Atarax (Hydroxyzine)

Brand name: Atarax

Generic Name: Hydroxyzine

Chemical name: Ethanol, 2 [-2 - [-4 - [(4-hlorofenil) phenylmethyl]-1-piperazinyl] ethoxy] -, dihydrochloride.

Dosage forms: Solution for intramuscular injection, coated tablets.

Composition

Tablets: the active ingredient - Hydroxyzine hydrochloride 25 mg 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 IM injection: the active ingredient - Hydroxyzine hydrochloride 100 mg in 2 ml inactive ingredients: sodium hydroxide, water for injection.

Description

White oblong pill, coated with a separation of the transverse risks for both parties.

Solution for intramuscular injection - clear, colorless solution.

Pharmacotherapeutic group: anxiolytic drug (tranquilizer).

ATC code: ¹ 05BB01.

Pharmacological properties

Diphenylmethane derivative, has a moderate anxiolytic activity, is also a sedative, antiemetic, antihistamine, and M-anticholinergic action. Blocks the central M-choline - and the H1-gistaminoretseptory and inhibits the activity of certain subcortical areas. Does not cause psychological dependence and addiction. The clinical effect occurs 15-30 minutes after ingestion of tablets. Has a positive effect on cognition, improves memory and attention. Relaxes skeletal and smooth muscle, has bronchodilatory and analgesic effects, a moderate inhibitory effect on gastric secretion. Hydroxyzine significantly reduces pruritus in patients with urticaria, eczema and dermatitis. Chronic administration is not marked withdrawal syndrome and deterioration of cognitive functions. Polysomnography in patients with insomnia and anxiety demonstrate lengthening the duration of sleep, decrease the frequency of nighttime awakenings after receiving a single dose or re-Hydroxyzine 50 mg. Reduction of muscular tension in patients with anxiety observed when taking the drug at a dose of 50 mg 3 times a day.

Pharmacokinetics. Absorption - high. Time to reach maximum concentration (TCmax) after oral administration - 2 h half-life (T1 / 2) in adults - 14 h. The 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. Oral bioavailability and intramuscular injection of 80%.

Hydroxyzine is more concentrated in the skin than in plasma. The distribution coefficient of 7-16 L / kg in adults. Hydroxyzine crosses the blood-brain barrier and the placenta, focusing to a greater extent in fetal than in maternal tissues. Hydroxyzine is metabolized in the liver. Cetirizine - the main metabolite (45%) is expressed H1-blocker. The total clearance of Hydroxyzine is 13 ml / min / kg. Only 0,8% Hydroxyzine excreted unchanged in the kidneys.

In children, the total clearance is 4 times shorter than those of adults, T1 / 2 - 11 hours in children under the age of 14 and 4 h at the age of 1 year.
In elderly patients with T1 / 2 was 29 h, the distribution coefficient of 22.5 L / kg.
In patients with liver T1 / 2 increased to 37 h, the concentration of metabolites in serum is higher than in younger patients with normal liver function. Antihistamine effect can be extended up to 96 hours after admission.

INDICATIONS FOR USE

Adults for relief of anxiety, psychomotor agitation, feelings of inner tension, irritability with neurological, psychiatric (generalized anxiety and adjustment disorder) and somatic diseases, as well as in chronic alcoholism, alcohol withdrawal syndrome, accompanied by symptoms of psychomotor agitation;
as a sedative during the period of sedation;
symptomatic treatment of pruritus.

CONTRAINDICATIONS

The drug is contraindicated in patients with hypersensitivity to any component of the drug, cetirizine, and other derivatives of piperazine, aminophylline and ethylenediamine.

Also contraindicated in patients with porphyria, pregnancy, during labor and breastfeeding.

Since the tablets include lactose, patients with hereditary galactose intolerance, with malabsorption of glucose-galactose drug is not recommended.

WITH CARE

In myasthenia gravis, prostatic hyperplasia with clinical symptoms, difficulty urinating, constipation, an increase in intraocular pressure, dementia, the propensity to seizures. Patients prone to arrhythmia or receiving medications that may cause arrhythmia. Patients while receiving treatment with other central depressant drug, or holinoblokatorami, the dose should be reduced.

Patients with severe and moderate degrees of renal impairment, as well as with liver failure should decrease the dose. Elderly patients the dose is reduced by decreasing glomerular filtration.

DOSAGE AND ADMINISTRATION

The drug is given by mouth in tablet form or injected intramuscularly.

Children

For the symptomatic treatment of pruritus.

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 for 1 hour before surgery, and further into the night before anesthesia.

Adults

For the symptomatic treatment of anxiety: 25-100 mg / day in split doses during the day or at night. The standard dose of 50 mg / day (12.5 mg in the morning, 12.5 mg by day and 25 mg at night).

In severe cases, the dose may be increased to 300 mg per day.

For sedation in surgical practice: 50-200 mg (1,5-2,5 mg / kg intramuscularly) is given 1 hour before surgery.

For the symptomatic treatment of pruritus: an initial dose of 25 mg, if necessary the dose may be increased four-fold (25 mg 4 times daily), and additionally on the night before anesthesia.

In elderly patients treatment begins with a half dose. In renal and / or hepatic insufficiency the dose should be reduced.

A single maximum dose should not exceed 200 mg maximum daily dose is no more than 300 mg.

SIDE EFFECTS

Mild and transient, usually disappearing after a few days of starting treatment or after dose reduction.

Side effects are mainly related to CNS depression or paradoxical stimulating effect on the CNS, anticholinergic activity, or hypersensitivity reactions.

Anticholinergic effects: dry mouth, urinary retention, constipation, or disturbance of accommodation are rare and mostly in elderly patients. May be drowsiness, weakness, particularly in early drug treatment. If this effect does not disappear after a few days of therapy, the drug 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, bronchial spasm. Clinically significant respiratory depression in the appointment of the recommended doses were observed.

Involuntary motor activity including rare instances of tremor and convulsions, disorientation observed in a large overdose.

OVERDOSAGE

Manifestation of an overdose of the drug can be pronounced anticholinergic effects, depression, or paradoxical CNS stimulation. Significant symptoms of overdose could be nausea, vomiting, involuntary motor activity, hallucinations, impaired consciousness, arrhythmia, hypotension.

If spontaneous vomiting is absent, we recommend immediate gastric lavage. Vomiting, call an artificial way. Shows the general supportive measures, which include monitoring vital body functions and monitor observation for patients until symptoms of intoxication and in the next 24 hours. Should a pressor effect of norepinephrine or appointed metaramenol. Epinephrine should not be given. Hemodialysis is not effective. A specific antidote does not exist.

INTERACTION WITH OTHER DRUGS

Must take into account the potentiating effect of Hydroxyzine in joint appointment with drugs, depressing the central nervous system, such as narcotic analgesics, barbiturates, tranquilizers, sleeping pills and alcohol. In this case, their dosage should be chosen individually.

Should be avoided joint appointment with MAO inhibitors and holinoblokatorami. The drug prevents the pressor action of adrenaline and anticonvulsant activity of phenytoin and inhibits the action of betahistine and drugs - cholinesterase inhibitors.

The effect of atropine, belladonna alkaloids, digitalis, antihypertensives, H2-receptor antagonist did not change under the action Hydroxyzine.

Is an inhibitor of P450 2D6 and in high doses can cause interactions with substrates of CYP2D6. Because hydroxyzine is metabolized in the liver, can be expected to increase its concentration in the blood during a joint appointment with the drugs - inhibitors of hepatic enzymes.

SPECIAL INSTRUCTIONS

If necessary, conduct allergy tests, the drug should be discontinued 5 days before the study.

As hydroxyzine can affect attention and psychomotor speed of reaction, patients should be warned about this when you need to operate the vehicle and machinery.

Injectable forms of the drug intended only for intramuscular injection and should not be administered intravenously, intraarterially, or subcutaneously. In intramuscular make sure that the needle does not hit in any vessel. The introduction of the drug under the skin can cause tissue damage.

During treatment with hydroxyzine should avoid drinking alcohol.

FORM

Coated tablets of 25 mg. 25 tablets in a blister blister with the instruction manual is packed in cardboard box.

Ampoules for IM injection of 100 mg / 2 ml of clear, white glass, 6 vials enclosed in a plastic holder, which is packaged together with instructions for use in a cardboard box.

STORAGE CONDITIONS

Pills - in a dry place at temperatures not above 25 ° C.
Ampoules - at or above 25 ° C.

Do not take the drug after the expiration date. Keep out of reach of children.

SHELF LIFE

5 years.