Nalorius^® (Tablets) Instructions for Use

Marketing Authorization Holder

NANOLEK LLC (Russia)

ATC Code

R06AX27 (Desloratadine)

Active Substance

Desloratadine (Rec.INN registered by WHO)

Dosage Form

Nalorius®

Film-coated tablets, 5 mg: 7, 10, 14, 20, 21, 30, 35 or 50 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets blue in color, round, biconvex; slight surface roughness is acceptable; the color of the tablet core is white or white with a yellowish or pinkish tint.

Excipients: calcium hydrogen phosphate dihydrate – 145.4 mg, microcrystalline cellulose – 14.8 mg, hypromellose (hydroxypropyl methylcellulose) – 3.7 mg, pregelatinized starch – 5.55 mg, croscarmellose sodium – 1.85 mg, colloidal silicon dioxide (aerosil) – 1.85 mg, magnesium stearate – 1.85 mg.

Shell composition Opadry II blue (lactose monohydrate – 36%, hypromellose (E464) – 28%, titanium dioxide (E171) – 23%, polyethylene glycol (macrogol) (E1521) – 10%, indigo carmine (E132) – 2.5%, brilliant blue (E133) – 0.38%, yellow iron oxide (E172) – 0.12%) – 4.967 mg, simethicone emulsion (water, polydimethylsiloxane, polyethylene glycol sorbitan tristearate, methylcellulose, silica gel, polyethylene glycol stearate, sorbic acid, benzoic acid, sulfuric acid) – 0.033 mg.

7 pcs. – blister packs (1) – cardboard packs.
7 pcs. – blister packs (2) – cardboard packs.
7 pcs. – blister packs (3) – cardboard packs.
7 pcs. – blister packs (5) – cardboard packs.
10 pcs. – blister packs (1) – cardboard packs.
10 pcs. – blister packs (2) – cardboard packs.
10 pcs. – blister packs (3) – cardboard packs.
10 pcs. – blister packs (5) – cardboard packs.

Clinical-Pharmacological Group

Histamine H₁-receptor blocker. Antiallergic drug

Pharmacotherapeutic Group

Systemic antihistamines; other systemic antihistamines

Pharmacological Action

Histamine H₁-receptor blocker (long-acting). It is the primary active metabolite of loratadine. It inhibits the release of histamine and leukotriene C₄ from mast cells. It prevents the development and alleviates the course of allergic reactions. It has antiallergic, antipruritic, and anti-exudative effects. It reduces capillary permeability, prevents the development of tissue edema, and relieves smooth muscle spasm.

It has practically no sedative effect and, when taken at a dose of 7.5 mg, does not affect the speed of psychomotor reactions. In comparative studies of desloratadine and loratadine, no qualitative or quantitative differences in the toxicity of the two drugs at comparable doses (taking into account the concentration of desloratadine) were identified.

Pharmacokinetics

After oral administration, it begins to be detected in plasma within 30 minutes. Food does not affect distribution. Bioavailability is proportional to the dose in the range from 5 mg to 20 mg. Plasma protein binding is 83-87%. After a single dose of 5 mg or 7.5 mg, C_max is reached in 2-6 hours (on average in 3 hours). It does not penetrate the blood-brain barrier.

It is intensively metabolized in the liver by hydroxylation to form 3-OH-desloratadine, conjugated with glucuronide; only a small part of the orally administered dose is excreted by the kidneys (<2%) and with feces (<7%). T_1/2 is 20-30 hours (on average – 27 hours). When desloratadine was used at doses from 5 mg to 20 mg once a day for 14 days, no signs of clinically significant accumulation were detected.

Indications

Seasonal allergic rhinitis, chronic idiopathic urticaria.

ICD codes

Dosage Regimen

Administer orally once daily. Intake is independent of food.

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

For children aged 6 to 11 years, the dose is 2.5 mg (half a tablet).

For children aged 1 to 5 years, the dose is 1.25 mg (a quarter of a tablet).

Ensure accurate dosing for pediatric patients; use a suitable tablet splitter if necessary.

The total daily dose must not be exceeded.

For patients with severe renal impairment, use requires special caution.

The drug is contraindicated for children under 1 year of age.

Adverse Reactions

Nervous system disorders: headache, hallucinations, psychomotor hyperactivity, convulsions.

Gastrointestinal disorders: dry mouth, hepatitis.

Other: photosensitivity, myalgia, dyspnea, feeling of fatigue.

Contraindications

Phenylketonuria, pregnancy, lactation, children under 1 year of age, hypersensitivity to desloratadine.

Use in Pregnancy and Lactation

Desloratadine is contraindicated for use during pregnancy and during the lactation period (breastfeeding).

Use in Renal Impairment

Desloratadine should be used with caution in severe renal impairment.

Pediatric Use

Contraindicated in children under 2 years of age.

Special Precautions

Desloratadine should be used with caution in severe renal impairment.

Effect on ability to drive vehicles and operate machinery

No adverse effects on driving a car or operating complex machinery have been reported.

Drug Interactions

Studies of interaction with ketoconazole and erythromycin did not reveal clinically significant changes.

Does not affect the effects of ethanol.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

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.