L-TSET

General characteristics. Structure:

Active ingredient: levocetirizine dihydrochloride; 5 ml of syrup contain a levotsetirizin of dihydrochloride of 2,5 mg.

Auxiliary вещества:глицерин, propylene glycol, sodium methylparahydroxybenzoate (Е 219), sodium пропилпарагидроксибензоат (Е 217), sucrose, ice acetic acid, sodium acetate trihydrate, flavoring additive of a peppermint, flavoring additive of banana, quinolinic yellow (Е 104), the water purified.

Pharmacological properties:

Levotsetirizin is active stable R-enantiomer of a tsetirizin which concerns to group of competitive antagonists of a histamine. Pharmacological action is caused by blocking of H1-histamine receptors. Likeness to H1-histamine receptors at a levotsetirizin is twice higher, than at a tsetirizin. Influences a gistaminozavisimy stage of allergic reactions, reduces permeability of vessels and migration of eosinophils, limits release of mediators of an inflammation. Prevents development and considerably facilitates the course of allergic reactions, has anti-exudative, antipruritic, antiinflammatory effect, has practically no anticholinergic and antiserotoninovy effect. In therapeutic doses has practically no sedation.

Pharmacokinetic parameters of a levotsetirizin have linear dependence and almost do not differ from those at a tsetirizin.
Absorption. Drug is quickly soaked up at use inside, meal does not influence extent of absorption, but reduces its speed; bioavailability reaches 100%.
At 50% of patients effect of drug develops in 12 min. after reception of a single dose, and at 95% – in 0,5–1 hour. The maximum concentration (Cmax) in serum is reached in 50 min. after one-time intake of a therapeutic dose and keeps for 2 days. Cmax makes 207 ng/ml after single application and 308 ng/ml – after repeated use in a dose of 5 mg respectively.
Distribution. There is no information concerning distribution of drug in tissues of the person, and also concerning penetration of a levotsetirizin through a blood-brain barrier. In researches the biggest concentration is recorded in a liver and kidneys, and the lowest – in tissues of the central nervous system. Distribution volume – 0,4 l/kg. Linkng with proteins of plasma – 90%.

Biotransformation. In a human body about 14% of a levotsetirizin are exposed to metabolism. Process of metabolism includes an oksidation, N-and O-dealkylation and connection with taurine. Dealkylation, first of all, happens with the participation of CYP 3A4 cytochrome while in the course of an oksidation a number of tsitokhromny isoforms is involved. Levotsetirizin does not influence activity of tsitokhromny isoenzymes 1A2, 2C9, 2C19, 2D6, 2E1, 3A4 in concentration which even exceed the doses of 5 mg, maximum after reception, orally. Considering low extent of metabolism, lack of strengthening of the oppressing action, interaction of a levotsetirizin with other substances (and vice versa) it is improbable.

Removal. Excretion of drug occurs generally due to glomerular filtering and active canalicular secretion. The elimination half-life makes 7,9 ± 1,9 hours, the general clearance – 0,63 ml/min. Does not collect, it is completely brought out of an organism in 96 hours. 85,4% of a dose of drug are removed in not changed view with urine, about 12,9% – with excrements.
At patients with renal failures (the clearance of creatinine <40 ml/min.) clearance of drug decreases, and the elimination half-life is extended (so, at patients who are on a hemodialysis the general clearance decreases by 80%), and it demands selection of the corresponding mode of dosing. When carrying out a standard 4-hour hemodialysis an insignificant part (less than 10%) of a levotsetirizin is removed. It is allocated in breast milk.

Indications to use:

- Symptomatic treatment of allergic rhinitises, including year-round allergic rhinitises;
- Chronic idiopathic small tortoiseshell.

Route of administration and doses:

Drug is appointed to adults and children age of 2 years inside, on an empty stomach.
To adults and children 6 years are more senior appoint 5 mg (10 ml of syrup) of 1 times a day. To children age from 2 to 6 years – on 1,25 mg (2,5 ml of syrup) 2 times a day.
Patients of advanced age (on condition of normal function of kidneys) do not have need in a dose decline.
For patients with a chronic renal failure the dose of drug depends on clearance of creatinine. At value of clearance from 30 to 49 ml/min. the dose is reduced twice – 10 ml of syrup every other day; at value of clearance from 10 to 29 ml/min. the dose of drug is reduced by 3 times – 10 ml of syrup once in 3 days. At value of clearance of creatinine less than 10 ml/min. administration of drug is contraindicated. Correction of the mode of dosing is not necessary to patients with a liver failure.
The maximum daily dose – 10 mg (20 ml of syrup).
Duration of treatment depends on a look, weight and displays of a disease: at a pollinosis appoint on average for 3–6 weeks; in case of short-term contact with allergen (pollen of plants) it is enough to use drug for 1 week. At chronic diseases (year-round rhinitis, an idiopathic small tortoiseshell) treatment duration – up to 12 months.

Features of use:

Drug should be accepted regularly at the same time. Drug at some patients serves as the drowsiness reason therefore it is recommended to accept it in the evening.
If the patient forgot to accept drug in certain time, it is necessary to accept it as soon as possible. If there are only several hours before reception of the following dose, it is necessary to pass the previous dose and to accept only a dose which answers the scheme.
With care to apply at a chronic renal failure (correction of the mode of dosing is necessary).
Meal does not influence extent of absorption, but reduces its speed.
As drug contains sucrose, administration of drug is not recommended to patients with hereditary intolerance of fructose, a syndrome of disturbance of absorption of a glucose/galactose and deficit of sucrose/isomaltase.

Use during pregnancy or feeding by a breast. Drug is contraindicated during pregnancy.
During feeding by a breast use of drug needs to be stopped.

Ability to influence the speed of reactions at control of motor transport or work with other mechanisms.
It is necessary to keep from control of motor transport or work with other mechanisms during drug use.

Children. Drug is not used to children age up to 2 years.

Side effects:

- From a nervous system: headache, drowsiness, fatigue, weakness.
- From cardiovascular system: heart consciousness.
- From organs of sight: vision disorder.
- From gepatobiliarny system: hepatitis.
- From immune system: hypersensitivity, including anaphylaxis, Quincke's disease.
- From respiratory system: asthma.
- From the alimentary system: dryness in a mouth, nausea.
- From skin and hypodermic cellulose: itch, rashes, urticaria.
- Others: increase in body weight, an abdominal pain, a myalgia, can change indicators of hepatic tests.

Interaction with other medicines:

Simultaneous use of drug with pseudoephedrine, Cimetidinum, ketokonazoly, erythromycin, azithromycin, glipezidy or diazepam does not render clinically significant adverse interactions. Combined use with theophylline (400 mg/days) reduces the general clearance of a levotsetirizin by 16% (the kinetics of theophylline does not change). At use in therapeutic doses there are no data on strengthening of effect of demulcents, however it is desirable to refrain from use of sedatives during performing therapy.

Contraindications:

Hypersensitivity to a levotsetirizin, a tsetirizin or its primary connection – a hydrazine. Severe form of a chronic renal failure (clearance of creatinine <10 ml/min.).

Overdose:

At overdose strengthening of side effect of drug is possible.
Symptoms: adults have a drowsiness, children have a mental and motive excitement which is replaced by drowsiness.
Treatment: the symptomatic and supported therapy, a gastric lavage. The specific antidote to a levotsetirizin does not exist. The hemodialysis is not effective.

Storage conditions:

To store at a temperature not above 25 °C, in dry, protected from light and the place, unavailable to children.
After the first opening of a bottle to store drug no more than 4 weeks.

Issue conditions:

Without recipe

Packaging:

On 10 tablets in the blister; on 1 or 3 blisters in cardboard packaging.