Eridex®

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT Eridez® (Eridez)

Composition:

Active substance: desloratadine;

One orally disintegrating tablet contains desloratadine 5 mg;

Excipients: carbomer potassium salt, potassium hydroxide, iron oxide red (E 172), magnesium stearate, sodium croscarmellose, aspartame (E 951), microcrystalline cellulose, mannitol (E 421), "Tutti Frutti" flavoring (containing propylene glycol (E 1520)).

Pharmaceutical form. Orally disintegrating tablets.

Main physicochemical properties: round, flat, reddish-brown tablets with bevelled edges and "5" embossed on one side.

Pharmacotherapeutic group. Antihistamines for systemic use. Other antihistamines for systemic use. Desloratadine. ATC code R06AX27.

Pharmacological properties.

Pharmacodynamics.

Desloratadine is a non-sedating, long-acting antihistamine with selective antagonistic activity at peripheral H1 receptors. After oral administration, desloratadine selectively blocks peripheral histamine H1 receptors. In vitro studies have demonstrated desloratadine's anti-allergic properties on endothelial cells. These were manifested by inhibition of proinflammatory cytokine release—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.

Studies have shown that, in addition to its antihistaminic activity, desloratadine exerts anti-allergic and anti-inflammatory effects.

Desloratadine does not penetrate the central nervous system (CNS) and does not affect psychomotor function.

In patients with allergic rhinitis, desloratadine effectively relieves symptoms such as sneezing, rhinorrhea, nasal and ocular itching, tearing, eye redness, and palate itching. Desloratadine provides effective symptom control for up to 24 hours.

Pharmacokinetics.

Absorption

Desloratadine plasma concentrations can be detected within 30 minutes after administration.

Desloratadine is well absorbed, with peak concentrations reached approximately 3 hours after intake.

Distribution

Desloratadine bioavailability was dose-proportional over the range of 5 mg to 20 mg. Desloratadine is moderately bound to plasma proteins (83–87%). No evidence of clinically significant drug accumulation was observed after administration of 5 mg to 20 mg once daily for 14 days.

It has been established that food (a high-fat, high-calorie breakfast) and grapefruit juice do not affect the distribution of desloratadine.

Metabolism

Desloratadine does not inhibit CYP3A4 in vivo, and in vitro studies have shown that the drug does not inhibit CYP2D6 and is neither a substrate nor an inhibitor of P-glycoprotein.

Elimination

The elimination half-life is approximately 27 hours. The extent of desloratadine accumulation corresponds to its half-life (approximately 27 hours) and the once-daily dosing regimen.

Preclinical safety data.

Desloratadine is the principal active metabolite of loratadine. Preclinical studies of both compounds have not revealed qualitative or quantitative differences in their toxicological profiles at comparable desloratadine exposure levels. Data from standard studies on pharmacological safety, repeated-dose toxicity, genotoxicity, and reproductive toxicity indicate no special hazard for humans with desloratadine. Furthermore, no studies conducted to date have demonstrated carcinogenic potential for either desloratadine or loratadine.

Clinical characteristics.

Indications.

Relief of symptoms associated with:

• allergic rhinitis;
• urticaria.

Contraindications.

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

Interaction with other medicinal products and other forms of interaction.

In clinical studies of desloratadine tablets, no clinically significant interactions were observed when co-administered with erythromycin or ketoconazole. In clinical-pharmacological studies, no enhancement of the negative impact of ethanol on psychomotor function was noted when the drug was used concomitantly with alcohol. However, during the post-marketing period, cases of alcohol intolerance and alcohol intoxication during the use of the drug were reported. Therefore, caution should be exercised when consuming alcohol during treatment with desloratadine.

Special precautions for use

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

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

The medicinal product contains the excipient aspartame, which is a source of phenylalanine; therefore, its use may be hazardous for patients with phenylketonuria.

In addition, the medicinal product Eridez® contains 5 mg of potassium per dose and should thus be used with caution in patients with impaired renal function and/or those on a potassium-restricted diet.

The medicinal product Eridez® also contains the excipient mannitol, which may cause a mild laxative effect.

Use during pregnancy or breastfeeding.

Desloratadine did not show teratogenic effects in animal studies.

The safety of using the drug during pregnancy has not been established; therefore, the use of Eridez® is not recommended during pregnancy.

Breastfeeding.

Desloratadine passes into breast milk; therefore, the use of Eridez® is not recommended in women who are breastfeeding.

Ability to influence reaction rate while driving or operating machinery.

No reduction in performance has been observed in patients receiving desloratadine. However, patients should be informed that very rarely somnolence may occur in some individuals, which could affect their ability to drive or operate machinery.

Method of Administration and Dosage.

Adults and adolescents (aged 12 years and older): 1 tablet once daily, regardless of food intake, to relieve symptoms associated with allergic rhinitis (including intermittent and persistent allergic rhinitis) and urticaria.

Treatment of intermittent allergic rhinitis (symptoms present less than 4 days per week or less than 4 weeks) should be based on clinical history: discontinue after symptoms resolve and resume upon their recurrence. For persistent allergic rhinitis (symptoms present more than 4 days per week or longer than 4 weeks), treatment should continue throughout the entire period of allergen exposure.

Method of Administration.

Immediately before administration, carefully open the blister pack and remove the orally disintegrating tablet without crushing it, so that it remains intact. Place the tablet in the mouth, where it will disintegrate rapidly. No water or other liquid is required to swallow the tablet. The dose should be taken immediately after opening the blister.

Children.

This medicinal product in this dosage form is indicated for use in children aged 12 years and older.

Overdose.

In case of overdose, standard measures aimed at removing the unabsorbed active substance should be implemented. Symptomatic and supportive treatment is recommended. During studies involving multiple doses administered to adults and adolescents, doses up to 45 mg of desloratadine (9 times the therapeutic dose) did not result in clinically significant adverse effects.

Desloratadine is not eliminated by hemodialysis. It is unknown whether desloratadine is removed by peritoneal dialysis.

Adverse Reactions

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

The most commonly 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 commonly reported adverse reaction was headache, occurring in 5.9% of patients treated with desloratadine and in 6.9% of patients receiving placebo.

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 events have been observed (frequency unknown): QT interval prolongation, arrhythmias, and bradycardia.

The frequency of adverse reactions is classified as follows: very common (≥ 1/10), common (≥ 1/100 to < 1/10), uncommon (≥ 1/1,000 to < 1/100), rare (≥ 1/10,000 to < 1/1,000), very rare (< 1/10,000), frequency not known (cannot be estimated from available data).

Reporting of suspected adverse reactions.

Reporting of suspected adverse reactions after drug registration is of great importance. It enables continuous monitoring of the benefit-risk balance of the medicinal product. Healthcare and pharmacy professionals, as well as patients or their legal representatives, are encouraged to report all cases of suspected adverse reactions and/or lack of efficacy via the Automated Pharmacovigilance Information System at the following link: https://aisf.dec.gov.ua.

Shelf life. 3 years.

Storage conditions.

Store in the original packaging at a temperature not exceeding 25 °C.

Keep out of reach of children.

Packaging.

Dispersible tablets 5 mg; 10 tablets per blister pack, 1 blister pack per carton.

Availability category. Over-the-counter (without prescription).

Manufacturer.

GenePharm S.A.

(manufacturing of the finished product, primary and secondary packaging, batch control, batch release)

Pharmapas S.A.

(manufacturing of the finished product, primary and secondary packaging, batch control, batch release)

Manufacturer's address and place of business.

18 Km Meresono Avenue, Pallini, 153 51, Greece

28 Octovriou 1, Agia Barbara, 123 51, Greece

Marketing Authorization Holder. JSC "Pharmaceutical Company "Darnytsia".

Address of the Marketing Authorization Holder.

13 Boryspylska Street, Kyiv, 02093, Ukraine