Tsetirizin

General characteristics. Structure:

Active ingredient: 0,01 g of a tsetirizin dihydrochloride.

Excipients: cellulose microcrystallic, lactoses monohydrate, кросповидон, magnesium stearate, silicon dioxide colloid (aerosil).

Cover: [a gipromelloza, talc, titanium dioxide, a macrogoal 4000 (polyethyleneglycol 4000)] or [a cover film dry white, containing a gipromelloza, talc, titanium dioxide, a macrogoal 4000].

Antihistaminic drug.

Pharmacological properties:

Pharmacodynamics. The competitive antagonist of a histamine, Hydroxyzinum metabolite, blocks H1-gistami-new receptors. Prevents development and facilitates the course of allergic reactions, possesses antipruritic and antiexudative action. Influences an early stage of allergic reactions, limits release of mediators of an inflammation at a "late" stage of allergic reaction, reduces migration of eosinophils, neutrophils and basophiles. Reduces permeability of capillaries, edematization of fabrics warns, removes a spasm of smooth muscles.

Eliminates skin reaction to introduction of a histamine, offending allergens, and also to cooling (at a cold urticaria).

Practically has no anticholinergic and antiserotoninovy effect.

In therapeutic doses practically does not cause sedation. The beginning of action after one-time reception of 10 mg of a tsetirizin - in 20 min. (at 50% of patients) and in 60 min. (at 95% of patients), proceeds more than 24 h. Against the background of course treatment tolerance to antihistaminic action of a tsetirizin does not develop. After the treatment termination action remains to 3 days.

Pharmacokinetics. Time of achievement of the maximum concentration after intake - is quickly soaked up 1 hour from a zheluchno-intestinal path. Food does not influence completeness of absorption (AUC), but extends time of achievement of the maximum concentration on 1 h and reduces the size of the maximum concentration by 23%. At reception in a dose of 10 mg once a day during 10 days equilibrium concentration in plasma makes 310 ng/ml and is noted in 0,5-1,5 h after reception. Communication with proteins of plasma — 93% also does not change at concentration of a tsetirizin in the range of 25-1000 ng/ml. Pharmacokinetic parameters of a tsetirizin change linearly at appointment it in a dose of 5-60 mg. Distribution volume — 0,5 l/kg.

In small amounts it is metabolized in a liver by O-dealkylation with formation pharmacological of an inactive metabolite (unlike other blockers of H1 - the histamine receptors which are metabolized in a liver with participation of system of P450 cytochrome). Does not kumulirut. 2/3 drugs are removed in not changed look by kidneys and about 10% - through intestines.

System clearance - 53 ml/min. An elimination half-life adults - 7-10 h, at children     have 6-12 years - 6 h, children have 2-6 years - 5 h, children from 6 months to 2 years have 3 h. At elderly patients the elimination half-life increases by 50%, the system clearance decreases by 40% (depression of function of kidneys).

At patients with a renal failure (the clearance of creatinine is lower than 40 ml/min.) the clearance of drug decreases, and the elimination half-life is extended (so, at the patients who are on a hemodialysis, the general clearance decreases by 70% and makes 0,3 ml/min., and the elimination half-life is extended by 3 times) that demands corresponding change of the mode of dosing.

At patients with chronic diseases of a liver (hepatocellular, cholestatic or biliary cirrhosis) lengthening of an elimination half-life for 50% and decrease in the general clearance by 40% is noted (correction of the mode of dosing is required only at the accompanying reduction in the rate of glomerular filtering).
Gets into breast milk.

Indications to use:

Seasonal and year-round allergic rhinitis and conjunctivitis (itch, sneezing, rhinorrhea, dacryagogue, conjunctiva hyperemia), small tortoiseshell (including chronic idiopathic small tortoiseshell), hay fever (pollinosis), itch, Quincke's disease (Quincke's edema), pruritic allergic dermatosis.

Route of administration and doses:

Inside, irrespective of meal, without chewing and washing down with enough liquid, preferably in the evening. To adults and children 6 years (with body weight more than 30 kg) — on 1 tablet are aged more senior once a day.

Features of use:

The simultaneous use with the alcohol and medicines oppressing the central nervous system is not recommended.

Influence on control of vehicles and mechanisms. During treatment it is necessary to refrain from occupations potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions. At exceeding of a dose of 10 mg/days ability to bystry reactions can worsen.

Use at pregnancy and in the period of a lactation. Use of drug during pregnancy is not recommended. As цетиризин gets into breast milk, it is not appointed during breastfeeding.

Side effects:

Drug is usually well transferred. By-effects arise seldom and have passing character.

From the alimentary system: dryness in a mouth, dyspepsia.

From a nervous system: dizziness, headache, drowsiness, fatigue, excitement, migraine.

Allergic reactions: Quincke's disease, skin rashes, itch, urticaria.

Interaction with other medicines:

Combined use with theophylline (400 mg/days) leads to decrease in the general clearance of a tsetirizin (the kinetics of theophylline does not change).

Myelotoxic medicines strengthen manifestations of a gematoksichnost of drug.

Clinically significant interactions with other medicines are not revealed (pseudoephedrine, Cimetidinum, ketokonazoly, erythromycin, azithromycin, diazepam, glipizidy).

Contraindications:

Hypersensitivity to a tsetirizin, other components of drug, Hydroxyzinum, reduced function of kidneys (clearance of creatinine of 30-49 ml/min.), a chronic renal failure, children's age up to 6 years, pregnancy, the lactation period.

With care. Advanced age (decrease in glomerular filtering is possible).

Overdose:

Symptoms (at reception of a single dose of 50 mg): dryness in a mouth, drowsiness, an urination delay, a lock, concern, an acrimony.

Treatment: gastric lavage, symptomatic therapy. The specific antidote is not revealed. The hemodialysis is inefficient.

Storage conditions:

In the dry, protected from light place at a temperature not over 25 ºС. To store in the place, unavailable to children. Period of validity 2 years. Not to use after a period of validity.

Issue conditions:

Without recipe

Packaging:

Tablets, film coated, 10 mg. On 10 tablets in a blister strip packaging from a film of polyvinyl chloride and aluminum foil. 1, 2 or 3 blister strip packagings together with the application instruction in a pack from a cardboard.