What does atarax do? Atarax: instructions, application, reviews. Atarax and anesthesia


A derivative of diphenylmethane, it has moderate anxiolytic activity.
Drug: ATARAX®
Active substance of the drug: hydroxyzine
ATX encoding: N05BB01
KFG: Tranquilizer (anxiolytic)
Registration number: P No. 011405/02
Registration date: 05/26/06
Owner reg. credential: UCB S.A. PHARMA SECTOR (Belgium)

Atarax release form, drug packaging and composition.

White coated tablets with a score line.
Film-coated tablets
1 tab.
hydroxyzine hydrochloride
25 mg

Excipients: lactose monohydrate, microcrystalline cellulose, colloidal silicon anhydride, magnesium stearate, titanium dioxide (E171), hydroxypropyl methylcellulose, macrogol.

25 pcs. - blisters (1) - cardboard packs.

The solution for intramuscular administration is colorless, transparent.
Solution for intramuscular administration
1 ml
1 amp.
hydroxyzine hydrochloride
50 mg
100 mg

Excipients: sodium hydroxide, water for injection.

2 ml - ampoules (6) - plastic trays (1) - cardboard packs.

The description of the drug is based on the officially approved instructions for use.

Pharmacological action of Atarax

A derivative of diphenylmethane, it has moderate anxiolytic activity; It also has a sedative, antiemetic, antihistamine and m-anticholinergic effect. Blocks central m-cholinergic receptors and histamine H1 receptors and inhibits the activity of certain subcortical zones. Does not cause mental dependence or addiction. The clinical effect occurs 15-30 minutes after taking the drug orally.

Has a positive effect on cognitive abilities, improves memory and attention. Relaxes skeletal and smooth muscles, has bronchodilator and analgesic effects, and a moderate inhibitory effect on gastric secretion. Hydroxyzine significantly reduces itching in patients with urticaria, eczema and dermatitis. With long-term use, there was no withdrawal syndrome or deterioration of cognitive functions. Polysomnography in patients with insomnia and anxiety clearly demonstrates an increase in sleep duration and a decrease in the frequency of night awakenings after a single or repeated dose of hydroxyzine at a dose of 50 mg. A decrease in muscle tension in patients with anxiety was noted when taking the drug at a dose of 50 mg 3 times a day.

Pharmacokinetics of the drug.

Suction

Hydroxyzine is rapidly absorbed from the gastrointestinal tract. Cmax is observed 2 hours after taking the drug.

After a single dose of the drug in a single dose of 25 mg or 50 mg in adults, the plasma concentration is 30 ng/ml and 70 ng/ml, respectively.

Bioavailability when taken orally and intramuscularly is 80%.

Distribution

Hydroxyzine is more concentrated in tissues (particularly skin) than in plasma. The distribution coefficient is 7-16 l/kg.

Hydroxyzine passes through the BBB and the placental barrier, while concentrating to a greater extent in the tissues of the fetus than in the mother's body. Metabolites are found in breast milk.

Metabolism and excretion

Hydroxyzine is biotransformed in the liver; the main metabolite (45%) is cetirizine, which is a histamine H1 receptor blocker. The total clearance of hydroxyzine is 13 ml/min/kg. T1/2 in adults is 14 hours. Only 0.8% of hydroxyzine is excreted unchanged in the urine.

Pharmacokinetics of the drug.

in special clinical cases

In children, the total clearance is 4 times less than in adults, T1/2 in children aged 14 years is 11 hours, in children aged 1 year - 4 hours.

In elderly patients, T1/2 is 29 hours, the distribution coefficient is 22.5 l/kg.

In patients with impaired liver function, T1/2 increases to 37 hours, the concentration of metabolites in the blood serum is higher than in young patients with normal liver function. The antihistamine effect can last for 96 hours.

Indications for use:

Adults: to relieve anxiety, psychomotor agitation, feelings of internal tension, increased irritability in neurological, mental (including generalized anxiety, adaptation disorders) and somatic diseases, chronic alcoholism; withdrawal syndrome in chronic alcoholism, accompanied by psychomotor agitation;

As a sedative during premedication;

Skin itching (as symptomatic therapy).

Dosage and method of administration of the drug.

The drug is taken orally or administered intramuscularly.

For the symptomatic treatment of itching in children aged 12 months to 6 years, the drug is prescribed in a daily dose of 1-2.5 mg/kg body weight in several doses; children over 6 years of age - at a dose of 1-2 mg/kg/day in several doses.

For premedication in children, the drug is prescribed at a dose of 1 mg/kg body weight 1 hour before surgery, and additionally in the evening before surgery.

For the symptomatic treatment of anxiety, adults are prescribed a dose of 25-100 mg/day in several doses during the day or at night. The average dose is 50 mg/day (12.5 mg in the morning, 12.5 mg in the afternoon and 25 mg at night). If necessary, the dose can be increased to 300 mg/day.

For premedication in surgical practice, it is administered intramuscularly at a dose of 50-200 mg (1.5-2.5 mg/kg) 1 hour before surgery, and also additionally in the evening before surgery.

For the symptomatic treatment of itching, the initial dose is 25 mg; if necessary, the dose can be increased 4 times (25 mg 4 times a day).

The maximum single dose should not exceed 200 mg, the maximum daily dose is no more than 300 mg.

Patients with moderate to severe renal insufficiency, as well as hepatic insufficiency, require a dose reduction.

In elderly patients, the initial dose should be reduced by 2 times in case of reduced glomerular filtration.

Side effects of Atarax:

Side effects associated with anticholinergic effects: rarely (mainly in elderly patients) - dry mouth, urinary retention, constipation, impaired accommodation.

From the central nervous system: drowsiness, general weakness (especially at the beginning of treatment), headache, dizziness. If weakness and drowsiness do not disappear after a few days from the start of therapy, the dose of the drug must be reduced.

From the cardiovascular system: arterial hypotension, tachycardia.

From the digestive system: nausea, changes in liver function tests.

Other: increased sweating, allergic reactions, fever, bronchospasm.

When using the drug in recommended doses, no clinically significant respiratory depression was observed. Involuntary motor activity (including very rare cases of tremors and convulsions), disorientation were observed with significant overdose.

Side effects observed when taking Atarax are usually mild, transient and disappear within a few days of starting treatment or after reducing the dose.

Contraindications to the drug:

Porphyria;

Pregnancy;

Period of labor;

Lactation period (breastfeeding);

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

The drug should be prescribed with caution for myasthenia gravis, prostatic hyperplasia with clinical manifestations, difficulty urinating, constipation, increased intraocular pressure, dementia, a tendency to seizures, a predisposition to the development of arrhythmia, and with the simultaneous use of drugs that have arrhythmogenic effects. When used concomitantly with other CNS depressants or anticholinergics, the dose should be reduced.

Use during pregnancy and lactation.

Atarax is contraindicated for use during pregnancy and labor.

If it is necessary to use Atarax during lactation, breastfeeding should be stopped.

Special instructions for the use of Atarax.

If allergy tests are necessary, Atarax should be discontinued 5 days before the test.

Injection forms of the drug are intended for intramuscular administration only. Atarax should not be administered intravenously, intravenously, or subcutaneously. When administered subcutaneously, the drug may cause tissue damage. When administering intramuscularly, make sure that the needle does not enter the vessel.

Patients taking Atarax should avoid drinking alcohol.

Impact on the ability to drive vehicles and operate machinery

Patients taking Atarax, if necessary to drive a car or operate machinery, should be warned that the drug may affect concentration and the speed of psychomotor reactions.

Drug overdose:

Symptoms: increased anticholinergic effects, depression or paradoxical stimulation of the central nervous system, nausea, vomiting, involuntary motor activity, hallucinations, impaired consciousness, arrhythmia, arterial hypotension; rarely - tremors, convulsions, disorientation, which occur when the recommended doses are significantly exceeded.

Treatment: if spontaneous vomiting is absent, it is necessary to induce it artificially or perform gastric lavage. Carry out general measures aimed at maintaining the vital functions of the body, and monitor the patient until the symptoms of intoxication disappear in the next 24 hours.

If it is necessary to obtain a vasopressor effect, norepinephrine or metaramenol is prescribed. Epinephrine should not be used. There is no specific antidote. The use of hemodialysis is ineffective.

Interaction of Atarax with other drugs.

Atarax potentiates the effect of drugs that depress the central nervous system, such as opioid analgesics, barbiturates, tranquilizers, hypnotics, ethanol (alcohol), which requires dose adjustment when these drugs are administered simultaneously with Atarax.

Atarax, when used simultaneously, interferes with the pressor effect of epinephrine (adrenaline) and the anticonvulsant activity of phenytoin, and also interferes with the action of betahistine and cholinesterase blockers.

With simultaneous use, Atarax does not affect the activity of atropine, belladonna alkaloids, cardiac glycosides, antihypertensive drugs, histamine H2 receptor blockers; Co-administration with MAO inhibitors and anticholinergics should be avoided.

Hydroxyzine is an inhibitor of the 2D6 isoenzyme of the cytochrome P450 system and, when used in high doses, may cause interaction with CYP2D6 substrates. Since hydroxyzine is metabolized in the liver, an increase in its concentration in the blood can be expected when co-administered with liver enzyme inhibitors.

Terms of sale in pharmacies.

The drug is available with a prescription.

Terms of storage conditions for the drug Atarax.

The drug should be stored in a dry place at a temperature not exceeding 25°C, out of the reach of children. Shelf life: 5 years.

Atarax (Latin Atarax) is a common tranquilizer that is not addictive. Let's look at what this medicine helps with and whether there are any substitutes.

Indications for use

These tablets should be taken for panic attacks, insomnia, allegri, which is accompanied by itching, urticaria, nervous tics and eczema. Since these pills are sedative, they are prescribed to women during menopause. For men, it is indicated for chronic alcoholism. According to doctors, adults should drink the remedy for internal anxiety and tension, as well as before surgery.

Composition, types, how much it costs

International name of the drug (INN): Hydroxyzine hydrochloride, this is the active substance. The abstract states that excipients include:
ICC
magnesium stearate
silicon colloidal anhydride
lactose monohydrate
titanium dioxide
hydroxypropyl methylcellulose
macrogoal

The release form of the medicine comes in the form of a solution for injections and tablets. Tablets can be covered with either a hard shell or a film. Photos of each unit are available on the Internet. The tablets are produced in a blister containing 25 pieces. The package contains 1 blister. Ampoules in a package of 6 pcs. The shelf life of hydroxyziline is 5 years. The pharmacological drug is sold according to a doctor's prescription. Its cost varies from 296-318 rubles.

Analogs

There are times when an antidepressant is simply not suitable for the patient. This happens when an allergy to some component occurs or the medicine does not provide a positive effect. Therefore, you can replace Atarax with its analogue. Wikipedia suggests the following drugs:

  • 1. Grandaxin
  • 2. Afobazole
  • 3. Phenibut
  • 4. Teraligen
  • 5. Corvalol
  • 6. Adaptol
  • 7. Vidal
  • 8. Amitriptyline
  • 9. Mexidol
  • 10. Strezam
  • 11. Cipralex

How long can I take it without a break?

The description of the drug says that Atarax is a strong tranquilizer. In terms of time, you cannot drink it without a break for longer than 14 days, and preferably 10. But the main course is prescribed by a doctor, since each disease has its own nuances.

Instructions for use Atarax

You need to take the tablets an hour before meals, and administer the solution later - 30 minutes. Symptomatic anxiety in adults requires 25-100 ml during the day intermittently. The optimal dosage is 50 ml per day. Complex syndrome requires taking 300 mg per day. Before surgery, 50-200 mg may be prescribed one hour before surgery.

Symptomatic itching should be treated at a dose of 25 mg; if the drug has little effect, then increase it up to 4 times a day, as well as at night. A single dose cannot exceed 200 mg.

Dosage for children

The manufacturer does not recommend taking the medicine to children under one year of age. From one to six years old, you should give 1-2 mg per kilogram of weight, divided into morning and evening. Over 6 years of age, it is recommended to use the drug at least two mg/kg per day. For insect bites, half a tablet is enough for a child. In individual cases, a specialist prescription is needed.

For neurosis

For chronic neurosis, the medicine is prescribed in a dosage of 100-150 mg per day and always before bedtime. The sedative acts like a sleeping pill, so you should not drive a vehicle after taking it. The course of treatment for neurosis depends on the manifestation of the disease. The minimum period is 7-10 days. However, the duration of treatment can be increased, while the amount of medication per day is halved.

During pregnancy

During pregnancy and breastfeeding, Atarax is strictly prohibited. Its active drug enters the blood, placenta and milk. You must stop feeding if you take this medicine.

Nervous disorders in children often require the use of medications called anxiolytics. Their main effect is to reduce anxiety and fears. One such remedy is Atarax. Is it possible to give it to a child, when should it be done and in what dosage should it be used when treating children?

Release form

The drug is produced:

  • In tablets. This form of Atarax is represented by oblong tablets, which have a transverse dividing line. These tablets are coated with a white coating and placed in blisters of 25 pieces. One cardboard pack includes 1 blister.
  • In solution. This clear, colorless liquid is intended for intramuscular injections, therefore it is bottled in 2 ml ampoules. One pack contains 6 ampoules.

Compound

The active substance of Atarax is represented by hydroxyzine in the form of hydrochloride. One tablet contains 25 mg of this compound, and 1 ml of the injection form contains 50 mg (one ampoule of the drug contains 100 mg).

The tablet form of the drug additionally includes silicon anhydride, lactose, microcrystalline cellulose and other substances that provide the tablets with hardness and shape. In the Atarax solution, the only auxiliary components are sodium hydroxide and sterile water.

Operating principle

The main ingredient of Atarax is a histamine receptor blocker (H1 receptors). It has a sedative effect. It is thanks to him that the medicine is considered an anxiolytic. The drug helps:

  • Calm the anxiety.
  • Reduce the manifestations of nervous system excitation.
  • Eliminate the feeling of internal tension.
  • Reduce irritability.
  • Improve memory and attention.

At the same time, such a medicine does not provoke addiction, and if you take it for a long time, the completion of treatment does not lead to withdrawal syndrome.

Atarax also has the properties of dilating the bronchi, blocking vomiting and reducing the secretion of gastric juice. For allergic skin diseases, the active substance Atarax effectively eliminates itching.

Indications

In childhood, Atarax is often prescribed to eliminate itching caused by allergies. This medication is also often included in the complex of drugs used in surgical treatment.

In neurology, Atarax is used:

  • With neurosis.
  • For organic pathologies of the central nervous system, the symptoms of which are nervous excitement and anxiety.
  • After a concussion or brain injury, if the child has anxiety and other nervous disorders.
  • With neurotic enuresis.
  • For panic attacks, manifested by lack of air, nausea, dizziness, fear of death and other symptoms.
  • For genetic disorders of the central nervous system, for example, Tourette's disease.

For more information about the use of the drug Atarax, watch the video:

At what age is it allowed to take it?

The instructions for use of Atarax prohibit the treatment of infants under one year old with this drug. For children aged 1 year, the drug can only be prescribed as intramuscular injections. Atarax can be taken orally by children over 3 years of age. However, it is not recommended to give this medicine without consulting a doctor.

Contraindications

The use of Atarax in children is prohibited not only at an early age, but also in cases of hypersensitivity to its active substance. You should not give the medicine if you are intolerant to aminophylline, cetirizine or ethylenediamine.

Due to the presence of lactose, tablets are not prescribed for problems with galactose or glucose metabolism. The injection form of the drug cannot be injected into a vein, artery or under the skin. Porphyria is also a contraindication for treatment with Atarax. This medicine is not prescribed for adults during pregnancy and breastfeeding.

If the child's liver function is impaired or kidney failure has developed, the dosage of Atarax should be reduced. Convulsive disorders, hyperthyroidism and cardiovascular diseases in the child also require dose adjustment and pediatrician attention.

Side effects

The most common negative effect of Atarax treatment is drowsiness and a feeling of lethargy. Also, many patients experience headaches and increased fatigue from taking this drug.

Less commonly, the medicine provokes:

  • Allergies.
  • Insomnia.
  • Nausea.
  • Dizziness.
  • Tremor.
  • Dermatitis.
  • Excited state.
  • Confused consciousness.
  • Cardiopalmus.
  • Temperature increase.
  • Cramps.
  • Decreased blood pressure.
  • Constipation.
  • Vomiting.
  • Urinary disorders.
  • Pain at the injection site (for injection use).

Very rare side effects include angioedema, anaphylaxis, bronchospasm, hallucinations, problems with vision and spatial orientation. Sometimes Atarax causes hepatitis.

Instructions for use and dosage

  • The daily dose of Atarax for itching is calculated based on the baby’s body weight. At the age of 1-6 years, it is from 1 to 2.5 mg of the active drug compound per kilogram of weight, and for children over six years of age - from 1 to 2 mg. The calculated amount is divided into several doses.
  • If the drug is used during surgical treatment, the dosage will be 1 mg for each kg of the child’s body weight. This amount of Atarax is given one hour before surgery.
  • How long a child needs to take the drug is determined by the doctor individually in each case.

Overdose

If you give a child Atarax in a larger dose than prescribed, it will negatively affect the central nervous system, causing nausea, increased heart rate, increased body temperature, and a feeling of drowsiness. Serious poisoning will lead to tremors, hallucinations, depression of consciousness, arrhythmia, respiratory failure and even coma.

If the drug was taken orally and an overdose was detected immediately, perform gastric lavage and immediately call an ambulance. Doctors will perform intubation if necessary, monitor breathing and circulation, and prescribe symptomatic medications.

Interaction with other drugs

If you take Atarax together with other medications that have a depressant effect on the nervous system, this therapeutic effect will be enhanced. This interaction is observed with barbiturates, hypnotics, tranquilizers and narcotic analgesics.

You should not prescribe Atarax and anticholinergic drugs at the same time, or combine this drug with MAO inhibitors. Atarax does not affect treatment with antihypertensive drugs, H2-histamine blockers, atropine or cardiac glycosides.

Terms of sale

To buy Atarax at a pharmacy, you need to show a prescription written by your doctor. The price of 25 tablets of this drug is about 280-300 rubles.

Storage conditions and shelf life

The medicine should be kept out of the reach of small children, where the temperature will not exceed +25°C. Treatment with Atarax, which has expired (5 years), is not recommended.

First of all, it should be noted that Atarax belongs to the pharmacological group of anxiolytic drugs, that is, it is a sedative antihistamine. It is produced in the form of a solution for intramuscular administration and in the form of film-coated tablets.

The dominant element is hydroxyzine, which, in turn, penetrating the brain, blocks the productivity of histamine receptors, and the patient feels excessive drowsiness. That is why, given this nuance, Atarax is preferred to be used at night.

In addition, this medication is not addictive, and its effect occurs within half an hour after taking one tablet. Thanks to the effects of hydroxyzine, patients noticeably improve memory and concentration, and also experience relaxation of skeletal and smooth muscles, an analgesic effect and a moderate inhibitory effect on gastric secretion.

If we talk about analogues of Atarax, there are quite a lot of them, for example, Stremaza, Vinpotropil and other no less prominent representatives of this pharmacological group.

Atarax: indications and contraindications

First, you need to clarify that Atarax is more of an “adult” drug (although sometimes it is prescribed to children), which is very often recommended for various degrees of neuralgia, to suppress anxiety, as a powerful sedative for stress, and also in the presence of unbearable skin itching allergic in nature.

However, do not forget that this sedative has its own clinical contraindications, which also must be taken into account before starting treatment. First of all, Atarax is prohibited during pregnancy, children under six months, and also with a diagnosis of porphyria. It should be used with caution in patients with impaired renal function or reduced intestinal activity; as well as in identifying diseases such as dementia, epilepsy, arrhythmia and glaucoma.

Atarax: Side effects and overdose

Since Atarax has a direct effect on the central nervous system, to one degree or another suppressing the functioning of its receptors, certain side effects have been identified that worsen with its systematic use. Thus, some patients complain of excessive drowsiness, periodic dizziness, dry mouth, weakness throughout the body, migraine attacks, problems with urination, insomnia, tachycardia, tremors of the limbs, convulsions, as well as significant disturbances in the digestive process.

In case of an overdose of Atarax, the patient’s depressed state may be depressed and his attacks of unreasonable panic may worsen.

Atarax: Instructions for use

If we talk about the method of using this medication, then it is important to clarify that the detailed instructions for Atarax, of course, contain descriptions of daily doses in each clinical case, but your treatment must be fully discussed with a specialist, otherwise the consequences may be extremely undesirable. In addition, recommended dosages vary significantly, depending on a number of factors.

Features of treatment with Atarax

Atarax should be prescribed exclusively by a knowledgeable specialist, who must also specify the dosage, individual in each clinical case. In addition, due to the sedative effect while using Atarax, it is better to completely abandon all types of work related to responsibility for your life and the lives of other people. If the patient’s work is directly related to driving a car, for example, then using this drug for treatment is not recommended. Also, the course of treatment should not be accompanied by alcohol consumption.

An important point is that the use of Atarax when combined with certain medications can only worsen side effects. So, when using antipsychotic medications, for example, the patient experiences more frequent attacks of dizziness, nausea, and muscle weakness becomes much more noticeable.

That is why, during treatment with Atarax, the use of barbiturates, benzodiazepines, sleeping pills, painkillers containing opium, as well as tricyclic antidepressants is prohibited. You should also not use other antihistamines with a sedative effect, including Chlorphenamine and Promethazine. Psychotic drugs, antispasmodics and MAO inhibitors are also prohibited.

Atarax: Patient reviews of the drug

To be honest, reviews about Atarax are controversial, since this drug “suited” some patients, but only harmed others. Perhaps this is due to the specifics of each organism, but the majority of comments found on various medical forums on the Internet were approximately the following: “The nervous system has noticeably calmed down, but the general condition has become worse than ever: constant apathy, drowsiness and excessive fatigue.” From this we can conclude that Atarax “works”, but can cause side effects.

The average price for Atarax amp 2ml No. 6 is 300 rubles.


05:36 Atarax: instructions, application, reviews -

Today, stress has become a common phenomenon in modern society. Many people are not able to cope with emotional shocks and anxiety on their own, which is why the medical drug Atarax is very popular. General information about the drug Atarax First of all, it should be noted that Atarax belongs to the pharmacological group of anxiolytic drugs, that is, it is a sedative antihistamine. It is produced in the form of a solution for intramuscular [...]


Atarax: instructions for use and reviews

Latin name: Atarax

ATX code: N05BB01

Active substance: hydroxyzine

Manufacturer: USB Pharma S.A. (USB Pharma, S.A.) (Belgium), Laboratoires Thissen (Belgium)

Updating the description and photo: 19.08.2019

Atarax is a tranquilizer used to relieve itching, reduce anxiety and psychomotor agitation. It has a moderate anxiolytic, as well as antiemetic, sedative, analgesic, antihistamine and m-anticholinergic effect.

Release form and composition

Dosage forms of Atarax:

  • film-coated tablets: oblong, white, with a transverse line on both sides (25 pcs. in blisters of PVC-Al foil, 1 blister in a cardboard pack);
  • solution for intramuscular administration: transparent, colorless (2 ml in transparent glass ampoules, 6 ampoules in plastic trays, 1 tray in a cardboard box).

Composition of 1 tablet:

  • active substance: hydroxyzine hydrochloride – 25 mg;
  • auxiliary components: lactose monohydrate, MCC (microcrystalline cellulose), magnesium stearate, colloidal silicon dioxide (anhydrous);
  • shell: Opadry Y-1-7000 (titanium dioxide, hypromellose, macrogol 400).

Composition of 1 ampoule (2 ml solution):

  • active substance: hydroxyzine hydrochloride – 100 mg;
  • auxiliary components: sodium hydroxide and water for injection.

Pharmacological properties

Pharmacodynamics

Hydroxyzine is a diphenylmethane derivative that inhibits the activity of certain subcortical zones. It has moderate anxiolytic activity and a moderate inhibitory effect on gastric secretion. It has a sedative, H1-histamine-blocking, M-anticholinergic and antiemetic effect. It also has an antipruritic effect against urticaria, eczema and dermatitis.

In patients with insomnia and anxiety, polysomnography demonstrates an increase in sleep duration and a decrease in the frequency of night awakenings after a single or repeated dose of the drug at a dose of 50 mg. A decrease in muscle tension in patients with anxiety was noted when using Atarax at a dose of 50 mg 3 times a day.

Hydroxyzine does not cause addiction or mental dependence. With long-term treatment, it does not cause deterioration in cognitive functions and the development of withdrawal syndrome.

The sedative effect develops within 30–45 minutes.

The H1-histamine blocking effect occurs approximately 1 hour after taking the drug. In liver failure, this effect can last up to 96 hours after a single dose.

Hydroxyzine has a moderate analgesic effect and has sympatholytic and antispasmodic activity.

Pharmacokinetics

After a single IM dose of 50 mg, the maximum concentration (Cmax) is approximately 65 ng/ml.

Hydroxyzine, when taken orally, is well absorbed from the gastrointestinal tract. The maximum concentration is observed after 2 hours and is 30 ng/ml in adults when taking a dose of 25 mg, 70 ng/ml when taking a dose of 50 mg. Bioavailability – 80%.

Hydroxyzine is concentrated more in tissues than in plasma. The distribution coefficient in adults is 7–16 l/kg. Passes through the blood-brain barrier and the placenta, concentrating predominantly in fetal rather than maternal tissues. Hydroxyzine metabolites pass into breast milk. After oral administration, the drug penetrates well into the skin, where the concentration is much higher than the level in the blood serum (both after a single and after multiple doses).

The drug is metabolized in the liver, the main metabolite (45%) is cetirizine, a pronounced H1 blocker. The total clearance is 13 ml/min/kg. Only 0.8% of hydroxyzine is excreted unchanged through the kidneys. Cetirizine is excreted in the urine mainly unchanged (16% of the intramuscular dose of the drug, 25% of the dose taken orally).

The total clearance of hydroxyzine is 13 ml/min/kg. In children this figure is 2.5 times less than in adults.

The half-life (T ½) in adults is on average 14 hours (from 7 to 20 hours), in children aged 14 years – 11 hours, in children aged 1 year – 4 hours.

In elderly patients, the distribution coefficient is 22.5 l/kg. Indicator T ½ = 29 hours.

In the presence of concomitant liver diseases, the T ½ value increases to 37 hours, the concentration of metabolites in the blood serum is higher than in patients with normal hepatic function.

In renal failure, the AUC (area under the concentration-time curve) does not change significantly, but the duration of cetirizine exposure increases. Hemodialysis does not remove this metabolite from the body.

Indications for use

According to the instructions, Atarax is prescribed to adults:

  • Relief of psychomotor agitation, anxiety, increased irritability and feelings of internal tension in mental, neurological and somatic diseases;
  • Treatment of withdrawal syndrome in chronic alcoholism, which is accompanied by psychomotor agitation;
  • Symptomatic treatment of skin itching.

In pediatrics, the drug is used for premedication and symptomatic treatment of itching of allergic origin.

Contraindications

The use of Atarax is contraindicated in case of porphyria, hypersensitivity to the components of the drug, pregnancy, as well as during labor and lactation.

The drug is used with caution:

  • Myasthenia;
  • Predisposition to the development of arrhythmia;
  • Difficulty urinating;
  • Increased intraocular pressure;
  • Tendency to seizures;
  • Prostatic hyperplasia with clinical manifestations;
  • Constipation;
  • Dementia.

Instructions for use of Atarax: method and dosage

Solution for intramuscular administration

In the form of a solution, Atarax is administered intramuscularly.

  • premedication: 1 mg/kg body weight 1 hour before surgery, if necessary, the same dose can be administered the night before anesthesia;
  • symptomatic treatment of itching: children 1–6 years old – 1–2.5 mg/kg per day in several doses, children over 6 years old – 1–2 mg/kg per day in several doses.
  • premedication: 50–200 mg 1 hour before surgery, if necessary, the same dose can be administered at night before anesthesia;
  • symptomatic treatment of itching: at the beginning of treatment - 25 mg 1 time per day, if necessary, increase the dose to 25 mg 4 times per day;
  • symptomatic treatment of anxiety: morning and afternoon – 12.5 mg, at night – 25 mg (total daily dose – 50 mg). In serious cases, the daily dose may be increased to 300 mg.

The maximum permissible doses of Atarax: single - 200 mg, daily - 300 mg.

The initial dose for elderly patients is reduced by 2 times.

A dose reduction is required in patients with renal and/or hepatic insufficiency. In case of insufficient liver function, a dose reduction of 33% is recommended.

Film-coated tablets

Atarax is taken orally. The initial daily dose for the symptomatic treatment of itching is 25 mg, if necessary it can be increased to 100 mg (4 doses of 25 mg), while the maximum dose should not exceed 300 mg per day and 200 mg at a time.

The daily dose of Atarax for adults to relieve anxiety symptoms is 50 mg and in severe cases can be increased to 300 mg. A quarter of the daily requirement should be taken in the morning and afternoon, the rest - before bed.

In old age, as well as in cases of renal and liver failure, it is recommended to reduce the dose of the drug by half.

For premedication for children, Atarax is prescribed at a dose of 1 mg per kilogram of body weight. Take the drug the night before anesthesia.

For the symptomatic treatment of itching in children, the drug is prescribed depending on age:

  • 3–6 years: 1–2.5 mg/kg/day (in several doses);
  • from 6 years and older: 1–2 mg/kg/day (in several doses).

Side effects

The use of Atarax may cause the following side effects:

  • Headache, drowsiness, general weakness and dizziness (if symptoms do not go away a few days after starting the drug, the dose taken must be reduced);
  • Arterial hypotension and tachycardia;
  • Nausea, changes in liver function tests;
  • Increased sweating, fever, allergic reactions and bronchospasm.

In old age, taking the drug can lead to the development of accommodation disorders, urinary retention, dry mouth and constipation.

Overdose

An overdose of Atarax is usually manifested by a pronounced anticholinergic effect, depression or paradoxical stimulation of the central nervous system. If the recommended dose is significantly exceeded, the following symptoms may occur: nausea, vomiting, drowsiness, hallucinations or confusion, tremor, involuntary motor activity, hyperthermia, tachycardia. Arrhythmia, arterial hypotension, convulsions, depression of consciousness and breathing may also occur, resulting in coma and cardiopulmonary collapse.

In case of overdose, maintenance therapy is indicated, including monitoring the patient until the symptoms of intoxication disappear and the next 24 hours, monitoring the vital functions of the body, including the respiratory tract, blood circulation, cardiovascular activity and blood pressure. Oxygen therapy is provided if necessary.

Patients with altered mental status should be assessed for concomitant use of alcohol or other drugs. In these cases, if necessary, oxygen inhalation is performed, glucose (dextrose), thiamine, and naloxone are administered.

To obtain a vasopressor effect, metaraminol or norepinephrine is prescribed. Epinephrine should not be used.

If the dose of Atarax in tablets is significantly exceeded, gastric lavage can be performed after preliminary endotracheal intubation. There is no specific antidote for hydroxyzine. Hemodialysis is ineffective.

According to the literature, with the development of severe and life-threatening anticholinergic effects that cannot be treated with other means, it is possible to use physostigmine in a therapeutic dose. However, this drug should not be used only to maintain the patient's state of wakefulness, and it is not recommended for use in patients with cardiac conduction disorders. It is important to consider that in combination with cyclic antidepressants, physostigmine can accelerate the development of attacks and cardiac arrest.

special instructions

Atarax should be used with caution in combination with drugs that depress the central nervous system: tranquilizers, ethanol, opioid analgesics, barbiturates and hypnotics.

The drug should not be taken simultaneously with MAO inhibitors and anticholinergics.

Impact on the ability to drive vehicles and complex mechanisms

During the period of use of Atarax, the speed of reactions and the ability to concentrate may deteriorate. This effect may be enhanced by concomitant use of other sedatives. During therapy, it is recommended to refrain from performing potentially hazardous activities, including driving vehicles and operating complex machinery.

Use during pregnancy and lactation

Atarax is contraindicated for use during pregnancy and lactation.

Use in childhood

In the form of a solution for intramuscular administration, Atarax is contraindicated in children under 1 year old, in the form of tablets - up to 3 years old.

The dose for children is adjusted depending on age and body weight.

For impaired renal function

In patients with impaired renal function, with repeated use of the drug, accumulation of cetirizine (hydroxyzine metabolite) is possible, and therefore it is recommended to reduce the dose of Atarax for this category of patients.

For liver dysfunction

Use in old age

Drug interactions

Hydroxyzine does not affect the action of H2-histamine receptor blockers, cardiac glycosides, antihypertensive drugs, belladonna alkaloids and atropine.

The effect of hydroxyzine is potentiated by the simultaneous use of drugs that depress the central nervous system, such as ethanol, hypnotics, barbiturates, narcotic analgesics, and tranquilizers. If their combined use is necessary, individual dosage selection is required. You should refrain from drinking alcohol during treatment.

As an inhibitor of the CYPD6 isoenzyme, in high doses, hydroxyzine can interact with substrates of the CYP2D6 isoenzyme.

Hydroxyzine interferes with the action of cholinesterase inhibitors and betahistine, the pressor effect of epinephrine, and the anticonvulsant activity of phenytoin.

Cimetidine, administered twice daily at a dose of 600 mg, increases the serum concentration of hydroxyzine by 36% and reduces the maximum concentration of its main metabolite cetirizine by 20%.

Hydroxyzine is metabolized in the liver, so its concentration in the blood may increase with the combined use of inhibitors of microsomal liver enzymes.

With the simultaneous use of drugs that can cause arrhythmia, the risk of prolongation of the QT interval and the development of torsade de pointes (TdP) increases.

The CYP3A4/5 isoenzyme and alcohol dehydrogenase are involved in the metabolism of hydroxyzine, which is why it is possible to increase the plasma concentration of the drug with simultaneous use of drugs that can inhibit the CYP3A4/5 isoenzyme, such as ketoconazole, itraconazole, voriconazole, clarithromycin, telithromycin, delavirdine, stiripentol , posaconazole, some HIV protease inhibitors, including nelfinavir, indinavir, saquinarine, ritonavir, atazanavir, saquinarine/ritonavir, lopinavir/ritonavir, tipranavir/ritonavir. However, inhibition of one metabolic pathway may be partially compensated by the activity of another.

Analogs

Analogues of Atarax are Phenazepam, Relium, Relanium, Elenium, Sibazon, Diazepam, Gidazepam, Tazepam, Grandaxin, Anvifen, Phenorelaxan, etc.

Storage conditions and periods

A prescription drug with a shelf life of 5 years should be stored at a temperature not exceeding 25 °C.

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