Дезлоратадин Канон Uses, Dosage, Side Effects and more

Дезлоратадин Канон is a long-acting, tricyclic, non-sedating, selective peripheral histamine H1-receptor antagonist which inhibits the release of pro-inflammatory mediators from human mast cells and basophils.

Дезлоратадин Канон is a long-acting second-generation H1-receptor antagonist which has a selective and peripheral H1-antagonist action. Histamine is a chemical that causes many of the signs that are part of allergic reactions, such as the swelling of tissues. Histamine is released from histamine-storing cells (mast cells) and attaches to other cells that have receptors for histamine. The attachment of the histamine to the receptors causes the cell to be "activated," releasing other chemicals which produce the effects that we associate with allergies. Дезлоратадин Канон blocks one type of receptor for histamine (the H1 receptor) and thus prevents activation of cells by histamine. Unlike most other antihistamines, Дезлоратадин Канон does not enter the brain from the blood and, therefore, does not cause drowsiness.

Attribute	Details
Trade Name	Дезлоратадин Канон
Availability	Prescription only
Generic	Desloratadine
Desloratadine Other Names	Descarboethoxyloratadine, Desloratadina, Desloratadine
Related Drugs	prednisone, cetirizine, loratadine, fluticasone nasal, promethazine, diphenhydramine, Zyrtec, Xolair
Type
Formula	C19H19ClN2
Weight	Average: 310.821 Monoisotopic: 310.123676325
Protein binding	Desloratadine is bound approximately 82 to 87% to plasma proteins, while its active metabolite, 3-hydroxydesloratadine, is bound approximately 85 to 89%.
Groups	Approved, Investigational
Therapeutic Class	Non-sedating antihistamines
Manufacturer
Available Country	Russia
Last Updated:	January 7, 2025 at 1:49 am

Uses

Allergic Rhinitis: Дезлоратадин Канон is used for the relief of the nasal and non-nasal symptoms of allergic rhinitis (Both seasonal and perennial) in patients 2 years of age and older.

Chronic Idiopathic Urticaria: Дезлоратадин Канон is also used for the symptomatic relief of pruritus, reduction in the number of hives, and size of hives, in patients with chronic idiopathic urticaria 2 years of age and older.

Дезлоратадин Канон is also used to associated treatment for these conditions: Allergic Rhinitis (AR), Asthma, Chronic Idiopathic Urticaria, Common Cold, Nasal Congestion, Perennial Allergic Rhinitis (PAR), Seasonal Allergic Rhinitis, Nasal symptoms, Non-nasal symptoms, Antihistamine

How Дезлоратадин Канон works

Like other H1-blockers, Дезлоратадин Канон competes with free histamine for binding at H₁-receptors in the GI tract, uterus, large blood vessels, and bronchial smooth muscle. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms (eg. nasal congestion, watery eyes) brought on by histamine.

Dosage

Pediatric drops :

• Child 6 -11 months of age: 2 ml drops once daily
• Child 1 -2 years of age: 2.5 ml drops once daily

Syrup:

• Child 6-11 months of age: 2 ml once daily
• Child 1-5 years of age: 2.5 ml once daily
• Child 6-11 years of age: 5 ml once daily
• Adults & > 12 years of age: 10 ml once daily

Tablet:

• Adults and children 12 years of age and over: 5 mg daily

Side Effects

Дезлоратадин Канон is generally well tolerated. However, dry mouth, fatigue, somnolence and myalgia are commonly reported side-effects. Less common side-effects may include dizziness, headache and nausea. Rarely rash, pruritus and urticaria may occur.

Toxicity

Information regarding desloratadine overdose is limited, although somnolence has been reported. In case of overdose, symptomatic and supportive treatment, including removing the unabsorbed drug, is recommended; note, however, that desloratadine and its active metabolite 3-hydroxydesloratadine cannot be eliminated by hemodialysis.

In animal studies, lethality was observed at or above doses of 250 mg/kg in rats and of 353 mg/kg in mice (oral LD₅₀), doses that represent 120 and 290 times the human exposure based on the recommended daily oral dose. In monkey, no deaths occurred at doses up to 250 mg/kg, representing an exposure roughly 810 times that of the recommended dose in humans.

Precaution

Hepatic and renal impairment. Pregnancy and lactation.

Interaction

Concomitant administration of Erythromycin, Ketoconazole, Azithromycin, Fluoxetine, and Cimetidine with Дезлоратадин Канон increased the plasma concentration of Дезлоратадин Канон. But there were no clinically relevant changes in the safety profile of Дезлоратадин Канон.

Food Interaction

• Take with or without food. The absorption is unaffected by food.

Disease Interaction

Moderate: asthma, renal/hepatic impairment

Elimination Route

Дезлоратадин Канон administered orally for ten days to healthy volunteers as a 5 mg tablet once daily resulted in a mean T_max of approximately 3 hours, a mean steady-state C_max of 4 ng/ml, and a mean steady-state AUC of 56.9 ng*hr/ml. A similar profile was observed using 10 ml of an oral solution containing 5 mg of desloratadine. Food was found not to affect desloratadine absorption.

Half Life

Дезлоратадин Канон has a mean plasma elimination half-life of approximately 27 hours.

Elimination Route

Approximately 87% of a C-desloratadine dose was equally recovered in urine and feces as metabolic products.

Pregnancy & Breastfeeding use

Pregnancy: There are no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, Дезлоратадин Канон should be used in pregnancy only if clearly needed.

Lactation: Дезлоратадин Канон passes into breast milk. Therefore, a decision should be made whether to discontinue nursing or to discontinue Дезлоратадин Канон, taking into account the importance of the drug to the mother.

Contraindication

Дезлоратадин Канон is contraindicated in patient having hypersensitivity to this medication or to any of its ingredients or Loratadine.

Special Warning

Paediatric Use: The safety and effectiveness of Дезлоратадин Канон in pediatric patients under 2 years of age have not been established.

Geriatric Use: In general, dose selection for an elderly patient should be cautious, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.

In adult patients with liver or renal impairment: A starting dose of one 5 mg tablet every other day is recommended based on pharmacokinetic data.

Acute Overdose

No clinically relevant adverse events have been reported in case of overdosage. However, in the event of overdosage, symptomatic and supportive treatment is recommended.

Storage Condition

Store in a cool and dry place, protected from light.

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