Parlazin

General characteristics. Structure:

Active ingredient: tsetirizina dihydrochloride of 10 mg

Excipients: silicon dioxide colloid anhydrous, magnesium stearate, lactoses monohydrate, cellulose microcrystallic. Structure of a cover: the gipromelloza, titanium dioxide, a macrogoal 400, ariavit Sanset yellow.

Pharmacological properties:

Selective blocker histamine H1 receptors from group of derivatives of piperazin. Is the main carboxylated Hydroxyzinum metabolite. In comparison with Hydroxyzinum it less липофилен, gets into TsNS worse and to a lesser extent causes sedation. In comparison with other antihistamines цетиризин has more polar (less lipophilic) groups attached to a side chain of ethylamine that reduces its receipt in TsNS, increases selectivity in relation to histamine H1 receptors, and also reduces the side effects connected with holinoblokiruyushchy activity. Drug oppresses migration of eosinophils and inhibits factors of a chemotaxis of eosinophils. Substantially reduces accumulation of eosinophils in skin, and also the skin allowing reaction to a histamine estimated by the sizes of a blister and hyperemia. Besides, drug oppresses also other cells of inflammatory infiltrate (including neutrophils). Парлазин® prevents development and facilitates the course of allergic reactions, possesses antipruritic and antiexudative action. Reduces permeability of capillaries, edematization of fabrics warns, removes a spasm of smooth muscles. Effect of drug begins in 20 min. after reception, the maximum effect develops in 1 h, action duration - 24 h.

Pharmacokinetics. Absorption After intake drug is soaked up quickly and completely. The concomitant use of food exerts insignificant impact. Distribution Linkng with proteins of plasma makes 93%. The seeming Vd of a tsetirizin - 0.5-0.8 l/kg that it is significantly less, than at other selective blockers histamine H1 receptors. Gets through GEB in insignificant quantities and practically H1 receptors do not interact with central histamine. It is allocated with breast milk. Metabolism is not exposed to intensive metabolism in a liver. One inactive metabolite which is formed at oxidizing O-dealkylation of a side chain is found (it is revealed in a blood plasma, Calais). Removal of T1/2 makes 7.4-9 h. At use of drug in a dose of 10 mg about 60% of a tsetirizin are removed with urine in not changed look during 24 h, 10% are removed in the next 4 days; 10% - are removed with a stake within 5 days. The O-alkylated metabolite is removed with a stake, also removal with bile is supposed. The pharmacokinetics in special clinical cases At children final T1/2 makes 6.2 h (33% less, than at adults). Children under 4 years have T1/2 - 4.9 h. At elderly people and at patients with chronic diseases of a liver of T1/2 increases by 50%. T1/2 can increase also at a renal failure. At a renal failure easy or moderate severity of T1/2 makes 19-21 h. The renal clearance at normal function of kidneys makes 40 ml/min., at a renal failure of easy degree - 7 ml/min., at a renal failure of moderate severity - 1.5 ml/min. Though clinical value of these factors is not established, at such patients it is necessary to carry out drug dose adjustment. At a hemodialysis the pharmacokinetics of a tsetirizin does not change.

Indications to use:

— seasonal and year-round allergic rhinitis and conjunctivitis;

— pollinosis (hay fever);

— pruritic allergic dermatosis;

— small tortoiseshell (including chronic idiopathic);

— Quincke's edema.

Route of administration and doses:

To adults and teenagers 12 years are more senior appoint 10 mg (1 таб. or 20 drops) 1 times/days, are preferable for the night.

To children at the age of 6-12 years appoint 5 mg (1/2 таб. or 10 drops) 2 times/days (in the morning and in the evening) or on 10 mg (1 таб. or 20 drops) 1 times/days (evening). To children at the age of 2-6 years appoint 5 mg (10 drops) of 1 times/days. It is also possible to divide this dose into 2 receptions on 2.5 mg (on 5 drops in the morning and in the evening). To children at the age of 1-2 years appoint 2.5 mg (5 drops) of 2 times/days.

Patients of advanced age and patients with a renal failure are recommended to reduce a daily dose to 5 mg. A pill is taken inside, washing down with a large amount of water (200 ml). Drops before reception dissolve in water.

Features of use:

At development of hypersensitivity reactions treatment by the drug Parlazin® should be stopped. At patients with a renal failure in connection with delay of removal of drug cumulation of a tsetirizin is possible. At Parlazin's appointment of this category of patients in the recommended doses for adults the side effects connected with holinoblokiruyushchy action and influence on TsNS can be noted. Therefore at use of drug for patients with renal failures the dose decline is recommended. At patients of advanced age the risk of development of holinoblokiruyushchy effects of drug increases (dryness in a mouth, an ischuria). When strengthening such symptoms treatment by Parlazin should be stopped. The holinoblokiruyushchy or oppressing influence on TsNS expressed at Parlazin's appointment in standard doses, as a rule, does not arise. Nevertheless, the risk of accumulation of a tsetirizin increases (in connection with the progressing reduction of function of kidneys at elderly patients). It is necessary to consider that Parlazin® in the form of tablets contains lactose. Therefore patients with a lactose intolerance have to be informed on it. Treatment by Parlazin should be stopped in 3 days prior to carrying out the prik-test for the purpose of the prevention of distortion of reaction. It is necessary to abstain from the use of alcoholic beverages during treatment by Parlazin. To Children aged till 1 year Parlazin® do not appoint use in pediatrics in any dosage form since in this age group safety and efficiency of drug is not established. For treatment of children aged from 1 year up to 6 years it is necessary to apply Parlazin® in the form of drops to intake. Парлазин® in the form of tablets it is possible to apply at children at the age of 6 years and is more senior. Influence on ability to driving of motor transport and to control of mechanisms At the first reception of Parlazin it is necessary to pay attention to a possibility of development of side effects (drowsiness). Patients are recommended to abstain from driving of the car or control of mechanical devices before disappearance of side effects. Further in need of driving of motor transport or during the work requiring special attention, patients should not exceed a daily dose of 10 mg.

Side effects:

From TsNS: seldom – drowsiness (depending on a dose), feeling of fatigue, a headache, migraine, dizziness, concern (increase in a physical activity).

From the alimentary system: dryness in a mouth, nausea. Intensity of above-mentioned symptoms can be reduced, having divided a day dose into 2 receptions.

Allergic reactions: seldom (≤2%) - a Quincke's edema, rash.

Interaction with other medicines:

It is not established clinically significant interaction of a tsetirizin with glipizidy, diazepam, Cimetidinum, azithromycin, pseudoephedrine, ketokonazoly, erythromycin. At simultaneous use of a tsetirizin with theophylline (400 mg/days) decrease in the general clearance of a tsetirizin by 16% is noted. The theophylline pharmacokinetics at the same time does not change.

Contraindications:

— pregnancy;

— period of a lactation (breastfeeding);

— children's age till 1 year;

— children's age up to 6 years (for tablets);

— hypersensitivity to a tsetirizin or other components of drug.

Overdose:

Symptoms: often - feeling of fatigue, drowsiness. At children the concern and irritability which drowsiness follows is noted. At reception of a single dose of 50 mg the urination delay, a lock can be noted.

Treatment: it is necessary to cause vomiting, to wash out a stomach. If necessary carry out the supporting and symptomatic treatment. There is no specific antidote. The hemodialysis is not effective.

 

Storage conditions:

Drug in the form of tablets should be stored in the place, unavailable to children, at a temperature not above 25 °C. A period of validity – 2 years. Drug in the form of drops should be stored in protected from light, the place, unavailable to children, at a temperature not above 25 °C. A period of validity - 4 years. It is necessary to store an open bottle no more than 4 weeks.

Issue conditions:

According to the recipe

Packaging:

Tablets, film coated light orange color, biconvex, oblong, with a facet, with risky on one party and an engraving "Е 511" on other party, inodorous; on a break: outside ring of a cover of light orange color, kernel of a tablet of white or almost white color.