Tsetirizin

General characteristics. Structure:

Active agent: a tsetirizina dihydrochloride - 10,0 mg.

Excipients (kernel): cellulose microcrystallic - 119,0 mg, mg lactose-60,0, croscarmellose sodium - 7,0 mg, magnesium stearate - 3,0 mg, silicon dioxide colloid-1,0 mg.

Excipients (cover): опадрай II 85F48105 White - 6,0 mg, polyvinyl alcohol - 2,814 mg, a macrogoal of 3350 - 1,416 mg, talc-1,044 of mg, titanium dioxide - 0,726 mg.

Pharmacological properties:

Pharmacodynamics. Tsetirizin treats group of competitive antagonists of a histamine, blocks H1-histamine receptors, has practically no anticholinergic and antiserotoninovy effect. Possesses the expressed antiallergic action, prevents development and facilitates the course of allergic reactions. Has antipruritic and antiexudative effect. Influences a "early" stage of allergic reactions, and also reduces migration of cells of an inflammation; allocation of the mediators participating in a "late" stage of 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). In therapeutic doses practically does not render sedation. Against the background of course reception tolerance does not develop. Effect of drug after reception of a tsetirizin in a single dose of 10 mg begins in 20 minutes (at 50% of patients), in 1 hour (at 95% of patients), and remains within 24 hours. After drug withdrawal the effect remains up to 3 days.

Pharmacokinetics. Absorption: after intake drug is quickly and well soaked up from digestive tract. The maximum concentration (Cmax) of a tsetirizin is defined approximately in 30 - 90 minutes.
Meal has no significant effect on absorption size, but extends time of achievement of the maximum concentration (Tsgpakh) for 1 hour and Stakh reduces size by 23%.
Distribution: цетиризин contacts proteins of a blood plasma approximately for 93%. Size of volume of distribution (Vd) low (0,5 l/kg).
Metabolism: цетиризин in small amounts it is metabolized by O-dealkylation 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. In addition to kidneys it is removed through intestines. The size of system clearance makes about 54 ml/min. The size of an elimination half-life makes about 10 hours. At children aged from 6 up to 12 years the size of an elimination half-life decreases till 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 general clearance decreases by 70%.
Against the background of chronic diseases of a liver and at elderly patients at administration of drug in a dose of 10 mg increase in size of an elimination half-life by 50% and reduction of system clearance by 40% is noted.

Indications to use:

• Treatment of symptoms of year-round and seasonal allergic rhinitis and allergic conjunctivitis, such as itch, sneezing, rhinorrhea, dacryagogue, conjunctiva hyperemia;
• Hay fever (pollinosis);
• Small tortoiseshell, including chronic idiopathic small tortoiseshell;
• Other allergic dermatosis, including atopic dermatitis which are followed by an itch and rashes.

Route of administration and doses:

Features of use:

Patients with injury of a spinal cord, a hyperplasia have prostates, and also in the presence of other contributing factors to an ischuria, respect for care as цетиризин can increase risk of an ischuria is required.
At objective assessment of ability to driving of motor transport and control of mechanisms any undesirable phenomena are authentically not revealed at administration of drug in the studied dose. But, nevertheless, during use of drug it is reasonable to abstain from occupations potentially dangerous types of activity demanding the increased concentration and speed of psychomotor reactions.

Side effects:

• From circulatory and lymphatic system: thrombocytopenia.
• From the central and peripheral nervous system: drowsiness, dizziness, headache, aggression, excitement, confusion, depression, hallucinations, sleeplessness, tic, spasms, dyskinesia, dystonia, paresthesia, faint, tremor, memory disturbance, confusion of consciousness, suicide ideas, вертиго.
• From organs of sight: accommodation disturbance, indistinct sight, nystagmus.
• From cardiovascular system: tachycardia.
• From respiratory system: rhinitis, pharyngitis.
• From bodies of digestive tract: dryness in a mouth, a food faddism, nausea, abdominal pain, diarrhea, increase in appetite.
• From gepatobiliarny system: abnormal liver function (increase in activity of transaminases, alkaline phosphatase, gammaglutamattransferaza, concentration of bilirubin).
• From an urinary system: frustration of an urination, enuresis, ischuria.
• From skin and hypodermic cellulose: itch, rash, urticaria, resistant erythema, Quincke's disease.
• From immune system: hypersensitivity, up to development of an acute anaphylaxis.
• From a metabolism: increase in body weight.
• Other: fatigue, adynamy, indisposition, peripheral hypostases.

Interaction with other medicines:

When studying medicinal interaction of a tsetirizin with pseudoephedrine, Cimetidinum, ketokonazoly, erythromycin, azithromycin, diazepam and glipizidy clinically significant interactions are not revealed. Combined use with theophylline (400 mg/days) leads to decrease in the general clearance of a tsetirizin by 16% (the kinetics of theophylline does not change).
At simultaneous use with macroleads and ketokonazoly changes on the electrocardiogram are not noted. Tsetirizin, at simultaneous use with protease VICh-1 inhibitor ritonaviry, did not change pharmacokinetics of a ritonavir. When using drug in therapeutic doses, data on interaction with alcohol it is not obtained (at concentration of alcohol in blood - 0.5 g/l). However it is necessary to abstain from alcohol intake during therapy by drug in order to avoid oppression of the central nervous system.
Before conducting allergological tests the three-day "washout" period is recommended in view of the fact that H1-histamine receptors blockers inhibit development of skin allergic reactions.

Contraindications:

• Hypersensitivity to a tsetirizin, Hydroxyzinum or derivatives of piperazin, and also other components of drug;
• End-stage of a renal failure (clearance of creatinine less than 10 ml/min.);
• Lactose intolerance, deficit of lactase or glyukozo-galaktozny malabsorption;
• Pregnancy, lactation period;
• Children's age up to 6 years.

WITH CARE
• The chronic renal failure (clearance of creatinine more than 10 ml/min.) - is required correction of the mode of dosing;
• Chronic diseases of a liver;
• Epilepsy, patients with the increased convulsive readiness;
• Patients with the contributing factors to an ischuria;
• Advanced age (decrease in glomerular filtering is possible).

USE AT PREGNANCY And in the period of the LACTATION Use of drug during pregnancy is contraindicated. In need of use of drug in the period of a lactation it is necessary to resolve an issue of the breastfeeding termination.

Overdose:

At a single dose of drug in a dose of 50 mg the following symptoms can be observed: confusion, diarrhea, dizziness, increased fatigue, headache, indisposition, mydriasis, itch, weakness, sedation, drowsiness, stupor, tachycardia, tremor, ischuria.
Treatment: right after administration of drug - a gastric lavage or an artificial call of vomiting. Reception of absorbent carbon, carrying out a symptomatic and maintenance therapy is recommended. There is no specific antidote. The hemodialysis is inefficient.

Storage conditions:

To store in the dry, protected from light place at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

Without recipe

Packaging:

Tablets, film coated on 10 mg.
On 10 tablets in a blister strip packaging from a film of the polyvinyl chloride and printing aluminum foil varnished. On 10, 20, 30, 40, 50 or 100 tablets in bank polymeric for medicines. To one bank or 1, 2, 3, 4, 5 or 10 blister strip packagings together with the application instruction place in cardboard packaging (pack).