The pharmaceutical parameters of cetyrizin change linearly.
Suction. After taking it inside, the drug is quickly and completely absorbed from the LCD. Eating does not affect the completeness of absorption, although its speed decreases. In adults, after a single medication in therapeutic dose Cmax in blood plasma is 300 ng / ml and is achieved through (1 ± 0.5) h.
Distribution. Cetirisin on (93 ± 0.3)% binds to blood plasma proteins. Vd is 0.5 l / kg. When taking the drug at a dose of 10 mg for 10 days, cetyrizin cumulation is not observed.
Metabolism. In small quantities, it is metabolized in the body by O-dealkylation (unlike other antagonists H1-histamines that are metabolized in the liver using a cytochrome system) with the formation of pharmacologically inactive metabolite.
The conclusion. In adults T1/2 is approximately 10 hours; in children from 6 to 12 years old - 6 hours, from 2 to 6 years old - 5 hours, from 6 months to 2 years old - 3.1 hours. Approximately 2/3 of the accepted dose of the drug is withdrawn by the kidneys unchanged.
In elderly patients and patients with chronic liver diseases with a single medication at a dose of 10 mg T1/2 increases by about 50%, and system clearance is reduced by 40%.
In patients with renal failure of mild severity (Cl creatinine> 40 ml / min), pharmacokinetic parameters are similar to those in patients with normal kidney function.
In patients with moderate renal failure and in patients undergoing hemodialysis (Cl creatinine <7 ml / min), when taking the drug inward at a dose of 10 mg T1/2 lengthens 3 times, and the total clearance is reduced by 70% relative to these indicators in patients with normal kidney function, which requires a corresponding change in the dosing mode.
Cetirisin is practically not removed from the body during hemodialysis.
The pharmaceutical parameters of cetyrizin when used in doses of 5 to 60 mg change linearly.
Suction. Cmax in blood plasma is achieved through (1 ± 0.5) h and is 300 ng / ml.
Various pharmacokinetic parameters, such as Cmax in blood plasma and AUC are homogeneous.
Eating does not affect the completeness of cetyrizin absorption, although its speed decreases. The bioavailability of various dosage forms of cetyrizin (rathering, capsules, tablets) is comparable.
Distribution. Cetirisin on (93 ± 0.3)% binds to blood plasma proteins.
Vd is 0.5 l / kg. Cetirisin does not affect the binding of warfarin with proteins.
Metabolism. Cetirisin is not exposed to extensive primary metabolism.
The conclusion. T1/2 is approximately 10 hours.
When taking the drug in a daily dose of 10 mg for 10 days, cetyrizin cumulation was not observed.
Approximately 2/3 of the accepted dose of the drug is withdrawn with urine in an unchanged form.
Elderly patients. In 16 elderly patients with a single medication in a dose of 10 mg T1/2 was 50% higher, and clearance was 40% lower compared to patients of not old age. The decrease in cetirizin clearance in older patients is probably due to a decrease in the function of the kidneys in this category of patients.
Renal failure. In patients with renal failure of mild severity (Cl creatinine> 40 ml / min), pharmacokinetic parameters are similar to those in healthy volunteers with normal kidney function.
In patients with moderate renal failure and in patients undergoing hemodialysis (Cl creatinine <7 ml / min), when taking the drug inward at a dose of 10 mg T1/2 lengthens 3 times, and the overall clearance is reduced by 70% relative to healthy volunteers with normal kidney function.
For patients with renal failure of moderate or severe degree, a corresponding change in the metering mode is required (see. “Method of application and doses”).
Cetirisin is poorly removed from the body during hemodialysis.
Pediatric failure. In patients with chronic liver diseases (hepatocellular, cholestatic and biliar cirrhosis) with a single medication at a dose of 10 or 20 mg T1/2 increases by about 50%, and clearance is reduced by 40% compared to healthy entities. Correction of the dose is necessary only if the patient with liver failure also has concomitant renal failure.
Children. T1/2 in children from 6 to 12 years old it is 6 hours, from 2 to 6 years old - 5 hours, from 6 months to 2 years old - reduced to 3.1 hours.
Inside.
Children over 6 years old and adults : initial dose - 5 mg (1/2 table. or 10 drops) once a day, if necessary, can be increased to 10 mg (1 table. or 20 drops) 1 time a day. Sometimes the initial dose is 5 mg (1/2 tab. or 10 drops) may be sufficient to achieve a therapeutic effect. Daily dose - 10 mg (1 table. or 20 drops).
Children from 6 to 12 months : 2.5 mg (5 drops) 1 time per day.
Children from 1 year to 2 years : 2.5 mg (5 drops) up to 2 times a day.
Children from 2 to 6 years old : 2.5 mg (5 drops) 2 times a day or 5 mg (10 drops) 1 time a day.
Sick with renal failure, the dose decreases depending on the creatinine clearance: with Cl creatinine 30–49 ml / min - 5 mg 1 time per day, at 10–29 ml / min - 5 mg per day.
Because Ralizon® excreted by kidneys, when prescribing the drug, patients with renal failure and elderly patients should be adjusted to the extent of creatinine clearance. Creatinin clearance for men can be calculated based on the concentration of serum creatinine, according to the following formula:
Cl creatinine, ml / min
Creatinine clearance for women can be calculated by multiplying the value obtained by a coefficient of 0.85.
| Renal failure | Cl creatinine, ml / min | Dosing mode |
| Missing (norm) | ≥80 | 10 mg / day |
| Easy | 50–79 | 10 mg / day |
| Medium | 30–49 | 5 mg / day |
| Heavy | 10–29 | 5 mg per day |
| The terminal stage is patients on hemodialysis | <10 | taking the drug is contraindicated |
For adult patients with renal and liver failure, dosing is carried out according to the table above.
Children with renal failure are adjusted for creatinine clearance and body weight.
Patients with impaired liver function only do not need to correct the dosing mode.
Inside.
Drops dissolve in a small amount of water before taking.
Adults and adolescents over 12 years old: 10 mg (20 drops or 1 table.) once a day, preferably at night.
Children aged 6–12 years: 5 mg each (10 drops or 1/2 table.) 2 times a day (morning and evening) or 10 mg (20 drops or 1 whole tablet) in the evening.
Children aged 1-6 years recommended to assign Ralizon® in the medicinal form of a drop for taking in.
Children aged 2–6 years: 5 mg (10 drops per day) once. You can also divide this dose by 2 doses of 2.5 mg (5 drops in the morning and evening).
Children aged 1-2 years: 2.5 mg (5 drops) 2 times a day.
Special patient groups
It may be necessary to reduce the dose of y elderly patients.
At kidney function violation the dose should be set individually, in accordance with the function of the kidneys. The table below will assist in the selection of doses. To use this table, you should evaluate Cl creatinine in a patient in ml / min. After determining the concentration of creatinine of blood serum (mg / dl), the value of Cl creatinine can be estimated using the following formula:
Cl creatinine = [(140 − age, years) × body weight, kg) / (72 − creatinine blood serum, mg / dl]
When calculating creatinine clearance for women, the result must be multiplied by 0.85. The table shows the doses depending on Cl creatinine.
Table
The dose selection depending on the clearance of creatinine
| Cl creatinine, ml / min | Dosage |
| ≥80 | 10 mg 1 time per day |
| 50–79 | 10 mg 1 time per day |
| 30–49 | 5 mg 1 time per day |
| 11–29 | 5 mg 1 time in 2 days |
| ≤10 (hemodialysis) | contraindicated |
Inside, dig into a spoon or dissolve in water.
The amount of water for dissolving the drug must correspond to the amount of fluid that the patient (especially the child) is able to swallow. The solution should be taken immediately after preparation.
Adults. 10 mg (20 drops) 1 time per day. Sometimes an initial dose of 5 mg (10 drops) can be enough if this allows satisfactory control of the symptoms.
Elderly age. In elderly patients with normal kidney function, there is no need to reduce the dose.
Violation of the function of the kidneys. When prescribing the drug to patients with impaired renal function, in the case when alternative treatment cannot be prescribed, the dose should be adjusted depending on the value of Cl creatinine, since cetyrizin is removed from the body mainly by the kidneys.
The Cl creatinine indicator for men can be calculated based on the concentration of serum creatinine in the blood plasma according to the following formula:
Cl creatinine, ml / min = (140 - age, years) × body weight, kg) / (72 × Cl creatinineserum, mg / dl).
Cl creatinine for women can be calculated by multiplying the value obtained by a coefficient of 0.85.
| Renal failure | Cl creatinine, ml / min | Dosing mode |
| Norma | ≥80 | 10 mg / day |
| Easy | 50–79 | 10 mg / day |
| Medium | 30–49 | 5 mg / day |
| Heavy | <30 | 5 mg per day |
| The terminal stage is patients on hemodialysis | <10 | The drug is contraindicated |
Violation of liver function. Patients with impaired liver function do not need to correct the dosing mode. In patients with impaired liver function and kidneys, dosing correction is recommended (see. table above).
Children. The use of children from 6 to 12 months is possible only by appointment of a doctor and under strict medical supervision. Children from 6 to 12 months — 2.5 mg (5 drops) 1 time a day; from 1 year to 6 years — 2.5 mg (5 drops) 2 times a day; from 6 to 12 years — 5 mg (10 drops) 2 times a day; over 12 years old — 10 mg (20 drops) 1 time a day, sometimes the initial dose is 5 mg (10 drops) may be enough, if this allows satisfactory control of the symptoms.
Children with renal failure are adjusted for Cl creatinine and body weight.
Instructions for opening a bottle
The bottle is closed with a lid with a safety device that prevents children from opening it. The bottle opens when the lid is pressed heavily down, followed by screwing it off counterclockwise. After using the bottle cover, you must screw it tight again.
Inside, swallowing in its entirety, drinking with a small amount of water, regardless of the time of eating.
Zinzet is used as prescribed by a doctor (to avoid complications).
Children from 2 to 6 years old: 2.5 mg each (1/2 h.syrup spoons) 2 times a day or 5 mg (1 h.spoon) 1 time per day; from 6 to 12 years: 10 mg each (1 table. or 2 hours. syrup spoons) 1 time per day or 5 mg (1/2 table. or 1 h.spoon syrup) 2 times a day, morning and evening; adults and children over 12 years old: 10 mg each (1 table. or 2 hours. spoons of syrup) 1 time per day.
For elderly people or patients with severe impaired liver and / or kidney function, the drug is prescribed individually by a doctor, in a reduced dose.
If the time of taking the drug is accidentally missed, the next dose should be taken as soon as possible. In the event that the time for the next drug is approaching, the next dose should be taken on schedule, without increasing the total dose.
Inside, swallowing in its entirety, drinking with a small amount of water, regardless of the time of eating.
The drug Ralizon is used as prescribed by a doctor (to avoid complications).
Children from 2 to 6 years old: 2.5 mg each (1/2 h.syrup spoons) 2 times a day or 5 mg (1 h.spoon) 1 time per day; from 6 to 12 years: 10 mg each (1 table. or 2 hours. syrup spoons) 1 time per day or 5 mg (1/2 table. or 1 h.spoon syrup) 2 times a day, morning and evening; adults and children over 12 years old: 10 mg each (1 table. or 2 hours. spoons of syrup) 1 time per day.
For elderly people or patients with severe impaired liver and / or kidney function, the drug is prescribed individually by a doctor, in a reduced dose.
If the time of taking the drug is accidentally missed, the next dose should be taken as soon as possible. In the event that the time for the next drug is approaching, the next dose should be taken on schedule, without increasing the total dose.
