Levocetirizine

Levocetirizine
ATC Code R06AE09
Formula C21H25ClN2O3
Molar Mass (g·mol−1) 388,89
Melting Point (°C) 110-115
CAS Number 130018-77-8
PUB Number 1549000
Drugbank ID DB06282

Basics

Levecetirizine is a drug from the group of antihistamines. It belongs to the second generation of H1 antihistamines, which are less sedating than those of the first generation. It is used for allergic reactions such as hay fever, or for skin rashes of unknown cause. Levocetirizine is taken perorally.

From a chemical point of view, levocetirizine is the (R)-enantiomer of the antihistamine cetirizine. Levocetirizine has higher selectivity for the H1 receptor than cetirizine, resulting in a more favorable side effect profile for patients. It was first approved in Europe in the early 2000s.

Pharmacology

Pharmacodynamics

Levocetirizine is a highly selective H1 receptor antagonist. It binds to the H1-receptor, preventing the binding of its endogenous ligand histamine. The failure to bind histamine reduces typical symptoms of allergic reactions.

Pharmacokinetics

Levocetirizine has a very broad therapeutic range and a long duration of action, making once-daily administration sufficient. Plasma protein binding of the substance is about 96%. About 85% of the administered oral dose is excreted unchanged. The remaining 15% is metabolized by the liver to a variety of metabolites and excreted in the urine. The average half-life of levocetirizine is approximately 7 hours.

Drug Interactions

There are no known significant interactions with other drugs.

Toxicity

Adverse effects:

  • Mild drowsiness or fatigue
  • Headache
  • Dry mouth
  • Drowsiness
  • Visual disturbances (mainly blurred vision)
  • Palpitations

Pregnancy and lactation

Use in pregnancy appears to be safe, but is not considered well studied. The safety of use in lactation is unclear.

Toxicological Data

The maximum non-lethal dose in mice and rats is 240mg/kg.

Editorial principles

All information used for the content comes from verified sources (recognised institutions, experts, studies by renowned universities). We attach great importance to the qualification of the authors and the scientific background of the information. Thus, we ensure that our research is based on scientific findings.

Markus Falkenstätter

Markus Falkenstätter
Author

Markus Falkenstätter is a writer on pharmaceutical topics in Medikamio's medical editorial team. He is in the last semester of his pharmacy studies at the University of Vienna and loves scientific work in the field of natural sciences.

Mag. pharm Stefanie Lehenauer

Mag. pharm Stefanie Lehenauer
Lector

Stefanie Lehenauer has been a freelance writer for Medikamio since 2020 and studied pharmacy at the University of Vienna. She works as a pharmacist in Vienna and her passion is herbal medicines and their effects.

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