Cetrine coated pills 10mg N20
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Active ingredients
Cetirizine
Release form
Pills
Composition
Cetirizine dihydrochloride 10 mg; Excipients: lactose - 106.5 mg, corn starch - 65 mg, povidone K30 - 2 mg, magnesium stearate - 1.5 mg. The composition of the film shell: hypromellose - 3.3 mg, macrogol 6000 - 0.661 mg, titanium dioxide - 0.706 mg, talc - 1.183 mg, sorbic acid - 0.05 mg, polysorbate 80 - 0.05 mg, dimethicone - 0.05 mg.
Pharmacological effect
Histamine H1 receptor blocker. Cetirizine - hydroxyzine metabolite, competitive histamine antagonist. It prevents the development and facilitates the course of allergic reactions, has antipruritic and anti-exudative action .; It affects the early histamine-dependent stage of allergic reactions, limits the release of inflammatory mediators at the late stage of an allergic reaction, reduces the migration of eosinophils, neutrophils and basophils, stabilizes the membranes of mast cells. Reduces capillary permeability, prevents the development of tissue edema, relieves spasm of smooth muscles. Eliminates skin reactions to the introduction of histamine, specific allergens, as well as cooling (with cold urticaria). Reduces histamine-induced bronchoconstriction in bronchial asthma; Cetirizine does not have anticholinergic and antiserotonin action. In therapeutic doses does not have a sedative effect .; The effect after taking drops in a single dose of 10 mg develops after 20 minutes in 50% of patients and after 60 minutes in 95% of patients, lasts more than 24 hours. After taking the tablet, the effect occurs after 20 minutes. Against the background of a course of treatment, tolerance to the antihistamine effect of cetirizine does not develop. After cessation of treatment, the effect lasts up to 3 days.
Pharmacokinetics
The pharmacokinetic parameters of cetirizine change linearly with the appointment of the drug in a dose of 5-60 mg.; After oral administration, cetirizine is rapidly and completely absorbed from the gastrointestinal tract. Food intake does not affect the completeness of suction, although the rate of absorption decreases and the value of Cmax decreases by 23%. In adults, after a single dose of the drug in a therapeutic dose of Cmax in the blood plasma is achieved after 1 ± 0.5 h and is 300 ng / ml .; Distribution; Plasma protein binding is 93 ± 0.3% and does not change when the concentration of cetirizine is in the range of 25-1000 ng / ml. Vd is 0.5 l / kg.When taking the drug in a dose of 10 mg for 10 days, cetirizine is not cumulated. Cetirizine is excreted in breast milk .; Metabolism; In small quantities, it is metabolized in the body by O-dealkylation (unlike other histamine H1 receptor antagonists, which are metabolized in the liver using the cytochrome P450 system), with the formation of a pharmacologically inactive metabolite .; Withdrawal; In adults, T1 / 2 is about 10 hours. About 2/3 of the dose taken is excreted in the urine unchanged, 10% in the feces. System clearance - 53 ml / min; Pharmacokinetics in special groups of patients; In elderly patients and patients with chronic liver diseases, a single dose of the drug at a dose of 10 mg T1 / 2 is increased by about 50%, and the systemic clearance is reduced by 40% .; T1 / 2 in children aged 6 to 12 years old is 6 hours, at the age of 2 to 6 years old - 5 hours, at the age of 6 months to 2 years old - 3.1 hours; In patients with mild renal insufficiency (CC> 40 ml / min), pharmacokinetic parameters are similar to those in patients with normal renal function. In patients with renal failure of moderate severity and in patients on hemodialysis (CC <7 ml / min), when the drug is taken orally at a dose of 10 mg T1 / 2, it is 3 times longer, and the total clearance is reduced by 70% (0.3 ml / min / kg), relative to patients with normal renal function, which requires a corresponding change in dosing regimen. Cetirizine is practically not removed from the body during hemodialysis .; In patients with chronic liver diseases (hepatocellular, cholestatic or biliary cirrhosis), T1 / 2 lengthened by 50% and the total clearance decreased by 40% (correction of the dosing regimen is required only with a concomitant decrease in GFR).
Indications
- seasonal and perennial allergic rhinitis; - allergic conjunctivitis; - pollinosis (hay fever); - urticaria (including chronic idiopathic); - other allergic dermatosis (including atopic dermatitis and neurodermatitis), accompanied by itching and rashes; - angioedema (angioedema).
Contraindications
- children's age up to 6 months (for drops), due to the limited data on the efficacy and safety of the drug; - children's age up to 6 years (for pills); - pregnancy; - lactation period; - terminal stage of renal failure (CC less than 10 ml / min); - hypersensitivity to cetirizine, hydroxyzine or piperazine derivatives,as well as other components of the drug .; With caution, a drug should be prescribed for chronic renal failure (with CC> 10 ml / min, correction of the dosing regimen is required); patients with predisposing factors for urinary retention; in epilepsy and patients with increased convulsive readiness; elderly patients (with age-related reduction of glomerular filtration); at children's age till 1 year (for drops).
Use during pregnancy and lactation
Experimental studies on animals did not reveal any direct or indirect adverse effects of cetirizine on the developing fetus (including in the postnatal period), the course of pregnancy and childbirth also did not change. Adequate and strictly controlled clinical studies on the safety of the drug during pregnancy have not been conducted, so cetirizine should not be used during pregnancy .; Cetirizine is excreted in breast milk, so the issue of discontinuing breastfeeding for the period of use of the drug should be resolved.
Dosage and administration
The drug is taken orally .; Tablets should be taken regardless of the meal, not chewed and squeezed 200 ml of water .; Adults and children over 6 years old are prescribed in the form of pills in 10 mg (1 tab.) 1 time / day or 5 mg (1/2 tab.) 2 times / day, or in the form of drops - the initial dose is 5 mg 1 times / day (10 drops), if necessary, the dose can be increased to 10 mg (20 drops) 1 time / day. Sometimes an initial dose of 5 mg (10 drops) may be enough to achieve a therapeutic effect .; Children between the ages of 6 months and 12 months are prescribed 2.5 mg (5 drops) 1 time / day; children aged 1 to 2 years old - 2.5 mg (5 drops) up to 2 times / day; children aged 2 to 6 years old - 2.5 mg (5 drops) 2 times / day or 5 mg (10 drops) 1 time / day; Since Cetirizine is excreted mainly by the kidneys, when prescribing the drug in patients with renal insufficiency and in elderly patients, the dose should be adjusted depending on the size of the CC; When QA> 80 ml / min (normal) or 50-79 ml / min (mild renal failure), the drug is prescribed in the usual dosing regimen - 10 mg (1 tab. Or 20 drops) / day. When CC is from 30 to 49 ml / min (average degree of renal failure), the drug is prescribed in 5 mg (1/2 tab. Or 10 drops) of the drug 1 time / day.When CC is from 10 to 29 ml / min (severe stage of renal failure), 5 mg (1/2 tab. Or 10 drops) every other day. With CC less than 10 ml / min (end-stage renal failure), use of the drug is contraindicated .; QC for men can be calculated based on the concentration of serum creatinine, according to the following formula: QC (ml / min) = [140 - age (years)] × body weight (kg) / 72 × KK serum (mg / dl) .; QC for women can be calculated by multiplying the value obtained by a factor of 0.85; With a combination of renal and hepatic insufficiency, the drug is also prescribed in the above regimen .; Patients with impaired liver function and normal renal function do not need to adjust the dosage regimen .; Elderly patients with normal renal function dose adjustment is not required.
Side effects
Possible side effects are listed below for body systems and frequency of occurrence: very often (> 1/10); often (1/10 - 1/100); infrequently (1/100 - 1/1000); rarely (1/1000 - 1/10 000); very rarely (<1/10 000), unknown (impossible to estimate, based on available data) .; On the part of the digestive system: often - dry mouth, nausea; infrequently - diarrhea, abdominal pain .; On the part of the immune system: rarely - hypersensitivity reactions; very rarely - anaphylactic shock .; Of the nervous system: often - headache, fatigue, dizziness, drowsiness; infrequently - paresthesia (violation of sensitivity); rarely seizures; very rarely - dysgeusia, dyskinesia, dystonia, syncope, tremor, tic; unknown - memory impairment, incl. amnesia.; Mental disorders: infrequently - agitation; rarely - aggression, confusion, depression, hallucinations, sleep disturbances; unknown - suicidal ideation .; On the part of the organ of vision: very rarely - accommodation disturbances, blurred vision, nystagmus .; On the part of the organ of hearing and labyrinth disturbances: the frequency is unknown - vertigo .; Since the cardiovascular system: rarely - tachycardia .; On the part of the respiratory system: often - rhinitis, pharyngitis .; On the part of the skin and subcutaneous tissues: infrequently - rash, itching; rarely - urticaria; very rarely - angioedema, persistent erythema .; From the urinary system: very rarely - dysuria, enuresis; unknown - urinary retention .; Other: infrequently - asthenia, malaise; rarely - peripheral edema,weight gain; unknown - increased appetite .; Laboratory and instrumental data: rarely - increased activity of hepatic transaminases, alkaline phosphatase, GGT and bilirubin concentration; very rarely - thrombocytopenia .; If any of the side effects indicated in the instructions are aggravated or any other side effects that are not indicated in the instructions are noted, the patient should inform the physician.
Overdose
Symptoms: a single dose of cetirizine in a dose of 50 mg showed confusion, diarrhea, dizziness, fatigue, headache, indisposition, mydriasis, itching, anxiety, weakness, sedation, drowsiness, stupor, tachycardia, tremor, urinary retention .; Treatment: immediately after taking the drug - gastric lavage or stimulation of vomiting. The use of activated carbon, symptomatic and supportive therapy is recommended. There is no specific antidote. Hemodialysis is ineffective.
Interaction with other drugs
When studying the pharmacokinetic interaction of cetirizine with pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, glipizide, diazepam and antipyrine, no clinically significant undesirable interaction was found .; With simultaneous use with theophylline (400 mg / day), the total clearance of cetirizine is reduced by 16% (the kinetics of theophylline does not change) .; With simultaneous use with ritonavir, the AUC of cetirizine increased by 40%, while the similar indicator of ritonavir slightly changed (-11%) .; The simultaneous use of macrolide antibiotics (azithromycin, erythromycin) and ketoconazole does not lead to changes in the patients' ECG .; At therapeutic doses, cetirizine showed no clinically significant interaction with ethanol (at an ethanol concentration of 0.5 g / l in blood). However, one should refrain from drinking alcohol .; Myelotoxic drugs increase the hematotoxicity of the drug.
special instructions
Patients with spinal cord injury, prostatic hyperplasia, as well as with other predisposing factors for urinary retention, require caution because cetirizine may increase the risk of urinary retention .; Methyl parahydroxybenzoate and propyl parahydroxybenzoate, which are part of the drug in the form of drops, can cause allergic reactions, includingslow type .; The drops do not contain sugar, sucralose is used as a sweetener, which does not affect the content of glucose in the blood serum, therefore Cetrine; in drops can be prescribed to patients with diabetes mellitus .; Before prescribing allergy tests, a three-day wash-out period is recommended due to the fact that inhibitors of histamine H1 receptors (including cetirizine) inhibit the development of allergic skin reactions .; If you exceed the dose of 10 mg / day, the speed of psychomotor reactions may slow down .; Use in pediatrics; Due to the potential inhibitory effect on the central nervous system, care should be taken when prescribing cetirizine in drops to children under 1 year of age with the following risk factors for sudden infant death syndrome (but not limited to this list): - sleep apnea syndrome or sudden infant death in infants with a brother or sister; - mother’s abuse of drugs or tobacco during pregnancy; - The young age of the mother (19 years and younger); - Abuse of tobacco care by a nurse caring for a child (1 pack of cigarettes per day or more); - children who regularly fall asleep face down, which are not placed on their backs; - premature (less than 37 weeks of gestation) or born with underweight (below the 10th percentile of gestational age); - combined use of drugs that have a depressant effect on the central nervous system; Impact on the ability to drive vehicles and control mechanisms; When an objective assessment of the ability to drive vehicles and control mechanisms was not reliably revealed any adverse events when taking the drug in the recommended dose, but during the period of treatment it is advisable to refrain from driving vehicles and other potentially dangerous species activities requiring increased concentration and speed of psychomotor reactions.