Instructions Erius syrup 0.5 mg/ml bottle 60 ml
Composition
active ingredient: desloratadine;
1 ml of syrup contains 0.5 mg of desloratadine;
excipients: propylene glycol, sorbitol solution that does not crystallize, citric acid anhydrous, sodium citrate dihydrate, sodium benzoate (E 211), disodium edetate, sucrose, natural and artificial flavor with chewing gum flavor (No. 15864), FD&C yellow dye No. 6 (E 110), purified water.
Dosage form
Syrup.
Main physicochemical properties: clear orange liquid.
Pharmacotherapeutic group
Antihistamines for systemic use.
ATX code R06A X27.
Pharmacological properties
Pharmacodynamics.
Desloratadine is a potent, selective, non-sedating peripheral histamine H1 receptor blocker. Desloratadine is the primary active metabolite of loratadine.
After oral administration, Erius® selectively blocks peripheral H1-histamine receptors, as the drug almost does not penetrate the blood-brain barrier.
Numerous studies have shown that in addition to its antihistamine activity, Erius® has demonstrated its antiallergic and anti-inflammatory properties. It has been established that Erius® inhibits the cascade of various reactions that underlie allergic inflammation, namely:
release of pro-inflammatory cytokines, including IL-4, IL-6, IL-8, IL-13;
release of pro-inflammatory chemokines such as RANTES;
production of superoxide anion by activated polymorphonuclear neutrophils;
adhesion and chemotaxis of eosinophils;
expression of adhesion molecules such as P-selectin;
IgE-dependent release of histamine, prostaglandin D2, and leukotriene C4;
acute allergic bronchospasm and allergic cough in animal studies.
The safety of Erius® in children has been demonstrated in 3 clinical studies. The drug was administered to children aged 6 months to 11 years who required antihistamine therapy at a daily dose of 1 mg (age group 6 to 11 months), 1.25 mg (age group 1 to 5 years) or 2.5 mg (age group 6 to 11 years). The treatment was well tolerated, as confirmed by the results of clinical laboratory tests, the state of vital body functions and ECG data (including QT interval length).
In clinical studies, daily use of Erius® at a dose of up to 20 mg for 14 days was not accompanied by statistically clinically significant changes in the cardiovascular system. In a clinical pharmacology study, the use of Erius® 45 mg/day (9 times the therapeutic dose) for 10 days did not cause prolongation of the QT interval.
Desloratadine almost does not penetrate the blood-brain barrier. When using the recommended dose of 5 mg, the frequency of drowsiness did not exceed that in the placebo group. In clinical studies, Erius® did not affect psychomotor functions when taking a dose of up to 7.5 mg.
In addition to the conventional classification of allergic rhinitis into seasonal and perennial, allergic rhinitis can also be alternatively classified into intermittent and persistent based on the duration of symptoms. Intermittent allergic rhinitis is defined as the presence of symptoms for less than 4 days per week or for less than 4 weeks. In the case of persistent allergic rhinitis, symptoms are observed for 4 days or more per week or for a period exceeding 4 weeks.
The clinical efficacy of Erius® in the treatment of seasonal allergic rhinitis was demonstrated in four placebo-controlled, multiple-dose clinical trials.
In patients with allergic rhinitis, Erius® effectively eliminated the following symptoms: sneezing, nasal discharge and itching, as well as eye irritation, tearing and redness, and itching of the palate.
Pharmacokinetics.
Desloratadine begins to be detected in plasma within 30 minutes after taking the drug. Erius® effectively controls symptoms for 24 hours. Desloratadine is well absorbed. The maximum concentration of desloratadine in plasma is achieved on average after 3 hours, the half-life is on average 27 hours. The degree of cumulation of desloratadine corresponds to its half-life (approximately 27 hours) and the frequency of administration (once a day). The bioavailability of desloratadine was proportional to the dose in the range from 5 to 20 mg.
Desloratadine is moderately (83–87%) bound to plasma proteins. When desloratadine was administered at a dose of 5 to 20 mg once daily for 14 days, there was no evidence of clinically significant accumulation of the drug.
Poor metabolism of desloratadine has been reported in approximately 8% of subjects, with significant increases in plasma levels and prolonged half-life. The prevalence of poor metabolism may be related to race. This finding is currently considered clinically irrelevant.
When conducting cross-comparative studies with the same dose of the drug, bioequivalence of the drug in the form of tablets and syrup was revealed.
The results of the studies showed that desloratadine does not inhibit CYP3A4 or CYP2D6 and is neither a substrate nor an inhibitor of P-glycoprotein.
Indication
To relieve symptoms associated with allergic rhinitis, such as sneezing, nasal discharge, itching, swelling and nasal congestion, as well as itching and redness of the eyes, tearing, itching of the palate and cough.
To relieve symptoms associated with hives, such as itching and rash.
Contraindication
Hypersensitivity to desloratadine, to any auxiliary component of the drug or to loratadine.
Interaction with other medicinal products and other types of interactions
No clinically significant changes in plasma concentrations of desloratadine were observed with repeated concomitant use with ketoconazole, erythromycin, azithromycin, fluoxetine, or cimetidine. Since the enzyme responsible for the metabolism of desloratadine has not been identified, interactions with other drugs cannot be completely excluded.
Food (fatty high-calorie breakfast) or grapefruit juice do not affect the distribution of desloratadine.
Impact on laboratory test results
The use of Erius® should be discontinued approximately 48 hours before skin testing, as antihistamines may prevent or reduce the manifestation of positive dermatological reactions to irritants.
Application features
In clinical pharmacology studies, Erius® did not potentiate the following effects of alcohol: impaired psychomotor function and drowsiness. The results of psychomotor tests did not differ significantly in patients who used Erius® and patients who took placebo, either alone or with alcohol.
In patients with severe renal insufficiency, Erius® should be taken under medical supervision. The drug contains sorbitol, so it should not be used in patients with congenital fructose intolerance.
Desloratadine should be used with caution in patients with a history of seizures. Children may be more susceptible to developing a new seizure while receiving desloratadine. The physician should consider discontinuing desloratadine in patients who experience a seizure while receiving desloratadine.
Use during pregnancy or breastfeeding
A large amount of data on the use of desloratadine during pregnancy (more than 1000 cases) indicate the absence of teratogenic, fetotoxic effects and adverse effects on the newborn. Animal studies have not revealed direct or indirect adverse effects on reproductive function. As a precautionary measure, it is preferable to avoid the use of the drug Erius® during pregnancy.
Desloratadine passes into breast milk, therefore, nursing women are advised to decide whether it is necessary to discontinue breastfeeding or to avoid the use of the drug, taking into account the benefit of breastfeeding for the child and the benefit of the drug for the mother.
Fertility: There are no data on the effect on fertility.
Ability to influence reaction speed when driving vehicles or other mechanisms
Clinical trial data indicate that Erius® has no or negligible influence on the ability to drive or use machines. Patients should be advised that most people do not experience drowsiness. It should be noted that individual responses to medications may vary. Patients are advised not to engage in activities that require concentration, such as driving or operating machinery, until they have determined how they respond to the medication.
Method of administration and doses
To eliminate symptoms associated with allergic rhinitis (including intermittent and persistent) and urticaria, Erius® is used regardless of meals in the following doses:
Adults and adolescents (≥12 years): 10 ml of syrup (5 mg desloratadine) once daily.
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 disappearance of symptoms and resume after their reappearance. In persistent allergic rhinitis (presence of symptoms more than 4 days per week or more than 4 weeks), treatment should be continued throughout the entire period of contact with the allergen.
Children. The efficacy and safety of Erius® syrup in children under 6 months of age have not been established. The drug is not recommended for use in children under 6 months of age for the treatment of chronic idiopathic urticaria and in children under 12 months of age for the treatment of allergic rhinitis. The following dosage regimen is used for treatment:
children aged 6 to 11 months: 2 ml of syrup (1 mg desloratadine) once a day;
aged 1 to 5 years: 2.5 ml of syrup (1.25 mg of desloratadine) once a day;
aged 6 to 11 years: 5 ml of syrup (2.5 mg of desloratadine) once a day.
Overdose
When desloratadine was used in doses up to 45 mg (9 times the recommended dose) in clinical studies in adults and adolescents, no clinically significant effects were observed.
Desloratadine is not removed by hemodialysis, and 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 frequently reported adverse events compared to placebo were fatigue (1.2%), dry mouth (0.8%) and headache (0.6%). In clinical trials of Aerius® in children aged 2 to 11 years, the incidence of adverse reactions was similar in both the syrup and placebo groups. In children aged 6 to 23 months, the most frequent adverse events (compared to placebo) were diarrhoea (3.7%), pyrexia (2.3%) and insomnia (2.3%).
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 that have been reported very rarely during post-marketing experience are listed in the table below. The frequency of adverse reactions is classified as follows: very common (≥1/10), common (≥1/100, <1/10), uncommon (≥1/1,000, <1/100), rare (≥1/10,000, <1/1,000), and not known.
| Organ classes/systems | Frequency of occurrence | Adverse reactions |
| Metabolic and nutritional disorders | Frequency unknown | Increased appetite |
| From the psyche | Rare Frequency unknown | Hallucinations Abnormal behavior, aggression |
| From the nervous system | Frequent Common (for children under 2 years of age) Rare | Headache Insomnia Dizziness, drowsiness, insomnia, psychomotor hyperactivity, seizures, depressed mood |
| From the heart | Rare | Tachycardia, palpitations, QT prolongation, supraventricular tachyarrhythmia |
| Gastrointestinal tract | Frequent Common (for children under 2 years of age) Rare | Dry mouth Diarrhea Abdominal pain, nausea, vomiting, dyspepsia, diarrhea |
| Hepatobiliary system | Rare Frequency unknown | Increased liver enzymes, increased bilirubin, hepatitis Jaundice |
| Musculoskeletal and connective tissue disorders | Rare | Myalgia |
| Skin and subcutaneous tissue disorders | Frequency unknown | Photosensitivity |
| From the organs of vision | Frequency unknown | Dry eyes |
| General violations | Frequent Common (for children under 2 years of age) Rare Frequency unknown | Fatigue Temperature increase Hypersensitivity reactions (anaphylaxis, angioedema, shortness of breath, itching, rash, urticaria) Asthenia |
| Research | Frequency unknown | Weight gain |
Desloratadine has little or no penetration into the central nervous system. When used at the recommended adult dose of 5 mg, there was no increase in the incidence of drowsiness compared to placebo. In clinical studies, Aerius® at a single daily dose of 7.5 mg had no effect on psychomotor performance.
Expiration date
2 years.
Storage conditions
Store out of the reach of children at a temperature not exceeding 30 °C.
Packaging
60 ml or 120 ml bottles, closed with a cap with first-open control and child-resistant opening, complete with a measuring spoon or dosing syringe, in a cardboard box.
Vacation category
Without a prescription.
Producer
Organon Heist B.V./
Organon Heist BV
Location of the manufacturer and address of its place of business.
Industriepark 30, Heist-op-den-Berg, 2220, Belgium/
Industriepark 30, Heist-op-den-Berg, 2220, Belgium.
