Cetirizine - a metabolite of hydroxyzine, a strong and selective antagonist of peripheral histamine H receptors1. In addition, it has an anti-allergic effect - it inhibits the influx of cells in the late phase of the inflammatory reaction, especially eosinophils, to the skin and conjunctiva. It inhibits the reaction leading to the formation of wheals and redness. It relieves the symptoms of rhinitis and does not affect lung function. Cmax in steady-state blood occurs within +/- 0.5 hours. Cetirizine is approximately 93% bound to plasma proteins. The first pass metabolism is not significantly affected. About 2/3 of the dose is excreted unchanged in the urine. Final T0,5 is about 10 hours and is shorter in children.
Contraindications:
Hypersensitivity to Cetirizine, hydroxyzine, other piperazine derivatives or other components of the preparation. 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:
Use with caution in patients with epilepsy or with the risk of seizures and in patients with moderate or severe renal impairment. Tablets are not recommended for use in children under 6 years of age, as this dosage form does not allow dose adjustment.
Pregnancy and lactation:
Caution should be exercised when using the preparation in pregnant and breast-feeding women. Cetirizine is excreted in human milk at concentrations of 0.25-0.90 plasma concentrations (depending on the time of sampling after administration).
Side effects:
Uncommon: agitation, paresthesia, diarrhea, pruritus, rash, weakness, malaise. Rarely: hypersensitivity reactions, aggressive behavior, confusion, depression, hallucinations, insomnia, convulsions, movement disorders, tachycardia, elevated transaminases, alkaline phosphatase and GGT, increased bilirubin, urticaria, edema, weight gain. Very rare: thrombocytopenia, anaphylactic shock, tics, dysgeusia, syncope, tremor, dystonia, dyskinesia, accommodation disorder, blurred vision, eyeball rotation, angioneurotic edema, drug eruption, painful or difficult urination, involuntary urination. Frequency unknown: amnesia, memory problems. In addition, you may experience: drowsiness, tiredness, pain and dizziness, paradoxical stimulation of the nervous system, dryness of the oral mucosa.
Dosage:
Orally. Adults and children> 12 years: 10 mg once a day. Children 6-12 years: 5 mg twice daily. In patients with hepatic impairment and in the elderly, no dosage adjustment is necessary. In adult patients with impaired renal function, the dosage depends on the creatinine clearance (CCr) - CCr = 50-79 ml / min: 10 mg once a day; CCr = 30-49 ml / min: 5 mg once a day; CCr <30 ml / min: 5 mg every other day; CCr <10 ml / min, dialysis patients: do not use. In children with impaired renal function, the dose should be determined individually based on the creatinine clearance, age and weight of the patient. The tablets should be taken with a glass of water. The tablets can be divided into halves.