Desloratadine

Desloratadine
ATC Code R06AX27
Formula C19H19ClN2
Molar Mass (g·mol−1) 310,82
Physical State solid
CAS Number 100643-71-8
PUB Number 124087
Drugbank ID DB00967
Solubility practically insoluble in water

Basics

Desloratadine is a second-generation tricyclic antihistamine that has a selective and peripheral H1-antagonistic effect. It is the active descarboethoxy metabolite of loratidine. It is used for the treatment of allergic reactions. Desloratidine has a long-lasting effect and does not cause drowsiness because it does not cross the blood-brain barrier. It was patented in 1984 and has been used in medicine since 2001.

Pharmacology

Pharmacodynamics

Like other H1 blockers, desloratadine competes with free histamine for binding to H1 receptors in the GI tract, uterus, major blood vessels, and bronchial smooth muscle. This blocks the action of endogenous histamine, which subsequently results in temporary relief of negative symptoms caused by histamine (e.g., stuffy nose, watery eyes).

Pharmacokinetics

Desloratadine is well absorbed from the intestine and reaches peak blood plasma concentrations after approximately three hours. In the bloodstream, 83 to 87% of the substance is bound to plasma proteins. Desloratadine is metabolized to the active metabolite 3-hydroxydesloratadine, which is subsequently glucuronidated and excreted in equal amounts in urine and feces.

Drug Interactions

The potential for drug-drug interactions with desloratadine is considered to be very low. No relevant drug interactions are known to date.

Toxicity

Side effects

The most common side effects are

  • tiredness
  • Dry mouth
  • Headache

Toxicological Data

In animal studies, an oral LD50 was observed at or above doses of 250 mg/kg in rats. This is approximately 120 times a normal therapeutic dose for humans. Therefore, the use of desloratadine is considered to be markedly safe.

Sources

  • Aktories, Förstermann, Hofmann, Starke: Allgemeine und spezielle Pharmakologie und Toxikologie, Elsvier, 2017
  • Drugbank
  • PubChem

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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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