Active substanceCetirizineCetirizine
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  • Dosage form: & nbspTfilm-covered abeys.
    Composition:

    1 tablet contains:

    CORE


    Active substance:


    Cetirizine dihydrochloride

    10.00 mg

    Excipients:


    Lactose Monohydrate

    75.00 mg

    Corn starch

    40.00 mg

    Povidone

    4.00 mg

    Magnesium stearate

    1.00 mg

    FILM SHELL


    Opadry 33G28707:

    (ready to use mixture):

    3.60 mg

    Hypromellose

    1.440 mg

    Titanium dioxide (E171)

    0.864 mg

    Lactose Monohydrate

    0.792 mg

    Macrogol 3000

    0.288 mg

    Triacetin

    0.216 mg)

    Description:

    Round, slightly biconcave tablets, covered with a film shell of white color, with a risk.

    Pharmacotherapeutic group:antiallergic agent - H1-histamine receptor blocker
    ATX: & nbsp

    E.06.A.E.07   Cetirizine

    Pharmacodynamics:

    Cetirizine is a competitive histamine antagonist and a metabolite of hydroxyzine. Cetirizine selectively blocks peripheral H1-gistaminovye receptors. Affects the "early" histamine-dependent stage of allergic reactions, limits the release of inflammatory mediators of the "late" stage of the allergic reaction, reduces the migration of eosinophils, neutrophils and basophils, and stabilizes the membranes of mast cells.

    Eliminates the skin reaction to the administration of histamine, specific allergens, and also to cooling (with cold urticaria).

    Reduces histamine-induced bronchoconstriction in bronchial asthma of the lung course.

    It has anti-allergic, antipruritic and antiexcudative action.

    Reduces the permeability of capillaries, prevents the development of edema of tissues.

    Has a weak anticholinergic and antiserotonin effect.

    In therapeutic doses, it usually does not cause sedation.

    The action of cetirizine begins 20 minutes after ingestion.The maximum effect is manifested 1 hour after ingestion and lasts more than 24 hours. Against the background of course treatment of tolerance to antihistamine effect of cetirizine does not develop. After cessation of treatment, the effect lasts up to 3 days.

    Pharmacokinetics:

    Cetirizine has a linear pharmacokinetics in the dose range of 5 to 60 mg. Quickly absorbed from the gastrointestinal tract (GIT); absorption - 70%. Achieves maximum concentration (CmOh) in the blood plasma (about 300 ng / ml) 1 hour after ingestion, and the equilibrium concentration - after 3 days of use. With prolonged use in the body does not accumulate. Half-life (T1/2) is about 10 hours.

    The degree of absorption of cetirizine is not dependent on food intake, but the rate of absorption may decrease. Bioavailability of cetirizine when taken orally in the form of tablets or a solution is the same.

    The amount of cetirizine distribution is very small, compared to other antihistamines and preparations, and is approximately 0.5 l / kg. In plasma, approximately 93% of cetirizine binds to albumin.

    Less than 14% of the drug is metabolized in the liver by O-dealkylation to form pharmacologicallyinactive metabolite.

    Cetirizine is not subject to active metabolism with the effect of "first" passage through the liver. Unchanged cetirizine is excreted by the kidneys, and metabolites - with bile through the intestine. In a small amount it is secreted into breast milk.

    Special patient groups

    Elderly patients

    In elderly patients, T1/2 Increased by 50%, and the clearance is reduced by 40%. Delayed excretion is mainly a result of reduced total clearance of cetirizine, which depends on the function of the kidneys.

    Children

    Children cetirizine reaches a higher concentration in the blood plasma and is quickly excreted from the body. The overall clearance is higher by approximately 33%, and T1/2 is shorter by 33% and is 6 hours for children aged 6-12 years.

    Impaired renal function

    In healthy volunteers and patients with mild impairment of renal function (creatinine clearance (CK) of more than 40 ml / min), the pharmacokinetics of cetirizine are the same. In patients with moderate renal dysfunction T1/2 increased by 3 times, and the clearance is reduced by 70% compared with volunteers with normal renal function. Patients with moderate or severe renal dysfunction need dose adjustment.In patients on hemodialysis (CC less than 7 ml / min) after a single application of cetirizine inside T1/2 increases by 3 times, and the clearance is reduced by 70% compared to healthy volunteers. Only 9.4% of the dose is excreted from the body during hemodialysis.

    Impaired liver function

    In patients with cirrhosis who received 10 or 20 mg of cetirizine as a single dose, there was an increase in T1/2 by 50% and a decrease in clearance by 40% compared with healthy people. A change in the dose is only necessary for those patients with liver diseases who have concomitant renal dysfunction.

    Indications:

    - Seasonal and year-round allergic rhinitis and conjunctivitis;

    - Pollinosis (hay fever);

    - tourine (including chronic idiopathic);

    - zallergic allergic dermatoses;

    - abouttech Quincke.

    Contraindications:

    Hypersensitivity to cetirizine, hydroxyzine or accessory components of the drug, terminal renal failure (QC less than 10 mL / min and need for hemodialysis), pregnancy, breastfeeding, children under 6 years of age (this dosage form), lactase deficiency, fructose intolerance or lactose, glucose-galactose malabsorption syndrome.

    Carefully:

    Chronic renal failure (with the exception of terminal, see "Method of application"), elderly age (possibly reducing glomerular filtration), chronic liver disease.

    Pregnancy and lactation:

    Data on the clinical use of cetirizine in pregnant women are not available, therefore, do not use Lethisen® during pregnancy.

    Cetirizine is secreted into breast milk, so during the period of Lethisen®, breastfeeding should be discontinued.

    Dosing and Administration:

    Inside, regularly, preferably at one time, with a small amount of liquid.

    Adults and teenagers over 12 years of age

    The recommended daily dose is 1 tablet (10 mg) once a day.

    Children from 6 to 12 years old

    Recommended daily dose - 1/2 tablets (5 mg) 2 times a day.

    Elderly patients

    Correction of the dose is not required.

    Dysfunction of the liver

    Correction of the dose is not required.

    The duration of treatment is determined by the doctor.

    Adult patients with impaired renal function

    Renal failure

    Creatinine clearance

    (ml / min)

    Dose and frequency of admission

    Normal kidney function

    ≥80

    10 mg once a day

    Lightweight

    50-79

    10 mg once a day

    Average

    30-49

    5 mg once a day

    Heavy

    less than 30

    5 mg once a day, every 2 days

    Terminal, the need for hemodialysis

    10-30

    Contraindicated

    In children with impaired renal function The dose should be adjusted individually, taking into account the CK, the patient's age and body weight (the use of Lethisen® in a medicinal form for oral administration is recommended).

    Side effects:

    Classification of the incidence of adverse events (WHO):

    very often -> 1/10

    often from> 1/100 to <1/10

    infrequently - from> 1/1000 to <1/100

    rarely from> 1/10000 to <1/1000

    very rarely - from <1/10000, including individual messages.

    From the nervous system:

    often: headache, dizziness; rarely: migraine, drowsiness;

    very rarely: convulsions, change and loss of taste, paresthesia, dyskinesia, fainting, aggressiveness; agitation, confusion, depression, insomnia, dystonia, tremor, tick, hallucinations, confusion;

    From the respiratory system:

    often: pharyngitis, rhinitis;

    From the digestive system:

    often: dryness of the oral mucosa, nausea;

    rarely: abdominal pain;

    Very rarely: diarrhea, impaired liver function (increased activity of "liver" transaminases, alkaline phosphatase, gamma-glutamintransferase and bilirubin concentration);

    From the side of the cardiovascular system:

    very rarely: tachycardia;

    From the urinary system:

    very rarely: upset urination, enuresis;

    From the sense organs:

    very rarely: disruption of accommodation, blurred vision, nystagmus;

    From the skin:

    very rarely: itching, rash, hives;

    Allergic reactions:

    very rarely: anaphylactic shock, angioedema, hypersensitivity reactions;

    Other:

    often: weakness;

    very rarely: weight gain, asthenia, general malaise, edema of the lower limbs;

    Laboratory indicators: thrombocytopenia.

    Overdose:

    Symptoms: confusion, diarrhea, dizziness, headache, general malaise, mydriasis, itching, anxiety, blocking, drowsiness, tachycardia, tremor, urinary retention, stupor, confusion.

    Treatment: there is no specific antidote. In case of an overdose, symptomatic or supportive treatment is recommended. It is necessary to monitor the functions of the cardiovascular and respiratory systems.

    If after taking the drug inside a little time, you should induce vomiting and rinse the stomach, take Activated carbon.

    There is no specific antidote. Hemodialysis is ineffective.

    Interaction:

    The pharmacokinetic interaction of cetirizine with pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, diazepam, and glipizide was not detected.

    Simultaneous application of cetirizine with theophylline (400 mg / day) leads to a decrease in the total clearance of cetirizine by 16% (theophylline kinetics does not change). With simultaneous application with macrolides and ketoconazole, there are no changes on the electrocardiogram.

    Myelotoxic drugs increase the manifestation of hematotoxicity of the drug.

    Special instructions:

    If you miss a dose, you should take it as soon as possible. If the next dose of Lethisen® remains several hours, take a standard dose at the usual time, leaving the previous dose missed.

    Since in some patients, Lethisen® can cause drowsiness, it is recommended to take it in the evening.

    In therapeutic doses, there was no clinically significant interaction with ethanol (with ethanol concentration in the blood up to 0.5 g / l). Nevertheless, it is recommended to refrain from drinking alcohol during treatment.

    Lethisen® contains lactose, therefore it is contraindicated in patients with lactase deficiency, lactose intolerance, glucose-galactose malabsorption syndrome.
    Effect on the ability to drive transp. cf. and fur:

    Lethisen® in some patients can cause drowsiness, so it is necessary to refrain from driving vehicles and working with complex technical devices that require a high concentration of attention and speed of psychomotor reactions.

    Form release / dosage:

    Tablets, film-coated, 10 mg.

    Packaging:

    For 10 tablets in a blister of PVC / aluminum foil.

    For 1 or 2 blisters in a pack of cardboard along with instructions for use.

    Storage conditions:

    At temperatures not higher than 30 ° C, in the original packaging.

    Keep out of the reach of children.

    Shelf life:

    5 years.

    Do not use the drug after the expiration date.

    Terms of leave from pharmacies:Without recipe
    Registration number:П N013437 / 01
    Date of registration:29.09.2011
    Expiration Date:Unlimited
    Date of cancellation:2018-02-06
    The owner of the registration certificate:KRKA, dd, Novo mesto, AOKRKA, dd, Novo mesto, AO
    Manufacturer: & nbsp
    KRKA, d.d. Slovenia
    Representation: & nbspKRKA, dd, Novo mesto, AOKRKA, dd, Novo mesto, AO
    Information update date: & nbsp06.02.2018
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