Кларотадин®

General characteristics. Structure:

Active ingredient: 0,01 g of a loratadin in 1 tablet.

Excipients: sugar milk (lactose), cellulose microcrystallic, calcium stearate, sodium starch glycollate.

Pharmacological properties:

Pharmacodynamics. The H1-antihistaminic drug which is not possessing the central and anticholinergic action. Has antiallergic, antipruritic and anti-exudative effect. Effect of drug begins to develop in 30 min. after reception and continues during 24 h. Long administration of drug does not cause development of resistance to its action.

Loratadin and his metabolites do not get through a blood-brain barrier.

Pharmacokinetics. Absorption. At intake in the recommended therapeutic dose лоратадин it is quickly and completely soaked up from digestive tract. The defined concentration of a loratadin appear in a blood plasma in 15 min. after administration of drug. Time of achievement of the maximum concentration of a loratadin in plasma makes 1,3-2,5 h, and time of achievement of the maximum concentration of its active metabolite is equal to 2,5 h. The concomitant use of food and a loratadin slows down achievement of the maximum concentration of a loratadin and its active metabolite in plasma for 1 hour, but the maximum concentration of these substances in plasma remains without changes and no clinical manifestations of interaction of a loratadin with food are noted. At elderly people time of achievement of the maximum concentration increases up to 1,5 h, and at alcoholic damage of a liver increases with increase in disease severity. The maintenance of a loratadin and its active metabolite in a blood plasma reaches stationary level at most of patients for the fifth days of reception.

Communication with proteins of plasma — 97%.

Metabolism. Loratadin is metabolized in a liver with formation of an active metabolite of a dezkar-boetoksiloratadin mainly under the influence of P450 CYP3A4 cytochrome and to a lesser extent under the influence of P450 CYP2D6 cytochrome. In the presence of a ketokonazol which is CYP3A4 inhibitor лоратадин turns in дезкарбоэтоксилоратадин mainly under the influence of CYP2D6.

Removal. Loratadin is brought by kidneys and with bile. An average elimination half-life the lorata-dyne makes 8,4 h (range from 3 to 20 h), and for an active metabolite — 28 h (range from 8,8 to 92 h). At elderly patients the elimination half-life of a loratadin increases up to 18,2 h (range from 6,7 to 37 h), and a dezkarboetoksiloratadin to 17,5 h (range from 11 to 38 h). At alcoholic damage of a liver the elimination half-life increases with increase in disease severity. At patients with a chronic renal failure and when carrying out a hemodialysis the pharmacokinetics practically does not change.

Indications to use:

• seasonal and year-round rhinitis (including pollinosis);
• allergic conjunctivitis;
• small tortoiseshell (including chronic idiopathic);
• Quincke's edema;
• the pseudo-allergic reactions caused by release of a histamine;
• pruritic dermatosis;
• allergic reaction to stings of insects.

Route of administration and doses:

To adults and children 12 years are more senior: appoint inside 10 mg (1 tablet) of 1 times a day. A daily dose — 10 mg.

To children from 2nd to 12 years with body weight less than 30 kg are appointed on 5 mg (1/2 tablets) of 1 times a day. A daily dose — 5 mg.

To children with body weight more than 30 kg — on 10 mg (1 tablet) of 1 times a day. A daily dose — 10 mg.

Features of use:

For the patients suffering from an abnormal liver function or a renal failure (the glomerular filtration rate is lower than 30 ml/min.), the initial dose of a klarotadin has to make 10 mg (1 tablet) every other day. It is not recommended to children up to 2 years.

During treatment it is necessary to abstain from occupations potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

• from a nervous system: uneasiness, excitement (at children), an adynamy, drowsiness, a hyperkinesia, paresthesias, a tremor, amnesia, a depression;
• from integuments and podkozhnozhirovy cellulose: dermatitis;
• from an urinogenital and urinary system: urine discoloration, painful desires on an urination, a dysmenorrhea, a menorrhagia, a vaginitis;
• from a metabolism: increase in body weight, perspiration, thirst;
• from a musculoskeletal system: spasms of gastrocnemius muscles, arthralgia, mialgiya;
• from the alimentary system: taste change, anorexia, lock or diarrhea, dyspepsia, gastritis, meteorism, increase in appetite, stomatitis;
• from respiratory system: cough, bronchospasm, xeromycteria, sinusitis;
• from sense bodys: vision disorder, conjunctivitis, eye and ears pain;
• from cardiovascular system: decrease or increase in arterial pressure, heartbeat;
• allergic reactions: Quincke's disease, small tortoiseshell, itch, photosensitization;
• others: dorsodynia, stethalgia, fever, fever, mammary gland pain, nictitating spasm, dysphonia.

Interaction with other medicines:

When using a loratadin in therapeutic doses of exponential action on alcohol it is not revealed.

Combined use of a loratadin with erythromycin, Cimetidinum and ketokonazoly increases concentration of a loratadin in a blood plasma that has no clinical implication and does not exert impact on data of an electrocardiography.

Inductors of a microsomal oxidation (Phenytoinum, ethanol, barbiturates, зиксорин, rifampicin, phenylbutazone, tricyclic antidepressants) reduce efficiency of drug.

Contraindications:

• hypersensitivity to any of drug components;
• pregnancy, lactation period;
• with care — a liver failure.

Overdose:

At reception of a loratadin in the doses considerably exceeding the recommended therapeutic dose of 10 mg (40-180 mg of a loratadin) at adult patients such symptoms as a headache, drowsiness, tachycardia can be shown. At use of a loratadin by children with body weight less than 30 kg in a dose over 10 mg can be observed extrapyramidal symptoms and increase of heartbeat.

In case of overdose it is necessary to see a doctor and to take measures to removal of drug from digestive tract and to decrease in absorption (induction of vomiting, a gastric lavage, reception of absorbent carbon). If necessary symptomatic therapy is carried out. Loratadin is not brought from an organism at a hemodialysis. Data on removal of a loratadin at peritoneal dialysis are not available.

Storage conditions:

In the dry place, at a temperature not above 25 °C. To store in the place, unavailable to children. A period of validity - 4 years.

Issue conditions:

Without recipe

Packaging:

The tablets containing 10 mg of a loratadin (0,01 g). On 7 or 10 tablets in a blister strip packaging. On 1, 2 or 3 blister strip packagings together with the application instruction place in a pack from a cardboard.