Tsetirizin Geksal

General characteristics. Structure:

Active veshchestvo:10 mg of a tsetirizin of dihydrochloride.

Excipients: lactoses monohydrate, cellulose microcrystallic, silicon dioxide colloid, magnesium stearate. Structure of a cover: white dye опадрай, consisting of lactose of monohydrate, titanium of dioxide, a gipromelloza, a macrogoal 4000.

Pharmacological properties:

Pharmacodynamics. Drug possesses the expressed antiallergic action. Practically does not possess sedation in pharmacological active doses, treats the selection antagonists of H1-histamine receptors and has practically no anticholinergic and antiserotoninovy effect, prevents development and facilitates the course of allergic reactions. Has antipruritic and antiexudative effect. Influences an early stage of allergic reactions, and also reduces migration of cells of an inflammation; allocation of the mediators participating in late allergic reaction oppresses. 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). Tsetirizin considerably lowers hyperreactivity of the bronchial tree arising in response to release of a histamine at patients with bronchial asthma. The therapeutic effect of drug is shown on average in 60 minutes after reception. Against the background of course reception tolerance does not develop.

Pharmacokinetics. Absorption: after intake цетиризин it is quickly and well soaked up from digestive tract. The maximum level of concentration is defined approximately in 40 – 60 minutes.
Meal has no significant effect on absorption size, however in this case absorption speed slightly decreases.
Distribution: цетиризин contacts proteins of a blood plasma approximately for 93%. The size of volume of distribution (Vd) low (0,5 l/kg), drug in a cell does not get.
Drug does not get through a blood-brain barrier.
Metabolism: цетиризин it is poorly metabolized in a liver with formation of an inactive metabolite.
At 10-day use in a dose of 10 mg of accumulation of drug it is not observed.
Removal: approximately for 70% occurs kidneys generally in not changed look.
The size of system clearance makes about 54 ml/min.
After a single dose of a single dose the size of an elimination half-life makes about 10 hours. At children aged from 2 up to 12 years the size of an elimination half-life decreases till 5-6 o'clock.
At a renal failure (the clearance of creatinine is lower than 11-31 ml/min.) and at the patients who are on a hemodialysis (clearance of creatinine less than 7 ml/min.) the size of an elimination half-life increases by 3 times, the clearance decreases by 70%.
Against the background of chronic diseases and at elderly patients increase in size of an elimination half-life by 50% and reduction of clearance by 40% is noted.
The hemodialysis is inefficient.

Indications to use:

Year-round and seasonal allergic rhinitis (symptomatic therapy); small tortoiseshell, including chronic idiopathic; the dermatosis proceeding with an itch (atopic dermatitis, neurodermatitis); allergic conjunctivitis.

Route of administration and doses:

Inside, irrespective of meal, without chewing and washing down with enough liquid, preferably in the evening.
To children aged from 6 up to 12 years:

at body weight less than 30 kg: on ½ tablets, coated, in the evening
at body weight more than 30 kg: on 1 tablet, coated, in the evening.

Reception 2 times a day (in the morning and in the evening) on ½ tablets is possible.
To adults and teenagers 12 years are aged more senior it is recommended to accept on 1 tablet of a tsetirizin, preferably in the evening.
At a renal failure it is necessary to reduce the recommended dose twice.
At an abnormal liver function it is necessary to select a dose individually, it is especially careful at a simultaneous renal failure.
With normal function of kidneys of correction of a dose it is not required to elderly patients.
At seasonal allergic rhinitis duration of therapy makes usually from 3 to 6 weeks, and at short-term influence of pollen happens enough and one week.
Therapy duration for children is aged more senior than 6 years makes from 2 to 4 weeks, and at short-term influence of allergen reception within 1 week is sufficient.

Features of use:

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.
The simultaneous use of the medicines oppressing the central nervous system, alcohol is not recommended.

The instruction for patients with a diabetes mellitus:
1 tablet corresponds less than 0,01 bread. piece.

Side effects:

- From the alimentary system: dryness in a mouth, dyspepsia.
- From TsNS: headache, drowsiness, fatigue, dizziness, excitement, migraine.
- Allergic reactions: skin rash, Quincke's disease, small tortoiseshell, skin itch.
Drug is usually well transferred. By-effects arise seldom and have passing character.

Interaction with other medicines:

It is not established clinically significant interactions of a tsetirizin with other medicines.
Joint use with theophylline (400 mg/days) leads to decrease in the general clearance of a tsetirizin (the kinetics of theophylline does not change).

Contraindications:

- Hypersensitivity in relation to a tsetirizin or other components of drug; - the Serious illness of kidneys.
- Children's age up to 6 years.
- Pregnancy, lactation period.

With care:
Chronic pyelonephritis of average and heavy severity (correction of the mode of dosing is required), advanced age (decrease in glomerular filtering is possible).

Overdose:

Symptoms: drowsiness, block, weakness, a headache, tachycardia, an acrimony, an urination delay, fatigue (are possible most often at reception in day of 50 mg of a tsetirizin).
Treatment: carry out symptomatic therapy. The specific antidote is not revealed. The hemodialysis is inefficient. Carry out a gastric lavage, appoint absorbent carbon.

Storage conditions:

At a temperature not above 25 °C.
To store in the place, unavailable to children.

Issue conditions:

Without recipe

Packaging:

Tablets coated 10 mg, on 7 or on 10 tablets in a blister strip packaging from PVC / aluminum foil. On 1, 2, 3 or 5 blisters in a cardboard pack together with the application instruction.