Desloratadine

Structural formula
General
Non-proprietary name	Desloratadine
other names	8-chloro-11- (piperidin-4-ylidene) -5,6-dihydro-11 H -benzo [5,6] cyclohepta [1,2-b] pyridine ( IUPAC )
Molecular formula	C 19 H 19 ClN 2
External identifiers / databases
CAS number 100643-71-8 EC number 638-878-8 ECHA InfoCard 100.166.554 PubChem 124087 DrugBank DB00967 Wikidata Q418060
Drug information
ATC code	R06 AX27
Drug class	Antihistamine
Mechanism of action	Antihistamine
properties
Molar mass	310.82 g · mol -1
safety instructions
Please note the exemption from the labeling requirement for drugs, medical devices, cosmetics, food and animal feed GHS labeling of hazardous substances H and P phrases H: 302-318-361-411 P: ?
As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Desloratadine is a drug from the group of antihistamines that is used to treat allergic rhinitis and chronic urticaria . Desloratadine is a derivative and metabolite of the antihistamine loratadine and was brought onto the market by the pharmaceutical company Essex Pharma when the patent protection for loratadine expired. Desloratadine was subject to medical prescription in Germany until February 21, 2020 , when it was switched to OTC. Tablets approved outside of Germany require a prescription.

Mechanism of action

The mechanism of action of desloratadine corresponds to that of loratadine; as an H ₁ antihistamine, it blocks the special binding sites for histamine , the histamine H ₁ receptors , and thus inhibits the effects of histamine (e.g. reddening of the skin, itching, drop in blood pressure and bronchospasm ); Desloratadine also stabilizes mast cells , blocking the release of histamine. Desloratadine also acts as a FIASMA (functional inhibitor of acid sphingomyelinase ).

Comparison with loratadine

In contrast to loratadine, desloratadine has a three to four times higher affinity for the H ₁ receptor . Loratadine can therefore be formally regarded as a prodrug of desloratadine. In addition, desloratadine has a longer plasma half-life . Both substances have the property that they are transported back through permeable glycoproteins at the blood-brain barrier , so that both loratadine and desloratadine only reach the central nervous system to a limited extent and there are fewer side effects such as e.g. B. Can cause sedation . They therefore both belong to the second generation antihistamines .

A therapeutic advantage of desloratadine is classified as marginal, since loratadine is also almost completely converted into desloratadine in the liver. The temporal proximity between the loss of patent protection for loratadine and the market launch of desloratadine suggests that this was also a reason for its introduction.

Trade names

Monopreparations

Aerius (D, A, CH, I, BG), Dasselta (D, A), Azomyr (A), Neoclarityn (A), LoranoPro (D)

Combination preparations

Aerinaze (A)

Web links

• Pharmaceutical Newspaper
• Public Assessment Report (EPAR) of the European Medicines Agency (EMA) for: Desloratadine

Individual evidence

1. ↑ There is not yet a harmonized classification for this substance . A labeling of 13-chloro-2- (piperidin-4-ylidene) -4-azatricyclo [9.4.0.0³, ⁸] pentadeca-1 (15), 3,5,7,11 is shown, which is derived from a self-classification by the distributor , 13-hexaene in the Classification and Labeling Inventory of the European Chemicals Agency (ECHA), accessed on January 15, 2020.
2. ↑ Chronic idiopathic urticaria: Desloratadine stops itchy wheals , www.deutsche-apotheker-zeitung.de, November 17, 2002.
3. ↑ Entire legal regulation for prescription regulation . Federal legal information system. October 23, 2014. Retrieved April 12, 2016.
4. ^ Ordinance on the prescription requirement for medicinal products . Federal Ministry of Justice and Consumer Protection & juris GmbH. November 30, 2015. Retrieved April 12, 2016.
5. ↑ Kornhuber J, Muehlbacher M, Trapp S, Pechmann S, Friedl A, Reichel M, Mühle C, Terfloth L, Groemer T, Spitzer G, Liedl K, Gulbins E, Tripal P: Identification of novel functional inhibitors of acid sphingomyelinase . In: PLoS ONE . 6, No. 8, 2011, p. E23852. doi : 10.1371 / journal.pone.0023852 .
6. ↑ https://www.ncbi.nlm.nih.gov/pubmed/?term=P-GLYCOPROTEIN+LIMITS+THE+BRAIN+PENETRATION+OF+NONSEDATING+BUT+NOT+SEDATING+H1-ANTAGONISTS
7. ^ Ulrich Schwabe, Dieter Paffrath: Drug Ordinance Report 2004: Current data, costs, trends and comments . Springer, 2004, ISBN 3540213597 .
8. ↑ Antje-Christina Raasch: Strategy and success factors when the patent expiry of the antihistamine Lisino from essex pharma . In: The patent expiry of pharmaceuticals as a challenge in the management of the product life cycle . Springer, 2006, ISBN 978-3-8350-0632-4 , pp. 211-225.
9. ↑ Red List Online, as of August 2009.
10. ↑ AM comp. d. Switzerland, as of August 2009.
11. ↑ AGES-PharmMed, as of August 2009.

This article is about a health issue. It is not used for self-diagnosis and does not replace a diagnosis by a doctor. Please note the information on health issues !