Pharmacodynamics:
Cetirizine has a pronounced anti-allergic effect. It has practically no sedative effect in pharmacologically active doses, belongs to selective antagonists of H1-histamine receptors and has practically no anticholinergic and antiserotonin action, prevents development and facilitates allergic reactions.
It has an antipruritic and antiexudative effect. It affects the early stage of allergic reactions and also reduces migration of inflammatory cells; it inhibits the release of mediators involved in late allergic reactions.
Limits capillary permeability, prevents the development of tissue edema, relieves smooth muscle spasm. It eliminates the skin reaction to the introduction of histamine, specific allergens and also to cooling (in case of cold urticaria).
Cetirizine significantly reduces bronchial hyperresponsiveness arising in response to histamine release in patients with bronchial asthma. The therapeutic effect of the drug is manifested on average 60 minutes after intake. Tolerance does not develop during a course of administration.
Pharmacokinetics:
Intake: After oral administration cetirizine is quickly and well absorbed from the gastrointestinal tract. The maximum level of concentration is determined after about 40 – 60 minutes.
Food intake has no significant effect on the amount of absorption, but in this case the absorption rate is slightly reduced.
Distribution: Cetirizine binds with blood plasma proteins by about 93%. Volume of distribution (Vd) is low (0.5 l/kg), the drug does not penetrate into cells.
The drug does not penetrate through the blood-brain barrier.
Metabolism: cetirizine is slightly metabolized in liver with formation of inactive metabolite.
When administered in 10-day dose of 10 mg there is no accumulation of preparation.
Elimation: approximately 70% of drug is kidney-acquired mostly unchanged.
Systemic clearance is approximately 54 ml/min.
After a single single single dose the half-life is about 10 hours. In children aged 2 to 12 years, the half-life is reduced to 5-6 hours.
In patients with impaired renal function (creatinine clearance less than 11-31 ml/min) and in patients on hemodialysis (creatinine clearance less than 7 ml/min) the value of half-life is increased by 3 times, clearance is decreased by 70%.
In chronically ill and elderly patients half-life increases by 50% and clearance decreases by 40%.
Hemodialysis is ineffective.
Indications
Active ingredient
How to take, the dosage
Over the body, regardless of meals, without chewing and drinking plenty of liquid, preferably in the evening.
In children aged 6 to 12 years:
It is possible to take 2 times a day (morning and evening) of ½ tablet.
Adults and adolescents over 12 years of age are recommended to take 1 tablet of cetirizine, preferably in the evening.
In case of renal insufficiency, the recommended dose should be reduced by half.
If liver function is impaired, the dose should be adjusted individually, especially with caution in concomitant renal failure.
Elderly patients with normal renal function do not need dose adjustments.
In seasonal allergic rhinitis the duration of therapy is usually from 3 to 6 weeks, and if the pollen exposure is transient, one week is usually sufficient.
The duration of therapy for children over the age of 6 years is 2 to 4 weeks, and with short-term exposure to the allergen one week is sufficient.
Interaction
No clinically significant interactions of cetirizine with other medicinal products have been established.
The co-administration with theophylline (400 mg/day) leads to decreased total clearance of cetirizine (the kinetics of theophylline is not changed).
Special Instructions
At the time of treatment it is necessary to refrain from potentially dangerous activities requiring increased concentration and quick psychomotor reactions.
The concomitant use of drugs that depress the central nervous system and alcohol is not recommended.
Persons with diabetes:
1 tablet corresponds to less than 0.01 bread units.
Contraindications
With caution: moderate to severe chronic pyelonephritis (dosage regimen adjustment is required), advanced age (decrease of glomerular filtration is possible).
Side effects
Digestive system disorders: dry mouth, dyspepsia.
CNS disorders: headache, drowsiness, fatigue, dizziness, agitation, migraine.
Allergic reactions: skin rash, angioedema, urticaria, itching.
The drug is usually well tolerated. Side effects are rare and transient.
Overdose
Symptoms: drowsiness, lethargy, weakness, headache, tachycardia, increased irritability, urinary retention, fatigue are possible (most often when taking 50 mg of cetirizine daily).
Treatment: symptomatic therapy is carried out. No specific antidote has been identified. Hemodialysis is ineffective. Gastric lavage is performed, activated charcoal is prescribed.
Similarities
Weight | 0.030 kg |
---|---|
Shelf life | 3 years |
Conditions of storage | At a temperature not exceeding 25 °C |
Manufacturer | Salutas Pharma GmbH, Germany |
Medication form | pills |
Brand | Salutas Pharma GmbH |
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