Alestamin^® (Tablets) Instructions for Use

Marketing Authorization Holder

Sandoz, d.d. (Slovenia)

Manufactured By

Sandoz, Private Limited (India)

ATC Code

R06AX27 (Desloratadine)

Active Substance

Desloratadine (Rec.INN registered by WHO)

Dosage Form

Alestamin®

Film-coated tablets, 5 mg: 10, 20, 30 or 60 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets light blue in color, round, biconvex, with an imprint of “5” on one side.

Excipients: corn starch – 20 mg, microcrystalline cellulose (Avicel PH101) – 49 mg, hypromellose (E-6 LV Premium) – 3 mg, microcrystalline cellulose (Avicel PH 112) – 20 mg, colloidal anhydrous silicon dioxide – 1.5 mg, hydrogenated vegetable oil – 1.5 mg.

Film coating composition: opadry blue (hypromellose – 62.5%, titanium dioxide – 30.3%, macrogol-400 – 6.25%, indigo carmine (E132) – 0.95%) – 3 mg.

10 pcs. – Al/Al blisters (1) – cardboard packs.
10 pcs. – Al/Al blisters (2) – cardboard packs.
10 pcs. – Al/Al blisters (3) – cardboard packs.
10 pcs. – Al/Al blisters (6) – cardboard packs.

Pharmacotherapeutic Group

Antiallergic agent – H₁-histamine receptor blocker

Pharmacological Action

Long-acting histamine H₁-receptor blocker. It is the primary active metabolite of loratadine. Inhibits the release of histamine and leukotriene C₄ from mast cells. Prevents the development and alleviates the course of allergic reactions. Has antiallergic, antipruritic, and anti-exudative effects.

Reduces capillary permeability, prevents the development of tissue edema, and relieves spasm of smooth muscles. 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). Does not penetrate the BBB. 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 using desloratadine at a dose of 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, with or without food.

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

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

For children aged 1 to 5 years, the recommended dose is 1.25 mg (one-quarter tablet).

Use with caution in patients with severe renal impairment.

This medication is contraindicated in children under 1 year of age.

Do not exceed the recommended daily dose.

Adverse Reactions

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

Digestive system disorders: dry mouth, hepatitis.

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

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 (breastfeeding) period.

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 the ability to drive vehicles and operate machinery

No adverse effects on driving a car or operating complex technical devices have been noted.

Drug Interactions

A study 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.