Instructions Loratadine tablets 10 mg No. 10
Composition
active ingredient: loratadine;
1 tablet contains loratadine 10 mg;
Excipients: lactose monohydrate; potato starch; calcium stearate.
Dosage form
Pills.
Main physicochemical properties: white or almost white tablets, round in shape with a flat surface, with a bevel.
Pharmacotherapeutic group
Antihistamines for systemic use.
ATX code R06A X13.
Pharmacological properties
Pharmacodynamics
Loratadine is a tricyclic selective blocker of peripheral H1-histamine receptors. When used in the recommended dose, it does not have a clinically significant sedative and anticholinergic effect. During long-term treatment, no clinically significant changes in vital signs, laboratory tests, physical examination data of the patient or in the electrocardiogram were detected. Loratadine has no significant effect on the activity of H2-histamine receptors. It does not block the uptake of norepinephrine and has virtually no effect on the cardiovascular system or on 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 drug resistance after 28 days of use of loratadine.
Clinical efficacy and safety.
Over 10,000 subjects (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 highly 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).
Renal impairment. In patients with chronic renal impairment, the AUC and maximum plasma concentration (Cmax) of loratadine and its active metabolite were increased compared with those in patients with normal renal function. The mean elimination half-life of loratadine and its active metabolite was not significantly different from that in healthy subjects. In patients with chronic hepatic impairment, hemodialysis did not affect the pharmacokinetics of loratadine and its active metabolite.
Elderly patients: The pharmacokinetics of loratadine and its active metabolite were similar in healthy adult volunteers and healthy elderly volunteers.
Indication
Symptomatic treatment of allergic rhinitis and chronic idiopathic urticaria.
Contraindication
Loratadine 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 the drug 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 responsible for an increased incidence of adverse reactions.
Increased plasma concentrations of loratadine have been reported after concomitant use with ketoconazole, erythromycin and cimetidine, which were not accompanied by 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. Therefore, 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 testing, as antihistamines may neutralize or otherwise attenuate a positive skin reactivity index reaction.
Ability to influence reaction speed when driving vehicles or other mechanisms
Loratadine has no or negligible influence on the ability to drive and use machines. However, the patient should be informed that drowsiness has been reported very rarely, which may affect the ability to drive and 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. There is evidence that loratadine/metabolites pass into 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 the drug on female or male fertility.
Method of administration and doses
Method of application.
Oral. Tablets can be taken regardless of meals.
Dosage.
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 the drug in syrup form.
Elderly patients.
No dosage adjustment is required for the elderly.
Patients with impaired liver function.
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.
There is no need for dose adjustment for patients with renal impairment.
Children
The efficacy and safety of the drug in children under 2 years of age have not been established.
The drug in tablet form should be prescribed for body weight over 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
List of adverse reactions: Adverse reactions reported during post-marketing experience are listed below by system organ class. The 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); not known (cannot be estimated from the available data).
Within each frequency grouping, adverse reactions are presented in order of decreasing seriousness.
Immune system disorders: very rarely - anaphylaxis, including angioedema.
From the nervous system: very rarely - dizziness, convulsions.
Cardiac disorders: very rarely – tachycardia, palpitations.
From the digestive tract: very rarely - nausea, dry mouth, gastritis.
On the part of the hepatobiliary system: very rarely - pathological changes in liver function.
Skin and subcutaneous tissue disorders: very rarely – rash, alopecia.
General disorders and administration-related disorders: very rarely - increased fatigue.
Expiration date
5 years.
Storage conditions
Store in the original packaging at a temperature not exceeding 25 ºС.
Packaging
10 tablets in a blister, 1 blister in a pack.
Vacation category
Without a prescription.
Producer
PJSC "Kyivmedpreparat".
Location of the manufacturer and its business address
Ukraine, 01032, Kyiv, Saksaganskoho St., 139.
