Desloratadine

Pharmacological properties

desloratadine is a selective blocker of peripheral histamine H1 receptors that does not have a sedative effect. desloratadine is the primary active metabolite of loratadine. the substance does not penetrate the GEB.

Numerous studies have shown that in addition to the antihistamine, desloratadine has an anti-allergic and anti-inflammatory effect. It was found that desloratadine suppresses a cascade of various reactions that underlie the development of allergic inflammation, namely:

• isolation of pro-inflammatory cytokines, including IL-4, IL-6, IL-8, IL-13;
• secretion of pro-inflammatory chemokines such as RANTES;
• production of superoxide anion by activated polymorphonuclear neutrophils;
• adhesion and chemotaxis of eosinophils;
• expression of adhesion molecules such as P-selectin;
• IgE-dependent secretion of histamine, prostaglandin D2 and leukotriene C4;
• acute allergic bronchospasm (in animals).

The safety of desloratadine in children has been demonstrated in 3 clinical studies. The drug was used in children aged 6 months to 11 years who needed antihistamine therapy at a daily dose of 1 mg (age group 6-11 months), 1.25 mg (age group 1 year to 5 years) or 2 5 mg (6–11 years). The treatment was well tolerated, which was confirmed by the results of clinical laboratory tests, the state of vital body functions and ECG data (including the length of the Q – T interval).

During clinical trials, daily use of the drug desloratadine in a dose of up to 20 mg for 14 days was not accompanied by statistically significant clinical changes in the cardiovascular system. During a clinical and pharmacological study, the use of desloratadine 45 mg / day (9 times the therapeutic dose) for 10 days did not cause an extension of the Q – T interval.

When using the recommended dose of 5 mg, the frequency of drowsiness did not exceed that in the placebo group. In clinical trials, desloratadine did not affect psychomotor function when taking doses up to 7.5 mg.

Pharmacokinetics Desloratadine effectively controls symptoms for up to 24 hours. C_max desloratadine in plasma is achieved after an average of 3 hours, T_½ is an average of 27 hours. The degree of cumulation of desloratadine corresponds to its T_½ (about 27 hours) and frequency of use (1 time per day). Desloratadine begins to be detected in blood plasma within 30 minutes after administration.

The bioavailability of desloratadine is proportional to the dose in the range of 5–20 mg.

Desloratadine moderately (83–87%) binds to plasma proteins. When using desloratadine in a dose of 5–20 mg once a day for 14 days, there were no signs of clinically significant cumulation of the drug.

In pharmacokinetic studies in the pediatric population, it was found that AUC and C_max desloratadine (when used in recommended doses) can be equated with those in adults who took desloratadine in the form of syrup in a dose of 5 mg.

Studies have shown that desloratadine does not inhibit CYP 3A4 or CYP 2D6 and is neither a substrate nor an inhibitor of P-glycoprotein.

Food (fatty high-fat breakfast) or grapefruit juice do not affect the distribution of desloratadine.

Indications

To eliminate symptoms associated with:

• allergic rhinitis, such as sneezing, nasal discharge, itching, swelling and nasal congestion, as well as itching and redness of the eyes, lacrimation, itching of the palate and coughing;
• urticaria, such as itching and rashes.

Application

The drug is taken orally, regardless of food intake.

Children aged:

6–11 months: 2 ml of syrup (1 mg of desloratadine) once a day;

1 year – 5 years: 2.5 ml of syrup (1.25 mg of desloratadine) once a day;

6–11 years: 5 ml of syrup (2.5 mg of desloratadine) once a day.

Adults and adolescents over the age of 12 years: 10 ml of syrup (5 mg of desloratadine) 1 time per day.

To correctly measure the dose of the syrup, you should use a metering device attached to the pack (pipette-dispenser, which has a graduated graduation from 0.5 to 2.5 ml).

The duration of treatment depends on the severity of the disease.

Therapy of intermittent allergic rhinitis (the presence of symptoms less than 4 days a week or less than 4 weeks) must be carried out taking into account the anamnesis: stop after the symptoms disappear and resume after their repeated occurrence.

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 throughout the entire period of contact with the allergen.

Contraindications

Hypersensitivity to desloratadine or any auxiliary component of the drug.

Side effects

Usually desloratadine is well tolerated, but sometimes side effects are possible.

Mental disorders: hallucinations.

Nervous system: dizziness, drowsiness, insomnia, psychomotor hyperactivity, cramps, headache.

Cardiovascular system: tachycardia, palpitations.

Digestive tract: dry mouth, diarrhea, abdominal pain, nausea, vomiting, dyspepsia.

Hepatobiliary system: increased activity of liver enzymes, plasma bilirubin levels, hepatitis.

Musculoskeletal system and connective tissue: myalgia.

Immune system: hypersensitivity reactions (including anaphylaxis, Quinckes edema, shortness of breath).

Skin and subcutaneous tissue: itching, rash, and urticaria.

General disorders: fatigue, fever.

special instructions

In patients with severe renal failure, desloratadine should be administered under the supervision of a physician.

The drug contains sorbitol, so it should not be used in patients with congenital fructose intolerance, glucose-galactose malabsorption syndrome, or sucrose-isomaltase deficiency.

Use during pregnancy and lactation. The safety of desloratadine in pregnant women has not been established, so it is not recommended to use it during pregnancy.

Desloratadine passes into breast milk, therefore it is not recommended to use it for women who are breastfeeding.

Children. The effectiveness and safety of desloratadine in children under 6 months of age have not been established.

The ability to influence the reaction rate when driving vehicles or other mechanisms. Patients should be informed that in very rare cases drowsiness may occur, which may affect the ability to drive a car and sophisticated equipment.

Interactions

Clinically significant changes in the plasma concentration of desloratadine with repeated combined use with ketoconazole, erythromycin, azithromycin, fluoxetine, cimetidine were not detected.

Due to the fact that the enzyme responsible for the metabolism of desloratadine has not been established, the possibility of interaction with other drugs cannot be completely excluded.

Desloratadine does not enhance the negative effects of ethanol on psychomotor functions.

Overdose

In case of an overdose, take standard measures aimed at removing the non-adsorbed active substance, apply symptomatic treatment.

When using desloratadine in doses up to 45 mg (9 times higher than recommended) during clinical trials in adults and adolescents, clinically significant effects were not observed.

Desloratadine is not excreted by hemodialysis; the possibility of its excretion by peritoneal dialysis has not been established.

Storage conditions

In the original packaging at a temperature not exceeding 25 ° C.