Pharmacodynamics and pharmacokinetics
The substance blocks the work of central n1-histamine and m-cholinergic receptors . The drug exhibits a sedative effect and has moderate anxiolytic activity . Hydroxyzine is a fairly mild tranquilizer that also has an antiemetic effect.
The product improves cognitive abilities, attention and accelerates memory processes. As a rule, Hydroxyzine preparations do not cause dependence, either mental or physiological. Even after prolonged use, withdrawal syndrome does not develop.
This substance also has antispasmodic, antihistamine and anticholinergic effects, relieves pain and moderately inhibits the production of gastric acids. The medicine is often prescribed to reduce itching in eczema, urticaria, dermatitis , etc.
Depending on the dosage form, the effect of taking the substance will be observed within 10-40 minutes. The antihistamine effect occurs 60 minutes after oral administration.
After taking the tablets, the substance is quickly absorbed by the body. Reaches its maximum concentration in the blood within 2 hours. The drug overcomes the blood-brain and placental barriers. The half-life is up to 7 hours in children, about 20 in adults.
In persons suffering from liver failure, due to the fact that the drug is metabolized in the liver (metabolite - ceterizine ), the antihistamine effect can last a long time (more than 90 hours), and the half-life will increase to 37.
Pharmacokinetic parameters in elderly people are slightly altered, the half-life lasts up to 29 hours. Hydroxyzine is excreted through the kidneys in the form of metabolites, less than one percent remains unchanged.
During clinical trials and animal studies, no carcinogenic or mutagenic effects of the drug on the body were revealed.
Indications for use
Hydroxyzine hydrochloride is prescribed:
- to eliminate anxiety and increased excitability of the nervous system;
- alcoholics during abstinence;
- for psychoneurotic disorders ;
- as part of complex treatment after operations and some injuries;
- for premedication ;
- with internal tension, adaptation disorders, generalized anxiety , somatic diseases;
- to relieve symptoms of atopic dermatitis, itchy dermatosis, urticaria, eczema ;
- as an antiemetic according to indications.
Release form and composition
Dosage form – film-coated tablets: white, round, convex on both sides, scored; on a cross section, almost white in color (10 and 25 pieces each in blister packs, in a cardboard pack 1 or 2 packages of 25 tablets or 2, 3 or 5 packages of 10 tablets).
Active substance: hydroxyzine hydrochloride, 1 tablet – 25 mg.
Additional components:
- excipients: mannitol, magnesium stearate, pregelatinized corn starch, microcrystalline cellulose, colloidal silicon dioxide;
- shell: opadry white, including hyprolose (hydroxypropylcellulose), hypromellose (hydroxypropylmethylcellulose), titanium dioxide.
Contraindications
The medicine is not recommended for use:
- patients with glaucoma ;
- with prostatic hypertrophy ;
- if the patient has increased seizure activity;
- with myasthenia gravis ;
- patients with renal and liver failure;
- for dementia ;
- pregnant women;
- with porphyria ;
- during lactation;
- if you are allergic to the active substance, including if hypersensitivity reactions to other piperazine derivatives, cetirizine, ethylenediamine or aminophylline ;
- during labor.
Substitutes for their effect on the body
Substitutes for Hydroxyzine are also medications with different active ingredients, but having the same therapeutic direction as it.
Grandaxin
Grandaxin belongs to the pharmacological group of psycholeptic and tranquilizer medications, with the main active component tofisopam. Grandaxin is able to correct the functioning of the psycho-vegetative system and does not have an anticonvulsant or strong sedative effect. The medication gently calms the central nervous system and relieves the patient's heightened sense of anxiety.
Elderly patients, as well as those with severe mental pathologies, most often develop negative effects. This must be taken into account when prescribing.
Grandaxin is prescribed for mental and neurotic conditions:
- strong emotional overexcitation;
- dysfunction of the nervous system;
- increased level of anxiety;
- apathy;
- depression;
- obsessive thoughts and experiences.
Grandaxin is often prescribed to patients after suffering severe mental trauma or stress. Often, women during menopause and PMS are prescribed Grandaxin in monotherapy or as part of a complex with hormonal drugs. The drug is used in cardiology, as well as for the treatment of myopathy and myasthenia gravis, when neurotic conditions manifest themselves as a result of complications of these diseases. Grandaxin quickly copes with alcohol withdrawal syndrome and related conditions.
The medication is not prescribed for:
- allergies to the composition;
- pronounced aggression and depression;
- disorders in the functioning of the cardiac and respiratory systems.
Also not prescribed during lactation and in the 1st trimester of pregnancy and in pediatrics. The medication can be used with caution in patients with the following pathologies:
- glaucoma;
- epilepsy;
- systemic atherosclerosis;
- respiratory failure.
The dosage and duration of the therapeutic course are determined by the doctor based on the pathology of each patient and the stage of its progression. Standard dosages are 1-2 tablets 1-3 times a day. The daily minimum is 3 tablets.
Adverse reactions manifest themselves in the form of skin allergies, dyspepsia and jaundice, as well as excessive effects on the central nervous system (drowsiness, headache and dizziness), disturbances in heart rhythm and soreness in the muscular system.
Noofen
Noofen is a psychostimulant and nootropic drug based on phenibut. The effectiveness of this drug has 3 directions:
- antihypoxic and antimnestic effect;
- tranquilizing effect;
- corrective cognitive functions.
Noofen increases a person's intelligence, memory quality and concentration. The medication helps schoolchildren remember academic topics more easily, increases the efficiency, attentiveness and perseverance of students.
Noofen is used for:
- emotional overexcitation and anxiety;
- decreased memory, concentration and attention;
- reduced intellectual development;
- asthenic condition;
- neuroses and psychopathy;
- anxiety, an unreasonable feeling of fear;
- childhood enuresis, stuttering;
- alcohol syndrome;
- deviations in the functioning of the vestibular apparatus;
- menopause in women.
Noofen is not prescribed in the following cases:
- kidney dysfunction;
- allergy to the composition of the medicine;
- children 8 years old and during lactation in women.
Doses are prescribed personally. Standard dosages for children over 8 years of age are 250-500 mg per day, and for adults - 250-750 mg per day. The duration of drug therapy is 21-45 days.
Negative effects occur very rarely, but patients still noted the following reactions:
- urticaria, redness of the epidermis and swelling of the larynx;
- dizziness and weakening of muscle tone;
- dyspepsia with nausea and diarrhea;
- headache.
Afobazole
Afobazole is an anti-anxiety medication. The active ingredient is fabomotizole, which is an anxiolytic. The medicine is prepared in tablet form.
Fabomotizol affects neuron receptors in the brain, stabilizes the effects of gamma-aminobutyric acid, and corrects the transmission of impulses from neurons along the fibers of the nervous system. The drug is also a neuroprotector that protects parts of the brain from hypoxia and the action of free radicals due to oxygen deficiency or intoxication (alcohol, medications, poisons and poisonous gases).
The drug is prescribed for the following reasons:
- asthenic (alcohol) syndrome;
- anxiety disorders;
- lupus erythematosus;
- cerebral and myocardial ischemia;
- bronchial asthma;
- cardiac arrhythmia and hypertension;
- itching of the skin and allergic dermatitis;
- oncological neoplasms.
The drug is also prescribed during the period of abstinence from nicotine and alcohol, for neurocirculatory dystonia, and for women with PMS. Afobazole is not used in pediatric practice, during lactation and pregnancy, as well as in case of allergic reactions in a patient to the medicinal composition of Afobazole.
The tablet is taken after meals. The daily dosage is 30 mg, divided into 3 administration procedures. The doctor may double the dosage if necessary. The average therapeutic course will last 2-4 weeks. The doctor sets the treatment regimen individually for each patient and, based on the dynamics of therapy, the course can be increased to 2 months.
Adverse reactions are manifested by symptoms of central nervous system depression - body fatigue, headache, drowsiness, as well as allergic reactions - urticaria, allergic rhinitis and shortness of breath.
Side effects
In the first few days of using Hydroxyzine, drowsiness, general weakness, dizziness and headache may occur.
The following may also appear:
- tachycardia , allergic reactions, nausea;
- constipation and urinary retention;
- dry mucous membranes, increased sweating;
- disturbances of vision and accommodation of the eye;
- low blood pressure , fever , increased levels of liver enzymes;
- bronchospasm.
Very rarely, patients undergoing treatment with Hydroxyzine experienced convulsions, tremors and disorientation , paradoxical agitation and increased motor activity, ataxia .
As a rule, most reactions are transient or disappear after reducing the daily dosage.
Hydroxyzine, instructions for use (Method and dosage)
The drug is prescribed orally or intramuscularly , depending on the form of release, disease and age.
For the symptomatic treatment of anxiety, adults are recommended to take 25 to 100 mg of the substance per day. As a rule, 12.5 mg is used in the morning and at lunch and 25 before bed.
Children before surgery are prescribed 1 mg per kg of weight 60 minutes before the procedure. Administration of one dose the night before is also indicated.
Premedication for adults is carried out in dosages of 50 to 200 mg orally or 1.5-2.5 mg per kg of patient weight intramuscularly , one hour before surgery.
To eliminate itching, use from 25 to 100 mg of the drug, 3-4 times a day.
For the treatment of itching in children from one to 6 years of age, 1-2.5 mg per kg of child weight per day is prescribed, in several doses.
Children over 6 years of age - from 1 to 2 mg per kg of body weight per day, the dosage regimen is the same.
The maximum daily dosage is 300 mg. The maximum single dosage is 200 mg.
Elderly persons are recommended to begin treatment with doses reduced by half.
In case of hepatic and renal failure, dose adjustment is required.
If you need to quickly achieve a therapeutic effect, Hydroxyzine solution is administered intramuscularly , deeply, 50-100 mg at a time. It is recommended to administer the drug every 4-6 hours.
Cost of medicines
Hydroxyzine is in the middle price segment. Foreign analogues are much more expensive than the original medication.
Name of the drug and its analogues | Dosage of the main component in mg | Quantitative composition of packaging | average price |
Hydroxyzine | 25 10 | 10 10 | 255-280 230-235 |
Atarax | 25 | 25 | 327-330 |
Sonanorma | 25 | 10 | 221-230 |
Grandaxin | 50 50 | 60 20 | 854-880 369-380 |
Noofen | 250 | 20 | 973-990 |
Afobazole | 10 | 60 | 532-550 |
Gidazepam | 50 | 10 | 98-110 |
Phenazepam | 25 | 50 | 171-190 |
Overdose
If therapeutic doses are exceeded, the following may develop: tremor , hallucinations , convulsions , hypersedation , low blood pressure, nausea, disorientation and confusion .
If an overdose of tablets occurs, it is recommended to induce vomiting and rinse the stomach. Monitoring of the patient's vital functions, administration of norepinephrine , caffeine sodium benzoate and blood substitutes are also indicated, measures should be taken to maintain the normal functioning of the body. The drug does not have a specific antidote ; hemodialysis is not performed.
Interaction
Hydroxyzine reduces the effectiveness of adrenaline .
The drug enhances the sedative effect of taking narcotic analgesics, tranquilizers, alcohol, barbiturates, hypnotics , and other drugs that depress the central nervous system.
It is not recommended to combine this substance with anticholinergics or MAO inhibitors .
The drug reduces the anticonvulsant effect of taking phenytoin .
The medicine is not recommended to be combined with cholinesterase .
The drug inhibits P450 2D6 and in high dosages may cause interaction with CYP2D6 .
When used in combination with liver enzyme inhibitors, the plasma concentration of the drug may increase.
special instructions
The doctor calculates the dose for children individually, taking into account body weight and in accordance with dosage recommendations. It should be taken into account that the minimum dose after dividing the tablet is 12.5 mg.
If it is necessary to conduct a methacholine test or perform allergy tests, you should stop taking the drug 5 days before. Otherwise, you may get false results.
The dose of Hydroxyzine Canon should be reduced when simultaneously prescribing drugs that depress the central nervous system (CNS) or drugs with m-anticholinergic properties.
The drug may prolong the QT interval on the electrocardiogram (ECG). When used in combination with other drugs that can interfere with cardiac activity, the risk of developing arrhythmias increases. It is believed that other drugs that cause ECG changes (eg, tricyclic antidepressants, antiparkinsonian drugs, phenothiazines, lithium carbonate, atropine, thioridazine, procainamide, quinidine) may enhance and aggravate the changes caused by hydroxyzine, thereby increasing the risk of sudden death. For this reason, it is recommended to avoid the simultaneous use of two or more drugs that prolong the QT interval, as additive effects may occur that could lead to the development of severe and potentially life-threatening arrhythmias.
During treatment, you should refrain from drinking alcohol and engaging in potentially hazardous activities that require quick reactions and increased attention.
Reviews of Hydroxyzine
Some reviews about the medicine:
- “... Before using this medicine, I tried everything. Grandaxin , Coaxil, nothing helped me. Only with Hydroxyzine did I feel better, calmer and more confident”;
- “... I was prescribed medicine for panic attacks and insomnia. After taking it I slept very well. When you stop drinking, of course, it’s hard to stop drinking at first, but overall I liked the effect of the medicine.”
- “A neurologist recently prescribed this drug to my daughter; she is too mobile and has decreased concentration. During treatment, my daughter remained active and cheerful, but became more confident, focused and attentive, and her mood stopped changing sharply. I didn’t notice any adverse reactions.”