Shop brand name: Atarax
The international non-proprietary name – hydroxyzine
Chemical name: ethanol, 2 [-2 - [- 4 - [(4-chlorophenyl) phenylmethyl] -1-piperazinyl] ethoxy] -, dihydrochloride.
Dosage form: solution for intramuscular administration; coated tablets.
Structure of Atarax
Tablets: active substance - 25 mg of hydroxyzine hydrochloride; Other ingredients: microcrystalline cellulose (Avicel PH 102®), magnesium stearate, colloidal silicon dioxide (Aerosil 200®), lactose monohydrate, Opadray® Y-1-7000: titanium dioxide, hydroxypropyl methylcellulose 2910 5cP, macrogol 400.
Solution for the i/m: active substance - 100 mg of hydroxyzine hydrochloride in 2 ml; Inactive components: sodium hydroxide, water for injections.
White oblong film-coated tablets, with a dividing cross-scored on both sides.
The solution for intramuscular injection - a clear, colorless solution.
Antianxiety drug (tranquilizer).
ATC code: 05BB01.
Diphenylmethane derivative has moderate anxiolytic activity; also has sedative, antiemetic, antihistamine, and M-anticholinergic action. Does central M-choline - and the H1-gistaminoretseptory and inhibits the activity of certain subcortical areas. It does not cause mental dependence and addiction. The clinical effect occurs within 15-30 minutes after ingestion of tablets. 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 is not marked withdrawal symptoms and deterioration of cognitive functions. Polysomnography in patients with insomnia and anxiety demonstrate lengthening of the duration of sleep, reduce the frequency of nighttime awakenings after a single or repeated hydroxyzine 50 mg. Reduced muscle tension anxiety in patients receiving the drug observed at a dose of 50 mg three times a day.
Absorption - high. The time to maximum concentration (TCmax) after oral administration - 2 hours; half-life (T1 / 2) in adults -. 14 hours metabolites found in breast milk. After a single dose of 25 mg TCmax in adults is 30 mg / ml and 70 mg / ml after administration of 50 mg of hydroxyzine. The bioavailability of the oral and intramuscular administration is 80%.
Hydroxyzine is more concentrated in the skin than in plasma. The distribution coefficient is 7-16 liters / kg for adults. Hydroxyzine penetrates the blood-brain barrier and the placenta, concentrating mainly in fetal than in maternal tissues. Hydroxyzine is metabolized in the liver. Cetirizine - the main metabolite (45%), is expressed by H1-blocker. Hydroxyzine total clearance of 13 ml / min / kg. Only 0.8% of Hydroxyzine is excreted unchanged via the kidneys.
In children, the total clearance is 4 times shorter than that of adults, T1 / 2 - 11 hours in children aged 14 years and 4 hours in the age of 1 year.
In elderly patients with T1 / 2 was 29 hours, the distribution ratio is 22.5 L / kg.
Patients with liver T1 / 2 was increased to 37 h, the concentration of metabolites in serum is higher than in young patients with normal liver function. The antihistamine effect can be extended up to 96 hours after ingestion.
Indications for Atarax
The drug is contraindicated in patients with hypersensitivity to any component of the drug, cetirizine and other piperazine derivatives, aminophylline or ethylenediamine.
Contraindicated in patients with porphyria also; during pregnancy, during labor and breastfeeding.
Since the tablets include lactose, patients with hereditary galactose intolerance, malabsorption of glucose-galactose preparation is not recommended.
In myasthenia gravis, prostatic hyperplasia with clinical symptoms, difficulty urinating, constipation, with an increase in intraocular pressure, dementia, tendency to seizures. Patients prone to arrhythmia or receiving drugs that can cause arrhythmia. Patients receiving treatment at the same time by other means, oppressive central nervous system, or choline-blocker, the dose should be reduced.
Patients with moderate and severe degrees of severity of renal failure, as well as with hepatic impairment dose reduction is necessary. Elderly patient dose is reduced in the case of a reduced glomerular filtration rate.
The drug is given orally in tablet form or injected intramuscularly.
For symptomatic treatment of itching.
At the age of 12 months to 6 years: 1 mg / kg to 2.5 mg / kg / day in divided doses.
At the age of 6 years and older: 1 mg / kg to 2.0 mg / kg / day in divided doses.
For sedation - 1 mg / kg 1 hour prior to surgery, as well as an additional night before anesthesia.
For symptomatic treatment of anxiety: 25-100 mg per day in separate dosages throughout the day or at night. The standard dose of 50 mg per day (morning, 12.5 mg, 12.5 mg and 25 mg day at night).
In severe cases, the dose can be increased to 300 mg per day.
For sedation in surgical practice: 50-200 mg (1.5-2.5 mg / kg i.m.) injected for 1 hour before surgery.
For symptomatic treatment of pruritus: an initial dose of 25 mg, as appropriate dose may be increased to four times (25 mg 4 times daily), as well as an additional night before anesthesia.
Elderly patients are treated with half dose. In renal and / or hepatic insufficiency dose should be reduced.
The single maximum dose should not exceed 200 mg, the maximum daily dose is not more than 300 mg.
Mild and transient, generally disappear after a few days from the beginning of treatment or after dose reduction.
Side effects are mainly related to CNS depression or paradoxical stimulant effect on the central nervous system anticholinergic activity, or hypersensitivity reaction.
Anticholinergic effects: dry mouth, urinary retention, constipation, or disturbance of accommodation are rare and mostly in elderly patients. There may be drowsiness, weakness, especially in the beginning of drug treatment. If this effect does not disappear after a few days of therapy, the dose should be reduced.
There were reports of other side effects, such as headache, dizziness, excessive sweating, hypotension, tachycardia, allergic reactions, nausea, tachycardia, fever, changes in liver function tests, bronchospasm. Clinically significant respiratory depression were observed in the appointment of the recommended doses.
Involuntary motor activity, including the very rare instances of tremor and convulsions, disorientation observed at large overdose.
A manifestation of an overdose of the drug can be pronounced anticholinergic effects, depression or paradoxical CNS stimulation. Symptoms of overdose may be significant nausea, vomiting, involuntary motor activity, hallucinations, impaired consciousness, arrhythmia, hypotension.
If spontaneous vomiting is absent, immediate gastric lavage is recommended. Vomiting is necessary to cause an artificial way. Showing general supportive measures, including monitoring of vital body functions and monitor observation of the patient before the disappearance of symptoms of intoxication and in the next 24 hours. Should you require pressor effect of norepinephrine or appointed metaramenol. Epinephrine should not be used. Hemodialysis is not effective. There is no specific antidote.
Interaction with other drugs
It is necessary to take into account the potentiating effect of hydroxyzine with a joint appointment with the drugs depressing the central nervous system, such as narcotic analgesics, barbiturates, tranquilizers, sleeping pills and alcohol. In this case, their dosage should be individualized.
Avoid joint appointment with MAO inhibitors and choline-blocker. The drug inhibits the pressor effect of adrenaline and anticonvulsant activity of phenytoin and prevents the action of betahistine and drugs - cholinesterase blockers.
Effect of atropine, belladonna alkaloids, digitalis, antihypertensive agents, H2 receptor antagonists are not changed under the influence of hydroxyzine.
It is an inhibitor of P450 2D6, and at 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 drugs - inhibitors of liver enzymes.
If necessary, conduct allergy tests, the drug should be discontinued 5 days prior to the study.
As hydroxyzine can affect attention and speed of psychomotor reactions, patients should be warned about this, if necessary, and driving mechanisms.
Injectable forms of the drug are intended for intramuscular injection, and it should not be administered intravenously, intraarterially or subcutaneously. Intramuscular administration should make sure that the needle does not hit in any vessel. When administered to the skin the drug may cause tissue damage.
During treatment Hydroxyzine should avoid drinking alcohol.
Tablets coated with 25 mg. 25 tablets in a blister; blister with instruction on use is packed in a cardboard box.
Ampoules for i / m injection 100 mg / 2 ml clear, white glass solution, 6 vials are enclosed in a plastic holder, which is packed together with the instructions for use in a cardboard box.
Tablets - in a dry place at temperatures not above 25 ° C.
The vials - at temperatures not above 25 ° C.
Do not take the medication after the expiration date. Keep out of the reach of children.
Conditions of supply of pharmacies: