Ksizal (xyzal)


KSIZAL (Xyzal)
     Synonym : Levotsetirizin, Levocetirizine
     The composition and the form of :
Pill-coated-1 table.
levotsetirizina digidrohlorid 5 mg
support substances : MKTS; lactose Monohydrate; colloidal silicon dioxide; magnesium stearate
shell : polymer (E464), titanium dioxide (E171), macrogol-400
     Description pharmaceutical form : White or almost white oval tablets, coated. On one side pills embossed marking "Y".
     Description : A stable R-enantiomer tsetirizina referring to a group of competitive histamine antagonist.
     The drugs act : Antigistaminnoe, anti.
Lock H1- gistaminovye receptors. Affinity to H1- gistaminovym receptors have levotsetirizina 2 times higher than that of tsetirizina. Has impact on gistaminzavisimuyu phase allergic reactions, reduces migration Eosinophils, vascular permeability, limited release of mediators of inflammation
Warn development and easier for allergic reactions, has protivoekssudativnoe, protivozudnoe, anti-inflammatory, virtually no-antiholinergicheskoe and antiserotoninovoe. In therapeutic doses virtually no sedative effect.
     Pharmacokinetics : Pharmacokinetic parameters levotsetirizina change linearly, and little different from any of tsetirizina. Препарат быстро всасывается при приеме внутрь, прием пищи не влияет на полноту всасывания, но снижает его скорость; биодоступность достигает 100%.
Cmax serum obtained by 0.9 h after a single reception inside and therapeutic dose of 207 ng / ml. The volume of distribution - 0.4 l / kg. Linking plasma proteins - 90%. In small quantities (less than 14%) is metabolized in the liver by O-dealkylation education pharmacologically active metabolite (unlike other H1- gistaminovyh receptor antagonists, which metabolised in the liver by means of tsitohroma).
T1 / 2 at 7-10 h, the total clearance - 0.63 ml / min / kg. Not kumuliruet completely withdrawn from the body for 96 hours In unaltered with urine output 85.4% preparation. Patients who are violating kidney function (Cl creatinine <40 mL / min) d. drug reduced, and T1 / 2 is extended (as in patients in hemodialysis, the total clearance reduced by 80%), which requires dosing regime. Less than 10% levotsetirizina removed during hemodialysis. Penetrates into breast milk.
     Clinical pharmacology : The operation began after 12 min after administration of a single dose of 50% through 0,5-1 hours from 95% and maintained for a period of 24 hours or more.
     Indications : For adults and children over 6 years, and treatment of symptoms of seasonal allergic rhinitis and allergic conjunctivitis (such as sneezing, rinoreya, watering, konyunktivy hyperemia), hay fever (pollinoz), urticaria (including chronic idiopathic, oedema Quincke) and other allergic dermatosis, accompanied by itching of the skin and crust.
     Contraindications : Increased susceptibility to any of the components of a drug or piperazine derivatives, severe chronic renal failure (Cl creatinine <10 mL / min), children under 6 years of age.
With caution, chronic renal failure (requires correction mode dosing), advanced age (perhaps reducing klubochkovoy filtering).
     Application of pregnancy and breast-feeding : Do not assign women during pregnancy and lactation.
     Side effects : Headache, drowsiness, dry mouth, fatigue; Rarely, migraines, dizziness, diarrhoea phenomenon, allergic reactions (angionevrotichesky swelling, rash, urticaria, itch).
     Collaboration : Joint use of macrolides or ketokonazolom not trigger changes in the EKG accurate.
Joint application with teofillinom (400 mg / d) reduced by 16% the total clearance levotsetirizina (kinetics teofillina unchanged).
When used in therapeutic doses does not have data on the interaction with alcohol. Nevertheless, it is necessary to refrain from alcohol.
     Overdosing : The symptoms : drowsiness; Children overdose can be increased irritability and anxiety.
Treatment : If you have symptoms of overdose (especially in children) receiving the drug should be discontinued; Should washed stomach reception activated carbon, symptomatic therapy. There is no specific antidote, hemodialysis is not effective.
     Dosing and Administration : inside, not liquid, food or shock, squeezed a small amount of water.
Adults and children 6 years of age in a daily dose of 5 mg (Table 1). .
Older patients with normal renal function decline dose is not required; In patients with chronic renal insufficiency dose must be calculated taking into account creatinine clearance under the table below.
Kidney function creatinine clearance ml / min dose and multiplicity of the reception
Norma? 80 5 1 mg once a day
Light violation 50-79 5 1 mg once a day
Moderate violation 30-49 5 1 mg every 2 days
Expressed violation of <30 5 1 mg every three days
Terminal Stage
- hemodialysis patients <10 regime installed
Patients with liver failure correction dosing is not required.
The length of treatment depends on the disease : in pollinoze appoint an average of over 1-6 weeks; Chronic diseases (round rhinitis, atopic dermatitis), the duration of treatment could increase to 18 months.
     Special instructions : The objective assessment of the ability to drive a car or work with the arrangements do not reliably identify any unintended consequences of the appointment of the recommended dose of 5 mg nevertheless advisable to refrain from engaging in potentially hazardous activities that require high concentration and psychomotor speed response .
     Shelf life : 3 years
     Storage conditions : dry place at a temperature not exceeding 25 ° C

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