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

Round biconvex tablets, covered with a film coating of blue color. On the cross-section, two layers are visible: the core is from white or almost white to white with a slightly pinkish hue of color and a blue casing. Roughness of the surface of tablets is allowed.

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:

Antihistamine is a long-acting drug, H1-gistaminovyh peripheral receptor blocker. 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-4, IL-6, IL-8, IL-13, release of pro-inflammatory chemokines, production of superoxide anions by activated polymorphonuclear neutrophils, adhesion and chemosensitivity of eosinophils,the division of adhesion molecules, such as P-selectin, lgE-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 (CNS), has almost 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 an electrocardiogram (ECG).

The action of desloratadine 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 (GIT), with determined concentrations of desloratadine in the blood plasma are reached within 30 minutes, and the maximum concentration in the blood plasma (CmOh) - approximately 3 hours later.

Distribution

The binding of desloratadine to plasma proteins is 83-87%. When applied at a dose of 5 mg to 20 mg once a day for 14 days, no signs of clinically significant cumulation of desloratadine were detected. Simultaneous food intake or simultaneous use of grapefruit juice does not affect the distribution of desloratadine (when taken at a dose of 7.5 mg once a day). Does not penetrate the blood-brain barrier (BBB).

Metabolism

Exposed to intensive metabolism by hydroxylation to form 3-OH-desloratadine, coupled with glucuronide. Is not an inhibitor of isoenzymes CYP3A4 and CYP2D6 and is not a substrate or an inhibitor of P-glycoprotein.

Excretion

It is excreted from the body in the form of a glucuronide compound and in a small amount in unchanged form, a small part is excreted by the kidneys (2%) and with calves (7%). The half-life (T1 / 2) is an average of 27 hours.

Indications:

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

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

Contraindications:

Hypersensitivity to desloratadine and other components of the drug or loratadine, pregnancy, the period of breastfeeding, children under 12 years.

Carefully:

Renal failure is severe.

Pregnancy and lactation:

The use of desloratadine is contraindicated in pregnancy and during breastfeeding (insufficient data on efficacy and safety).

Dosing and Administration:

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

Adults and children over 12 years of age: 5 mg (1 tablet) once a day.

In seasonal (intermittent) allergic rhinitis (if symptoms last less than 4 days per 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 (persistent) allergic rhinitis (in the presence of 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:

The most common undesirable effects (≥1 / 100 to <1/10): increased fatigue (in 1.2% of cases), dry mouth (0.8%) and headache (0.6%).

Very rarely (<1/10000), the following undesirable effects were noted:

- from the side of the nervous system: hallucinations, dizziness, drowsiness, insomnia, psychomotor hyperactivity, convulsions;

- from the side of the liver and bile ducts: increased activity of liver enzymes, increased concentrations of bilirubin, hepatitis;

- from the digestive system: abdominal pain, nausea, vomiting, indigestion, diarrhea;

- from the cardiovascular system: tachycardia, palpitations;

- from the musculoskeletal system: myalgia;

- allergic reactions: anaphylaxis, angioedema, dyspnea, pruritus, rash, including urticaria;

- from the skin and subcutaneous tissues: photosensitization.

Frequency unknown: lengthening interval QT, jaundice, asthenia.

Post-registration period.

Children: Frequency unknown - lengthening interval QT, arrhythmia, bradycardia.

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

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 a clinical pharmacological study, the use of desloratadine at a dose of 45 mg per day (9 times the recommended dose) for 10 days did not cause an extension of the interval QT and was not accompanied by the appearance of serious side effects.

Treatment: 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. If you ingest large amounts of the drug, you should immediately consult a doctor.

Interaction:

There were no clinically significant interactions in studies with co-administration with azithromycin, ketoconazole, erythromycin, fluoxetine, and cimetidine. Simultaneous intake of food or grapefruit juice does not affect the effectiveness of the drug.

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

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. When these undesirable phenomena appear, one should refrain from performing these activities.

Form release / dosage:Tablets, film-coated 5 mg.

Packaging:

For 10 tablets in a planar cell package. 1, 3 contoured cell packs together with instructions for use are placed in a pack of cardboard.

Storage conditions:

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-004335

Date of registration:13.06.2017

Expiration Date:13.06.2022

The owner of the registration certificate:TATHIMFARMPREPARATY, JSC TATHIMFARMPREPARATY, JSC Russia

Manufacturer: & nbsp

TATHIMFARMPREPARATY, JSC Russia

Information update date: & nbsp23.10.2017

Illustrated instructions

Instructions

Desloratadine (Desloratadine)