Dezal, 5 mg 30 pcs.

Pharmacotherapeutic group: anti-allergic agent – H1-histamine receptor blocker

ATX code: R06AX27

Pharmacological properties

Pharmacodynamics

A long-acting antihistamine drug, blocker of peripheral H₁-histamine receptors. Desloratadine is the primary active metabolite of loratadine. It inhibits the cascade of allergic inflammatory reactions, including release of pro-inflammatory cytokines, including interleukins IL-4, IL-6, IL-8, IL-13, release of pro-inflammatory chemokines, production of superoxide anions by activated polymorphonuclear neutrophils, eosinophil adhesion and chemotaxis, release of adhesion molecules, such as P-selectin, IgE – mediated release of histamine, prostaglandin D₂ and leukotriene C₄. Thus, it prevents and facilitates the development of allergic reactions, has antipruritic and antiexudative effects, reduces capillary permeability, prevents the development of tissue edema, smooth muscle spasm.

The drug has no effect on the central nervous system, it has practically no sedative effect (does not cause sleepiness) and does not affect the speed of psychomotor reactions when taken in recommended doses. In clinical and pharmacological studies of desloratadine in the recommended therapeutic dose no prolongation of the QT interval on the electrocardiogram was observed.

The action of desloratadine starts within 30 minutes after oral administration and lasts for 24 hours.

Pharmacokinetics

absorption

.p> After oral administration of the drug, desloratadine is well absorbed from the gastrointestinal tract. It is detected in blood plasma after 30 minutes, and the maximum plasma concentration (C_max) is reached after approximately 3 hours. The bioavailability of desloratadine is dose-proportional when administered between 5 mg and 20 mg.

Distribution

The binding to plasma proteins is 83-87%. When administered in adults and adolescents for 14 days at a dose of 5 mg to 20 mg once daily there are no signs of clinically significant cumulation of desloratadine. The degree of accumulation of desloratadine is consistent with the value of the elimination half-life and the frequency of its administration once daily. Simultaneous intake of food (fatty food, high-fat breakfast food) or grapefruit juice does not affect the distribution of desloratadine (when taken at a dose of 7.5 mg once daily). Does not penetrate through the blood-brain barrier.

Metabolism

It is not an inhibitor of CYP3A4 isoenzymes in vivo and CYP2D6 in vitro and is not a substrate or inhibitor of P-glycoprotein. It is intensively metabolized in the liver by hydroxylation to form 3-hydroxydesloratadine, which is then glucuronized.

Elimation

The terminal phase of the half-life is about 27 h. Only a small portion of the oral dose is excreted by the kidneys (less than 2%) and through the intestine (less than 7%).

Indications

Active ingredient

Composition

1 tablet contains:

actingagent: desloratadine – 5.00 mg;

excipients: microcrystalline cellulose – 55.00 mg, pregelatinized corn starch – 15.00 mg, mannitol – 22.00 mg, talc – 2.50 mg, magnesium stearate – 0.50 mg;

film sheath: Opadray Blue 03F20404 (hypromellose 6cP – 1.90 mg, titanium dioxide (E 171) – 0.61 mg, macrogol 6000 – 0.34 mg, indigo carmine aluminum dye (E 132) – 0.14 mg) about 3.00 mg.

How to take, the dosage

Ingestion, regardless of meals.

Adults and adolescents (12 years and older) – 1 tablet of 5 mg once daily.

The treatment of seasonal (intermittent) allergic rhinitis (presence of symptoms lasting less than 4 days per week or less than 4 weeks per year) should be performed according to the patient’s medical history, assessing the course of the disease. If symptoms disappear, the drug should be discontinued and resumed after their reappearance.

In case of year-round (persistent) allergic rhinitis (the presence of symptoms lasting more than 4 days per week or more than 4 weeks per year), long-term treatment for the duration of contact with the allergen is suggested.

Interaction

Clinically significant interaction with other medicinal products (including azithromycin, ketoconazole, fluoxetine, cimetidine and erythromycin) has not been revealed. Simultaneous intake of food or grapefruit juice has no effect on the effectiveness of the drug.

Desloratadine does not increase the effect of ethanol on the central nervous system. Nevertheless, cases of alcohol intolerance and alcohol intoxication have been reported during post-registration use. Therefore, desloratadine should be used with caution simultaneously with alcohol.

Childhood

Interaction studies of desloratadine have only been performed with adult patients.

Special Instructions

Synopsis

Contraindications

Side effects

The most common side effects (≥1/100 to < 1/10), the frequency of which was slightly higher than with placebo (“pacifier”): increased fatigue (1.2%), dry mouth (0.8%), and headache (0.6%).

In children aged 12 to 17 years, the most common side effect in clinical trials was headache (5.9%), the frequency of which was no higher than with placebo (6.9%).

The information on side effects is based on the results of clinical studies and post-registration observations.

The adverse reactions are systematized according to the World Health Organization (WHO) Classification: Very common (≥1/10); common (≥1/100, < 1/10); infrequent (≥1/1000, < 1/100); rare (≥1/10000, < 1/1000); very rare (< 1/10000); frequency unknown (cannot be determined from available data).

Psychiatric: very rare – hallucinations; frequency unknown – abnormal behavior, aggression.

Nervous system disorders:often – headache; very rarely – dizziness, drowsiness, insomnia, psychomotor hyperactivity, seizures.

Hepatic and biliary tract disorders: very rare – increased liver enzyme activity, increased bilirubin concentration, hepatitis; frequency unknown – jaundice.

In the digestive system:often – dry mouth; very rare – abdominal pain, nausea, vomiting, dyspepsia, diarrhea.

Cardiovascular system:very rarely – tachycardia, palpitations; frequency unknown – prolongation of the QT interval.

Motor system disorders:very rarely – myalgia.

Skin and subcutaneous tissue: frequency unknown – photosensitization.

General disorders: frequently, increased fatigue; very rarely, anaphylaxis, angioedema, dyspnea, itching, rash, including urticaria; frequency unknown, asthenia.

Post-registration period

children: frequency unknown – QT interval prolongation, arrhythmia, bradycardia, abnormal behavior, aggression.

If any of the side effects listed in the instructions worsen, or if you notice any other side effects not listed in the instructions, tell your doctor.

Overdose

Symptoms: Taking a dose 9 times the recommended dose (45 mg) did not result in any clinically significant symptoms.

Treatment: Gastric lavage, administration of activated charcoal; symptomatic therapy if necessary. Desloratadine is not excreted by hemodialysis; the effectiveness of peritoneal dialysis has not been established.

In case of accidental ingestion of large amounts of the drug it is necessary to consult a physician immediately.

Pregnancy use

Similarities