Aerius 5mg 20 tablets

Form

tableti

Dosage mg

5

Pack

20

AERIUS film-coated tablets 5 mg 1. Medical Product Name AERIUS film-coated tablets 5 mg 2. Qualitative and Quantitative Composition Active substance Desloratadine 5 mg Excipient(s) Lactose monohydrate (animal origin) 5.8 mg For a full list of excipients, see section 6.1 3. Pharmaceutical Form Film-coated tablet AERIUS 5 mg film-coated tablet is a light blue, round, flat tablet. It is marked with "SP" on one side. See blog: AERIUS - anti-allergy, antihistamine 4. Clinical Features 4.1. Therapeutic Indications AERIUS is indicated for the relief of symptoms associated with allergic rhinitis, such as sneezing, nasal discharge and itching, nasal congestion/stuffiness, as well as itchy, watery, and red eyes, itchy palate, and cough. AERIUS is also indicated for the relief of symptoms associated with urticaria, such as relief of itching, rash, and redness. 4.2 Dosage and Method of Administration Dosage/Frequency of Use and Duration Adolescents and Adults over 12 years of age The recommended dose of AERIUS is one tablet once daily. For intermittent allergic rhinitis with symptoms occurring less than 4 days per week or less than 4 weeks per year, treatment should be based on medical history, should be discontinued when symptoms disappear and resumed upon their reappearance. For persistent allergic rhinitis with symptoms occurring more than 4 days per week or more than 4 weeks per year, treatment should be continued throughout the period of allergen exposure. Method of Administration It is administered orally. The dose can be taken with or without food. Additional Information on Special Populations Hepatic Insufficiency No data are available in patients with impaired liver function. Renal Insufficiency AERIUS should be used with caution in patients with severe renal impairment. Pediatric Population The efficacy and safety of AERIUS in the pediatric population under 12 years of age have not yet been established. Clinical trial experience regarding the efficacy of desloratadine use in adolescents aged 12-17 years is limited. (See sections 4.8 and 5.1). Elderly Population No specific studies in elderly patients are available. 4.3 Contraindications Hypersensitivity to loratadine or to the active substance or to any of the excipients listed in section 6.1 4.4 Special Warnings and Precautions for Use Renal Dysfunction AERIUS should be used with caution in patients with severe renal impairment (see section 5.2). Seizures Desloratadine is indicated with caution in patients who are prone to seizures, with a personal or family history, especially in young children who are prone to seizures during desloratadine treatment (see section 4.8). Medical personnel may consider discontinuing desloratadine therapy in patients who develop seizures during treatment. Each tablet of this medicinal product contains 5.8 mg of lactose. Patients with rare hereditary problems of galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicinal product. 4.5 Interactions with Other Medicinal Products and Other Forms of Interaction In clinical trials where desloratadine tablets were co-administered with erythromycin or ketoconazole, no clinically significant interactions were observed (see section 5.1). In clinical pharmacology studies, co-administration of AERIUS tablets with alcohol did not potentiate the adverse effects of alcohol on psychomotor performance (see section 5.1). However, there have been post-marketing reports of alcohol intolerance and intoxication. Therefore, caution is recommended when taking the product with alcohol. Additional Information on Special Populations Pediatric Population Interaction studies have only been conducted in adults. 4.6 Pregnancy and Lactation General Advice Pregnancy Category C. Women of Childbearing Potential/Contraception No data are available on the effects on fertility in women of childbearing potential. Pregnancy A large body of evidence on pregnant women (outcomes of over 1000 pregnancies) indicates that desloratadine has no malformative or feto/neonatal toxicity. Animal studies are insufficient with respect to effects on pregnancy and/or embryonic/fetal development and/or parturition and/or postnatal development (see section 5.3). The potential risk to humans is unknown. AERIUS should not be used during pregnancy unless clearly necessary. Lactation Desloratadine has been detected in the breast milk of lactating mothers. The effects of desloratadine on neonates/infants are unknown. A decision should be made whether to discontinue AERIUS or breastfeeding, taking into account the benefit of breastfeeding for the child and the benefit of treatment for the woman. Reproductive Ability/Fertility No data are available on the effects on male and female fertility. 4.7 Effects on Ability to Drive and Use Machines Based on clinical studies, AERIUS has no or negligible effect on the ability to drive and use machines. Patients should be advised that most people do not experience drowsiness. However, as the response to all medicinal products varies from individual to individual, patients should be advised not to engage in activities requiring mental alertness, such as driving and operating machinery, until they have determined their reaction to the medicinal product. 4.8 Side Effects Summary of the Safety Profile In clinical trials for allergic rhinitis and chronic idiopathic urticaria, patients taking the recommended daily dose of 5 mg AERIUS experienced more adverse events than those taking placebo in 3% of cases. The most frequently reported adverse events, more often than with placebo, were fatigue (1.2%), dry mouth (0.8%), and headache (0.6%). Pediatric Population In a clinical trial of 578 adolescent patients aged 12-17 years, the most frequent adverse event was headache, reported in 5.9% of patients taking AERIUS and 6.9% of patients taking placebo. Other adverse events described in clinical trials compared to placebo and reported in the post-marketing period are listed below. Frequencies are defined as: very common (≥ 1/10); common (≥ 1/100 to < 1/10); uncommon (≥ 1/1000 to < 1/100); rare (≥ 1/10,000 to < 1/1000); very rare (< 1/10,000), not known (cannot be estimated from available data). Metabolism and Nutrition Disorders Not known: Increased appetite Psychiatric Disorders Very rare: Hallucinations. Not known: Behavioral disturbances, aggression, depressive mood Nervous System Disorders Common: Headache Very rare: Dizziness, somnolence, insomnia, psychomotor hyperactivity, convulsions. Eye Disorders Not known: Dry eyes Cardiac Disorders Very rare: Tachycardia, palpitations. Not known: QT prolongation Gastrointestinal Disorders Common: Dry mouth Very rare: Abdominal pain, nausea, vomiting, dyspepsia, diarrhea. Hepatobiliary Disorders Very rare: Increased liver enzymes, hepatitis, increased bilirubin. Not known: Jaundice Skin and Subcutaneous Tissue Disorders Not known: Photosensitivity Musculoskeletal, Connective Tissue and Bone Disorders Very rare: Myalgia. General Disorders and Administration Site Conditions Common: Fatigue Very rare: Hypersensitivity reactions (such as anaphylaxis, angioedema, dyspnea, pruritus, rash and urticaria). Not known: Asthenia Investigations Not known: Weight gain Additional Information on Special Populations Pediatric Population Other adverse events of unknown frequency have been reported from post-marketing data in pediatric patients, including QT interval prolongation, arrhythmia, bradycardia, abnormal behavior, and aggression. Retrospective observational studies have shown an increased incidence of new seizures in patients aged 0 to 19 years taking desloratadine compared to periods when desloratadine was not taken. Among children aged 0-4 years, the adjusted absolute increase was 37.5 (95% confidence interval (CI) 10.5-64.5) per 100,000 person-years (PY) with a background incidence of new onset of 80.3 per 100,000 PY. Among patients aged 5-19 years, the adjusted absolute increase was 11.3 (95% CI 2.3-20.2) per 100,000 PY, with a background incidence of 36.4 per 100,000 PY (see section 4.4). Reporting of Suspected Adverse Events Reporting of suspected adverse events after authorization of the medicinal product is important. It allows for continuous monitoring of the benefit/risk balance of the medicinal product. 4.9 Overdose and Treatment The side effect profile associated with overdose appears similar to that observed with therapeutic doses in post-marketing use, but the magnitude of effects may be higher. Treatment in case of overdose Consider standard measures to remove the unabsorbed active substance. Symptomatic and supportive treatment is recommended. Desloratadine is not removed by hemodialysis; it is not known if it is removed by peritoneal dialysis. Symptoms Based on a multiple-dose clinical trial in which up to 45 mg of desloratadine (9 times the clinical dose) was administered, no clinically significant effects were observed. Pediatric Population The side effect profile associated with overdose appears similar to that observed with therapeutic doses in post-marketing use, but the magnitude of effects may be higher. 5 Pharmacological Properties 5.1 Pharmacodynamic Properties Pharmacotherapeutic group: Other antihistamines for systemic use Mechanism of Action Desloratadine is a non-sedating, long-acting, potent, selective peripheral histamine H1-receptor antagonist. Desloratadine selectively blocks peripheral histamine H1 receptors, as it is unable to cross the blood-brain barrier after oral administration. Desloratadine has demonstrated anti-allergic properties in in vitro studies. These include suppression of the release of pro-inflammatory cytokines such as IL-4, IL-6, IL-8 and IL-13 from human mast cells/basophils and suppression of the expression of the adhesion molecule P-selectin on endothelial cells. The clinical significance of these observations has not yet been confirmed. Clinical Efficacy and Safety No statistically or clinically significant cardiovascular effects were observed in a multiple-dose clinical trial using up to 20 mg of desloratadine daily for 14 days. In a clinical pharmacology study using 45 mg of desloratadine daily (nine times the clinical dose) for ten days, no QTc interval prolongation was observed. In multiple-dose interaction studies with ketoconazole and erythromycin, no changes in desloratadine plasma concentrations were observed. Pharmacodynamic Effects Desloratadine does not readily cross the blood-brain barrier. In controlled clinical trials, at the recommended dose of 5 mg daily, the incidence of somnolence was not increased compared to placebo. Desloratadine, administered at a single daily dose of 7.5 mg, did not affect psychomotor performance in clinical studies. In a single-dose study in adults, 5 mg desloratadine did not affect flight performance, did not cause increased subjective somnolence, and did not impair the ability to perform flight tasks. In clinical pharmacology studies, desloratadine did not potentiate the effects of alcohol on psychomotor performance and somnolence. Psychomotor test results did not differ significantly between patients taking desloratadine and placebo alone or with alcohol. In patients with allergic rhinitis, AERIUS was effective in relieving symptoms such as sneezing, nasal discharge/congestion and itching, as well as itchy and red eyes, watery eyes, and itchy palate. AERIUS effectively controls symptoms for 24 hours. Pediatric Population The efficacy of AERIUS has not been unequivocally demonstrated in a study in adolescents aged 12-17 years. In addition to the established classification of rhinitis as seasonal and perennial (throughout the year), allergic rhinitis can be divided into intermittent and persistent based on the duration of symptom persistence. In intermittent rhinitis, symptoms occur less than 4 days per week or less than 4 weeks per year. In persistent rhinitis, symptoms occur more than 4 days per week or more than 4 weeks per year. Based on the aggregated scores of quality of life questionnaires in patients with rhinoconjunctivitis, AERIUS effectively alleviated the condition of patients with seasonal allergic rhinitis. Greater improvement was observed in the area of daily activities and practical problems limited by the presence of symptoms. Chronic idiopathic urticaria was studied in the form of a classic model of urticaria, based on the similarity of their underlying pathophysiological mechanisms, despite the absence of etiology and problems. In the prospective selection of patients with chronic diseases. Since histamine release is a causal factor in all types of urticaria, it is expected that desloratadine will be an effective agent for relieving symptoms of other types of urticaria, including chronic idiopathic urticaria, as indicated in clinical recommendations. In two placebo-controlled six-week studies in patients with chronic idiopathic urticaria, AERIUS effectively relieved itching and reduced the size and number of rashes by the end of the first course of treatment. In each study, the effect was maintained for 24 hours after dosing, as in other studies of antihistamines in chronic idiopathic urticaria, a small proportion of patients who were considered resistant to antihistamine treatment were excluded. A 50% reduction in itching was observed in 55% of patients treated with desloratadine, compared to 19% of patients receiving placebo. Treatment with AERIUS also significantly reduced the negative impact of the disease on sleep and daytime activities, as determined by a four-point scale used to assess these variables. 5.2 Pharmacokinetic Properties General Characteristics Absorption Plasma concentrations of desloratadine become measurable within 30 minutes of administration. Desloratadine is well absorbed and maximum concentrations are reached approximately 3 hours later. The terminal elimination half-life of desloratadine is approximately 27 hours. The degree of desloratadine accumulation corresponds to its half-life (approximately 27 hours) and once-daily dosing frequency. In a pharmacokinetic study comparing patient demographic data to the general population of patients with seasonal allergic rhinitis, 4% of subjects achieved higher concentrations of desloratadine. This percentage may vary by ethnicity. The maximum concentration of desloratadine was approximately 3 times higher for approximately 7 hours, and the terminal elimination half-life was approximately 89 hours. The safety profile of these individuals did not differ from the general population. Distribution Desloratadine was moderately bound to plasma proteins (83-87%). With once-daily doses of 5 to 20 mg for 14 days, no clinically significant accumulation of the drug was observed. Biotransformation Since the enzyme responsible for the metabolism of desloratadine has not yet been identified, some interactions with other drugs cannot be fully excluded. In vivo and in vitro studies have shown that desloratadine does not inhibit CYP3A4 or CYP2D6 activity and is neither a substrate nor an inhibitor of P-glycoprotein. In a multiple-dose pharmacokinetic study in healthy adult patients treated with the tablet form, it was found that the metabolism of desloratadine was impaired in four subjects. In these cases, Cmax concentration is approximately 3 times higher for approximately 7 hours, and the terminal elimination half-life is approximately 89 hours. In a series of pharmacological and clinical studies, desloratadine plasma concentrations were higher in 6% of subjects. The prevalence of this slow metabolizer phenotype is comparable in adults (6%) and pediatric (6%) subjects aged 2-11 years and is higher in Black individuals (18% in adults, 16% in pediatric cases) than in White individuals (2% in adults, 3% in pediatric cases). However, the safety profile in these cases does not differ from the general population. Elimination In a study of single administration of desloratadine at a dose of 7.5 mg, it was found that food (a high-fat, high-calorie breakfast) did not affect the disposition of desloratadine. In another study, grapefruit juice had no effect on the disposition of desloratadine. Linearity/Non-linearity The bioavailability of desloratadine is dose-proportional in the range of 5 mg to 20 mg. Characteristics in Patients Patients with Renal Impairment The pharmacokinetics of desloratadine were compared between patients with chronic kidney disease (CKD) and healthy individuals in one single-dose study and one multiple-dose study. In the single-dose study, the exposure to desloratadine was approximately 2 and 2.5 times higher in patients with mild and severe chronic kidney disease, respectively, than in healthy individuals. In the multiple-dose study, steady state was reached after 11 days, and compared to healthy individuals, the exposure to desloratadine was ~1.5 times higher in patients with mild and moderate chronic kidney disease, and ~2.5 times higher in patients with severe chronic kidney disease. In both studies, the exposure to desloratadine and its metabolite 3-hydroxydesloratadine (AUC and Cmax) was not clinically significant. 5.3 Preclinical Safety Data Desloratadine is the major active metabolite of loratadine. There are no comparative clinical studies with desloratadine and loratadine demonstrating qualitative or quantitative differences in desloratadine exposure with respect to the toxicity profile of desloratadine and loratadine. Non-clinical data do not reveal any special hazard to humans based on traditional studies of safety pharmacology, repeated dose toxicity, genotoxicity and carcinogenic potential, and reproductive and developmental toxicity. Clinical studies of desloratadine and loratadine have shown that it has no carcinogenic potential. 6 Pharmaceutical Properties 6.1 List of Excipients Calcium hydrogen phosphate dihydrate Microcrystalline cellulose Corn starch Talc Opadry II Blue 32B10817 [Lactose monohydrate (animal origin), hypromellose, titanium dioxide, macrogol 400, indigotine (E 132)] Opadry Clear YS-1-19025A (hypromellose, macrogol 400) Carnauba wax White beeswax (source of honey bee) Purified water 6.2 Incompatibilities Not applicable to this product 6.3 Shelf Life 24 months 6.4 Special Precautions for Storage Store below 25°C, protected from moisture. 6.5 Nature and Contents of Packaging PVC/PCTFE/Aluminum blister pack containing 20 tablets 6.6 Disposal of Unused Medicinal Products and Special Instructions for Disposal Unused products or waste should be disposed of in accordance with the "Regulation on the Control of Medical Waste" and the "Rules for the Control of Packaging Waste".