Лордес®

General characteristics. Structure:

Active ingredient: 0,5 mg of a dezloratadin in 1 ml of syrup.

Excipients: propylene glycol (monopropylene glycol), anhydrous citric acid, sodium citrate, Natrium benzoicum, dinatrium эдетат, a sukroza (the sugar refined), sorbitol of 70% solution, beta carotene (лукаротин 1 CWDY), the red charming EXPERT (E129), Fragrance Tutti Frutti (AG 7322), water purified.

Pharmacological properties:

Pharmacodynamics. Dezloratadin, active agent of Lordes, is the selection blocker peripheral histamine H1 receptors. Dezloratadin is primary active metabolite of a loratadin. High-quality or quantitative discrepancies of toxicity of a dezloratadin and loratadin in comparable doses (taking into account concentration of a dezloratadin) are not revealed. The mechanism of action of a dezloratadin consists in blocking of release of a histamine and C4 leukotriene from mast cells, thereby preventing development and facilitating the course of allergic reactions.

Has antiallergic, antipruritic and antiexudative effect. Reduces permeability of capillaries, edematization of fabrics warns, eliminates a spasm of unstriated muscles. Dezloratadin does not get through a blood-brain barrier, respectively, does not cause drowsiness and does not change the speed of psychomotor reactions.

Pharmacokinetics. Bioequivalence of drug in the form of tablets and syrup is revealed. Dezloratadin begins to be defined in a blood plasma within 30 min. after reception. The maximum concentration of a dezloratadin (C max) in plasma is reached on average in 3 h (T max). Bioavailability of a dezloratadin is proportional to a dose from 5 to 20 mg. It is established that food (a fat high-calorific breakfast) or grapefruit juice do not influence distribution of a dezloratadin. Dezloratadin moderately (83 – 87%) contacts proteins of plasma. Does not get through a blood-brain barrier, gets through a placental barrier and into breast milk. Is exposed to intensive metabolism.

The main way of metabolism of a dezloratadin - a hydroxylation in situation 3 with education 3-OH dezloratadin, connected to a glucuronide. At use of a dezloratadin in a dose from 5 to 20 mg once a day within 14 days of signs of clinically significant cumulation of drug it is not revealed. Extent of cumulation of a dezloratadin corresponds to its elimination half-life and frequency rate of use (once a day). The elimination half-life (T1/2) makes 20–30 h (on average 27 h). Dezloratadin is brought from an organism in the form of glyukuronidny connection. A small part of a dose is removed in not changed view with a stake and urine.

Indications to use:

- seasonal and year-round allergic rhinitis;

- chronic idiopathic small tortoiseshell.

Route of administration and doses:

Drug is accepted inside. Before the use contents of a bottle should be shaken up well.

Children: from 1 to 5 years on 2,5 ml (1/2 measured spoons - 1,25 mg) drug once a day; from 6 to 11 years on 5,0 ml (1 measured spoon - 2,5 mg) once a day;

Adults and teenagers (since 12 years): 10,0 ml of syrup (5,0 mg) once a day.

Лордес® accept irrespective of meal. The course of treatment is appointed by the doctor individually.

Features of use:

Efficiency and safety of use of Lordes® syrup for children till 1 year is not established. At children aged from 1 to 2 years at use ЛОРДЕСа diarrhea, fervescence, sleeplessness which frequency was slightly higher, than at placebo use were noted.

Children aged from 2 up to 11 years at Lordes's use had the same frequency of side effects, as at placebo use. At use of drug for adults and teenagers in the recommended dose of 5 mg a day the frequency of emergence of drowsiness was not higher, than at placebo use.

Лордес® does not cause disturbance of psychomotor function and drowsiness. As drug contains 0,4 g of a sukroza in a single dose of drug, it is necessary to appoint it with care the patient with a diabetes mellitus. At prolonged use (two and more than a week) Lordesa due to the maintenance of a sukroza perhaps damaging action on teeth.

At daily use of the drug Lordes® in a dose to 20 mg within 14 days of clinically significant changes from cardiovascular system was not revealed.

In case of a heavy renal failure, ЛОРДЕС® it is necessary to apply with care.

Drug contains sorbitol in the structure. Patients with hereditary intolerance of fructose, a sprue of a glucose/galactose or sakharo-izomaltazny insufficiency have to abstain from administration of drug ЛОРДЕС®.

Pregnancy and period of a lactation. Safety of use of the drug Lordes® for pregnant women is not established therefore it is not recommended to appoint it during pregnancy.

Dezloratadin gets into breast milk therefore the women nursing should not appoint Lordes®.

Features of influence of medicine on ability to manage the vehicle and potentially dangerous mechanisms. Influence of Lordes® on driving or work with difficult technical devices was not noted. However, it is necessary to consider that in rare instances after administration of drug drowsiness which can exert impact on ability to drive the car or other mechanisms is observed.

Side effects:

Often (> 1%, <10%):

- increased fatigue.

Not often (≥1/1000, <1/100):

- headache;

- dryness in a mouth.

Very seldom (<1/10000):

- hypersensitivity reactions (rash, urticaria, itch, Quincke's disease, asthma, acute anaphylaxis);

- dizziness, drowsiness, sleeplessness, psychomotor hyperactivity, spasms;

- tachycardia, the felt heartbeat;

- nausea, vomiting, dyspepsia, diarrhea, abdominal pain, increase in activity of "hepatic transaminases", increase in concentration of bilirubin, hepatitis;

- mialgiya.

Interaction with other medicines:

Clinically significant interactions of a dezloratadin with other medicines are not revealed.

Лордес® does not strengthen the oppressing effect of ethanol on psychomotor function.

Clinically significant interactions with ketokonazoly and erythromycin are not revealed.

Contraindications:

- hypersensitivity to active agent or other components of drug;

- children's age till 1 year;

- pregnancy and period of a lactation;

- heavy degree of a chronic renal failure;

- hereditary intolerance of fructose, disturbance of absorption of a glucose/galactose or insufficiency of invertase/isomaltase in an organism - in connection with availability of sugar and sorbitol as a part of syrup.

Overdose:

Symptoms: a headache, dryness in a mouth, fatigue.

Treatment: gastric lavage, reception of absorbent carbon, symptomatic therapy. ЛОРДЕС® it is not removed by means of a hemodialysis.

Storage conditions:

To store at a temperature not above 25 °C, in the dry, protected from light place. To store in the place, unavailable to children! Period of storage 3 years. Not to apply after the storage expiration.

Issue conditions:

According to the recipe

Packaging:

100 ml of drug place in a bottle of orange glass with the screwing-up cover with control of the first opening.

On a bottle paste the self-adhesive label. 1 bottle together with a measured spoon or a volumetric glass and the instruction on a medical use in the state and Russian languages is placed in a cardboard pack.