Dezloratadin Kanon

General characteristics. Structure:

Active agent: дезлоратадин 5 mg;
excipients: hydrophosphate calcium dihydrate of 61,7 mg; povidone of 6,8 mg; calcium stearate of 0,7 mg; croscarmellose sodium (primelloza) of 4,8 mg; cellulose of microcrystallic 41 mg;
structure of a film cover: Опадрай II white 4 mg, including: polyvinyl alcohol of 1,88 mg, macrogoal (polyethyleneglycol 3350) of 0,94 mg, talc of 0,7 mg, titanium dioxide of 0,48 mg.

Description:
Tablets are round, biconvex, film coated white or almost white color. On cross section almost white or white with a creamy shade or color, white with a pinkish shade.

Pharmacological properties:

Pharmacodynamics. Antihistaminic drug of long action. Is primary active metabolite of a loratadin. Inhibits the cascade of reactions of an allergic inflammation, including release of pro-inflammatory cytokines, including interleykina of IL-4, IL-6, IL-8, IL-13, release of pro-inflammatory chemokines (RANTES), products of superoxidic anions the activated polymorphonuclear neutrophils, adhesion and a chemotaxis of eosinophils, allocation of molecules of adhesion, such as P-selectin,
The IgE-mediated release of a histamine, D2 prostaglandin and C4 leukotriene. Thus, prevents development and facilitates the course of allergic reactions, possesses antipruritic and antiexudative action, reduces permeability of capillaries, edematization of fabrics, a spasm of smooth muscles warns.
Drug does not make impact on the central nervous system, practically does not possess sedation (does not cause drowsiness) and does not influence the speed of psychomotor reactions. Does not cause lengthening of an interval of QT on an ECG.
Action of a dezloratadin begins within 30 minutes after intake and 24 hours proceed.

Pharmacokinetics. Dezloratadin is well soaked up in digestive tract. Is defined in a blood plasma in 30 minutes after intake. The maximum concentration is reached on average in 3 hours after reception. Does not get through a blood-brain barrier. Communication with proteins of plasma makes 83-87%. At use for adults and teenagers within 14 days in a dose from 5 mg to 20 mg of 1 times in days of clinically significant cumulation of drug it is not noted. The concomitant use of food or grapefruit juice does not influence distribution of a dezloratadin at use in a dose of 7,5 mg of 1 times a day.
Dezloratadin is not CYP3A4 and CYP2D6 inhibitor and is not substrate or inhibitor of a P-glycoprotein. It is intensively metabolized in a liver by a hydroxylation with education 3-ON-dezloratadina, connected to a glucuronide. Only a small part of the dose accepted inside is removed by kidneys (<2%) and through intestines (<7%). An elimination half-life – 20-30 hours (on average – 27 hours).

Indications to use:

- allergic rhinitis (elimination or simplification of sneezing, a congestion of a nose, mucifying from a nose, an itch in a nose, an itch of the sky, an itch and reddening of eyes, dacryagogue);
- small tortoiseshell (reduction or elimination of a skin itch, rash).

Route of administration and doses:

Inside, irrespective of meal, to adults and teenagers since 12 years on 1 tablet a day. The tablet should be swallowed entirely, washing down with water.

Features of use:

Researches of efficiency of a dezloratadin at rhinitises of an infectious etiology were not conducted.
Influence on ability to drive the car and other mechanical means
An adverse effect on driving or difficult technical devices was not noted.

Side effects:

WHO classification of frequency of development of side effects:
very often - ≥1/10 appointments (> 10%)
often      - from ≥1/100 to <1/10 appointments (> 1% and <10%)
infrequently  - from ≥1/1000 to <1/100 appointments (> 0.1% and <1%)
seldom      - from ≥1/10000 to <1/1000 appointments (> 0.01% and <0.1%)
very seldom - <1/10000 appointments (<0.01%)
Disturbances from immune system
Very seldom: allergic reactions, including an anaphylaxis.
Disturbances from a nervous system
Infrequently: headache.
Disturbances from heart
Very seldom: tachycardia, heartbeat.
Disturbances from digestive tract
Infrequently: dryness in a mouth.
Disturbances from skin and hypodermic fabrics
Very seldom: rash.
The general frustration and disturbances in an injection site
Often: increased fatigue.
Laboratory and tool data
Very seldom: increase in activity of enzymes of a liver, increase in concentration of bilirubin.

Interaction with other medicines:

Interaction with other medicines is not revealed. Meal does not exert impact on efficiency of drug. Dezloratadin does not strengthen effect of alcohol on the central nervous system.

Contraindications:

- hypersensitivity to any of substances which is a part of drug;
- pregnancy and lactation;
- age up to 12 years.

With care: heavy chronic renal failure.

Use at pregnancy and in the period of a lactation:
Dezloratadin Kanon is not recommended to accept drug during pregnancy as the corresponding clinical trials were not conducted and safety of use during pregnancy is not established.
Dezloratadin gets into breast milk therefore the women nursing should not accept drug Dezloratadin Kanon.

Overdose:

Symptoms. Reception of the dose exceeding recommended by 5 times did not lead to emergence of any symptoms. During clinical tests daily use for adults and teenagers of a dezloratadin in a dose to 20 mg within 14 days was not followed statistically or clinically significant changes from cardiovascular system. In a kliniko-pharmacological research use of a dezloratadin in a dose of 45 mg a day (is 9 times higher than the recommended dose) within 10 days did not cause lengthening of an interval of QT and was not followed by emergence of serious side effects.
Treatment. At accidental intake of a large amount of drug it is necessary to see a doctor immediately. The gastric lavage, reception of absorbent carbon is recommended; if necessary – symptomatic therapy. Dezloratadin is not brought at a hemodialysis, efficiency of peritoneal dialysis is not established.

Storage conditions:

In the dry, protected from light place at a temperature not above 25 °C. To store in the place, unavailable to children. Period of validity: 2 years. Not to apply after a period of validity.

Issue conditions:

According to the recipe

Packaging:

Tablets, film coated, 5 mg.
On 7, 10 or 30 tablets in a blister strip packaging from a film of the polyvinyl chloride and printing aluminum foil varnished.
On 1, 2, 3 blister strip packagings on 7 or 10 tablets or on 1, 2 blister strip packagings on 30 tablets together with the application instruction place in a pack from a cardboard.