Desloratadine FT syrup 0.5mg/ml vial 100ml №1

Name:
Desloratadine FT syrup.
Description:
Transparent, yellowish solution with a characteristic strawberry odor. Main active ingredient Other antihistamines for systemic use. selective antagonistic effect on peripheral H1-histamine receptors. After oral administration, desloratadine selectively blocks peripheral H1-histamine receptors, since it practically does not penetrate the blood-brain barrier. Desloratadine is the main active metabolite of loratadine. In vitro studies have shown that desloratadine has anti-allergic effects, including inhibition of the release of pro-inflammatory cytokines, including IL-4, IL-6, IL-8 and IL-13, from human mast cells/basophils. Desloratadine also inhibits the expression of the adhesion molecule (P-selectin) in endothelial cells. These data have no confirmed clinical significance. The fact that desloratadine practically does not penetrate the blood-brain barrier has been confirmed in controlled studies. When using the recommended dose of 5 mg / day of desloratadine in adults and adolescents, the incidence of drowsiness was not higher than that in the placebo group. In clinical and pharmacological studies in adults, desloratadine did not increase the effects of alcohol, such as impaired psychomotor function and drowsiness. The results of the psychomotor test did not reveal a significant difference in patients who received desloratadine and placebo alone or in combination with alcohol (see section “Interaction with other medicinal products and other forms of interaction”). In a multiple-dose study of desloratadine in adults and adolescents at daily doses of up to 20 mg daily for 14 days, desloratadine did not cause clinically or statistically significant changes in the cardiovascular system. In a study in which adults and adolescents took desloratadine at a dose of 45 mg / day (which is 9 times the recommended therapeutic dose) for 10 days, there was also no prolongation of the QTc interval on the ECG. Dosing recommendations for desloratadine in children over 6 months of age are based on comparative pharmacokinetic studies. The safety of the use of syrup containing desloratadine was studied in 3 placebo-controlled studies in 246 children aged 6 months to 11 years. Children aged 6 months to 11 years with a history of seasonal allergic rhinitis or chronic idiopathic urticaria received desloratadine at doses of 1 mg/day (age 6-11 months), 1.25 mg/day (age 1-5 years) and 2 .5 mg / day (age 6-11 years). The treatment was well tolerated, as evidenced by clinical tests, laboratory tests, vital signs and ECG data (changes in the intervals between the waves, including the QTc interval were assessed). Given the recommended doses, the pharmacokinetics of desloratadine in children was comparable to that in adults. The efficacy of oral desloratadine has not been studied in pediatric studies. However, since the pathogenesis and course of allergic rhinitis and chronic urticaria, as well as the pharmacokinetic profile of desloratadine, are similar in children and adults, efficacy data in adults may also indicate efficacy in children. Desloratadine selectively blocks H1-histamine receptors, thereby preventing the secretion of histamine, a causative factor for all types of urticaria, regardless of etiology. It is assumed that desloratadine will be effective in relieving symptoms not only of chronic idiopathic urticaria, which was a clinical model in the study of the effectiveness of desloratadine, but also of its other types, according to clinical recommendations (with the exception of acute onset urticaria as one of the manifestations of an anaphylactic reaction (see section “Special instructions and precautions”) In 2 placebo-controlled studies in patients with chronic idiopathic urticaria lasting 6 weeks, desloratadine effectively relieved itching and reduced the size and number of rashes by the end of the first course of treatment. In each of the studies, the effect was maintained for 24 hours post-dose Studies excluded a minority of patients not responding to antihistamines Relief of pruritus greater than 50% was observed in 55% of patients treated with desloratadine compared with 19% of patients treated with placebo. It also significantly reduced the negative impact of the disease on sleep and daily activity, which was assessed on a four-point scale. Pharmacokinetics Absorption Desloratadine is well absorbed. Within 30 minutes after oral administration, desloratadine can be detected in blood plasma. Peak plasma concentration is reached after approximately 3 hours. The relative bioavailability of desloratadine is dose proportional over the dose range of 5 mg to 20 mg. Absolute bioavailability is unknown. Distribution Desloratadine is moderately (83-87%) bound to plasma proteins. In patients with renal and / or hepatic insufficiency, the degree of binding of desloratadine and 3-hydroxydesloratadine to plasma proteins is not changed compared to that in patients with normal renal and hepatic function. There is no evidence of a clinically significant accumulation of desloratadine after taking it in doses of 5-20 mg 1 time per day for 14 days. Metabolism Desloratadine is metabolized to the active metabolite 3-hydroxydesloratadine and then glucuronidated. The enzyme that is responsible for the metabolism of desloratadine has not been established, so interactions of desloratadine with other drugs cannot be ruled out. In vivo and in vitro studies have shown that desloratadine does not inhibit CYP3A4 and CYP2D6, and is neither a substrate nor an inhibitor of P-glycoprotein. Withdrawal The half-life in the final phase is about 27 hours. Administration of 14C-labeled desloratadine showed that about 84% of the total dose was equally excreted in the urine and feces. Plasma analysis of the metabolite 3-hydroxydesloratadine showed that its Tmax and t1/2 are similar to Tmax and t1/2 of desloratadine. Desloratadine is practically not excreted by hemodialysis (0.3%). There are no data on the elimination of desloratadine by peritoneal dialysis. Effect of food on pharmacokinetics In a study with a single dose of desloratadine at a dose of 7.5 mg, food (a high-calorie, high-fat breakfast) or grapefruit juice did not affect the pharmacokinetics of desloratadine. Special patient groups Patients with impaired renal function The pharmacokinetics of desloratadine in patients with chronic renal failure (CRF) was compared with the pharmacokinetics in healthy subjects in one study when taking a single dose and in one study when taking multiple doses of desloratadine. In a single dose study, the AUC of desloratadine was 2 and 2.5 times greater in patients with mild/moderate and severe renal impairment, respectively, than in healthy volunteers. In a study using repeated doses of desloratadine, steady state was achieved after 11 days of treatment. Compared with healthy subjects, the AUC of desloratadine was approximately 1.5 times higher in patients with mild to moderate CKD and approximately 2.5 times higher in patients with severe CKD. In both studies, changes in Cmax and AUC of desloratadine and 3-hydroxydesloratadine were not clinically significant. Patients with impaired hepatic function The pharmacokinetics of desloratadine after oral administration of a single dose in patients with mild (4 patients), moderate (4 patients) and severe (4 patients) hepatic insufficiency (Child-Pugh classification) was compared with that in 8 subjects with normal liver function. . In patients with hepatic insufficiency, regardless of its degree, an increase in AUC of approximately 2.4 times was observed compared with healthy subjects. The clearance of desloratadine in patients with mild, moderate and severe hepatic insufficiency was 37%, 36% and 28%, respectively, of that in healthy study subjects. There was also an increase in the mean half-life in patients with hepatic insufficiency. Mean values of Cmax and AUC of 3-hydroxydesloratadine had no statistically significant differences from similar values in healthy subjects. The degree of plasma protein binding of desloratadine and 3-hydroxydesloratadine did not change in patients with liver disease. The frequency of adverse reactions with a maximum of 10 days of treatment in patients with moderate hepatic impairment (Child-Pugh class B) was not increased. Children In separate studies using a single dose, Cmax and AUC of desloratadine were comparable in children who received the recommended doses according to age, and in adults who received desloratadine syrup at a dose of 5 mg. Thus, in children aged 6 to 11 years, a single dose of 2.5 mg of desloratadine as an oral solution and in children from 2 to 5 years of age, a single dose of 1.25 mg of desloratadine as an oral solution resulted in concentrations of desloratadine in blood plasma comparable to that of adults who took 5 mg desloratadine tablets. However, the Cmax and AUC of the metabolite desloratadine (3-hydroxydesloratadine) were 1.27 and 1.61 times higher when adults received an oral solution containing 5 mg of desloratadine in a single dose, compared with Cmax and AUC obtained in children. from 2 to 11 years who received 1.25-2.5 mg of desloratadine as a solution for internal use. A single dose oral solution of desloratadine containing 0.625 mg or 1.25 mg was given to children aged 6–11 months and 12–23 months, respectively. The results of the pharmacokinetic analysis revealed that a dose of 1 mg for children aged 6-11 months and 1.25 mg for children aged 12-23 months is necessary in order to achieve a plasma concentration of desloratadine similar to that when taken in adults once doses of 5 mg desloratadine as a solution for internal use. Elderly patients In elderly subjects (65 years of age and older), after repeated doses of desloratadine tablets, the mean Cmax and AUC were 20% higher than in subjects under the age of 65 years. Total clearance (Cl/F) after adjusting for body weight was similar in subjects of both age groups. The mean plasma half-life of desloratadine was 33.7 hours in subjects aged 65 years and older. Pharmacokinetic parameters for 3-hydroxydesloratadine were found to be unchanged in elderly subjects compared to younger subjects. Differences in pharmacokinetic parameters associated with age are unlikely to be clinically significant, so dose adjustment in elderly patients is not required. Slow Metabolic Individuals The conversion of desloratadine (DL) to 3-hydroxydesloratadine (3-DL) is significantly delayed in a portion of the population due to a phenotypic polymorphism that is not yet fully understood. The prevalence of persons with a slow metabolism among the Caucasian population is 6% (adults and children aged 2 to 11 years), and among the black population – 18% (adults) and 16% (children). They have higher concentrations of desloratadine in the blood. The ratio of areas under the concentration-time curve of desloratadine and 3-hydroxydesloratadine is also higher (AUC DL / AUC 3-DL > 10 at normal < 4). These subjects belong to the group of individuals with a slow metabolism. In a pharmacokinetic study using repeated doses of desloratadine in healthy adult volunteers, it was found that in 4 people who turned out to be individuals with a slow metabolism, Cmax was reached 7 hours after taking desloratadine and was almost 3 times higher, and the elimination half-life was about 89 hours. Similar pharmacokinetic parameters were observed in a repeated dose study in children with a slow metabolism who were diagnosed with allergic rhinitis. Exposure (AUC) of desloratadine was approximately 6 times greater and Cmax approximately 3-4 times higher and reached after 3-6 hours compared to AUC and Cmax in children with normal metabolism of desloratadine. The elimination half-life in children with a slow metabolism of desloratadine is about 120 hours. The degree of exposure to desloratadine was similar in slow-metabolizing adults and children at age-appropriate doses. The overall safety profile in these subjects did not differ from that in the general population. In children under 2 years of age with a slow metabolism, the effect of desloratadine has not been studied. Indications for use For relief of symptoms: - allergic rhinitis; - urticaria. Method of administration and doses Method of application of the drug with a dosing syringe Take orally, regardless of food intake. After opening the vial, the drug is suitable for use within 6 months. The dosing syringe with insert attached to the package allows you to accurately dose the drug. Using a dosing syringe for dosing a medicine: 1. Remove the cap from the vial, insert, if necessary, the insert into the neck of the vial so that it is tightly fixed. Insert the dosing syringe into the hole of the insert (the diagram is shown in Figure 1). 2. Turn over the vial with the syringe and pull the syringe plunger until the plunger tip reaches the mark corresponding to the required volume of the drug (the diagram is shown in Figure 2). 3. If an air bubble has formed in the syringe, completely release the syrup into the vial and repeat the procedure for dialing the desired volume of syrup. 4. Turn the vial with the syringe to its original vertical position. Make sure that the syringe plunger has not moved and the plunger tip is still at the desired mark. Pull the syringe out of the hole in the liner (the liner should be left fixed in the neck of the vial). Close the bottle with a lid. 5. The patient should be in an upright position (except for younger patients, see points 7-10). Slowly push down on the plunger of the syringe, gradually releasing the drug. Sharp pressure on the piston is not allowed. When releasing the drug, point the opening of the syringe towards the inside of the cheek. 6. Disassemble the syringe and rinse it in clean drinking water. Wait for the natural drying of the barrel and piston of the syringe. The use of the drug in young children (under 3 years), including infants (up to 1 year), age: 7. After completing the above steps 1-4, the child should be given the position as for feeding (see Figure 3). 8. Insert the tip of the syringe into the child's mouth and slowly release the contents towards the inside of the cheek. 9. It is necessary to maintain pauses during the administration of the drug in order to allow the child to gradually swallow the drug. 10. After the child has taken the drug, give him a small amount of water to drink so that the residual amount of syrup in the oral cavity is swallowed. 11. Follow step 6. Patients or parents/guardians whose children are prescribed Desloratadine FT should be informed about the need to keep the drug vial and dosing syringe out of the reach of children. Dosing regimen Adults and adolescents (≥ 12 years): 10 ml syrup (5 mg desloratadine) once daily. Treatment of intermittent allergic rhinitis (symptoms less than 4 days a week or less than 4 weeks in a row) should be carried out taking into account the data of the anamnesis: the use can be stopped after the symptoms disappear and resumed after their reappearance. In persistent allergic rhinitis (symptoms for 4 or more days per week or more than 4 weeks), therapy can be carried out throughout the entire period of contact with the allergen. Children: - aged 6 months to 11 months: 2 ml syrup (1 mg desloratadine) once a day; - at the age of 1 to 5 years: 2.5 ml of syrup (1.25 mg of desloratadine) once a day; - aged 6 to 11 years: 5 ml syrup (2.5 mg desloratadine) once a day. There is limited clinical experience with the efficacy of desloratadine in children under 17 years of age. It should be borne in mind that most cases of rhinitis in children under 2 years of age are of an infectious origin and there are no data on the use of desloratadine in infectious rhinitis. Children under 6 months of age: The efficacy and safety of oral liquid desloratadine has not been established in children under 6 months of age. Elderly patients: Safety and efficacy in elderly patients have not been established. Patients with impaired renal function: use with caution. Patients with hepatic impairment: There are no data on the use of desloratadine. Use during pregnancy and lactation Pregnancy Safety in the use of desloratadine during pregnancy in humans has not been proven. However, a large amount of data on pregnant women (more than 1000 pregnancies) indicates the absence of toxicity in desloratadine, which leads to malformations or has other negative effects on intrauterine and neonatal development. However, the use of desloratadine during pregnancy should be avoided. Lactation Desloratadine passes into breast milk. The effect of desloratadine, supplied with mother's milk, on newborns / infants is not known. The decision to stop breastfeeding or to refrain from taking a medicinal product containing desloratadine should be based on an assessment of the benefits of breastfeeding for the child and the benefits of using desloratadine for the woman. Precautions Desloratadine is not indicated for the treatment of anaphylactic reactions. It is necessary to inform patients in whom acute urticaria is a manifestation of an anaphylactic reaction (an anaphylactic reaction may also cause respiratory symptoms, symptoms of the cardiovascular system, etc.) to seek immediate medical attention. Desloratadine should be used with caution in patients with convulsions in a personal history or in a history of relatives. Young children may be more prone to seizures when treated with desloratadine. The attending physician should consider discontinuing the use of desloratadine if the patient develops convulsions during drug treatment. The efficacy and safety of oral liquid desloratadine has not been established in children under 6 months of age. In children under 2 years of age, the diagnosis of allergic rhinitis is particularly difficult to distinguish from other forms of rhinitis. It is necessary to pay attention to the presence or absence of upper respiratory tract infections or structural abnormalities, taking into account the history, physical examination data and laboratory and instrumental studies. Also, if necessary, appropriate laboratory and skin tests should be performed. In about 6% of adults and children aged 2 to 11 years, desloratadine is metabolized slowly, they have higher serum concentrations (see the Pharmacokinetics section). The safety of desloratadine in children aged 2-11 years with a slow metabolism is similar to that in children with a standard metabolism of desloratadine. The effect of desloratadine in children under 2 years of age with a slow metabolism has not been studied. Desloratadine should be used with caution in patients with renal insufficiency. Auxiliary components 1 ml of the drug contains 150.0 mg of sorbitol. Sorbitol is a source of fructose. The total consumption of sorbitol (or fructose) with the simultaneous use of drugs or products containing sorbitol (or fructose) should be taken into account. The content of sorbitol in oral medicinal products may affect the bioavailability of other medicinal products taken at the same time. Patients with hereditary fructose intolerance should not be prescribed Desloratadine FT. The medicinal product contains white crystalline sugar. Patients with rare hereditary fructose intolerance, glucose-galactose malabsorption or sucrase-isomaltase deficiency should not take Desloratadine FT. 1 ml of the drug contains 1 mg of sodium benzoate. 1 ml of the drug contains about 100 mg of propylene glycol. 1 ml of the drug Desloratadine FT contains less than 1 mmol (23 mg) of sodium. This amount of sodium is negligible, so you can ignore it. Interaction with other drugs In repeated dose interaction studies, the simultaneous use of 7.5 mg of desloratadine with ketoconazole or erythromycin resulted in an increase in the AUC of desloratadine by 39% and 14%, respectively. In addition, there was an increase in the AUC of the metabolite (3-hydroxydesloratadine) by 72% when used simultaneously with ketoconazole and by 40% when used simultaneously with erythromycin. However, these changes in pharmacokinetic parameters were not clinically significant. No ECG changes occurred. Simultaneous administration of 5 mg of desloratadine and azithromycin led to an increase in serum Cmax of azithromycin by 15% and an increase in AUC of azithromycin by 5%. The combined use of desloratadine and fluoxetine did not lead to a change in the AUC of desloratadine, but led to an increase in its Cmax by 15%. Cmax and AUC of 3-hydroxydesloratadine were increased by 17% and 13%, respectively. Co-administration with cimetidine resulted in an increase in Cmax and AUC of desloratadine by 12% and 19%, respectively, and a decrease in Cmax and AUC of 3-hydroxydesloratadine by 11.2% and 2.8%, respectively. It is impossible to exclude the interaction of desloratadine with other drugs that are metabolized using enzymes of the cytochrome P450 system (see subsection "Pharmacokinetics"). In clinical and pharmacological studies in adults, desloratadine did not increase the effects of alcohol (impaired psychomotor function and drowsiness). The results of the psychomotor test did not reveal a significant difference in patients who received desloratadine and placebo alone or in combination with alcohol. However, in the post-marketing period, cases of alcohol intolerance and intoxication have been reported. Therefore, caution should be exercised in cases of simultaneous use of alcohol and desloratadine. Contraindications - hypersensitivity to desloratadine or to any of the components of the drug (see section "Composition"); - hypersensitivity to loratadine. Composition 1.0 ml of syrup contains: - active ingredient: desloratadine 0.5 mg; - excipients: white crystalline sugar (sucrose), non-crystallizing sorbitol solution (E420), propylene glycol, sodium citrate, sodium benzoate (E 211), strawberry flavor, anhydrous citric acid, disodium edetate, purified water. OverdoseSymptoms Based on a repeated dose study in adults and adolescents where the study dose was 45 mg, 9 times the recommended clinical dose, no clinically significant overdose effects were observed. At the post-registration stage, it was found that the profile of adverse reactions in case of overdose in both adults and children is similar to the profile of adverse reactions when using desloratadine at therapeutic doses, however, the effects may be more pronounced (see section "Side Effects"). Treatment In case of significant overdose, gastric lavage should be carried out along with standard symptomatic and supportive treatment. Desloratadine is practically not excreted by hemodialysis, the excretion of desloratadine during peritoneal dialysis has not been studied. Side effectsSyrup containing desloratadine was taken in the course of studies by about 246 children aged 6 months to 11 years. The overall frequency of adverse reactions in children aged 2 to 11 years was similar in the desloratadine and placebo groups. In children aged 6-23 months, the most commonly reported adverse reactions compared with placebo were diarrhea (3.7%), fever (2.3%), and insomnia (2.3%). In a study, subjects aged 6-11 years did not experience adverse reactions after oral administration of a single dose of desloratadine 2.5 mg. In a clinical study involving 578 subjects aged 12-17 years, headache occurred more often than other adverse reactions (5.9% cases in patients in the desloratadine group and 6.9% of cases in patients in the placebo group). In clinical studies in adults and adolescents using recommended doses of desloratadine for indications including allergic rhinitis and chronic idiopathic urticaria, the incidence of adverse reactions was 3% higher than in the placebo group. The most common were fatigue (1.2%), dry mouth (0.8%) and headache (0.6%). Other adverse reactions reported in the post-marketing period with the use of desloratadine in children, and the frequency of which has not been established, included QT prolongation, arrhythmias, bradycardia, behavioral disturbances and aggression. The list below includes adverse reactions that occurred during clinical trials, the frequency of which exceeded those in the placebo groups, as well as other adverse reactions recorded during post-marketing studies. The undesirable reactions listed below are distributed according to the frequency of occurrence and in accordance with the system organ classification. The frequency of occurrence of adverse reactions is estimated according to the following classification: very often (≥ 1/10); often (from ≥ 1/100 to < 1/10); infrequently (from ≥ 1/1000 to < 1/100); rarely (from ≥ 1/10000 to < 1/1000); very rarely (< 1/10000); frequency unknown (frequency cannot be determined from available data). Adults: Metabolic and nutritional disorders: frequency unknown - increased appetite, weight gain. Mental disorders: very rarely - hallucinations; frequency unknown - abnormal behavior, aggression. Nervous system disorders: often - headache; very rarely - dizziness, drowsiness, insomnia, psychomotor hyperactivity, convulsions. Heart disorders: very rarely - tachycardia, palpitations; frequency unknown - prolongation of the QT interval. Gastrointestinal disorders: often - dry mouth; very rarely - abdominal pain, nausea, vomiting, dyspepsia, diarrhea. On the part of the liver and biliary tract: very rarely - an increase in the activity of liver enzymes, an increase in the level of bilirubin, the development of hepatitis; frequency unknown - jaundice. Skin and subcutaneous tissue disorders: frequency unknown - photosensitivity. Musculoskeletal and connective tissue disorders: very rarely - myalgia. General disorders and disorders at the injection site: often - increased fatigue; very rarely - hypersensitivity reactions (such as anaphylaxis, Quincke's edema, shortness of breath, itching, rash and urticaria); frequency unknown - asthenia. Children: Cardiac disorders: frequency unknown - prolongation of the QT interval on the ECG, arrhythmia, bradycardia. Nervous system disorders: often (in children under 2 years of age) - insomnia. Mental disorders: the frequency is unknown - a violation of behavior, aggression. Gastrointestinal disorders: often (in children under 2 years of age) - diarrhea. General disorders and disorders at the injection site: often (in children under 2 years old) - high fever. Packing: 60 ml, or 100 ml, or 150 ml in plastic bottles made of polyethylene terephthalate, sealed with polymer screw caps. Each vial, together with a 5.0 ml dosing syringe with an orange plunger (with graduation, ml: 1.0; 1.25; 2.0; 2.5; 3.0; 3.75; 4.0; 5, 0; with a division of 0.25 ml and 0.5 ml), the insert for the syringe dispenser and the leaflet are placed in a pack of cardboard. The insert for the syringe dispenser can be inserted into the neck of the bottle or enclosed in a pack complete with a syringe -dispenser. Storage conditions Store at a temperature not exceeding 25 ° C. Keep out of the reach of children. Shelf life 2 years. Shelf life is indicated on the package. Do not use after the expiry date stated on the packaging. Shelf life after opening 6 months. Dispensing conditionsWithout a doctor's prescription. Buy Desloratadine FT syrup 0.5 mg/ml vial 100 ml №1