active substance: cetirizine dihydrochloride;
1 tablet contains cetirizine dihydrochloride 10 mg
auxiliary substances: lactose, corn starch, 30, magnesium stearate, hypromellose (2910/5), polyethylene glycol (macrogol 6000), talc, titanium dioxide (E 171), simeticone emulsion (SE 4).
Basic physical and chemical properties: tablets, film-coated, oblong, white or almost white color with a notch on one side.
Antihistamines for systemic use. Derivatives of piperazine. Code ATX R06A E07.
Cetirizine, a metabolite of hydroxyzine that is formed in the human body, is a powerful selective antagonist of peripheral h 1 receptors. Research associate with the receptor in terms of UI vitro did not show significant affinity for other receptors in addition to H1 receptors.
It has been shown that in addition to this, the anti-1 effect causes cetirizine anti-allergic effect: in a dose of 10 mg 1 or 2 times a day it inhibits the late phase of the mobilization of eosinophils in the skin and conjunctiva of patients with atopic dermatitis, which was conducted provocative test for the presence of Allergy.
Studies among healthy volunteers have shown that cetirizine at doses of 5 and 10 mg strongly inhibits reactions with the appearance of bubbles and inflammatory hyperemia caused by very high concentrations of histamine in the skin, but no correlation with effectiveness.
No addiction to the antihistamine effect of cetirizine (suppression of blisters and inflammatory hyperemia) was revealed. When after repeated doses of cetirizine treatment stopped, the normal reaction of the skin to histamine was restored within 3 days.
In patients with allergic rhinitis on the background of bronchial asthma mild or moderate cetirizine dose of 10 mg once a day reduced symptoms of rhinitis, without affecting lung function. This study confirms the safety of cetirizine in allergic patients who have mild to moderate bronchial asthma.
Cetirizine, intended in a high dose of 60 mg for 7 days, did not cause statistically significant elongation of THE Qt interval.
It has been demonstrated that in the recommended doses, cetirizine improves the quality of life of patients with year-round and seasonal allergic rhinitis.
The peak concentration in the blood plasma in equilibrium is about 300 ng/ml and is achieved within 1.0 ± 0.5 hours. After taking cetirizine at a dose of 10 mg for 10 days of cumulation was observed. The distribution of such pharmacokinetic parameters as the maximum concentration in blood plasma (Cmax) and the area under the pharmacokinetic curve (AUC) is uniform among volunteers.
The degree of absorption of cetirizine is not reduced with food, but reduced the absorption rate. Bioavailability of cetirizine in the form of solution, capsules or tablets is similar.
The estimated volume of distribution in the body is 0.50 l/kg. Percentage of cetirizine bind with blood plasma proteins is 93 ± 0.3 percent. Cetirizine does not affect the binding of warfarin with plasma proteins.
Cetirizine does not undergo significant metabolism at the first pass. About 2/3 of the substance is excreted with urine in an unmodified form. The final half-life is approximately 10: 00.
In the dose range from 5 to 60 mg pharmacokinetics cetirizine is linear.
Special populations of patients.
Elderly patients after a single dose of the drug at a dose of 10 mg, the half-life increased by about 50% and clearance decreased by 40% in 16 elderly patients compared with normal patients. The decrease in cetirizine clearance in these elderly volunteers age is clearly associated with a reduction in them functions of the kidneys.
Children:the half-life of cetirizine is approximately 6: 00 at the age of 6-12.
Patients with impaired renal function pharmacokinetic parameters of the drug were similar in patients with mild renal impairment (creatinine clearance of 40 ml/min) and healthy volunteers. In patients with moderate renal impairment, there was a threefold increase in the half-life and a decrease in clearance by 70% compared to healthy volunteers.
In patients who were on hemodialysis (creatinine clearance below 7 ml/min), after a single oral administration of cetirizine at a dose of 10 mg, there was a threefold increase in the half-life period and a decrease in clearance by 70% compared to conventional patients. Cetirizine is poorly removed by hemodialysis. In patients with moderate or severe impaired renal function require dose adjustment (see Section "Method of application and dosage").
Patients with impaired liver function in patients with chronic liver diseases (hepatocellular, cholestatic diseases and biliary cirrhosis), who once took 10 or 20 mg of cetirizine, there was an increase in the half-life by 50% and a decrease in clearance by 40% compared with healthy patients.
Dose adjustment in patients with impaired liver function is necessary only in the presence of concomitant renal impairment.
Symptomatic therapy of nasal and eye symptoms of seasonal and permanent allergic rhinitis, chronic idiopathic urticaria.
Hypersensitivity to the active substance or to any auxiliary substance that is part of the drug, hydroxyzine or any derivative piperazine.
Patients with severe impairment of renal function with a creatinine clearance less than 10 ml/min.
Patients with rare hereditary forms of galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose should not take cetirizine in the form of coated tablets.
Interaction with other medicinal products and other forms of interaction
Pharmacokinetic interactions were studied with cetirizine and pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin; pharmacokinetic interactions were not observed. In the study of repeated use of theophylline (400 mg 1 time per day) and cetirizine there was a slight (16%) decrease in clearance of cetirizine, while theophylline disposition was not disturbed while taking cetirizine.
In studies of the use of cetirizine with cimetidine, glipizide, diazepam and pseudoephedrine, there is no evidence of side pharmacodynamic interactions.
In studies of the use of cetirizine with azithromycin,erythromycin, ketoconazole, theophylline and pseudoephedrine no evidence of adverse clinical interactions. In addition, the simultaneous use of cetirizine with macrolides or ketoconazole has never led to clinically significant changes in ECG.
In the study of repeated use of ritonavir (600 mg 2 times a day) and cetirizine (10 mg per day), the duration of exposure to cetirizine increased by about 40%, while the disposition of ritonavir slightly violated (-11%) while taking cetirizine.
The amount of absorption of cetirizine is not reduced with food, although the rate of absorption is decreased by 1:00.
No data on the effect of sedatives when used in therapeutic doses. But you should avoid the use of sedatives while taking the drug.
When taken in therapeutic doses, there were no clinically significant interactions with alcohol (at blood alcohol levels of 0.5 g/l). However, it is recommended to avoid the simultaneous use of alcohol.
Use caution in patients prone to urinary retention (spinal injury, prostate hyperplasia), as cetirizine may increase the risk of urinary retention.
It is recommended to appoint with caution patients with epilepsy and patients at risk of seizures.
Antihistamines suppress the skin Allergy test, so before its implementation, the drug should be discontinued 3 days before the study (a period of withdrawal).
Use with caution in patients with chronic renal insufficiency (dosage regimen correction is required) and elderly patients with renal insufficiency (glomerular filtration may be reduced).
Application during pregnancy and lactation
Pregnancy. Insufficient data on the effect of the drug during pregnancy. Animal studies do not indicate direct or indirect harmful effect on pregnancy, embryonal/fetal development, birth or postnatal development. Care should be taken to prescribe the drug to pregnant women in cases where, according to the doctor, the benefits of the use exceeds the potential risk to the fetus.
Lactation. Cetirizine passes into breast milk in concentrations that make up 25-90% of the concentration in blood plasma depending on time after treatment. Therefore, caution should be prescribed to women who breastfeed.
The ability to influence the reaction rate when driving motor transport or operating other mechanisms
An objective assessment of ability to drive vehicles, the presence of occult sleepiness and ability to work on the Assembly line did not reveal any clinically significant effects when using the drug at the recommended dose of 10 mg.
Patients who intend to drive, engage in potentially hazardous activities or operate machinery should not exceed the recommended dose and must take into account the reaction of their organism to this drug. In sensitive patients, simultaneous administration of the drug with other drugs that inhibit the activity of the Central nervous system can lead to additional deterioration in concentration and decreased productivity.
Method of application and doses
Children aged 6 to 12 years : 5 mg 2 times a day (? tablet 2 times per day).
Adults and children over 12 years: 10 mg 1 time per day (1 tablet 1 time per day).
The tablets should be swallowed with a large glass of water.
Elderly patients: evidence suggests that the dose should not be reduced in elderly patients with normal kidney function.
Patients with impaired renal function moderate and severe : data on the ratio "performance/safety" for patients with impaired renal function no. Since cetirizine is excreted primarily through the kidneys (see section "Pharmacological properties"), in cases where you can not apply another method of treatment, the intervals between doses should be set individually. Adjust the dose of the drug should be according to the information given in the table. In order to use this dosing table, it is necessary to calculate the clearance of patient creatinine (CL CR) in ml/min. CL CR (ml/min) can be calculated using a specific serum creatinine level (mg/DL) using the following formula:
CL CR = [140-age (in years)] ? body weight (kg) (? 0.85 for women)
72 ? serum creatinine (mg/DL)
Dosage adjustment for adult patients with impaired renal function.
grouppick (ml/min)Dose and frequency of administration
Renal function was normal? 8010 mg 1 time per day
The impairment of renal function easy степени50-7910 mg 1 time per day
The impairment of renal function the average degree тяжести30-495 mg 1 time per day
The impairment of renal function severe<305 mg 1 time every 2 days
End-stage kidney disease -
patients subject to hemodialysis<10противопоказано
Children with impaired renal function dose should be selected individually, taking into account the importance of renal clearance of each patient, as well as his age and body weight.
Patients with abnormal liver function in patients who have only hepatic impairment, adjust the dose.
Patients with impaired liver and kidney function : recommended dose adjustment (see Above "patients with impaired renal function of moderate to severe").
The duration of treatment is determined by the doctor individually depending on the course of the disease.
To administer the drug to children under the age of 6 years. The drug in the form of coated tablets is not recommended for children under 6 years old, since this dosage form does not allow you to choose the right dose.
Symptoms. The symptoms observed in overdose cetirizine, mainly associated with its effect on the Central nervous system or of manifestations may resemble the anticholinergic effect.
To undesirable phenomena, which were observed after administration of doses at least 5 times greater than the recommended daily dose are: confusion, diarrhoea, dizziness, fatigue, headache, malaise, mydriasis, pruritus, restlessness, sedation, somnolence, stupor, tachycardia, tremor and urinary retention.
Treatment. The specific antidote of cetirizine is unknown. In case of overdose, it is recommended to carry out symptomatic or supportive therapy. After taking the drug as soon as possible to carry out gastric lavage. Cetirizine, removal by dialysis is ineffective.
Clinical studies have shown that the use of cetirizine in recommended doses can lead to minor adverse effects on the Central nervous system, including drowsiness, fatigue, dizziness and headache. In some cases, there have been reports of paradoxical stimulation of the Central nervous system.
Although cetirizine is a selective antagonist of peripheral h 1 receptors without relative anticholinergic activity, there have been reports of isolated cases of difficulty urinating, ocular accommodation disorders and dry mouth.
There have been reports of cases of liver dysfunction with increased levels of liver enzymes, combined with increased levels of bilirubin. In most cases, these symptoms disappeared after discontinuation of cetirizine dihydrochloride.
In double-blind controlled studies or pharmacokinetic comparison of cetirizine and placebo or antihistamines at the recommended doses (10 mg daily for cetirizine), in which available quantitative data on security, attended by more than 3200 patients taking cetirizine. Among this set of patients there were reports of the following adverse events due to the intake of cetirizine at a dose of 10 mg in placebo-controlled studies, the frequency of which was 1% or higher:
Adverse event (according to the terminology of adverse events who)Cetirizine 10 mg
(N = 3260)placebo
(N = 3061))
Body as a whole - General disorders
From the Central and peripheral nervous system
The gastro-intestinal tract
From the respiratory system
Although drowsiness occurred statistically more often than in the placebo group, in most cases its degree is mild or moderate. Objective tests, as demonstrated in other studies, showed that the use of the drug in the recommended daily doses in healthy volunteers daily activity was not disturbed.
Among children aged 6 months to 12 years, who were included in placebo-controlled clinical or pharmacoklinical studies, there were adverse reactions to the drug, the frequency of which was 1% or higher:
Adverse reactions to the drug
(According to the terminology of adverse events who)Tsetirizin
(N = 1656)placebo
(N = 1294)
The gastro-intestinal tract
From the respiratory system
Body as a whole - General disorders
Experience of post-registration application
In addition to the side effects, which were reported during clinical trials and the above, during the post-registration application reported isolated cases of the following adverse reactions to the drug. These side effects, which were reported less frequently, were estimated by frequency of occurrence (infrequently ? 1/1000 to <1/100, rarely ? 1/10000 to <1/1000, very rarely <1/10000) based on experience of post-registration application.
From the blood and lymphatic system
Very rarely thrombocytopenia.
From the immune system
Very rarely anaphylactic shock.
Infrequently mental excitement with anxiety (agitation).
Rarely aggression, confusion, depression, hallucinations, insomnia.
Very rarely nervous TIC.
The frequency is unknown: suicidal thoughts.
From the nervous system
Rarely spasms, motor disorders.
Very rarely dysgeusia, syncope, tremor, dystonia, dyskinesia.
The frequency is unknown-amnesia, memory disturbance.
By the organs of vision
Very rarely: accommodation disorders, blurred vision, disorders of movement of the eyeball.
From the heart
On the part of the hearing organs and balance
Frequency not known: vertigo.
The gastro-intestinal tract
From the digestive system
Rare: abnormal liver function (increased transaminases, alkaline phosphatase, gamma-glutamyl transpeptidase and bilirubin).
On the part of the skin and subcutaneous tissue
Uncommon: pruritus, rash.
Very rare angioneurotic oedema, fixed drug erythema.
From the kidneys and urinary tract
Very rarely dysuria, enuresis.
The frequency of unknown urinary retention.
From the side of nutrition and metabolism: the frequency is unknown - increased appetite.
Infrequently asthenia, malaise.
Changes in laboratory and instrumental studies
Rare: increase body weight.
Does not require special storage conditions. Keep out of reach of children.
№ 10 № 30 (10x 3): 10 tablets in a blister, 1 or 3 blisters in a cardboard box.
Category home away from home
Without a prescription.
Manufacturer's location and address of the place of business
In kabelovny 130, 102 37 Praha 10 doln? Mecholupy, Czech Republic.
Ketotifen No. 30 comes in the form of tablets of 1 mg. Are the stabilizer of the membranes of the fat cells. They have antianaphylactic and anti-allergic effects. Intended for the relief of asthma attacks. Active element-ketotifen 1 mg.
Indications for use
The drug is prescribed in the following pathological conditions:
Complications of asthma in hay fever.
Rhinitis allergic Genesis.
Dermatoses of allergic origin.
Do not use if individual immunity activedata components of the tablets. It is not prescribed to patients under 3 years, as well as nursing and pregnant women.
Instructions for use
The medicine is intended for oral use. Patients are prescribed 2 tablets per day twice a day. The medicine is taken with meals.
Patients with 2 years in the weight up to 25 kg – half tablet twice a day. If therapeutic measures do not give the necessary result for 28 days, the dosage can be increased to 1 mg 2 times a day. Children weighing more than 25 kg are prescribed 2 tablets twice a day.