Aerius^® (Tablets, Syrup) 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

Antiallergic agent – H₁-histamine receptor blocker

Pharmacological Action

A long-acting non-sedative antihistamine drug. It is the primary active metabolite of loratadine. It suppresses the release of histamine from mast cells.

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, and the release of adhesion molecules, such as P-selectin.

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

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.

In clinical and pharmacological studies of the use of desloratadine at the recommended therapeutic dose, no prolongation of the QT interval on the ECG was noted.

The action of the drug Aerius^® begins within 30 minutes after oral administration and lasts for 24 hours.

Pharmacokinetics

Absorption

After oral administration, Desloratadine is well absorbed from the gastrointestinal tract. It is detected in blood plasma 30 minutes after oral administration. C_max is reached on average 3 hours after administration.

Distribution

The binding of desloratadine to plasma proteins is 83-87%. When used in adults and adolescents for 14 days at doses from 5 mg to 20 mg once a day, no signs of clinically significant accumulation of desloratadine were detected.

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

Metabolism

It is intensively metabolized by hydroxylation to form 3-OH-desloratadine, conjugated with glucuronide. Desloratadine is not an inhibitor of CYP3A4 and CYP2D6 and is not a substrate or inhibitor of P-glycoprotein.

Excretion

Only a small part of the orally administered dose is excreted by the kidneys (<2%) and through the intestines (<7%) unchanged.

T_1/2 – on average 27 hours.

Indications

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

ICD codes

Dosage Regimen

Tablets

For oral administration.

The tablet should be swallowed whole, without chewing, and washed down with water.

It is advisable to take the drug regularly at the same time of day, regardless of meals.

Adults and adolescents from 12 years old – 1 tablet (5 mg) once a day.

When treating seasonal allergic rhinitis (presence of symptoms lasting less than 4 days per week or less than 4 weeks per year) it is necessary to assess the course of the disease. After the symptoms disappear, the drug should be discontinued. If symptoms recur, treatment can be resumed.

For perennial allergic rhinitis (presence of symptoms lasting more than 4 days per week and more than 4 weeks per year) long-term treatment is expected throughout the period of contact with the allergen.

For urticaria, use in the presence of symptoms, the individual duration of therapy is determined by the doctor.

Syrup

Orally, regardless of meals, with a small amount of water.

Children aged from 6 to 12 months – 1 mg (2 ml of syrup) once a day.

Children aged from 1 year to 5 years – 1.25 mg (2.5 ml of syrup) once a day.

Children aged from 6 to 11 years – 2.5 mg (5 ml of syrup) once a day.

Adults and adolescents from 12 years old – 5 mg (10 ml of syrup) once a day.

Adverse Reactions

In children aged from 6 to 23 months the following side effects were observed, the frequency of which was somewhat higher than with placebo: diarrhea (3.7%), increased body temperature (2.3%), insomnia (2.3%).

In children aged from 2 to 11 years when using the drug Aerius^® syrup, the frequency of side effects was the same as with placebo.

According to the results of clinical studies in children aged from 6 to 11 years when taking the drug in recommended doses (2.5 mg/day), no side effects were detected.

In children aged 12-17 years according to the results of clinical studies, the most common side effect was headache (5.9%), the frequency of which was not higher than with placebo (6.9%).

In adults and adolescents aged 12 years and older according to the results of clinical studies, side effects were recorded in 3% of patients compared to the group using placebo, among which the most frequently noted were increased fatigue (1.2%), dry mouth (0.8%), headache (0.6%).

When using the drug Aerius^® in adults and adolescents at the recommended dose of 5 mg/day, the frequency of drowsiness was not higher than with placebo.

Information on side effects is provided based on the results of clinical studies and post-registration surveillance data.

According to WHO, side effects are classified according to their frequency of occurrence as follows: very common (≥1/10), common (from ≥1/100 to <1/10), uncommon (from ≥1/1000 to <1/100), rare (from ≥1/10,000 to <1/1000), very rare (<1/10,000), frequency unknown (cannot be estimated from the available data).

Psychiatric disorders: very rare – hallucinations; frequency unknown – abnormal behavior, aggression.

Nervous system disorders common – headache, in children under 2 years – insomnia; very rare – dizziness, drowsiness, insomnia, psychomotor hyperactivity, convulsions.

Hepatobiliary disorders very rare – increased activity of liver enzymes, increased bilirubin concentration, hepatitis; frequency unknown – jaundice.

Gastrointestinal disorders common – dry mouth, in children under 2 years – diarrhea; very rare – abdominal pain, nausea, vomiting, dyspepsia, diarrhea, increased appetite.

Cardiac disorders very rare – tachycardia, palpitations; frequency unknown – QT interval prolongation.

Musculoskeletal and connective tissue disorders very rare – myalgia.

Skin and subcutaneous tissue disorders frequency unknown – photosensitivity.

General disorders and administration site conditions: common – increased fatigue, in children under 2 years – fever; very rare – anaphylaxis, angioedema, dyspnea, itching, rash, including urticaria; frequency unknown – asthenia.

Investigations weight gain.

Post-registration period

Children frequency unknown – QT interval prolongation, arrhythmia, bradycardia, abnormal behavior, aggression.

If any of the above side effects worsen, or the patient notices any other side effects, they should inform the doctor.

Contraindications

• Hypersensitivity to desloratadine, other components of the drug or loratadine;
• Pregnancy;
• Breastfeeding period;
• Children under 6 months of age;
• Hereditary diseases (fructose intolerance, glucose/galactose malabsorption or sucrase/isomaltase deficiency in the body) due to the presence of sucrose and sorbitol in the syrup.

With caution

Severe renal impairment.

History of convulsions.

Use in Pregnancy and Lactation

The use of the drug Aerius^® during pregnancy is not recommended due to the lack of clinical data on its safety during this period.

Desloratadine is excreted in breast milk, therefore the use of the drug Aerius^® during breastfeeding is not recommended.

Use in Renal Impairment

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

Pediatric Use

The efficacy and safety of the drug Aerius^® in the form of syrup in children under 6 months of age has not been established, use in this category of patients is contraindicated.

Special Precautions

No studies have been conducted on the efficacy of the drug Aerius^® in rhinitis of infectious etiology.

Caution should be exercised when using the drug Aerius^® in patients with a history of convulsions, especially in pediatric patients. The use of the drug should be discontinued if convulsions develop.

Use in pediatrics

The efficacy and safety of the drug Aerius^® in the form of syrup in children under 6 months of age has not been established.

Effect on ability to drive vehicles and machinery

The potential for the development of such side effects as dizziness and drowsiness should be taken into account. If the described adverse events occur, one should refrain from performing these activities.

Overdose

Symptoms: taking a dose 5 times higher than the recommended one did not lead to the appearance of any symptoms.

In clinical studies, daily use of desloratadine in adults and adolescents at a dose of 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, the use of desloratadine at a dose of 45 mg/day (9 times higher than the recommended one) for 10 days did not cause QT interval prolongation and was not accompanied by the appearance of serious side effects.

Treatment: in case of accidental ingestion of a large amount of the drug, the patient should immediately consult a doctor. Gastric lavage, intake of activated charcoal is performed; if necessary – symptomatic therapy. Desloratadine is not removed by hemodialysis, the effectiveness of peritoneal dialysis has not been established.

Drug Interactions

Studies have not revealed interaction with azithromycin, ketoconazole, erythromycin, fluoxetine and cimetidine.

Food intake does not affect the effectiveness of the drug.

Aerius^® does not enhance the effect of ethanol on the central nervous system. Nevertheless, during post-registration use, cases of alcohol intolerance and alcohol intoxication have been recorded, therefore Desloratadine should be used with caution simultaneously with alcohol.

Storage Conditions

The drug should be stored out of the reach of children at a temperature not exceeding 30°C (86°F).

Shelf Life

Shelf life – 2 years.

Dispensing Status

The drug is available without a prescription.

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.