Loratadine-Akrikhin (Tablets) Instructions for Use

Marketing Authorization Holder

Akrikhin Chemical and Pharmaceutical Plant, JSC (Russia)

Contact Information

AKRIKHIN JSC (Russia)

ATC Code

R06AX13 (Loratadine)

Active Substance

Loratadine (Rec.INN registered by WHO)

Dosage Forms

	Loratadine-Akrikhin	Tablets 10 mg: 7, 10, 21 or 30 pcs.
		Syrup 100 mg/100 ml: 100 ml bottle with a measuring spoon

Dosage Form, Packaging, and Composition

Tablets white or almost white, flat-cylindrical, with a bevel.

Excipients: lactose monohydrate – 110 mg, microcrystalline cellulose – 75 mg, calcium stearate – 2 mg, sodium carboxymethyl starch – 3 mg.

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

Syrup as a clear liquid from light yellow to yellow in color, with a faint fruity odor.

Excipients: sucrose – 35 g, propylene glycol – 20 g, benzoic acid – 0.1 g, citric acid – 0.3 g, ethanol (rectified ethyl alcohol) – 1.58 g, tropaeolin O dye – 0.001 g, orange flavor – 0.08 g, purified water – up to 100 ml.

100 ml – dark glass bottles (1) complete with a measuring spoon – cardboard packs.

Clinical-Pharmacological Group

Histamine H₁-receptor blocker. Antiallergic drug

Pharmacotherapeutic Group

H1 histamine receptor blocker

Pharmacological Action

Long-acting histamine H₁-receptor blocker. It has antiallergic, antipruritic, and anti-exudative effects. It prevents the development and alleviates the course of allergic reactions.

It suppresses the release of histamine and leukotriene C4 from mast cells. It reduces capillary permeability, prevents the development of tissue edema, and relieves smooth muscle spasms.

It does not affect the CNS (as it does not cross the BBB) and does not cause addiction.

The antiallergic effect develops within 30 minutes, reaches a maximum after 8-12 hours, and lasts for 24 hours.

Pharmacokinetics

Absorption and Distribution

It is rapidly and completely absorbed from the gastrointestinal tract. The time to reach C_max in blood plasma after taking the drug is 1.3-2.5 hours; food intake delays the time to reach C_max by 1 hour.

Plasma protein binding is 97%. The C_ss of loratadine and the metabolite in plasma are reached on the 5th day of administration. It does not cross the BBB.

Metabolism and Excretion

It is metabolized in the liver to form the active metabolite descarboethoxyloratadine with the participation of isoenzymes CYP3A4 and, to a lesser extent, CYP2D6.

It is excreted by the kidneys and with bile. The T_1/2 of loratadine is 3-20 hours (average 8.4 hours), and of the active metabolite is 8.8-92 hours (average 28 hours).

Pharmacokinetics in Special Patient Groups

The C_max of the drug in the blood plasma in elderly people increases by 50%. The T_1/2 of loratadine and the active metabolite in elderly patients is 6.7-37 hours (average 18.2 hours) and 11-38 hours (17.5 hours), respectively.

In alcoholic liver disease, C_max and T_1/2 increase in proportion to the severity of the disease.

In patients with chronic renal failure and during hemodialysis, the pharmacokinetics practically do not change.

Indications

• Seasonal and perennial rhinitis (including hay fever);
• Allergic conjunctivitis;
• Urticaria (including chronic idiopathic);
• Angioedema;
• Pseudoallergic reactions caused by histamine release;
• Pruritic dermatoses;
• Allergic reaction to insect bites.

ICD codes

Dosage Regimen

The drug is taken orally.

Adults and Children weighing more than 30 kg are prescribed 10 mg (1 tablet or 2 measuring spoons of syrup) once a day.

Children aged 2 to 12 years weighing less than 30 kg are prescribed 5 mg (1 measuring spoon of syrup) once a day.

In renal impairment, the initial dose is 10 mg every other day.

In hepatic impairment, the initial dose of the drug is 5 mg/day or 10 mg every other day.

Adverse Reactions

Adverse events occurred with approximately the same frequency as with placebo.

In adults headache, increased fatigue, dry mouth, drowsiness, nausea, gastritis, allergic reactions (rash), anaphylaxis, alopecia, impaired liver function, tachycardia.

In children headache, increased nervous excitability, sedative effect.

Contraindications

• Lactation period;
• Children weighing less than 30 kg (for tablets);
• Children under 2 years of age (for syrup);
• Lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome (for tablets);
• Hypersensitivity to any component of the drug.

With caution, the drug should be prescribed for hepatic impairment, pregnancy.

Use in Pregnancy and Lactation

The use of the drug during pregnancy is possible only in cases where the intended benefit to the mother outweighs the potential risk to the fetus.

Breastfeeding should be discontinued during treatment (excreted in breast milk).

Use in Hepatic Impairment

With caution, the drug should be prescribed for hepatic impairment.

Use in Renal Impairment

In renal impairment, the initial dose of the drug should be 10 mg every other day.

Pediatric Use

Contraindicated in children weighing less than 30 kg (tablets) and in children under 2 years of age (syrup).

Special Precautions

Effect on the ability to drive vehicles and operate machinery

During the treatment period, caution should be exercised when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Overdose

Symptoms drowsiness, tachycardia, headache.

Treatment gastric lavage, intake of activated charcoal. It is not removed by hemodialysis.

Drug Interactions

CYP3A4 inhibitors (including erythromycin, ketoconazole) and CYP3A4 and CYP2D6 inhibitors (cimetidine and others), when used concomitantly with loratadine, increase the plasma concentration of loratadine, without causing clinical manifestations and without affecting ECG data.

Microsomal oxidation inducers (phenytoin, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants) reduce the effectiveness of loratadine.

Loratadine does not enhance the effect of ethanol on the CNS.

Storage Conditions

The drug in tablet form should be stored in a dry place, out of the reach of children, at a temperature not exceeding 25°C (77°F); shelf life – 5 years.

The drug in syrup form should be stored in a dry place, out of the reach of children, at a temperature from 12°C (53.6°F) to 15°C (59°F); shelf life – 4 years.

Dispensing Status

The drug is approved for use as an over-the-counter product.

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.