L-cet (levocetirizine dihydrochloride) syrup 2.5 mg/5 ml. 100 ml. vial

Description

L-cet syrup 100 ml Composition
active substance: levocetirizine dihydrochloride;

5 ml of syrup contains levocetirizine dihydrochloride 2.5 mg;

excipients: glycerin, propylene glycol, purified sodium methyl parahydroxybenzoate (E 219), sodium propyl parahydroxybenzoate (E 217), sucrose, glacial acetic acid, sodium acetate perihydrate, peppermint flavor, banana flavor, purified water.

L-cet syrup 100 ml Dosage form
Syrup.

Basic physical and chemical properties: colorless transparent viscous liquid with a characteristic odor.

L-cet syrup 100 ml Pharmacotherapeutic group
Antihistamines for systemic use. Piperazine derivatives.

ATX code R06A E09.

Pharmacodynamics
Levocetirizine is an active stable R-enantiomer of cetirizine and belongs to the group of competitive histamine antagonists. The pharmacological action is due to the blocking of H1 receptors. The affinity for H1-receptors of levocetirizine is 2 times higher than that of cetirizine. Affects the histamine-dependent stage of the development of an allergic reaction, reduces the migration of eosinophils, vascular permeability, and limits the release of inflammatory mediators. It prevents the development and facilitates the course of allergic reactions, has an antiexudative, antiallergic, anti-inflammatory effect, almost no anticholinergic and antiserotonin effect.

Pharmacokinetics
Pharmacokinetic parameters of levocetirizine have a linear relationship, do not depend on dose and time, and have low variability in different patients. The pharmacokinetic profile with the introduction of a single enantiomer is the same as with the use of cetirizine. No chiral inversion is observed during absorption or withdrawal.

Absorption.

Levocetirizine is rapidly and intensively absorbed after oral administration.

The degree of absorption of the drug does not depend on the dose and does not change with food intake, but the maximum concentration (Cmax) of the drug decreases and reaches its maximum value later. Bioavailability is 100%.

In 50% of patients, the effect of levocetirizine develops within 12 minutes after taking a single dose, and in 95% – after 0.5-1 hours. The maximum concentration (Cmax) in the blood serum is reached 50 minutes after a single oral administration of a therapeutic dose. Equilibrium concentration in the blood is achieved after 2 days of taking the drug. Cmax is 270 ng / ml after a single use and 308 ng / ml after repeated use at a dose of 5 mg, respectively.

Distribution.

There is no information on the distribution of the drug in human tissues, as well as on the penetration of levocetirizine through the blood-brain barrier. In studies, the highest concentration was recorded in the liver and kidneys, and the lowest in the tissues of the central nervous system. The distribution of levocetirizine is limited, since the volume of distribution is 0.4 l / kg. Plasma protein binding – 90%.

Metabolism.

In humans, the metabolic rate is less than 14% of the dose of levocetirizine, and therefore the difference due to genetic polymorphism or concomitant use of enzyme inhibitors is expected to be small. Metabolic processes include aromatic oxidation, N- and O-dealkylation, and taurine binding. Dealkylation primarily occurs with the participation of cytochrome CYP 3A4, while numerous and / or undefined CYP isoforms are involved in the aromatic oxidation process. Levocetirizine did not affect the activity of cytochrome isoenzymes 1A2, 2C9, 2C19, 2D6, 2E1, 3A4 at concentrations that significantly exceeded the maximum after taking a dose of 5 mg orally. Given the low degree of metabolism and the lack of the ability to suppress metabolism, the interaction of levocetirizine with other substances (and vice versa) is unlikely.

Output.

Excretion of the drug occurs mainly due to glomerular filtration and active tubular secretion. The half-life of levocetirizine from blood plasma in adults (T1 / 2) is 7.9 ± 1.9 hours. The half-life is shorter in young children. The average apparent total clearance in adults is 0.63 ml / min / kg. Basically, the excretion of levocetirizine and its metabolites from the body in the urine (an average of 85.4% of the drug dose is excreted). Only 12.9% of the levocetirizine dose is excreted in the feces.

Special populations

Impaired renal function

The apparent body clearance of levocetirizine correlates with creatinine clearance. Therefore, in patients with moderate and severe renal impairment, it is recommended to select the intervals between doses of levocetirizine taking into account creatinine clearance. With anuria at the end-end stage of kidney disease, the total body clearance of patients compared with the total body clearance in persons without such disorders decreases by about 80%. The amount of levocetirizine excreted by a standard 4-hour hemodialysis procedure was <10%.

Indications
Symptomatic treatment of allergic rhinitis (including perennial allergic rhinitis) and urticaria.

Contraindications
Hypersensitivity to levocetirizine, cetirizine, hydroxyzine, any other piperazine derivatives or any other excipient of the drug.

Severe chronic renal failure (creatinine clearance <10 ml / min).