Цетрин®

General characteristics. Structure:

Active ingredient: tsetirizina dihydrochloride of 10 mg.
Excipients: lactose of 106,5 mg, starch of corn 65 mg, povidone (K-30) of 2 mg, magnesium stearate of 1,5 mg;
Film cover: gipromelloza of 3,3 mg, macrogoal of 6000 0,661 mg, titanium dioxide of 0,706 mg, talc of 1,183 mg, sorbic acid of 0,05 mg, mg polysorbate 80 0,05, диметикон 0,05 mg.

Description:
round biconvex tablets, film coated, white or almost white color with risky on one party.

Pharmacological properties:

Pharmacodynamics. The competitive antagonist of a histamine, Hydroxyzinum metabolite, blocks H1 - histamine 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). Reduces a gistaminoindutsirovanny bronkhokonstriktion at bronchial asthma of an easy current.
Practically has no anticholinergic and antiserotoninovy effect. In therapeutic doses practically does not cause sedation. The beginning of effect after one-time reception of 10 mg of a tsetirizin – 20 min., 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 (TCmax) after intake – about 1 h is quickly soaked up from digestive tract. Food does not influence completeness of absorption (AUC), but extends on 1 h TCmax and reduces the size of the maximum concentration (Cmax) by 23%. At reception in a dose of 10 mg once a day during 10 days equilibrium concentration of drug (Css) 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). Tsetirizin does not kumulirutsya. About 2/3 drugs are removed in not changed look by kidneys and about 10% – with a fecal masses.
System clearance – 53 ml/min. An elimination half-life (T1/2) adults – 10 h, at children have 6–12 years – 6 h, 2–6 years – 5 h, 0,5–2 years – 3,1 h. At elderly sick T1/2 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 T1/2 is extended (so, at the patients who are on a hemodialysis, the general clearance decreases by 70% and makes 0,3 ml/min., and T1/2 is extended by 3 times) that demands corresponding change of the mode of dosing. Practically is not removed during a hemodialysis. At patients with chronic diseases of a liver (hepatocellular, cholestatic or biliary cirrhosis) lengthening of T1/2 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; allergic conjunctivitis; pollinosis (hay fever); small tortoiseshell, including chronic idiopathic small tortoiseshell; pruritic allergic dermatosis (atopic dermatitis, neurodermatitis); Quincke's disease (Quincke's edema).

Route of administration and doses:

Inside, irrespective of meal, without chewing, tablets wash down 200 ml of water.
The adult – on 10 mg (1 таб.) once a day or on 5 mg (1/2 таб.) 2 times a day.
To children 6 years – on 5 mg are more senior (1/2 таб.) 2 times a day or on 10 mg (1 таб.) once a day.
At patients with reduced function of kidneys (clearance of creatinine of 30-49 ml/min.) appoint 5 mg/days (1/2 таб.), at a heavy chronic renal failure (clearance of creatinine of 10-30 ml/min.) – 5 mg/days (1/2 таб.) every other day.

Features of use:

At exceeding of a dose of 10 mg/days ability to bystry reactions can worsen. In the recommended doses does not strengthen effect of ethanol (at its concentration no more than 0,8 g/l), nevertheless it is recommended to abstain from its use during treatment. During treatment it is necessary to be careful during the driving of motor transport and occupation other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.
(From 2 years) Tsetrin® is applied to children's age in the form of syrup.

Side effects:

Usually Tsetrin® is transferred well. Are in some cases possible: drowsiness, dryness in a mouth; seldom – a headache, dizziness, migraine, discomfort in digestive tract (dyspepsia, an abdominal pain, a meteorism), allergic reactions (a Quincke's disease, rash, a small tortoiseshell, an itch).

Interaction with other medicines:

Pharmacokinetic interaction with pseudoephedrine, Cimetidinum, ketokonazoly, erythromycin, azithromycin, diazepam and glipizidy is not revealed. Joint appointment 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 gematotoksichnost of drug.

Contraindications:

Hypersensitivity (including to Hydroxyzinum); pregnancy, lactation period; children's age up to 6 years (for this dosage form).

With care
Chronic renal failure (average and heavy degree of manifestation – needs correction of the mode of dosing), advanced age (decrease in glomerular filtering is possible).

Overdose:

Symptoms (arise at reception of a single dose of 50 mg) – dryness in a mouth, drowsiness, an urination delay, locks, concern, an acrimony. Treatment: gastric lavage, purpose of symptomatic medicines. The specific antidote does not exist. The hemodialysis is inefficient.

Storage conditions:

In the dry place at a temperature not above 25 °C. To store in the place, unavailable to children! Period of validity 2 years. Not to use after the expiry date specified on packaging.

Issue conditions:

Without recipe

Packaging:

Tablets, film coated, 10 mg. On 10 tablets in PVC / the aluminum blister. On 2 or 3 blisters together with the application instruction are packed into a pack cardboard.