Elcet, 5 mg 14 pcs

Levocetirizine is the active ingredient of Elcet – it is the R-enantiomer of cetirizine, which belongs to the group of competitive histamine antagonists and blocks H1-histamine receptors. Levocetirizine has 2 times higher affinity for H1-histamine receptors than cetirizine.

Levocetirizine affects histamine-dependent stage of allergic reactions and decreases migration of eosinophils, decreases vascular permeability and limits release of inflammatory mediators and cytokines (VCAM-1 and others).

Levocetirizine prevents and facilitates the development of allergic reactions, has antiexudative, antipruritic action, practically has no anticholinergic and antiserotonin action. In therapeutic doses it has practically no sedative effect.

Pharmacokinetics

The pharmacokinetic parameters of levocetirizine change linearly and are virtually identical to those of cetirizine.

The drug is quickly and completely absorbed from the gastrointestinal tract after oral administration. Food intake does not affect the completeness of absorption, although its rate decreases. In adults, after a single therapeutic dose (5 mg) the Cmax in plasma is 270 ng/ml and is reached after 0.9 h, after re-administration of the drug in 5 mg dose – 308 ng/ml. Css is reached after 2 days.

Levocetirizine is 90% bound to plasma proteins. Vd is 0.4 l/kg. Bioavailability reaches 100%.

In small amounts (less than 14%) it is metabolized in the body by N- and O-dealkylation (unlike other H1-histamine receptor antagonists, which are metabolized in the liver by the cytochrome system) to form a pharmacologically inactive metabolite.

Because of the low metabolism and lack of metabolic potential, interaction of levocetirizine with other drugs seems unlikely.

In adults the T1/2 is (7.9±1.9) h; in young children the T1/2 is shorter. In adults, total clearance is 0.63 ml/min/kg. About 85.4% of the administered dose is excreted unchanged by the kidneys via glomerular filtration and tubular secretion; about 12.9% – via the intestine. In patients with renal insufficiency (creatinine Cl less than 40 ml/min) clearance of the preparation decreases and T1/2 is prolonged (thus, in patients on hemodialysis total clearance decreases by 80%), which requires appropriate change of dosage regimen. Less than 10% of levocetirizine is removed during a standard 4-hour hemodialysis procedure.

Indications

Active ingredient

How to take, the dosage

Enally, without chewing, with food or on an empty stomach, with a small amount of water. Adults and children over 6 years of age – in a daily dose of 5 mg (1 tablet).

Because levocetirizine is excreted by the kidneys, the dose should be adjusted according to creatinine clearance when giving the drug to patients with renal insufficiency and elderly patients.

The creatinine clearance for men can be calculated based on serum creatinine concentration using the following formula:

CK (ml.min) = (140 – age (years)) * body weight (kg) / 72 * CK (serum) (mg/dL)

The creatinine clearance for women can be calculated by multiplying the value obtained by a factor of 0.85.

In elderly patients with normal renal function, no dose reduction is necessary; in patients with chronic renal insufficiency, the dose should be calculated based on creatinine clearance according to the table below.

Special Instructions

It is advisable to refrain from engaging in potentially hazardous activities that require increased concentration and quick psychomotor reactions (although no adverse effects have been identified at the recommended dose of 5 mg).

Contraindications

Hypersensitivity to levocetirizine or piperazine derivatives or other drug components;

Lactose intolerance, lactase deficiency, glucose-galactose malabsorption, renal failure (CK lower than 10 ml/min) and patients on hemodialysis;

Pregnancy and lactation, and children under 6 years of age (due to lack of data on the efficacy and safety of the drug).

With caution

Chronic renal failure (dosing regimen adjustment required); advanced age (decreased glomerular filtration possible).

Similarities