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 levocetirizine at a dose equal to half the dose of Cetirizine is comparable to that of Cetirizine, both on the skin and on the nasal mucosa. 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. 12.9% of the dose is excreted in the faeces.
Contraindications:
Hypersensitivity to the active substance, other piperazine derivatives or any of the excipients. Patients with severe renal impairment with a creatinine clearance less than 10 ml / min. Due to the lactose content, the preparation should not be used in patients with galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose.
Precautions:
Use with caution when taking with alcohol. In children from 2 to 6 years, the use of levocetirizine in the form of film-coated tablets is not recommended due to the inability to properly dose the drug. The use of levocetirizine in infants and children under 2 years is not recommended. Caution should be exercised in patients at risk of urinary retention (eg spinal cord injury, prostatic hyperplasia), because levocetirizine may increase the risk of urinary retention.
Pregnancy and lactation:
Caution should be exercised when using the drug in pregnant or breast-feeding women, due to the lack of clinical data.
Side effects:
Common: headaches, drowsiness, dry mouth, fatigue. Uncommon: weakness, abdominal pain. Not known: hypersensitivity (including anaphylactic reaction), increased appetite, aggression, agitation, hallucinations, depression, insomnia, suicidal thoughts, convulsions, paresthesia, dizziness, fainting, tremor, disturbed taste, blurred vision, blurred vision, dizziness ( of labyrinth origin), palpitations, tachycardia, shortness of breath, nausea, vomiting, hepatitis, angioneurotic edema, persistent drug eczema, pruritus, rash, urticaria, muscle pain, painful or difficult urination, urinary retention, edema, weight gain, abnormal results of liver function tests.
Dosage:
Orally. Adults and children> 6 years: 5 mg per day (1 table). Patients with impaired renal function: mild renal impairment (creatinine clearance 50-79 ml / min): 5 mg (1 tablet) once a day, moderate renal impairment (creatinine clearance 30-49 ml / min): 5 mg ( 1 tablet) every 2 days, severe renal dysfunction (creatinine clearance <30 ml / min): 5 mg (1 tablet) every 3 days. No dosage adjustment is necessary for patients with hepatic impairment. In periodic allergic rhinitis (symptoms <4 days in a week or lasting less than 4 weeks), the treatment may be discontinued immediately after the symptoms have resolved and resumed after their recurrence. In chronic allergic rhinitis (symptoms> 4 days in the week and lasting longer than 4 weeks) you can continue treatment during the exposure to allergens. The tablet should be swallowed whole with liquid; take regardless of the meal.
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