Claritin

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT CLARITINEâ (CLARITINEâ)

Composition:

Active substance: loratadine;

1 ml of syrup contains loratadine 1 mg;

Excipients: sodium dihydrogen phosphate dihydrate, phosphoric acid concentrated, disodium edetate, artificial flavoring 936.1368U, glycerin, propylene glycol, sucralose, maltitol liquid, sorbitol solution crystallizing, sodium benzoate (E 211), purified water.

Pharmaceutical form. Syrup.

Main physicochemical characteristics: clear syrup, colorless to pale yellow, free from foreign particles.

Pharmacotherapeutic group.

Antihistamines for systemic use. ATC code R06A X13.

Pharmacological Properties.

Pharmacodynamics.

Loratadine (the active ingredient of Claritin®) is a tricyclic antihistamine with selective activity against peripheral H1-receptors.

When administered at the recommended dose, it does not produce clinically significant sedative or anticholinergic effects. During prolonged treatment, no clinically significant changes were observed in vital function parameters, laboratory test results, physical examination findings, or electrocardiograms. Claritin® has no significant effect on H2-histamine receptor activity. It does not inhibit norepinephrine uptake and has virtually no effect on the cardiovascular system or cardiac pacemaker activity.

After a single 10 mg dose, skin tests for histamine response demonstrated that the antihistaminic effect becomes clinically evident within 1–3 hours, reaches peak effect between 8 and 12 hours after administration, and lasts for 24 hours. No development of tolerance was observed during 28 days of treatment.

Clinical Efficacy and Safety

Over 10,000 patients (aged 12 years and older) participated in controlled clinical trials receiving loratadine 10 mg tablets. Loratadine 10 mg once daily was more effective than placebo and demonstrated efficacy similar to that of clemastine in treating both nasal and non-nasal symptoms of allergic rhinitis. In these studies, the incidence of drowsiness was lower with loratadine compared to clemastine and similar to that observed with terfenadine and placebo.

Children

In pediatric studies, approximately 200 children (aged 6 to 12 years) with seasonal allergic rhinitis received loratadine syrup at doses up to 10 mg once daily. In another study, 60 children (aged 2 to 5 years) received loratadine syrup at a dose of 5 mg once daily. No unexpected adverse reactions were observed. Efficacy in children was similar to that observed in adults.

Pharmacokinetics.

Absorption. Loratadine is rapidly and extensively absorbed. Food intake slightly prolongs the absorption time of loratadine but does not affect its clinical effect. The bioavailability of loratadine and its active metabolite is directly proportional to the dose.

Distribution. Loratadine is highly bound (97% to 99%) to plasma proteins, while its active metabolite is moderately bound (73% to 76%).

The elimination half-life of loratadine and its active metabolite in plasma in healthy volunteers is approximately 1 and 2 hours, respectively, after administration.

Metabolism. After oral administration, loratadine is rapidly and well absorbed and metabolized primarily by CYP3A4 and CYP2D6 into desloratadine. The major metabolite, desloratadine, is pharmacologically active and largely responsible for the clinical effect. Time to reach maximum plasma concentration (Tmax) is 1–1.5 hours for loratadine and 1.5–3.7 hours for desloratadine.

Excretion. Approximately 40% of the administered dose is excreted in urine and 42% in feces over 10 days, primarily as conjugated metabolites. About 27% of the administered dose is excreted in urine within the first 24 hours. Less than 1% of the active substance is excreted unchanged in active form—either as loratadine or desloratadine.

The mean terminal elimination half-life in healthy adult volunteers is 8.4 hours (range: 3 to 20 hours) for loratadine and 28 hours (range: 8.8 to 92 hours) for its major active metabolite.

Renal Impairment. In patients with impaired renal function, the area under the plasma concentration-time curve (AUC) and maximum plasma concentration (Cmax) of loratadine and its active metabolite are higher than in patients with normal renal function. The mean elimination half-life of loratadine and its active metabolite does not differ significantly from that in healthy volunteers. In patients with chronic renal impairment, hemodialysis does not affect the pharmacokinetics of loratadine and its active metabolite.

Hepatic Impairment. In patients with chronic alcoholic liver disease, AUC and Cmax values for loratadine are approximately twice as high, while corresponding values for the active metabolite do not change significantly compared to patients with normal hepatic function. The elimination half-life of loratadine and its active metabolite is 24 and 37 hours, respectively, and increases depending on the severity of liver disease.

Elderly Patients. Pharmacokinetic parameters of loratadine and its active metabolite are similar in healthy adult volunteers, including the elderly.

Clinical characteristics.

Indications.

Symptomatic treatment of allergic rhinitis and chronic idiopathic urticaria in adults and children aged 2 years and older.

Contraindications.

Hypersensitivity to the active substance or to any of the other components of the medicinal product.

Interaction with other medicinal products and other forms of interaction.

Claritin® does not enhance the depressant effect of alcohol on psychomotor reactions.

Concomitant use of loratadine with CYP3A4 or CYP2D6 inhibitors may lead to increased loratadine levels, thereby enhancing adverse effects.

Concomitant administration of loratadine with ketoconazole, erythromycin, or cimetidine has been associated with increased plasma concentrations of loratadine; however, this increase was not clinically significant, including on electrocardiographic parameters.

Children

Studies on interactions with other medicinal products have been conducted only in adult patients.

Special precautions for use

Claritin® should be used with caution in patients with severe impairment of liver function.

Claritin® syrup should not be administered to patients with rare hereditary disorders of fructose intolerance, galactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome, or sucrase-isomaltase deficiency. If you have been diagnosed with intolerance to certain sugars, consult your doctor before taking this medication.

The medication should be discontinued no later than 48 hours prior to skin allergy testing to prevent false test results.

Use during pregnancy or breastfeeding.

Pregnancy. Extensive data from over 1000 exposed pregnancies indicate that loratadine does not cause developmental abnormalities and is not fetotoxic or harmful to newborns. Animal studies have not revealed direct or indirect adverse effects on reproductive function. However, as a precautionary measure, it is advisable to avoid using Claritin® during pregnancy.

Breastfeeding. Pharmacokinetic data indicate that loratadine and its metabolites are excreted in breast milk. Since a risk to the infant cannot be excluded, Claritin® should not be used during breastfeeding.

Fertility. There are no data available regarding the effect of the product on male or female fertility.

Ability to affect reaction speed when driving or operating machinery.

Claritin® has no effect or only a negligible effect on the ability to drive or operate machinery. However, patients should be informed that somnolence may very rarely occur, which may affect their ability to drive or operate machinery.

Dosage and Administration

Route of Administration

For oral use. The syrup can be taken regardless of food intake.

Dosage

Adults and children aged 12 years and older: take 10 ml of syrup (10 mg of loratadine) once daily.

Dosage for children aged 2 to 12 years depends on body weight:

Children with body weight above 30 kg: 10 ml (10 mg) of syrup once daily.

Children with body weight up to 30 kg: 5 ml (5 mg) of syrup once daily.

Elderly Patients

Dosage adjustment is not required for elderly patients.

Patients with Hepatic Impairment

In patients with severe hepatic impairment, a lower initial dose should be administered due to possible reduction in loratadine clearance. For adults and children with body weight above 30 kg, the recommended initial dose is 10 mg every other day; for children with body weight up to 30 kg, the recommended initial dose is 5 mg every other day.

Patients with Renal Impairment

No dosage adjustment is necessary for patients with renal impairment.

Pediatric Use

The efficacy and safety of the medicinal product in children under 2 years of age have not been established.

Overdose

In cases of overdose, anticholinergic symptoms have been reported, including drowsiness, tachycardia, and headache. Symptomatic and supportive treatment should be administered for the required duration. Standard measures to remove unabsorbed drug from the stomach are recommended, such as gastric lavage and administration of powdered activated charcoal with water.

Loratadine is not effectively removed by hemodialysis; it is also unknown whether loratadine is removed by peritoneal dialysis. After emergency treatment, the patient should remain under medical supervision.

Adverse Reactions

In clinical trials involving adults and adolescents, adverse reactions were reported in 2% of patients (exceeding the rate in patients receiving placebo) when loratadine was administered at the recommended dose of 10 mg once daily for indications including allergic rhinitis (AR) and chronic idiopathic urticaria (CIU). The most commonly reported adverse reactions occurring more frequently than with placebo were: somnolence (1.2%), headache (0.6%), increased appetite (0.5%), and insomnia (0.1%). In clinical trials in children aged 2 to 12 years, the following adverse events were observed: headache (2.7%), nervousness (2.3%), and fatigue (1%).

Adverse reactions reported during the post-marketing period are listed below in the table by system organ class. The frequency of adverse reactions was defined as follows: very common (≥ 1/10), common (≥ 1/100 to < 1/10), uncommon (≥ 1/1000 to < 1/100), rare (≥ 1/10,000 to < 1/1000), very rare (< 1/10,000), and frequency not known (cannot be estimated from the available data).

Within each group, adverse reactions are listed in order of decreasing severity.

Shelf life. 3 years.

Shelf life after opening the bottle - 1 month.

Storage conditions.

Store at a temperature not exceeding 25 °C in a place inaccessible to children.

Packaging.

60 ml or 120 ml in a bottle, 1 bottle with a measuring cup in a cardboard box.

Dispensing category. Over-the-counter.

Manufacturer.

Delpharm Montréal Inc. / Delpharm Montréal Inc.

Manufacturer's address and place of business.

3535 Route Trans Canada Highway Pointe-Claire, QC, Canada, H9R 1B4 /
3535 Route Trans Canada Highway Pointe-Claire, QC, Canada, H9R 1B4.