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 occurs after 2 days of use. Levocetirizine is 90% bound to plasma proteins. It is slightly metabolised (<14% of the administered dose). 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 impairment in patients with a creatinine clearance less than 10 ml / min.
Precautions:
Levocetirizine is not recommended for use in infants and children up to 2 years of age (no data available). The preparation is not recommended in the form of tablets. powl. children between 2 and 6 years of age, as dose adjustment is not possible; it is recommended to use levocetirizine in pharmaceutical forms intended for children. Caution should be used when taking the drug together with alcohol. Caution should be exercised in patients with predisposing factors for urinary retention (eg spinal cord injury, prostatic hyperplasia) as levocetirizine may increase the risk of urinary retention. The drug contains lactose - should not be used in patients with rare hereditary galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose.
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 women. It is not known whether levocetirizine is excreted in human milk. A decision should be made to discontinue breast-feeding or to discontinue the medicine, taking into account the benefits of natural feeding as well as the benefits of treatment for the mother.
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. Mild 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 the 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 with or without food. It is recommended to take the dose once a day.