Loratadine syrup 5mg/5ml 100ml bottle No. 1

Loratadine syrup 5mg/5ml 100ml bottle No. 1

Trade name: Loratadine. International nonproprietary name: Loratadine. Dosage form: syrup 5 mg/5 ml. Composition: 5 ml of solution contains the active ingredient: loratadine - 5 mg; excipients: propylene glycol, sodium benzoate, edible citric acid, edible sorbitol, rectified ethyl alcohol, flavoring additive, purified water.

Description: Transparent, colorless or yellowish liquid with a faint fruity odor. Pharmacotherapeutic group: antihistamines for systemic use. Loratadine. The ATX code is R06AX13.

Indications for use Allergic rhinitis (seasonal and year-round), conjunctivitis, hay fever, urticaria (including chronic idiopathic), angioedema, pruritic dermatosis; pseudo-allergic reactions caused by the release of histamine; allergic reactions to insect bites.

Contraindications Hypersensitivity to the components of the drug, lactation period, children under 2 years of age (due to the presence of alcohol in the composition of the drug).

With caution: Liver failure, pregnancy.

Method of administration and dosage: Orally, at least 1 hour before meals. Adults and children over 12 years of age weighing more than 30 kg - 10 mg 1 time per day (2 teaspoons of syrup). For liver failure, the initial dose is 5 mg once a day. Children aged 2 to 12 years weighing less than 30 kg - 5 mg 1 time per day (1 teaspoon).

Side effects In adults: headache, dizziness, increased fatigue, tachycardia, increased appetite, dry oral mucosa, drowsiness, nausea, gastritis, allergic reactions (rash), anaphylaxis, alopecia, liver dysfunction. In children: headache, increased nervous excitability, sedation.

Interaction with other drugs When used simultaneously with ketoconazole, erythromycin, cimetidine, an increase in the concentration of loratadine in plasma is observed, but without any clinical manifestations, including electrocardiographic ones. Loratadine does not affect the effect of ethanol on the central nervous system.

Special instructions It is recommended to discontinue treatment at least 1 week before performing a skin test for allergens. Pregnancy and lactation The safety of loratadine during pregnancy has not been established, so its use is only possible if the expected benefit to the mother outweighs the potential risk to the fetus. Loratadine is excreted in breast milk, therefore, when prescribing the drug during lactation, the issue of stopping breastfeeding should be considered. Influence on the ability to drive vehicles and operate machinery. During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions due to the risk of drowsiness. In the future, the degree of restriction is determined individually for each patient.

Overdose Symptoms of overdose are associated with the anticholinergic effect of loratadine. In case of overdose, the following are possible: headache, drowsiness, tachycardia. Treatment: gastric lavage, taking activated charcoal, symptomatic and supportive therapy. Hemodialysis is not effective, and there is no information about the effectiveness of peritoneal dialysis.

Storage conditions In a place protected from light, at a temperature of 2 to 30 C. Keep out of the reach of children.

Packaging In bottles of 50 ml or 100 ml, in package No. 1.

Shelf life: 2 years. Do not use after the expiration date.

Conditions for dispensing from pharmacies Without a doctor's prescription.

Loratadine syrup 5mg/5ml 100ml No.1

Name

Loratadine syrup 5 mg 5 ml in 100 ml bottle in pack No. 1

Description

Transparent colorless or yellowish liquid with a faint fruity odor.

Main active ingredient

Loratadine

Release form

syrup

Dosage

5mg

Pharmacological properties

Pharmacodynamics

H1-histamine receptor blocker (long-acting). Suppresses the release of histamine and leukotriene C4 from mast cells. Prevents the development and facilitates the course of allergic reactions. It has antiallergic, antipruritic, antiexudative effects. Reduces capillary permeability, prevents the development of tissue edema. The antiallergic effect develops after 1–3 hours, reaches a maximum after 8–12 hours and lasts 24 hours. It does not affect the central nervous system (CNS) (since it does not penetrate the blood-brain barrier (BBB)) and is not addictive.

Pharmacokinetics

Quickly and completely absorbed from the gastrointestinal tract (GIT). Cmax in elderly people increases by 50%, with alcoholic liver damage - with increasing severity of the disease. Loratadine and its active metabolite desloratadine reach maximum plasma concentrations (Tmax) between 1–1.5 hours and 1.5–3.7 hours after dosing, respectively. Loratadine is 97–99% protein bound, desloratadine to a lesser extent (73–76%). Css of loratadine and metabolite in plasma are achieved on the 5th day of administration. Does not penetrate the blood-brain barrier. Metabolized in the liver to form the main active metabolite desloratadine with the participation of cytochrome isoenzymes CYP3A4 and, to a lesser extent, CYP2D6. Desloratadine is pharmacologically active and makes a significant contribution to the clinical effect. T? loratadine – 3–20 hours (average 8.4), desloratadine – 8.8–92 hours (average 28 hours); in elderly patients, respectively, 6.7–37 hours (average 18.2 hours) and 11–38 hours (17.5 hours). For alcoholic liver damage T? increases in proportion to the severity of the disease. It is excreted by the kidneys (approximately 40% of the dose taken within 10 days after administration) and with bile (approximately 42% of the dose taken in the form of conjugated metabolites within 10 days after administration). Approximately 27% of the dose is eliminated in the first 24 hours after administration. Less than 1% of the dose is excreted as active substances (unconjugated loratadine or desloratadine). In patients with chronic renal failure and during hemodialysis, the pharmacokinetics remain virtually unchanged. Despite the fact that the maximum concentration and AUC of the drug after administration are higher in such people, the half-life and elimination time of loratadine do not change significantly in them. In persons with liver disease and severe liver failure, the maximum concentration of the drug in the blood and its AUC increase by more than 2 times, and the half-life of loratadine and desloratadine increases to 24 and 37 hours, respectively. This should be taken into account when choosing the drug administration regimen. In elderly patients, the pharmacokinetics of loratadine does not change compared to mature patients.

Indications for use

Symptomatic treatment of allergic rhinitis and chronic idiopathic urticaria in adults and children over 2 years of age.

Directions for use and doses

Inside, regardless of food intake. Adults and children over 12 years of age weighing more than 30 kg - 10 mg 1 time per day (corresponding to 10 ml of syrup). Children aged 2 to 12 years weighing less than 30 kg - 5 mg 1 time per day (which corresponds to 5 ml of syrup). Patients with Hepatic Impairment In patients with severe hepatic impairment, the initial dose should be reduced due to the risk of reduced clearance of loratadine. For adults and children weighing more than 30 kg, the recommended initial dose is 10 mg (10 ml syrup) every other day; for children weighing 30 kg or less, a dose of 5 mg (5 ml of syrup) every other day is recommended. Persons with impaired renal function, as well as elderly patients, do not require special dose adjustment.

Use during pregnancy and lactation

The safety of loratadine during pregnancy has not been established, so its use should be avoided. Loratadine is excreted in breast milk, therefore, when prescribing the drug during lactation, the issue of stopping breastfeeding should be considered. There are no data on the effect of loratadine on fertility in women and men.

Precautionary measures

It is recommended to discontinue treatment at least 48 hours before performing a skin test for allergens. The syrup contains a small amount of sodium (less than 1 mmol per syrup dose), so its intake does not require adjustment of dietary salt intake in persons on a low-salt diet. The syrup contains sorbitol and should not be used in patients with rare congenital fructose intolerance. The syrup contains ethyl alcohol in small quantities (less than 100 mg per daily dose).

Interaction with other drugs

When used simultaneously with inhibitors of cytochromes CYP3A4 or CYP2D6, the undesirable effects of loratadine may be enhanced due to an increase in its concentration in the blood. Inhibitors of cytochrome activity such as ketoconazole, erythromycin, cimetidine lead to an increase in the concentration of loratadine in plasma, but without any clinical manifestations, including electrocardiographic ones. Loratadine does not affect the effect of ethanol and does not enhance the effect of sedatives on the central nervous system. Drug interaction studies of loratadine have not been conducted in children.

Contraindications

Hypersensitivity to the active substance or components of the drug, lactation period, children under 2 years of age.

Compound

5 ml of syrup contain the active ingredient: loratadine – 5 mg; excipients: propylene glycol, sodium benzoate E 211, edible citric acid monohydrate, sorbitol E 420, rectified ethyl alcohol, Duchess AN1374 flavoring, purified water.

Overdose

Overdose symptoms are associated with the anticholinergic effects of loratadine. In case of overdose, the following are possible: headache, drowsiness, tachycardia. Treatment: gastric lavage, taking activated charcoal, symptomatic and supportive therapy. Hemodialysis is not effective, and there is no information about the effectiveness of peritoneal dialysis.

Side effect

During clinical studies in adults and adolescents, the most commonly observed symptoms were somnolence (1.2%), headache (0.6%), increased appetite (0.5%), and insomnia (0.1%). After registration, loratadine is very rare (

Storage conditions

In a place protected from light, at a temperature from 2? C to 30? C. Keep out of the reach of children.

Loratadine-Eco

Loratadine is quickly and well absorbed from the gastrointestinal tract. The time to reach the maximum concentration (Tmax) of loratadine in the blood plasma is 1-1.5 hours, and its active metabolite desloratadine is 1.5-3.7 hours. Eating increases the plasma time (Tmax) of loratadine and desloratadine by approximately 1 hour, but does not affect the effectiveness of the drug. The maximum concentration (Cmax) in the blood plasma of loratadine and desloratadine does not depend on food intake. In patients with chronic kidney disease (Cmax) and the area under the concentration-time curve (AUC) of loratadine and its active metabolite are increased compared to those in patients with normal renal function. The half-lives (T1/2) of loratadine and its active metabolite do not differ from those in healthy patients. T1/2 increases with alcoholic liver damage (depending on the severity of the disease) and does not change in the presence of chronic renal failure.

Loratadine has a high degree (97-99%), and its active metabolite has a moderate degree (73-76%) of binding to plasma proteins.

Loratadine is metabolized to desloratadine with the participation of the cytochrome CYP3A4 isoenzyme and, to a lesser extent, the CYP2D6 isoenzyme system. Excreted through the kidneys (approximately 40% of the oral dose) and intestines (approximately 42% of the oral dose) for more than 10 days, mainly in the form of conjugated metabolites. Approximately 27% of an oral dose is excreted through the kidneys within 24 hours after taking the drug. Less than 1% of the active substance is excreted unchanged through the kidneys within 24 hours after taking the drug.

The bioavailability of loratadine and its active metabolite is dose-dependent.

The pharmacokinetic profiles of loratadine and its active metabolite were comparable in adults and elderly healthy volunteers.

The T1/2 period of loratadine ranges from 3 to 20 hours (average 8.4 hours), desloratadine - from 8.8 to 92 hours (average 28 hours); in elderly patients, respectively, from 6.7 to 37 hours (average 18.2 hours) and from 11 to 38 hours (average 17.5 hours). With alcoholic liver damage, the half-life increases in proportion to the severity of the disease and does not change in the presence of chronic renal failure. Hemodialysis in patients with chronic renal failure does not affect the pharmacokinetics of loratadine and its active metabolite.