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

Excipients: calcium hydrogen phosphate dihydrate 140.3 mg, salted (microcrystalline cellulose 98%, silicon colloidal dioxide 2% 21.6 mg, hypromellose hydroxypropyl methylcellulose 3.6 mg, croscarmellose sodium impellose 0.9 mg, silicon colloidal dioxide (aerosil) - 1.8 mg, magnesium stearate - 1.8 mg;

composition of the shell: opahedra II blue (polyvinyl alcohol 40.0%, titanium dioxide (E171) 24.66%, talc (E553b) 14.80%, macrogol (polyethylene glycol) (E1521) 20.20%, aluminum varnish based on indigo carmine (E132) 0.34%) 4.967 mg emulsion simethicone 30% (water 50.0-69.5%, dimethicone (polydimethylsiloxane) 25.5-33.0%, macrogol (polyethylene glycol) sorbitan tristearate 3.0-7.0%, methylcellulose 1.0-5.0%, silica gel 1.0-5.0%), 0.033 mg.

Description:Round, biconvex tablets, film-coated, blue. Insignificant roughness of the surface is permissible. The color of the tablets on the break is white or white with a yellowish or pinkish tinge.

Pharmacotherapeutic group:Antiallergic agent - H2-histamine receptor blocker

ATX: & nbsp

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

R.06.A.X.27 Desloratadine

Pharmacodynamics:

Antihistamine is a long-acting drug. Desloratadine is the primary active metabolite of loratadine. Inhibits the cascade of allergic inflammation reactions, including the release of pro-inflammatory cytokines, including interleukins (IL) IL-4, IL-6, IL-8, IL-13, 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, possesses antipruritic and antiexclusive action, reduces permeability of capillaries, prevents the development of edema of tissues, spasm of smooth musculature.

The drug has no effect on the central nervous system (CNS), has no sedative effect and does not affect the rate of psychomotor reactions. In clinico-pharmacological studies of the use of desloratadine in the recommended therapeutic zone there was no lengthening of the interval QT on an electrocardiogram (ECG).

The effect of desloratadine begins within 30 minutes after ingestion and lasts for 24 hours.

Pharmacokinetics:

After taking the drug inside desloratadine is well absorbed from the gastrointestinal tract (GIT). It is determined in the blood plasma 30 minutes after ingestion. The maximum concentration (C_m_Oh) is achieved on average 3 hours after admission. Bioavailability of desloratadine is dose-proportional when taking a dose in the range from 5 mg to 20 mg.

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 once a day, there are no signs of clinically significant cumulation of the drug.

Simultaneous intake of food or grapefruit juice does not affect the distribution of desloratadine (when administered at a dose of 7.5 mg 1 time per day). Does not penetrate the blood-brain barrier.

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

The half-life (T_1/2) is 20-30 hours (on average - 27 hours). Desloratadine is excreted from the body in the form of a glucuronide compound and in a small amount in unchanged form (kidneys less than 2% and through the intestine less than 7%).

Indications:

- Cezone and year-round allergic rhinitis (elimination or alleviation 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, skin rashes).

Contraindications:

- Hypersensitivity to desloratadine, loratadine, as well as to other components of the drug;

- pregnancy and the period of breastfeeding;

- children under 12 years.

Carefully:

- Severe renal insufficiency;

- cramps in the anamnesis.

Pregnancy and lactation:

The use of the drug in pregnancy is contraindicated due to the lack of clinical data on the safety of the drug Desloratadine in this period. Desloratadine excreted in breast milk, therefore its use during breastfeeding is contraindicated.

Dosing and Administration:

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

Adults and teenagers from 12 years old - 1 tablet (5 mg) once a day.

With seasonal allergic rhinitis (if symptoms last less than 4 days a week or less than 4 weeks per year), it is necessary to evaluate the course of the disease. With the disappearance of symptoms, the drug should be discontinued, if the symptoms reappear, the drug should be resumed.

With year-round allergic rhinitis (with symptoms lasting more than 4 days a week or more than 4 weeks per year), the drug should be taken during the entire exposure period of the allergen.

Side effects:

According to the World Health Organization (WHO), the undesirable effects are classified according to the frequency of their development as follows: very often (≥1/10), often (≥1 / 100 and <1/10), infrequently (≥1 / 1000 and < 1/100), rarely (≥1 / 10000 and <1/1000) and very rarely (<1/10000), including individual messages; frequency is unknown - according to available data, it was not possible to establish the frequency of occurrence.

From the central nervous system: often - headache; very rarely dizziness, drowsiness, insomnia, psychomotor hyperreactivity, hallucinations, convulsions: frequency unknown - abnormal behavior, aggression.

From the cardiovascular system: very rarely - tachycardia, palpitation; frequency unknown - interval elongation QT.

From the digestive system: often - dry mouth; very rarely - abdominal pain, nausea, vomiting, indigestion, diarrhea.

From the liver and bile ducts: very rarely - increased activity of liver enzymes, increased concentrations of bilirubin, hepatitis.

From the musculoskeletal system: very rarely - myalgia.

Allergic reactions: very rarely - anaphylaxis, angioedema, dyspnea, itching, skin rash, urticaria.

From the skin and subcutaneous tissues: frequency unknown - photosensitivity.

Other: often - increased fatigue.

Post-registration period.

Children: frequency unknown - interval elongation QT, arrhythmia, bradycardia, abnormal behavior, aggression.

If any of the side effects listed in the manual are aggravated, or if you notice any other side effects not listed in the instructions, tell your doctor.

Overdose:

Symptoms. Taking a dose that exceeds the recommended dose by 5 times 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, 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 the appearance of serious side effects.

Treatment. If you ingest large amounts of the drug, you should immediately consult a doctor. Recommended gastric lavage, reception of activated charcoal; if necessary, symptomatic therapy. Desloratadine is not excreted in hemodialysis, the effectiveness of peritoneal dialysis is not established.

Interaction:

When studying the drug interaction with multiple simultaneous use of desloratadine with ketoconazole, erythromycin, azithromycin, fluoxetine and cimetidine clinically significant changes in the concentration of desloratadine in plasma were not detected.

Simultaneous reception grapefruit juice does not affect the effectiveness of the drug.

Desloratadine does not increase the effect alcohol on the central nervous system, nevertheless, during the post-registration use cases of alcohol and alcohol intolerance were reported. therefore desloratadine Alcohol should be used with caution.

Special instructions:

Drug efficacy studies Desloratadine with rhinitis of infectious etiology was not performed.

In clinical trials, it has been shown that increasing the dose and increasing the frequency of administration does not affect the effectiveness of the drug, so it is necessary to warn patients that it is not recommended to increase the dosage and frequency of admission.

Care should be taken when using the drug Desloratadine in patients with seizures in the anamnesis, especially in patients of childhood. In the case of seizures, the use of Desloratadine should be discontinued.

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

Consideration should be given to the potential for the development of side effects such as dizziness and drowsiness. During drug treatment, care should be taken when performing potentially hazardous activities requiring increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Tablets, film-coated, 5 mg.

Packaging:

For 7 or 10 tablets in a contour mesh package.

For 1, 2, 3, 4 or 5 contour squares with instructions for use in a cardboard pack.

Storage conditions:

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

Keep out of the reach of children.

Shelf life:

4 years. Do not use after the expiration date.

Terms of leave from pharmacies:Without recipe

Registration number:LP-004567

Date of registration:06.12.2017

Expiration Date:06.12.2022

The owner of the registration certificate:BIOKOM, CJSC BIOKOM, CJSC Russia

Manufacturer: & nbsp

BIOKOM, CJSC Russia

Information update date: & nbsp18.12.2017

Illustrated instructions

Instructions

Desloratadine (Desloratadine)