Desal (Tablets, Solution) Instructions for Use

ATC Code

R06AX27 (Desloratadine)

Active Substance

Desloratadine (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Histamine H₁-receptor blocker. Antiallergic drug

Pharmacotherapeutic Group

Systemic antihistamines; other systemic antihistamines

Pharmacological Action

Desloratadine is a long-acting antihistamine, a blocker of peripheral histamine H₁-receptors. Desloratadine is the primary active metabolite of loratadine. It inhibits the cascade of allergic inflammation reactions, including the release of pro-inflammatory cytokines, such as interleukins IL-4, IL-6, IL-8, IL-13, the release of pro-inflammatory chemokines, the production of superoxide anions by activated polymorphonuclear neutrophils, eosinophil adhesion and chemotaxis, the release of adhesion molecules, such as P-selectin, IgE-mediated release of histamine, prostaglandin D₂, and leukotriene C₄.

Thus, the drug prevents the development and alleviates the course of allergic reactions, has antipruritic and anti-exudative effects, reduces capillary permeability, prevents the development of tissue edema, and spasm of smooth muscles.

The drug does not affect the central nervous system, practically does not have a sedative effect (does not cause drowsiness) and does not affect the speed of psychomotor reactions when taken in recommended doses. It does not cause QT interval prolongation on the ECG.

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

Pharmacokinetics

Administration of desloratadine as an oral solution is equivalent to its use in tablet form containing a similar amount of the active substance.

Absorption

After oral administration, Desloratadine is well absorbed from the gastrointestinal tract. It is detected in blood plasma after 30 minutes, and C_max is reached in approximately 3 hours. No clinically significant changes in desloratadine plasma concentrations were observed with repeated administration of ketoconazole and erythromycin. The bioavailability of desloratadine is proportional to the dose in the range from 5 mg to 20 mg.

Distribution

Plasma protein binding is 83-87%. When used in adults and adolescents for 14 days at doses from 5 mg to 20 mg once daily, no signs of clinically significant accumulation of desloratadine were noted. The degree of accumulation of desloratadine is consistent with the T_1/2 value and its once-daily dosing frequency. AUC and C_max values in children were similar to those in adults receiving 5 mg of desloratadine.

Concomitant intake of food or grapefruit juice does not affect the distribution of desloratadine (when taken at a dose of 7.5 mg once daily). It does not penetrate the blood-brain barrier.

Metabolism

The enzymes responsible for the metabolism of desloratadine are not yet known, so interaction with some drugs cannot be completely ruled out. It 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-OH-desloratadine, which is then glucuronidated.

Excretion

T_1/2 is about 27 hours. Desloratadine is excreted from the body as a glucuronide conjugate and in small amounts unchanged (in urine – less than 2% and through the intestine – less than 7%).

Indications

For the relief or elimination of symptoms

• allergic rhinitis (sneezing, nasal congestion, rhinorrhea, nasal itching, itching of the palate, itchy and red eyes, lacrimation);
• urticaria (skin itching, rash).

ICD codes

Dosage Regimen

Tablets

Orally, regardless of meals.

Adults and adolescents (12 years and older) – 5 mg (1 tablet) once daily.

Solution

Take orally, regardless of meals.

Children aged 1 to 5 years – 2.5 ml of solution (1.25 mg) once daily.

Children aged 6 to 11 years – 5 ml of solution (2.5 mg) once daily.

Adults and adolescents (12 years and older)– 10 ml of solution (5 mg) once daily.

Adverse Reactions

In children aged 2 to 11 years, the incidence of side effects with desloratadine was the same as with placebo.

In children under 2 years of age, the following side effects were observed with desloratadine, the frequency of which was somewhat higher than with placebo: diarrhea (3.7%), fever (2.3%), insomnia (2.3%).

In adults and adolescents aged 12 years and older, the following side effects were observed with desloratadine, the frequency of which was somewhat higher than with placebo: increased fatigue (1.2%), dry mouth (0.8%), headache (0.6%).

When the drug was used in adults and adolescents at the recommended dose of 5 mg/day, the incidence of drowsiness was no higher than with placebo.

During post-marketing surveillance, the following adverse reactions were very rarely reported.

Psychiatric disorders: hallucinations.

Nervous system disorders: dizziness, drowsiness, insomnia, psychomotor hyperactivity.

Cardiovascular system disorders: tachycardia, palpitations.

Gastrointestinal disorders: abdominal pain, nausea, vomiting, dyspepsia, diarrhea.

Hepatobiliary disorders: increased liver enzyme activity, increased bilirubin concentration, hepatitis.

Musculoskeletal and connective tissue disorders: myalgia.

Allergic reactions: anaphylaxis, angioedema, itching, rash, urticaria.

Contraindications

• Hypersensitivity to the active substance or any excipient of the drug;
• Pregnancy;
• Lactation (breastfeeding);
• Children under 1 year of age (efficacy and safety have not been established);
• Hereditary diseases – fructose intolerance, glucose/galactose malabsorption or sucrase/isomaltase deficiency in the body (due to the presence of sorbitol in the preparation).

Use with caution in severe renal impairment.

Use in Pregnancy and Lactation

The use of the drug during pregnancy is contraindicated due to the lack of clinical data on its safety during this period.

Desloratadine is excreted in breast milk, so its use during breastfeeding is contraindicated.

Use in Renal Impairment

The drug should be used with caution in severe renal failure.

Pediatric Use

Contraindicated for use in children under 12 years of age, as efficacy and safety have not been established.

Special Precautions

The efficacy and safety of Desal in children under 1 year of age have not been established.

The differential diagnosis between allergic rhinitis and rhinitis of other origins in children under 2 years of age presents certain difficulties. When conducting a differential diagnosis, attention should be paid to the presence or absence of foci of infection or structural anomalies of the upper respiratory tract, a thorough history should be taken, an examination should be performed, and appropriate laboratory tests and skin tests should be conducted.

Approximately 6% of adults and children aged 2 to 11 years have a low capacity for desloratadine metabolism; Desloratadine is eliminated more slowly in this group of patients. The safety profile of desloratadine in children aged 2 to 11 years with low metabolism is similar to that in children with normal desloratadine metabolism. The effect of desloratadine on children under 2 years of age with low metabolism has not been studied.

In case of severe renal impairment, Desal should be used with caution.

Effect on ability to drive vehicles and operate machinery

Studies of the effect of desloratadine on the ability to drive a car did not reveal any impairment of concentration. However, it should be borne in mind that very rarely, some patients may develop drowsiness; in this case, caution should be exercised when driving vehicles and operating machinery.

Overdose

Symptoms: taking a dose 9 times higher than the recommended dose (45 mg) did not lead to any clinically significant symptoms. Drowsiness may develop.

Treatment: gastric lavage, administration of activated charcoal is necessary; if necessary, symptomatic therapy. Desloratadine is not removed by hemodialysis; the effectiveness of peritoneal dialysis has not been established.

If a large amount of the drug is accidentally ingested, the patient should consult a doctor immediately.

Drug Interactions

No clinically significant interaction with other drugs has been identified (including with ketoconazole and erythromycin).

Desloratadine does not enhance the effect of ethanol on the central nervous system.

Storage Conditions

The drug should be stored out of the reach of children at a temperature not exceeding 25°C (77°F).

Shelf Life

Shelf life – 3 years.

Dispensing Status

The drug is approved for use as an over-the-counter product.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.