Instruction for use: Desloratadine

Latin name of the substance Desloratadine

Desloratadinum (genus. Desloratadini)

Chemical name

8-chloro-6,11-dihydro-11- (4-piperidinylidene) -5H-benzo [5,6] cyclohepta [1,2-b] pyridine

Gross formula

C₁₉H₁₉ClN₂

Pharmacological group of the substance Desloratadine

H1-Antihistamines

The nosological classification (ICD-10)

J30 Vasomotor and allergic rhinitis: Allergic rhinopathy; Allergic rhinosinusopathy; Allergic diseases of the upper respiratory tract; Allergic rhinitis; Allergic rhinitis seasonal; Vasomotor runny nose; Prolonged allergic rhinitis; All-year-round allergic rhinitis; All-year allergic rhinitis; Year-round or seasonal allergic rhinitis; All-the-year-round rhinitis of an allergic nature; Rhinitis vasomotor allergic; Exacerbation of pollinosis in the form of rhinoconjunctival syndrome; Acute allergic rhinitis; Edema of the nasal mucosa; Edema of the nasal mucosa; Edema of the mucous membrane of the nasal cavity; Swelling of the nasal mucosa; Swelling of the nasal mucosa; Pollinosis; Permanent allergic rhinitis; Rhinoconjunctivitis; Rhinosinusitis; Rhinosinusopathy; Seasonal allergic rhinitis; Seasonal allergic rhinitis; Hay rhinitis; Chronic allergic rhinitis; Allergic diseases of the respiratory tract

L50.1 Idiopathic urticaria: Idiopathic urticarial; Chronic idiopathic urticaria

CAS code

100643-71-8

Characteristics of the substance Desloratadine

White or almost white powder. Slightly soluble in water, very soluble in ethanol and propylene glycol. Molecular weight is 310.8.

Pharmacology

Pharmacological action - anti-inflammatory, anti-allergic, antihistamine.

Selectively blocks peripheral histamine H1 receptors. Suppresses the cascade of cytotoxic reactions: the release of proinflammatory cytokines, incl. Interleukin-4 (IL-4), interleukin-6 (IL-6), interleukin-8 (IL-8), interleukin-13 (IL-13), RANTES type chemokines, superoxide anion production by activated polymorphonuclear neutrophils, adhesion and chemotaxis Eosinophils, expression of adhesion molecules, incl. P-selectin, IgE-dependent histamine release, PGD2 and LTS4.

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 significant (statistical or clinical) changes in the cardiovascular system. In a clinical pharmacological study, the use of desloratadine at a dose of 45 mg / day (9 times the therapeutic dose) for 10 days did not cause prolongation of the QTc interval and was not accompanied by serious side effects. Application in a dose of 7.5 mg is not accompanied by disorders of psychomotor functions, and in a dose of 5 mg - an increase in the incidence of drowsiness compared with the placebo group.

Studies in animals have shown the ability of desloratadine to eliminate acute allergic bronchospasm.

Bioavailability is proportional to the dose (in the range of 5 to 20 mg). Desloratadine begins to be detected in the plasma within 30 minutes after administration. Time to achieve Cmax in the plasma after a single intake of 5 or 7.5 mg - 2-6 hours (an average of 3 hours). It binds to plasma proteins at 83-87%. T1 / 2 - 20-30 hours (an average of 27 hours). It does not pass through the BBB, it penetrates the placental barrier and into breast milk. Extensively metabolized by hydroxylation to form 3-OH-desloratadine and glucuronation. It is excreted in urine (less than 2% unchanged) and feces (less than 7% unchanged). When taking doses of 5-20 mg / day for 2 weeks cumulation is not observed.

Application of substance Desloratadine

Symptomatic therapy of seasonal and year-round allergic rhinitis, chronic idiopathic urticaria.

Contraindications

Hypersensitivity, pregnancy, breast-feeding. For syrup (in addition, due to the presence of sucrose and sorbitol in the composition): hereditarily transmitted fructose intolerance, impaired glucose / galactose absorption or sucrose / isomaltose insufficiency.

Restrictions

Severe renal insufficiency, children's age (up to 1 year), children's age (up to 12 years) for tablets (safety and efficacy not determined).

Application in pregnancy and breastfeeding

Contraindicated in pregnancy.

Action category for fetus by FDA - C.

At the time of treatment, breastfeeding should stop (penetrates into breast milk).

Side effects of Desloratadine

Tablets. Increased fatigue (1.2%), dry mouth (0.8%), headache (0.6%). Very rarely - tachycardia, palpitation, increased activity of hepatic enzymes, increased bilirubin concentrations, allergic reactions, including anaphylaxis and rash.

Syrup. In children under 2 years of age, the following adverse events were noted (frequency slightly higher than with placebo): diarrhea, fever, insomnia.

In children 2-11 years of age, the incidence of side effects was comparable to placebo.

In adults and adolescents older than 12 years (the frequency is slightly higher than when using placebo): increased fatigue, dry mouth, headache.

When using desloratadine at the recommended dose of 5 mg / day, the incidence of drowsiness was not higher than with placebo.

Dizziness, drowsiness, tachycardia, palpitation, abdominal pain, nausea, vomiting, dyspepsia, diarrhea, increased bilirubin, hepatic enzymes in the blood serum, allergic reactions (anaphylaxis, angioedema, itching, rash, urticaria) are very rare side effects. ).

Interaction

In the study of drug interaction with repeated combined use of desloratadine with ketoconazole, erythromycin, azithromycin, fluoxetine and cimetidine, no clinically significant changes in desloratadine concentration in plasma have been detected. Simultaneous food intake does not affect the distribution of desloratadine in the body. Desloratadine does not increase the effect of alcohol on the central nervous system.

Overdose

Symptoms: increased severity of adverse reactions.

Treatment: gastric lavage, the appointment of activated charcoal, if necessary - symptomatic therapy. Hemodialysis is ineffective. The effectiveness of peritoneal dialysis is not established.

Routes of administration

Inside.

Precautions for the substance Desloratadine

The influence of desloratadine on the ability to drive vehicles and control mechanisms has not been established.