Name:
Tsetrin tab. p / o 10 mg in bl. in pack. No. 10×2
Description:
Coated tablets, white or almost white, round, with a biconvex surface, one side is smooth, on the other a dividing line. The tablet can be divided into equal doses. The main active ingredient is cetirizine. Release form Tablets. Dosage 10mg. Pharmacological action Pharmacodynamics Mechanism of action Cetirizine, a metabolite of hydroxyzine, is a potent selective H1 peripheral receptor antagonist with virtually no effect on other receptors. In addition to blockade of peripheral H1 receptors, cetirizine has anti-allergic properties. When using the drug at a dose of 10 mg 1 or 2 times a day, the drug suppresses the accumulation of eosinophils in the skin and conjunctiva in the late phase in atopic patients after an allergen provocation. Clinical efficacy and safety Studies in healthy volunteers have shown that cetirizine at a dose of 5 mg or 10 mg significantly reduces the “triple response” – a skin reaction like “flowering” caused by a high concentration of histamine in the skin, however, the correlation of this effect with clinical efficacy has not been proven. In one 35-day study conducted with children aged 5-12 years, no development of tolerance was detected, i.e. inability to suppress the “bloom” response to the antihistamine effect of cetirizine. After stopping the use of repeated doses of cetirizine for three days, the skin again acquired the characteristic ability to respond to histamine. The 6-week, placebo-controlled study included 186 patients with allergic rhinitis and concomitant mild to moderate asthma. Cetirizine at a dose of 10 mg/day relieved the symptoms of rhinitis and did not affect respiratory function. This study confirmed the safety of cetirizine in allergic patients with mild to moderate asthma. In one placebo-controlled study, it was shown that the use of high doses of cetirizine (60 mg / day) for 7 days did not statistically significantly prolong the QT interval. Based on studies conducted, it has been found that cetirizine at recommended doses improves the quality of life of patients suffering from persistent or seasonal allergic rhinitis. Pharmacokinetics Absorption The equilibrium maximum concentration is approximately 300 ng / ml and is reached within 1.0 ± 0.5 hours. Cetirizine at a dose of 10 mg/day with a repeated dose for 10 days did not accumulate. The distribution of pharmacokinetic parameters, such as maximum plasma concentration (Cmax) and area under the curve (AUC), is unimodal. Food does not affect the completeness of absorption, although the rate of absorption decreases. The degree of bioavailability is similar when using cetirizine in the form of a solution, capsules or tablets. Distribution The apparent volume of distribution is approximately 0.50 l/kg. 93 ± 0.3% of cetirizine binds to plasma proteins. Cetirizine does not affect the binding of warfarin to plasma proteins. Biotransformation Cetirizine does not undergo significant presystemic metabolism. Withdrawal About 2/3 of the dose is excreted unchanged in the urine. The half-life is about 10 hours. Linearity/Nonlinearity Cetirizine has linear kinetics over a dose range of 5 to 60 mg. Special Patient Populations Elderly In 16 elderly volunteers, after a single oral dose of cetirizine 10 mg, half-life was increased by approximately 50% and clearance was reduced by 40% compared to non-elderly subjects. Decreased clearance of cetirizine in these elderly volunteers was probably associated with worsening renal function. Children and Infants The elimination half-life of cetirizine was approximately 6 hours in children aged 6 to 12 years and 5 hours in children aged 2 to 6 years. In children aged 6 to 24 months, the elimination half-life was reduced to 3.1 hours. Patients with impaired renal function In patients with mild renal insufficiency (CC> 40 ml / min), the pharmacokinetics of the drug was similar to that in healthy volunteers. In moderate renal insufficiency, compared with healthy volunteers, the half-life increased three times, and the clearance decreased by 70%. Compared with healthy volunteers, in patients on hemodialysis (CC < 7 ml / min), after a single dose of cetirizine 10 mg, the half-life increased three times, and the clearance decreased by 70%. Cetirizine is poorly removed by hemodialysis. With moderate to severe impairment of renal function, dose adjustment is necessary (see section Dosage and administration). Patients with impaired liver function In patients with chronic hepatic impairment (hepatocellular, cholestatic and biliary cirrhosis), compared with healthy individuals, after oral administration of 10 mg or 20 mg of cetirizine, the half-life decreased by 50%, and clearance decreased by 40%. In patients with impaired liver function, dose adjustment is necessary only in case of concomitant impaired renal function. Preclinical safety studies Preclinical studies of safety, pharmacological properties, repeated dose toxicity, genotoxicity, carcinogenic potential and reproductive toxicity did not reveal any specific risk to humans. Indications for use For adults and children 6 years of age and older: - relief of symptoms of seasonal and year-round allergic rhinitis (hay fever, hay fever); the maximum duration of treatment for seasonal rhinitis in children is 4 weeks; - allergic conjunctivitis; - chronic idiopathic urticaria. Dosage and administration Seasonal allergic rhinitis Adults and adolescents over 12 years of age: The recommended dose is 10 mg (1 tablet) once a day. Children 6 to 12 years old: 10 mg (1 tablet) once a day. The maximum duration of treatment is 4 weeks. The dose may be divided into 2 doses of 5 mg (1/2 tablet) in the morning and evening, respectively. Allergic conjunctivitis Adults and adolescents over 12 years of age: The recommended dose is 10 mg (1 tablet) once a day. Children 6 to 12 years old: 10 mg (1 tablet) once a day. The maximum duration of treatment is 4 weeks. The dose can be divided into 2 doses of 5 mg (1/2 tablet) in the morning and evening, respectively. Perennial allergic rhinitis and chronic idiopathic urticaria Adults and adolescents over 12 years of age: The recommended dose is 10 mg (1 tablet) once a day. Children 6 to 12 years old: 10 mg (1 tablet) once a day. The dose may be divided into 2 doses of 5 mg (1/2 tablet) in the morning and evening, respectively. Patients requiring a special dosing regimen Elderly patients With an age-related decrease in glomerular filtration, the drug is prescribed for elderly patients at the same dose as for patients with renal insufficiency. Patients with renal insufficiency There are no data on the efficacy and safety of the use of cetirizine in patients with renal insufficiency. Since cetirizine is primarily excreted by the kidneys, in cases where alternative treatment cannot be used, dosing intervals should be individualized according to renal function. The intervals between taking the drug are individually adjusted depending on the degree of renal failure. Dosing is carried out in accordance with the table below. When using this table, creatinine clearance (CC) is calculated in ml/min. QC for women can be calculated by multiplying the resulting value by a factor of 0.85. Dosage for patients with renal insufficiency Renal insufficiency CC (ml / min) Dosing regimen Norm ≥ 80 10 mg Mild 50-79 10 mg Average 30-49 5 mg (1/2 tablet) / day Severe 10-29 5 mg (1/2 2 tablet) every other day End-stage - patients on dialysis < 10 drug contraindicated In children with renal insufficiency, the dose should be adjusted on an individual basis taking into account the patient's renal clearance, age and body weight. Patients with hepatic insufficiency Patients with only impaired liver function dosing adjustment is not required. For patients with hepatic and renal insufficiency, a dosage adjustment is required (see Patients with Renal Insufficiency). Taking the drug The drug should be taken in the evening, due to the more intense manifestation of symptoms at this time of day. The tablet is swallowed whole without chewing and washed down with water. Cetrine is taken with or without food. In case of mild side effects in adults and adolescents over 12 years of age, it is recommended to take 5 mg (1/2 tablet) of Cetrin in the morning and evening, respectively. Use during pregnancy and lactation Pregnancy There are currently no clinical studies available on the use of cetirizine in pregnant women. Experimental studies on animals did not reveal any direct or indirect toxic effect of cetirizine on the course of pregnancy, embryonic development, embryonic development, including in the postnatal period. The potential risk for women is unknown. When taking the drug during pregnancy, caution should be exercised. Lactation Cetirizine is excreted in breast milk, so the drug should be administered with caution during the period of feeding. Precautions - In patients with renal insufficiency, the dose should be adjusted accordingly (see section "Method of administration and doses"). - In elderly patients, a decrease in kidney function is possible, which should be taken into account when dosing the drug. - The use of Cetrin in patients with epilepsy and with a tendency to convulsions should be carried out with caution. - In children under 6 years of age, the use of film-coated tablets is not recommended, since the release form does not allow adjustment of the dose of the drug. - When taking Cetrin, you should refrain from drinking alcohol and CNS antidepressants, since cetirizine can cause increased drowsiness. - Caution must be observed in patients who have predisposing factors for urinary retention (spinal cord injury, prostatic hyperplasia), as cetirizine may increase the risk of urinary problems. Use in children Cetirizine should not be used in children under 6 years of age due to the lack of sufficient information on its efficacy and safety in this age group. Interaction with other drugs When used simultaneously with pseudoephedrine, cimetidine, ketoconazole, erythromycin or azithromycin, no effect on the pharmacokinetics of cetirizine was detected. No pharmacodynamic interactions were observed. In vitro tests have shown that cetirizine does not affect the protein-binding properties of warfarin. With simultaneous use with azithromycin, erythromycin, ketoconazole, theophylline and pseudoephedrine, no clinically significant adverse interactions were detected, no changes were noted on the electrocardiogram. With the simultaneous use of cetirizine (20 mg / day) with theophylline (400 mg / day), a slight but stable increase in the area under the curve of dependence of concentration and time per day was revealed, cetirizine by 19%, theophylline - 11%. Moreover, peak plasma levels reached 7.7% and 6.4% for cetirizine and theophylline, respectively. At the same time, the total clearance of cetirizine decreased by 16%, the clearance of theophylline - by 10%, if theophylline treatment was carried out before the appointment of cetirizine. However, when initially treated with cetirizine, there was no significant effect on theophylline pharmacokinetics. After a single dose of 10 mg of cetirizine, the effect of alcohol does not increase significantly; 1 out of 16 psychometric tests showed a statistically significant interaction with diazepam 5 mg. With the simultaneous daily use of cetirizine (10 mg) with glipizide, the blood glucose concentration decreased slightly. However, this was clinically insignificant. However, it is recommended to take these drugs separately - glipizide in the morning and cetirizine in the evening. Eating does not affect the completeness of absorption, although its rate decreases by 1 hour. With repeated administration of ritonavir (600 mg twice a day) and cetirizine (10 mg / day), the degree of action increased by 40%, while the effect of ritonavir changed slightly (-11%) while taking cetirizine. A three-day "washout" period is recommended before the appointment of allergic tests. Antihistamines have an inhibitory effect on skin allergy tests. Contraindications - hypersensitivity to cetirizine, hydroxyzine or piperazine derivatives, as well as other components of the drug; - end-stage renal disease (creatinine clearance < 10 ml/min); - congenital galactose intolerance, lactase deficiency and glucose-galactose malabsorption syndrome. Composition Each tablet contains: active substance: cetirizine hydrochloride - 10 mg; excipients: anhydrous lactose, corn starch, povidone (K-30), magnesium stearate, tablet shell (including hypromellose, sorbic acid, titanium dioxide (E171), purified talc, macrogol 6000, polysorbate 80, dimethicone). Overdose The symptoms observed after an overdose of cetirizine are mainly related to effects on the central nervous system or to effects that may indicate an anticholinergic effect. With a single dose of the drug at a dose of 50 mg, the following symptoms were observed: confusion, diarrhea, dizziness, fatigue, headache, malaise, mydriasis, itching, weakness, anxiety, sedation, drowsiness, stupor, tachycardia, tremor, urinary retention. Treatment: immediately after taking the drug - gastric lavage or stimulation of vomiting. It is recommended to take activated charcoal, conduct symptomatic and supportive therapy. There is no specific antidote. Hemodialysis is ineffective. Side effects According to clinical studies, cetirizine at all recommended doses can cause only minimal adverse reactions from the central nervous system, such as drowsiness, fatigue, dizziness and headache. In some cases, paradoxical stimulation of the CNS was observed. Despite the fact that cetirizine is a selective peripheral H1 receptor antagonist and relatively does not have anticholinergic activity, urinary and visual disturbances, as well as dry mouth, have been observed in isolated cases. There have been cases of abnormal liver function with an increase in liver enzymes with an accompanying elevated level of bilirubin. In most cases, these changes disappear when treatment with cetirizine is discontinued. Clinical studies In double-blind controlled clinical or pharmacoclinical studies of cetirizine compared with placebo or other antihistamines at the recommended doses (for cetirizine this was 10 mg/day), for which quantitative safety data are available, 3200 patients were included receiving cetirizine . Based on these pooled data from placebo-controlled studies, the following adverse reactions were observed for cetirizine 10 mg occurring at a frequency of 1% or more Adverse Reaction (WHO-ART) Cetirizine 10 mg (n=3260) Placebo (n=3061) General disorders Fatigue 1.63% 0.95% Nervous system disorders Dizziness Headache 1.10% 7.42% 0.98% 8.07% Gastrointestinal disorders Abdominal pain Dry mouth Nausea 0.98% 2.09% 1.07% 1.08% 0.82% 1.07% 1.08% 0.82% 1.14% Mental disorders Sleepiness 9.63% 5.00% Respiratory system disorders Pharyngitis 1.29% 1.34% Despite the statistically more frequent development of drowsiness compared to placebo, in most cases its severity was mild to moderate. Data from objective tests conducted in other studies showed that daily activity in young healthy volunteers did not deteriorate when the drug was used at recommended doses. Children and adolescents Adverse reactions observed at a frequency of 1% or more in clinical or pharmacoclinical studies in children aged 6 months to 12 years are listed below: Adverse reaction (WHO-ART) Cetirizine (n=1656) Placebo (n=1294 ) Gastrointestinal disorders Diarrhea Cetirizine (n=1656) 1.0% Placebo (n=1294) 0.6% Psychiatric disorders Drowsiness Cetirizine (n=1656) 1.8% Placebo (n=1294) 1.4% Respiratory system disorders Rhinitis Cetirizine (n=1656) 1.4% Placebo (n=1294) 1.1% General Disorders Fatigue Cetirizine (n=1656) 1.0% Placebo (n=1294) 0.3% cases of use: very often (≥1/10), often (≥1/100, <1/10), infrequently (≥1/1000, <1/100), rarely (≥1/10000, <1/1000) , very rare (<1/10000), frequency unknown (due to insufficient data). Blood and lymphatic system disorders: Very rare: thrombocytopenia. Immune system disorders: Rare: hypersensitivity reactions. Very rare: anaphylactic shock. Metabolic and nutritional disorders: Frequency unknown: increased appetite. Psychiatric disorders: Uncommon: agitation. Rare: aggression, confusion, depression, hallucinations, sleep disturbance. Very rare: tick. Frequency unknown: nightmares. Nervous system disorders: Uncommon: paresthesia. Rare: convulsions. Very rare: taste perversion, dyskinesia, dystonia, fainting, tremor. Frequency unknown: deafness, amnesia, memory impairment. Frequency unknown: Suicidal thoughts. On the part of the organ of vision: Very rarely - disturbance of accommodation, blurred vision, nystagmus. Frequency unknown: vasculitis. On the part of the organ of hearing and labyrinth: Frequency unknown: vertigo. Cardiac disorders: Rare: tachycardia Gastrointestinal disorders: Uncommon: diarrhea. Liver and biliary tract disorders: Rare: changes in liver function tests (increased levels of transaminases, alkaline phosphatase, γ-glutamate transferase and bilirubin). Frequency unknown: hepatitis. Skin and subcutaneous tissue disorders: Uncommon: rash, itching. Rare: urticaria. Very rare: angioedema, persistent erythema. Frequency unknown: acute generalized exanthematous pustulosis. Muscular, skeletal and connective tissue disorders: Rare: movement disorders. Frequency unknown: arthralgia. Renal and urinary disorders: Very rare: dysuria, enuresis. Frequency unknown: urinary retention. General disorders and reactions at the injection site: Uncommon: asthenia, malaise. Rare: peripheral edema. Laboratory and instrumental data: Rare: weight gain. In the post-registration period, the following undesirable effects were observed: itching and / or urticaria after discontinuation of cetirizine. Reporting adverse reactions: It is important to report suspected adverse reactions after registration of a medicinal product in order to ensure continuous monitoring of the benefit-risk balance of the medicinal product. Healthcare professionals are encouraged to report any suspected adverse drug reactions through national adverse drug reaction and drug failure reporting systems. If the patient experiences any adverse reactions, it is recommended to consult a doctor. This recommendation applies to any possible adverse reactions, including those not listed in the instructions for medical use. You can also report adverse reactions to the adverse drug reactions (actions) information database, including reports of drug failures. By reporting adverse reactions, you help to get more information about the safety of the drug. Storage conditions Store in a place protected from light and moisture, at temperatures up to 25 ° C. Keep out of the reach of children. in cont. cell. pack No. 10x2
INN | CETIRIZINE |
---|---|
The code | 141 409 |
Barcode | 4 810 201 019 802 |
Dosage | 10mg |
Active substance | cetirizine |
Manufacturer | Dr. Reddy's Lab. Ltd., India packed by JSC Borisovsky zad med. drugs, Belarus |
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