The instruction for medical use of Allerway Torgovoye medicine a name of Allerway the International unlicensed name Levotsetirizin Lekarstvennaya the Tablet form, film coated, 5 mg Structure One tablet contains active agent – a levotsetirizin of dihydrochloride of 5 mg, excipients: lactoses of monohydrate (Flowlac 100), cellulose microcrystalline (Avicel PH 102), silicon dioxide colloidal, magnesium stearate Structure of a cover – Opadry white OY-58900 the Description of the Tablet, oval form, with a biconvex surface coated white color with an engraving of R 5 on one party. Pharmacotherapeutic group Antihistaminic drugs of systemic action. Piperazin derivatives. Levotsetirizin. The ATX R06AE09 code the Pharmacological Pharmacokinetics Pharmacokinetic Parameters properties of a levotsetirizin change linearly and practically do not differ from pharmacokinetics of a tsetirizin. Absorption After intake drug is quickly and completely absorbed from digestive tract. Meal does not affect completeness of absorption though its speed decreases. At adults, after single dose of drug in a therapeutic dose (5 mg), the maximum concentration (Cmax) in blood plasma is reached in 0.9 h and makes 270 ng/ml, after repeated reception in a dose of 5 mg/days – 308 ng/ml. Constant level of concentration is reached in 2 days. Levotsetirizin’s distribution to 90% contacts proteins of blood plasma. The volume of distribution (Vd) is 0.4 l/kg. The bioavailability reaches 100%. Metabolism In small amounts (& lt, 14%) is metabolized in an organism by N- and O-dealkylation (unlike other antagonists of H1-histamine receptors which are metabolized in a liver by means of the system of cytochromes) with formation pharmacological of an inactive metabolite. Dealkylation first of all is mediated with CYP 3A4, during aromatic oxidation the numerous and/or unknown CYP isoforms participate. Levotsetirizin does not influence activity of isoenzymes of CYP 1A2, 2S9, 2S19, 2D6, 2E1 and 3A4 in the concentration considerably exceeding the peak of the concentration reached at reception of 5 mg of a dose. Because of the low metabolic rate and lack of metabolic potential the interaction of a levotsetirizin with other medicines is represented improbable. Removal At adults elimination half-life (T1/2) makes 8 ± 2 h, at small children of T1/2 is shortened. At adults the general clearance is 0.63 ml/min. About 85.4% of the accepted dose of drug are removed by kidneys in not changed look by glomerular filtration and canalicular secretion, about 12.9% – through intestines. At patients with a renal failure (the clearance of creatinine (CC) & lt, 40 ml/min.) the clearance of drug decreases, and T1/2 is extended (so, at the patients who are on a hemodialysis, the general clearance decreases by 80%) that demands corresponding change of the mode of dosing. Less than 10% of a levotsetirizin are removed during the standard 4-hour procedure of a hemodialysis. The pharmacodynamics Active agent of drug – levotsetirizin, R-enantiomer of a tsetirizin, belongs to group of competitive antagonists of a histamine, blocks N1-histamine receptors. The affinity to H1 receptors at a levotsetirizin is twice higher, than at a tsetirizin. Levotsetirizin influences a gistaminozavisimy stage of allergic reactions and also reduces migration of eosinophils, reduces vascular permeability, limits release of mediators of inflammation. Levotsetirizin prevents development and facilitates a course of allergic reactions, possesses antiexudative, antipruritic action, has practically no anticholinergic and antiserotoninovy effect. In therapeutic doses practically does not render sedation. Effect of drug begins in 12 min. after reception of a single dose at 50% of patients, in 1 hour – at 95% and remains within 24 hours. Indications – symptomatic treatment of allergic rhinitis (including persistent allergic rhinitis) both small tortoiseshells the Route of administration and doses Is applied inside with food or on an empty stomach, washing down with a small amount of water, not chewing. Children aged from 6 up to 12 years the Recommended day dose makes 5 mg (1 film coated tablet). Teenagers of 12 years are also more senior and adults the Recommended day dose makes 5 mg (1 film coated tablet). Elderly patients Correction of a dose is recommended to elderly patients with a moderate and heavy renal failure (see. Adult patients with a renal failure below). Adult patients with a renal failure Intervals of dosing have to be individualized depending on function of kidneys. Address the following table and correct a dose, as shown below. To use this table of dosing, assessment of clearance of creatinine of the patient (KK) in ml/min. of KK (ml/min.) it is required it can be estimated on creatinine of the serum (mg/dl) determined by the following formula: KK = [140 – age (years)] x the weight (kg) (x 0.85 for women) 72 x creatinine of serum (mg/dl) Correction of dosing for patients with a renal failure: The Clearance of Creatinine group (ml/min.) the Dosage and frequency Normal ≥80 5 mg once a day of Insignificant 50 – 79 5 mg once a day Moderated 30 – 49 5 mg once in 2 days Heavy & lt, 30 5 mg once in 3 days the End-stage of a renal failure – patients on dialysis & lt, 10 Are available contraindications the Children having a renal failure the Dose has to be corrected on an individual basis taking into account renal clearance of the patient and his / her body weight. Patients with a liver failure the Dose adjustment is not required to patients only with a liver failure. Regulation of a dose is recommended to patients with a liver and renal failure (see. Adult patients with a renal failure above). Use duration Periodic allergic rhinitis (symptoms & lt, 4 days/week or less than 4 weeks) has to be considered depending on a disease and its history, reception can be stopped only after disappearance of symptoms, and it can be renewed again when symptoms appear. In case of persistent allergic rhinitis (симптомы>, 4 days/week and within more than 4 weeks) continuous therapy can be offered the patient during contact with allergens. There is a clinical experience of use from 5 mg of a levotsetirizin in the form of tablets with a film cover with the 6th monthly period of treatment. For a chronic small tortoiseshell and chronic allergic rhinitis there is a clinical experience of use of a racemate up to one year. Side effects At children at the age of 6 – 12 years: – a headache, drowsiness At teenagers of 12 years and adults: – a headache, drowsiness, dryness in a mouth, fatigue Post-marketing experience: – the hypersensitivity, including an anaphylaxis, a Quincke’s disease, rash, an itching, a small tortoiseshell – increase in appetite, nausea, vomiting – aggression, excitement, hallucinations, a depression, insomnia, suicide thoughts, spasms, paresthesias, dizziness, a faint, a tremor, a dysgeusia, a disorder of vision, the obscured sight – heartbeat, tachycardia – short wind – hepatitis – a dysuria, an ischuria – muscle pain – hypostasis – increase in weight, the Contraindication abnormal liver function – hypersensitivity to derivatives of piperazin or any of drug components – a severe form of chronic kidney disease (KK less than 10 ml/min.) – children’s age up to 6 years – pregnancy and the period of a lactation Medicinal interactions These researches of interaction with levotsetiriziny (including researches with the inductors CYP3A4) are absent, researches of connection of a tsetirizin with a racemate did not show any clinically significant adverse interactions (with antipyrine, pseudoephedrine, Cimetidinum, ketokonazoly, erythromycin, azithromycin, glipizidy and diazepam). Small decrease in clearance of a tsetirizin (16%) was observed in a research with several doses of theophylline (400 mg once a day) while the arrangement of theophylline does not change at simultaneous use of a tsetirizin. At simultaneous use of a ritonavir (600 mg twice a day) and a tsetirizina (10 mg a day), extent of influence of a tsetirizin was increased approximately by 40%, and the arrangement of a ritonavir was slightly changed (-11%) that accompanied further absorption of a tsetirizin. Extent of absorption of a levotsetirizin does not decrease with meal though the speed of absorption decreases. Sensitive patients have a simultaneous use of a tsetirizin or levotsetirizin and alcohol or other depressants of central nervous system can have effect on the central nervous system though it was shown that the racemate of a tsetirizin does not strengthen effect of alcohol. Special instructions Patients with chronic kidney disease and patients of advanced age with a moderate and heavy renal failure: Correction of the mode of dosing is required (see the Route of administration and doses Adult patients with a renal failure). To patients with the contributing factors of an ischuria to accept with extra care (for example, defeat of a chord of a spinal cord, a prostate hyperplasia) as levotsetirizin can increase risk of development of an ischuria. Due to presence of lactose, patients with rare hereditary intolerance of a galactose, deficiency of Lappa lactase or glyukozo-galaktozny malabsorption, should not take this drug. Features of influence of medicine on ability to run the vehicle or potentially dangerous mechanisms At objective assessment of ability to driving of the car and work with mechanisms any undesirable phenomena are authentically not revealed when assigning of the recommended dose of 5 mg. Nevertheless, it is reasonable to abstain from the occupations potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions. Overdose Symptoms: symptoms of intoxication in the form of drowsiness, children have a concern and acrimony. Treatment: at emergence of symptoms of overdose (especially at children) administration of drug should be stopped, gastric lavage, intake of activated carbon, symptomatic therapy is necessary. There is no specific antidote. The hemodialysis is not effective. The form of release and packing On 10 tablets pack into blister strip packaging from aluminum foil. On 1 or 3 planimetric packs together with the instruction for medical use in the state and Russian languages place in a cardboard pack. Storage conditions In the dry place protected from light at a temperature not above 25 °C. To store out of children’s reach! A period of storage 2 years not to accept after an expiration date Prescription status from drugstore According to the prescription the Dr. Producer. Reddi’s Laboratoris Limited, India Owner of the registration certificate Dr. Reddi’s Laboratoris Limited, India the Address of the organization taking in the territory of the Republic of Kazakhstan claims from consumers on quality of products and for post-registration observation of safety medicinal a sredstvapredstavitelstvo of the Dr. of Reddi’s Laboratoris Limited company in the Republic of Kazakhstan: 050057 Almaty, 22nd Line St., 45
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