Clargotil^® (Tablets) Instructions for Use

Marketing Authorization Holder

Gedeon Richter-Rus, JSC (Russia)

Under License

GEDEON RICHTER, Ltd. (Hungary)

ATC Code

R06AX13 (Loratadine)

Active Substance

Loratadine (Rec.INN registered by WHO)

Dosage Form

Clargotil®

Tablets 10 mg: 10 pcs.

Dosage Form, Packaging, and Composition

Tablets are white, flat-cylindrical, with an engraving “L” above a score on one side.

Excipients: microcrystalline cellulose, lactose monohydrate, colloidal silicon dioxide (aerosil), magnesium stearate.

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

Clinical-Pharmacological Group

Histamine H₁-receptor blocker. Antiallergic drug

Pharmacotherapeutic Group

H1 histamine receptor blocker

Pharmacological Action

Histamine H₁-receptor blocker. It has antiallergic, antipruritic, and antiexudative effects.

It reduces capillary permeability, prevents the development of tissue edema, and reduces increased smooth muscle tone. It does not affect the CNS.

The antiallergic effect develops within 30 minutes, reaching a maximum in 8-12 hours, and the duration of action is 24 hours.

Pharmacokinetics

Absorption

After oral administration, the drug is rapidly absorbed from the gastrointestinal tract. Food intake slows down the time to reach maximum concentration. C_max of loratadine and its active metabolite is reached 1-2.5 hours after administration.

Distribution

Plasma protein binding is 97-99%. It does not penetrate the blood-brain barrier.

Metabolism

It is metabolized in the liver by the cytochrome P₄₅₀ system to form an active metabolite, descarboethoxyloratadine.

Excretion

The mean T_1/2 of loratadine is 8 hours, and that of descarboethoxyloratadine is about 28 hours. Loratadine is excreted in the urine and bile.

Pharmacokinetics in special clinical cases

In elderly patients, C_max increases by 50%; in alcoholic liver disease – with increasing severity of the disease.

T_1/2 increases in alcoholic liver disease.

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

Indications

• Treatment of seasonal and perennial allergic rhinitis and relief of symptoms associated with these conditions: sneezing, itching of the nasal mucosa, rhinorrhea, burning and itching sensation in the eyes;
• Urticaria (including chronic idiopathic urticaria);
• Skin diseases of allergic origin (including allergic pruritic dermatoses) in adults and children over 2 years of age;
• Pseudoallergic reactions;
• Allergic reactions to insect bites;
• Pruritus of various etiologies;
• Allergic conjunctivitis;
• Hay fever;
• Angioedema.

ICD codes

Dosage Regimen

Adults (including the elderly) and children over 12 years of age are prescribed 10 mg (1 tab.) once a day.

Children aged 2 to 12 years with a body weight less than 30 kg are prescribed 5 mg (1/2 tab.) once a day, with a body weight more than 30 kg – 10 mg (1 tab.) once a day.

For patients with impaired liver function, the initial dose is 5 mg/day.

The tablets should be taken orally at least 1 hour before meals, without chewing, with a small amount of liquid.

Adverse Reactions

From the CNS and peripheral nervous system rarely – increased fatigue, anxiety, excitability (in children), dizziness, headache, asthenia, drowsiness, blepharospasm, dysphonia, hyperkinesia, paresthesia, tremor, amnesia, depression.

From the digestive system rarely – dry mouth, nausea, vomiting, gastritis, taste change, anorexia, constipation or diarrhea, flatulence, increased appetite, stomatitis.

From the respiratory system rarely – cough, bronchospasm, dryness of the nasal mucosa, sinusitis.

From the senses conjunctivitis, visual disturbances, pain in the eyes and ears.

From the cardiovascular system decrease or increase in BP; rarely – palpitations.

From the urinary system change in urine color, painful urination.

From metabolism weight gain, sweating, thirst.

From the musculoskeletal system arthralgia, myalgia, calf muscle cramps, back pain.

Allergic reactions rarely – urticaria, itching, photosensitivity; in isolated cases – angioedema.

Other dermatitis, dysmenorrhea, menorrhagia, vaginitis, chest pain, breast pain, fever, chills.

Contraindications

• Hypersensitivity to the components of the drug;
• Pregnancy;
• Lactation (breastfeeding).

Use in Pregnancy and Lactation

The drug is contraindicated during pregnancy and lactation (breastfeeding).

Use in Hepatic Impairment

For patients with impaired liver function, the initial dose is 5 mg/day.

Use in Renal Impairment

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

Pediatric Use

Children aged 2 to 12 years with a body weight less than 30 kg are prescribed 5 mg (1/2 tab.) once a day, with a body weight more than 30 kg – 10 mg (1 tab.) once a day.

Special Precautions

The drug should be prescribed with caution in hepatic insufficiency.

Effect on ability to drive vehicles and mechanisms

During treatment, one should refrain from engaging in potentially hazardous activities that require increased attention and speed of psychomotor reactions.

When used in recommended doses, the drug does not affect psychophysical activity and the ability to drive vehicles.

Overdose

Symptoms when taking the drug in doses significantly exceeding the recommended ones, drowsiness, tachycardia, and headache may occur.

Treatment gastric lavage, induction of vomiting, administration of activated charcoal, laxatives. If necessary, symptomatic therapy is carried out. Loratadine is not removed from the body by hemodialysis; peritoneal dialysis is not effective.

Drug Interactions

With simultaneous use of Clargotil^® with erythromycin, cimetidine, ketoconazole, an increase in the plasma concentration of loratadine is possible (which has no clinical significance and does not affect the ECG).

Inducers of microsomal oxidation (phenytoin, ethanol, barbiturates, zixorin, rifampicin, phenylbutazone, tricyclic antidepressants) reduce the effectiveness of loratadine.

Loratadine does not enhance the effect of ethanol.

Storage Conditions

The drug should be stored in a dry, light-protected place at a temperature not exceeding 25°C (77°F).

Shelf Life

Shelf life – 3 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.