Erius

General characteristics. Structure:

Active agent: 1 ml дезлоратадин (micronized) 500 mkg;
Auxiliary вещества:пропиленгликоль, sorbitol (liquid, uncrystallizable), citric acid anhydrous, citrate sodium a dihydrate, Natrium benzoicum, dinatrium эдетат, sucrose, fragrance No. 15864, dye yellow No. 6 (E110), the water purified.

Pharmacological properties:

Antihistaminic drug of long action, blocker peripheral histamine H1 receptors. 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 TsNS, 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.
 
Erius's action begins within 30 min. after intake and continues during 24 h.

 

Pharmacokinetics.
Absorption
 
After administration of drug inside дезлоратадин it is well absorbed from a GIT, at the same time the defined concentration of a dezloratadin in a blood plasma are reached within 30 min., and Cmax - approximately in 3 h.

Distribution
 
Linkng of a dezloratadin 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 / 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/). Does not get through GEB.
 
Metabolism

Is exposed to intensive metabolism by a hydroxylation with education 3-ON-dezloratadina, connected to a glucuronide. Is not CYP3A4 and CYP2D6 inhibitor and is not substrate or inhibitor of the R-glycoprotein.

Removal
 
Dezloratadin is brought from an organism in the form of glyukuronidny connection and in a small amount (less than 2% with urine and less than 7% with a stake) in not changed look.
 
T1/2 averages 27 h (20-30 h).

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:

To children aged from 1 year up to 5 years appoint 1:25 mg (2.5 ml of syrup) of 1 times/; to children aged from 6 up to 11 years - on 2.5 mg (5 ml of syrup) of 1 times/; to adults and teenagers 12 years - on 5 mg (10 ml of syrup) of 1 times / are more senior
 
Syrup is accepted inside, irrespective of meal, washing down with a small amount of water.

Features of use:

Use in pediatrics
 
Efficiency and safety of use of Erius in the form of syrup at children aged till 1 year is not established.
 
In most cases rhinitis at children under 2 years has the infectious nature. Researches of efficiency of Erius at rhinitises of an infectious etiology were not conducted.
 
The differential diagnosis between allergic rhinitis and rhinitis of other origin at children under 2 years presents certain difficulties. When carrying out the differential diagnosis it is necessary to pay attention to existence or lack of the centers of an infection or structural anomalies of upper parts of respiratory tracts, to carry out careful collecting the anamnesis, inspection, and also the corresponding laboratory researches and skin tests.
 
Influence on ability to driving of the car and to control of mechanisms
 
In the recommended dose of Erius® does not influence ability to driving of vehicles or control of mechanisms.

Side effects:

At children under 2 years at Erius's use the following undesirable phenomena which frequency was slightly higher, than at placebo use were noted: diarrhea, fervescence, sleeplessness.
 
Children aged from 2 up to 11 years at Erius's use had the same frequency of side effects, as at placebo use.
 
At adults and teenagers (12 years are also more senior) at Erius's use the following undesirable phenomena which frequency was slightly higher, than at placebo use were noted: increased fatigue, dryness in a mouth, a headache.
 
At use of drug for adults and teenagers in the recommended dose of 5 mg/frequency of emergence of drowsiness was not higher, than at placebo use.
 
The following side effects were very seldom noted.
 
From TsNS: dizziness, drowsiness.
 
From cardiovascular system: tachycardia, heartbeat.
 
From the alimentary system: an abdominal pain, nausea, vomiting, dyspepsia, diarrhea, increase in content of bilirubin, liver enzymes in blood serum.
 
Allergic reactions: anaphylaxis, Quincke's disease, itch, rash, small tortoiseshell.

Interaction with other medicines:

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

Contraindications:

— pregnancy;
 
— lactation (breastfeeding);
 
— age till 1 year (for syrup);
 
— age up to 12 years (for tablets, coated);
 
— hereditarily the transmitted diseases (intolerance of fructose, disturbance of absorption of a glucose/galactose or insufficiency of invertase/isomaltase in an organism) in connection with availability of sucrose and sorbite as a part of syrup;

— hypersensitivity to drug components.
 
With care it is necessary to use drug at a renal failure of heavy degree.

 

Use at pregnancy and feeding by a breast
Use of drug at pregnancy is not recommended due to the lack of clinical data on safety of its use during this period.
 
Dezloratadin is allocated with breast milk therefore Erius's use during breastfeeding is not recommended.

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 / (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: at accidental intake of a large amount of drug - a 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:

Drug should be stored in the place, unavailable to children, at a temperature not above 30 °C. A period of validity - 2 years.

Issue conditions:

Without recipe

Packaging:

60 ml - bottles of dark glass (1) complete with the dosing spoon graduated on 2.5 ml and 5 ml - packs cardboard.
120 ml - bottles of dark glass (1) complete with the dosing spoon graduated on 2.5 ml and 5 ml - packs cardboard.