Influences gistaminozavisimuyu step allergic reactions by inhibiting eotaxin facilitate transendothelial migration of eosinophils by blocking the expression of vascular cell adhesion molecule 1, reduces migration of eosinophils, vascular permeability reduces, limits release of inflammatory mediators. It prevents the primobolan acetate development and facilitates the allergic reaction has antiexudativ, antipruritic action, virtually no anticholinergic and antiserotoninovogo action. At therapeutic doses, virtually no sedative action does not alter the parameters of the electrocardiogram (ECG), in particular, QT-interval.
The pharmacokinetic parameters of levocetirizine vary linearly and do not differ from the pharmacokinetics of cetirizine. Absorption. Following oral administration of levocetirizine is rapidly absorbed in the gastrointestinal tract. Food does not affect the extent of absorption, although its speed is reduced. After a single oral therapeutic dose maximum concentration (C max ) in plasma is achieved in adults and 0.9 hours is 207 ng / ml after repeated administration at a dose of 5 mg / day – 308 ng / ml. Bioavailability is 100%. Distribution. The equilibrium concentration is reached after 2 days. Levocetirizine Plasma protein binding is 90%. The volume of distribution of the drug is 0.4 l / kg. Metabolism. Less than 14% is metabolized in the liver by incorporating aromatic oxidation, N- and O-dealkylation and taurine conjugation. The dealkylation occurs in the presence of the isoenzyme CYP3A4, and the oxidation of aromatic compounds involving multiple and / or unidentified P450 isoenzymes. Levocetirizine no effect on the activity of isozymes CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP2E1 and CYP3A4 at concentrations greatly exceeding the C max after oral dose of 5 mg. Due to the low level of metabolism and absence of metabolic potential of the interaction of levocetirizine with other drugs is unlikely. Elimination. In adults, the half-life (T1 / 2)) is 7,9 ± 1,9 h, the total klirens- 0.63 ml / min / kg. Completely eliminated from the body within 96 hours Approximately 85.4% of the dose excreted by the kidneys in unchanged form by glomerular filtration and tubular secretion.; about 12.9% is excreted in the feces.Pharmacokinetics in special clinical situations. In patients with renal impairment (creatinine clearance (CC) of less than 40 ml / min) levocetirizine clearance decreases and T 1/2 is increased (in patients on hemodialysis, total clearance is reduced by 80%), which requires a corresponding change in the dosing regime. Less than 10% of levocetirizine removed during a standard 4-hour dialysis procedure. In children, the youngest age group T 1/2 decreases.
- Hypersensitivity to levocetirizine, and other ingredients; Hypersensitivity to a piperazine derivative; end-stage renal failure (creatinine clearance less than 10 mL / min); lactose intolerance, lactase deficiency, glucose-galactose malabsorption; Children under 6 years of age; pregnancy; during breastfeeding.Be wary
of moderate and severe renal impairment (creatinine clearance greater than 10 mL / min, but less than 50 mL / min); older age (perhaps decreased glomerular filtration).Pregnancy and lactation
Insufficient clinical data on the use of levocetirizine in pregnant women, so you should not use the drug levocetirizine -Teva during pregnancy.
Levocetirizine is excreted in breast milk. If necessary, use of the drug levocetirizine -Teva breastfeeding should be discontinued.
The frequency of side effects is classified according to the recommendations of the World Organization zdravooohraneniya: very often – at least 10%; often – at least 1% but less than 10%; infrequently – at least 0.1% but less than 1%; rare – less than 0.01% but less than 0.1%; very rarely – less than 0.01%, including isolated cases. From the nervous system: often – headache, drowsiness, aggression, agitation, convulsions; rarely – headache, dizziness. From a sight organ: often – blurred vision. Since the cardiovascular system: very rarely – tachycardia. Respiratory system: very rarely – dyspnea. From the digestive system: often – dryness of the oral mucosa ; rare – abdominal pain; very rarely – nausea, dyspepsia, diarrhea, changes in liver function tests, hepatitis. From the musculoskeletal system: rarely – myalgia. On the part of metabolism: rarely – weight gain. Allergic reactions: rarely – itching, skin rash, urticaria, angioedema, anaphylaxis. Other: often – fatigue, primobolan acetate feeling tired; rarely – fatigue.
Overdosing Symptoms: drowsiness (adults), agitation and anxiety, changing sleepiness (in infants). Treatment is symptomatic: immediately after taking the drug to gastric lavage or induce vomiting artificial.It is recommended the use of activated carbon, the holding of symptomatic and supportive therapy. No specific antidote. Hemodialysis is ineffective.
Interaction with other drugs
the study of the drug interaction of levocetirizine with pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, glipizide and diazepam clinically significant adverse interactions have been identified. The simultaneous use of macrolides or ketoconazole did not cause significant changes in the ECG.
In an application with theophylline (400 mg / day), total clearance of cetirizine is reduced by 16%, the pharmacokinetic parameters of theophylline does not change.
In some cases, while the use of levocetirizine with ethanol or drugs , have a depressing effect on the central nervous system (CNS), may enhance their effect on the central nervous system, although it is proved that levocetirizine does not enhance the effect of ethanol.
Do not exceed the recommended daily dose.
Patients should be warned that consumption of alcohol is not recommended during treatment with levocetirizine.
Effects on ability to drive vehicles and management mechanisms
The ability to drive vehicles and operate machinery when used at the recommended dose of levocetirizine is not changed. However, given that the period of treatment may develop side effects (drowsiness, dizziness) care must be taken during the activities potentially hazardous activities that require high concentration and psychomotor primobolan acetate speed reactions.