Atarax
Atarax: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Atarax
ATX code: N05BB01
Active ingredient: hydroxyzine
Manufacturer: YUSB Pharma S. A. (USB Pharma, SA) (Belgium), Laboratoires Thissen (Belgium)
Description and photo update: 2019-19-08
Prices in pharmacies: from 263 rubles.
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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, on both sides there is a transverse risk (25 pcs. in blisters made of PVC-Al foil, 1 blister in a cardboard box);
- 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);
- sheath: Opadray 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 a moderate anxiolytic activity and a moderate inhibitory effect on gastric secretion. It has a sedative, H 1 -histamine blocking, M-anticholinergic and antiemetic effect. It also has an antipruritic effect on urticaria, eczema and dermatitis.
In patients with insomnia and anxiety, polysomnography shows an increase in sleep duration and a decrease in the frequency of nocturnal awakenings after a single or repeated administration 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 is not addictive and non-addictive. With long-term treatment, it does not cause a deterioration in cognitive functions and the development of a withdrawal syndrome.
Sedation develops within 30–45 minutes.
H 1 -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, has sympatholytic and antispasmodic activity.
Pharmacokinetics
After a single intramuscular dose of 50 mg, the maximum concentration (Cmax) is approximately 65 ng / ml.
Oral administration of hydroxyzine 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 is 80%.
Hydroxyzine is more concentrated in tissues than in plasma. The distribution coefficient in adults is 7–16 l / kg. Passes through the blood-brain barrier and placenta, concentrating mainly 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 dose 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. In unchanged form, only 0.8% of hydroxyzine is excreted 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 indicator is 2.5 times less than in adults.
The half-life (T ½) in adults is an average of 14 hours (from 7 to 20 hours), in children aged 14 years - 11 hours, at the age of 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 for 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 itchy skin.
In pediatrics, the drug is used for premedication and symptomatic treatment of itching of allergic origin.
Contraindications
The use of Atarax is contraindicated in porphyria, hypersensitivity to the components of the drug, pregnancy, as well as during labor and lactation.
The drug is used with caution:
- Myasthenia gravis;
- Predisposition to the development of arrhythmia;
- Difficulty urinating;
- Increased intraocular pressure;
- Tendency to convulsive seizures;
- Prostatic hyperplasia with clinical manifestations;
- Constipation;
- Dementia.
Instructions for the use of Atarax: method and dosage
Solution for i / m administration
In the form of a solution, Atarax is administered intramuscularly.
Recommended dosages for children:
- premedication: 1 mg / kg body weight 1 hour before surgery, if necessary, it is possible to administer the same dose at night before anesthesia;
- symptomatic treatment of itching: children 1–6 years old - 1–2.5 mg / kg per day in several doses, children from 6 years old - at 1–2 mg / kg per day in several doses.
Recommended dosages for adults:
- premedication: 50-200 mg 1 hour before surgery, if necessary, it is possible to administer the same dose at night before anesthesia;
- symptomatic treatment of itching: at the beginning of treatment - 25 mg 1 time per day, if necessary, the dose is increased to 25 mg 4 times a day;
- symptomatic treatment of anxiety: morning and afternoon - 12.5 mg, at night - 25 mg (total daily dose - 50 mg). In serious cases, an increase in the daily dose of up to 300 mg is allowed.
The maximum allowable 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 impairment. If hepatic function is insufficient, 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 each), while the maximum dose should not exceed 300 mg per day and 200 mg at a time.
The daily dose of Atarax for adults for relieving symptoms of anxiety is 50 mg and in severe cases can be increased to 300 mg. A quarter of the daily allowance must be taken in the morning and afternoon, the rest before bedtime.
In old age, as well as with renal and hepatic insufficiency, it is recommended to reduce the dose of the drug by half.
For premedication, Atarax is prescribed for children at a dose of 1 mg per kilogram of body weight. The drug is taken the night before anesthesia.
For the symptomatic treatment of itching for children, the drug is prescribed depending on age:
- 3–6 years: 1–2.5 mg / kg / day (in divided doses);
- 6 years and older: 1–2 mg / kg / day (in divided doses).
Side effects
The use of Atarax can cause the following side effects:
- Headache, drowsiness, general weakness and dizziness (if symptoms persist within a few days after starting the drug, the dose taken should 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, tremors, involuntary motor activity, hyperthermia, tachycardia. Arrhythmia, arterial hypotension, convulsions, depression of consciousness and respiration may also occur, as a result of which coma and cardiopulmonary collapse are possible.
In case of an overdose, supportive 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 checked for concomitant use of alcohol or other drugs. In these cases, if necessary, oxygen is inhaled, glucose (dextrose), thiamine, naloxone are injected.
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 to hydroxyzine. Hemodialysis is ineffective.
According to the literature, with the development of severe and life-threatening anticholinergic effects that cannot be treated by 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, it is not recommended to prescribe it to 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 conjunction with drugs that inhibit the effect of the central nervous system: tranquilizers, ethanol, opioid analgesics, barbiturates and hypnotics.
Do not take the drug simultaneously with MAO inhibitors and anticholinergics.
Influence on the ability to drive vehicles and complex mechanisms
During the period of application of Atarax, the speed of reactions and the ability to concentrate may deteriorate. This effect can be enhanced by the concomitant use of other sedatives. During therapy, it is recommended to refrain from performing potentially hazardous activities, including driving vehicles and operating complex mechanisms.
Application during pregnancy and lactation
Atarax is contraindicated for use during pregnancy and lactation.
Pediatric use
In the form of a solution for intramuscular administration, Atarax is contraindicated in children under 1 year of age, in the form of tablets - up to 3 years.
The dose for children is adjusted according to age and body weight.
With impaired renal function
In patients with impaired renal function with repeated use of the drug, the accumulation of cetirizine (a metabolite of hydroxyzine) is possible, and therefore it is recommended to reduce the dose of Atarax for this category of patients.
For violations of liver function
In case of liver failure, it is recommended to reduce the daily dose of the drug or the frequency of its use.
Use in the elderly
Elderly patients are recommended to reduce the initial dose of Atarax by two times.
Drug interactions
Hydroxyzine does not affect the action of H 2 -histamine receptor blockers, cardiac glycosides, antihypertensive drugs, belladonna alkaloids and atropine.
The action of hydroxyzine is potentiated with the simultaneous use of agents that depress the central nervous system, such as ethanol, hypnotics, barbiturates, narcotic analgesics, tranquilizers. If necessary, their combined appointment requires individual selection of doses. 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.
During the period of taking Atarax, it is not recommended to prescribe anticholinergics and monoamine oxidase (MAO) inhibitors.
Hydroxyzine interferes with the action of cholinesterase and betahistine inhibitors, the pressor effect of epinephrine, and the anticonvulsant activity of phenytoin.
Cimetidine, used twice a day at 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, therefore, its concentration in the blood can increase with the combined use of inhibitors of liver microsomal enzymes.
With the simultaneous use of drugs that can cause arrhythmia, the risk of prolongation of the QT interval and the development of pirouette-type ventricular tachycardia increases.
The CYP3A4 / 5 isoenzyme and alcohol dehydrogenase are involved in the metabolism of hydroxyzine, which may lead to an increase in the plasma concentration of the drug with the simultaneous use of drugs that are capable of inhibiting the CYP3A4 / 5 isoenzyme, such as ketoconazole, itraconazole, voriconazole, clarithromycin, delpirentromycin, stirycin, posaconazole, some HIV protease inhibitors, including nelfinavir, indinavir, saquinarin, ritonavir, atazanavir, saquinarin / ritonavir, lopinavir / ritonavir, tipranavir / ritonavir. However, inhibition of one metabolic pathway can be partially compensated by the work of another.
Analogs
Atarax analogues are Phenazepam, Relium, Relanium, Elenium, Sibazon, Diazepam, Gidazepam, Tazepam, Grandaksin, Anvifen, Fenorelaxan, 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.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Atarax
Reviews about Atarax are mostly positive. It is used as a hypnotic and sedative, and also as an antipruritic drug for dermatological diseases. Atarax reduces anxiety, normalizes sleep, reduces panic attacks, and helps with withdrawal symptoms well: eliminates aggressiveness, headache, dizziness, sweating and other accompanying symptoms. However, it should not be taken simultaneously with alcohol, since hydroxyzine enhances the effect of ethanol and its depressant effect on the central nervous system.
In pediatrics, Atarax is used mainly in the treatment of skin diseases accompanied by severe itching.
In some negative reviews, patients indicate drowsiness, lethargy and decreased ability to work after taking the drug.
The price of Atarax in pharmacies
The cost of Atarax tablets (25 pcs. Per pack) varies in the range of 270–358 rubles. The price of Atarax in the form of a solution for intramuscular injection (6 ampoules per package) is approximately 334 rubles.
Atarax: prices in online pharmacies
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Drug name Price Pharmacy |
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Atarax 25 mg film-coated tablets 25 pcs. 263 r Buy |
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Atarax tablets p.p. 25mg 25 pcs. 304 RUB Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
