Levocetirizine | Elcet tablets coated.pl.ob. 5 mg 14 pcs

Release form

Film-coated tablets



packaging 14 tablets

Pharmacological action

Levocetirizine - active substance of the drug Elcet is the R-enantiomer of cetirizine, which belongs to the group of competitive histamine antagonists and blocks H1-histamine receptors. The affinity for H1-histamine receptors in levocetirizine is 2 times higher than in cetirizine.

Levocetirizine has an effect on the histamine-dependent stage of allergic reactions, and also reduces the migration of eosinophils, reduces vascular permeability, limits the release of inflammatory mediators and cytokines (VCAM-1, etc.).

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

Pharmacokinetics

The pharmacokinetic parameters of levocetirizine vary linearly and practically do not differ from the pharmacokinetics of cetirizine.

After oral administration, the drug is rapidly and completely absorbed from the digestive tract. Eating does not affect the completeness of absorption, although its speed decreases. In adults, after a single dose of the drug in a therapeutic dose (5 mg), Cmax in blood plasma is 270 ng / ml and is achieved after 0.9 hours, after repeated administration at a dose of 5 mg - 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 quantities (less than 14%), it is metabolized in the body by N- and O-dealkylation (unlike other antagonists of H1-histamine receptors, which are metabolized in the liver by a system of cytochromes) with the formation of a pharmacologically inactive metabolite. Due to the low level of metabolism and the lack of metabolic potential, the interaction of levocetirizine with other drugs seems unlikely.

In adults, T1 / 2 is (7.9 ± 1, 9) h in young children T1 / 2 is shortened. In adults, the total clearance is 0.63 ml / min / kg. About 85.4% of the accepted dose of the drug is excreted by the kidneys unchanged by glomerular filtration and tubular secretion of about 12.9% through the intestines. In patients with renal failure (Cl creatinine less than 40 ml / min), the clearance of the drug decreases, and T1 / 2 lengthens (for example, in patients on hemodialysis, the overall clearance decreases by 80%), which requires a corresponding change in the dosage regimen. Less than 10% of levocetirizine is removed during the standard 4-hour hemodialysis procedure.

Contraindications

Hypersensitivity to levocetirizine or piperazine derivatives, as well as other components of the

preparation Lactose intolerance, lactase deficiency, glucose-galactose malabsorption, renal failure (CK less than 10 ml / min) and patients , children under 6 years of age (due to lack of data on the effectiveness and safety of the drug).

Precautions

chronic renal failure (dosage adjustment required) older age (possibly reduced glomerular filtration).

Special instructions

It is advisable to refrain from engaging in potentially hazardous activities that require an increased concentration of attention and speed of psychomotor reactions (although no undesirable effects were detected with a recommended dose of 5 mg).

Composition

Active ingredient:

levocetirizine dihydrochloride - 5 mg

:

microcrystalline cellulose,

lactose monohydrate,

Alzen hydrogen phosphate dihydrate, sodium carboxymethyl

,

povidone, magnesium stearate



shell: hypromellose, macrogol 6000 (polyethylene glycol 6000), titanium dioxide.

Dosage and administration

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

Since levocetirizine is excreted by the kidneys, when prescribing the drug to patients with renal failure and elderly patients, the dose should be adjusted depending on the size of creatinine clearance.

Creatinine clearance for men can be calculated based on the concentration of serum creatinine according to the following formula:

KK (ml.min) = (140 - age (years)) * body weight (kg) / 72 * KK (serum) (mg / dl)

Creatinine clearance for women can be calculated multiplying the resulting value by a factor of 0.85.

In elderly patients with normal renal function, a dose reduction is not required in patients with chronic renal failure, dose calculation must be carried out taking into account creatinine clearance according to the table below.

Storage conditions

In a dry, dark place, at a temperature not exceeding 25 РC.

Shelf life

2 years.

active substance

levocetirizine

Terms and conditions

without prescription

Dosage form

tablet

Prescribing

Children over 6 years old, For adults

Indications

Krapivnitsa, Neyrodermit, Allergiya, sensitization rhinitis, diathesis, sensitization konayunktivit, Pollinoz, dermatoses