Atarax (hydroxyzine)

 

Hydroxine: Atarax, Hydroxysine, Hydroxysin hydrochloride.

Atarax

Atarax – anxiolytic for the treatment of neuroses and neurotic conditions, withdrawal of alcohol withdrawal syndrome. Significantly reduces itching in patients with hives, eczema and dermatitis. Has antiemetic effect.

 

Latin name:

ATARAX / ATARAX.

 

Composition and form of release:

Atarax tablets, coated with a shell, 25 pcs. Each. packaged.

1 tablet of Atarax contains hydroxysine hydrochloride 25 mg.

Atarax syrup 200 ml in bottles of 1 pc. packaged.

5 ml of Atarax syrup contains hydroxyzine hydrochloride 10 mg.

Atarax injection for 2 ml in ampoules of 6 pcs. packaged.

1 ml of Atarax solution contains hydroxyzine hydrochloride 50 mg.

 

Active-active substance:

Hydroxysin / Hydroxysin hydrochloride / Hydroxyzine.

There are other Anti-Anxiety pills that are more effective. Like Xanax.

Pharmacologic effect:

Atarax (hydroxyzine) is a derivative of diphenylmethane (piperazine). Anxiolytic, antihistamine (blocker of histamine H1 receptors), antipruritic agent. The anxiolytic activity of Atarax is apparently due to influence on subcortical structures.

Atarax significantly reduces itching in patients with hives, eczema and dermatitis.

For Atarax is also characterized by pronounced sedative, antiemetic, moderate m-cholinoblock (spasmolytic, bronchodilator) and central miorelaksiruyuschee effect.

Sedation is manifested after 5-10 minutes after taking liquid forms and 30-45 minutes after taking the tablets.

The antihistamine effect appears about 1 hour after ingestion.

At long reception the syndrome of cancellation and deterioration of cognitive functions was not noted. There was no mutagenic and carcinogenic effect.

 

Pharmacokinetics:

Hydroxysin is rapidly absorbed from the digestive tract, the peak concentration in the plasma is achieved 2 hours after oral administration. More concentrated in tissues than in plasma. The distribution coefficient is 13-19 l / kg in adults and 16-18 l / kg in children.

Hydroxyzine passes through the blood-brain and placental barriers.

Metabolised in the liver. The main metabolite (45%), cetirizine, is a pronounced H1-blocker. Only 0.8% of the drug is excreted unchanged by the kidneys.

The half-life period depends on the age and is 7 hours in children, 20 hours in adults and 29 hours in the elderly.

In patients with liver disease, T1 / 2 may increase to 37 hours, and the antihistamine effect – prolonged to 96 hours.

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Indications:

neuroses and neurotic states: relief of anxiety (generalized anxiety and adaptation disorder), psychomotor agitation, internal tension, irritability, anxiety;

organic lesions of the central nervous system, accompanied by increased excitability;

chronic alcoholism, withdrawal syndrome, accompanied by symptoms of arousal;

premedication and postoperative period (as a sedative, for preventing and stopping vomiting, as part of combination therapy);

symptomatic itching therapy.

 

Dosing and Administration:

Adults:

Adults for symptomatic treatment of anxiety – 25-100 mg in several doses during the day or at night (1-4 times / day). The standard dose is 50 mg / day (12.5 mg in the morning, 12.5 mg in the afternoon and 25 mg at night). In serious cases (in psychiatry) the dose may be increased to 300 mg / day. The usual duration of treatment is 4 weeks.

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

The maximum single dose is 200 mg, the daily dose is 300 mg.

Children:

Children are prescribed depending on age and body weight.

Children from 12 months to 6 years for symptomatic treatment of pruritus – from 1 to 2.5 mg / kg / day, in several ways.

Children from 6 years and older – 1-2 mg / kg / day, in several receptions.

In / m.

To quickly achieve a therapeutic effect, a solution of hydroxyzine is injected deep in the / m. For premedication in surgical practice – in / m, 50-200 mg (1.5-2.5 mg / kg) for 1 h before the operation. For premedication, children – 1 mg / kg for 1 hour before surgery and an additional night before anesthesia. Then you can enter with an interval of 4-6 hours.

 

Overdose:

In case of an overdose, the usual metabolic pathways may be overloaded and biotransformation proceeds in a different way.

Symptoms: hypersedition, involuntary motor activity, tremor, convulsions, hallucinations, impaired consciousness, cardioarrhythmia, arterial hypotension, nausea, vomiting.

Treatment: induction of vomiting (in the absence of spontaneous), gastric lavage, general supportive measures, incl. control of vital body functions. With arterial hypotension, the administration of norepinephrine or metamrinol (but not epinephrine). Assign oxygen, naloxone, glucose, thiamine. With sinus arrhythmia, physostigmine should not be prescribed.

There is no specific antidote. The use of hemodialysis or hemoperfusion is inexpedient.

 

Contraindications:

hypersensitivity to hydroxyzine and any of the components of the drug, cetirizine, aminophylline or ethylenediamine;
porphyria;
benign prostatic hyperplasia;
angle-closure glaucoma;
pregnancy, the period of labor, breastfeeding.

Application in pregnancy and lactation:

Contraindicated in pregnancy. For the duration of treatment, breastfeeding should be discontinued. With the appointment of hydroxyzine in the period of labor, newborns had arterial hypotension, impaired motor activity and clonic convulsions, urinary retention and signs of hypoxia, and depression of the central nervous system.

Side effects:

Slightly expressed, transient and, as a rule, disappear within a few days from the start of treatment or after a reduction in the dose.
They are mainly associated with CNS depression or paradoxical stimulation of the CNS, anticholinergic activity or hypersensitivity reaction.
Anticholinergic effects: dry mouth, urinary retention, constipation, disruption of accommodation are rare and, mainly, in elderly patients.
Possible drowsiness, general weakness, especially at the beginning of treatment with the drug (if this effect does not disappear after a few days from the start of therapy, the dose of the drug should be reduced).
Also there were headache, dizziness, excessive sweating, arterial hypotension, tachycardia, allergic reactions, nausea, fever, changes in functional liver tests, bronchospasm.
Clinically significant respiratory depression in the appointment of recommended doses is not noted.

Precautions and special instructions:

Caution should be exercised in appointing patients with difficulty urinating, constipation, myasthenia gravis, dementia, kidney and / or liver failure.
They are used with caution in patients prone to arrhythmia or receiving antiarrhythmic drugs, as well as in patients predisposed to convulsive reactions.
With simultaneous treatment with drugs that depress the central nervous system, or holinoblokatorami, you need a dose adjustment.
Patients with liver dysfunction or patients suffering from a moderate or severe form of liver failure, the dose should be reduced.
The dose should be reduced in elderly patients (treatment starts with half the therapeutic dose).
If such side effects as drowsiness and weakness do not disappear after a few days of treatment, it is necessary to reduce the dose.
Joint use with MAO inhibitors should be avoided.
Avoid drinking alcohol during treatment.
If it is necessary to carry out allergological tests, the hydroxyzine intake should be stopped 5 days before the test.
Injection forms are for I / m administration only. With the / m introduction, make sure that the needle is not in any vessel; if you get under the skin of the drug, tissue damage is possible, with / in the introduction – hemolysis.

Influence on the ability to drive or work with machinery:
Causes sedation. Use with caution in patients whose activities are associated with the need for high concentration of attention and rapid psychomotor reactions.

Patient interaction:

It is an inhibitor of P450 2D6 and in high doses can interact with substrates CYP2D6. Inhibitors of hepatic enzymes have the potential to increase the concentration of hydroxyzine in the blood.
Hydroxysin enhances the effect of alcohol, narcotic analgesics, tranquilizers, anxiolytics, barbiturates, hypnotics.
Joint use with MAO inhibitors should be avoided.
Prevents the development of the pressor effect of epinephrine (adrenaline), anticonvulsant activity of phenytoin, the action of betagistin and anticholinesterase drugs.
Does not change the effect of atropine, alkaloids belladonna, digitalis, hypotensive drugs, H2-antihistamines.
It reduces side effects (from the digestive tract) theophylline.

Storage conditions:

List B. In a dry place, at a temperature below 25 ° C
Shelf life is indicated on the package.
Terms of leave from the pharmacy – on prescription