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Atarax® [Hydroxyzine]

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2019-09-19
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Clinical Pharmacology

Pharmacotherapeutic group: anxiolytic agent (tranquilizer)

ATX Code: [N05BB01]

Pharmacological properties

Pharmacodynamics
Hydroxysin is a first-generation H1-histamine receptor blocker, a derivative of phenothiazine with antimuscarinic and sedative properties and diphenylmethane, and contributes to the inhibition of the activity of certain subcortical zones.
It has H1-histamine blocking, bronchodilatory and antiemetic effects, has a moderate inhibitory effect on gastric secretion. Hydroxysin significantly reduces itching in patients with urticaria, eczema and dermatitis.
Hydroxysin has a positive effect on cognitive abilities, improves attention and memory. Hydroxysin does not cause addiction and psychological dependence, with prolonged use of the withdrawal syndrome is not marked. Hydroxysin is able to inhibit the central nervous system, also has an anticholinergic, antihistamine, antispasmodic, local anesthetic, sympathetic effect, has muscle relaxant activity.
In liver failure, the H1-histamine-blocking effect can be prolonged up to 96 h after a single dose. It has moderate anxiolytic activity.
Polysomnography in patients with insomnia and anxiety demonstrates lengthening the duration of sleep, reducing the frequency of nightly awakenings after taking a single or re-hydroxyzine 50 mg. A decrease in muscle tension in patients with anxiety was observed when taking the drug in a dose of 50 mg 3 times a day. The H1-histamine-blocking effect occurs approximately 1 hour after ingestion of pills. Sedation appears after 30-45 minutes.

Pharmacokinetics.

Absorption: Absorption is high. The time to reach the maximum concentration (TSmakh) after ingestion - 2 hours. After taking the average dose of 50 mg TSmah in adults is 70 mg / ml.
Distribution: The distribution coefficient is 7–16 l / kg in adults. Hydroxyzine penetrates the blood-brain barrier and the placenta, concentrating more in fetal than in maternal tissues. After ingestion, hydroxyzin penetrates the skin well, and the concentrations of hydroxyzine in the skin far exceed those in the blood serum, both after a single dose and after multiple doses. The plasma concentration of hydroxyzine does not necessarily reflect its binding to tissues or distribution in the receptors of the skin. Influences skin inflammation depending on serum concentration.
Metabolism: Hydroxysin is metabolized in the liver. Cetirizine - the main metabolite (45%) is a blocker of H1-histamine receptors. Metabolites are found in breast milk.
Excretion: The half-life (T1 / 2) in adults is 14 hours (range: 7-20 hours). The total clearance of hydroxyzine is 13 ml / min / kg. About 0.8% hydroxyzine is excreted unchanged through the kidneys. The main metabolite cetirizine is excreted mainly in the urine, also unchanged (25% of the accepted dose of hydroxyzine).
Pharmacokinetics in special groups of patients.
In elderly patients
In elderly patients, T1 / 2 was 29 hours. The volume of distribution is 22.5 l / kg. It is recommended to reduce the daily dose of hydroxyzine when prescribing for elderly patients.
Children under 1 year
In children, the total clearance is 2.5 times higher than in adults. Dose should be adjusted. The half-life is 4 hours.
Children from 1 year to 14 years
The half-life is 11 hours.
In patients with hepatic impairment
In patients with secondary liver dysfunction due to primary biliary cirrhosis, the total clearance was approximately 66% of the value recorded in healthy volunteers. In patients with liver diseases, T1 / 2 increased up to 37 hours, the concentration of metabolites in the blood serum was higher than in young patients with normal liver function.Patients with hepatic impairment are recommended to reduce the daily dose or frequency of administration.
In patients with renal failure
The pharmacokinetics of hydroxyzine was studied on the example of 8 patients with severe renal insufficiency (creatinine clearance 24 + 7 ml / min). The duration of exposure to hydroxyzine did not change significantly, while the duration of exposure to cetirizine was increased. To avoid any significant accumulation of cetirizine metabolite after repeated use of hydroxyzine in patients with impaired renal function, the daily dose of hydroxyzine should be reduced.

Indications

  • Symptomatic treatment of anxiety in adults.
  • As a sedative in the period of sedation.
  • Symptomatic treatment of allergic itch

Composition

1 tablet, film coated, contains ::

active ingredient: hydroxyzine hydrochloride 25 mg;
excipients: cornstarch pregelatinized starch 30 mg, colloidal silicon dioxide 0.7 mg, magnesium stearate 1 mg, mannitol 40 mg, microcrystalline cellulose 33.3 mg;
film coating composition: white opadry - 4 mg, including: hypromellose (hydroxypropyl methylcellulose) 1.35 mg, hyprolosis (hydroxypropyl cellulose) 1.35 mg, talc 0.8 mg, titanium dioxide 0.5 mg

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Atarax® [Hydroxyzine]

Dosage and Administration

The drug is administered orally.

Adults:

For symptomatic treatment of anxiety: a standard dose of 50 mg per day, divided into 3 doses (1/2 pills (12.5 mg) in the morning, 1/2 pills (12.5 mg) in the afternoon, and 1 tablet (25 mg at night). When anxiety in severe cases, the drug is used in a dose of 50-100 mg 4 times a day.
For symptomatic treatment of allergic itching: an initial dose of 1 tablet (25 mg) at bedtime, if necessary, the dose can be increased to 1 tablet (25 mg) 3-4 times a day.
For sedation in surgical practice: 2-8 pills (50-200 mg) at night before anesthesia.
A single maximum dose for an adult should not exceed 8 pills (200 mg), the maximum daily dose is no more than 12 pills (300 mg).
Children:
For symptomatic treatment of allergic pruritus:
At the age of 3 to 6 years: from 1.0 mg / kg / day to 2.5 mg / kg / day in several doses.
At the age of 6 years and older: from 1.0 mg / kg / day to 2.0 mg / kg / day in several doses.
For sedation: 1 mg / kg overnight before anesthesia.
The dosage is calculated by the doctor individually, depending on the child's body weight in accordance with the recommended doses, it should be noted that the minimum dosage received, after dividing the tablet, is 12.5 mg.

Use in special patient groups:
When used in the elderly, the dose is adjusted individually, taking into account associated diseases in the range of recommended doses (see Pharmacokinetics section).
Use in patients with renal failure and liver dysfunction:
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, the drug is used in half the dose due to a decrease in the excretion of the main metabolite of hydroxyzine, cetirizine.

Adverse reactions

Possible side effects are listed below for body systems and frequency of occurrence.
WHO classification of the incidence of side effects:
very often -> 1/10 of appointments (> 10%)
often from> 1/100 to <1/10 of appointments (> 1% and <10%)
infrequently - from> 1/1000 to <1/100 of appointments (> 0.1% and <1%)
rarely from> 1/10000 to <1/1000 of appointments (> 0.01% and <0.1%)
very rarely - <1/10000 appointments (<0.01%)
The most frequent adverse reactions were drowsiness, headache, lethargy, dry mouth and fatigue.
Immune system disorders:
rarely: hypersensitivity;
very rarely: anaphylactic shock.
Nervous system disorders:
infrequently: dizziness, insomnia, tremor;
seldom: spasms, dyskinesia.
Mental Disorders:
infrequently: agitation, confusion;
rarely: hallucinations, disorientation.
Violations by the organ of vision:
seldom: accommodation disturbance, visual disturbance.
Heart failure:
rarely: tachycardia;
frequency is unknown: prolongation of the QT interval on the electrocardiogram, ventricular tachycardia of the "pirouette" type.
Vascular dysfunction:
rarely: lower blood pressure.
Disorders of the respiratory system, organs of the chest and mediastinum:
very rare: bronchospasm.
Disorders of the gastrointestinal tract:
infrequently: nausea;
rarely: vomiting, constipation.
Disorders of the liver and biliary tract:
rarely: impaired liver function tests;
frequency unknown: hepatitis.
Kidney and urinary tract disorders:
rarely: urinary retention.
Violations of the skin and subcutaneous tissues:
seldom: itch, rash (erythematous, maculo-papular), urticaria, dermatitis;
very rarely: angioedema, excessive sweating, acute generalized exantomous pustular rash, erythema multiforme, Stevens-Johnson syndrome
Common disorders:
rarely: hyperthermia, malaise.
The following side effects were observed when taking cetirizine, the main metabolite of hydroxyzine: thrombocytopenia, aggression, depression, tic, dystonia, paresthesia, ocular curvature, diarrhea, dysuria, enuresis, asthenia, edema, weight gain, and can be observed when taking hydroxyzine.

Precautions: myasthenia, prostatic hyperplasia with clinical manifestations, difficulty of urination, constipation, glaucoma, dementia, convulsive disorders including epilepsy, the tendency to fibrillation, including electrolyte imbalance (hypokalemia, hypomagnesemia), patients with heart disease patients had a history (in case of heart failure and arterial hypertension) or when using drugs that can cause arrhythmia in hyperthyroidism. Hydroxysin helps reduce gastrointestinal motility, the development of stenosing peptic ulcers, respiratory failure.

Drug interactions

It is necessary to take into account the potentiating effect of hydroxyzine when used in conjunction with drugs that depress the central nervous system (CNS), such as narcotic analgesics, barbiturates, tranquilizers, hypnotics, alcohol. In this case, their doses should be adjusted individually. Concurrent use with monoamine oxidase inhibitors (MAO) and holinoblockers should be avoided. The drug interferes with the pressure of epinephrine and the anticonvulsant activity of phenytoin, and also interferes with the action of betahistine and cholinesterase inhibitors.
It was established that the use of cimetidine in a dose of 600 mg twice a day increases the concentration of hydroxyzine in serum by 36% and reduces the maximum concentration of the metabolite cetirizine by 20%.
The effect of atropine, belladonna alkaloids, cardiac glycosides, antihypertensives, H2-histamine receptor blockers do not change under the action of hydroxyzine. Hydroxyzine is an inhibitor of the CYP2D6 isoenzyme and in high doses can cause drug interactions with CYP2D6 substrates. Since hydroxyzine is metabolized in the liver, an increase in its plasma concentration can be expected with simultaneous use of microsomal liver enzymes with inhibitors. As hydroxyzine is metabolized by alcohol dehydrogenase and isoenzyme CYP3A4 / 5 may increase in plasma hydroxyzine concentration while the use of drugs, potentially inhibiting the isozyme CYP3A4 / 5 (telithromycin, clarithromycin, delavirdine, stiripentolom, ketoconazole, voriconazole, itraconazole, posaconazole and several inhibitors of HIV protease including atazanavir, indinavir, nelfinavir, ritonavir, saquinarine, lopinavir / ritonavir, saquinarine / 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 can potentially cause arrhythmia may increase the risk of prolonging the QT interval and the occurrence of ventricular tachycardia of the "pirouette" type.
The use of the drug at the same time as agents with ototoxic effects, such as gentamicin, may mask such symptoms of ototoxicity as dizziness. The drug should be canceled 3 days before the planned skin tests with allergens.

Pregnancy and Lactation

The drug Hydroxysin Canon is contraindicated in pregnancy, during childbirth and breastfeeding.

Special instructions

With simultaneous use with drugs that have m-anticholinergic properties and drugs that inhibit the central nervous system, the dose of hydroxyzine should be reduced.
Hydroxysin can lead to a prolongation of the QT interval on an electrocardiogram, so simultaneous use with other drugs that can disrupt heart activity may increase the risk of developing arrhythmias.It is assumed that other drugs that cause changes on the electrocardiogram (atropine, anti-Parkinsonian drugs, lithium carbonate, quinidine, phenothiazines, procainamide, tricyclic antidepressants, thioridazine) can aggravate and exacerbate the changes that can be caused by hydroxyzine, and increase the risk of sudden death. It is necessary to avoid the simultaneous use of two or more drugs that lengthen the QT interval, because of the danger of additive effects that may cause the development of potentially life-threatening and severe cardiac arrhythmias.
In renal and / or hepatic insufficiency, the doses should be reduced.
Elderly dosage should be selected individually, starting with half the minimum dose, and adjusting the range of recommended doses. If it is necessary to make allergy tests or to conduct a methacholine test, the hydroxyzin canon should be discontinued 5 days prior to the study in order to prevent obtaining distorted data.
During treatment with the drug Hydroxysin Canon should avoid taking alcohol.

Impact on the ability to drive vehicles and mechanisms
Hydroxysin Canon can impair the ability to concentrate and the speed of psychomotor reactions. Taking other sedative drugs may enhance this effect. Therefore, you should refrain from driving and other potentially hazardous activities that require high concentration of attention and psychomotor reactions.

Overdosage

Symptoms of toxicity on the part of the central nervous system are associated with excessive m-anticholinergic effects, suppression or paradoxical stimulation of the central nervous system. These symptoms include nausea, vomiting, tachycardia, hyperthermia, drowsiness, pupillary reflex disorder, tremor, confusion, or hallucinations. Subsequently, depression of consciousness, respiration, convulsions, lowering blood pressure, arrhythmia may develop. It is possible the coma and the cardiopulmonary collapse to worsen.
Treatment: It is necessary to monitor the condition of the respiratory tract, the state of respiration and blood circulation with the help of electrocardiographic (ECG) monitoring, to ensure adequate oxygenation. Cardiac activity and blood pressure should be monitored within 24 hours after symptoms disappear.
In large doses, hydroxyzin can lead to a prolongation of the QT interval and obvious changes on the electrocardiogram.
In case of violation of mental status, it is necessary to exclude the use of other drugs or alcohol, if necessary, the patient should be inhaled with oxygen, enter naloxone, dextrose (glucose) and thiamine. The use of analeptics is not permissible.
If it is necessary to obtain a vasopressor effect, norepinephrine or metaraminol is administered. Epinephrine should not be used. In the case of ingestion of a significant amount of the drug, you can perform a gastric lavage with previous endotracheal intubation. It is possible to use activated carbon, but there is insufficient evidence of its effectiveness. There is no specific antidote. Hemodialysis is not effective.
Literary data show that in the event of the development of severe, life-threatening, intractable m-holinoblokiruyuschih effects not controlled by other drugs, it is possible to use a therapeutic dose of physostigmine. Physostigmine should not be used only to bring the patient to consciousness. If a patient has taken tricyclic antidepressants, physostigmine can cause convulsive seizures and irreversible cardiac arrest.Physostigmine should also be avoided in patients with impaired cardiac conduction.

  • Brand name: Hydroxyzine
  • Active ingredient: Hydroxyzine
  • Dosage form: pills, film coated white, round, biconvex, with risky; in cross section, almost white.
  • Manufacturer: Canonpharma
  • Country of Origin: Russia

Studies and clinical trials of Hydroxyzine (Click to expand)

  1. Anxiolytic effect of hydroxyzine: a double-blind trial versus placebo and buspirone
  2. Hydroxyzine-associated tardive dyskinesia
  3. Precolumn fluorescence labeling method for simultaneous determination of hydroxyzine and cetirizine in human serum
  4. Prevention of “learned helplessness” in the rat by hydroxyzine
  5. Chiral separation and quantitation of cetirizine and hydroxyzine by maltodextrin-mediated CE in human plasma: Effect of zwitterionic property of cetirizine on enantioseparation
  6. Effect of hydroxyzine on attention and memory
  7. Acute effects of hydroxyzine on nocturnal sleep and sleep tendency the following day: A C-EEG study
  8. A multicentre double-blind placebo-controlled study investigating the anxiolytic efficacy of hydroxyzine in patients with generalized anxiety
  9. Effects of fexofenadine and hydroxyzine on brake reaction time during car-driving with cellular phone use
  10. Evaluation of the cognitive, psychomotor and pharmacokinetic profiles of rupatadine, hydroxyzine and cetirizine, in combination with alcohol, in healthy volunteers
  11. Turbidimetric carbamazepine immunoassay on the ADVIA® 1650 and 2400 analyzers is free from interference of antihistamine drugs hydroxyzine and cetirizine
  12. Analytical performance evaluation of ADVIA Chemistry Carbamazepine_2 assay: minimal cross-reactivity with carbamazepine 10, 11-epoxide and none with hydroxyzine or cetirizine
  13. Comparative studies on distribution, excretion, and metabolism of Hydroxyzine-3H and its methiodide-14C in rats
  14. Effect of UV irradiation and tritiation on hydroxyzine
  15. Sensitive assay for determination of hydroxyzine in plasma and its human pharmacokinetics
  16. Simultaneous determination of hydroxyzine hydrochloride and benzyl alcohol in injection solutions by high-performance liquid chromatography
  17. Determination of prednisolone in the presence of hydroxyzine and in formulations containing analgesics
  18. Determination of colloidal electrolytes: conductimetric titration of hydroxyzine hydrochloride with ammonium molybdate
  19. Transport of hydroxyzine and triprolidine across bovine olfactory mucosa: Role of passive diffusion in the direct nose-to-brain uptake of small molecules
  20. Gas chromatographic identification and quantification of hydroxyzine: Application in a fatal self-poisoning
  21. Hydroxyzine, promethazine and thioridazine interaction with phospholipid monomolecular layers at the air–water interface
  22. PIII-76A study to evaluate the pharmacokinetics of pamoic acid following oral administration as hydroxyzine pamoate (Vistaril®) in healthy male subjects
  23. Simultaneous determination of ephedrine sulfate, hydroxyzine hydrochloride and theophylline in tablets by reversed-phase high-performance liquid chromatography
  24. Hydroxyzine inhibits experimental allergic encephalomyelitis (EAE) and associated brain mast cell activation

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