Ksizal pills coated 5 mg N14
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Active ingredients
Levocetirizine
Release form
Pills
Composition
Levocetirizine dihydrochloride 5 mg. Auxiliary substances: lactose monohydrate, microcrystalline cellulose, colloidal silicon dioxide, magnesium stearate. The composition of the shell: opadry Y-1-7000 (hypromellose, titanium dioxide (E171), macrogol 400).
Pharmacological effect
The histamine H1 receptor blocker, cetirizine enantiomer, belongs to the group of competitive histamine antagonists. The affinity for histamine H1 receptors in levocetirizine is 2 times higher than that of cetirizine. Levocetirizine affects the histamine-dependent stage of allergic reactions, and also reduces the migration of eosinophils, reduces vascular permeability, limits the release of inflammatory mediators. It prevents the development and facilitates the course of allergic reactions, has anti-exudative, antipruritic action, practically does not have anticholinergic and antiserotonin action. In therapeutic doses, almost no sedative effect.
Pharmacokinetics
Absorption The pharmacokinetic parameters of levocetirizine vary linearly and are practically the same as cetirizine pharmacokinetics. After oral administration, levocetosirzine is rapidly absorbed from the gastrointestinal tract. Meal does not affect the degree of absorption, although its rate decreases. After a single ingestion in a therapeutic dose of Cmax in adults, plasma is reached after 0.9 h and is 207 ng / ml, after repeated administration at a dose of 5 mg / day - 308 ng / ml. Bioavailability is 100%. The distribution of Css is achieved in 2 days. The binding of levocetirizine to plasma proteins is 90%. Vd is 0.4 l / kg. Metabolism Less than 14% is metabolized in the liver by N- and O-dealkylation (unlike other histamine H1-receptor blockers that are metabolized in the liver with the participation of cytochrome P450 isoenzymes) with the formation of a pharmacologically inactive metabolite. Due to the low level of metabolism and the lack of metabolic potential, the interaction of levocetirizine with other drugs seems unlikely. Intake of adults is 7.9 ± 1.9 h, the total clearance is 0.63 ml / min / kg. About 85.4% of the dose is excreted by the kidneys unchanged by glomerular filtration and tubular secretion; about 12.9% is output throughintestine. Pharmacokinetus in special clinical situations In patients with renal insufficiency (CC less than 40 ml / min), the clearance of levocetirizine decreases, and T1 / 2 increases (in patients undergoing hemodialysis, the total clearance decreases by 80%), which requires a corresponding change in the dosage regimen . Less than 10% of levocetirizine is removed during a standard 4-hour hemodialysis procedure. In young children, T1 / 2 is shortened.
Indications
Symptomatic therapy of allergic diseases and conditions: - year-round (persistent) and seasonal (intermittent) allergic rhinitis and allergic conjunctivitis (itching, sneezing, rhinorrhea, tearing, conjunctival hyperemia, nasal congestion); - pollinosis, hay fever; . Chronic idiopathic urticaria); - Quincke edema; - Other allergic dermatosis, accompanied by itching and rash.
Contraindications
- terminal stage of renal failure (QC less than 10 ml / min); - children's age up to 6 years (for pills); - children's age up to 2 years (for drops for oral administration); - pregnancy; - hypersensitivity to the components of the drug, especially in patients with galactosemia or severe lactose intolerance (for pills); - hypersensitivity to levocetirizine or piperazine derivatives. The drug should be used with caution in chronic renal failure (correction of the dosage regimen is required), in patients residential age (age under reducing glomerular filtration).
Precautionary measures
Use in patients with impaired liver functionPatients with hepatic insufficiency do not require dose adjustment. Use when impaired renal function is contraindicated in the terminal stage of renal failure (CC less than 10 ml / min). For patients with chronic renal insufficiency with CK 49-30 ml / min, the dose is reduced 2 times (1 tab. every other day), with CK 29-10 ml / min, the dose is reduced by 3 times (1 tab. 1 time in 3 days). The use in children is contraindicated in children under 6 years of age (for pills); at children's age till 2 years (for drops for intake). Children over 6 years: daily dose of 5 mg (1 tab. or 20 drops). Children aged from 2 to 6 years: on 1.25 mg (5 drops) 2 times / day; daily dose - 2.5 mg (10 drops). Use in elderly patients Since levocetirizine is eliminated by the kidneys, when prescribing the drug in elderly patients, the dose should be adjusted depending on the CC value.
Use during pregnancy and lactation
Adequate and strictly controlled clinical studies on the safety of the drug in pregnant women have not been conducted, therefore, Xyzal; Levocetirizine is excreted in breast milk, so if you need to use the drug during lactation, breastfeeding at the time of admission should be discontinued. In experimental studies on animals, no direct or indirect adverse effects of levocetirizine on the developing fetus ( during the postnatal period), the course of pregnancy and childbirth also did not change.
Dosage and administration
The drug is administered orally during a meal or on an empty stomach. Tablets are taken with a small amount of water, without chewing. Drops for ingestion are taken with a teaspoon. If necessary, the dose of the drug can be diluted in a small amount of water immediately before use. Adults and children over 6 years old: daily dose of 5 mg (1 tab. Or 20 drops). Children aged 2 to 6 years: 1.25 mg (5 drops) 2 times / day; the daily dose is 2.5 mg (10 drops). Since levocetirizine is eliminated by the kidneys, when prescribing the drug to elderly patients and patients with renal insufficiency, the dose should be adjusted depending on the CK.KK value, using the following formula. men: QC (ml / min) = [140-age (years)] × body weight (kg) / 72 × serum creatinine (mg / dL) For women: obtained value × 0.85RCC failure (ml / min) Dose and frequency of administrationNorma> 80 5 mg / dayEasy degree 50-79 5 mg / daySre Negative degree 30-49 5 mg / day 1 time in 2 days Severe <30 5 mg / day 1 time in 3 days Terminal stage (patients on hemodialysis) <10 The drug is contraindicated above. For patients with impaired liver function only, a dosage regimen adjustment is not required. Duration of use depends on the indication. The course of treatment of pollinosis averages 1-6 weeks. In chronic diseases (year-round rhinitis, atopic dermatitis), the duration of treatment may increase up to 18 months.
Side effects
Possible side effects are listed below for body systems and frequency of occurrence: often (≥1 / 10); infrequently (from ≥1 / 100 to <1/10); rarely (from ≥1 / 1000 to <1/100); very rarely (from ≥1 / 10 000 to <1/1000). On the CNS side: infrequently - headache, fatigue, drowsiness; rarely - asthenia; very rarely - aggression, agitation, convulsions, hallucinations, depression, blurred vision. From the side of the cardiovascular system: very rarely - tachycardia. From the respiratory system: very rarely - to dyspnea. From the digestive system: not often - dry mouth; rarely - abdominal pain; very rarely - nausea, diarrhea, hepatitis, altered functional liver samples. From the musculoskeletal system: very rarely - myalgia. From the metabolic side: very rarely - weight gain. Allergic reactions: very rarely - itching, rash, urticaria, angioedema, anaphylaxis.
Overdose
Symptoms: drowsiness (in adults), agitation and anxiety, alternating with drowsiness (in children). Treatment: immediately after taking the drug, wash the stomach or induce artificial vomiting. It is recommended the appointment of activated carbon, conducting symptomatic and supportive therapy. There is no specific antidote. Hemodialysis is ineffective.
Interaction with other drugs
The study of the interaction of levocetirizine with other drugs was not carried out. When studying the drug interaction of the racemate cetirizine with pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, glipizide and diazepam, we did not reveal any clinically significant undesirable interaction. cetirizine is reduced by 16%, theophylline pharmacokinetic parameters do not change. In some cases, the simultaneous use of levocetirizine with ethane scrap or drugs, have a depressing effect on the CNS, may enhance their effect on the central nervous system, although it is proved that the racemate cetirizine potentiate the effect of alcohol.
special instructions
The patient should be careful when taking the drug and the simultaneous use of alcohol. The effect on the ability to drive vehicles and control mechanisms. At an objective assessment of the ability to drive vehicles and work with mechanisms, no adverse events were clearly observed when prescribing the drug at the recommended dose.However, during the period of treatment, it is advisable to refrain from engaging in potentially hazardous activities that require increased concentration and psychomotor speed.