Composition, form of production and packaging
? Drops for oral administration are colorless or almost colorless, without sediment, with a weak characteristic smell of acetic acid.
cetirizine dihydrochloride 10 mg
Auxiliary substances: glycerol 250 mg, propylene glycol 350 mg, sodium saccharinate 10 mg, sodium acetate trihydrate 10 mg, methyl parahydroxybenzoate 1.35 mg, propyl parahydroxybenzoate 0.15 mg, glacial acetic acid 0.5 mg, purified water up to 1 ml.
20 ml - a bottle of a dropper of dark glass (1) - packs 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 oral administration 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. In case of oral administration at doses of 5 to 60 mg, cetirizine has a linear pharmacokinetics (kinetics of zero order). 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 starting material, and therefore it 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 as unchanged substance through the kidneys, and 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 plasma is 8-12 hours in adults.
Pharmacokinetics in specific patient groups
T 1/2 is approximately 6 hours in children aged 6 to 12 years and approximately 5 hours in children aged 1 to 6 years.
Because of the higher incidence of decreased renal function in elderly patients, cetirizine clearance in them can be reduced.
With multiple admission, the pharmacokinetics of cetirizine do not significantly change with mild renal insufficiency compared to healthy volunteers. However, in patients with moderate renal insufficiency, T 1/2 cetirizine increases threefold, and the clearance decreases by 70% compared to patients with normal renal function. In patients receiving hemodialysis treatment, a threefold increase in T 1/2 and a 70% reduction in clearance even after a single administration of 10 mg of cetirizine 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. Drops before use dissolve in a small amount of water.
Adults and children aged 12 years: 10 mg (20 drops) 1 time / day, preferably overnight.
Children aged 1-2 years: 2.5 mg (5 drops) 2 times / day.
Children aged 2-6 years: 5 mg (10 drops) once. It is also possible to divide this dose into two divided 2.5 mg (5 drops each morning and evening).
Children aged 6-12 years: 5 mg (10 drops) 2 times / day in the morning and evening; or 10 mg (20 drops) in the evening.
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 determination of the serum creatinine concentration (mg%), the CK value (ml / min) can be estimated by the following formula:
CC = [140 - age (years)]? body weight (kg) / 72 - serum creatinine (mg%)
In women, the obtained value should be multiplied by 0.85
Selection of dose depending on QC
CK (ml / min) Dosing
? 80 10 mg 1 time / day
50-79 10 mg 1 time / day
30 mg 5 mg 1 time / day
11-29 5 mg once every two days
10 (hemodialysis) Contraindicated
Usually the drug is well tolerated. In very rare cases, the following side effects may occur.
From the hematopoiesis: thrombocytopenia.
From the nervous system: drowsiness, dizziness, headache, aggression, agitation, confusion, depression, hallucinations, insomnia, teak, seizures, dyskinesia, dystonia, parasthesia, fainting, tremor.
From the side of the organ of vision: disruption of accommodation, visual impairment, nystagmus.
From the cardiovascular system: tachycardia.
On the part of the respiratory system: rhinitis, pharyngitis.
On the part of the digestive system: dryness of the oral mucosa, nausea, abdominal pain, diarrhea, impaired liver function (increased activity of hepatic transaminases, alkaline phosphatase, GGT, bilirubin concentration).
From the urinary system: urination disorder, urinary incontinence.
From the skin and subcutaneous tissue: itching, rash, hives, angioedema.
Allergic reactions: hypersensitivity, up to the development of anaphylactic shock.
Other: weight gain, fatigue, asthenia, malaise, swelling.
- renal failure (CC less than 10 ml / min);
- lactation period (breastfeeding);
- Children's age up to 1 year;
- 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 excreted in 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
Caution should be used for chronic renal failure of moderate and severe degree (correction of the dosing regimen is required).
Contraindicated use of the drug in renal failure (KK less than 10 ml / min).
APPLICATION FOR CHILDREN
The drug is contraindicated for use in children under 1 year.
APPLICATION IN ELDERLY PATIENTS
It may be necessary to reduce the dose in elderly patients .
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 the effect 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 rarely 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.
Drops contain an auxiliary substance methyl parahydroxybenzoate, which can cause late allergic reactions.
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 (when taking a single dose of 50 mg): dryness of the oral mucosa, drowsiness, stupor, urinary retention, constipation, anxiety, increased irritability
Treatment: gastric lavage, 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 cetirizine group with ketoconazole did not cause clinically significant ECG changes.
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 in a place protected from light, inaccessible to children, at a temperature of no higher than 25 В° C. Shelf life - 4 years.
The open vial should be stored for no more than 4 weeks.