Ezlor (Tablets) Instructions for Use

Marketing Authorization Holder

Atoll LLC (Russia)

Manufactured By

Ozon, LLC (Russia)

Contact Information

OZON LLC (Russia)

ATC Code

R06AX27 (Desloratadine)

Active Substance

Desloratadine (Rec.INN registered by WHO)

Dosage Form

Ezlor

Film-coated tablets, 5 mg: 10, 20, 30, 40, 50, 60, 80 or 100 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets white or almost white, cylindrical, biconvex; a cross-section shows two layers – a white or almost white core and a film coating.

Excipients: lactose monohydrate 70 mg, microcrystalline cellulose 12.1 mg, povidone 3 mg, magnesium stearate 0.9 mg, croscarmellose sodium 4 mg.

Film coating composition: Opadry II 85F48105 White 3 mg (including polyvinyl alcohol 1.407 mg, macrogol 3350 0.708 mg, talc 0.522 mg, titanium dioxide 0.363 mg).

10 pcs. – blister packs (aluminum/PVC) (1) – cardboard packs.
10 pcs. – blister packs (aluminum/PVC) (2) – cardboard packs.
10 pcs. – blister packs (aluminum/PVC) (3) – cardboard packs.
10 pcs. – blister packs (aluminum/PVC) (4) – cardboard packs.
10 pcs. – blister packs (aluminum/PVC) (5) – cardboard packs.
10 pcs. – blister packs (aluminum/PVC) (6) – cardboard packs.
10 pcs. – blister packs (aluminum/PVC) (8) – cardboard packs.
10 pcs. – blister packs (aluminum/PVC) (10) – cardboard packs.
10 pcs. – polymer jars (1) – cardboard packs.
20 pcs. – polymer jars (1) – cardboard packs.
30 pcs. – polymer jars (1) – cardboard packs.
40 pcs. – polymer jars (1) – cardboard packs.
50 pcs. – polymer jars (1) – cardboard packs.
100 pcs. – polymer jars (1) – cardboard packs.

Clinical-Pharmacological Group

Histamine H₁-receptor blocker. Antiallergic drug

Pharmacotherapeutic Group

Systemically acting antihistamines; other systemically acting antihistamines

Pharmacological Action

Long-acting H₁-histamine receptor blocker. It is the primary active metabolite of loratadine. It inhibits the cascade of allergic inflammation reactions, including the release of anti-inflammatory cytokines such as interleukins IL-4, IL-6, IL-8, IL-13, the release of proinflammatory chemokines (RANTES), the production of superoxide anions by activated polymorphonuclear neutrophils, eosinophil adhesion and chemotaxis, the release of adhesion molecules such as P-selectin, IgE-mediated release of histamine, prostaglandin D2, and leukotriene C4.

Thus, it prevents the development and alleviates the course of allergic reactions, has antipruritic and anti-exudative effects, reduces capillary permeability, prevents the development of tissue edema, and spasm of smooth muscles.

The drug does not affect the CNS, has practically no sedative effect (does not cause drowsiness) and does not affect the speed of psychomotor reactions. It does not cause QT interval prolongation on the ECG. The action of the drug begins within 30 minutes after oral administration and lasts for 24 hours.

Pharmacokinetics

Absorption

After oral administration, Desloratadine is well absorbed from the gastrointestinal tract, with detectable plasma concentrations of desloratadine achieved within 30 minutes, and maximum concentration reached in approximately 3 hours.

Distribution

The binding of desloratadine to plasma proteins is 83-87%. When used in adults and adolescents for 14 days at doses from 5 mg to 20 mg once daily, no clinically significant accumulation of desloratadine was noted. Concurrent intake of food or grapefruit juice does not affect the distribution of desloratadine (when taken at a dose of 7.5 mg once daily). It does not cross the blood-brain barrier.

Metabolism

It undergoes extensive metabolism in the liver by hydroxylation to form 3-OH-desloratadine, conjugated with glucuronide. It is not an inhibitor of CYP3A4 and CYP2D6 isoenzymes and is not a substrate or inhibitor of P-glycoprotein.

Elimination

Only a small portion of the orally administered dose is excreted by the kidneys (< 2%) and through the intestines (< 7%). T_1/2 is 20-30 hours (average 27 hours).

Indications

• Allergic rhinitis (relief or elimination of sneezing, nasal congestion, nasal discharge, nasal itching, itching of the palate, itching and redness of the eyes, lacrimation);
• Urticaria (reduction or elimination of skin itching, rash).

ICD codes

Dosage Regimen

Swallow the tablet whole with water; do not chew.

Take the dose once daily at the same time each day, with or without food.

For adults and adolescents 12 years and older, the standard dose is one 5 mg tablet daily.

Do not exceed the recommended daily dose.

For patients with severe renal impairment, use with caution; no specific dosage adjustment is recommended, but closer monitoring may be required.

The duration of treatment depends on the indication and clinical response; continue use for as long as allergen exposure persists for allergic rhinitis.

For chronic idiopathic urticaria, continue treatment until symptoms are controlled.

If a dose is missed, take it as soon as remembered unless it is almost time for the next scheduled dose; in that case, skip the missed dose and resume the usual schedule.

Do not take a double dose to make up for a forgotten one.

Discontinue use and consult a physician if symptoms persist or worsen after starting therapy.

Adverse Reactions

The frequency of adverse effects is classified according to World Health Organization recommendations: very common – not less than 10%; common – not less than 1%, but less than 10%; uncommon – not less than 0.1%, but less than 1%; rare – not less than 0.01%, but less than 0.1%; very rare – less than 0.01%.

Immune system disorders very rare – rash, including urticaria, angioedema, urticaria, dyspnea, anaphylactic shock.

Nervous system disorders uncommon – headache; very rare – dizziness, drowsiness, insomnia, psychomotor hyperactivity, convulsions, hallucinations.

Cardiac disorders very rare – tachycardia, palpitations.

Gastrointestinal disorders uncommon – dry mouth; very rare – nausea, vomiting, dyspepsia, diarrhea, abdominal pain, increased liver enzyme activity, increased bilirubin concentration, hepatitis.

Musculoskeletal and connective tissue disorders very rare – myalgia.

General disorders common – increased fatigue.

Contraindications

• Hypersensitivity to any of the components of the drug;
• Pregnancy and lactation;
• Age under 12 years;
• Lactose intolerance, lactase deficiency, or glucose-galactose malabsorption syndrome.

With caution severe renal impairment.

Use in Pregnancy and Lactation

The use of the drug during pregnancy is contraindicated due to the lack of clinical data on its safety during pregnancy.

Desloratadine is excreted in breast milk, therefore the use of the drug during breastfeeding is contraindicated.

Use in Renal Impairment

Should be used with caution in severe renal impairment.

Pediatric Use

Contraindicated in children under 12 years of age.

Special Precautions

Effect on ability to drive vehicles and operate machinery

At the recommended dose, the drug does not affect the ability to drive vehicles or operate machinery.

Overdose

Symptoms intake of a dose five times the recommended dose did not lead to any symptoms. In clinical studies, daily use of desloratadine in adults and adolescents at doses up to 20 mg for 14 days was not accompanied by statistically or clinically significant changes in the cardiovascular system. In a clinical-pharmacological study, the use of desloratadine at a dose of 45 mg per day (9 times the recommended dose) for 10 days did not cause QT interval prolongation and was not accompanied by the occurrence of serious adverse effects.

Treatment in case of accidental ingestion of a large amount of the drug – gastric lavage, administration of activated charcoal; if necessary – symptomatic therapy. Desloratadine is not eliminated by hemodialysis; the effectiveness of peritoneal dialysis has not been established.

Drug Interactions

No interactions with other medicinal products have been identified.

Food intake does not affect the efficacy of the drug.

Desloratadine does not enhance the effect of alcohol on the central nervous system.

Storage Conditions

In a light-protected place at a temperature not exceeding 25°C (77°F). Keep out of reach of children.

Shelf Life

Shelf life – 3 years.

Dispensing Status

Over-the-counter.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.