Instructions Loratadine tablets 0.01 g blister No. 20
Composition
active ingredient: loratadine;
1 tablet contains 10 mg of loratadine, calculated as 100% substance (0.01 g);
Excipients: potato starch, lactose monohydrate, povidone, calcium stearate.
Dosage form
Pills.
Main physicochemical properties: round, white tablets with a flat surface, with a bevel and a score or without a score.
Pharmacotherapeutic group
Antihistamines for systemic use. ATX code R06A X13.
Pharmacodynamics
Loratadine is a tricyclic antihistamine with selective activity against peripheral H1 receptors.
In most patients, when used at the recommended dose, loratadine does not have clinically significant sedative and anticholinergic effects. During long-term treatment, no clinically significant changes in vital signs, laboratory tests, physical examination, or electrocardiogram were observed. Loratadine has no significant effect on H2-histamine receptors. The drug does not inhibit norepinephrine uptake and has virtually no effect on cardiovascular function or cardiac pacemaker activity.
Studies with histamine skin tests after a single dose of 10 mg have shown that the antihistamine effect occurs after 1-3 hours, reaches a peak after 8-12 hours and lasts for more than 24 hours. There was no development of tolerance to the drug after 28 days of use of loratadine.
Clinical efficacy and safety.
Over 10,000 patients (aged 12 years and older) have been treated with loratadine (10 mg tablets) in controlled clinical trials. Loratadine (tablets) 10 mg once daily was more effective than placebo and as effective as clemastine in improving symptoms (nasal and non-nasal) of allergic rhinitis. In these trials, somnolence occurred less frequently with loratadine than with clemastine and was about the same as with terfenadine and placebo.
Among the participants in these studies (aged 12 years and older), 1000 patients with chronic idiopathic urticaria were enrolled in placebo-controlled trials. Loratadine 10 mg once daily was more effective than placebo in the treatment of chronic idiopathic urticaria, as evidenced by the reduction of pruritus, erythema, and allergic rash. In these studies, the incidence of somnolence was similar between loratadine and placebo.
Children. Approximately 200 children (aged 6 to 12 years) with seasonal allergic rhinitis received loratadine (syrup) at doses up to 10 mg once daily in controlled clinical trials. 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 in adults.
Pharmacokinetics
Absorption. Loratadine is rapidly and well absorbed. Administration of the drug with food may slightly delay the absorption of loratadine, but this does not affect the clinical effect. The bioavailability of loratadine and its active metabolite is dose-proportional.
Distribution: Loratadine is extensively bound (97% to 99%) to plasma proteins, and its active metabolite is moderately bound (73% to 76%). In healthy volunteers, the plasma half-lives of loratadine and its active metabolite are approximately 1 and 2 hours, respectively.
Biotransformation. After oral administration, loratadine is rapidly and well absorbed and extensively metabolized during the first pass through the liver, mainly by CYP3A4 and CYP2D6. The main metabolite, desloratadine, is pharmacologically active and is largely responsible for the clinical effect. Loratadine and desloratadine reach maximum plasma concentrations (Tmax) 1-1.5 hours and 1.5-3.7 hours, respectively, after administration.
Excretion: Approximately 40% of the dose is excreted in the urine and 42% in the feces within 10 days, mainly as conjugated metabolites. Approximately 27% of the dose is excreted in the urine within the first 24 hours. Less than 1% of the active substance is excreted in unchanged active form - as loratadine or desloratadine. In healthy adult volunteers, the mean elimination half-life of loratadine was 8.4 hours (range 3 to 20 hours) and that of the main active metabolite was 28 hours (range 8.8 to 92 hours).
Hepatic impairment. In patients with chronic alcoholic liver disease, the AUC and Cmax of loratadine were twice as high, and those of its active metabolite were not significantly altered, compared with those in patients with normal liver function. The half-lives of loratadine and its active metabolite are 24 and 37 hours, respectively, and increase with the severity of liver disease.
Elderly patients: The pharmacokinetics of loratadine and its active metabolite were similar in healthy adult volunteers and healthy elderly volunteers.
Indication
Symptomatic treatment of chronic idiopathic urticaria and allergic rhinitis.
Contraindication
The drug is contraindicated in patients with hypersensitivity to the active substance or to any other component of the drug.
Interaction with other medicinal products and other types of interactions
When used simultaneously with alcohol, the effects of loratadine are not enhanced, which is confirmed by studies of psychomotor function.
A potential interaction may occur with all known inhibitors of CYP3A4 or CYP2D6, leading to increased levels of loratadine, which in turn may be the cause of an increased incidence of adverse reactions.
Increased plasma concentrations of loratadine have been reported following concomitant administration with ketoconazole, erythromycin and cimetidine, without clinically significant changes (including ECG).
Children: Drug interaction studies have only been conducted in adult patients.
Application features
Loratadine should be used with caution in patients with severe hepatic impairment.
This medicine contains lactose. Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.
Loratadine should be discontinued at least 48 hours before skin tests, as antihistamines may neutralize or otherwise weaken a positive reaction when determining the skin reactivity index.
Ability to influence reaction speed when driving vehicles or other mechanisms
In general, the drug has no or negligible effect on the reaction speed when driving or operating other mechanisms.
However, the patient should be informed that very rarely cases of drowsiness have been reported, which may affect the ability to drive or use machines.
Use during pregnancy or breastfeeding
Pregnancy: There are very limited data from the use of loratadine in pregnant women. Animal studies do not indicate direct or indirect harmful effects with respect to reproductive toxicity. As a precautionary measure, it is preferable to avoid the use of loratadine during pregnancy.
Breastfeeding: Physicochemical data indicate that loratadine/metabolites are excreted in breast milk. Since a risk to the child cannot be excluded, Loratadine should not be used during breast-feeding.
Fertility: There are no data on the effect of loratadine on female or male fertility.
Method of administration and doses
Oral. Tablets can be taken regardless of meals.
Adults and children over 12 years of age should take 1 tablet (10 mg of loratadine) once a day.
For children aged 2 to 12 years, the dosage depends on body weight. For body weight over 30 kg: 10 mg (1 tablet) once a day. For children weighing less than 30 kg, use loratadine in syrup form.
Elderly patients: No dosage adjustment is required for the elderly.
Patients with hepatic impairment. Patients with severe hepatic impairment should be given a lower starting dose as their clearance of loratadine may be reduced. For adults and children weighing more than 30 kg, the recommended starting dose is 10 mg every other day.
Patients with renal impairment: No dose adjustment is necessary for patients with renal impairment.
Children
The efficacy and safety of loratadine in children under 2 years of age have not been established. Loratadine tablets should be administered to children weighing more than 30 kg.
Overdose
Overdose of loratadine increases the incidence of anticholinergic symptoms. Drowsiness, tachycardia and headache have been reported in overdose. In case of overdose, symptomatic and supportive treatment is recommended for the necessary period of time. Activated charcoal in the form of an aqueous suspension may be used. Gastric lavage may also be performed. Loratadine is not removed from the body by hemodialysis; the effectiveness of peritoneal dialysis in removing the drug is unknown. After emergency care, the patient should remain under medical supervision.
Adverse reactions
Summary of the safety profile. In clinical trials in adults and adolescents, when loratadine was used at the recommended dose of 10 mg daily in indications including allergic rhinitis and chronic idiopathic urticaria, adverse reactions were reported in 2% of patients (which was higher than in patients receiving placebo). Adverse reactions reported 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 reactions were reported: headache (2.7%), nervousness (2.3%) or fatigue (1%).
Immune system disorders: anaphylaxis, including angioedema.
From the nervous system: dizziness, convulsions.
Cardiovascular system: tachycardia, palpitations.
Gastrointestinal: nausea, dry mouth, gastritis.
On the part of the hepatobiliary system: pathological changes in liver function.
Skin and subcutaneous tissue disorders: rash, alopecia.
General disorders and administration-related disorders: fatigue.
Expiration date
4 years.
Do not use the drug after the expiration date indicated on the package.
Storage conditions
Store in the original packaging at a temperature not exceeding 25 ºС.
Keep out of reach of children.
Packaging
10 tablets in a blister. 2 blisters in a pack.
Vacation category
Without a prescription.
Producer
PJSC "Farmak".
Location of the manufacturer and its business address
Ukraine, 04080, Kyiv, Frunze St., 74.
