Erius

General characteristics. Structure:

Active agent: 5,0 mg of a dezloratadin.

Inactive components: disubstituted calcium phosphate, microcrystallic cellulose, corn starch, talc. Structure of a cover of a tablet: blue film covering (lactoses monohydrate, gidroksipropilmetiltsellyuloz, titanium dioxide, polyethyleneglycol, varnish aluminum blue FD&C No. 2), transparent film covering (gidroksipropilmetiltsellyuloz, polyethyleneglycol), karnaubsky wax, white wax.

Pharmacological properties:

ERIUS (дезлоратадин) – not sedative is long the operating antihistaminic drug possessing the selection antagonistic action on peripheral H1-histamine receptors. Dezloratadin is primary active metabolite of a loratadin.

Pharmacodynamics. After intake of ERIUS selectively blocks peripheral H1-histamine receptors and does not get through a blood-brain barrier. The numerous researches in vitro (mainly on cells of the person) and in vivo showed that in addition to antihistaminic activity of ERIUS has antiallergic and antiinflammatory effect. In these researches it is established that ERIUS suppresses the cascade of various reactions which are the cornerstone of development of an allergic inflammation, including the following:

- release of pro-inflammatory cytokines, including IL-4, IL-6, IL-8, IL-13;
- release of pro-inflammatory chemokines, such as RANTES;
- products of superoxidic anion the activated polymorphonuclear neutrophils;
- adhesion and chemotaxis of eosinophils;
- expression of molecules of adhesion, such as R-selectin;
- IgE-dependent allocation of a histamine, D2 prostaglandin and C4 leukotriene;
- an acute allergic bronchospasm (in researches on animals).
At clinical tests daily use ЭРИУСа 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 ЭРИУСа on 45 mg/days (is 9 times higher than a therapeutic dose) within 10 days did not cause lengthening of an interval of QTc.

ERIUS does not get through a blood-brain barrier. At its use in the recommended dose of 5 mg the frequency of drowsiness did not exceed that in group of placebo. In clinical trials of ERIUS at reception in a dose of 7,5 mg did not influence psychomotor function. When studying interaction with ketokonazoly and erythromycin of clinically significant changes of concentration ЭРИУСа in plasma it is not revealed. In kliniko-pharmacological researches ERIUS did not strengthen such effects of alcohol as disturbance of psychomotor function and drowsiness. Results of psychomotor tests significantly did not differ at the patients receiving ERIUS and placebo separately or in combination with alcohol.

Pharmacokinetic properties. Dezloratadin begins to be defined in plasma within 30 min. after reception. The maximum concentration of a dezloratadin in plasma is reached during from 2 to 6 hours (on average in 3 hours) after a single dose of drug in a dose of 5 mg or 7,5 mg. Dezloratadin is extensively metabolized in an organism; only a small part of the dose accepted inside is removed with urine (<2%) and a stake (<7%). The main way of metabolism of a dezloratadin - a hydroxylation in a position 3 with education 3-ON-dezloratadina, connected to a glucuronide. In the form of glyukuronidny connection drug then is removed from an organism. The elimination half-life makes from 20 to 30 hours (on average 27 h). Extent of cumulation of a dezloratadin corresponded to its elimination half-life (about 27 h) and frequency rates of use (once a day). Bioavailability of a dezloratadin was proportional to a dose in the range from 5 mg to 20 mg.

Dezloratadin moderately (83-87%) contacts proteins of a pazma. At use of a dezloratadin in a dose from 5 mg to 20 mg once a day within 14 days of signs of clinically significant cumulation of drug it is not revealed. In a research with a single dose of a dezloratadin in a dose of 7,5 mg food (a fat high-calorific breakfast) did not exert impact on distribution of a dezloratadin.

Indications to use:

- ERIUS is applied to bystry stopping of symptoms of seasonal allergic rhinitis, such as sneezing, allocations of a nose, by an itch and a congestion of a nose, an itch and reddening of eyes, dacryagogue, a sky itch.
- ERIUS is applied, also, at a chronic idiopathic small tortoiseshell to reduction and elimination of an itch and rash.

Route of administration and doses:

Adults and teenagers of 12 years: on one tablet of 5 mg a day irrespective of meal. Drug is intended for intake. The tablet should be swallowed entirely, without chewing and to wash down with water.

Features of use:

Efficiency and safety ЭРИУСа at children aged up to 12 years still is up to the end not investigated. At a renal failure of heavy degree reception ЭРИУСа needs to be carried out with care.

USE AT PREGNANCY AND the LACTATION. ЭРИУС it is not recommended to accept during pregnancy as the corresponding clinical trials were not conducted and safety of use ЭРИУСа during pregnancy is not established. Dezloratadin gets into breast milk therefore the women nursing should not accept ERIUS.

INFLUENCE ON the PSYCHOMOTOR FUNKTSIYU.KAKOGO-libo of influence ЭРИУСа on ability of driving or difficult technical devices is noted.

Side effects:

The undesirable phenomena were compared at 659 patients receiving ERIUS of 5 mg and 661 patients receiving placebo. In clinical trials character and frequency of undesirable effects at use ЭРИУСа in general were comparable to placebos, those at use.

In controlled and uncontrollable clinical trials of ERIUS did not cause clinically significant undesirable reactions, including from cardiovascular system. At use ЭРИУСа in the recommended dose of 5 mg/days the frequency of the undesirable phenomena was 4% higher, than in group of placebo. Increase in frequency of drowsiness is noted. The headache was observed at 2% of the patients receiving ERIUS. Dryness in a mouth and exhaustion met seldom (> 1/1000? 1/100).

Interaction with other medicines:

In clinical trials of signs of significant interaction ЭРИУСа with ketokonazoly and erythromycin it is not revealed. ERIUS did not strengthen overwhelming effect of alcohol on psychomotor function.

Contraindications:

Hypersensitivity to active agent or any inactive component. Pregnancy and period of breastfeeding.

Overdose:

In case of overdose the standard actions directed to removal of not absorbed active agent are shown. The symptomatic treatment is recommended.

ERIUS is not removed at a hemodialysis; the possibility of its removal at peritoneal dialysis is not established.

Storage conditions:

To store at a temperature from +2 °C to +30 °C, in the dry place not available to children.

Issue conditions:

Without recipe

Packaging:

On 7 or 10 tablets in packaging.