Last Updated on February 19, 2017 by Dr.Derek Fhisher
Most popular brand: Atarax
Active ingredient: Hydroxyzine
Available dosage forms: 25, 10 mg
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Hydroxyzine general information
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There are contraindications. Before taking consult your doctor.
The commercial name abroad (abroad) – Hizin, Hidroxina, Hydroze, Masmoran, Neurax, Orgatrax, Otarex, Vistaject, Vistaril.
Currently, the analogues (generics) of the drug in pharmacies of Moscow is not for sale!
All tranquilizers (anxiolytics) here.
All the drugs used in neurology and psychiatry, here.
Ask a question or leave a review about the medicine (please do not forget to specify the name of the drug in the body of the message) here.
Preparations containing Hydroxyzine (Hydroxyzine, ATC (ATC code) N05BB01):
Common forms of release (more than 100 proposals in Moscow pharmacies)
Atarax (Hydroxyzine) – instructions for use. Prescription drug information is intended only for healthcare professionals!
Clinico – pharmacological group:
Mode of action
diphenylmethane derivative, has a moderate anxiolytic activity; also has sedative, antiemetic, antihistamine, and m – anticholinergic action. Does central m – cholinergic and histamine H1 – receptors and inhibits the activity of certain subcortical areas. It does not cause mental dependence and addiction. The clinical effect after 15 – 30 minutes after ingestion of the drug.
It has a positive influence on cognitive abilities, improves memory and attention. It relaxes skeletal and smooth muscles, has a bronchodilator and analgesic effects, a moderate inhibitory effect on gastric secretion. Hydroxyzine reduces the itching in patients with urticaria, eczema and dermatitis. Chronic administration were observed cindroma cancellations and deterioration of cognitive functions. Polysomnography in patients with insomnia and anxiety demonstrates lengthening the duration of sleep, reduce the frequency of nighttime awakenings after single or repeated administration of hydroxyzine at a dose of 50 mg. Reduced muscular tension in patients with anxiety observed while taking the drug at a dose of 50 mg 3 times a day.
Hydroxyzine highly absorbed from the gastrointestinal tract. Cmax observed after 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 in the plasma concentration is 30 ng / ml and 70 ng / ml, respectively.
Oral bioavailability and / m the introduction of 80%.
Hydroxyzine more concentrated in the tissues (including the skin) than in plasma. The distribution coefficient is 7 – 16 l / kg.
Hydroxyzine penetrate the BBB and placental barrier, concentrating mainly in fetal tissues than in the mother. The metabolites are found in breast milk.
Metabolism and excretion
Hydroxyzine is metabolized in the liver. The major metabolite (45%) – cetirizine, which is a blocker of histamine H1 – receptors. Hydroxyzine total clearance of 13 ml / min / kg. T1 / 2 in adults is 14 hours. Only 0.8% of Hydroxyzine is excreted unchanged in the urine.
Pharmacokinetics in special clinical situations
In children, the total clearance is 4 times less than in adults, T1 / 2 children under the age of 14 years is 11 hours, in children aged 1 year – 4 hours.
In elderly patients T1 / 2 of 29 hours, the distribution ratio is 22.5 L / kg.
in patients with impaired liver function T1 / 2 is increased up to 37 h, the concentration of metabolites in serum is higher than in young patients with normal liver function. The antihistamine effect may persist for 96 hours.
Indications for use of the drug Atarax ®
- adults: for the relief of anxiety, agitation, feelings of inner tension, irritability with neurological, psychiatric (including generalized anxiety, adjustment disorder) and somatic diseases, chronic alcoholism; abstinence syndrome in chronic alcoholism, accompanied by psychomotor agitation;
- as a sedative during premedication;
- itchy skin (as a symptomatic therapy).
The drug is taken orally.
For the symptomatic treatment of pruritus in children aged 12 months to 6 years, the drug is administered in a daily dose of 1 – 2.5 mg / kg body weight in divided doses; children over 6 years of age – a dose of 1 – 2 mg / kg / day in divided doses.
For sedation medication for children is prescribed in a dose of 1 mg / kg body weight for 1 hour prior to surgery, as well as an additional night before the operation.
For adults for symptomatic treatment of anxiety is prescribed in doses of 25 – 100 mg per day in divided doses during the day or at night. An average dose of 50 mg per day (morning, 12.5 mg, 12.5 mg and 25 mg day at night). If necessary, the dose may be increased to 300 mg per day.
for the symptomatic treatment of pruritus initial dose is 25 mg, if appropriate dose may be increased 4 times (25 mg four times a day).
The maximum single dose should not exceed 200 mg, the maximum daily dose is not more than 300 mg.
In elderly patients the initial dose should be reduced by 2 times.
Patients with renal failure secondary to severe, as well as with hepatic impairment dose reduction is necessary.
The side effects associated with anticholinergic effects: rarely (mainly in elderly patients) – dry mouth, urinary retention, constipation, accommodation.
From the CNS: drowsiness, weakness (especially at the beginning of treatment), headache, dizziness. If the weakness and drowsiness do not disappear after a few days of therapy, the drug dose should be reduced. Very rarely (if a large overdose) – tremors, convulsions, disorientation.
Cardio – vascular system: hypotension, tachycardia.
From the digestive system: nausea, changes in liver function tests.
Others: increased sweating, allergic reactions, fever, bronchospasm.
When using the drug at the recommended doses were observed clinically significant respiratory depression. Spontaneous motor activity (including very rare cases of tremor and seizures), disorientation observed at large overdose.
Side effects observed when taking the drug Atarax ®, usually mild, transient and disappear after a few days from the beginning of treatment or after dose reduction.
Contraindications to the use of the drug Atarax ®
- during labor;
- lactation (breastfeeding);
- hypersensitivity to the drug;
- Hypersensitivity to cetirizine and other piperazine derivatives, aminophylline or ethylenediamine.
Not recommended to prescribe pills Atarax ® patients with hereditary galactose intolerance and malabsorption of glucose and galactose since in the tablets include lactose.
Caution should be prescribed the drug in infants, prostatic hyperplasia with clinical symptoms, difficulty urinating, constipation, with an increase in intraocular pressure, dementia, tendency to seizures; with predisposition to arrhythmia; while the use of drugs with arrhythmogenic effect; together with other means, oppressive central nervous system, or holinoblokatorami (requires dose reduction). Requires dose reduction in patients with severe renal impairment or moderate, with liver failure, in elderly patients with a decrease in glomerular filtration rate.
Use of the drug Atarax ® Pregnancy and breastfeeding
Atarax ® contraindicated during pregnancy, during labor and delivery.
If you need to use Atarax during lactation should stop breastfeeding.
Application for violations of liver function
Patients with hepatic impairment dose reduction is necessary.
Application for violations of renal function
Patients with renal failure secondary to severe dose reduction is necessary.
When the need for allergy tests Atarax intake should be discontinued 5 days before the study.
Patients taking Atarax ®, should refrain from drinking alcohol.
Effects on ability to drive vehicles and management mechanisms
Patients taking Atarax ®, if necessary driving and mechanisms should be warned that the drug can affect the concentration of attention and speed of psychomotor reactions.
Symptoms: increased anticholinergic effects, depression or paradoxical CNS stimulation, nausea, vomiting, involuntary motor activity, hallucinations, impaired consciousness, arrhythmia, hypotension; rarely – tremors, convulsions, disorientation that occur when a large overdose.
Treatment: if spontaneous vomiting is absent, you must call it by artificial means or to gastric lavage. Carry out general measures aimed at maintenance of the vital functions of the body, and the monitor observation of the patient before the disappearance of symptoms of intoxication in the next 24 hours.
In the case of need for vasopressor effect of norepinephrine or appointed metaramenol. Do not use epinephrine. There is no specific antidote. The use of hemodialysis is ineffective.
Atarax ® potentiates the effect of drugs which depress the central nervous system, such as opioids, barbiturates, tranquilizers, sleeping pills, ethanol (if combinations require individual selection of doses of drugs).
Atarax ® while the application prevents the pressor effect of epinephrine (adrenaline) and anticonvulsant activity of phenytoin and prevents the action of betahistine and cholinesterase blockers.
In an application Atarax ® It does not affect the activity of atropine, belladonna alkaloids, cardiac glycosides, antihypertensives, histamine H2 – receptors.
Avoid joint appointment Atarax with MAO inhibitors and holinoblokatorami.
Hydroxyzine inhibitor is isozyme CYP2D6 and when used in high doses can cause interactions with substrates of CYP2D6. As hydroxyzine is metabolized in the liver, can be expected to increase its concentration in the blood when coadministered with inhibitors of liver enzymes.
of the pharmacies vacation Terms
The drug is released with a prescription.
Conditions and terms
The drug should be stored out of reach of children, dry place at temperatures no higher than 25 ° C. Shelf life – 5 years.