Dezloratadin

General characteristics. Structure:

Active ingredient: 5 mg of a dezloratadin in 1 tablet.

The drug having antihistaminic, antiallergic, antiinflammatory effect.

Pharmacological properties:

Pharmacodynamics. Selectively blocks peripheral histamine H1 receptors. Suppresses the cascade of cytotoxic reactions: release of pro-inflammatory cytokines, including интерлейкина−4 (ИЛ−4), интерлейкина−6 (ИЛ−6), интерлейкина−8 (ИЛ−8), интерлейкина−13 (ИЛ−13), chemokines like RANTES, products of superoxidic anion the activated polymorphonuclear neutrophils, adhesion and a chemotaxis of eosinophils, an expression of molecules of adhesion, including. R-selectin, IgE-dependent allocation of a histamine, PGD2 and LTS4 .

During clinical tests daily use for adults and teenagers of a dezloratadin in a dose to 20 mg within 14 days was not followed significant (statistical or clinical) by changes from cardiovascular system. In a kliniko-pharmacological research use of a dezloratadin in a dose of 45 mg/days (in 9 times more of therapeutic) within 10 days did not cause lengthening of an interval of QTc  and was not followed by emergence of serious side effects. Use in a dose of 7,5 mg is not followed by disturbances of psychomotor functions, and in a dose of 5 mg — increase in frequency of emergence of drowsiness in comparison with group of placebo.

Researches on animals showed ability of a dezloratadin to eliminate an acute allergic bronchospasm.

Pharmacokinetics. Bioavailability is proportional to a dose (in the range from 5 to 20 mg). Dezloratadin begins to be defined in plasma within 30 min. after reception. Time of achievement of Cmax  in plasma after a single dose of 5 or 7,5 mg — 2–6 h (on average 3 h). Contacts proteins of plasma for 83–87%. T1/2  — 20–30 h (on average 27 h). Does not pass through GEB, gets through a placental barrier and into breast milk. Also the glyukuronirovaniya is extensively metabolized by a hydroxylation with education 3-ON-dezloratadina. It is removed with urine (less than 2% in not changed look) and excrements (less than 7% in not changed look). At reception of doses of 5-20 mg/days during 2 weeks of cumulation it is not observed.

Indications to use:

Symptomatic therapy of seasonal and year-round allergic rhinitis, chronic idiopathic small tortoiseshell.

Route of administration and doses:

Inside, irrespective of meal, to adults and teenagers at the age of 12 years is also more senior — 5 mg/days. To children (in the form of syrup) aged from 1 year up to 5 years — 1,25 mg/days, 6–11 years — 2,5 mg/days.

Features of use:

Use at pregnancy and feeding by a breast. It is contraindicated at pregnancy. Category of action on a fruit on FDA — C. For the period of treatment it is necessary to stop breastfeeding (gets into breast milk).

Influence of a dezloratadin on ability to driving of motor transport and to control of mechanisms is not established.

Side effects:

Tablets. Increased fatigue (1,2%), dryness in a mouth (0,8%), a headache (0,6%). Very seldom — tachycardia, heartbeat, increase in activity of liver enzymes, increase in concentration of bilirubin, allergic reactions, including an anaphylaxis and rash.

Syrup. At children under 2 years the following undesirable phenomena (frequency slightly higher were noted, than at placebo use): diarrhea, fervescence, insomniya.

At children the frequency of development of side effects 2-11lt it was comparable with placebo.

At adults and teenagers 12 years (frequency slightly higher are more senior, than at placebo use): increased fatigue, dryness in a mouth, a headache.

At use of a dezloratadin in the recommended dose of 5 mg/days the frequency of emergence of drowsiness was not higher, than at placebo use.

Among very rare side effects dizziness, drowsiness, tachycardia, heartbeat, an abdominal pain, nausea, vomiting, dyspepsia, diarrhea, increase in content of bilirubin, liver enzymes in blood serum, allergic reactions (an anaphylaxis, a Quincke's disease, an itch, rash, a small tortoiseshell) are noted.

Interaction with other medicines:

When studying medicinal interaction at repeated combined use of a dezloratadin with ketokonazoly, erythromycin, azithromycin, fluoxetine and Cimetidinum of clinically significant changes of concentration of a dezloratadin in plasma it is not revealed. The concomitant use of food does not influence distribution of a dezlotadin in an organism. Dezlotadin does not strengthen effect of alcohol on TsNS.

Contraindications:

Hypersensitivity, pregnancy, feeding by a breast. For syrup (in addition, in connection with existence in composition of sucrose and sorbitol): hereditarily the fructose transferred intolerance, disturbance of absorption of a glucose/galactose or insufficiency of sucrose/isomaltose.

Restrictions to use. The expressed renal failure, children's age (till 1 year), children's age (up to 12 years) for the tableted forms (safety and efficiency of use are not defined).

Overdose:

Symptoms: strengthening of expressiveness of side reactions.

Treatment: a gastric lavage, purpose of absorbent carbon, if necessary — symptomatic therapy. The hemodialysis is inefficient. Efficiency of peritoneal dialysis is not established.

Storage conditions:

To store at a temperature of 15-25 °C, in dry, protected from light and the place, unavailable to children. Period of validity 3 years. Not to use after the expiry date specified on packaging.

Issue conditions:

Without recipe

Packaging:

Tablets of 5 mg, 20 tablets in each blister, on one, two or three blisters together with the application instruction in cardboard packaging.