Ibuprofen and hydroxyzine

Tab., coated film coated, 25 mg: 20, 25, 30 or 50 pcs.

10 pcs. - cellular contour packings (2) - packs of cardboard.
10 pcs. - cellular contour packings (3) - packs of cardboard.
10 pcs. - cellular contour packings (5) - packs of cardboard.
25 pcs. - cellular contour packings (1) - packs of cardboard.
25 pcs. - cellular contour packings (2) - packs of cardboard.

Clinical and pharmacological group: Anxiolytic (tranquilizer)

Pharmacotherapeutic group: Anxiolytic agent (tranquilizer)

Pharmacological action

Hydroxyzine is a blocker of H ₁ -histamine receptors of the first generation, a derivative of phenothiazine with antimuscarinic and sedative properties and diphenylmethane, promotes inhibition of the activity of certain subcortical zones.

H ₁ has a histamine blocking, bronchodilating and antiemetic effect, has a moderate inhibitory effect on gastric secretion. Hydroxyzine significantly reduces itching in patients with urticaria, eczema, and dermatitis.

Hydroxyzine has a positive effect on cognitive abilities, improves attention and memory. Hydroxyzine does not cause addiction and psychological dependence, with prolonged use of the withdrawal syndrome was not observed.
Hydroxyzine is capable of depressing the central nervous system, also has anticholinergic, antihistamine, antispasmodic, local anesthetic, sympatholytic effects, and has muscle relaxant activity.

In hepatic insufficiency H ₁ - histamine-blocking effect may be prolonged up to 96 hours after a single dose. It has moderate anxiolytic activity.

Polysomnography in patients with insomnia and anxiety demonstrates an increase in sleep duration, a decrease in the frequency of nocturnal awakenings after taking a single or repeated dose of hydroxyzine at a dose of 50 mg. A decrease in muscle tension in patients with anxiety was noted when taking the drug at a dose of 50 mg 3 times a day.

H ₁ - histamine-blocking effect occurs approximately 1 hour after oral administration of the tablets. The sedative effect appears after 30-45 minutes.

Pharmacokinetics

Absorption

Absorption is high. TC _max after oral administration - 2 hours. After taking an average dose of 50 mg, TC _max in adults is 70 mg / ml.

Distribution

The distribution coefficient is 7-16 l/kg in adults. Hydroxyzine crosses the blood-brain barrier and the placenta, concentrating more in fetal than maternal tissues. After oral administration, hydroxyzine penetrates the skin well, while the concentration of hydroxyzine in the skin is much higher than the concentration in the blood serum, both after single and after multiple doses. The plasma concentration of hydroxyzine does not necessarily reflect its binding to tissues or distribution to skin receptors. It has an effect on skin inflammation depending on the serum concentration.

Metabolism

Hydroxyzine is metabolized in the liver. Cetirizine - the main metabolite (45%) is a blocker of H ₁ -histamine receptors. Metabolites are found in breast milk.

Elimination

T _1/2 in adults - 14 hours (range: 7-20 hours). The total clearance of hydroxyzine is 13 ml / min / kg. About 0.8% of hydroxyzine is excreted unchanged through the kidneys. The main metabolite cetirizine is excreted mainly in the urine, also unchanged (25% of the dose of hydroxyzine taken).

Pharmacokinetics in special groups of patients

In elderly patients

In elderly patients T _1/2 was 29 hours. The volume of distribution is 22.5 l/kg. It is recommended to reduce the daily dose of hydroxyzine when administered to elderly patients.

Children under 1 year old

In children, the total clearance is 2. 5 times higher than in adults. The dose must be adjusted. T _1/2 4 hours.

Children aged 1 to 14

T _1/2 11 o'clock.

In patients with hepatic insufficiency

In patients with secondary liver dysfunction due to primary biliary cirrhosis, the total clearance was approximately 66% of the value recorded in healthy volunteers. In patients with liver disease, T _1/2 increased up to 37 hours, the concentration of metabolites in the blood serum is higher than in young patients with normal liver function. Patients with hepatic insufficiency are advised to reduce the daily dose or frequency of administration.

In patients with renal insufficiency

The pharmacokinetics of hydroxyzine was studied in 8 patients with severe renal insufficiency (creatinine clearance 24+7 ml/min). The duration of exposure to hydroxyzine did not change significantly, while the duration of exposure to cetirizine was increased. To avoid any significant accumulation of the cetirizine metabolite after repeated use of hydroxyzine in patients with impaired renal function, the daily dose of hydroxyzine should be reduced.

Indications of the drug Hydroxyzine Canon

• symptomatic treatment of anxiety in adults;
• as a sedative during premedication;
• symptomatic treatment of itching of allergic origin.

Open list of ICD-10 codes

Dosage regimen

The drug is used orally.

Children:

For the symptomatic treatment of itching of allergic origin:

From 3 to 6 years of age: 1.0 mg/kg/day to 2.5 mg/kg/day in divided doses.

Ages 6 years and older: 1.0 mg/kg/day to 2.0 mg/kg/day in divided doses.

For premedication: 1 mg/kg at night before anesthesia.

The dosage is calculated by the doctor individually depending on the body weight of the child in accordance with the recommended doses, it should be noted that the minimum dosage received, after dividing the tablet, is 12.5 mg.

Adults:

For symptomatic treatment of anxiety: standard dose of 50 mg per day divided into 3 doses (1/2 tablet (12.5 mg) in the morning, 1/2 tablet (12.5 mg) in the afternoon

For the symptomatic treatment of allergic pruritus: initial dose 1 tablet (25 mg) at bedtime, if necessary, the dose may be increased to 1 tablet (25 mg) 3-4 times daily.0017

For premedication in surgical practice: 2-8 tablets (50-200 mg) at night before anesthesia.

Single maximum adult dose should not exceed 8 tablets (200 mg), the maximum daily dose is not more than 12 tablets (300 mg).

Use in special groups of patients:

When used in the elderly, the dose is selected individually, taking into account concomitant diseases in the recommended dose range (see section Pharmacokinetics).

Use in patients with renal insufficiency and impaired liver function:

Patients with severe and moderate renal insufficiency, as well as with hepatic insufficiency, dose reduction is necessary. In patients with hepatic insufficiency, it is recommended to reduce the daily dose by 33%. In patients with severe and moderate renal insufficiency, the drug is used in half the dose due to a decrease in the excretion of the main metabolite of hydroxyzine, cetirizine.

Side effects

Possible side effects are listed below by body system and frequency of occurrence.

WHO classification of side effects:

very common - ≥1/10 prescriptions (>10%)

common - ≥1/100 to <1/10 prescriptions (>1% and <10%)

infrequently - from ≥ 1/1000 to <1/100 appointments (>0. 1% and <1%)

rarely - from ≥ 1/10000 to <1/1000 appointments (>0.01% and <0.1%)

very rare - <1/10000 prescriptions (<0.01%)

The most common adverse reactions were drowsiness, headache, lethargy, dry mouth and fatigue.

Immune system disorders:

rare: hypersensitivity;

very rare: anaphylactic shock.

Nervous system disorders:

Uncommon: dizziness, insomnia, tremor;

rare: convulsions, dyskinesia.

infrequently: agitation, confusion;

rare: hallucinations, disorientation.

Eye disorders:

rare: disturbance of accommodation, visual impairment.

Cardiac disorders:

rare: tachycardia;

frequency unknown: prolongation of the QT interval on the electrocardiogram, ventricular tachycardia of the "pirouette" type.

Vascular disorder:

rare: decrease in blood pressure.

Respiratory, thoracic and mediastinal disorders:

very rare: bronchospasm.

Gastrointestinal disorders:

infrequently: nausea; rarely: vomiting, constipation.

Liver and biliary disorders:

rare: abnormal liver function tests;

frequency unknown: hepatitis.

Renal and urinary disorders:

rare: urinary retention.

Rut and subcutaneous tissue disorders:

rare: pruritus, rash (erythematous, maculo-papular), urticaria, dermatitis;

very rare: angioedema, increased sweating, acute generalized exanthematous-pustular rash, erythema multiforme, Stevens-Johnson syndrome.

General disorders:

rare: hyperthermia, malaise.

The following side effects have been observed with cetirizine, the main metabolite of hydroxyzine: thrombocytopenia, aggression, depression, tic, dystonia, paresthesia, oculogeric crisis, diarrhea, dysuria, enuresis, asthenia, edema, weight gain and may occur with hydroxyzine.

Contraindications for use

• hypersensitivity to any of the components of the drug, cetirizine and other piperazine derivatives, aminophylline or ethylenediamine;
• porphyria;
• children under 3 years of age;
• pregnancy, childbirth and breastfeeding.

With caution: in myasthenia gravis, prostatic hyperplasia with clinical manifestations, difficulty urinating, constipation, glaucoma, dementia, convulsive disorders, including epilepsy, with a tendency to arrhythmias, including electrolyte imbalance (hypokalemia, hypomagnesemia), in patients with a history of heart disease (with heart failure and arterial hypertension) or with the use of drugs that can cause arrhythmia, with hyperthyroidism. Hydroxyzine contributes to a decrease in gastrointestinal motility, the development of a stenosing peptic ulcer, and respiratory failure.

Use during pregnancy and lactation

Hydroxysin Canon is contraindicated during pregnancy, childbirth and breastfeeding.

Use in hepatic impairment

Patients with hepatic impairment require a dose reduction. In patients with hepatic insufficiency, it is recommended to reduce the daily dose by 33%.

Use in Impaired Renal Function

Patients with severe to moderate renal impairment require dose reduction. In patients with severe and moderate renal insufficiency, the drug is used in half the dose due to a decrease in the excretion of the main metabolite of hydroxyzine, cetirizine.

Use in children

Contraindicated in children under 3 years of age.

Use in elderly patients

When used in elderly patients, the dose is selected individually, taking into account concomitant diseases in the recommended dose range (see section Pharmacokinetics).

Special instructions

When used simultaneously with drugs with m-anticholinergic properties and drugs that depress the central nervous system, the dose of hydroxyzine must be reduced.

Hydroxyzine can lead to prolongation of the QT interval on the electrocardiogram, so concomitant use with other drugs that can interfere with cardiac activity may increase the risk of arrhythmias. It is suggested that other drugs that cause changes in the electrocardiogram (atropine, antiparkinsonian drugs, lithium carbonate, quinidine, phenothiazines, procainamide, tricyclic antidepressants, thioridazine) may exacerbate and exacerbate the changes that can be caused by hydroxyzine and increase the risk of sudden death. The simultaneous use of two or more drugs that prolong the QT interval should be avoided because of the risk of additive effects that can lead to the development of potentially life-threatening and severe cardiac arrhythmias.

Doses should be reduced in case of renal and/or hepatic insufficiency.

In the elderly, the dosage should be adjusted individually, starting with half the minimum dose, and adjusting in the range of recommended doses. If it is necessary to set up allergic tests or conduct a methacholine test, taking the drug Hydroxysin Canon should be discontinued 5 days before the study to prevent obtaining distorted data.

Alcohol should be avoided during treatment with Hydroxysin Canon.

Influence on the ability to drive vehicles and mechanisms

Canon hydroxyzine may impair the ability to concentrate and the speed of psychomotor reactions. Taking other sedative medicines may increase this effect. Therefore, one should refrain from driving vehicles and engaging in other potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.

Overdose

Symptoms of CNS toxicity are associated with excessive m-anticholinergic action, suppression or paradoxical stimulation of the CNS. These symptoms include nausea, vomiting, tachycardia, pyrexia, drowsiness, impaired pupillary reflex, tremors, confusion, or hallucinations. Subsequently, depression of consciousness, respiration, convulsions, lowering blood pressure, and arrhythmia may develop. Possible aggravation of coma and cardiopulmonary collapse.

Treatment: It is necessary to control the state of the respiratory tract, the state of respiration and circulation using Electrocardiographic (ECG) monitoring, to ensure adequate oxygenation. Heart activity and blood pressure should be monitored within 24 hours after the symptoms disappear.

At high doses, hydroxyzine can lead to QT interval prolongation and marked electrocardiogram changes.

In case of mental status disturbance, other drugs or alcohol should be avoided, if necessary, the patient should be given oxygen inhalation, naloxone, dextrose (glucose) and thiamine. The use of analeptics is not allowed.

If a vasopressor effect is needed, norepinephrine or metaraminol is given. Epinephrine should not be used. In case of ingestion of a significant amount of the drug, it is possible to perform gastric lavage with previous endotracheal intubation. Activated charcoal may be used, but there is insufficient evidence to support its effectiveness. There is no specific antidote. Hemodialysis is not effective.

Literature data indicate that in the case of the development of severe, life-threatening, intractable m-anticholinergic effects that are not stopped by other drugs, it is possible to use a therapeutic dose of physostigmine. Physostigmine should not be used solely to bring the patient to consciousness. If the patient was taking tricyclic antidepressants, the use of physostigmine can provoke seizures and irreversible cardiac arrest. The use of physostigmine should also be avoided in patients with cardiac conduction disorders.

Drug interactions

It is necessary to take into account the potentiating effect of hydroxyzine when used together with drugs that depress the central nervous system (CNS), such as narcotic analgesics, barbiturates, tranquilizers, hypnotics, alcohol. In this case, their doses should be selected individually. Simultaneous use with MAO inhibitors (MAO) and anticholinergics should be avoided. The drug interferes with the pressor action of epinephrine and the anticonvulsant activity of phenytoin, and also interferes with the action of betahistine and drugs - cholinesterase inhibitors.

Cimetidine 600 mg twice daily has been found to increase serum hydroxyzine concentration by 36% and decrease the maximum concentration of cetirizine metabolite by 20%.

The effect of atropine, belladonna alkaloids, cardiac glycosides, antihypertensive drugs, blockers of H ₂ -histamine receptors do not change under the action of hydroxyzine. Hydroxyzine is an inhibitor of the CYP2D6 isoenzyme and in high doses can cause drug interactions with CYP2D6 substrates. Since hydroxyzine is metabolized in the liver, an increase in its plasma concentration can be expected when used simultaneously with inhibitors of microsomal liver enzymes. Since hydroxyzine is metabolized by alcohol dehydrogenase and the CYP3A4 / 5 isoenzyme, it is possible to increase the concentration of hydroxyzine in plasma when used simultaneously with drugs that potentially inhibit the CYP3A4 / 5 isoenzyme (telithromycin, clarithromycin, delavirdine, styripentol, ketoconazole, voriconazole, itraconazole, posaconazole and some HIV protease inhibitors including atazanavir, indinavir, nelfinavir, ritonavir, saquinarine, lopinavir/ritonavir, saquinarine/ritonavir, and tipranavir/ritonavir). However, the inhibition of one metabolic pathway can be partially compensated by the work of another. The concomitant use of hydroxyzine with medicinal products that have the potential to cause arrhythmia may increase the risk of QT interval prolongation and torsades de pointes.

The use of the drug simultaneously with drugs that have an ototoxic effect, such as gentamicin, may mask symptoms of ototoxicity such as dizziness. The drug should be canceled 3 days before the planned skin tests with allergens.

• 
  Dsm mental health diagnosis
• 
  What is the opposite of worry
• 
  Joyce meyer four personality types
• 
  How to get over a betrayal
• 
  Diagnosis bipolar depression
• 
  How to overcome being an introvert
• 
  How to stop feelings of jealousy
• 
  Yoga meditations for beginners
• 
  Modeling social learning
• 
  Feeling sad after christmas
• 
  How to know if i have bpd