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 alleviates the symptoms of allergic rhinitis. 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 to any of the excipients. Severe renal dysfunction with creatinine clearance less than 10 ml / min. The drug should not be used in patients with rare hereditary galactose intolerance, lactase deficiency (Lapp type) or malabsorption of glucose-galactose.
Precautions:
Levocetirizine is not recommended for use in infants and children under the age of 2 years. It is not recommended for children 2-6 years of age, because the form of the drug (ret. Table) does not allow the appropriate dose adjustment; it is recommended to use the drug in pharmaceutical forms intended for children. Caution should be used when taking the drug together with alcohol
Pregnancy and lactation:
There are no clinical data on the use of levocetirizine during pregnancy. Animal studies do not indicate harmful effects with respect to pregnancy, embryonal / fetal development, parturition or postnatal development. Caution should be exercised when prescribing to pregnant or breast-feeding women.
Side effects:
Common: headache, drowsiness, dry mouth, fatigue. Uncommon: weakness, abdominal pain. Very rare: hypersensitivity (including anaphylaxis), aggression, agitation, blurred vision, palpitations, shortness of breath, nausea, hepatitis, angioneurotic edema, persistent drug-induced eczema, pruritus, rash, urticaria, muscle pain, weight gain, abnormal results of liver function tests.
Dosage:
Orally. Adults and children from 6 years: the recommended daily dose is 5 mg (1 table). In adult patients with impaired renal function, the intervals between consecutive doses must be determined individually depending on renal function. Light renal impairment - creatinine clearance 50-79 ml / min: 5 mg once a day; moderate renal impairment - creatinine clearance 30-49 ml / min: 5 mg every other day; severe renal impairment - creatinine clearance <30 ml / min: 5 mg every third day; end-stage renal disease - dialysis patients: contraindicated. In children with impaired renal function, the dose should be adjusted individually taking into account the patient's renal clearance and body weight. There are no specific data on the use in children with impaired renal function. In patients with impaired hepatic function and in elderly patients, no dosage adjustment is necessary if the kidneys are normal. Periodic allergic rhinitis (symptoms <4 days in a week or for less than 4 weeks) should be treated according to the course of the disease; treatment can be discontinued immediately after the symptoms have resolved and resumed after re-occurrence. In the case of chronic allergic rhinitis (symptoms> 4 days in a week)and lasting longer than 4 weeks), the patient may be advised to continue treatment during exposure to allergens. Clinical experience in the use of levocetirizine at a dose of 5 mg in the form of powl. includes a 6-month treatment period. Clinical experience with the use of racemate in the treatment of chronic urticaria and chronic allergic rhinitis covers up to 1 year. Table. should be swallowed whole with liquid. The drug can be taken regardless of the meal. It is recommended to take a daily dose once a day.
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