Alerik

INSTRUCTION FOR MEDICAL USE OF THE MEDICINAL PRODUCT ALEK (ALERIC®)

Composition:

Active substance: loratadine;

1 tablet contains 10 mg of loratadine;

Excipients: microcrystalline cellulose, lactose, colloidal anhydrous silicon dioxide, magnesium stearate, crospovidone, pregelatinized starch, stearic acid.

Pharmaceutical form. Tablets.

Main physicochemical properties: white, round, biconvex tablets with a break line on one side, free from spots and defects.

Pharmacotherapeutic group.

Antihistamines for systemic use. ATC code R06AX13.

Pharmacological Properties

Pharmacodynamics

Loratadine is a tricyclic antihistamine with selective activity towards peripheral H1-receptors. Loratadine exerts antiallergic, anti-exudative, and antipruritic effects; reduces capillary permeability, relieves smooth muscle spasm, and prevents tissue edema. Loratadine is a long-acting antihistamine agent for systemic use.

In most patients, loratadine administered at the recommended dose does not produce clinically significant sedative or anticholinergic effects. During prolonged treatment, no clinically significant changes have been observed in vital function parameters, laboratory test results, physical examination findings, or electrocardiograms. Loratadine has no significant effect on H2-histamine receptors. The drug does not inhibit norepinephrine uptake and has virtually no effect on cardiovascular system function or cardiac pacemaker activity. Loratadine also does not potentiate the central nervous system depressant effects of alcohol.

Studies involving skin tests with histamine after a single 10 mg dose showed that the antihistamine effect begins within 1–3 hours, reaches its peak within 8–12 hours, and lasts from 24 to 48 hours. There was no evidence of developing tolerance to the drug after 28 days of loratadine administration.

Pharmacokinetics

Absorption. Loratadine is rapidly and well absorbed. Administration of the drug with food may slightly delay loratadine absorption, but this does not affect the clinical effect. The bioavailability parameters of loratadine and its active metabolite are dose-proportional.

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

In healthy volunteers, the plasma half-life of loratadine and its active metabolite is approximately 1 hour and 2 hours, respectively.

Biotransformation. After oral administration, loratadine is rapidly and well absorbed and extensively metabolized during first-pass metabolism through the liver, primarily via CYP3A4 and CYP2D6 enzymes. The main metabolite, desloratadine, is pharmacologically active and largely responsible for the clinical effect. Loratadine and desloratadine reach maximum plasma concentration (Tmax) at 1–1.5 hours and 1.5–3.7 hours, respectively, after drug administration.

Elimination. Approximately 40% of the dose is excreted in urine and 42% in feces within 10 days, primarily as conjugated metabolites. About 27% of the dose is excreted in urine within the first 24 hours. Less than 1% of the active substance is excreted unchanged and active—either as loratadine or desloratadine. There is no likelihood of drug accumulation, even at doses of 40 mg per day.

In healthy adult volunteers, the mean elimination half-life of loratadine was 8.4 hours (range 3–20 hours), and that of the main active metabolite was 28 hours (range 8.8–92 hours).

Renal impairment. In patients with chronic renal impairment, AUC and maximum plasma concentration (Cmax) values of loratadine and its active metabolite were increased compared to those in patients with normal renal function. The mean elimination half-life of loratadine and its active metabolite did not differ significantly from values in healthy volunteers. In patients with chronic hepatic 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 of loratadine were twice as high, while those of its active metabolite did not change significantly compared to patients with normal liver 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 were similar in healthy adult volunteers and healthy elderly volunteers.

Clinical characteristics.

Indications.

Symptomatic treatment of allergic rhinitis and chronic idiopathic urticaria.

Contraindications.

Hypersensitivity to loratadine or any of the excipients of the medicinal product.

Interaction with other medicinal products and other forms of interaction.

When used concomitantly with alcohol, the effects of the medicinal product Alerik are not enhanced, as confirmed by psychomotor function studies.

Potential interaction may occur when using known inhibitors of CYP3A4 or CYP2D6, leading to increased levels of loratadine, which in turn may increase the frequency of adverse reactions.

In controlled studies, increased plasma concentrations of loratadine have been reported after concomitant administration with ketoconazole, erythromycin, and cimetidine, without clinically significant changes (including on ECG).

Children. Interaction studies with other medicinal products have been conducted only in adult patients.

Special precautions for use.

A lower initial dose should be administered to patients with severe hepatic impairment due to a possible reduction in loratadine clearance (recommended initial dose: 10 mg every other day).

Aleric tablets contain lactose; therefore, the drug must not be administered to patients with rare hereditary galactose intolerance, Lapp lactase deficiency, or glucose-galactose malabsorption. The drug should be discontinued no later than 48 hours before performing skin allergy testing to avoid false-negative results.

Use during pregnancy or breastfeeding.

Extensive data on the use of loratadine in pregnant women (more than 1000 documented cases) do not indicate any congenital or fetal-neonatal toxicity of loratadine. Animal studies have not shown any direct or indirect harmful effects on reproductive function. As a precautionary measure, the use of Aleric during pregnancy is not recommended. Loratadine is excreted in breast milk; therefore, the use of loratadine during breastfeeding is also not recommended.

Ability to influence reaction speed when driving or operating machinery.

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

Dosage and Administration

Orally. Tablets can be taken regardless of food intake.

Adults and children aged 12 years and older: one tablet (10 mg of loratadine) once daily.

For children aged 2 to 12 years, dosage is based on body weight. Children under 12 years of age with body weight above 30 kg: 10 mg (1 tablet) once daily. For children with body weight below 30 kg, another pharmaceutical form of the drug should be used.

Dosage adjustment in elderly patients and patients with renal insufficiency is not required.

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.

Children.

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

The medicinal product should be administered to children with body weight above 30 kg.

Overdose.

Symptoms observed in case of overdose include somnolence, tachycardia, and headache. In case of overdose, symptomatic and supportive treatment is recommended. Standard measures to remove the unabsorbed drug from the stomach are advised: gastric lavage and administration of powdered activated charcoal in water. Loratadine is not removed from the body by hemodialysis; it is also unknown whether loratadine is eliminated by peritoneal dialysis.

After emergency treatment, the patient should remain under medical supervision.

Side effects.

The adverse reactions listed below are classified by organ system classes. Frequency is defined as: very common (≥1/10), common (≥1/100 to <1/10), uncommon (≥1/1,000 to <1/100), rare (≥1/10,000 to <1/1,000), very rare (<1/10,000), and not known (cannot be estimated from the available data).

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

Immune system disorders: very rare – hypersensitivity reactions (including angioedema and anaphylaxis).

Nervous system disorders: very rare – dizziness, convulsions.

Cardiac disorders: very rare – tachycardia, palpitations.

Gastrointestinal disorders: very rare – nausea, dry mouth, gastritis.

Hepatobiliary disorders: very rare – pathological changes in liver function.

Skin and subcutaneous tissue disorders: very rare – rash, alopecia.

General disorders: very rare – fatigue.

Investigations: frequency not known – weight gain.

Shelf life. 3 years.

Storage conditions.

Keep out of reach and sight of children. Store at a temperature not exceeding 25 °C.

Packaging.

7 or 30 tablets in a blister pack, 1 blister pack in a cardboard box.

Pharmaceutical schedule. Over-the-counter (without prescription).

Manufacturer.

TOV US Farmatsiya / US Pharmacia Sp. z o.o.

Manufacturer's address.

ul. Ziebicka 40, 50-507 Wroclaw, Poland.

Marketing authorization holder.

Unilab, LP

Address of the marketing authorization holder.

966 Hungerford Drive, Suite 3B, Rockville, MD 20850, USA.