Active substanceLevocetirizineLevocetirizine
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  • Dosage form: & nbspfilm-coated tablets
    Composition:

    1 tablet contains: active substance: levocetirizine dihydrochloride 5.0 mg; Excipients: lactose monohydrate - 64.0 mg, microcrystalline cellulose - 30.0 mg, magnesium stearate - 1.0 mg; film sheath: opadray white - 3.0 mg (hypromellose - 1,875 mg, titanium dioxide - 0,9375 mg, macrogol 400 - 0,1876 mg).

    Description:Oval biconvex tablets covered with a film shell, white or almost white with an engraved "L9CZ" on one side and "5" on the other side. On the cross section, the core of the tablet is white or almost white in color.
    Pharmacotherapeutic group:Antiallergic agent-H1 histamine receptor blocker
    ATX: & nbsp

    R.06.A.E.   Piperazine derivatives

    E.06.A.E.09   Levocetirizine

    Pharmacodynamics:

    Levocetirizine is the active substance of the drug Levocetirizine Sandoz®, the levorotatory enantiomer of cetirizine, a competitive histamine antagonist; blocks H1-gistaminovye receptors, affinity for which is twice as high as that of cetirizine. Has an effect on the histamine-dependent stage of allergic reactions; reduces the migration of eosinophils, reduces vascular permeability, limits the release of inflammatory mediators. Prevents development and facilitates the course of allergic reactions, has antiexudative, antipruritic effect; practically does not have anticholinergic and antiserotonin action. In therapeutic doses, it practically does not have a sedative effect.

    The effect of the drug is most pronounced during the first 12 hours after application and lasts for 24 hours.

    Pharmacokinetics:

    Pharmacokinetic parameters of levocetirizine vary linearly. After oral administration, it is quickly and completely absorbed from the gastrointestinal tract (GIT). Eating does not affect the fullness of suction, but reduces its speed. The maximum concentration (CmOh) in the blood plasma is achieved after about 1 hour and is 270 ng / ml after a single dose. The equilibrium concentration is achieved after 2 days. Bioavailability of levocetirizine reaches 100%. Levocetirizine 90% bind to blood plasma proteins, the volume of distribution - 0.4 l / kg. Less than 14% of levocetirizine is metabolized in the liver with the formation of a pharmacologically inactive metabolite.

    The half-life (T1/2) in adults - 7.9 ± 1.9 hours. The total clearance is 0.63 ml / min / kg. 85.4% of the accepted dose of the drug is excreted by the kidneys, 12.9% through the intestine.

    In renal failure (creatinine clearance (CK) less than 40 ml / min), the clearance of levocetirizine decreases. In patients on hemodialysis, the total clearance is reduced by 80%, which requires a corresponding change in the dosing regimen. Less than 10% of levocetirizine is removed during the standard 4-hour hemodialysis procedure.

    Indications:

    - Symptomatic treatment of year-round (persistent) and seasonal (intermittent) allergic rhinitis and allergic conjunctivitis (itching, sneezing, rhinorrhea, nasal congestion, lacrimation, conjunctival hyperemia);

    - hives;

    - Pollinosis (hay fever);

    - other allergic dermatoses, accompanied by itching and rashes.

    Contraindications:

    - Hypersensitivity to levocetirizine, other piperazine derivatives or other components of the drug;

    - deficiency of lactase, lactose intolerance, glucose-galactose malabsorption;

    - terminal stage of renal failure (CK ≤10 ml / min);

    - children under 6 years of age (experience is insufficient);

    - pregnancy;

    - the period of breastfeeding.

    Carefully:In patients with chronic renal failure of moderate to severe severity (dose adjustment is required); in elderly patients (there may be a decrease in glomerular filtration rate); in patients with spinal cord injury, prostatic hyperplasia, and in the presence of other predisposing factors to urinary retention, since levocetirizine may increase the risk of urinary retention; when used with alcohol.
    Pregnancy and lactation:

    Adequate and strictly controlled clinical trials on the safety of the drug in pregnant women have not been carried out, therefore Levocetirizine Sandoz® is contraindicated in pregnancy.

    Because the levocetirizine penetrates into breast milk, if it is necessary to use the drug during lactation it is recommended to abandon breastfeeding.

    Dosing and Administration:

    Inside, swallowing whole, with enough water, regardless of food intake.

    Adults and children over 6 years of age - 5 mg (1 tablet) once a day. Patients with hepatic insufficiency correction of the dose is not required. Patients with chronic renal failure and elderly patients

    - with SC from 50 to 79 ml / min dose adjustment is not required;

    - with QC from 30 to 49 ml / min dose reduced by 2 times (1 tablet every other day);

    - with QC less than 30 ml / min dose reduced by 3 times (1 tablet 1 time in 3 days).

    In the treatment of seasonal (intermittent) rhinitis (the presence of symptoms less than 4 days a week or their total duration is less than4 weeks), the duration of treatment depends on the duration of the symptomatology: treatment may be discontinued if symptoms disappear and are resumed when symptoms appear.

    In the treatment of year-round (persistent) allergic rhinitis (the presence of symptoms more than 4 days a week and their total duration of more than 4 weeks) treatment can continue throughout the exposure period of allergens.

    There is a clinical experience of continuous use of the drug Levocetirizine Sandoz® in adult patients lasting up to 6 months.

    If you miss one dose of the drug, you should not take an additional dose of the drug to compensate for a missed dose, it is recommended that you take the next dose at the usual time.

    Side effects:

    During clinical trials in men and women 12-71 years, most often (≥1 / 100, <1/10), the following side effects occurred: headache, drowsiness, dryness of the oral mucosa, fatigue; infrequently (≥1 / 1000, <1/100) there were asthenia and abdominal pain.

    During clinical trials in children aged 6 to 12 years, most often (≥1 / 100, <1/10) there was a headache and drowsiness.

    During the post-marketing use of the drug, the following side effects were observed, the frequency of which is unknown due to insufficient data:

    From the immune system: hypersensitivity reactions, including anaphylactic shock.

    From the central nervous system: headache, drowsiness, fatigue, seizures, aggression, agitation, tremor, anxiety, insomnia, hallucinations, depression, suicidal thoughts, paresthesia, dizziness, fainting, dysgeusia (dyspnea), thrombosis of the dura mater.

    From the sense organs: impaired vision, vertigo, blurred vision, inflammatory manifestations.

    From the cardiovascular system: heart palpitations, angina pectoris, tachycardia, jugular vein thrombosis.

    From the digestive system: dryness of the oral mucosa, pain in the abdomen, nausea, vomiting.

    From the liver and bile ducts: hepatitis.

    From the urinary system: dysuria, urinary retention.

    From the skin and soft tissues: angioedema, persistent drug erythema, pruritus, rash, hives, hypotrichosis, cracks,photosensitization.

    From the side of the musculoskeletal and connective tissue: muscle pain.

    From the respiratory system: shortness of breath, increased symptoms of rhinitis.

    From the side of metabolism: weight gain.

    Other: asthenia, increased appetite, cross-reactivity, peripheral edema.

    Laboratory indicators: increased activity of "liver" transaminases.

    If any of the side effects listed in the manual are aggravated, or if you notice any other side effects not listed in the instructions, tell your doctor.

    Overdose:

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

    Treatment: there is no specific antidote. Immediately after administration, it is necessary to rinse the stomach or induce vomiting. Symptomatic and maintenance therapy is recommended. Hemodialysis is ineffective.

    Interaction:

    The interaction of levocetirizine with other drugs has not been studied. In the study of the drug interaction of the racemate cetirizine with phenazone, pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, glipizide and diazepam, no clinically relevant undesirable interactions have been identified. Theophylline (400 mg / day) reduces the total clearance of levocetirizine by 16%, while the kinetics of theophylline does not change.

    In the study, while taking ritonavir (600 mg twice daily) and cetirizine (10 mg per day), it was shown that the exposure of cetirizine increased by 40%, and the exposure of ritonavir slightly changed (-11%).

    With the simultaneous use of levocetirizine with alcohol or drugs that have an inhibitory effect on the central nervous system, it is possible to increase their influence on the central nervous system.

    Special instructions:There is no need for special precautions when destroying an unused preparation.
    Effect on the ability to drive transp. cf. and fur:Levocetirizine may lead to increased drowsiness, hence, the drug Levocetirizine Sandoz® can influence the ability to drive a car or work with machinery. During the treatment period, it is necessary to refrain from engaging in potentially dangerous activities that require a high concentration of attention and speed of psychomotor reactions.
    Form release / dosage:
    Tablets, film-coated, 5 mg.
    Packaging:

    For 7 tablets in a blister of PVC / PVDC / A1.

    By 1, 2, 3 or 4 blisters together with instructions for use in cardboard pack.

    For 10 tablets in a blister of PVC / PVDC / A1.

    For 1, 2, 3, 4, 5 or 10 blisters together with instructions for use in a cardboard box.

    Storage conditions:Store at a temperature not exceeding 25 ° C. Keep out of the reach of children.
    Shelf life:2 years. Do not use the product after the expiry date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:LP-002759
    Date of registration:15.12.2014 / 10.09.2015
    Expiration Date:15.12.2019
    The owner of the registration certificate:Sandoz d.Sandoz d. Slovenia
    Manufacturer: & nbsp
    Representation: & nbspSANDOZ SANDOZ Switzerland
    Information update date: & nbsp06.03.2018
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