medicalmeds.eu Medicines Antihistaminic drugs for system use. Loratadin

Loratadin

Producer: "Vishpha" Ukraine

Code of automatic telephone exchange: R06A X13

Release form: Liquid dosage forms. Syrup.

Indications to use:

General characteristics. Structure:

Active ingredient: The loratadina of 5 mg contains 5 ml of syrup.
Excipients: propylene glycol, sodium saccharin, glycerin, citric acid monohydrate, sorbite solution which does not crystallize (supports E 420), methylparahydroxybenzoate (Е 216), пропилпарагидроксибензоат (Е 218), Wild Strawberry AKF 434 fragrance (supports E 124, E 122), the water purified.

Transparent siropoobrazny liquid of bright red color with a characteristic smell, sweet-sour taste.

Pharmacological properties:

Pharmacological properties. Loratadin — antihistamine with the selection influence on peripheral _H1-histamine receptors. The antiallergic effect of Loratadin develops for the first 30 min. after administration of drug, reaches a maximum for 8–12 h and 24 h Loratadin lasts and his metabolites do not get through a blood-brain barrier. Drug does not influence TsNS, has no anticholinergic and sedative effect, does not influence the speed of psychomotor reactions.

Loratadin is quickly soaked up from digestive tract. Time of achievement of the maximum concentration of drug in plasma _(Tmax) makes 1–1,3 h, and time of achievement of the maximum concentration of the main metabolite, dezloratadin — about 2,5 h. Meal extends time of achievement _{of Tmax} of Loratadin and a dezloratadin for 1 h. The maximum concentration _(Cmax) of Loratadin and a dezloratadin does not depend on meal. Cmax increases at patients of advanced age with a chronic renal failure or with alcoholic damage of a liver.

Almost in all cases the level of influence of metabolites is higher than the level of influence of initial substance. The defined concentration begin to come to light in a blood plasma in 15 min. after oral administration of drug. At the research in vitro of microsomes of a liver of the person it was revealed that Loratadin is metabolized in дезлоратадин generally under the influence of _{P450 3A4 cytochrome} (CYP3A4) and a smaller measure — _{P450 2D6 cytochrome} (CYP3D6). The period of a semi-conclusion makes 8,4 hours for Loratadin, 28 h — for his metabolites. About 27% of the entered dose are removed with urine for the first days. In the presence of a ketokonazol, inhibitor CYP3A4, Loratadin turns in дезлоратадин, mainly under the influence of CYP3D6. The period of a semi-conclusion increases at alcoholic damage of a liver and does not change in the presence of a chronic renal failure.

Loratadin's pharmacokinetics at children at use of a single dose of 2,5 mg does not differ 1–2 years in age from pharmacokinetics at adults and children 2 years are more senior.

Indications to use:

Seasonal (pollinosis) and year-round allergic rhinitis and allergic conjunctivitis — elimination of the symptoms connected with these diseases such as sneezing, an itch of a mucous membrane of a nose, a rhinorrhea, a burning sensation and an itch in eyes, dacryagogue. Chronic idiopathic small tortoiseshell; skin diseases of an allergic origin.

Route of administration and doses:

Adults and children age of 12 years accept 10 ml (10 mg) of 1 times a day.

Children age from 2 to 12 years: with body weight less than 30 kg — on 5 ml (5 mg), with body weight more than 30 kg — po10 ml (10 mg) of 1 times a day.

To children the age from 1 to 2 years recommends Loratadin's reception in a dose of 2,5 ml (2,5 mg) of 1 times a day.

Treatment duration by drug is determined individually.

Features of use:

At a serious illness of kidneys and a liver Loratadin accept under supervision of the doctor. Patients with a heavy liver failure need a drug dose decline through possible reduction of clearance of Loratadin (the initial dose of 5 mg of 1 times a day or on 10 mg every other day is recommended).

Loratadin does not exponentiate effect of alcohol. Meal does not influence effect of drug.

For 48 h before conducting diagnostic tests (for example, provocative tests with allergens), in order to avoid undesirable results, administration of drug should be stopped.

Use during pregnancy or feeding by a breast. For today there are no reliable data concerning safety of use of Loratadin during pregnancy and feeding by a breast therefore it is possible to use drug during these periods when the advantage of use of drug exceeds potential risk for the fruit/child.

Ability to influence speed of response at control of motor transport or work with other mechanisms. Loratadin has no klinicheskiznachimy sedative effect at use and does not influence ability to manage vehicles or difficult technical mechanisms in the recommended doses (on 10 mg of 1 times a day).

Children. Efficiency and safety of use of Loratadin for children are not finished by age till 1 year. It should be noted that Loratadin's pharmacokinetics at children age from 1 to 2 years at use of a single dose of 2,5 mg does not differ from pharmacokinetics at adults and children in age of 2 years.

Side effects:

Fatigue, headache, drowsiness, dryness in a mouth, gastrointestinal frustration (nausea, gastritis), allergic rash. Possible single cases of an alopecia, anaphylaxis, disturbance of hepatic functions, tachycardias and heart consciousness.

Interaction with other medicines:

At simultaneous use of drug with ketokonazoly, erythromycin, Cimetidinum increase in concentration of Loratadin in a blood plasma which did not exert clinically meaning impact on important functions and indicators of laboratory researches including an ECG was registered.

Contraindications:

Hypersensitivity to drug or other components of drug, the period of pregnancy and feeding by a breast, children's age till 1 year.

Overdose:

At overdose noted drowsiness, tachycardia and a headache. At one-time reception in a dose of 160 mg of any side effects, including changes on the electrocardiogram, it was not revealed.

In case of overdose the symptomatic and supporting treatments are recommended. Standard actions for extraction of the rest of drug from a stomach are recommended: a gastric lavage, the crushed absorbent carbon with water. Loratadin is not brought by a hemodialysis. After acute management the patient has to remain under medical supervision.