Levocetirizine (Cetirizine-R-enantiomer) is a potent and selective antagonist of peripheral histamine H-receptors1. It inhibits endothelial migration of eosinophils through skin and lung cells. The effect of a dose of levocetirizine equal to half the dose of Cetirizine is comparable to that of Cetirizine, both on the skin and on the nasal mucosa. Levocetirizine relieves symptoms of allergic rhinitis, including nasal congestion. It inhibits the reaction leading to the formation of wheals and redness. Levocetirizine is rapidly and extensively absorbed from the gastrointestinal tract, reaching Cmax during 0.9 h. Steady state is reached after 2 days of use. It is 90% bound to plasma proteins. It is metabolized to a small extent (<14%). T0,5 in adults it is 7.9 ± 1.9 h. Levocetirizine and its metabolites are mainly excreted in the urine - an average of 85.4% of the administered dose. Only 12.9% of the dose is excreted in the faeces.
Contraindications:
Hypersensitivity to levocetirizine, other piperazine derivatives or any of the excipients. Severe renal impairment with creatinine clearance <10 ml / min. Due to the lactose content, do not use in patients with galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose.
Precautions:
Levocetirizine is not recommended for use in infants and children <2 years of age. It is not recommended to administer to children from 2 to 6 years of age, because the available drug form (ret. Table) does not allow the appropriate dose adjustment; it is recommended to use the drug in pharmaceutical forms intended for children. Take special care when consuming alcohol while using the drug.
Pregnancy and lactation:
Animal studies do not indicate any adverse effects of levocetirizine on pregnancy or on the health of the fetus and / or newborn. Caution should be exercised when recommending levocetirizine to pregnant or breast-feeding women.
Side effects:
Common: headache, drowsiness, dry mouth, fatigue. Uncommon: weakness, abdominal pain. Very rare: hypersensitivity (including anaphylactic reaction), aggression, agitation, convulsions, blurred vision, palpitations, shortness of breath, nausea, hepatitis, angioedema, pruritus, persistent drug eruption, rash, urticaria, muscle pain, weight gain, abnormal liver function tests.
Dosage:
Orally. Adults and children> 6 years: 5 mg per day (1 table). In patients with hepatic impairment and in the elderly, no dosage adjustment is necessary. In patients with renal insufficiency, the dosage depends on the creatinine clearance (CCr) - CCr = 50-79 ml / min: 5 mg once a day; CCr = 30-49 ml / min: 5 mg every 2 days; CCr <30 ml / min: 5 mg every 3 days; CCr <10 ml / min - dialysis patients: do not use. In children with impaired renal function, the dose should be determined individually based on the value of renal clearance and body weight; lack of detailed data on the use in children with impaired renal function. The tablet should be taken orally, swallowed whole with liquid. The drug can be taken regardless of the meal.
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