Ezlor - instructions for use, dose, side effects, contraindications

auxiliary substances (core): lactose monohydrate (milk sugar) 70.0 mg; cellulose microcrystalline 12.1 mg; Povidone (polyvinylpyrrolidone) 3.0 mg; magnesium stearate 0.9 mg; croscarmellose sodium 4.0 mg;

auxiliary substances (shell): fall off II 85F48105 White 3.0 mg, incl. (polyvinyl alcohol 1.407 mg, macrogol 3350 0.708 mg, talc 0.522 mg, titanium dioxide 0.363 mg).

Description:

Round, biconvex tablets covered with a film shell of white or almost white color, two layers are visible on a cross section - a core of white or almost white color and a film membrane.

Pharmacotherapeutic group:antiallergic agent - H1-histamine receptor blocker

ATX: & nbsp

R.06.A.X Other antihistamines for systemic use

R.06.A.X.27 Desloratadine

Pharmacodynamics:

Blocker H₁-gistaminovyh receptors (long-acting). It is the primary active metabolite of loratadine. Inhibits a cascade of allergic inflammation reactions, including the release of anti-inflammatory cytokines, including interleukins IL-4, IL-6, IL-8, IL-13, the release of pro-inflammatory chemokines (RANTES), the production of superoxide anions by activated polymorphonuclear neutrophils, the adhesion and chemotaxis of eosinophils, the release of adhesion molecules such as P-selectin, IgE-mediated release of histamine, prostaglandin D2 and leukotriene C4. Thus, it prevents development and facilitates the course of allergic reactions, has antipruritic and antiexcudative action, reduces permeability of capillaries, prevents the development of edema of tissues, spasm of smooth muscles.

The drug has no effect on the central nervous system, has practically no sedative effect (does not cause drowsiness) and does not affect the rate of psychomotor reactions. Does not cause lengthening of the interval QT on the ECG.

The action of the drug begins within 30 minutes after ingestion and lasts for 24 hours.

Pharmacokinetics:

Suction

After taking the drug inside desloratadine is well absorbed from the gastrointestinal tract, with determined concentrations of desloratadine in the blood plasma reached within 30 minutes, and the maximum concentration - after about 3 hours.

Distribution

The binding of desloratadine to plasma proteins is 83-87%. When used in adults and adolescents for 14 days at a dose of 5 mg to 20 mg 1 time / day clinically significant cumulation of desloratadine is not noted. Simultaneous food intake or simultaneous consumption of grapefruit juice does not affect the distribution of desloratadine (when taken at a dose of 7.5 mg 1 time / day). Does not penetrate the blood-brain barrier.

Metabolism

It is subjected to intensive metabolism in the liver by hydroxylation to form 3-OH-desloratadine, combined with glucuronide. Is not an inhibitor of isoenzymes CYP3A4 and CYP2D6 and is not a substrate or an inhibitor of P-glycoprotein.

Excretion

Only a small part of the dose taken internally is excreted by the kidneys (<2%) and through the intestine (<7%). Half-life is 20-30 hours (on average - 27 hours).

Indications:

- Allergic rhinitis (elimination or relief of sneezing, nasal congestion, mucus discharge from the nose, itching of the nose, itching of the palate, itching and redness of the eyes, lachrymation);

- urticaria (reduction or elimination of itching, rash).

Contraindications:

- Hypersensitivity to any of the components that make up the drug;

- pregnancy and lactation;

- age up to 12 years;

- lactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome.

Carefully:Severe kidney failure.

Pregnancy and lactation:

The use of the drug in pregnancy is contraindicated due to the lack of clinical data on the safety of its use during pregnancy.

Desloratadine is excreted in breast milk, so the use of the drug during breastfeeding is contraindicated.

Dosing and Administration:

The tablet should be swallowed whole, not liquid, squeezed with a small amount of water. The drug should preferably be taken at the same time of the day, regardless of the time of ingestion.

Adults and adolescents aged 12 years or over - 1 tablet (5 mg) once a day.

Side effects:

The incidence of side effects is classified according to the recommendations of the World Health Organization: very often - not less than 10%; often - not less than - 1%, but less than 10%; infrequently - not less than 0,1%, but less than 1%; rarely - not less than 0.01%, but less than 0.1%; very rarely - less than 0.01%.

From the immune system: very rarely - a rash, including hives, angioedema, urticaria, dyspnea, anaphylactic shock.

From the central nervous system: infrequently - a headache; very rarely - dizziness, drowsiness, insomnia, psychomotor hyperactivity, convulsions, hallucinations.

From the cardiovascular system: very rarely - tachycardia, palpitation.

From the gastrointestinal tract: infrequently dry mouth; Very rarely - nausea, vomiting, indigestion, diarrhea, abdominal pain, increased activity of "liver" enzymes, increased bilirubin concentration, hepatitis.

From the osteomuscular system and connective tissue: very rarely - myalgia.

Other: often - increased fatigue.

Overdose:

Symptoms: taking a dose that exceeds the recommended dose by a factor of 5 did not lead to any symptoms. In clinical trials, the daily use of desloratadine in adults and adolescents at doses up to 20 mg for 14 days was not accompanied by statistically or clinically significant changes in the cardiovascular system. In the clinical pharmacological study of the use of desloratadine at a dose of 45 mg per day (9 times higher than recommended) for 10 days did not cause lengthening of the interval QT and was not accompanied by serious side effects.

Treatment: with the occasional ingestion of a large amount of the drug - gastric lavage, the reception of activated charcoal; if necessary, symptomatic therapy. Desloratadine is not excreted in hemodialysis, the effectiveness of peritoneal dialysis is not established.

Interaction:

Interactions with other drugs have not been identified.

Eating does not affect the effectiveness of the drug.

Desloratadine does not enhance the effect of alcohol on the central nervous system.

Effect on the ability to drive transp. cf. and fur:

In the recommended dose, the drug does not affect the ability to drive vehicles or control mechanisms.

Form release / dosage:

Tablets, film-coated, 5 mg.

Packaging:

For 10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

By 10, 20, 30, 40, 50, or 100 tablets in cans of polymeric for medicines.

One jar or 1, 2, 3, 4, 5, 6, 8 or 10 contour squares, together with the instructions for use, are placed in a cardboard package (pack) of cardboard.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date.

Terms of leave from pharmacies:Without recipe

Registration number:LP-002161

Date of registration:26.07.2013

Expiration Date:26.07.2018

The owner of the registration certificate:ATOLL, LLC ATOLL, LLC Russia

Manufacturer: & nbsp

OZONE, LLC Russia

Information update date: & nbsp01.01.2016

Illustrated instructions

Instructions

Ezlor (Ezlor)