The derivative of diphenylmethane is the hydroxyzine. The instructions for use state that the substance is a white fine powder, highly soluble in water and odorless. 374.9 grams per mole is the molecular weight of the compound.
Clinical and pharmacological group
The drug has a sedative, anxiolytic effect. This is due to the inhibitory effect on the activity of certain subcortical structures of the central nervous system as well as the blocking effect on the central H_1-histamine and m-cholinergic receptors.
"Hydroxyzine", analogues of the drug have a pronounced sedative effect and moderate anxiolytic activity. They have a stimulating effect on cognitive abilities, improve attention and memory. Mental dependence and addiction do not occur, after prolonged use of withdrawal syndrome is not observed. Anticholinergic, antihistamine, antispasmodic effects are also manifested. "Hydroxyzine" relieves spasm of smooth muscles, thereby causing bronchodilating and analgesic effects, has an antiemetic effect and a moderate inhibitory effect on gastric secretion. When urticaria, dermatitis, eczema, etc., itching decreases with therapy with Atarax (hydroxyzine - the active substance).
The instruction says that a
sedative effect is achieved, as a rule, within 10-45 minutes after ingestion (depending on the form of the drug), antihistamine - an hour after ingestion. In patients with liver pathology, an antihistamine effect can be expected within 96 hours.
Mutagenic and carcinogenic effects of the drug are not observed.
Pharmacokinetics
When ingested, the drug is rapidly absorbed from the gastrointestinal tract, C_max is observed after two hours. The drug "Hydroxyzine" passes through the placenta and the BBB (the degree of concentration in the tissues of the embryo is greater than in the tissues of the mother). In the process of metabolism, cetirizine, the main metabolite, is formed in the liver. The value of T_1 / 2 depends on the age of the patient and can be 7 hours for children aged 2-10 years, 20 hours for adults, 29 hours for the elderly and the elderly; in patients with liver pathology, it can increase up to 37 hours. Excretion is carried out mainly by the kidneys (0.8% in its original form).
Indications for use
"Hydroxysine hydrochloride" is used to:
- eliminate anxiety and increased excitability of the nervous system;
- during withdrawal symptoms in persons with alcohol dependence;
- therapeutic treatment for psychoneurotic disorders;
- as part of complex treatment in the postoperative period and after some injuries;
- premedication
- to reduce internal stress, generalized anxiety, restore adaptation processes, in the complex therapy of somatic diseases;
- to eliminate the symptoms of eczema, itchy dermatosis, urticaria, atopic dermatitis;
- for antiemetic action according to indications.
Contraindications to the drug "Hydroxysin Canon"
Doctors' reviews indicate that the drug is not recommended for use:
- glaucoma patients;
- with hypertrophy of the prostate (prostate gland);
- patients who have increased convulsive activity;
- patients with myasthenia gravis;
- patients who are diagnosed with renal and liver failure;
- patients with dementia.
The drug is contraindicated:
- pregnant women;
- porphyria patients;
- during breastfeeding (for the period of treatment it is necessary to refuse breastfeeding);
- with allergic manifestations to the constituent substance (also in cases where hypersensitivity to other derivatives of cetirizine, aminophylline, piperazine or ethylenediamine was previously noted);
- during the period of labor.
About side effects
Patients may suffer from drowsiness, note general weakness, dizziness and headache at the beginning of therapy with Hydroxysin. The reviews of patients taking this drug indicate the following side effects:
- allergic reactions, palpitations, nausea;
- urinary retention, constipation;
- dry visible mucous membranes, increased sweating;
- visual impairment (violation of accommodation is possible);
- lowering blood pressure, increasing the enzymatic activity of the liver;
- bronchospasm may be noted.
Manifestations of seizures, tremors and disorientation, ataxia, paradoxical agitation and increased motor activity when using the drug are very rare.
Overdose
The vomiting reflex is caused first or the stomach is washed in case of an overdose of the Hydroxysin preparation. Instructions for use informs that in some cases it is necessary to monitor the vital functions of the patient, the introduction of caffeine-sodium benzoate, norepinephrine and even blood substitutes, all necessary measures are taken to maintain the adequate functioning of the body. This remedy does not have specific antidotes; hemodialysis is not justified.
Most often, these effects are reversible or their manifestations disappear after a review of the daily dosage.
Dosage and route of administration
The drug is administered orally or as an intramuscular injection. The dose depends on the nosology, age of the patient and on the form in which the drug "Hydroxyzine" is produced.
Instructions for use indicate that with symptomatic therapy for anxiety syndrome, adults are recommended to take from 25 to 100 mg of the constituent substance per day. The most commonly used dosage is 12.5 mg in the morning and at lunch and 25 in the evening.
In childhood, in the preoperative period, 1 mg per kg of live weight is used the day before in the evening and 60 minutes before the procedure itself.
For the purpose of sedation, adults are administered Hydroxysin in a dosage of 50-200 mg of the drug inside or in the form of an intramuscular injection of 1.5-2.5 mg per kg of patient weight one hour before surgery.
In order to stop itching, an effective dosage is from 25 to 100 mg of the drug in 3-4 doses.
For children from one year to 6 years, the dose of the drug does not exceed the value of 1-2.5 mg per kg of body weight per day in several doses.
In the same dosage regimen, children over the age of 6 are prescribed 1-2 mg per kg of body weight per day.
The maximum daily dosage is 300 mg. The maximum single dosage is 200 mg.
For elderly people, the initiation of therapy is recommended to be carried out in half dosage.
Hepatic and renal failure require dosage adjustment of the drug "Hydroxysin".
The instruction warns that to achieve the fastest therapeutic effect, the solution is administered intramuscularly, deeply in a dose of 50-100 mg at a time. The introduction of the drug in 4-6 doses per day is recommended.
In psychiatry, the drug is used in a dosage of up to 300 mg per day. The duration of this therapy is 4 weeks.
In case of side effects such as weakness, drowsiness, which do not stop for several days, the dose should be reduced.
Precautionary measures
With the simultaneous administration of "Hydroxysin" with "Adrenaline", the effectiveness of the latter decreases.
The drug has an enhancing effect on the sedative effect of narcotic analgesics, alcoholic beverages, tranquilizers, barbiturates, drugs used for sleeping pills, as well as other drugs that inhibit the central nervous system.
The combined use of this substance with MAO inhibitors or anticholinergics is not recommended.
When combining the drug with phenytoin, the anticonvulsant effect of taking the latter decreases.
The simultaneous use of this drug with cholinesterase blockers is undesirable.
A consequence of increasing the plasma concentration of the drug substance can be its use with inhibitors of liver enzymes.
Simultaneous therapy with drugs that inhibit the function of the central nervous system, or with anticholinergic drugs, requires dose adjustment.
With great caution, it is necessary to prescribe the drug to patients who are prone to arrhythmias or who use antiarrhythmic drugs, as well as to those patients who are predisposed to convulsive manifestations.
Conducted therapy is a contraindication for the use of alcoholic beverages. If it is necessary to conduct tests for allergic reactions, the administration of "Hydroxysin" must be canceled 5 days before the scheduled study. Caution is also necessary when using the drug during the period of driving a vehicle by drivers and patients whose profession requires an increased concentration of attention.
It should be borne in mind that the use of injection forms is possible only in the form of intramuscular injections. Subcutaneous administration of the drug or the ingress of the latter into large vessels can cause tissue damage.
Therapy with this tool can cause false results of allergological testing.
Terms of use and storage
Mandatory availability of a prescription for the drug "Hydroxyzine".
Instructions for use say that the oral form of the drug is stored for no more than 5 years.
"Hydroxyzine." Patient Reviews
In childhood, the use of the drug for hyperactivity, reduced concentration of attention helps the child to be confident, focused and attentive, eliminates a sharp change in mood. At the same time, during treatment with Atarax (Hydroxyzine), the instructions for use confirm that the child’s activity and cheerfulness remain the same. Side effects are rare.
According to the statements of patients who use Hydroxyzine (drug analogues) in certain cases, it follows that it causes calm and self-confidence to a greater extent than many other drugs. In panic attacks and insomnia, this substance contributes to better falling asleep and a better sleep. True, the withdrawal of the drug for the first few days has a severe effect on the process of falling asleep, but in principle the effect of therapy is very encouraging.
Drug price
You can buy the drug "Hydroxyzine", analogues, which contain hydroxyzine, in a pharmacy by prescription. The price will be 270-300 rubles for 25 tablets in a dosage of 25 mg.
"Hydroxyzine." Synonyms
The synonyms of Hydroxyzine are: Hydroxyzine Canon, Atarax, Masmoram, Atherax, Hydroxyzine, Hydroxyzine Hydrochloride, Alamon, Durax.