Release form, composition and packing
Tablets, coated in white, with the risk.
1 tab. Hydroxyzine hydrochloride 25 mg.
Excipients: lactose monohydrate, microcrystalline cellulose, colloidal silicon dioxide, magnesium stearate, titanium dioxide (E171), hydroxypropyl methylcellulose, macrogol.
Solution for IM injection is colorless and transparent.
1 ml 1 amp. Hydroxyzine hydrochloride 50 mg 100 mg.
Excipients: sodium hydroxide, water, d / and.
Clinico-pharmacological group: Tranquilizer (anxiolytic).
Pharmacological action
Diphenylmethane derivative, has a moderate anxiolytic activity, is also a sedative, antiemetic, antihistamine, and m-anticholinergic action. Blocks the central m-cholinergic receptors and histamine H1 receptors and inhibits the activity of certain subcortical areas. Does not cause psychological dependence and addiction.
The clinical effect occurs within 15-30 minutes after taking the drug inside. Has a positive effect on cognition, improves memory and attention. Relaxes skeletal and smooth muscle, has bronchodilatory and analgesic effects, a moderate inhibitory effect on gastric secretion. Hydroxyzine significantly reduces pruritus in patients with urticaria, eczema and dermatitis.
Chronic administration not noted cindroma withdrawal and deterioration of cognitive functions. Polysomnography in patients with insomnia and anxiety demonstrates the lengthening duration of sleep, decrease the frequency of nighttime awakenings after single or re-admission Hydroxyzine 50 mg. Reduction of muscular tension in patients with anxiety noted while taking the drug at a dose of 50 mg 3 times / day.
Pharmacokinetics
Suction
Hydroxyzine is rapidly absorbed from the gastrointestinal tract. Cmax observed after 2 h of ingestion. After a single dose of the drug in a single dose of 25 mg or 50 mg in adult plasma concentration is 30 ng / ml and 70 ng / ml, respectively. Oral bioavailability and IM administration is 80%.
Distribution
Hydroxyzine is more concentrated in the tissues (particularly in the skin) than in plasma.
The distribution coefficient of 7-16 L / kg. Hydroxyzine passes through the blood-brain barrier and placental barrier, thus concentrating more in fetal tissues than in the mother's body. Metabolites found in breast milk.
Metabolism and Elimination
Hydroxyzine biotransformed in the liver, the main metabolite (45%) - cetirizine, which is a blocker of histamine H1 receptors.
The total clearance of Hydroxyzine is 13 ml / min / kg. T1 / 2 in adults at 14 h. Only 0.8% Hydroxyzine is excreted unchanged in the urine.
Pharmacokinetics in special clinical situations
In children, the total clearance is 4 times less than in adults, T1 / 2 in children aged 14 years is 11 hours in children aged 1 - 4 hours in elderly patients T1 / 2 is 29 h, the distribution coefficient is 5.22 L / kg.
Patients with impaired liver function T1 / 2 increases to 37 h, the concentration of metabolites in serum is higher than in younger patients with normal liver function. Antihistamine effect may persist for 96 hours
Statement
adults: for relief of anxiety, psychomotor agitation, feelings of inner tension, irritability with neurological, psychiatric (including generalized anxiety, adjustment disorder) and somatic diseases, alcoholism, abstinence syndrome in chronic alcoholism, accompanied by psychomotor excitation;
as a sedative during the period of sedation;
itchy skin (as a symptomatic therapy).
Dosing regimen
The drug is taken orally or injected into the V / m. For the symptomatic treatment of itch in children aged 12 months to 6 years of preparation is administered in a daily dose of 1-2.5 mg / kg of body weight in divided doses for children aged over 6 years - 1-2 mg / kg / day in divided doses .
Premedication for children drug is prescribed at a dose of 1 mg / kg body weight 1 h before surgery, and an additional night before surgery. Adults for the symptomatic treatment of anxiety prescribe a dose of 25-100 mg / day in divided doses throughout the day or night. The average dose of 50 mg / day (12.5 mg in the morning, afternoon 12.5 mg and 25 mg at night).
If necessary, the dose may be increased to 300 mg / day. For sedation in surgical practice is introduced into the / m at a dose of 50-200 mg (1.5-2.5 mg / kg) 1 h before surgery, as well as optional evening before surgery. For the symptomatic treatment of pruritus starting dose is 25 mg, if necessary the dose may be increased by a factor of 4 (25 mg 4 times / day). The maximum single dose should not exceed 200 mg maximum daily dose is no more than 300 mg.
Patients with renal failure secondary to severe, as well as with liver failure should decrease the dose. Older patients should reduce the initial dose of 2-fold in the case of a reduced glomerular filtration rate.
Side effect
Adverse effects associated with anticholinergic action: rarely (mostly elderly patients) - dry mouth, urinary retention, constipation, disturbance of accommodation.
CNS: drowsiness, weakness (especially in the beginning of treatment), headache, dizziness. If the weakness and lethargy do not disappear after a few days of therapy, the drug dose should be reduced.
Cardio-vascular system: arterial hypotension, tachycardia.
From the digestive system: nausea, changes in liver function tests.
Other: increased sweating, allergic reactions, fever, bronchospasm. Using the drug in recommended doses were noted clinically significant respiratory depression. Involuntary motor activity (including very rare cases of tremor and convulsions), disorientation were observed at large overdose.
Side effects observed while taking Atarax are usually mild, transient and disappear within a few days of starting treatment or after dose reduction.
Contraindications
porphyria;
pregnancy;
during labor;
Lactation (breastfeeding);
Hypersensitivity to any component of the drug, cetirizine, and other derivatives of piperazine, aminophylline and ethylenediamine.
Not recommended to prescribe pills Atarax patients with hereditary galactose intolerance, as well as malabsorption of glucose and galactose, as in the tablets include lactose.
Precautions should be prescribed the drug for myasthenia gravis, prostatic hyperplasia with the clinical manifestations, difficulty urinating, constipation, an increase in intraocular pressure, dementia, the propensity to seizures, with predisposition to development of arrhythmias, while the application of drugs with arrhythmogenic action.
In an application with other central depressant drug, or holinoblokatorami dose should be reduced.
Pregnancy and lactation
Atarax is contraindicated in pregnancy, during labor. If necessary, use Atarax during lactation should stop breastfeeding.
Use in hepatic dysfunction
Patients with liver failure should decrease the dose.
Use in renal impairment
Patients with renal failure secondary to severe need to reduce dose.
Cautions
When the need for allergy testing method Atarax should be discontinued 5 days before the study. Injectable forms of the drug intended only for IM administration. Atarax should not be given to / a, / a, n / k. When s / c infusion drug can cause tissue damage. When i / m administration should make sure that the needle does not hit the vessel.
Patients taking Atarax should abstain from alcohol.
Effects on ability to drive vehicles and management mechanisms
Patients taking Atarax, if necessary, driving and machinery should be warned that the drug can affect the concentration of attention and speed of psychomotor reactions.
Overdose
Symptoms: increased anticholinergic effects, depression, or paradoxical CNS stimulation, nausea, vomiting, involuntary motor activity, hallucinations, impaired consciousness, arrhythmia, hypotension, rarely - tremors, convulsions, disorientation that occur when a significant excess of recommended doses.
Treatment: If spontaneous vomiting is absent, you must call it by artificial means or to gastric lavage.
Conduct general activities aimed at maintaining vital body functions, and monitor the observation of the patient until symptoms of intoxication in the next 24 hours
Tablets, coated in white, with the risk.
1 tab. Hydroxyzine hydrochloride 25 mg.
Excipients: lactose monohydrate, microcrystalline cellulose, colloidal silicon dioxide, magnesium stearate, titanium dioxide (E171), hydroxypropyl methylcellulose, macrogol.
Solution for IM injection is colorless and transparent.
1 ml 1 amp. Hydroxyzine hydrochloride 50 mg 100 mg.
Excipients: sodium hydroxide, water, d / and.
Clinico-pharmacological group: Tranquilizer (anxiolytic).
Pharmacological action
Diphenylmethane derivative, has a moderate anxiolytic activity, is also a sedative, antiemetic, antihistamine, and m-anticholinergic action. Blocks the central m-cholinergic receptors and histamine H1 receptors and inhibits the activity of certain subcortical areas. Does not cause psychological dependence and addiction.
The clinical effect occurs within 15-30 minutes after taking the drug inside. Has a positive effect on cognition, improves memory and attention. Relaxes skeletal and smooth muscle, has bronchodilatory and analgesic effects, a moderate inhibitory effect on gastric secretion. Hydroxyzine significantly reduces pruritus in patients with urticaria, eczema and dermatitis.
Chronic administration not noted cindroma withdrawal and deterioration of cognitive functions. Polysomnography in patients with insomnia and anxiety demonstrates the lengthening duration of sleep, decrease the frequency of nighttime awakenings after single or re-admission Hydroxyzine 50 mg. Reduction of muscular tension in patients with anxiety noted while taking the drug at a dose of 50 mg 3 times / day.
Pharmacokinetics
Suction
Hydroxyzine is rapidly absorbed from the gastrointestinal tract. Cmax observed after 2 h of ingestion. After a single dose of the drug in a single dose of 25 mg or 50 mg in adult plasma concentration is 30 ng / ml and 70 ng / ml, respectively. Oral bioavailability and IM administration is 80%.
Distribution
Hydroxyzine is more concentrated in the tissues (particularly in the skin) than in plasma.
The distribution coefficient of 7-16 L / kg. Hydroxyzine passes through the blood-brain barrier and placental barrier, thus concentrating more in fetal tissues than in the mother's body. Metabolites found in breast milk.
Metabolism and Elimination
Hydroxyzine biotransformed in the liver, the main metabolite (45%) - cetirizine, which is a blocker of histamine H1 receptors.
The total clearance of Hydroxyzine is 13 ml / min / kg. T1 / 2 in adults at 14 h. Only 0.8% Hydroxyzine is excreted unchanged in the urine.
Pharmacokinetics in special clinical situations
In children, the total clearance is 4 times less than in adults, T1 / 2 in children aged 14 years is 11 hours in children aged 1 - 4 hours in elderly patients T1 / 2 is 29 h, the distribution coefficient is 5.22 L / kg.
Patients with impaired liver function T1 / 2 increases to 37 h, the concentration of metabolites in serum is higher than in younger patients with normal liver function. Antihistamine effect may persist for 96 hours
Statement
adults: for relief of anxiety, psychomotor agitation, feelings of inner tension, irritability with neurological, psychiatric (including generalized anxiety, adjustment disorder) and somatic diseases, alcoholism, abstinence syndrome in chronic alcoholism, accompanied by psychomotor excitation;
as a sedative during the period of sedation;
itchy skin (as a symptomatic therapy).
Dosing regimen
The drug is taken orally or injected into the V / m. For the symptomatic treatment of itch in children aged 12 months to 6 years of preparation is administered in a daily dose of 1-2.5 mg / kg of body weight in divided doses for children aged over 6 years - 1-2 mg / kg / day in divided doses .
Premedication for children drug is prescribed at a dose of 1 mg / kg body weight 1 h before surgery, and an additional night before surgery. Adults for the symptomatic treatment of anxiety prescribe a dose of 25-100 mg / day in divided doses throughout the day or night. The average dose of 50 mg / day (12.5 mg in the morning, afternoon 12.5 mg and 25 mg at night).
If necessary, the dose may be increased to 300 mg / day. For sedation in surgical practice is introduced into the / m at a dose of 50-200 mg (1.5-2.5 mg / kg) 1 h before surgery, as well as optional evening before surgery. For the symptomatic treatment of pruritus starting dose is 25 mg, if necessary the dose may be increased by a factor of 4 (25 mg 4 times / day). The maximum single dose should not exceed 200 mg maximum daily dose is no more than 300 mg.
Patients with renal failure secondary to severe, as well as with liver failure should decrease the dose. Older patients should reduce the initial dose of 2-fold in the case of a reduced glomerular filtration rate.
Side effect
Adverse effects associated with anticholinergic action: rarely (mostly elderly patients) - dry mouth, urinary retention, constipation, disturbance of accommodation.
CNS: drowsiness, weakness (especially in the beginning of treatment), headache, dizziness. If the weakness and lethargy do not disappear after a few days of therapy, the drug dose should be reduced.
Cardio-vascular system: arterial hypotension, tachycardia.
From the digestive system: nausea, changes in liver function tests.
Other: increased sweating, allergic reactions, fever, bronchospasm. Using the drug in recommended doses were noted clinically significant respiratory depression. Involuntary motor activity (including very rare cases of tremor and convulsions), disorientation were observed at large overdose.
Side effects observed while taking Atarax are usually mild, transient and disappear within a few days of starting treatment or after dose reduction.
Contraindications
porphyria;
pregnancy;
during labor;
Lactation (breastfeeding);
Hypersensitivity to any component of the drug, cetirizine, and other derivatives of piperazine, aminophylline and ethylenediamine.
Not recommended to prescribe pills Atarax patients with hereditary galactose intolerance, as well as malabsorption of glucose and galactose, as in the tablets include lactose.
Precautions should be prescribed the drug for myasthenia gravis, prostatic hyperplasia with the clinical manifestations, difficulty urinating, constipation, an increase in intraocular pressure, dementia, the propensity to seizures, with predisposition to development of arrhythmias, while the application of drugs with arrhythmogenic action.
In an application with other central depressant drug, or holinoblokatorami dose should be reduced.
Pregnancy and lactation
Atarax is contraindicated in pregnancy, during labor. If necessary, use Atarax during lactation should stop breastfeeding.
Use in hepatic dysfunction
Patients with liver failure should decrease the dose.
Use in renal impairment
Patients with renal failure secondary to severe need to reduce dose.
Cautions
When the need for allergy testing method Atarax should be discontinued 5 days before the study. Injectable forms of the drug intended only for IM administration. Atarax should not be given to / a, / a, n / k. When s / c infusion drug can cause tissue damage. When i / m administration should make sure that the needle does not hit the vessel.
Patients taking Atarax should abstain from alcohol.
Effects on ability to drive vehicles and management mechanisms
Patients taking Atarax, if necessary, driving and machinery should be warned that the drug can affect the concentration of attention and speed of psychomotor reactions.
Overdose
Symptoms: increased anticholinergic effects, depression, or paradoxical CNS stimulation, nausea, vomiting, involuntary motor activity, hallucinations, impaired consciousness, arrhythmia, hypotension, rarely - tremors, convulsions, disorientation that occur when a significant excess of recommended doses.
Treatment: If spontaneous vomiting is absent, you must call it by artificial means or to gastric lavage.
Conduct general activities aimed at maintaining vital body functions, and monitor the observation of the patient until symptoms of intoxication in the next 24 hours
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