Loratek

General characteristics. Structure:

Active ingredient: дезлоратадин; 1 tablet contains a dezloratadin of 5 mg;
excipients: lactose anhydrous, cellulose microcrystallic, silicon dioxide colloid anhydrous, sodium is krokhmalglikolit, talc, magnesium stearate, a cover (a gipromeloza, polyethyleneglycol, talc, titanium dioxide (Е 171), a varnish covering indigo carmine (Е 132) and diamond blue (Е 133)).

Pharmacological properties:

Dezloratadin – nesedativny antihistaminic drug of long action; the high-selection blocker peripheral histamine H1 receptors. Prevents development and facilitates the course of allergic reactions, reduces permeability of capillaries, edematization of fabrics, a spasm of smooth muscles warns. Dezloratadin - primary active metabolite of a loratadin. Dezloratadin significantly (by 10 - 50 times) surpasses in antihistaminic activity лоратадин, терфенадин, фексофенадин and him similar. Dezloratadin is characterized by the highest relationship to H1 - histamine receptors, in comparison with other representatives of this group. The Afinnost to H2-histamine and muskarinovy receptors is 15 - 50 times less, than to H1 receptors that testifies to its high selectivity. Additional antiallergenic effects of Loratek are not connected with blockade of H1-histamine receptors.
Except antihistaminic activity дезлоратидин possesses antiallergic and antiinflammatory action. Dezloratidin suppresses the cascade of various reactions which are the cornerstone of development of an allergic inflammation, including such as:
- release of antiinflammatory cytokines and chemokines;
- products of superoxidic anion the activated polymorphonuclear neutrophils;
- release of antiinflammatory chemokines, such as RANTES;
- 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;
- acute allergic bronchospasm.
Antiallergenic and antiinflammatory properties cause high performance of a dezloratadin. Dezloratadin effectively eliminates both nasal symptoms of allergic rhinitis, and not nasal (an itch and reddening of eyes, dacryagogue, a sky itch, cough and so forth). Dezloratadin is effective also in case of a combination at the patient of bronchial asthma to allergic rhinitis. At these patients Loratek's action extends not only to rhinitis symptoms, but also to the clinical course of asthma, improving indicators of function of external respiration and reducing requirement in β2-агонистах.
As a result of researches it is revealed what дезлоратадин does not suppress CYP3A4 or CYP2D6 and is not either substrate, or R-glycoprotein inhibitor.
In a research with one-time reception of a dezloratadin in a dose of 7,5 mg it was shown that meal (a fat high-calorific breakfast) or grapefruit juice does not influence distribution of a dezloratadin.
Does not get through a blood-brain barrier, does not possess sedation.
Dezloratadin is defined in plasma for the first 30 min. after administration of drug. The maximum concentration of a dezloratadin in plasma is reached approximately in 3 hours. The elimination half-life averages 27 hours. Extent of cumulation of a dezloratadin answers its elimination half-life (27 hours) and frequency rates of use (once a day). Bioavailability of a dezloratadin is proportional to a dose in the range from 5 to 20 mg.
Dezloratadin moderately (83 - 87%) contacts proteins of plasma. At use of a dezloratadin in a dose from 5 to 20 mg once a day for 14 days of signs of clinically significant cumulation of drug it is not revealed.
When carrying out pharmacokinetic researches in pediatric practice it was revealed that AUC indicator (the area under a pharmakokinetichny curve) and the maximum concentration of a dezloratadin in Cmax blood plasma (at use in the recommended doses) can be equated to the same indicators at the adults receiving дезлоратадин in the form of syrup in a dose of 5 mg.

Indications to use:

Bystry elimination of allergic states, including pollinosis and allergic rhinitis (sneezing, allocation from a nose, an itch, hypostasis and puffiness of a nose, and also an itch of eyes, dacryagogue and reddening of eyes, a sky itch, cough); treatment of a chronic idiopathic small tortoiseshell.

Route of administration and doses:

Adults and children aged from 12 years: 1 tablet of Loratek of 5 mg of 1 times a day irrespective of meal. Duration of treatment is defined by duration of the period of contact of the patient with allergen.

Features of use:

Use during pregnancy or feeding by a breast.
Not to apply during pregnancy or feeding by a breast.

Ability to influence speed of response at control of motor transport or work with other mechanisms.
Does not influence.

Children. It is not necessary to use drug to children aged up to 12 years.

Appropriate security measures at use. It is necessary to appoint with care to patients with a heavy renal failure. Loratek's reception has no negative action on digestive tract therefore Loratek it is possible to apply irrespective of meal in any time, convenient for the patient. In kliniko-pharmacological researches дезлоратадин did not strengthen such effects of alcohol as disturbance of psychomotor function and drowsiness. Results of psychomotor tests significantly did not differ at patients who applied дезлоратадин and placebo separately or together with alcohol. Loratek has no sedation, results in block or drowsiness in the afternoon therefore it can be recommended to persons of any professions, including to those which activity requires special attention and speed of psychomotor reactions.

Side effects:

In clinical trials at use of a dezloratadin in the recommended dose of 5 mg / to Dob the frequency of the undesirable phenomena was 3% higher, than in group of placebo. At adults and teenagers (12 years are also more senior) at use of a dezloratadin such undesirable effects which frequency was slightly above, than at placebo use were observed: increased fatigue, dryness in a mouth, a headache. Isolated cases of dizziness, drowsiness, tachycardia, a heart consciousness, an abdominal pain, nausea, vomiting, dyspepsia, diarrhea, increase in content of bilirubin, liver enzymes in blood serum, allergic reactions (anfilaktichny shock, a Quincke's disease, an itch, rash, a small tortoiseshell) are celebrated.

Interaction with other medicines:

Clinically significant interaction of drug with other medicines is not established. Loratek can be applied in combination with drugs which block P450 cytochrome and alcohol. At simultaneous use with ketokonazoly and erythromycin of clinically significant changes of concentration of a dezloratadin in plasma it is not revealed. Loratek it is possible to appoint together with fluoxetine and azithromycin.

Contraindications:

Hypersensitivity to any of drug components.

Overdose:

In case of overdose the standard actions directed to removal of not adsorbed active agent are shown (to wash out a stomach, to accept absorbent carbon). The symptomatic treatment is recommended. In clinical trials of a dezloratadin at adults and children who accepted doses to 45 mg (that by 9 times was exceeded by recommended) heavy undesirable reactions are not revealed. Dezloratadin does not leave by a hemodialysis; the possibility of its removal at peritoneal dialysis is not established.

Storage conditions:

To store in original packaging at a temperature not above 25 °C in the place, unavailable to children.

Period of validity - 2 years.

Issue conditions:

Without recipe

Packaging:

On 10 tablets in the blister. On 1 blister in a cardboard box.