Aleron (levocetirizin) coated tablets 5 mg. №10

Description

Composition of Aleron (levocetirizine)

active substance: levocetirizine;

1 tablet contains:

• levocetirizine dihydrochloride 5 mg;

excipients: corn starch, lactose monohydrate, microcrystalline cellulose, sodium starch glycolate (type A), colloidal anhydrous silicon dioxide, magnesium stearate;

shell: Opadry White 1185 F 18378 (polyvinyl alcohol hydrolyzed, titanium dioxide (E 171), polyethylene glycol 3350, talc).

Pharmacotherapeutic group

Antihistamines for systemic use. Piperazine derivatives. ATX code R06A E09.

Pharmacodynamics

Levocetirizine is an active stable R-enantiomer of cetirizine belonging to the group of competitive histamine antagonists. The pharmacological effect is due to the blocking of H1-histamine receptors. Levocetirizine’s affinity for H1-histamine receptors is 2 times higher than that of cetirizine. It 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. Prevents the development and eases the course of allergic reactions, has an anti-exudative, anti-pruritic, anti-inflammatory effect, practically does not have an anti-cholinergic and anti-serotonin effect.

Pharmacokinetics.

Pharmacokinetic parameters of levocetirizine have a linear dependence and are almost no different from those of cetirizine.

The drug is quickly absorbed when used internally, eating does not affect the degree of absorption, but reduces its speed.

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. The volume of distribution is 0.4 l/kg. Binding to plasma proteins is 90%.

About 14% of levocetirizine is metabolized in the body. Given the low degree of metabolism, the absence of increased inhibitory action, the interaction of levocetirizine with other substances (and vice versa) is unlikely.

Excretion of the drug occurs mainly due to glomerular filtration and active tubular secretion. The elimination half-life (T1/2) is 7.9 + 1.9 hours, the total clearance is 0.63 ml/min/kg. Does not accumulate, is completely removed from the body in 96 hours. 85.4% of the drug dose is excreted unchanged with urine, about 12.9% with feces.

In patients with impaired renal function (creatinine clearance <40 ml/min), the clearance of the drug decreases, and the half-life (T1/2) is prolonged (for example, in patients undergoing hemodialysis, the total clearance decreases by 80%), which requires selection of the appropriate dosage regimen. During a standard 4-hour hemodialysis, a minor part (less than 10%) of levocetirizine is removed. Penetrates into breast milk.

Indication

Symptomatic treatment of allergic rhinitis (including year-round allergic rhinitis) and urticaria.

Contraindications to Aleron (levocetirizine)

Hypersensitivity to levocetirizine, to other piperazine derivatives, as well as to other components of the drug; severe form of chronic renal failure (creatinine clearance < 10 ml/min); rare hereditary galactose intolerance, lactase enzyme deficiency or glucose/galactose malabsorption.