Alergozan film-coated tablets 5 mg No. 30

Instructions for use Allergozan film-coated tablets 5 mg No. 30

Composition

active ingredient: desloratadine;

1 tablet contains desloratadine 5 mg;

excipients: microcrystalline cellulose, calcium hydrogen phosphate dihydrate, corn starch, hypromellose, talc, sodium stearyl fumarate, colloidal anhydrous silicon dioxide;

film coating: Opadry II 33G 205005 blue (hypromellose, lactose monohydrate, titanium dioxide (E 171), macrogol 3350, triacetin, indigo carmine aluminum lake (E 132), quinoline yellow aluminum lake (E 104)).

Dosage form

Film-coated tablets.

Main physicochemical properties: light blue, round, biconvex tablets, film-coated, 6 mm ± 0.2 mm in diameter.

Pharmacotherapeutic group

Other antihistamines for systemic use.

ATX code R06A X27.

Pharmacological properties

Pharmacodynamics

Desloratadine is a long-acting, non-sedating antihistamine that selectively antagonizes peripheral H1 receptors. 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 the cell adhesion molecule P-selectin on endothelial cells. The clinical significance of these observations remains to be confirmed.

In high-dose clinical studies in which desloratadine was administered daily at a dose of up to 20 mg for 14 days, no statistically or clinically significant changes in the cardiovascular system were observed. In a clinical pharmacology study in which desloratadine was administered at a dose of 45 mg per day (9 times the clinical dose) for 10 days, no prolongation of the QT interval was observed.

Desloratadine has little or no penetration into the central nervous system. In controlled clinical trials, no excess incidence of drowsiness was observed compared to placebo at the recommended dose of 5 mg/day. In clinical trials, desloratadine at a single daily dose of 7.5 mg had no effect on psychomotor performance.

In clinical pharmacology studies, alcohol-related impairments such as impaired performance or increased drowsiness did not progress when co-administered with alcohol. There were no significant differences in psychomotor performance between the desloratadine and placebo groups, either alone or with alcohol.

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 is effective in alleviating the severity of seasonal allergic rhinitis as measured by the Rhinoconjunctivitis Quality of Life Questionnaire. The greatest improvement was seen in items related to practical problems and daily activities that were limited by symptoms.

Chronic idiopathic urticaria has been studied in a clinical model of urticaria conditions. 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, in addition to chronic idiopathic urticaria, as recommended in clinical guidelines.

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 has no significant effect on sleep and daytime activity.

Pharmacokinetics

Absorption. Plasma concentrations of desloratadine can be determined within 30 minutes of dosing. Desloratadine is well absorbed, with peak concentrations occurring approximately 3 hours after dosing; the elimination half-life is approximately 27 hours. The extent of accumulation of desloratadine 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.

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 accumulation of the active substance.

Metabolism: 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 and is neither a substrate nor an inhibitor of P-glycoprotein.

Conclusion: In a single-dose study of desloratadine 7.5 mg, food intake (a high-fat, high-calorie breakfast) did not affect the pharmacokinetics of desloratadine. Grapefruit juice was also found to have no effect on the pharmacokinetics of desloratadine.

Indication

Desloratadine is prescribed to adults and children over 12 years of age to relieve 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 of the drug or to loratadine.

Interaction with other medicinal products and other types of interactions

In clinical studies of desloratadine tablets with concomitant use of erythromycin or ketoconazole, no clinically significant interactions were observed.

According to clinical and pharmacological studies, when the drug is used simultaneously with alcohol, there was no increase in the negative effect of ethanol on psychomotor function. 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 simultaneously during treatment with desloratadine.

Application features

In patients with severe renal insufficiency, desloratadine should be administered under medical supervision.

Desloratadine should be used with caution in patients with a medical or family history of seizures, especially young children, who are more likely to develop new seizures when treated with desloratadine. The physician may consider discontinuing desloratadine in patients who experience seizures during treatment.

Desloratadine contains lactose. Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.

Ability to influence reaction speed when driving vehicles or other mechanisms

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

Use during pregnancy or breastfeeding

Pregnancy: Desloratadine has not been shown to be teratogenic in animal studies. The safety of the drug during pregnancy has not been established, therefore the use of desloratadine during this period is not recommended.

Breastfeeding. Desloratadine passes into breast milk, so its use in women who are breastfeeding is not recommended.

Method of administration and doses

Administer orally, regardless of meals.

Adults and children over 12 years of age: 1 tablet once daily, with or without food, is recommended 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 in adolescents aged 12 to 17 years (see section 4.8).

There are no established data on the efficacy and safety of desloratadine in children under 12 years of age.

Overdose

In case of overdose, adverse reactions are similar to those observed at therapeutic doses, but the manifestations may be more severe.

Symptoms: In clinical studies in which desloratadine was administered at doses up to 45 mg (9 times the recommended dose), no clinically significant adverse reactions were observed.

Treatment. In case of overdose, standard measures should be taken to remove unabsorbed active substance. Symptomatic and supportive treatment is recommended. 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 reactions to desloratadine were reported at a rate of 3% more frequently in patients receiving the recommended dose of 5 mg daily than in patients receiving placebo.

The most frequently reported adverse reactions 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 receiving desloratadine and 6.9% of patients receiving placebo.

Other adverse reactions observed in the post-marketing period with an unknown frequency: QT prolongation, arrhythmia and bradycardia.

Summary table of adverse reaction frequencies.

Frequencies are defined as 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 (cannot be estimated from the available data).

Expiration date

2 years.

Storage conditions

Keep out of reach of children.

Store at a temperature not exceeding 25 °C.

Packaging

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

Vacation category

Without a prescription.

Producer

JSC "Sopharma".

Location of the manufacturer and its business address

16 Ilienskoe Shose St., Sofia, 1220, Bulgaria.