Atarax® (Atarax®)

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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
    pills inwards 
    CANONFARMA PRODUCTION, CJSC     Russia
  • Hydroxisin-native
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    NATIVA, LLC     Russia
    • Dosage form: & nbspsolution for intramuscular injection
    Composition:

    In 2 ml:

    active substance: hydroxyzine hydrochloride 100.00 mg;

    Excipients: sodium hydroxide (up to pH 5.2) about 10.00 mg, water for injection up to 2.00 ml.

    Description:

    A clear, colorless solution.

    Pharmacotherapeutic group:Anxiolytic agent (tranquilizer)
    ATX: & nbsp

    N.05.B.B.01   Hydroxysin

    Pharmacodynamics:

    Derivative diphenylmethane, has a moderate anxiolytic activity; also has a sedative, antiemetic, antihistamine and M-anticholinergic action. It blocks central M-holino- and H1-gistaminoreceptors and inhibits the activity of certain subcortical zones. Does not cause mental dependence and addiction. Has a positive effect on cognitive abilities, improves memory and attention. Relaxes skeletal and smooth musculature, has bronchodilating and analgesic effects, moderate inhibitory effect on gastric secretion. Hydroxysin significantly reduces itching in patients with hives, eczema and dermatitis. At long reception the syndrome of cancellation and deterioration of cognitive functions was not noted. Polysomnography in patients with insomnia and anxiety clearly demonstrate the prolongation of the duration of sleep, a decrease in the frequency of nocturnal awakenings after single or repeated hydroxyzine administration 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.

    Pharmacokinetics:

    After the introduction of an intramuscular single dose of 50 mg CmOh usually is 65 ng / ml. The half-life (T1/2) In adults, an average of 14 hours. Metabolites are found in breast milk.

    Hydroxysin is more concentrated in tissues than in plasma. The distribution coefficient is 7-16 l / kg in adults. Hydroxysin penetrates the blood-brain barrier and the placenta, concentrating more in fetal than in maternal tissues. Hydroxysin is metabolized in the liver. Cetirizine - the main metabolite (45%), is expressed H1-blocker. 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 (16% of the intramuscular dose of hydroxyzine).

    Children the total clearance is 2.5 times shorter than in adults. Half-life T1/2 shorter than in adults: 11 hours - in children aged 14 years and 4 hours - at the age of 1 year.

    In elderly patients T1/2 was 29 h, the distribution coefficient was 22.5 l / kg.

    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.

    Antihistamine effect can be prolonged up to 96 h after administration.

    Indications:

    - Adults for relief of anxiety, psychomotor agitation, feelings of internal tension, increased irritability with neurological, psychic (generalized anxiety and adjustment disorder) and somatic diseases, as well as chronic alcoholism, alcohol withdrawal syndrome accompanied by symptoms of psychomotor agitation;

    - at As a sedative in the period of premedication;

    - fromImptomatic itching therapy.

    Contraindications:

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

    - porphyria;

    - children under 1 year;

    - pregnancy, the period of labor and breastfeeding;

    - intraarterial and subcutaneous administration.

    Carefully:

    With myasthenia, prostatic hyperplasia with clinical manifestations, difficulty urinating, constipation, glaucoma, dementia, a tendency to convulsive seizures, with a tendency to arrhythmia or when prescribing drugs that can cause arrhythmia.

    In patients with indications of lengthening the interval QT a history of alternative treatment should be considered.

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

    Patients with a severe and moderate degree of renal insufficiency, as well as with liver failure, need a dose reduction.

    The elderly patient is reduced in case of reduced glomerular filtration.

    Dosing and Administration:
    The drug is administered intramuscularly.

    Children

    For symptomatic treatment of pruritus:

    At the age from 12 months to 6 years: 1 mg / kg to 2.5 mg / kg / day in several doses.

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

    For premedication: 1 mg / kg 1 hour before the surgery, and if necessary, 1 mg / kg at night before anesthesia.

    Adults

    For symptomatic treatment of anxiety: A standard dose of 50 mg per day, divided into 3 doses (morning 12.5 mg, 12.5 mg and 25 mg day at night).

    In serious cases, the dose may be increased to 300 mg per day.

    For symptomatic treatment of pruritus: Initial dose of 25 mg, as appropriate dose may be increased to four times (25 mg 4 times daily).

    For premedication in surgical practice: 50-200 mg / day for 1 hour before surgery, and also if necessary for an additional overnight before anesthesia.

    In elderly patients treatment begins with a half dose.

    With renal and / or liver failure doses should be reduced. In patients with hepatic insufficiency, it is recommended to reduce the daily dose by 33%.

    A single maximum dose should not exceed 200 mg, the maximum daily dose is not more than 300 mg.

    Side effects:

    Possible side effects are given below by body system and frequency of occurrence: very often (≥1 / 10), often (≥1 / 100, <1/10) infrequently (≥1 / 1000 <1/100), rare (≥ 1/10000, <1/1000), very rarely (<1/10000).

    From the nervous system:

    Often: drowsiness.

    Often: headache, fatigue.

    Infrequently: dizziness, insomnia, tremor.

    Rarely: convulsions, dyskinesia

    Mental disorders:

    Infrequently: agitation, confusion.

    Rarely: hallucinations, disorientation.

    From the side of the organ of vision:

    Rarely: disturbance of accommodation, blurred vision.

    From the side of the cardiovascular system:

    Rarely: tachycardia, hypotension.

    On the part of the respiratory system, the organs of the thorax and the mediastinum:

    Rarely: bronchospasm.

    From the gastrointestinal tract:

    Often: dry mouth.

    Infrequently: nausea.

    Rarely: vomiting, constipation.

    General disorders:

    Often: general weakness.

    Rarely: hyperthermia, malaise.

    From the side of the kidneys and urinary tract:

    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.

    From laboratory and instrumental indicators:

    Rarely: change in functional liver samples.

    From the immune system:

    Rarely: hypersensitivity.

    Rarely: anaphylactic shock.

    In isolated cases prolonged pain in the injection site.

    Overdose:

    The manifestation of drug overdose may be expressed anticholinergic action, oppression or paradoxical stimulation of the central nervous system. Symptoms of a significant overdose can be, nausea, vomiting, tachycardia, hyperthermia, drowsiness, involuntary motor activity, tremors, confusion, or hallucinations. Symptoms can be accompanied by depression of consciousness, arrhythmia, arterial hypotension, seizures, respiratory depression. A coma and a cardiopulmonary collapse may follow.

    It is necessary to control the airways, the state of respiration and circulation with continuous registration of the ECG (if necessary, provide oxygen therapy).

    Shared supportive measures including monitoring of vital body functions and monitoring of the patient until the symptoms of intoxication disappear and within the next 24 hours are shown.Patients with altered state of consciousness should be tested for the simultaneous use of other drugs or alcohol. In these cases, if necessary, oxygen therapy should be used, naloxone, glucose and thiamine.

    If it is necessary to obtain a vasopressor effect, norepinephrine or metamenamel. Epinephrine should not be appointed.

    Gastric lavage after a preliminary endotracheal intubation can be carried out when taking the drug orally in a significant amount. Hemodialysis is ineffective. There is no specific antidote.

    The literature data show that in the presence of severe, life-threatening, intractable anticholinergic effects that do not respond to other agents, it may be useful to use a therapeutic dose of physostigmine. Physostigmine should not be used only to keep the patient in a state of wakefulness. When combined with cyclic antidepressants, concomitant use of physostigmine may accelerate the onset of attacks and cardiac arrest. Also, physostigmine should be avoided in patients with cardiac conduction disorders.

    Interaction:

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

    It should avoid joint use with MAO inhibitors and holinoblokatorami.

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

    It has been established that the use of 600 mg twice a day of cimetidine increases the serum hydroxynine concentration by 36% and reduces the peak concentrations of cetirizine metabolite by 20%.

    The effect of atropine, alkaloids of belladonna, digitalis, hypotensive drugs, antagonists H1-receptors do not change under the action of hydroxysin.

    It is an inhibitor of P450 2D6 and in high doses can cause interaction with substrates CYP2D6. Since hydroxysine it is metabolized in the liver, we can expect an increase in its concentration in the blood in a joint appointment with drugs inhibitors of hepatic enzymes.

    Special instructions:

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

    During treatment with hydroxyzine, alcohol should be avoided.

    Injectable forms of the drug are intended only for intramuscular injections and should not be administered intravenously, intraarterially or subcutaneously. When intramuscular introduction, do not allow to enter the vessel. When administered under the skin, the drug can cause tissue damage, up to necrosis. After intravenous use of the solution for injection, cases of thrombophlebitis and, in rare cases, local necrosis of the tissues were reported. Intravenous use of the solution is also associated with a potential risk of accidental intraarterial injection, which leads to arterial thrombosis and subsequent tissue necrosis.

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

    Hydroxysin may impair the ability to concentrate and the speed of psychomotor reactions. Therefore, you should refrain from driving and machinery. Taking alcohol or other sedatives can enhance this effect.

    Form release / dosage:Solution for intramuscular injection, 50 mg / ml.
    Packaging:

    2 ml of the solution in the ampoule of clear glass.

    For 6 ampoules in a plastic pallet in a cardboard bundle along with instructions for use.

    Storage conditions:

    In the dark place at a temperature 15-25 FROM.

    Keep out of the reach of children.

    Shelf life:

    5 years.

    Do not take it after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:П N011405 / 02
    Date of registration:01.04.2011
    Expiration Date:Unlimited
    Date of cancellation:2018-04-12
    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: & nbsp12.04.2018
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