Desloratadine Canon, 5 mg 10 pcs

Pharmgroup:

Anti-allergic agent – H1-histamine receptor blocker.

Pharmic action:

Desloratadine Canon is a long-acting antihistamine drug.

It is the primary active metabolite of loratadine. It inhibits the cascade of allergic inflammatory reactions, including release of pro-inflammatory cytokines, including interleukins IL-4, IL-6, IL-8, IL-13, release of pro-inflammatory chemokines (RANTES), production of superoxide anions by activated polymorphonuclear neutrophils, eosinophil adhesion and chemotaxis, release of adhesion molecules such as P-selectin, IgE-mediated release of histamine, prostaglandin D2 and leukotriene C4.

Thereby it prevents development and facilitates the course of allergic reactions, has antipruritic and antiexudative effects, reduces capillary permeability and prevents development of tissue edema and smooth muscle spasm.

The drug has no effect on the central nervous system, it has practically no sedative effect (does not cause sleepiness) and does not affect the speed of psychomotor reactions. It does not cause prolongation of the QT interval on the ECG.

The action of desloratadine starts within 30 minutes after oral administration and lasts for 24 hours.

Pharmacokinetics:

Desloratadine is well absorbed in the gastrointestinal tract. Determined in blood plasma 30 minutes after oral administration. The maximum concentration is reached on average 3 hours after ingestion. It does not penetrate through the blood-brain barrier.

The binding to plasma proteins is 83-87%. When administered in adults and adolescents for 14 days in dose from 5 mg to 20 mg once daily there is no clinically significant cumulation of the drug. Concomitant ingestion of food or grapefruit juice does not affect the distribution of desloratadine when used at a dose of 7.5 mg once daily.

Desloratadine is not an inhibitor of CYP3A4 and CYP2D6 and is not a substrate or inhibitor of P-glycoprotein. It is intensively metabolized in the liver by hydroxylation to form 3-ON-desloratadine combined with glucuronide. Only a small part of the dose taken orally is excreted by the kidneys (< 2%) and through the intestine (< 7%). The elimination half-life is 20-30 hours (average – 27 hours).

Indications

– Allergic rhinitis (elimination or relief of sneezing, nasal congestion, nasal mucus discharge, nasal itching, palate itching, itching and red eyes, lacrimation);
– Urticaria (reduction or elimination of skin itching, rash).

Active ingredient

How to take, the dosage

Ingestion, regardless of meals, 1 tablet daily for adults and adolescents from 12 years of age. The tablet should be swallowed whole with water.

Interaction

Interaction with other medicinal products has not been revealed.

Eating has no effect on the effectiveness of the drug. Desloratadine does not increase the effect of alcohol on the central nervous system.

Special Instructions

There have been no studies on the effectiveness of desloratadine in rhinitis of infectious etiology.

Impact on the ability to drive a car and other mechanical devices:

No adverse effects on driving or operating complex technical devices have been noted.

Contraindications

– hypersensitivity to any of the substances included in the drug;
– pregnancy and lactation;
– age under 12 years.
With caution: severe chronic renal failure.

Side effects

WHO Classification of frequency of side effects:
very often – ≥1/10 appointments (>10%)
often – ≥1/100 to <1/10 appointments (>1% and <10%)
infrequent – ≥1/1000 to <1/100 appointments (>01% and <1%)
rare – ≥1/10000 to <1/1000 appointments (>0.01% and <0.1%)
very rare – <1/10000 appointments (<0.01%)

Immune system disorders
Very rare: allergic reactions, including anaphylaxis.

Nervous system disorders
Infrequent: headache.

Cardiac disorders
Very rare: tachycardia, palpitations.

Gastrointestinal tract disorders
Infrequent: dry mouth.

Skin and subcutaneous tissue disorders
Very rare: rash.

General disorders and disorders at the site of administration
Often: increased fatigue.

Laboratory and instrumental findings
Very rare: increased liver enzyme activity, increased bilirubin concentrations.

Overdose

Symptoms. Administration of 5 times the recommended dose did not result in any symptoms. In clinical trials, daily use in adults and adolescents of desloratadine in doses up to 20 mg for 14 days was not accompanied by statistically or clinically significant changes in the cardiovascular system.

In a clinical and pharmacological study, use of desloratadine at a dose of 45 mg daily (9 times the recommended dose) for 10 days did not cause QT interval prolongation and was not accompanied by any serious side effects.

Treatment. If an accidental ingestion of a large amount of the drug, it is necessary to consult a physician immediately. Gastric lavage, intake of activated charcoal is recommended; if necessary – symptomatic therapy. Desloratadine is not excreted by hemodialysis; the effectiveness of peritoneal dialysis has not been established.

Similarities