Active substanceLevocetirizineLevocetirizine
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  • Dosage form: & nbspdrops for oral administration
    Composition:

    Active substance: levocetirizine dihydrochloride 0.1 g (in 1 ml contains 5 mg of levocetirizine dihydrochloride);

    Excipients: glycerol (85 %) 5 g, propylene glycol 7 g, sodium saccharinate 0.2 g, sodium acetate trihydrate 0.12 g, methyl parahydroxybenzoate 0.027 g, propyl parahydroxybenzoate 0.003 g, acetic acid ice 0.010 g, water purified to 20 ml.

    Description:Colorless or almost colorless liquid without sediment, with a faint smell of acetic acid.
    Pharmacotherapeutic group:Antiallergic agent - H1-histamine receptor blocker
    ATX: & nbsp

    R.06.A.E.   Piperazine derivatives

    E.06.A.E.09   Levocetirizine

    Pharmacodynamics:

    Antiallergic agent. Enantiomer of cetirizine; a competitive histamine antagonist; blocks H1-histamine receptors, affinity for which is 2 times higher than 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 render anticholinergic and antiserotonergic action. In therapeutic doses, it practically does not have a sedative effect.

    The action begins 12 minutes after receiving a single dose in 50% of patients, after 1 hour - in 95 % and lasts for 24 hours.

    Pharmacokinetics:

    Pharmacokinetics is linear.Quickly absorbed when taken orally; food intake does not affect the fullness of absorption, but reduces its speed. Bioavailability is 100%. Time to reach the maximum concentration (TCmax) - 0.9 h, the maximum concentration (Cmah) - 207 ng / ml. The volume of distribution is 0.4 l / kg.

    The connection with plasma proteins is 90%. Less than 14% of the drug is metabolized in the liver by O-dealkylation to form a pharmacologically inactive metabolite. The half-life (T1 / 2) is 7-10 hours. The total clearance is 0.63 ml / min / kg. It is completely eliminated from the body in 96 hours. It is excreted by the kidneys (85.4%). With renal insufficiency (creatinine clearance less than 40 ml / min), clearance decreases (in patients on hemodialysis - by 80%), T1 / 2 - lengthens. Less than 10% is removed during hemodialysis. Penetrates into breast milk.

    Indications:

    Symptomatic treatment of year-round (persistent) and seasonal allergic rhinitis and conjunctivitis (itching, sneezing, rhinorrhea, lacrimation, congestion hyperemia); hay fever (hay fever); urticaria, incl. chronic idiopathic urticaria; edema of Quincke; allergic dermatoses, accompanied by itching and rashes.

    Contraindications:

    Hypersensitivity to the active (including to piperazine derivatives) or any auxiliary component of the drug; severe renal failure (creatinine clearance less than 10 ml / min); children under 2 years of age (due to lack of clinical data); pregnancy and lactation.

    Carefully:

    Chronic renal failure, elderly age (possibly reducing glomerular filtration).

    Pregnancy and lactation:

    The use of the drug in pregnancy is contraindicated, since controlled clinical studies on the safety of the drug in pregnant women have not been conducted. If it is necessary to use the drug in lactation, it is recommended to stop breastfeeding.

    Dosing and Administration:

    For oral administration. The drug should be taken with food or on an empty stomach. The required number of drops should be measured with a dropper in a tablespoon or a glass of water. Drops should be taken orally immediately after dilution. The daily dose is recommended at one time.

    The recommended dose for adults and children over 6 years old, elderly patients (subject to normal kidney function) is 5 mg (1 ml drops or 20 drops from a dropper) per day.The maximum daily dose should not exceed 5 mg.

    Children aged 2 to 6 years - the daily recommended dose is 2.5 mg for two doses in equal doses of 1.25 mg (2 times 0.25 ml drops = 2x5 drops from the dropper). The maximum daily dose should not exceed 2.5 mg.

    Patients with impaired renal function

    The frequency of admission should be set individually according to the function of the kidneys. In patients with chronic renal failure with creatinine clearance (CK) from 30 to 49 ml / min, the dose should be reduced 2 times (5 mg (1 ml drops or 20 drops from a dropper) every other day); with SC from 10 to 29 ml / min dose should be reduced 3 times (5 mg (1 ml drops or 20 drops from the dropper) every 3 days). In severe renal failure (CC less than 10 ml / min), the drug is contraindicated.

    Patients with impaired hepatic function

    When prescribing the drug to patients with an isolated impairment of liver function, no dose changes are required. Patients with combined disorders of the liver and kidneys are recommended dose adjustment (see the section "Patients with impaired renal function" above).

    Duration of the drug

    Duration of admission depends on the disease.

    In the treatment of persistent allergic rhinitis (symptoms <4 days / 1 week or less than 4 weeks), treatment is continued until symptoms disappear; If symptoms appear, treatment can be resumed. In the treatment of seasonal allergic rhinitis (symptoms> 4 days / 1 week or longer than 4 weeks) treatment continues throughout the exposure period of allergens.

    The course of treatment is determined by a doctor, on average, it is 1-6 weeks.

    In chronic diseases (year-round rhinitis, chronic idiopathic urticaria), the course of treatment can be longer in agreement with the doctor. There is a clinical experience of using the drug for up to 6 months.

    Side effects:

    The parameters used below for the frequency of side effects are defined as follows: very often:> 1/10; often: <1/10 and> 1/100; infrequently: <1/100 and> 1/1000; rarely: <1/1000 and> 1/10000; very rarely: <1/10000.

    From the immune system: very rarely - allergic reactions, including anaphylaxis.

    From the side of metabolism: very rarely - weight gain.

    From the central and peripheral nervous system: often - drowsiness, headache, increased fatigue; infrequently - asthenia; rarely - migraine, dizziness.

    On the part of the respiratory system: very rarely - dyspnoea.

    From the gastrointestinal tract: often - dry mouth, infrequently - abdominal pain; very rarely - nausea, indigestion.

    From the subcutaneous fat: very rarely - angioedema, skin itching, rash, urticaria.

    From the laboratory indicators: very rarely - a change in functional "liver" samples.

    If any side effects occur, incl. not specified in the instructions, you need to see a doctor.

    Overdose:

    Symptoms: drowsiness, in children - anxiety, irritability.

    Treatment: gastric lavage, Activated carbon, symptomatic therapy. There is no specific antidote. Hemodialysis is not effective.

    Interaction:

    Studies of the interactions of levocetirizine showed no clinically significant interactions with pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, glipizide, and diazepam. Joint use with macrolides or ketoconazole did not cause significant changes in the ECG.

    Theophylline (400 mg / day) reduces the total clearance of levocetirizine by 16%, while the kinetics of theophylline does not change.

    In sensitive patients, concurrent administration of levocetirizine with alcohol or other agents,oppressive central nervous system, can affect the central nervous system.

    Special instructions:

    Suprastinex in drops is not recommended for children under 2 years due to insufficient data on the use of the drug.

    During treatment it is recommended to refrain from using ethanol.

    Suprastinex® drops can cause allergic reactions (sometimes late), since they contain methyl parahydroxybenzoate and propyl parahydroxybenzoate.

    Effect on the ability to drive transp. cf. and fur:

    During the treatment period it is recommended to refrain from engaging in potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

    Form release / dosage:Drops for ingestion 5 mg / ml.
    Packaging:

    Drops for ingestion 5 mg / ml: 20 ml in a brown glass flask with PE dropper and PP cover with internal PE layer, provided with special protection from opening by children and control of the first opening. 1 bottle is placed in a cardboard box together with instructions for use.

    Storage conditions:

    At a temperature of no higher than 25 ° C. Do not freeze.

    Keep out of the reach of children.

    Shelf life:

    4 years. The open vial should not be stored for more than 6 weeks.Do not use after the expiry date printed on the package.

    Terms of leave from pharmacies:Without recipe
    Registration number:LP-000225
    Date of registration:16.02.2011
    The owner of the registration certificate:EGIS ZAO Pharmaceutical Plant EGIS ZAO Pharmaceutical Plant Hungary
    Manufacturer: & nbsp
    Representation: & nbspEGIS ZAO Pharmaceutical Plant EGIS ZAO Pharmaceutical Plant Hungary
    Information update date: & nbsp29.10.2015
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