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Desloratadine film-coated tablets 5 mg
Instruction
For medical use of the medicinal product
Desloratadine
(Desloratadine)
Composition:
Active ingredient: desloratadine;
1 film-coated tablet contains 5 mg of desloratadine;
Excipients: calcium hydrogen phosphate dihydrate, microcrystalline cellulose, corn starch, talc, carnauba wax, white wax, lactose, hypromellose, titanium dioxide (E 171), polyethylene glycol, indigo carmine (E 132).
Dosage form.
The pills are coated.
Main physicochemical properties: round, coated tablets, blue in color with convex upper and lower surfaces. When broken, a core surrounded by a single solid layer is visible under a magnifying glass.
Pharmacotherapeutic group.
Antihistamines for systemic use. other antihistamines for systemic use. desloratadine.
ATX code R06A X27.
Pharmacological properties.
Pharmacodynamics.
Desloratadine is a long-acting, non-sedating antihistamine that has selective antagonistic effects on peripheral H1 receptors. After oral administration, desloratadine selectively blocks peripheral histamine H1 receptors.
In vitro studies have shown that desloratadine has anti-allergic and anti-inflammatory properties on endothelial cells. This was demonstrated by inhibition of the release 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 clinical studies in which desloratadine was administered daily at a dose of up to 20 mg for 14 days, no statistically significant changes in the cardiovascular system were observed. In a clinical pharmacology study with the use of 45 mg per day (10 times the maximum daily clinical dose) for 10 days, no prolongation of the QT interval was observed.
In patients with allergic rhinitis, desloratadine effectively relieved symptoms such as sneezing, nasal discharge and itching, as well as eye irritation, tearing and redness, and itching of the palate. Desloratadine effectively controlled symptoms for 24 hours.
Desloratadine has little or no penetration into the central nervous system (CNS). In controlled clinical trials, the incidence of drowsiness at the recommended dose of 5 mg/day was no different from that of placebo. In clinical trials, a single dose of desloratadine at a daily dose of 7.5 mg did not affect psychomotor performance.
Desloratadine effectively alleviates the severity of seasonal allergic rhinitis as measured by the Rhinoconjunctivitis Quality of Life Questionnaire. The greatest improvement was observed in the questionnaire items related to practical problems and daily activities limited by symptoms.
Chronic idiopathic urticaria has been studied in a clinical model of urticaria conditions. Since histamine release is a causal factor in all forms of urticaria, desloratadine is expected to be effective in relieving symptoms in forms of urticaria other than chronic idiopathic urticaria.
In two placebo-controlled 6-week studies in patients with chronic idiopathic urticaria, desloratadine was effective in relieving pruritus and reducing the number and size of hives by the end of the first dosing interval. In each study, the effect was maintained throughout the 24-hour dosing interval. Itch relief of more than 50% was observed in 55% of patients taking desloratadine, compared with 19% of patients taking placebo.
Taking the drug does not have a significant effect on sleep and daytime activity.
Pharmacokinetics.
Absorption.
Desloratadine plasma concentrations can be determined 30 minutes after administration. Desloratadine is well absorbed, with peak concentrations occurring approximately 3 hours after administration; the elimination half-life is approximately 27 hours. The extent of desloratadine accumulation was consistent with its elimination half-life (approximately 27 hours) and once-daily dosing. The bioavailability of desloratadine was dose-proportional over the 5 to 20 mg range.
In a pharmacokinetic study in which the demographics of the patients were comparable to the general population with seasonal allergic rhinitis, 4% of the participants had higher concentrations of desloratadine. This number may vary depending on ethnicity. The maximum concentration of desloratadine was approximately 3-fold higher after approximately 7 hours, and 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%). When using desloratadine doses (from 5 to 20 mg) once a day for 14 days, there were no signs of clinically significant cumulation of the drug.
Biotransformation
The enzyme responsible for the metabolism of desloratadine has not yet been identified, therefore some interactions with other drugs cannot be completely excluded. Desloratadine does not inhibit CYP3A4 in vivo, in vitro studies have shown that the drug does not inhibit CYP2D6, a substrate or inhibitor of P-glycoprotein.
In a single-dose study of desloratadine 7.5 mg, food (a high-fat, high-calorie breakfast) did not affect the pharmacokinetics of desloratadine. Grapefruit juice was also found to have no effect on the pharmacokinetics of desloratadine.
Clinical characteristics.
Indication.
Elimination of symptoms associated with:
allergic rhinitis (see section "Pharmacological properties"); urticaria (see section "Pharmacological properties").
Contraindication.
Increased individual sensitivity to desloratadine, loratadine and any component of the drug.
Interaction with other drugs and other types of interactions.
In clinical studies of desloratadine tablets, no clinically significant interactions were observed when erythromycin or ketoconazole were co-administered.
In these clinical and pharmacological studies, when the drug was used together with alcohol, no increase in the negative effect of ethanol on psychomotor function was noted. However, in the post-registration period, cases of alcohol intolerance and alcohol intoxication were observed during the use of desloratadine. Therefore, caution should be exercised when using alcohol during treatment with the drug.
Due to the fact that the enzyme responsible for the metabolism of desloratadine has not been identified, interactions with other drugs cannot be completely ruled out.
Application features.
The use of the drug in patients with severe renal failure should be carried out under the supervision of a physician.
Desloratadine should be used with caution in patients with a history of seizures. Children may be more susceptible to developing a new seizure during treatment with desloratadine. The physician should consider discontinuing desloratadine in patients who experience a seizure while taking the drug.
Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.
Use during pregnancy or breastfeeding.
Desloratadine has not been shown to be teratogenic in animal studies.
The safety of the drug for use in pregnant women has not been established, therefore it is not recommended to use desloratadine during pregnancy.
Breastfeeding.
Desloratadine passes into breast milk, so women who are breastfeeding should not use desloratadine.
The ability to influence the reaction speed when driving vehicles or other mechanisms.
In clinical studies evaluating the ability to drive, no impairment was observed in patients taking desloratadine. However, patients should be informed of the possibility of drowsiness, which may affect their ability to drive and operate machinery.
Method of administration and doses.
The drug is taken orally.
Adults and children over 12 years of age should take 1 tablet (5 mg) once a day, regardless of meals, to relieve symptoms associated with allergic rhinitis (including intermittent and persistent allergic rhinitis) and urticaria.
Treatment of intermittent allergic rhinitis (presence of symptoms less than 4 days a week or less than 4 weeks) should be carried out taking into account the anamnesis: stop after the disappearance of symptoms and resume after their reappearance. With persistent allergic rhinitis (presence of symptoms more than 4 days a week or more than 4 weeks), treatment should be continued throughout the entire period of contact with the allergen.
Children.
There are limited clinical trial data on the efficacy of desloratadine tablets in adolescents aged 12 to 17 years (see Adverse Reactions section).
The efficacy and safety of the drug for children under 12 years of age have not been established.
Children over 12 years of age can use the drug after consulting a doctor.
Overdose.
In case of overdose, use standard measures aimed at removing unabsorbed active substance, apply symptomatic treatment.
When using desloratadine in doses up to 45 mg (9 times the recommended dose), no clinically significant effects were observed in studies in adults and adolescents.
Desloratadine is not removed by hemodialysis; its removal by peritoneal dialysis has not been established.
Adverse reactions.
In clinical trials in indications including allergic rhinitis and chronic idiopathic urticaria, adverse events were reported 3% more frequently in patients receiving 5 mg daily than in patients receiving placebo.
The most commonly reported side effects compared to placebo were fatigue (1.2%), dry mouth (0.8%), and headache (0.6%).
Children: In clinical trials involving 578 adolescents aged 12 to 17 years, the most common adverse reaction was headache; it occurred in 5.9% of patients taking desloratadine and in 6.9% of patients taking placebo.
There is a risk of psychomotor hyperactivity (abnormal behavior) associated with the use of desloratadine (which may manifest as anger and aggression, as well as agitation).
In the post-marketing period, the following events were observed (frequency unknown): QT prolongation, arrhythmias and bradycardia.
The frequency of adverse reactions is classified as follows: very common (≥1/10), common (≥1/100,
| Organ classes/systems | frequency of occurrence | adverse reactions |
| mental disorder | very rarely | hallucinations |
| From the nervous system | often | headache |
| very rarely | dizziness, drowsiness, insomnia, psychomotor hyperactivity, convulsions |
| From the heart | very rarely | tachycardia, rapid heartbeat |
| frequency unknown | QT prolongation, supraventricular tachyarrhythmia |
| Gastrointestinal tract | often | dry mouth |
| very rarely | abdominal pain, nausea, vomiting, dyspepsia, diarrhea |
| Liver and biliary tract disorders | very rarely | increased liver enzymes, increased bilirubin, hepatitis |
| frequency unknown | jaundice |
| Musculoskeletal and connective tissue disorders | very rarely | myalgia |
| Skin and subcutaneous tissue disorders | frequency unknown | photosensitivity |
| general disorders | often | increased fatigue |
| very rarely | hypersensitivity reactions (such as anaphylaxis, angioedema, shortness of breath, itching, rash and urticaria) |
| frequency unknown | asthenia |
| Metabolic and nutritional disorders | frequency unknown | increased appetite |
| research | frequency unknown | weight gain |
Expiration date.
2 years.
Storage conditions.
Store in original packaging at a temperature not exceeding 25 degrees Celsius, out of the reach of children.
Packaging.
10 tablets in a blister; 1 or 3 blisters in a cardboard pack.
Vacation category.
Without a prescription.
Producer.
Ciao "technologist".
Location of the manufacturer and address of its place of business.
Ukraine, 20300, Cherkasy region, Uman city, Stara Prorizna Street, Building 8.
Desloratadine syrup 0.5 mg/ml
Instruction
For medical use of the medicinal product
Desloratadine
(Desloratadine)
Composition:
Active ingredient: desloratadine;
1 ml of syrup contains 0.5 mg of desloratadine;
excipients: propylene glycol; sorbitol solution non-crystallizing
