Properties
- Form
- sirofi
- Dosage mg
- 2.5მგ/5
- Pack
- 1
What is it?
Instructions for use Desloben 2.5 mg/5 ml syrup Composition: Each 2.5 mg/5 ml syrup of Desloben contains 0.5 mg desloratadine as the active substance and propylene glycol as a solvent; sucrose and sorbitol as sweeteners; tutti frutti flavor as flavoring; sunset yellow (E110) as coloring and sodium benzoate (E211) as a preservative. Pharmacological properties: Pharmacodynamic properties: Pharmacotherapeutic group: Antihistamines - H1-receptor antagonists. Mechanism of action: Desloratadine is a non-sedating, long-acting histamine antagonist with selective antagonistic activity at peripheral H1 receptors. After oral administration, desloratadine selectively inhibits peripheral histamine H1 receptors and is not distributed to the central nervous system. In vitro studies have shown that desloratadine has anti-allergic effects. This includes the suppression of the release of pro-inflammatory cytokines IL-4, IL-6, IL-8, and IL-13 from human mast cells/basophils, as well as the suppression of the expression of the adhesion molecule P-selectin in endothelial cells. The clinical significance of these observations has not been established. Clinical efficacy and safety: Pediatric population: The efficacy of desloratadine syrup has not been studied in independent pediatric studies. The safety of desloratadine syrup has been demonstrated in three pediatric studies. Children aged 1-11 years requiring antihistamine treatment received a daily dose of desloratadine of 1.25 mg (ages 1-5) or 2.5 mg (ages 6-11). Treatment was well tolerated, as confirmed by clinical-laboratory analyses, vital signs, and ECG data, including QTc interval. At recommended doses, plasma concentrations of desloratadine (see "Pharmacokinetics") were comparable in pediatric and adult populations. Therefore, given the similar course of allergic rhinitis/chronic idiopathic urticaria and the desloratadine profile in adult and pediatric patients, it is possible to extrapolate efficacy data from adults to the pediatric population. The efficacy of desloratadine syrup has not been studied in pediatric studies involving children under 12 years of age. Adults and adolescents: In a multiple-dose clinical study in adults and adolescents, administration of desloratadine at a dose of 20 mg per day for 14 days did not result in statistically or clinically significant cardiovascular events. In a clinical pharmacology study in adults and adolescents, administration of desloratadine at a dose of 45 mg per day (nine times the clinical dose) for 10 days did not result in QT interval prolongation. Desloratadine does not cross the blood-brain barrier. In controlled clinical studies in adults and adolescents, administration of the recommended daily dose of 5 mg did not result in an increase in somnolence compared to placebo. In clinical studies in adults and adolescents, a single daily dose of 7.5 mg of desloratadine tablets did not affect psychomotor activity. In a single-dose study in adults, 5 mg of desloratadine did not affect standard measures of flight performance, nor did it increase subjective somnolence or impair the ability to perform a flight task. In clinical pharmacology studies in adults, concomitant alcohol intake did not enhance alcohol's effects, such as impairment of psychomotor function or somnolence. Psychomotor test results did not differ significantly between patients receiving desloratadine and placebo, alone or with alcohol. Multiple-dose interaction studies with ketoconazole and erythromycin did not reveal clinically significant changes in desloratadine plasma concentrations. The efficacy of desloratadine syrup has not been studied in pediatric studies involving children under 12 years of age. In adult and adolescent patients with allergic rhinitis, desloratadine tablets were effective in relieving symptoms such as sneezing, runny nose, and itching, as well as itchy eyes, watery eyes, redness, and itchy palate. Desloratadine effectively controlled symptoms for 24 hours. The efficacy of desloratadine tablets was not consistently demonstrated in studies of adolescents aged 12 to 17 years. In addition to the established classification of rhinitis (seasonal and perennial), allergic rhinitis can be divided into intermittent and persistent based on symptom duration. Intermittent allergic rhinitis symptoms occur less than 4 days per week or less than 4 weeks per year. Persistent allergic rhinitis symptoms occur more than 4 days per week or more than 4 weeks per year. Based on the total scores from the Rhinoconjunctivitis Quality of Life Questionnaire, desloratadine effectively improved the condition of patients with seasonal allergic rhinitis. Greater improvement was observed in the area of daily activities and practical problems limited by symptoms. Chronic idiopathic urticaria was studied as a clinical model of urticaria, based on the similarity of their underlying pathophysiological mechanisms, regardless of etiology, in prospective selection of patients with chronic conditions. Since histamine release is a causal factor in all types of urticaria, desloratadine is expected to be effective in managing 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, desloratadine effectively relieved itching and reduced the size and number of wheals by the end of the first treatment course. In each study, the effect was maintained for 24 hours after dosing. As with other antihistamine studies in chronic idiopathic urticaria, a small subset of patients considered refractory to antihistamine treatment was excluded. More than 50% reduction in itching was observed in 55% of patients treated with desloratadine, compared to 19% of patients receiving placebo. Desloratadine treatment also significantly reduced the negative impact of the disease on sleep and daytime activity, as determined by a four-point scale used to assess these variables. Pharmacokinetic properties: Absorption: In adults and adolescents, desloratadine plasma concentrations are detectable within 30 minutes of administration. Desloratadine is well absorbed, with peak plasma concentrations reached on average after 3 hours; the terminal elimination half-life averages 27 hours. The degree of desloratadine accumulation is consistent with its half-life (approximately 27 hours) and once-daily dosing. The bioavailability of desloratadine was dose-proportional in the dose range of 5 to 20 mg. In several pharmacokinetic and clinical studies, 6% of subjects achieved higher concentrations of desloratadine. The incidence of this poor metabolizer phenotype was comparable in adults (6%) and pediatric subjects aged 2 to 11 years (6%), and was higher in Black subjects (18% adults, 16% pediatric subjects) than in Caucasians (2% adults, 3% pediatric subjects) in both populations. In a multiple-dose pharmacokinetic study in healthy adult subjects, four subjects were found to be poor metabolizers of desloratadine. In these subjects, Cmax was almost threefold higher with a terminal half-life of approximately 89 hours, occurring approximately 7 hours after dosing. Similar pharmacokinetic parameters were observed in pediatric subjects aged 2 to 11 years who were poor metabolizers in a multiple-dose pharmacokinetic study with syrup. Desloratadine exposure (AUC) was almost 6 times higher, and Cmax was almost 3-4 times higher, occurring 3-6 hours after dosing, with a terminal half-life of approximately 120 hours. Exposure was similar in poor metabolizer adults and children when treated with age-appropriate doses. The overall safety profile in these individuals did not differ from the general population. The efficacy of desloratadine syrup in poor metabolizers under 2 years of age has not been studied. In independent studies of the recommended single dose in pediatric patients, AUC and Cmax values of desloratadine were compared to those in adults receiving desloratadine syrup at a dose of 5 mg. Distribution: Desloratadine is moderately bound (83-87%) to plasma proteins. In adults and adolescents, no clinically significant accumulation of the active substance was observed with once-daily administration of desloratadine (5-20 mg) for 14 days. Biotransformation: The enzyme responsible for the metabolism of desloratadine has not yet been identified, and therefore, interaction with other drugs cannot be completely ruled out. Desloratadine does not inhibit CYP3A4. In vivo and in vitro studies have shown that the drug does not inhibit CYP2D6 and is neither a substrate nor an inhibitor of P-glycoprotein. Excretion: 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. Another study showed that grapefruit juice did not affect the disposition of desloratadine. Patients with impaired renal function: The pharmacokinetics of desloratadine were compared in patients with chronic renal failure and healthy individuals in a single-dose study and a 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 moderate or severe chronic renal failure, respectively, than in healthy individuals. In the multiple-dose study, steady state was reached after 11 days, and the exposure to desloratadine was approximately 1.5 times higher in patients with mild to moderate chronic renal failure and approximately 2.5 times higher in patients with severe chronic renal failure compared to healthy individuals. In both studies, the change in exposure (AUC and Cmax) of desloratadine and 3-hydroxydesloratadine was not clinically significant. Indications: Desloben is indicated in adults, adolescents, and children aged 1 year and older for the relief of symptoms of allergic rhinitis and urticaria. Contraindications: Hypersensitivity to the active substance, any excipients, or loratadine. Warnings/Precautions: Desloratadine should be administered with caution in patients with a personal or family history of seizures, particularly young children who are more prone to developing seizures during desloratadine treatment. If seizures occur during treatment, the treating physician may decide to discontinue desloratadine. Pediatric population: In children under 2 years of age, it is very difficult to distinguish allergic rhinitis from other forms of rhinitis. The presence of upper respiratory tract infection or structural abnormalities should be considered, as well as the patient's history, medical examination, and appropriate laboratory and skin test data. Approximately 6% of adults and children aged 2-11 years are phenotypically poor metabolizers of desloratadine and exhibit high exposure (see "Pharmacokinetics"). In children aged 2-11 years who are poor metabolizers, the safety of desloratadine syrup is similar to that in children who are normal metabolizers. The effect of desloratadine syrup in poor metabolizers under 2 years of age has not been studied. In cases of severe renal impairment, Desloben should be used with caution (see "Pharmacokinetics"). This medicinal product contains sucrose and sorbitol; therefore, patients with rare hereditary problems of fructose intolerance, glucose-galactose malabsorption, or sucrose-isomaltase insufficiency should not take this product. This medicinal product contains the dye E110, which may cause allergic reactions. Interactions with other medicinal products and other forms of interaction: In clinical studies of desloratadine where erythromycin or ketoconazole was used in combination, no clinically significant interactions were observed (see "Pharmacodynamics"). Pediatric population: Interaction studies have only been conducted in adults. In a clinical pharmacology study, concomitant administration of desloratadine with alcohol did not enhance alcohol's adverse effects on psychomotor function (see "Pharmacodynamics"). However, cases of alcohol intolerance and intoxication have been reported in the post-marketing period. Therefore, caution is recommended when taking with alcohol. Pregnancy and lactation: Pregnancy: Large amounts of data in pregnant women (over 1000 deliveries) do not indicate fetal/neonatal malformations or toxicity of desloratadine. Animal studies have not shown direct or indirect harmful effects regarding reproductive toxicity. As a precautionary measure, it is advisable to avoid the use of Desloben during pregnancy. Breastfeeding: Desloratadine has been detected in newborns/infants of breastfed mothers. The effect of desloratadine on newborns/infants is unknown. A decision should be made whether to discontinue breastfeeding or to discontinue/refrain from desloratadine therapy, taking into account the benefits of breastfeeding for the infant and the benefits of therapy for the woman. Fertility: No data are available regarding male and female fertility. Effect on ability to drive and operate machinery: Based on clinical studies, desloratadine has no or negligible effect on the ability to drive and operate machinery. Patients should be informed that most people do not experience drowsiness. However, considering individual variations with any drug, it is not recommended to engage in activities requiring mental alertness, such as driving or operating machinery, until individual response to the drug is determined. Side effects/Adverse events: Summary of safety profile: Pediatric population: In clinical studies in children aged 6 months to 11 years, 246 children received desloratadine syrup. In children aged 2 to 11 years, the overall incidence of adverse events was similar in the desloratadine and placebo groups. In infants and children aged 6 to 23 months, the most frequent adverse reactions, higher than in the placebo group, were diarrhea (3.7%), fever (2.3%), and insomnia (2.3%). In an additional study, no adverse events were observed after a single dose of 2.5 mg desloratadine syrup in children aged 6-11 years. In a clinical study of 578 adolescent patients aged 12 to 17 years, the most frequent adverse event was headache, reported in 5.9% of patients in the desloratadine group and 6.9% in the placebo group. Adults and adolescents: In clinical studies in adults and adolescents with indications for allergic rhinitis and chronic idiopathic urticaria using recommended doses of desloratadine, adverse events were reported in 3% of patients, which is higher than in the placebo group. The most frequent adverse events, higher than in the placebo group, were fatigue (1.2%), dry mouth (0.8%), and headache (0.6%). Adverse events are listed in the table below. The table lists adverse events from clinical studies that are higher than in the placebo group, and other adverse reactions reported in the post-marketing period. Frequency is defined as follows: very common (≥1/10), common (≥1/100; <1/10), uncommon (≥1/1,000; <1/100), rare (≥1/10,000; <1/1,000), very rare (<1/10,000), and frequency unknown (frequency cannot be estimated from available data). System organ class | Frequency | Adverse reactions of desloratadine Metabolism and nutrition disorders | Frequency unknown | Increased appetite Psychiatric disorders | Very rare | Hallucinations | Frequency unknown | Unusual behavior, aggression Nervous system disorders | Common | Headache | Common (children under 2 years) | Insomnia | Very rare | Dizziness, somnolence, insomnia, psychomotor hyperactivity, convulsions Cardiac disorders | Very rare | Tachycardia, palpitations | Frequency unknown | QT interval prolongation Gastrointestinal disorders | Common | Dry mouth | Common (children under 2 years) | Diarrhea | Very rare | Abdominal pain, nausea, vomiting, dyspepsia, diarrhea Hepatobiliary disorders | Very rare | Increased liver enzyme levels, increased bilirubin, hepatitis | Frequency unknown | Jaundice Skin and subcutaneous tissue disorders | Frequency unknown | Photosensitivity Musculoskeletal and connective tissue disorders | Very rare | Myalgia General disorders and administration site conditions | Common | Fatigue | Common (children under 2 years) | Fever | Very rare | Hypersensitivity reactions (e.g., anaphylactic reaction, angioedema, dyspnea, pruritus, rash, and urticaria) | Frequency unknown | Asthenia Laboratory analyses | Frequency unknown | Weight gain Pediatric population: Other adverse reactions reported in the post-marketing period in children, with unknown frequency, include QT interval prolongation, arrhythmia, bradycardia, unusual behavior, and aggression. Dosage and administration: Dosage: Adults and adolescents (12 years and older): The recommended dose of Desloben is 10 ml (5 mg) of syrup once daily. Pediatric population: The physician should be informed that most cases of rhinitis in children under 2 years of age are infectious in nature (see "Warnings and Precautions") and there is no data related to the treatment of infectious rhinitis with desloratadine syrup. Children aged 1-5 years: 2.5 ml (1.25 mg) of Desloben syrup once daily. Children aged 6-11 years: 5 ml (2.5 mg) of Desloben syrup once daily. Adults and adolescents (12 years and older): 10 ml (5 mg) of Desloben syrup once daily. Clinical trial experience with the use of desloratadine in adolescents aged 12-17 years is limited (see "Adverse Events" and "Pharmacodynamics"). Treatment of intermittent allergic rhinitis (symptoms present less than 4 days per week or less than 4 weeks per year) should be based on an assessment of the patient's history, and treatment may be discontinued when symptoms disappear and resumed when symptoms reappear. For persistent allergic rhinitis (symptoms present more than 4 days per week or more than 4 weeks per year), treatment may be continued during the period of allergen exposure. Overdose: Adverse events associated with overdose reported in the post-marketing period are similar to those observed with therapeutic doses, but the severity of events may be higher. Treatment in case of overdose involves standard measures to remove unabsorbed active substance from the body. Symptomatic and supportive therapy is recommended. Desloratadine is not removed by hemodialysis; it is not known whether the drug is removed by peritoneal dialysis. Symptoms: In a multiple-dose clinical study in adults and adolescents, administration of desloratadine at a dose of 45 mg (nine times the clinical dose) did not result in clinically significant effects. Pediatric population: Adverse events associated with overdose reported in the post-marketing period are similar to those observed with therapeutic doses, but the severity of events may be higher. Dosage form: 150 ml syrup is presented in a 150 ml 28 PP amber glass bottle with a "VISTOP" type 28/20 PP plastic cap and a 5 ml capacity plastic spoon. Other pharmaceutical dosage forms: Desloben 5 mg film-coated tablets; presented in a transparent PVC/PE/PVDC-Al blister with 20 and 30 film-coated tablets. Storage conditions: Store at a temperature not exceeding 25°C, in its original packaging; protect from light. Keep out of reach of children. Shelf life: 2 years. Dispensing category: Pharmaceutical product group III, available without prescription.
