Composition, form of production and packaging
? The tablets covered with a film cover of light orange color, biconcave, oblong, with a facet, with a risk on one side and engraving "Р• 511" on the other side, without a smell; on the fracture: the outer ring of the shell is light orange, the core of the tablet is white or almost white.
cetirizine dihydrochloride 10 mg
Excipients: silicon dioxide colloidal anhydrous - 0.8 mg, magnesium stearate - 1.7 mg, lactose monohydrate - 11.5 mg, microcrystalline cellulose - 91 mg.
Composition of the shell: opadray Y-1-7000 (hypromellose, titanium dioxide (CI77891), macrogol 400) - 4 mg, ariovit sanset yellow (CI15985) (dye sunset yellow) - 0.01 mg.
5 pieces. - blisters (1) - packs of cardboard.
7 pcs. - blisters (1) - packs of cardboard.
10 pieces. - blisters (1) - packs of cardboard.
10 pieces. - blisters (3) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2016.
Cetirizine is a carboxylated metabolite of hydroxyzine, belongs to the class of antihistamine preparations of piperazine derivatives. The action of cetirizine and its antiallergic effects are based on selective blockade of peripheral histamine H 1 -receptors. With this mechanism, cetirizine suppresses early allergic reactions mediated by histamine, reduces the migration of inflammatory cells and the release of mediators associated with late allergic reactions. Cetirizine has only minor anticholinergic and antiserotonergic effects.
After ingestion, cetirizine is rapidly absorbed, C max in blood plasma is reached within 30-60 minutes. Simultaneous food intake does not affect the degree of absorption, however, food causes a delay in reaching Cmax in the plasma for 1.7 hours and reduces C max by 23%.
Cumulation after oral administration was not detected. When the drug is used in doses of 5 to 60 mg, cetirizine has a linear pharmacokinetics. The binding to plasma proteins is 93% and is independent of the concentration in the range of 25 to 1000 ng / ml; this range includes the therapeutic values вЂ‹вЂ‹of the concentration in the blood plasma. Being the main metabolite of hydroxyzine, cetirizine is more hydrophilic than the parent substance, and therefore has a very low ability to penetrate the BBB.Cetirizine penetrates into breast milk.
Only a small part of cetirizine is metabolized by conversion into a practically inactive O-dealkylated metabolite in the liver.
Within 24 hours, 60% of the ingested dose is excreted unchanged through the kidneys, another 10% is excreted over the next 4 days. Approximately 10% is excreted through the intestine, partly in the form of metabolites.
T 1/2 from the blood plasma in adults is 8-12 hours.
Pharmacokinetics in specific patient groups
T 1/2 in children aged 6 to 12 years is approximately 6 hours, in children aged 1 to 6 years - about 5 hours.
Because of the higher incidence of decreased renal function in elderly patients, cetirizine clearance in this age group may be reduced.
With multiple admission, the pharmacokinetics of cetirizine change insignificantly with mild renal failure compared to healthy volunteers. However, in patients with moderate renal insufficiency, the mean T.sub.1 of cetirizine increases threefold, and the clearance decreases by 70% compared to healthy. In patients on hemodialysis, a threefold increase in T 1/2 and a 70% decrease in clearance even after a single administration of cetirizine at a dose of 10 mg is possible.
In comparison with the same parameters of healthy volunteers, in patients with chronic hepatic insufficiency, there was approximately a 50% increase in T 1/2 and a 40% decrease in clearance.
- seasonal and year-round allergic rhinitis and conjunctivitis;
- Pollinosis (hay fever);
- itching allergic dermatoses;
- urticaria (including chronic idiopathic);
- Quincke's edema.
The drug is taken orally.
Adults and children from the age of 12 years are prescribed 1 tablet. (10 mg) 1 time / day, daily, preferably in the evening.
Children aged 6 to 12 years - 1/2 tab. (5 mg) 2 times / day, daily in the morning and in the evening or 1 tab. (10 mg) 1 time / day, daily, preferably in the evening.
Children aged 1 to 6 years are recommended to prescribe Parasitic В® in the form of a medicinal drop for oral administration.
It may be necessary to reduce the dose in elderly patients .
If the kidney function is disrupted, the dose should be set individually according to the function of the kidneys. The table below will assist in the selection of a dose.To use this table, you should assess QC in a patient in mL / min. After the determination of the serum creatinine concentration (mg / dl), the CK value (ml / min) can be estimated by the following formula:
CC = [140 - age (years)]? body weight (kg) / 72 - serum creatinine (mg / dL)
In women, the obtained value should be multiplied by 0.85.
Selection of a dose for kidney disease
Creatinine clearance (ml / min) Dose and frequency of admission
Normal function of the kidneys? 80 10 mg 1 time / day
Mild renal dysfunction 50-79 10 mg 1 time / day
Moderate renal dysfunction 30-49 5 mg 1 time / day
Severe renal impairment <30 5 mg once every two days
Renal failure - Patients on hemodialysis? 10 Contraindicated
Usually the drug is well tolerated.
The most frequent side effects (> 2%) are drowsiness (frequency increases depending on the dose), fatigue, headache, migraine, dizziness, dry mouth, nausea, abdominal pain, diarrhea, anxiety, increased motor activity. The intensity of these side effects can be reduced by dividing the daily dose into two doses.
Rarely (<2%) there are allergic reactions (angioedema, rash).
- renal failure with QC less than 10 ml / min;
- lactation period (breastfeeding);
- children's age till 6 years;
- lactose intolerance and glucose-galactose absorption disorder;
- Hypersensitivity to cetirizine or other components of the drug.
Caution should be used for chronic renal failure of moderate and severe degree (correction of the dosing regimen is required), as well as in elderly patients (correction of the dosing regimen is required).
PREGNANCY AND LACTATION
There are no data on clinical studies of the use of the drug during pregnancy, in connection with which ParasiticВ® is contraindicated in pregnancy.
Cetirizine penetrates into breast milk, so the drug is contraindicated during breastfeeding. If it is necessary to use the drug during lactation, it is necessary to solve the problem of stopping breastfeeding.
APPLICATION FOR FUNCTIONS OF THE LIVER
Contraindicated use of the drug in renal failure with QC less than 10 ml / min.
Caution should be used for chronic renal failure of moderate and severe degree (correction of the dosing regimen is required).
APPLICATION FOR CHILDREN
Contraindicated use of the drug in childhood to 6 years.
APPLICATION IN ELDERLY PATIENTS
Caution should be used in elderly patients (correction of the dosing regimen is required).
When hypersensitivity reactions appear, the drug should be discontinued immediately.
Due to a decrease in the rate of cetirizine excretion, it can accumulate in the body of patients with impaired renal function; while the frequency and severity of side effects of anticholinergic effects or effects on the central nervous system may increase, even if the usual dose is taken for adults. Therefore, in such cases it is recommended to reduce the dose.
Elderly patients are particularly sensitive to the anti-cholinergic effect of antihistamines (eg, dry mouth, urinary retention). If these side effects are observed for a long time, as well as when their intensity increases, the drug should be stopped. Although cetirizine less often causes anticholinergic side effects or a serious side effect on the CNS, it can accumulate (the age-related decrease in renal function is more likely in elderly patients) and cause anticholinergic side effects or side effects on the CNS, even with the administration of a usual dose for adults.
The coated tablets contain lactose, so this drug should not be given to patients with lactose intolerance and / or glucose-galactose absorption disorder.
The drug Parasitamin В® should be discontinued no less than 3 days before the allergic skin test is performed to avoid false negative results.
Impact on the ability to drive vehicles and manage mechanisms
During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.
Symptoms (with a single dose of 50 mg): confusion, dizziness, headache, fatigue, weakness, malaise, sedation, drowsiness, stupor, mydriasis, itching, tremor, diarrhea, urinary retention.
Treatment: gastric lavage, provocation of vomiting; reception of activated charcoal, symptomatic and maintenance therapy. There is no specific antidote. Hemodialysis is ineffective.
There was no interaction when combined with diazepam, cimetidine, azithromycin, erythromycin, ketoconazole, pseudoephedrine.
Joint application with theophylline (400 mg / day) leads to a decrease in the total clearance of cetirizine (theophylline kinetics does not change).
The combined use of cetirizine and antibiotics from the macrolide or cytirizine group with ketoconazole did not cause clinically significant changes in the ECG.
Ethanol: As with any other antihistamine drug, avoid drinking alcohol during treatment.
TERMS OF RELEASE FROM PHARMACY
The drug is approved for use as a means of OTC.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of reach of children at a temperature of no higher than 25 В° C. Shelf life - 4 years.