Levocetirizine-Teva (Levocetirizine-Teva)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceLevocetirizineLevocetirizine
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    • Dosage form: & nbspFilm-coated tablets.
    Composition:

    1 tablet contains: active substance: levocetirizine dihydrochloride 5.00 mg; Excipients: microcrystalline cellulose 30.00 mg, lactose monohydrate 63.50 mg, silicon dioxide colloid 0.50 mg, magnesium stearate 1.00 mg; sheath Opadry Y1-7000H white: Macrogol-400 0.1875 mg, titanium dioxide (E171) 0.9375 mg, hypromellose-2910 (E464) 1.875 mg.

    Description:Oval tablets covered with a film coating of white or almost white color.On one side - engraving "LC5". On the cross section, the nucleus is white or almost white in color.
    Pharmacotherapeutic group:H1-histamine receptor antagonist.
    ATX: & nbsp

    R.06.A.E.   Piperazine derivatives

    E.06.A.E.09   Levocetirizine

    Pharmacodynamics:Levocetirizine - cetirizine enantiomer refers to a group of histamine competitive antagonists, blocking the H1-histamine receptors (H1-GR), it has a high level of selectivity for H1-GH. Levocetirizine affects 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 development and facilitates the course of an allergic reaction, has an antiexudative, antipruritic effect, has almost no anticholinergic and antiserotonin action. In therapeutic doses, it practically has no sedative effect, does not change the parameters of the electrocardiogram (ECG), in particular the QT-interval.
    Pharmacokinetics:

    Pharmacokinetic parameters of levocetirizine vary linearly and practically do not differ from the pharmacokinetics of cetirizine.

    Suction. After oral administration levocetirizine quickly absorbed in the gastrointestinal tract. The intake of food does not affect the degree of absorption, although its rate decreases. After a single oral intake at the therapeutic dose, the maximum concentration (Cmax) in blood plasma in adults is achieved after 0.9 hours and is 207 ng / ml, after repeated intake at a dose of 5 mg / day - 308 ng / ml. Bioavailability is 100%.

    Distribution. The equilibrium concentration is achieved after 2 days. The binding of levocetirizine to plasma proteins is 90%. The volume of distribution of the drug is 0.4 l / kg.

    Metabolism. Less than 14% is metabolized in the liver by including oxidation processes of aromatic compounds, N- and O-dealkylation and taurine conjugation. Dealkylation occurs in the presence of an isoenzyme CYP3A4, and numerous and / or unidentified isoenzymes P450 participate in the oxidation of aromatic compounds. Levocetirizine does not affect the activity of isoenzymes CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP2E1 and CYP3A4 in a concentration much higher than Cmax after oral administration of a dose of 5 mg. Because of the low level of metabolism and the lack of a metabolic potential, the interaction of levocetirizine with other drugs is unlikely.

    Excretion. In adults, the half-life (T1/2) is 7.9 ± 1.9 hours, the total clearance is 0.63 ml / min / kg. Completely excreted from the body for 96 hours. About 85.4% of the dose is excreted by the kidneys unchanged through glomerular filtration and tubular secretion; about 12.9% is excreted with feces.

    Pharmacokinetics in special clinical cases. In patients with renal insufficiency (creatinine clearance (CK) less than 40 ml / min), the clearance of levocetirizine decreases, a T1/2 increases (in patients on hemodialysis, the overall clearance is reduced by 80%), which requires a corresponding change in the dosing regimen. Less than 10% of levocetirizine is removed during a standard 4-hour hemodialysis procedure.

    In children of younger age group T1/2 decreases.

    Indications:
    Symptomatic treatment:
    - year-round allergic rhinitis;
    - seasonal allergic rhinitis;
    - chronic idiopathic urticaria.
    Contraindications:Hypersensitivity to levocetirizine and other components of the drug; hypersensitivity to piperazine derivatives; terminal stage of renal failure (CC <> 10 ml / min); lactose intolerance, lactase deficiency, glucose-galactose malabsorption; children's age till 6 years; pregnancy; the period of breastfeeding.
    Carefully:The average and severe degree of renal failure (CC more than 10 ml / min, but less than 50 ml / min); elderly age (probably a decrease in glomerular filtration).
    Pregnancy and lactation:There is insufficient clinical data on the use of levocetirizine in pregnant women, so do not use Levocetirizine-Teva during pregnancy. Levocetirizine excreted in breast milk. If you need to use the drug Levocetirizine-Teva breastfeeding should be discontinued.
    Dosing and Administration:

    Inside, regardless of food intake. Tablets are swallowed, not liquid, squeezed with water. Adults and children over 6 years of age: 5 mg 1 time per day daily.

    The duration of application depends on the duration of the manifestation of the symptoms of the disease.On average, 3-6 weeks are used, in the case of a short-term exposure to an allergen, it may be sufficient to use for 1 week. With prolonged chronic course of the disease, treatment can last up to 6 months.

    Elderly patients: there is no need to adjust the dose.

    Patients with impaired renal function: dose should be adjusted depending on the QC (see table).

    Dose and multiplicity

    Kidney Failure (ml / min)

    admission

    The norm is more than 80 5 mg / day

    Light degree 50-79 5 mg / day

    Average degree 30-49 5 mg / day 1 time in 2 days

    Severe degree less than 30 5 mg / day 1 every 3 days

    Terminal stage (patients,

    less than 10 Admission contraindicated

    who are on hemodialysis)

    The QC is calculated by the formulas:

    for men: body weight (kg) х (140-age (full years)) / 72 x creatinine concentration in blood plasma (mg / dL);

    for women: 0.85 x SC men.

    Patients with hepatic impairment: correction of the dosing regimen is not required.

    Side effects:

    The incidence of side effects is classified according to the recommendations of the World Health Organization: very often - not less than 10%; often - not less than 1%, but less than 10%; infrequently - not less than 0,1%, but less than 1%; rarely - not 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 - migraine, dizziness.

    From the side of the organ of vision: often - visual impairment.

    From the cardiovascular system: very rarely - tachycardia.

    From the respiratory system: very rarely - dyspnoea.

    From the digestive system: often - dryness of the oral mucosa; infrequently - abdominal pain; very rarely - nausea, dyspepsia, diarrhea, changes in functional liver tests, hepatitis.

    From the musculoskeletal system: rarely myalgia.

    From the side of metabolism: rarely - an increase in body weight.

    Allergic reactions: very rarely - skin itching, skin rash, hives, angioedema, anaphylaxis.

    Other: often fatigue, fatigue; infrequently, asthenia.


    Overdose:

    Symptoms: drowsiness (in adults), agitation and anxiety, followed by drowsiness (in children).

    Treatment symptomatic: Immediately after taking the drug, rinse the stomach or induce vomiting. It is recommended to use activated carbon, symptomatic and maintenance therapy.There is no specific antidote. Hemodialysis is ineffective.

    Interaction:
    When studying the drug interaction of levocetirizine with pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, glipizide and diazepam, clinically significant undesirable interaction was not revealed. Simultaneous use with macrolides or ketoconazole did not cause significant changes in the ECG.
    With simultaneous application with theophylline (400 mg / day), the total clearance of cetirizine is reduced by 16%, the pharmacokinetic parameters of theophylline do not change. In some cases, while using levocetirizine with ethanol or drugs that have an inhibitory effect on the central nervous system (CNS), it is possible to increase their effect on the central nervous system, although it is proved that levocetirizine does not enhance the effect of ethanol.
    Special instructions:
    Do not exceed the recommended daily dose.
    The patient should be warned that alcohol consumption during treatment with levocetirizine is not recommended.
    Effect on the ability to drive transp. cf. and fur:The ability to drive vehicles and work with machinery when used, levocetirizine at the recommended dose does not change.However, given that during the treatment of adverse reactions (drowsiness, dizziness) may occur, caution should be exercised during occupations with potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.
    Form release / dosage:
    Tablets, film-coated 5 mg.

    Packaging:
    7 tablets per blister of aluminum laminated foil. 1 or 2 blisters with instructions for use in a pack of cardboard.
    10 tablets per blister of aluminum laminated foil. 1 blister with instructions for use in a pack of cardboard.
    Storage conditions:Store at a temperature not exceeding 25 ° C. Keep out of the reach of children.
    Shelf life:
    3 years. Do not use after the expiry date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:LP-001335
    Date of registration:08.12.2011
    Date of cancellation:2016-12-08
    The owner of the registration certificate:Teva Pharmaceutical Enterprises Co., Ltd.Teva Pharmaceutical Enterprises Co., Ltd. Israel
    Manufacturer: & nbsp
    Representation: & nbspTeva Teva Israel
    Information update date: & nbsp11.10.2015
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