Dezloratadin-Tev

General characteristics. Structure:

Active agent: дезлоратадин 5,000 mg;
excipients: cellulose of microcrystallic 65,800 mg, magnesium oxide of 2,250 mg, starch of prezhelatinizirovanny 4,750 mg, lactose of 4,500 mg, gipromelloza-4 one thousand 1,700 mg, zinc stearate of 1,000 mg;
film cover: Опадрай blue 03B90819 2,975 mg (gipromelloza of 60,00%, titanium dioxide of 27,21%, macrogoal-400 of 8,00%, indigo carmine (varnish aluminum E132) 4,79%).

Description
Round biconvex tablets, film coated blue color, with an engraving of "D" on one party and smooth on the other hand.

Pharmacological properties:

Pharmacodynamics. Antihistaminic drug of long action, H1-histamine peripheral receptors blocker. Dezloratadin 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, products of superoxidic anions the activated polymorphonuclear neutrophils, adhesion and a chemotaxis of eosinophils, allocation of molecules of adhesion, such as R-selectin, IgE - the mediated release of a histamine, D2 prostaglandin and C4 leukotriene. Thus, prevents development and facilitates the course of allergic reactions, possesses antipruritic and anti-exudative action, reduces permeability of capillaries, edematization of fabrics, a spasm of smooth muscles warns.
Drug does not make impact on the central nervous system (CNS), 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 the electrocardiogram (ECG).
Action of a dezloratadin begins within 30 min. after intake and continues during 24 h.

Pharmacokinetics. Absorption.
After administration of drug inside дезлоратадин it is well absorbed from the digestive tract (DT), at the same time the defined concentration of a dezloratadin in a blood plasma are reached within 30 min., and the maximum concentration in plasma (Cmax) - approximately in 3 h. Meal or alcohol practically does not change pharmacological properties of drug.
Distribution.
Linkng of a dezloratadin with proteins of plasma makes 83-87%. At use in a dose from 5 mg to 20 mg of 1 times a day within 14 days of signs of clinically significant cumulation of a dezloratadin it is not revealed. The concomitant use of food or the simultaneous use of grapefruit juice does not influence distribution of a dezloratadin (at reception in a dose of 7,5 mg of 1 times a day). Does not get through a blood-brain barrier (GEB).
Metabolism.
Is exposed to intensive metabolism by a hydroxylation with education 3-ON-dezloratadina, connected to a glucuronide. Is not inhibitor of isoenzymes of CYP3A4 and CYP2D6 and is not substrate or inhibitor of the R-glycoprotein.
Removal. It is brought out of an organism in the form of glyukuronidny connection and in a small amount in not changed look, a small part is removed by kidneys (2%) and with a fecal masses (7%). The elimination half-life (T1/2) averages 27 h (20-30 h).

Indications to use:

- Seasonal (pollinosis) and year-round allergic rhinitises (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).
- Chronic idiopathic small tortoiseshell (reduction or elimination of a skin itch, rash).

Route of administration and doses:

Inside, irrespective of meal at the same time days. The tablet should be swallowed entirely, without chewing, washing down with a small amount of water.
To adults and children 12 years are more senior: on 5 mg of 1 times a day.

Features of use:

For protection of tablets against light blisters should be stored in a cardboard pack.

Influence on ability to management of transport and work with the equipment
At development of undesirable reactions from the central nervous system, such as drowsiness, dizziness, hallucinations, performance of the actions demanding the increased concentration of attention and speed of psychomotor reactions is not recommended.

Side effects:

Frequency of development of side effects is classified according to recommendations of World Health Organization: very often - not less than 10%; often - not less than 1%, but less than 10%; infrequently - not less than 0,1%, but less than 1%; seldom - not less than 0,01%, but less than 0,1%; very seldom - less than 0,01%.
From immune system: very seldom - rash, including urticaria, a Quincke's disease, диспноэ, an acute anaphylaxis.
From TsNS: infrequently - a headache; very seldom - dizziness, drowsiness, sleeplessness, a psychomotor hyperactivity, spasms, hallucinations.
From cardiovascular system: very seldom - tachycardia, a heart consciousness.
From digestive tract: infrequently - dryness in a mouth; very seldom - nausea, vomiting, dyspepsia, diarrhea, an abdominal pain, increase in activity of "hepatic transaminases", increase in concentration of bilirubin, hepatitis.
From a musculoskeletal system and connecting fabric: very seldom - a mialgiya.
Others: often - increased fatigue.

Interaction with other medicines:

Clinically significant interaction with other medicines is not revealed.
Dezloratadin does not strengthen effect of ethanol on TsNS.
Meal does not exert impact on efficiency of drug.

Contraindications:

Hypersensitivity to a dezloratadin and other components of drug, pregnancy, the breastfeeding period, age up to 12 years, a lactose intolerance, insufficiency of lactase, glyukozo-galaktozny malabsorption.

With care
Renal failure of heavy degree.

Use at pregnancy and during breastfeeding
Drug use Dezloratadin-Tev contraindicated at pregnancy and during breastfeeding (there are not enough data on efficiency and safety).

Overdose:

Symptoms: reception of the dose exceeding recommended by 5 times did not lead to emergence of any symptoms.
During clinical trials 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 recommended) within 10 days did not cause lengthening of an interval of QT and was not followed by emergence of serious side effects.
Treatment: gastric lavage, reception of absorbent carbon; if necessary - symptomatic therapy. Dezloratadin is not brought at a hemodialysis, efficiency of peritoneal dialysis is not established.

Storage conditions:

To store at a temperature not above 25 °C. To store in the place, unavailable to children. Period of validity 3 years. Not to apply after the period of validity specified on packaging.

Issue conditions:

Without recipe

Packaging:

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