Blogir-3 tablets 5 mg No. 10
Composition
Active ingredient: desloratadine;
1 tablet contains 5 mg of desloratadine;
Excipients: polacrilin potassium; citric acid, monohydrate; iron oxide red (E 172); magnesium stearate; liquid flavoring with tutti-frutti flavor; croscarmellose sodium; aspartame (E 951); microcrystalline cellulose; mannitol (E 421).
Dosage form
Orodispersible tablets.
Main physicochemical properties: round, flat tablets of brownish-pink color with inclusions, with beveled edges and embossed "5" on one side.
Pharmacotherapeutic group
Antihistamines for systemic use.
ATX code R06A X27.
Pharmacological properties
Pharmacodynamics.
Desloratadine is a long-acting, non-sedating antihistamine that selectively antagonizes 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 relevance 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. In controlled clinical trials, the incidence of drowsiness at the recommended dose of 5 mg/day was not different from that observed with placebo. In clinical trials, a single dose of desloratadine at a daily dose of 7.5 mg had no effect on 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 that were 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 other forms of urticaria, including chronic idiopathic urticaria.
Pharmacokinetics.
Absorption.
Desloratadine plasma concentrations can be determined 30 minutes after administration. Desloratadine is well absorbed, with peak concentrations occurring approximately 3 hours after dosing; the elimination half-life is approximately 27 hours. The extent of accumulation of desloratadine was consistent with its elimination half-life (approximately 27 hours) and once-daily dosing. The bioavailability of desloratadine was dose-proportional over the range of 5 to 20 mg.
In a pharmacokinetic study in which the demographics of the patients were comparable to the general population with seasonal allergic rhinitis, 4% of the subjects had higher desloratadine concentrations. 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 of the general population.
Distribution.
Desloratadine is moderately bound to plasma proteins (83-87%). When desloratadine doses (5 to 20 mg) are administered once daily for 14 days, there is no evidence of clinically significant drug accumulation.
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.
Breeding.
In a single-dose study of desloratadine 7.5 mg, food intake (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.
Indication
Elimination of symptoms associated with:
allergic rhinitis (see section "Pharmacological properties");
urticaria (see section "Pharmacological properties").
Contraindication
Hypersensitivity to desloratadine or to any of the other ingredients of the drug, or to loratadine.
Interaction with other medicinal products and other types of interactions
In 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 the drug. Therefore, caution should be exercised when using alcohol during treatment.
Application features
In patients with severe renal impairment, desloratadine should be administered under medical supervision. Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine. Patients with phenylketonuria should not take this medicine due to the aspartame content. This medicine contains less than 1 mmol sodium, i.e. is essentially sodium-free.
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 (see section 4.8). The physician should consider discontinuing desloratadine in patients who experience a seizure while taking the drug.
Use during pregnancy or breastfeeding
Desloratadine has not been shown to be teratogenic in animal studies. The safety of the drug during pregnancy has not been established, therefore the use of desloratadine during pregnancy is not recommended.
Breast-feeding
Desloratadine passes into breast milk, so the use of the drug in women who are breastfeeding is not recommended.
Ability to influence reaction speed when driving vehicles or other mechanisms
In clinical trials evaluating the ability to drive, no impairment was observed in patients taking desloratadine. However, patients should be informed that very rarely some people experience drowsiness, which may affect their ability to drive or operate machinery.
Method of administration and doses
Adults and adolescents (12 years of age and older) should take 1 tablet once daily, with or without food, to relieve symptoms associated with allergic rhinitis (including intermittent and persistent allergic rhinitis) and urticaria. Do not take with water or other liquids. The tablet should be taken immediately after opening the blister.
Treatment of intermittent allergic rhinitis (presence of symptoms less than 4 days per week or less than 4 weeks) should be carried out taking into account the anamnesis: stop after the symptoms disappear and resume after their reappearance.
In case of 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 section 4.8).
The efficacy and safety of desloratadine in children under 12 years of age have not been established.
Overdose
In case of overdose, standard measures should be taken to remove unabsorbed active substance. Symptomatic and supportive treatment is recommended. In clinical studies in which desloratadine was administered at doses of 45 mg (9 times the recommended dose), no clinically significant adverse reactions were observed. Desloratadine is not removed by hemodialysis, and its removal by peritoneal dialysis has not been established.
Side effects
In clinical trials in indications including allergic rhinitis and chronic idiopathic urticaria, adverse reactions were reported 3% more frequently in patients receiving 5 mg daily than in patients receiving placebo. The most frequently reported adverse reactions 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, occurring in 5.9% of patients receiving desloratadine and 6.9% of patients receiving 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.
Other adverse reactions occurring with the use of the drug, which were reported very rarely during the post-marketing period, are classified by organ system and frequency of their occurrence: very common (≥1/10); common (≥1/100 - <1/10); uncommon (≥1/1000 - <1/100); rare (≥1/10000 - <1/1000); very rare (<1/10000); frequency unknown (cannot be estimated due to limited available data).
From the psyche
Very rare: hallucinations.
Frequency unknown: abnormal behavior, aggression, depressed mood.
From the nervous system
Common: headache.
Very rare: dizziness, drowsiness, insomnia, psychomotor hyperactivity, convulsions.
Cardiovascular system
Very rare: tachycardia, rapid heartbeat.
Frequency unknown: QT prolongation, supraventricular tachyarrhythmia.
Gastrointestinal tract Common: dry mouth.
Very rare: abdominal pain, nausea, vomiting, dyspepsia, diarrhea.
Liver and biliary tract disorders
Very rare: increased liver enzymes, increased bilirubin, hepatitis.
Frequency unknown: jaundice.
From the organs of vision
Frequency unknown: dry eyes.
Musculoskeletal and connective tissue disorders
Very rare: myalgia
Skin and subcutaneous tissue disorders
Frequency unknown: photosensitivity
General violations
Common: increased fatigue.
Very rare: hypersensitivity reactions (such as anaphylaxis, angioedema, dyspnoea, pruritus, rash and urticaria).
Frequency unknown: asthenia.
Research results
Frequency unknown: weight gain.
Metabolism and nutrition
Frequency unknown: increased appetite.
An increased incidence of seizures has been reported in patients aged 0 to 19 years after the use of desloratadine. Among children aged 0-4 years, the increase was 37.5 per 100,000 patient-years, while for patients aged 5-19 years, the rate was 11.3 per 100,000 patient-years (see section 4.4).
Reporting of suspected adverse reactions
Reporting suspected adverse reactions after the marketing authorisation of a medicinal product is an important procedure. It allows for continued monitoring of the benefit-risk balance of the medicinal product in question. Healthcare professionals should report any suspected adverse reactions via the national reporting system.
Expiration date
3 years.
Storage conditions
Store at a temperature not exceeding 25 °C.
Keep out of reach of children.
Packaging
10 tablets in a blister. 1 or 3 blisters in a cardboard pack.
Vacation category
Without a prescription.
Producer
Belupo, medicines and cosmetics, etc.
Location of the manufacturer and address of its place of business.
Danica Street 5, 48000 Koprivnica, Croatia.
