Tsetirizin-OBL

General characteristics. Structure:

Active ingredient: 10 mg of a tsetirizin of dihydrochloride in 1 tablet.

Excipients: cellulose microcrystallic, povidone, lactoses monohydrate, hydrophosphate calcium a dihydrate, sodium carboxymethylstarch (sodium of starch glikolit), magnesium stearate.

Excipients for a cover: gipromelloz (gidroksipropilmetiltsellyuloz), macrogoal 6000 (polyethyleneglycol 6000), titanium dioxide.

Pharmacological properties:

Pharmacodynamics. Tsetirizin 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. After intake цетиризин it is quickly and well soaked up from the zheludochno-a intestinal path (ZIP). 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.

Tsetirizin 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 (GEB).

Tsetirizin 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.

Approximately for 70% removal is made by 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 elimination half-life (Т½) makes about 10 hours. At children aged from 2 up to 12 years Т½ decreases till 5-6 o'clock.

At a renal failure (the clearance of creatinine (CC) is lower than 11-31 ml/min.) and at the patients who are on a hemodialysis (KK less than 7 ml/min.) Т½ increases by 3 times, the clearance decreases by 70%.

Against the background of chronic diseases and at elderly patients increase Т½ 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.

To adults and teenagers 12 years - on 1 tablet daily, preferably are aged more senior in the evening.

To children aged from 6-12 years - on ½ tablets twice a day in the morning and in the evening.

To children at the age of 2-6 years - on ½ tablets 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.

Correction of a dose is not required to elderly patients with normal function of kidneys.

Duration of reception is defined individually, usually at seasonal allergic rhinitis duration of therapy makes from 3 to 6 weeks, and at short-term influence of pollen happens enough and one week.

Features of use:

1) To children.  Use is contraindicated to children up to 6 years.

2) The adult with chronic diseases. Correction of the mode of dosing is required, to patients of advanced age (decrease in glomerular filtering is possible.

Data on possible influence of medicine for a medical use on ability to manage vehicles, mechanisms

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. At exceeding of a dose of 10 mg/days ability to speed of reactions can worsen. The simultaneous use of the means oppressing the central nervous system and alcohol intake is not recommended.

Side effects:

From a nervous system and sense bodys: drowsiness, fatigue, excitement, headache, dizziness, concern, nervousness, emotional lability, disturbance of concentration of attention and thinking, sleeplessness, depression, euphoria, confusion of consciousness, amnesia, depersonalization, ataxy, lack of coordination of movements, tremor, hyperkinesia, spasms of gastrocnemius muscles, paresthesia, dysphonia, myelitis, paralysis, ptosis, disturbance of accommodation and sight, eye pain, glaucoma, xerophthalmia, conjunctivitis, hematopsia, ototoxicity, sonitus, deafness, disturbance of feeling of a smell.

From bodies of a GIT: dryness in a mouth, change or lack of flavoring perception, increase in appetite, anorexia, stomatitis (including ulcer), discoloration and puffiness of language, increase in a sialosis, the increased cariosity, thirst, vomiting, dyspepsia, gastritis, an abdominal pain, a meteorism, diarrhea, a lock, hemorrhoids, a melena, rectal bleeding, an abnormal liver function.

From cardiovascular system: migraine, heartbeat, hypertensia, heart failure.

From respiratory system: rhinitis, nasal bleeding, nasal polyp, pharyngitis, cough, sinusitis, bronchitis, increase in bronchial secretion, bronchospasm, диспноэ, upper respiratory tract infection, pneumonia, hyperventilation.

From urinogenital system: urination delay, hypostases, polyuria, dysuria, hamaturia, infection of urinary tract, cystitis, easing libido, dysmenorrhea, intermenstrual bleeding, menorrhagia, vaginitis.

From a musculoskeletal system: arthralgia, arthritis, arthrosis, mialgiya, dorsodynia, muscular weakness.

From integuments: xeroderma, rash, bubble rashes, itch, acne, furunculosis, dermatitis, eczema, hyperkeratosis, erythema, increase in sweating, alopecia, Quincke's disease, hypertrichosis, photosensitization, seborrhea.

Others: indisposition, fever, fever, inflows, dehydration, diabetes mellitus, lymphadenopathy, mammary gland pain, increase in body weight, skin allergic reactions, including small tortoiseshell.

Interaction with other medicines:

It is not established clinically significant interactions of a tsetirizin with other medicines (M). Theophylline (400 mg/days) slightly reduces Tsetirizin's clearance (by 16%) (the kinetics of theophylline does not change).

Myelotoxic HP strengthen manifestations of a gematotoksichnost of drug.

Let's combine with azithromycin, pseudo-Epinephrinum, ketokonazoly, erythromycin, diazepam and Cimetidinum.

Contraindications:

The increased individual sensitivity to one of drug components, a renal failure (KK <10 ml/min.), children's age up to 6 years, pregnancy, the lactation period, deficit of lactase, a lactose intolerance, glyukozo-galaktozny malabsorption.

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:

In the dry place protected from light at a temperature not above 25 °C. To store in the place, unavailable to children. A period of validity - 2 years. Not to use after the period of validity specified on packaging.

Issue conditions:

Without recipe

Packaging:

Tablets, film coated, 10 mg. On 10, 14, 15, 20 or 30 tablets in a blister strip packaging from a film of the polyvinyl chloride and printing aluminum foil varnished. On 1, 2, 3, 4, 5, 6 blister strip packagings with the application instruction in a pack from a cardboard.