Elysium film-coated tablets 5 mg No. 10

Instructions for Elysium film-coated tablets 5 mg No. 10

Composition

active ingredient: desloratadine;

1 tablet contains 5 mg of desloratadine;

excipients: microcrystalline cellulose, corn starch, mannitol (E 421), talc, magnesium stearate;

film coating composition: Opadry Blue 03F20404 (hypromellose, titanium dioxide (E 171), polyethylene glycol (macrogol), indigo carmine aluminum lake (E 132)).

Dosage form

Film-coated tablets.

Main physicochemical properties: round, biconvex, blue tablets, film-coated, marked “LT” on one side.

Pharmacotherapeutic group

Antihistamines for systemic use. ATX code R06A X27.

Pharmacodynamics

Desloratadine is a long-acting, non-sedating antihistamine with selective peripheral H1-receptor antagonist activity. 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 the 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 the inhibition of the expression of adhesion molecules, such as P-selectin. The clinical relevance of these observations requires further confirmation.

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, when desloratadine was administered at a dose of 45 mg per day (10 times the maximum daily clinical dose) for

10 days, no prolongation of the QT interval was recorded.

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 somnolence at the recommended dose of 5 mg/day was not different from that of placebo. In clinical trials, a single dose of desloratadine at a daily dose of 7.5 mg did not affect psychomotor performance.

Desloratadine effectively alleviated 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, which were limited by symptoms.

Chronic idiopathic urticaria has been studied in a clinical urticaria model. 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 as well.

In two placebo-controlled 6-week studies in patients with chronic idiopathic urticaria, desloratadine was effective in relieving pruritus and reducing the number and size of hives by the end of the first dosing interval. In each study, the effect was maintained throughout the 24-hour dosing interval. Itch relief of more than 50% was observed in 55% of patients taking desloratadine compared with 19% of patients taking placebo. The drug did not significantly affect sleep or daytime activity.

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 desloratadine accumulation 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 participants had higher concentrations of desloratadine. 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 in 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 (a high-fat, high-calorie breakfast) did not affect the pharmacokinetics of desloratadine. Grapefruit juice also did not affect the pharmacokinetics of desloratadine.

Indication

Elimination of symptoms associated with:

• allergic rhinitis (see section "Pharmacological properties");
• urticaria (see section "Pharmacological properties").

Contraindication

Hypersensitivity to the active substance or to any of the excipients or to loratadine.

Interaction with other medicinal products and other types of interactions

In clinical studies of desloratadine tablets, no clinically significant interactions were observed when erythromycin or ketoconazole were co-administered.

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 with desloratadine.

Application features

In patients with severe renal insufficiency, Elysium should be administered under the supervision of a physician.

Desloratadine should be used with caution in patients with a history of seizures. Children may be more likely to develop a new seizure while receiving desloratadine. The physician should consider discontinuing desloratadine in patients who develop a seizure while receiving the drug.

Ability to influence reaction speed when driving vehicles or other mechanisms

In clinical studies, no impairment of the ability to drive was observed in patients taking desloratadine. Patients should be informed that very rarely, some people experience drowsiness while taking desloratadine, which may affect their ability to drive or operate machinery.

Use during pregnancy or breastfeeding

Desloratadine did not demonstrate teratogenic properties in animal studies.

The safety of the drug during pregnancy has not been established, therefore the use of Elysium during this period is not recommended.

Desloratadine passes into breast milk, so the use of Elysium in breastfeeding women is not recommended.

Method of administration and doses

Adults and children over 12 years of age: 1 tablet once daily, regardless of meals, for the relief of symptoms associated with allergic rhinitis (including intermittent and persistent allergic rhinitis) and urticaria.

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 Elysium tablets 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; its removal by peritoneal dialysis has not been established.

Adverse reactions

In clinical trials for 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 commonly reported side effects 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 treated with desloratadine and 6.9% of patients treated with 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.

Summary table of adverse reaction frequencies.

The frequency of adverse reactions is classified as follows: very common (≥1/10), common (≥1/100, <1/10), uncommon (≥1/1000, <1/100), rare (≥1/10000, <1/1000), very rare (<1/10000) and frequency unknown.

Expiration date

3 years.

Storage conditions

Store at a temperature not exceeding 25 ° C. Keep out of the reach of children.

Packaging

10 tablets in an aluminum blister. 1 or 3 blisters in a cardboard pack.

Vacation category

Without a prescription.

Producer

Actavis Ltd.

Location of the manufacturer and address of its place of business.

BLB 015, BLB 016, Bulebel Industrial Estate, Zeitoun, ZTN 3000, Malta.

Applicant.

Joint Ukrainian-Spanish enterprise "Sperco Ukraine".

Location of the applicant.

21027, Ukraine, Vinnytsia, 600-anniversary St., 25.

Phone: + 38(0432)52-30-36. E-mail: trade@sperco.com.ua

www.sperco.ua