Loratadine-Hemofarm (Tablets) Instructions for Use

Marketing Authorization Holder

Hemofarm Koncern A.D. (Serbia and Montenegro)

ATC Code

R06AX13 (Loratadine)

Active Substance

Loratadine (Rec.INN registered by WHO)

Dosage Forms

	Loratadine-Hemofarm	Tablets 10 mg: 10 pcs.
		Effervescent tablets 10 mg: 10 or 20 pcs.
		Syrup 5 mg/5 ml: 120 ml.

Dosage Form, Packaging, and Composition

Syrup transparent, from colorless to pale yellow, with a fruity odor.

Excipients: glycerol, propylene glycol, sucrose, sodium benzoate, citric acid monohydrate, cherry flavor “Cherry Flavour”, disodium edetate, purified water.

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

Tablets round, biconvex, from white to almost white, with a score on one side.

Excipients: lactose monohydrate, corn starch, colloidal anhydrous silicon dioxide, povidone, polysorbate 80, microcrystalline cellulose, crospovidone, talc, magnesium stearate.

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

Effervescent tablets round, from white to almost white.

Excipients: sodium bicarbonate, anhydrous sodium carbonate, anhydrous citric acid, povidone, polysorbate 80, colloidal anhydrous silicon dioxide, lactose monohydrate, macrogol 6000.

10 pcs. – plastic tubes (1) – cardboard packs.
10 pcs. – plastic tubes (2) – cardboard packs.

Clinical-Pharmacological Group

Histamine H₁-receptor blocker. Antiallergic drug

Pharmacotherapeutic Group

H1 histamine receptor blocker

Pharmacological Action

Histamine H₁-receptor blocker (long-acting). 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 antiexudative effects. Reduces capillary permeability, prevents the development of tissue edema, and relieves smooth muscle spasms.

The antiallergic effect develops within 30 minutes, reaches a maximum in 8-12 hours, and lasts 24 hours. The active metabolite desloratadine significantly contributes to the duration of action. Does not affect the CNS and does not cause addiction (because it does not penetrate the BBB).

Pharmacokinetics

Rapidly and completely absorbed from the gastrointestinal tract. C_max in blood plasma is reached in 1.3-2.5 hours; food intake delays it by 1 hour. C_max in elderly people increases by 50%; in alcoholic liver disease – with increasing severity of the disease. Plasma protein binding – 97%.

Metabolized in the liver to form the active metabolite descarbethoxyloratadine with the participation of the isoenzyme CYP3A4 and, to a lesser extent, CYP2D6.

The equilibrium concentration of loratadine and the metabolite in plasma is reached on the 5th day of administration. Does not penetrate the BBB.

T_1/2 of loratadine – 3-20 hours (average 8.4), of the active metabolite – 8.8-92 hours (average 28 hours); in elderly patients, respectively – 6.7-37 hours (average 18 hours) and 11-38 hours (17.5 hours). In alcoholic liver disease, T_1/2 increases with increasing severity of the disease.

Excreted by the kidneys and with bile.

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

Indications

• Allergic rhinitis (seasonal and perennial);
• Conjunctivitis;
• Pollinosis;
• Urticaria (including chronic idiopathic);
• Angioedema;
• Pruritic dermatoses;
• Pseudoallergic reactions;
• Allergic reactions to insect bites.

ICD codes

Dosage Regimen

Orally. The effervescent tablet is first dissolved in a glass of water (200 ml). Tablets should not be swallowed, chewed, or sucked in the mouth.

For young children and adults with swallowing difficulties, the use of syrup is recommended.

Children from 2 to 6 years (with body weight less than 30 kg): 5 mg (1 measuring spoon (5 ml) of syrup) once/day.

Children over 6 years (with body weight more than 30 kg) and adults: 10 mg (2 measuring spoons (10 ml) of syrup, or 1 tab., or 1 effervescent tab.) once/day.

In patients with hepatic and/or renal impairment (creatinine clearance < 30 ml/min), the drug is used every other day.

In elderly patients, there is no need to reduce the dose.

Adverse Reactions

From the digestive system dry mouth, taste change, anorexia, constipation or diarrhea, dyspepsia, gastritis, flatulence, increased appetite, stomatitis, nausea, vomiting, transient liver dysfunction.

From the nervous system: anxiety, agitation (in children), asthenia, drowsiness, blepharospasm, dysphonia, hyperkinesia, paresthesia, tremor, amnesia, depression, increased fatigue.

From the skin dermatitis, alopecia.

From the genitourinary system change in urine color, painful urge to urinate, dysmenorrhea, menorrhagia, vaginitis.

From metabolism: weight gain, sweating, thirst.

From the musculoskeletal system: calf muscle cramps, arthralgia, myalgia

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

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

From the cardiovascular system: decrease or increase in BP, palpitations.

Allergic reactions: angioedema, anaphylaxis, urticaria, itching, rash.

Other: photosensitivity, back pain, chest pain, fever, chills, breast pain, headache (in children).

Contraindications

• Pregnancy;
• Lactation period;
• Children under 2 years of age;
• Hypersensitivity.

With caution – hepatic and/or renal impairment (creatinine clearance < 30 ml/min).

Use in Pregnancy and Lactation

Contraindicated.

Use in Hepatic Impairment

With caution – hepatic impairment.

Use in Renal Impairment

With caution – renal impairment (creatinine clearance < 30 ml/min).

Pediatric Use

For young children and adults with swallowing difficulties, the use of syrup is recommended.

Children from 2 to 6 years (with body weight less than 30 kg): 5 mg (1 measuring spoon (5 ml) of syrup) once/day.

Children over 6 years (with body weight more than 30 kg) and adults: 10 mg (2 measuring spoons (10 ml) of syrup, or 1 tab., or 1 effervescent tab.) once/day.

Contraindicated in children under 2 years.

Geriatric Use

In elderly patients, there is no need to reduce the dose.

Special Precautions

During the treatment period, it is necessary to refrain from engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Overdose

Symptoms: drowsiness, tachycardia, headache.

Treatment: induction of vomiting, gastric lavage, intake of activated charcoal.

Drug Interactions

Erythromycin, cimetidine, ketoconazole increase the concentration of loratadine in blood plasma, without causing clinical manifestations and without affecting the ECG.

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

Shelf Life

Shelf life – 2 years.

Tablets and effervescent tablets should be stored at a temperature from 15°C (59°F) to 25°C (77°F), in a place protected from light and moisture, syrup – at a temperature from 15°C (59°F) to 25°C (77°F).

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.