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Mechanism of action

Derived piperazine, has moderate anxiolytic activity; also has a sedative, antiemetic, antihistamine and M-anticholinergic action. It blocks the central M-cholino and H1-histamine receptors and inhibits the activity of certain subcortical zones. Does not cause psychological dependence and addiction. The clinical effect occurs within 15-30 minutes after ingestion. It has a positive effect on positive abilities, improves memory and attention. Relaxes skeletal and smooth muscles, has bronchodilating and analgesic effects, moderate inhibitory effect on gastric secretion.

Absorption is high. TCmax after oral administration - 2 hours; T1 / 2 in adults - 12-20 hours, in children - 7 hours. Metabolites are found in breast milk.

Indications and usage

Hyperexcitability, anxiety; psychoneurotic conditions; abstinence alcohol syndrome; atopic dermatitis, eczema, pruritic dermatosis, urticaria; sedation; the postoperative period (as part of combination therapy); vomiting.

Inside, while eating, not chewing. Adults - 25-100 mg / day in 1-4 doses, for sedation - 50-200 mg 1 hour before surgery; in psychiatry, 100–300 mg / day, In anesthesiology, 1 mg / kg is prescribed the night before the operation and 1 hour before the operation.For a short-term effect, apply half the dose; if necessary, obtain a rapid therapeutic effect is prescribed in / m (in the area of ​​large muscles), with the subsequent transition to oral administration. Children from 1 year to 6 years for symptomatic treatment of itching - 1 mg / kg / day, maximum - 2.5 mg / kg / day; From 6 years old - 1 mg / kg / day, maximum - 2 mg / kg / day in several doses. In older patients, treatment begins with a half dose. In renal and / or hepatic insufficiency, the doses should be reduced.

Adverse reactions

Drowsiness, weakness, dry mouth; headache, dizziness, tremor, ataxia, acute glaucoma, acute urinary retention, tachycardia, constipation, accommodation disturbance, excessive sweating, decrease in blood pressure, increased transaminase activity, bronchospasm, allergic reactions. Overdose. Symptoms: pronounced anticholinergic action, depression or paradoxical stimulation of the central nervous system, tremor, convulsions, disorientation; rarely - lowering blood pressure, confusion, nausea, vomiting, involuntary physical activity, hallucinations, arrhythmia. Treatment: gastric lavage, with a significant decrease in blood pressure - in / in the infusion of blood substitutes, norepinephrine (epinephrine can not be entered), monitoring vital functions. To prevent the inhibitory effect on the central nervous system - parenteral administration of caffeine sodium benzoate. There is no specific antidote. Hemodialysis is ineffective.

Contraindications

Hypersensitivity (including Cetirizine and other piperazine derivatives, aminophylline and ethylenediamine), porphyria; pregnancy; lactation period; period of labor activity;. With care - myasthenia gravis, prostatic hyperplasia with clinical manifestations, difficulty urinating, constipation, dementia, increased intraocular pressure, a tendency to convulsive seizures, arrhythmia or antiarrhythmic drugs, renal / hepatic failure.

Special notes

It is necessary to refrain from engaging in potentially hazardous activities that require increased attention and quick mental and motor responses. The injection form is intended only for intramuscular injection (in the area of ​​large muscles). If accidentally injected under the skin, it can cause significant tissue damage. There are practically no methods for determination in biological fluids and tissues. If it is necessary to conduct allergological tests, the drug should be stopped 5 days before the study.

Drug Interactions

Enhances the action of opioid and non-opioid analgesics, barbiturates, anxiolytics, ethanol. Enhances the anticholinergic effect of antihistamines, antipsychotics (neuroleptics) and antidepressants. Interferes with the development of the pressor effect of epinephrine, alters the antiepileptic effect of phenytoin. Atropine and othersM-holinoblokatory effect on the activity of hydroxyzine do not have. Reduces the effect of betahistine and anticholinesterase drugs.