Hydroxisin Canon - instructions for use, dose, side effects, contraindications

Active substanceHydroxysinHydroxysin

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Hydroxysin Canon

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CANONFARMA PRODUCTION, CJSC Russia

Hydroxisin-native

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NATIVA, LLC Russia

Dosage form: & nbspfilm-coated tablets

Composition:

1 tablet, film-coated, contains:

active substance: hydroxyzine hydrochloride 25 mg;

Excipients: corn starch pregelatinized starch 30 mg, silicon dioxide colloid 0.7 mg, magnesium stearate 1 mg, mannitol 40 mg, microcrystalline cellulose 33.3 mg;

composition of film shell: opadray white 4 mg, including: hypromellose (hydroxypropylmethylcellulose) 1.35 mg, giprolose (hydroxypropyl cellulose) 1.35 mg, talc 0.8 mg, titanium dioxide 0.5 mg.

Description:

Round, biconvex tablets with a risk, covered with a film shell of white color. The cross section is almost white.

Pharmacotherapeutic group:Anxiolytic agent (tranquilizer)

ATX: & nbsp

N.05.B.B.01 Hydroxysin

Pharmacodynamics:

Hydroxyzine is a blocker of H₁-gistaminovyh receptors of the first generation, a phenothiazine derivative with antimuscarinic and sedative properties and diphenylmethane, promotes inhibition of the activity of certain subcortical zones.

Provides H₁-gastamine-blocking, bronchodilating and antiemetic effect, has a moderate inhibitory effect on gastric secretion. Hydroxysin significantly reduces itching in patients with hives, eczema and dermatitis.

Hydroxysin positively affects cognitive abilities, improves attention and memory. Hydroxysin addiction and mental dependence does not cause, with continued use of withdrawal syndrome is not noted. Hydroxysin is able to inhibit the central nervous system, also has anti-cholinergic, antihistamine, spasmolytic, local anesthetic, sympatholytic action, has miorelaksiruyuschey activity.

With hepatic insufficiency H₁The histamine-blocking effect can be prolonged up to 96 hours after a single dose.

Has moderate anxiolytic activity.

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

H₁The histamine-blocking effect occurs approximately 1 hour after ingestion of the tablets.

Sedation occurs after 30-45 minutes.

Pharmacokinetics:

Suction: Absorption is high. Time to reach the maximum concentration (Tc_max) after ingestion - 2 hours. After taking an average dose of 50 mg Tc_maxin adults it is 70 mg / ml.

Distribution: The distribution coefficient is 7-16 l / kg in adults. Hydroxysin penetrates the blood-brain barrier and the placenta, concentrating more in fetal than in maternal tissues. After oral administration hydroxysine well penetrates the skin, while the concentration of hydroxysin in the skin is much higher than the concentration in the blood serum both after a single and after repeated receptions. The plasma concentration of hydroxyzine does not necessarily reflect its binding to tissues or distribution in skin receptors. Influences skin inflammation depending on serum concentration.

Metabolism: Hydroxysin is metabolized in the liver. Cetirizine - the main metabolite (45%) is a blocker H₁-gistaminovyh receptors.Metabolites are found in breast milk.

Excretion: Half-life (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 the hydroxyzine is excreted unchanged through the kidneys. The main metabolite cetirizine excreted mainly in the urine, also in unchanged form (25% of the intake dose of hydroxyzine).

Pharmacokinetics in specific patient groups

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 for elderly patients.

Children under 1 year old

In children, the total clearance is 2.5 times higher than in adults. The dose should be adjusted. The half-life is 4 hours.

Children from 1 to 14 years old

The half-life is 11 hours.

In patients with hepatic insufficiency

In patients with secondary liver dysfunction due to primary biliary cirrhosis, the overall clearance was approximately 66% of the value recorded in healthy volunteers. In patients with liver disease T_1/2 increased to 37 hours, the concentration of metabolites in the serum of the blood is higher than in young patients with normal liver function.Patients with hepatic impairment are recommended to reduce the daily dose or the frequency of admission.

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 of hydroxysin did not change significantly, while the duration of exposure of cetirizine was increased. To avoid any significant accumulation of cetirizine metabolite after repeated use of hydroxysine in patients with impaired renal function, a daily dose of hydroxyzine should be lowered.

Indications:

- Symptomatic treatment of anxiety in adults;

- at As a sedative in the period of premedication;

- symptomatic treatment of pruritus of allergic origin.

Contraindications:

- Hypersensitivity to any of the drug components, cetirizine and other piperazine derivatives, aminophylline or ethylenediamine;

- porphyria;

- children under 3 years;

- pregnancy, the period of childbirth and breastfeeding.

Carefully:

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

Pregnancy and lactation:

Drug Gidroksizin Kanon is contraindicated in pregnancy, during childbirth and breastfeeding.

Dosing and Administration:

The drug is administered orally.

For children:

For symptomatic treatment of pruritus of allergic origin:

At the age from 3 to 6 years: from 1.0 mg / kg / day to 2.5 mg / kg / day in several doses.

At the age of 6 years and older: from 1.0 mg / kg / day to 2.0 mg / kg / day in several 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 recommended doses, and it should be noted that the minimum dose obtained after dividing the tablet is 12.5 mg.

Adults:

For symptomatic treatment of anxiety: a standard dose of 50 mg per day, divided into 3 doses (1/2 tablets (12.5 mg) in the morning, 1/2 tablets (12.5 mg) in the afternoon and 1 tablet (25 mg per night). In case of anxiety in severe cases, the drug is used in a dose of 50-100 mg 4 times a day.

For symptomatic treatment of pruritus of allergic origin: the initial dose of 1 tablet (25 mg) before bed, if necessary, the dose can be increased to 1 tablet (25 mg) 3-4 times a day.

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

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

Use in special patient groups:

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

Use in patients with renal insufficiency and impaired liver function:

Patients with severe and moderate renal insufficiency, as well as with liver failure, need a dose reduction. In patients with hepatic insufficiency, it is recommended to reduce the daily dose by 33%.

In patients with severe and moderate renal failure, the drug is used in a half dose due to a decrease in the excretion of the main metabolite of hydroxyzine-cetirizine.

Side effects:

Possible side effects are given below for body systems and frequency of occurrence.

Classification of WHO frequency of development of side effects:

very often - ≥1/10 appointments (> 10%)

often from ≥1 / 100 to <1/10 of appointments (> 1% and <10%)

infrequently - from ≥1 / 1000 to <1/100 of prescriptions (> 0.1% and <1%)

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

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

The most frequent undesirable reactions were drowsiness, headache, blocking, dry mouth and fatigue.

Immune system disorders:

rarely: hypersensitivity;

very rarely: apreventive shock.

Disturbances from the nervous system:

infrequently: dizziness, insomnia, tremor;

rarely: cramps, dyskinesia.

Disorders of the psyche:

infrequently: agitation, confusion;

rarely: hallucinations, disorientation.

Disturbances on the part of the organ of sight:

rarely: violation of accommodation, visual impairment.

Violation of the heart:

rarely: tachycardia;

frequency is unknown: interval lengthening QT on the electrocardiogram, ventricular tachycardia as pirouette.

Violation of the vessels:

rarely: lowering of blood pressure.

Disturbances from the respiratory system, organs of the chest and the mediastinum:

rarely: bronchospasm.

Disorders from the gastrointestinal tract:

infrequently: nausea;

rarely: vomiting, constipation.

Disturbances from the liver and bile ducts:

rarely: violation of functional liver samples;

frequency is unknown: hepatitis.

Disorders from the kidneys and urinary tract:

rarely: retention of urination.

Disturbances from the skin and subcutaneous tissues:

rarely: itching, rash (erythematous, maculopapular), hives, dermatitis;

rarely: angioedema, sweating, acute generalized exanthematous pustular eruption, erythema multiforme, Stevens-Johnson syndrome.

General disorders:

rarely: hyperthermia, malaise.

The following side effects were observed with cetirizine - the main metabolite of hydroxyzine: thrombocytopenia, aggression, depression, tick, dystonia, paresthesia, oculogic crisis, diarrhea, dysuria, enuresis, asthenia, edema,increase in body weight and can be observed with the intake of hydroxysin.

Overdose:

Symptoms of toxicity from the central nervous system fromcrocheted with excessive m-holinoblokiruyuschim action, suppression or paradoxical stimulation of the central nervous system. These symptoms include nausea, vomiting, tachycardia, hyperthermia, drowsiness, impaired pupillary reflex, tremor, confusion, or hallucinations. Subsequently, depression of consciousness, respiration, convulsions, lowering of arterial pressure, arrhythmia can develop. Possible aggravation of coma and cardiopulmonary collapse.

Treatment

It is necessary to monitor the state of the respiratory tract, the state of respiration and circulation using electrocardiographic (ECG) monitoring, and provide adequate oxygenation.

Cardiac activity and blood pressure should be monitored within 24 hours after the disappearance of symptoms. In large doses hydroxysine can lead to an elongation of the QT interval and obvious changes in the electrocardiogram.

In the case of a violation of mental status, you must exclude the use of other drugs or alcohol,if necessary, the patient should be inhaled with oxygen, enter naloxone, dextrose (glucose) and thiamine. The use of analeptics is not permissible.

If it is necessary to obtain a vasopressor effect, norepinephrine or metameninol. Do not use epinephrine.

If you ingest a significant amount of the drug, you can perform gastric lavage with a previous endotracheal intubation.

It is possible to use activated carbon, however, data that indicate its effectiveness is not enough.

There is no specific antidote. Hemodialysis is ineffective.

Literary data indicate that in the case of development of severe, life-threatening, intractable m-cholinoblocking effects not being treated with other drugs, a therapeutic dose of physostigmine may be used. Physostigmine should not be used only to bring the patient to consciousness. If the patient took tricyclic antidepressants, the use of physostigmine can trigger convulsive attacks and irreversible cardiac arrest.Also, physostigmine should be avoided in patients with cardiac conduction disorders.

Interaction:

It is necessary to take into account the potentiating action 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.

It should avoid simultaneous use with monoamine oxidase (MAO) inhibitors and holinoblockers.

The drug interferes with the pressor action of epinephrine and anticonvulsant activity of phenytoin, and also interferes with the action of betagistin and cholinesterase inhibitor drugs.

It was found that the use of cimetidine at a dose of 600 mg twice a day increases the serum hydroxynine concentration by 36% and reduces the maximum concentration of cetirizine metabolite by 20%.

The effect of atropine, alkaloids of belladonna, cardiac glycosides, hypotensive drugs, blockers H₂-gistaminovyh receptors do not change under the action of hydroxyzine. Hydroxysin is an inhibitor of the isoenzyme CYP2D6 and in high doses can be a cause of drug interaction with substrates CYP2D6. Because the hydroxysine it is metabolized in the liver, it is possible to expect an increase in its concentration in the blood plasma with simultaneous application with inhibitors of microsomal liver enzymes. Because the hydroxysine is metabolized by alcohol dehydrogenase and isoenzyme CYP3A4 / 5, it is possible to increase the concentration of hydroxyzine in blood plasma while simultaneously applying with drugs potentially inhibiting the isoenzyme CYP3A4 / 5 (telithromycin, clarithromycin, delavirdine, styipentol, ketoconazole, voriconazole, intraconazole, posaconazole and some HIV protease inhibitors, including atazanavir, indinavir, nelfinavir, ritonavir, saquinarin, lopinavir / ritonavir, saquinarin / ritonavir, and tipranavir / ritonavir). However, inhibition of one metabolic pathway can be partially compensated by the work of another.

The simultaneous use of hydroxyzine with drugs that potentially can cause arrhythmia may increase the risk of prolonging the QT interval and the occurrence of ventricular pirouette tachycardia.

Application of the drug simultaneously with the means, having ototoxic effect, e.g. gentamycin, can mask such ototoxicity symptoms as dizziness.

The drug should be discontinued 3 days before the planned carrying out of skin tests with allergens.

Special instructions:

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

Hydroxysin can lead to lengthening of the interval QT on an electrocardiogram, so simultaneous use with other drugs that are capable of interfering with cardiac activity may increase the risk of arrhythmias. It is assumed that other drugs that cause changes in the electrocardiogram (atropine, antiparkinsonian agents, lithium carbonate, quinidine, phenothiazines, procainamide, tricyclic antidepressants, thioridazine) can aggravate and exacerbate the changes that may be caused by hydroxysine, and increase the risk of sudden death. It is necessary to avoid the simultaneous use of two or more drugs that lengthen the interval QT, because of the danger of additive effects, which can cause the development of potentially life-threatening and severe cardiac arrhythmias.

In renal and / or liver failure, doses should be reduced.

In the elderly, the dosage should be selected individually, starting at half the minimum dose, and adjusting in the recommended dosage range.

If it is necessary to set allergological tests or conduct a methacholine test, taking the drug Hydroxysin Canon should be stopped 5 days before the test to prevent the receipt of distorted data.

During treatment with the drug Hydroxysin Canon should avoid drinking alcohol.

Effect on the ability to drive transp. cf. and fur:

Hydroxysin The canon can worsen the ability to concentrate and the speed of psychomotor reactions. Taking other sedatives can enhance this effect. Therefore, one should refrain from driving vehicles and practicing other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Film-coated tablets, 25 mg.

Packaging:

For 10 or 25 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

According to 2, 3, 5 contour cell packs of 10 tablets or 1, 2 contour cell packs of 25 tablets together with instructions for use are placed in a pack of cardboard.

Storage conditions:

In a dry, the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-002566

Date of registration:06.08.2014

Expiration Date:06.08.2019

The owner of the registration certificate:CANONFARMA PRODUCTION, CJSC CANONFARMA PRODUCTION, CJSC Russia

Manufacturer: & nbsp

CANONFARMA PRODUCTION, CJSC Russia

Representation: & nbspCANONFARMA PRODUCTION CJSC CANONFARMA PRODUCTION CJSC Russia

Information update date: & nbsp15.04.2017

Illustrated instructions

Instructions

Hydroxysin Canon (Hydroxyzine Canon)