H1-histamine receptor blocker (long-acting). It is the primary active metabolite of loratadine. Inhibits cascade of allergic inflammatory reactions, including release of anti-inflammatory cytokines, including interleukins IL-4, IL-6, IL-8, IL-13, release of pro-inflammatory chemokines (RANTES), 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.
Thereby it prevents development and facilitates the course of allergic reactions, has antipruritic and antiexudative effects, reduces capillary permeability and prevents development of tissue edema and 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. In clinical and pharmacological studies of desloratadine in the recommended therapeutic dose no prolongation of the QT interval on ECG was noted.
The action of the drug starts within 30 minutes after oral administration and lasts for 24 hours.
Absorption
After oral administration, desloratadine is well absorbed from the gastrointestinal tract, with detectable plasma concentrations of desloratadine reached within 30 minutes and a maximum concentration after approximately 3 hours.
Distribution
The binding of desloratadine to plasma proteins is 83-87%. When used in adults and adolescents for 14 days at a dose of 5 mg to 20 mg once daily there is no clinically significant cumulation of desloratadine. Concomitant intake of food or concomitant consumption of grapefruit juice has no effect on the distribution of desloratadine (when taken at a dose of 7.5 mg once daily). It does not penetrate through the blood-brain barrier.
Metabolism
It is subjected to intensive metabolism in the liver by hydroxylation to form 3-OH-desloratadine combined with glucuronide. It is not an inhibitor of CYP3A4 and CYP2D6 isoenzymes and is not a substrate or inhibitor of P-glycoprotein.
Elimation
Only a small portion of the ingested dose is excreted by the kidneys (< 2%) and through the intestine (< 7%). The elimination half-life is 20-30 hours (average – 27 hours).
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Indications
– Allergic rhinitis (elimination or relief of sneezing, nasal congestion, nasal mucus secretion, nasal itching, palate itching, itching and red eyes, lacrimation);
– Urticaria (reduction or elimination of skin itching, rash).
Active ingredient
Composition
Active ingredient:
desloratadine – 5.0 mg.
Additional Ingredients:
calcium hydrophosphate dihydrate – 170.0 mg;
microcrystalline cellulose – 50.0 mg;
Sodium carboxymethyl starch – 6.0 mg;
aspartame – 5.0 mg;
magnesium stearate – 2.4 mg;
colloidal silicon dioxide – 1.6 mg.
How to take, the dosage
Ingestion, regardless of the time of the meal. The tablet should be dissolved in a small amount of water (10-50 ml or ¼ cup), the solution should be stirred before use.
Adults and adolescents over 12 years of age – 1 tablet (5 mg) once a day.
In children 6 to 12 years of age, 1 tablet (2.5 mg) once daily.
In children from 1 to 6 years of age, 1 ½ tablet (1.25 mg to ½ tablet with a dose of 2.5 mg) once daily.
In case of seasonal (intermittent) allergic rhinitis (with symptoms lasting less than 4 days per week or less than 4 weeks per year), the course of the disease should be evaluated. If symptoms disappear, the drug should be stopped; if symptoms reappear, the drug should be resumed.
In case of year-round (persistent) allergic rhinitis (with symptoms lasting more than 4 days per week or more than 4 weeks per year), the drug should be taken for the duration of allergen exposure.
The duration of therapy with the drug should be determined by consulting your doctor.
Interaction
Special Instructions
In the recommended dose the drug does not affect the ability to drive vehicles or operate mechanisms.
The potential for side effects such as dizziness and somnolence must be considered. If the described adverse events occur, the following activities should be avoided.
Contraindications
– Hypersensitivity to desloratadine, other components of the drug or to loratadine,
– pregnancy and breastfeeding,
– children under 1 year of age,
– phenylketonuria.
Side effects
The frequency of side effects is classified according to the World Health Organization recommendations: very frequently – at least 10%; frequently – at least 1%, but less than 10%; infrequently – at least 0.1%, but less than 1%; rarely – at least 0.01%, but less than 0.1%; very rarely – less than 0.01%; the frequency is unknown (according to available data it is impossible to determine the frequency).
Immune system disorders: very rare – itching, rash, including urticaria, angioedema, dyspnea, anaphylaxis.
As to the central nervous system: often – headache, insomnia (in children under 2 years); very rarely – dizziness, somnolence, insomnia, psychomotor hyperactivity, seizures, hallucinations.
Cardiovascular system disorders: very rarely – tachycardia, palpitations, prolongation of QT interval.
Gastrointestinal tract: often – dry mouth, diarrhea (in children under 2 years of age); very rarely – nausea, vomiting, dyspepsia, diarrhea, abdominal pain, increased “liver” enzymes activity, increased concentration of bilirubin, hepatitis.
Skeletal and connective tissue disorders: very rarely – myalgia.
Skin and subcutaneous tissue disorders: very rare – photosensitization.
Others: frequent – increased fatigue, fever (in children younger than 2 years); frequency unknown – asthenia.
Post-registration period
Children: frequency unknown – prolongation of the QT interval, arrhythmia, bradycardia.
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 5 times the recommended dose did not result in any symptoms. In clinical trials, daily use in adults and adolescents in doses up to 20 mg for 14 days was not accompanied by statistically or clinically significant changes in the cardiovascular system.
In a clinical and pharmacological study, the use of desloratadine at a dose of 45 mg daily (9 times the recommended dose) for 10 days did not cause QT interval prolongation and was not accompanied by the occurrence of serious side effects.
Pregnancy use
Similarities
Weight | 0.010 kg |
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Shelf life | 3 years. Do not use after the expiration date. |
Conditions of storage | In the dark place at a temperature not exceeding 25 °С. Store out of the reach of children. |
Manufacturer | Ozon, Russia |
Medication form | dispersible tablets |
Brand | Ozon |
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