Active substanceCetirizineCetirizine
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  • Dosage form: & nbsp
    Film-coated tablets.
    Composition:
    Composition per one tablet:
    Cetirizine dihydrochloride 10 mg
    Auxiliary substances
    microcrystalline cellulose - 25 mg
    povidone, - 1.4 mg
    lactose monohydrate, - 40.8 mg
    calcium hydrogen phosphate dihydrate, -15 mg
    carboxymethyl starch sodium (sodium starch glycolate), 6.8 mg
    magnesium stearate - 1 mg
    Nominal tablet weight without shell - 100 mg
    Excipients for the shell
    hypromellose (hydroxypropylmethylcellulose) - 2.1 mg
    macrogol 6000 (polyethylene glycol 6000) - 0.6 mg
    titanium dioxide - 0.3 mg
    Nominal tablet weight with sheath - 103 mg
    Description:Tablets covered with a film coat of white or almost white color, biconvex, oblong with rounded ends, with a risk. On the cross-section of the tablet, the inner layer is white or almost white in color.
    Pharmacotherapeutic group:antiallergic agent-H1 histamine receptor blocker.
    ATX: & nbsp

    E.06.A.E.07   Cetirizine

    Pharmacodynamics:Cetirizine has a pronounced anti-allergic effect. Virtually does not have a sedative effect in pharmacologically active doses, it refers to selective antagonists of H1-histamine receptors and has almost no anticholinergic and antiserotonin action, prevents development and facilitates the course of allergic reactions. Has antipruritic and anti-exsudative effect. Affects the early stage of allergic reactions, and also reduces the migration of inflammatory cells; oppresses the selection of mediators involved in a late allergic reaction. Reduces the permeability of capillaries, prevents the development of edema of tissues, relieves spasm of smooth muscles. Eliminates the skin reaction to the administration of histamine, specific allergens, and also to cooling (with cold urticaria). Cetirizine significantly reduces the hyperreactivity of the bronchial tree arising in response to the release of histamine in patients with bronchial asthma. The therapeutic effect of the drug appears on average 60 minutes after admission. Against the background of the course, tolerance does not develop.
    Pharmacokinetics:

    After oral administration cetirizine quickly and well absorbed from the gastrointestinal tract (GIT). The maximum level of concentration is determined after about 40-60 minutes. Eating does not have a significant effect on the amount of absorption, but in this case, the rate of absorption is slightly reduced.

    Cetirizine binds to blood plasma proteins by about 93%. The volume of the distribution (Vd) low (0.5 l / kg), the drug inside the cell does not penetrate. The drug does not penetrate the blood-brain barrier (BBB).

    Cetirizine is poorly metabolized in the liver with the formation of an inactive metabolite. At 10-day application in a dose of 10 mg accumulation of the drug is not observed. Approximately 70% excretion is performed by the kidneys, mostly unchanged. The system clearance is about 54 ml / min.

    After a single dose, the half-life (T1/2) is about 10 hours. In children aged 2 to 12 years, T1/2 decreases to 5-6 hours.

    If the renal function is impaired (creatinine clearance (CC) is below 11-31 ml / min) and in patients on hemodialysis (CC less than 7 ml / min) T1/2 increases by 3 times, the clearance decreases by 70%.

    Against the background of chronic diseases and in elderly patients there is an increase in T1 / 2 by 50% and a decrease in clearance by 40%. Hemodialysis is ineffective.

    Indications:Seasonal and all-the-year-round allergic rhinitis and conjunctivitis (itching, sneezing, rhinorrhea, lacrimation, hyperemia of the conjunctiva), urticaria (including chronic idiopathic urticaria), hay fever, allergic dermatitis, including atopic, accompanied by itching.
    Contraindications:Increased individual sensitivity to one of the components of the drug, kidney failure (CC <10ml / min), children under 6 years of age, pregnancy, lactation, lactase deficiency, lactose intolerance, glucose-galactose malabsorption.
    Carefully:In chronic renal failure (CRF) with CK> 10 ml / min (correction of the dosing regimen is required), chronic liver diseases, in old age (glomerular filtration may be reduced).
    Dosing and Administration:

    Inside, regardless of food intake.

    Adults and adolescents over the age of 12 years - 1 tablet daily, preferably in the evening.

    Children aged 6-12 years - 1/2 tablet twice a day in the morning and in the evening.

    In chronic renal failure (CRF), the recommended dose should be reduced: with QC 30-49 ml / min - 5 mg 1 time per day, at 10-29 ml / min - 5 mg every other day. Children reduce the dose 2 times. Duration of reception is determined individually.

    When a violation of liver function it is necessary to select a dose individually, especially carefully with simultaneous renal failure.

    The elderly patients with normal renal function do not need dose adjustment. Duration of admission is determined individually, usually with seasonal allergic rhinitis, the duration of therapy is from 3 to 6 weeks, and with a short-term exposure to pollen, one week is enough.

    Side effects:

    From the nervous system and sensory organs: drowsiness, fatigue, agitation, headache, dizziness, anxiety, nervousness, emotional lability, impaired concentration and thinking, insomnia,depression, euphoria, confusion, amnesia, depersonalization, ataxia, impaired coordination of movements, tremor, hyperkinesis, calf muscle cramps, paresthesia, dysphonia, myelitis, paralysis, ptosis (from the central nervous system), violation of accommodation and vision, pain in the eyes , glaucoma, xerophthalmia, conjunctivitis, eye hemorrhage, ototoxicity, tinnitus, deafness, impaired sense of smell.

    On the part of the digestive system: dry mouth, change or lack of appetite, increased appetite, anorexia, aphthous stomatitis, discoloration and swelling of the tongue, increased salivation, increased cariousness, thirst, vomiting, dyspepsia, gastritis, abdominal pain, flatulence, diarrhea, constipation, hemorrhoids, melena, rectal bleeding, impaired liver function.

    From the cardiovascular system: Migraine, palpitations, increased blood pressure, heart failure.

    On the part of the respiratory system: rhinitis, epistaxis, polyps of the nasal cavity, pharyngitis, cough, sinusitis, bronchitis, increased bronchial secretion, bronchospasm, dyspnoea, upper respiratory tract infection, pneumonia, hyperventilation.

    From the genitourinary system: urinary retention, edema, polyuria, dysuria, hematuria, urinary tract infection, cystitis, decreased libido, dysmenorrhea, intermenstrual bleeding, menorrhagia, vaginitis.

    From the musculoskeletal system: arthralgia, arthritis, arthrosis, myalgia, back pain, muscle weakness.

    From the skin: dry skin, rash, blister rashes, itching, acne, furunculosis, dermatitis, eczema, hyperkeratosis, erythema, increased sweating, alopecia, angioedema, hypertrichosis, photosensitivity, seborrhea.

    Other: malaise, fever, chills, hot flashes, dehydration, diabetes mellitus, lymphadenopathy, pain in the mammary glands, weight gain, skin allergic reactions, incl. hives.

    Overdose:Symptoms: possible drowsiness, inhibition, weakness, headache, tachycardia, increased irritability, retention of urination, fatigue (most often with the intake of 50 mg of cetirizine per day).
    Treatment: conduct symptomatic therapy. A specific antidote has not been identified. Hemodialysis is ineffective. The stomach is washed, Activated carbon.
    Interaction:Clinically significant interactions of cetirizine with other drugs have not been established. Theophylline (400 mg / day) slightly (by 16%) decreases the clearance of cleirenscetirizine (theophylline kinetics does not change). Myelotoxic drugs increase the manifestation of hematotoxicity of the drug. Compatible with azithromycin, pseudoepinephrine, ketoconazole, erythromycin, diazepam and cimetidine.
    Special instructions:

    - Children

    The use of children under 6 years is contraindicated.

    - Adults with chronic diseases

    It is necessary to correct the dosage regimen, to the elderly (possibly reducing glomerular filtration).

    Effect on the ability to drive transp. cf. and fur: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. When the dose is exceeded 10 mg / day, the ability to speed up the reactions may worsen. It is not recommended simultaneous use of funds that depress the central nervous system and alcohol consumption.
    Form release / dosage:
    Tablets, film-coated, 10 mg.


    Packaging:
    By 10, 14, 15, 20 or 30 tablets in a contour mesh box made of polyvinyl chloride film and aluminum foil printed lacquered.
    On 1,2,3,4,5,6 contour cellular packings with the instruction on application in a pack from a cardboard.
    Storage conditions:In dry, dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.
    Shelf life:2 years. Do not use after the expiration date printed on the package.
    Terms of leave from pharmacies:Without recipe
    Registration number:LP-001445
    Date of registration:20.01.2012
    Date of cancellation:2017-01-20
    The owner of the registration certificate:OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp11.10.2015
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