Atarax® (Atarax®)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceHydroxysinHydroxysin
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  • Atarax®
    pills inwards 
    YUSB Farma S.A.     Belgium
  • Atarax®
    solution w / m 
    YUSB Farma S.A.     Belgium
  • Hydroxysin Canon
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    CANONFARMA PRODUCTION, CJSC     Russia
  • Hydroxisin-native
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    NATIVA, LLC     Russia
    • Dosage form: & nbspfilm-coated tablets
    Composition:

    Active substance: hydroxyzine hydrochloride 25 mg;

    Excipients: lactose monohydrate 54,80 mg, microcrystalline cellulose 28.00 mg, magnesium stearate 1.50 mg, silicon dioxide colloid (anhydrous) 0.70 mg;

    shell: Opadrai® Y-1-7000 3.30 mg (titanium dioxide 0.21 mg, hypromellose 2.06 mg, macrogol 400 1.03 mg).

    Description:

    White, oblong tablets, covered with a film sheath, with a transverse risk on both sides.

    Pharmacotherapeutic group:anxiolytic (tranquilizer)
    ATX: & nbsp

    N.05.B.B.01   Hydroxysin

    Pharmacodynamics:

    Derivative diphenylmethane, inhibits the activity of certain subcortical zones.

    Provides H1-gastamine-blocking, bronchodilating and antiemetic effect, has a moderate inhibitory effect on gastric secretion. Hydroxysin significantly reduces itching in patients with hives, eczema and dermatitis.

    With hepatic insufficiency H1The histamine-blocking effect can be prolonged up to 96 hours after a single dose.

    It has moderate anxiolytic activity and sedative effect.

    Polysomnography in patients with insomnia and anxiety shows an increase in the duration of sleep, a decrease in the frequency of nocturnal awakenings after taking single or repeated hydroxyzine at a dose of 50 mg. Reduction of muscle tension in patients with anxiety was noted when taking the drug at a dose of 50 mg 3 times a day. Does not cause mental dependence and addiction. With prolonged admission, there was no "withdrawal" syndrome and cognitive impairment.

    H1The histamine-blocking effect occurs approximately 1 hour after ingestion of the tablets. Sedation occurs after 30-45 minutes.

    Has spasmolytic and sympatholytic effects, and also has a moderate analgesic effect.

    Pharmacokinetics:

    Suction

    Absorption is high. Time to reach the maximum concentration (TcmOh) after oral administration - 2 hours After taking a single dose of 25 mg TcmOh in adults is 30 ng / ml and 70 ng / ml after taking 50 mg of hydroxyzine. Bioavailability with oral administration is 80%.

    Distribution

    Hydroxysin is more concentrated in tissues than in plasma. The distribution coefficient is 7-16 l / kg in adults.After oral administration hydroxysine well penetrates the skin, while the concentration of hydroxysin in the skin is much higher than the concentration in the blood serum both after a single and after repeated receptions. Hydroxysin penetrates the blood-brain barrier and the placenta, concentrating more in fetal than in maternal tissues.

    Metabolism

    Hydroxysin is metabolized in the liver. Cetirizine - the main metabolite (45%), is a blocker peripheral H1-gistaminovyh receptors. Metabolites are found in breast milk.

    Excretion

    Half-life (T1/2) in adults -14 h (range: 7-20 h). The total clearance of hydroxyzine is 13 ml / min / kg. Only 0.8% of hydroxyzine is excreted unchanged through the kidneys. The main metabolite cetirizine excreted mainly unchanged in the urine (25% of the intake dose of hydroxysin).

    Pharmacokinetics in specific patient groups

    In elderly patients

    In elderly patients, T1/2 was 29 h, the volume of distribution was 22.5 l / kg. It is recommended to reduce the daily dose of hydroxyzine for elderly patients.

    Children

    In children, the total clearance is 2.5 times higher than in adults. Half-life (T1/2) is shorter than in adults: 11 hours - in children aged 14 years and 4 hours - at the age of 1 year. The dose should be adjusted when used in children.

    In patients with hepatic insufficiency

    In patients with secondary liver dysfunction due to primary biliary cirrhosis, the overall clearance was approximately 66% of the value recorded in healthy volunteers. In patients with liver disease T1/2 increased to 37 hours, the concentration of metabolites in the serum is higher than in young patients with normal liver function. Patients with hepatic impairment are recommended to reduce the daily dose or the frequency of admission.

    In patients with renal insufficiency

    The pharmacokinetics of hydroxyzine was studied in 8 patients with severe renal insufficiency (creatinine clearance 24 ± 7 ml / min). The duration of exposure of the hydroxyzine (AUC [area under the curve]) did not change significantly, while the exposure time of the carboxyl metabolite, cetirizine, was increased. Hemodialysis is ineffective for the removal of this metabolite.To avoid any significant accumulation of the metabolite of cetirizine after repeated use of hydroxyzine, patients with impaired renal function should reduce the daily dose of hydroxyzine.
    Indications:

    - Symptomatic treatment of anxiety in adults;

    - as a sedative during the period of premedication;

    - symptomatic treatment of pruritus of allergic origin.

    Contraindications:

    - Hypersensitivity to any of the drug components, cetirizine and other piperazine derivatives, aminophylline or ethylenediamine;

    - porphyria;

    - children under 3 years;

    - pregnancy, childbirth and breastfeeding;

    - hereditary intolerance to galactose, lactase deficiency, or glucose-galactose malabsorption syndrome (since lactose is included in the tablet formulation);

    - interval lengthening QT in the anamnesis.

    Carefully:

    In myasthenia, prostatic hyperplasia with clinical manifestations, difficulty urinating, constipation, with glaucoma, dementia, propensity to convulsive seizures, with an inclination to arrhythmia, including electrolyte imbalance (hypokalemia, hypomagnesemia), in patients with a history of heart disease or with the use of drugs , which can cause arrhythmia.

    Pregnancy and lactation:

    The drug is contraindicated for use in pregnant women, during labor and breastfeeding.

    Dosing and Administration:

    Inside.

    Children

    For symptomatic treatment of pruritus of allergic origin

    At the age from 3 to 6 years: 1 mg / kg / day to 2.5 mg / kg / day in several doses.

    At the age of 6 years and older: 1 mg / kg / day to 2.0 mg / kg / day in several doses.

    For premedication - 1 mg / kg at night before anesthesia.

    The number of tablets is calculated by the doctor depending on the weight of the child in accordance with the recommended doses.

    Adults

    For symptomatic treatment of anxiety: a standard dose of 50 mg per day divided into 3 doses (1/2 tablet (12.5 mg) in the morning, 1/2 tablet (12.5 mg) in the afternoon and 1 tablet (25 mg) overnight).

    In severe cases, the dose may be increased to 12 tablets (300 mg) per day.

    For symptomatic treatment of pruritus of allergic origin: the initial dose of 1 tablet (25 mg) before bed, if necessary, the dose can be increased to 1 tablet (25 mg) 3-4 times a day.

    For premedication in surgical practice: 2-8 tablets (50-200 mg) at night before anesthesia.

    A single maximum dose for an adult should not exceed 8 tablets (200 mg), the maximum daily dose is not more than 12 tablets (300 mg).

    Use in special patient groups

    The dose is selected by the doctor individually taking into account the response to the treatment in the range of recommended doses.

    Application the old people

    In elderly patients, treatment starts with a half dose.

    For symptomatic treatment of anxiety: 1/2 tablet (12.5 mg) in the morning and 1/2 tablet (12.5 mg) in the evening.

    For symptomatic treatment of pruritus of allergic origin: the initial dose of 1/2 tablet (12.5 mg) before bed, if necessary, the dose can be increased to 1/2 tablet (12.5 mg) 3-4 times a day.

    For premedication in surgical practice: 1-4 tablets (25-100 mg) at night before anesthesia.

    Application the patients with renal insufficiency and impaired liver function

    Patients with severe and moderate renal insufficiency, as well as with liver failure, need a dose reduction. In patients with hepatic insufficiency, it is recommended to reduce the daily dose by 33%.

    In patients with severe and moderate renal insufficiency, a dose reduction is recommended because of decreased excretion of the main metabolite of hydroxyzine-cetirizine. It should reduce the dose of hydroxyzine or increase the interval between doses in proportion to the decrease in creatinine clearance,for example: half of the daily dose for moderate renal failure and a quarter of the daily dose for severe renal failure.

    Side effects:

    Possible side effects are given below for the body systems and frequency of occurrence: very often (≥1 / 10), often (≥1 / 100, <1/10), infrequently (≥1 / 1000, <1/100), rarely (≥ 1/10000, <1/1000), very rarely (<1/10000), the frequency is unknown (can not be estimated from available data).

    From the nervous system:

    Often: drowsiness.

    Often: headache, retardation.

    Infrequently: dizziness, insomnia, tremor.

    Rarely: cramps, dyskinesia.

    Mental disorders:

    Infrequently: agitation, confusion.

    Rarely: hallucinations, disorientation.

    From the side of the organ of vision:

    Rarely: violation of accommodation, impaired vision.

    From the heart:

    Rarely: tachycardia.

    Frequency unknown: elongation interval QT on the electrocardiogram, ventricular tachycardia as pirouette.

    From the respiratory system, chest and mediastinum:

    Rarely: bronchospasm.

    From the gastrointestinal tract:

    Often: dry mouth.

    Infrequently: nausea.

    Rarely: vomiting, constipation.

    From the liver and biliary tract

    Rarely: impaired functional liver tests.

    Frequency unknown: hepatitis.

    General disorders:

    Often: fatigue.

    Rarely: hyperthermia, malaise.

    From the side of the kidneys and urinary tracts:

    Rarely: retention of urination.

    From the skin and subcutaneous tissues:

    Rarely: itching, rash (erythematous, maculopapular), hives, dermatitis.

    Rarely: angioedema, sweating, fixed erythema medicament, acute generalized exanthematous pustular eruption, erythema multiforme, Stevens-Johnson syndrome.

    With the side of the immune system:

    Rarely: hypersensitivity.

    Rarely: anaphylactic shock.

    From the side of the vessels:

    Rarely: lowering of blood pressure.

    The following side effects were observed when taking cetirizine, the main metabolite of hydroxyzine: thrombocytopenia, aggression, depression, tic, dystonia, paresthesia, oculogic crisis, diarrhea, dysuria, enuresis, asthenia, edema, weight gain and can be observed with the intake of hydroxyzine.

    Overdose:

    Symptoms observed after a significant drug overdose are associated with excessive m-holin-blocking action, suppression or paradoxical stimulation of the CNS. These symptoms include nausea, vomiting, tachycardia, hyperthermia, drowsiness, impaired pupillary reflex, tremor, confusion, or hallucinations. Subsequently, depression of consciousness, respiration, convulsions, lowering of arterial pressure, arrhythmia can develop. Possible aggravation of coma and cardiopulmonary collapse.

    It is necessary to monitor the state of the respiratory tract, the state of breathing and circulation using ECG monitoring, and provide adequate oxygenation. Cardiac activity and blood pressure should be monitored within 24 hours after the disappearance of symptoms.

    In the case of a violation of mental status, it is necessary to exclude the taking of other drugs or alcohol, if necessary, the patient should be inhaled with oxygen, naloxone, dextrose (glucose) and thiamine.

    If it is necessary to obtain a vasopressor effect, norepinephrine or metameninol. Do not use epinephrine.

    If you ingest a significant amount of the drug, you can perform gastric lavage with a previous endotracheal intubation. It is possible to use activated carbon, however, data that indicate its effectiveness is not enough. There is no specific antidote. Hemodialysis is ineffective.

    Literary data indicate that in the case of development of severe, life-threatening, intractable m-cholinoblocking effects not being treated with other drugs, a therapeutic dose of physostigmine may be used. Physostigmine should not be used only to bring the patient to consciousness. If the patient took tricyclic antidepressants, the use of physostigmine can trigger convulsive attacks and irreversible cardiac arrest. Also, the use of physostigmine in patients with cardiac conduction disorders should be avoided.

    Interaction:

    It is necessary to take into account the potentiating action of hydroxyzine when combined with drugs that depress the central nervous system, such as narcotic analgesics, barbiturates, tranquilizers, hypnotics, alcohol.In this case, their doses should be selected individually.

    It should avoid simultaneous use with monoamine oxidase (MAO) inhibitors and holinoblockers.

    The drug interferes with the pressor action of epinephrine and anticonvulsant activity of phenytoin, and also interferes with the action of betagistin and cholinesterase inhibitor drugs.

    It was found that the use of cimetidine at a dose of 600 mg twice a day increases the serum hydroxynine concentration by 36% and reduces the maximum concentration of cetirizine metabolite by 20%.

    The effect of atropine, alkaloids of belladonna, cardiac glycosides, hypotensive drugs, blockers H2-gistaminovyh receptors do not change under the action of hydroxyzine.

    Hydroxysin is an inhibitor of the isoenzyme CYPD6 and in high doses may be the cause of drug interaction with isoenzyme substrates CYP2D6. Because the hydroxysine it is metabolized in the liver, we can expect an increase in its concentration in the blood with simultaneous application with inhibitors of microsomal liver enzymes.

    Because the hydroxysine metabolized by alcohol dehydrogenase and isoenzyme CYP3A4/5, it is possible to increase the concentration of hydroxyzine in the blood plasma when used simultaneously with drugs potentially inhibiting the isoenzyme CYP3A4/5 (telithromycin, clarithromycin, delavirdine, styipentol, ketoconazole, voriconazole, itraconazole, posaconazole and some HIV protease inhibitors, including atazanavir, indinavir, nelfinavir, ritonavir, saquinarin, lopinavir / ritonavir, saquinarin / ritonavir, and tipranavir / ritonavir). However, inhibition of one metabolic pathway can be partially compensated by the work of another.

    The simultaneous use of hydroxyzine with drugs that potentially can cause arrhythmia may increase the risk of lengthening the interval QT and the occurrence of ventricular tachycardia as pirouette.

    Special instructions:

    When used simultaneously with drugs that have m-cholinoblocking properties and drugs that depress the central nervous system, the dose of hydroxyzine should be reduced.

    In renal and / or liver failure, doses should be reduced.

    If it is necessary to prescribe allergological samples or conduct a methacholine test, the drug should be discontinued 5 days before the study forpreventing the acquisition of garbled data.

    During treatment with hydroxyzine, alcohol should be avoided.

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

    Hydroxysin may impair the ability to concentrate and the speed of psychomotor reactions. Taking other sedatives can enhance this effect. Therefore, one should refrain from driving vehicles and practicing other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

    Form release / dosage:

    Film-coated tablets, 25 mg.

    Packaging:

    For 25 tablets in a blister of PVC-aluminum foil.

    For 1 blister in a cardboard pack together with instructions for use.

    Storage conditions:

    In a dry place, at a temperature of no higher than 25 ° C.

    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:On prescription
    Registration number:П N011405 / 01
    Date of registration:07.12.2011
    The owner of the registration certificate: YUSB Farma S.A. YUSB Farma S.A. Belgium
    Manufacturer: & nbsp
    Representation: & nbspYUSB FARMA LLC YUSB FARMA LLC Russia
    Information update date: & nbsp16.01.2016
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