Cetirizine

Cetirizine
ATC Code R06AE07
Formula C21H25ClN2O3
Molar Mass (g·mol−1) 388,89
Physical State solid
Melting Point (°C) 110–115
Boiling Point (°C) 542.1
PKS Value 1.52; 2.92; 8.27
CAS Number 83881-51-0
PUB Number 2678
Drugbank ID DB00341
Solubility schlecht löslich in Wasser

Grundlagen

Cetirizine is a selective histamine antagonist and is used in allergic rhinitis and chronic urticaria. It belongs to the second-generation antihistamines.

Indications and use

Cetirizine is an orally active second-generation histamine H1 antagonist effective in the treatment of various allergic symptoms such as sneezing, cough, nasal congestion, and hives. One of the most common uses of this medication is in the treatment of hay fever (allergic rhinitis). However, cetirizine can also be used for symptomatic treatment of other allergic reactions.

Cetirizine is usually administered in the form of film-coated tablets. However, there are also formulations i.e. drops or oral solutions. Dosages are usually 10 mg film-coated tablets and 10 mg/ml or 1 mg/ml as drops and solution.

History

It was patented by USB Pharmaceuticals in 1981 and was first approved in 1987. It is on the World Health Organization's list of essential medicines and is available as a generic.

Pharmakologie

Pharmacodynamics and mechanism of action

The main action of cetirizine is achieved through its highly selective inhibition of peripheralH1 receptors. By binding and inhibiting these receptors, it minimizes or eliminates symptoms caused by histamine release, such as sneezing, itching, watery eyes, and runny nose. Cetirizine is not or minimally CNS-responsive, so it is not expected to cause central side effects such as sedation or drowsiness.

Cetirizine also exhibits anti-inflammatory properties independent ofH1 receptors. The effect is achieved by probably suppressing the NF-κB pathway and regulating the release of cytokines and chemokines, thereby regulating the recruitment of inflammatory cells. This mechanism is currently the subject of various investigations, but it is not yet relevant for therapeutic application.

Pharmacokinetics

Cetirizine is rapidly absorbed after oral administration. The time to maximum concentration (Tmax) is approximately 1 hour. Food intake has no effect on blood cetirizine concentrations, but Tmax is delayed by approximately 1 hour. The mean plasma protein binding of cetirizine is 93%. Approximately 50% of the dose is excreted in the urine as unchanged cetirizine. Cetirizine is metabolized primarily by oxidative O-dealkylation. The enzyme or enzymes responsible for this step of cetirizine metabolism have not yet been identified. Between 70-85% of the orally administered dose is excreted in the urine and 10-13% in the feces. The plasma elimination half-life is approximately 8 hours.

Drug Interactions

Since cetirizine, unlike many other drugs, is not degraded via the CYP450 enzyme system, the risk for serious interactions is relatively low.

Toxizität

Contraindications

Cetirizine should not be taken if:

  • there is a known allergy to the active substance
  • severe renal impairment exists (creatinine clearance < 10 mL/min)

Side effects

Common side effects of cetirizine include:

  • dizziness
  • drowsiness
  • drowsiness
  • dry mouth
  • sore throat
  • coughing
  • nausea
  • diarrhea
  • constipation
  • Headache
  • Restlessness
  • Paresthesia

Pregnancy and breast-feeding

The use of cetirizine is not expected to harm the fetus, but because of limited data on safety during pregnancy, use should be avoided or used only when directed by a health care professional.

Cetirizine can pass into breast milk and may cause adverse reactions in the nursing infant. Therefore, its use is strongly discouraged during breast-feeding.

Markus Falkenstätter

Markus Falkenstätter
Author

Markus Falkenstätter ist Autor zu pharmazeutischen Themen in der Medizin-Redaktion von Medikamio. Er befindet sich im letzten Semester seines Pharmaziestudiums an der Universität Wien und liebt das wissenschaftliche Arbeiten im Bereich der Naturwissenschaften.

Mag. pharm Stefanie Lehenauer

Mag. pharm Stefanie Lehenauer
Lector

Stefanie Lehenauer ist seit 2020 freie Autorin bei Medikamio und studierte Pharmazie an der Universität Wien. Sie arbeitet als Apothekerin in Wien und ihre Leidenschaft sind pflanzliche Arzneimittel und deren Wirkung.

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The contents shown do not replace the original package insert of the medicinal product, especially with regard to dosage and effect of the individual products. We cannot assume any liability for the correctness of the data, as the data was partly converted automatically. A doctor should always be consulted for diagnoses and other health questions. Further information on this topic can be found here.