Eridez-darnitsa

INSTRUCTION for medical use of the medicinal product Eridez-Darnitsia (Eridez-Darnitsa)

Composition:

active substance: desloratadine;

1 tablet contains 5 mg of desloratadine;

excipients: calcium hydrogen phosphate, microcrystalline cellulose, lactose monohydrate, maize starch, magnesium stearate, Opadry 85 F blue.

Medicinal form. Film-coated tablets.

Main physicochemical properties: blue, round, biconvex, film-coated tablets.

Pharmacotherapeutic group. Antihistamines for systemic use. ATC code R06AX27.

Pharmacological properties.

Pharmacodynamics.

Desloratadine is a selective blocker of peripheral histamine H1-receptors that does not cause sedative effects. Desloratadine is the principal active metabolite of loratadine. After oral administration, desloratadine selectively blocks peripheral H1-histamine receptors and does not penetrate the blood-brain barrier.

In addition to its antihistaminic activity, desloratadine exerts anti-allergic and anti-inflammatory effects. It has been shown that desloratadine inhibits a cascade of various reactions underlying the development of allergic inflammation, namely: the release of proinflammatory cytokines such as IL-4, IL-6, IL-8, and IL-13 from human mast cells/basophils, as well as inhibition of adhesion molecule expression, including P-selectin. The clinical significance of these observations remains to be confirmed.

In high-dose clinical studies, where desloratadine was administered daily at doses up to 20 mg for 14 days, no statistically significant cardiovascular effects were observed. In a clinical-pharmacological study using 45 mg daily (10 times the maximum recommended daily clinical dose) for 10 days, no QT interval prolongation was observed.

In patients with allergic rhinitis, desloratadine effectively relieved symptoms such as sneezing, rhinorrhea, and pruritus, as well as ocular symptoms including itching, tearing, and redness, and also relieved palatal itching. Desloratadine provided effective symptom control for 24 hours.

Desloratadine barely penetrates the central nervous system. In controlled clinical trials, at the recommended daily dose of 5 mg, the incidence of somnolence was not different from placebo.

Desloratadine does not cross the blood-brain barrier and does not affect psychomotor function when administered at doses up to 7.5 mg.

Desloratadine effectively improved the severity of seasonal allergic rhinitis, as measured by the total score of the rhinoconjunctivitis quality-of-life questionnaire. The greatest improvement was observed in questionnaire items related to practical problems and daily activities limited by symptoms.

Chronic idiopathic urticaria has been studied in a clinical model of urticaria. Since histamine release is a causative factor in all forms of urticaria, desloratadine is expected to effectively relieve symptoms in other forms of urticaria besides chronic idiopathic urticaria.

In two placebo-controlled, 6-week studies involving patients with chronic idiopathic urticaria, desloratadine effectively relieved pruritus and reduced the number and size of hives by the end of the first dosing interval. In each study, the effect lasted throughout the 24-hour dosing interval. A reduction in pruritus by more than 50% was observed in 55% of patients taking desloratadine, compared to 19% of patients receiving placebo. The drug did not significantly affect sleep or daytime activity.

Pharmacokinetics.

Desloratadine is detectable in plasma within 30 minutes after administration. The maximum plasma concentration of desloratadine is reached on average within 3 hours; the elimination half-life averages 27 hours. The extent of desloratadine accumulation corresponds to its half-life (approximately 27 hours) and frequency of administration (once daily). Desloratadine bioavailability is dose-proportional in the range of 5 to 20 mg.

Desloratadine is moderately bound (83–87%) to plasma proteins. No evidence of clinically significant drug accumulation was observed after administration of desloratadine at doses of 5 to 20 mg once daily for 14 days.

Food (a high-fat, high-calorie breakfast) or grapefruit juice does not affect the distribution of desloratadine.

Clinical characteristics.

Indications.

Relief of symptoms associated with:

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

Contraindications.

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

Interaction with other medicinal products and other forms of interaction.

If the patient is taking any other medicinal products, this must be reported to the physician.

Clinically significant changes in plasma concentrations of desloratadine were not observed during repeated co-administration with ketoconazole, erythromycin, azithromycin, fluoxetine, or cimetidine.

Clinical pharmacological studies did not show an enhanced negative effect of ethanol on psychomotor function when the medicinal product was used concomitantly with alcohol. However, during the post-marketing period, cases of alcohol intolerance and alcohol intoxication were reported during use of the medicinal product. Therefore, caution should be exercised when consuming alcohol during treatment with Eridez-Darnitsa.

Special precautions for use.

In patients with severe renal insufficiency, administration of the medicinal product Eridez-Darnytsia should be carried out under medical supervision.

Desloratadine should be prescribed with caution to patients who have a history of seizures. Children may be more susceptible to developing new seizures during desloratadine treatment. The physician must decide whether to discontinue desloratadine therapy in patients who experience a seizure while taking the drug.

If a patient has known sugar intolerances, a physician should be consulted before taking this medicinal product.

Use during pregnancy or breastfeeding.

The safety of Eridez-Darnytsia in pregnant women has not been established; therefore, it is not recommended during pregnancy. Desloratadine passes into breast milk; hence, the medicinal product should not be administered to women who are breastfeeding.

Ability to influence reaction rate when driving or operating machinery.

No effects of desloratadine on the ability to drive or operate machinery have been observed. However, patients should be warned that in very rare cases drowsiness may occur, which could affect their ability to drive or operate complex machinery.

Method of Administration and Dosage

Eridez-Darnitsya is intended for oral administration. Adults and children aged 12 years and older should take 1 tablet (5 mg) once daily, regardless of food intake, to relieve symptoms associated with allergic rhinitis (including intermittent and persistent allergic rhinitis) and urticaria. The tablet should be swallowed whole with water.

The duration of treatment is determined by the severity and course of the disease.

Treatment of intermittent allergic rhinitis (symptoms present for less than 4 days per week or less than 4 weeks) should be administered according to patient history: discontinue after symptoms resolve and resume upon their recurrence.

For persistent allergic rhinitis (symptoms present for more than 4 days per week or more than 4 weeks), treatment should be continued throughout the entire period of allergen exposure.

Children

The efficacy and safety of desloratadine in tablet form have not been studied in children under 12 years of age.

Overdose

In case of overdose, standard measures for removal of unabsorbed active substance should be applied. Symptomatic and supportive therapy is recommended. In clinical studies where desloratadine was administered at doses of 45 mg (9 times higher than the recommended dose), no clinically significant adverse reactions were observed. Desloratadine is not removed by hemodialysis; the effectiveness of peritoneal dialysis has not been established.

Adverse reactions.

During clinical trials for the approved indications, including allergic rhinitis and chronic idiopathic urticaria, adverse effects were reported in patients receiving a 5 mg daily dose 3 % more frequently than in patients receiving placebo.

The most commonly reported adverse reactions compared to placebo were increased fatigue (1.2 %), dry mouth (0.8 %), and headache (0.6 %).

Children. There is a risk of psychomotor hyperactivity (abnormal behavior) associated with the use of desloratadine (which may manifest as irritability and aggression, as well as nervousness).

In the post-marketing period, the following have been observed (frequency unknown): QT interval 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 not known.

If any adverse reactions occur, the patient should consult a doctor.

Shelf life. 2 years.

Do not use the medicinal product after the expiry date.

Storage conditions.

Store in the original packaging, protected from light, at a temperature not exceeding 25 ºC. Keep out of reach of children.

Packaging.

10 tablets in a blister pack; 1, 2, or 3 blisters per carton.

Release category. Over-the-counter.

Manufacturer: JSC "Pharmaceutical company "Darnytsia".

Manufacturer's address:

13, Boryspylska Street, Kyiv, 02093, Ukraine.