin.
The results of numerous studies indicate that, in addition to antihistamine activity, desloratadine has antiallergic and anti-inflammatory effects. Desloratadine does not cause changes in the cardiovascular system, does not penetrate into the central nervous system and does not affect psychomotor function.
In patients with allergic rhinitis, desloratadine effectively relieves symptoms such as sneezing, nasal discharge and itching, as well as eye irritation, watery eyes and redness, and itchy palate. Desloratadine effectively controls symptoms within 24 hours.
Pharmacokinetics. Plasma concentration of desloratadine can be determined 30 minutes after administration. Desloratadine is well absorbed, Cmax is reached after about 3 hours; T½ ≈27 hours. The degree of desloratadine cumulation corresponded to its T½ (≈27 hours) and the frequency of taking 1 time per day. The bioavailability of desloratadine was dose proportional, ranging from 5 to 20 mg. Desloratadine binds moderately to blood plasma proteins (83–87%). When using desloratadine at a dose of 5 to 20 mg once a day for 14 days, no signs of clinically significant cumulation of the preparation were detected.
Food (fatty high-calorie breakfast) does not affect the pharmacokinetics of desloratadine. It was also found that grapefruit juice does not affect the pharmacokinetics of desloratadine.
Elimination of symptoms associated with allergic rhinitis (sneezing, nasal discharge, itching, swelling and nasal congestion, itching and redness of the eyes, watery eyes, itching in the palate and cough), hives (itching, rash).
For adults and children over the age of 12, the preparation is prescribed in a dose of 5 mg (1 tablet) 1 time per day, regardless of food intake. the preparation is recommended to be taken regularly at the same time of day. the tablet must be swallowed whole, without chewing and with a little water. the duration of treatment depends on the severity and course of the disease.
Treatment for intermittent allergic rhinitis (the presence of symptoms less than 4 days a week or less than 4 weeks) should be carried out taking into account the anemnesis data: stop after the symptoms disappear and resume after their recurrence. With persistent allergic rhinitis (the presence of symptoms more than 4 days a week or more than 4 weeks), it is necessary to continue treatment during the entire period of contact with the allergen.
Hypersensitivity to the active substance or to any component of the preparation, or to loratadine.
Desloratadine is usually well tolerated, but side effects are sometimes possible.
Mental disorders: hallucinations.
From the nervous system: headache, dizziness, drowsiness, insomnia, psychomotor hyperactivity, convulsions.
From the heart: tachycardia, palpitations.
From the digestive tract: dry mouth, diarrhea, abdominal pain, nausea, vomiting, dyspepsia.
From the hepatobiliary system: increased activity of liver enzymes, increased bilirubin levels, hepatitis.
From the musculoskeletal system and connective tissue: myalgia.
General disorders: hypersensitivity reactions (including anaphylaxis, angioedema, shortness of breath, itching, rash and urticaria), increased fatigue.
In patients with high-grade renal insufficiency, Edem should be administered under the supervision of a physician. patients with rare hereditary manifestations of galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome should not take this preparation.
Clinically significant changes in the concentration of the preparation in the blood plasma during repeated combined use with ketoconazole, erythromycin, azithromycin, fluoxetine, cimetidine were not revealed. due to the fact that the enzyme responsible for the metabolism of desloratadine has not been established, the likelihood of interaction with other preparations cannot be completely excluded.
In clinical and pharmacological studies, desloratadine, which was taken together with alcohol, did not enhance the negative effect of ethanol on psychomotor function.
In case of overdose, standard measures should be taken to remove the unabsorbed active substance. symptomatic and supportive treatment is recommended. in clinical studies where desloratadine was administered in doses of 45 mg (9 times the recommended), clinically significant adverse reactions were not observed. desloratadine is not excreted by hemodialysis; the possibility of its removal during peritoneal dialysis has not been established.
In its original packaging at a temperature not exceeding 25 ° c.
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