Last Updated on February 19, 2017 by Dr.Derek Fhisher
Most popular brand: Zyrtec
Active ingredient: Cetirizine
Available dosage forms: 5, 10 mg
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Cetirizine general information
Cetirizine is also used when treating hives. Take cetirizine tablets orally. Cetirizine 10 mg is, in addition, the very best treatment for hay fever. Generic Cetirizine can likewise be used to ease the symptoms of the condition called chronic idiopathic urticaria.
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Active – active substance / start: cetirizine
Alerza; Allertek; Analergin; Zetrinal; Zintset; Zyrtec; Zodak; Letizen S; Cetirizine; Parlazin; Cetirizine hydrochloride; Tsetirinaks; Tsetrin.
Cetirizine – blocker of peripheral histamine H1 – receptors protvoallergicheskoe antihistamine agent. It does not have a significant sedative effect. It is used for treatment of allergic rhinitis, conjunctivitis, urticaria, atopic dermatitis, bronchial asthma in adults and children older than 2 years.
Active – active substance:
cetirizine hydrochloride / cetirizine / Cetirizine.
Dosage Forms:
Tablets.
Drops for intake.
Cetirizine
Properties / Action:
Cetirizine – blocker of peripheral histamine H1 – receptors protvoallergicheskoe antihistamine agent, a metabolite of hydroxyzine as well. The pharmacologically active doses has no significant sedative effect.
Cetirizine inhibits gistaminoposredovannuyu early phase of the allergic reaction, prevent various physiological and pathophysiological effects of histamine, such as expansion and increased capillary permeability (edema, urticaria, flushing), stimulation of the sensory nerve endings (itching, pain) and smooth muscle organs respiratory and gastro – intestinal tract.
At a late stage of an allergic reaction Cetirizine inhibits histamine release and migration of eosinophils and other cells, thus weakening, late allergic reactions. It reduces the expression of adhesion molecules such as ICAM – 1 and VCAM – 1, which are markers of allergic inflammation. It inhibits the action of neurotransmitters, and other inducers of histamine release, such as PAF (platelet – activating factor) and substance P.
Cetirizine significantly reduces the hyperreactivity of the bronchial tree, occurs in response to the release of histamine in patients with bronchial asthma. These effects of cetirizine is not accompanied by central action, which is confirmed by psychometric tests and EEG data.
Cetirizine inhibits cutaneous reactions in patients with cold urticaria and dermographism.
Cetirizine – selective antagonist of the H1 – receptors and devoid of much – any significant anticholinergic and antiserotoninovogo action.
six-week study involving 168 patients with allergic rhinitis in conjunction with mild to moderate asthma demonstrated the efficacy of cetirizine 10 mg in rhinitis and demonstrated safety of cetirizine in patients with allergic rhinitis and asthma mild to moderate severity.
The use of Cetirizine in therapeutic doses of 10 mg / day improved the quality of life of patients with perennial and seasonal allergic rhinitis. Purpose
cetirizine high dose exceeding 6 times daily therapeutic dose (60 mg / day) and placebo as control for 7 days showed no elongation QT interval on an electrocardiogram.
The action of cetirizine begins 20 minutes after taking the drug, an antihistamine maximum effect is achieved within 1 hour.
The action of cetirizine usually lasts for 24 hours, so it is enough to take the drug once a day. The skin recovers its normal reactivity to histamine within 3 days after discontinuation.
There were no tolerance to its antihistamine effect.
Pharmacokinetics:
Cetirizine is rapidly absorbed from the gastro – intestinal tract, its absorption is 70%. The drug with food does not affect the absorption, but the absorption rate is somewhat reduced. Cetirizine largely associated transport proteins in blood plasma. Cetirizine does not penetrate the blood-brain barrier. The maximum drug concentration in plasma (0.3 mg / ml) is achieved between the thirtieth and sixty minutes after administration of cetirizine 10 mg. In adults, the plasma half-life of approximately 10 hours in children 6 to 12 years – 6 hours and 2 to 5 years – 5 hours. If the kidney function decreases total clearance of cetirizine. Cetirizine is practically not metabolized in the liver. Two-thirds of the dose of the drug is excreted unchanged in the urine. The use of Cetirizine 10 mg / day did not result in accumulation of cetirizine.
In patients with impaired renal function decreases systemic clearance of cetirizine. When CC is higher than 40 ml / min pharmacokinetic properties of the drug did not differ from that of healthy volunteers. In patients with moderately impaired renal function T1 / 2 of cetirizine was increased 3-fold and clearance decreased by 70%. Patients on hemodialysis (creatinine clearance less than 7 ml / min), while taking cetirizine at a dose of 10 mg of T1 / 2 of the drug was increased 3-fold and clearance decreased by 70%.
In patients with chronic diseases of the liver (hepatocellular, and cholestatic biliary cirrhosis) when taking 10 – 20 mg elongation observed T1 / 2 cetirizine 50%, while the clearance was reduced by 40%.
Indications:
Symptomatic therapy of adults and children over 2 years old:
Dosage and administration:
Inside. Take before or after a meal, washed down with a small amount of liquid. Cetirizine should be taken regularly at the same time. Time dosing (morning or evening) is determined depending on the individual patient’s needs. Cetirizine causes drowsiness in some patients, so that patients are advised to take the drug in the evening.
Children 2 to 6 years: 5 mg daily (10 drops) once or 5 drops morning and evening.
children 6 to 12 years: 10 mg per day (1 tablet or 20 drops per day), once, 2.1 or 2 tablets twice a day, morning and evening.
Vzrooslye and children 12 years and older: 10 mg per day (1 tablet or 20 drops) once.
There is currently no data indicating the need to reduce the dose in elderly patients with normal renal function.
Patients with moderate renal impairment (creatinine clearance 11 -. 13 ml / min) and in patients on hemodialysis (. creatinine clearance less than 7 ml / min) and in patients with impaired hepatic function is recommended to appoint 1/2 tablet per day.
If the patient has forgotten to take the pill at a certain time, you should take it as soon as possible. If there is only a few hours before the next dose, skip the previous dose and take only the dose corresponding to the scheme.
The duration of treatment is determined by your doctor.
Overdose:
The main initial signs of overdose are usually agitation and irritability, followed by drowsiness occurs. There may be itching, rash, urinary retention, tachycardia and tremor.
After receiving too many tablets you need to call a doctor. Before arrival of the doctor should try to induce vomiting in a patient, if he is conscious, to remove the drug from the stomach. Further measures will be taken by your doctor.
Just when overdose recommended gastric lavage, the appointment of activated charcoal and laxatives, as well as to monitor the functions of the cardiovascular and respiratory systems. If necessary spend symptomatic therapy.
Hemodialysis is ineffective. There is no specific antidote.
Contraindications:
Cetirizine is contraindicated in persons with a history data on the presence of a hypersensitivity reaction to any component of the drug, as well as to hydroxyzine.
Pregnancy, breast-feeding, child up to 2 years (up to 6 years with impaired renal or hepatic function).
Use during pregnancy and lactation:
contraindicated. Data regarding adverse effects on the fetus are not available, but the risk can not be completely excluded. Therefore Cetirizine should not be taken during the first trimester of pregnancy. In the later stages of pregnancy, the drug is prescribed only under strict indications. Cetirizine passes into breast milk, so the period of treatment to interrupt breast-feeding.
Side effects:
Cetirizine is generally well tolerated. The majority of side effects during treatment with cetirizine had mild or moderate severity.
The objective study of psychomotor functions have shown that the incidence of sedation, occurring when receiving cetirizine, no different from its frequency with placebo.
There are reports of poorly expressed and quickly pass reactions include headache, dizziness, drowsiness, fatigue, feelings of dryness in the mouth, excitement, gastro – intestinal disorders.
Less marked weakness, nausea, vomiting, abdominal pain, diarrhea, constipation and increased appetite.
During treatment with cetirizine may experience a transient increase in liver transaminases (in less than 1.5% of patients). Also, there may be hemolytic anemia or thrombocytopenia.
Hypersensitivity reactions such as skin reactions and vascular edema are very rare.
Special instructions and precautions:
It is necessary to be careful and to take smaller doses of the drug in patients with renal insufficiency of moderate severity, patients on hemodialysis, and patients with impaired hepatic function.
Cetirizine appears slower in the elderly than in younger people, so sometimes it takes some adjustment of the dose for patients over the elderly.
Although therapeutic doses (at a concentration of drug in blood plasma of 0.8 g / l) cetirizine does not potentiate the effects of alcohol, however when co-administered with caution.
sometimes recommended control hemogram and liver transaminase activity, especially in the case of jaundice or bruising and / or bleeding. If necessary, interrupt treatment.
The efficacy and safety of cetirizine for children under the age of 2 years has not been established.
Effects on ability to drive vehicles and management mechanisms:
The objective methods of studying potentially hazardous activities management capabilities significantly have not revealed any – any adverse events in the appointment of the recommended dose of 10 mg. However, patients should be advised not to exceed the prescribed dose while driving or working on the machines and to use caution.
The impact of the drug on psychomotor reaction may be enhanced by the simultaneous intake of alcohol or sedatives.
Drug Interactions:
So far, information about possible interactions with other drugs cetirizine received. According to these studies, either diazepam or cimetidine did not interact with cetirizine.
When concomitant administration of cetirizine and theophylline as well (especially if doses higher than 400 mg of theophylline) may experience an increase in serum concentrations and relative overdose of cetirizine – the reduced clearance.
Compatible with azithromycin th, psevdoepinefrinom, ketoconazole om, om erythromycin, cimetidine and diazepam.
Storage:
Store in a dry place at room temperature 15 – 25 ° C.
Do not take the medication after the expiration date printed on the package.
Terms of pharmacy holiday – without a prescription.
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