Desloratadine

Desloratadine
Clinical data
Trade names	Aerius, others
Other names	Descarboethoxyloratadine
AHFS/Drugs.com	Monograph
MedlinePlus	a602002
License data	US DailyMed: Desloratadine;
Pregnancy; category	AU: B1;
Routes of; administration	By mouth
Drug class	Second-generation antihistamine
ATC code	R06AX27 (WHO) ;
Legal status
Legal status	AU: S2 (Pharmacy medicine); CA: OTC; UK: POM (Prescription only); US: ℞-only; EU: Rx-only / OTC;
Pharmacokinetic data
Bioavailability	Rapidly absorbed
Protein binding	83–87%
Metabolism	UGT2B10, CYP2C8
Metabolites	3-Hydroxydesloratadine
Onset of action	within 1 hour
Elimination half-life	27 hours, 33.7 hours in elderly patients
Duration of action	up to 24 hours
Excretion	40% as conjugated metabolites into urine; Similar amount into the feces
Identifiers
	IUPAC name 8-chloro-6,11-dihydro-11-(4-piperdinylidene)- 5H-benzo[5,6]cyclohepta[1,2-b]pyridine;
CAS Number	100643-71-8 ;
PubChem CID	124087;
IUPHAR/BPS	7157;
DrugBank	DB00967 ;
ChemSpider	110575 ;
UNII	FVF865388R;
KEGG	D03693 ;
ChEBI	CHEBI:291342 ;
ChEMBL	ChEMBL1172 ;
CompTox Dashboard (EPA)	DTXSID1044196 ;
ECHA InfoCard	100.166.554
Chemical and physical data
Formula	C19H19ClN2
Molar mass	310.83 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES Clc4cc2c(C(/c1ncccc1CC2)=C3/CCNCC3)cc4;
	InChI InChI=1S/C19H19ClN2/c20-16-5-6-17-15(12-16)4-3-14-2-1-9-22-19(14)18(17)13-7-10-21-11-8-13/h1-2,5-6,9,12,21H,3-4,7-8,10-11H2 ; Key:JAUOIFJMECXRGI-UHFFFAOYSA-N ;
	(verify)

Desloratadine, sold under the brand name Aerius among others, is a tricyclic H₁ inverse agonist that is used to treat allergies. It is the major active metabolite of loratadine.

It was patented in 1984 and came into medical use in 2001.^[8] It was brought to the market in the US by Schering Corporation, later named Schering-Plough.^[3]

^ Murdoch D, Goa KL, Keam SJ (7 April 2003). "Desloratadine: an update of its efficacy in the management of allergic disorders". Drugs. 63 (19): 2051–2077. doi:10.2165/00003495-200363190-00010. PMID 12962522. S2CID 195689362.
^ Schering Corporation (2000). "CLARITIN brand of Loratadine - Full Prescribing Information (US FDA)" (PDF). US FDA. Retrieved 17 May 2024. loratadine is metabolized to descarboethoxyloratadine predominantly by cytochrome P450 3A4 (CYP3A4) and, to a lesser extent, by cytochrome P450 2D6 (CYP2D6).
^ ^a ^b ^c "Clarinex- desloratadine tablet, film coated". DailyMed. 14 November 2022. Retrieved 18 May 2024.
^ "Clarinex-D 12 HOUR- desloratadine and pseudoephedrine sulfate tablet, extended release". DailyMed. 14 November 2022. Retrieved 18 May 2024.
^ "Desloratadine ratiopharm EPAR". European Medicines Agency (EMA). 13 January 2012. Retrieved 23 March 2025.
^ "Neoclarityn EPAR". European Medicines Agency (EMA). 15 January 2001. Retrieved 23 March 2025.
^ "Aerius EPAR". European Medicines Agency (EMA). 15 January 2001. Retrieved 24 March 2025.
^ Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 549. ISBN 9783527607495.

[murdoch-1] Murdoch D, Goa KL, Keam SJ (7 April 2003). "Desloratadine: an update of its efficacy in the management of allergic disorders". Drugs. 63 (19): 2051–2077. doi:10.2165/00003495-200363190-00010. PMID 12962522. S2CID 195689362.

[loratadine-fda-2000-2] Schering Corporation (2000). "CLARITIN brand of Loratadine - Full Prescribing Information (US FDA)" (PDF). US FDA. Retrieved 17 May 2024. loratadine is metabolized to descarboethoxyloratadine predominantly by cytochrome P450 3A4 (CYP3A4) and, to a lesser extent, by cytochrome P450 2D6 (CYP2D6).

[Clarinex_FDA_label-3] "Clarinex- desloratadine tablet, film coated". DailyMed. 14 November 2022. Retrieved 18 May 2024.

[4] "Clarinex-D 12 HOUR- desloratadine and pseudoephedrine sulfate tablet, extended release". DailyMed. 14 November 2022. Retrieved 18 May 2024.

[Desloratadine_ratiopharm_EPAR-5] "Desloratadine ratiopharm EPAR". European Medicines Agency (EMA). 13 January 2012. Retrieved 23 March 2025.

[Neoclarityn_EPAR-6] "Neoclarityn EPAR". European Medicines Agency (EMA). 15 January 2001. Retrieved 23 March 2025.

[7] "Aerius EPAR". European Medicines Agency (EMA). 15 January 2001. Retrieved 24 March 2025.

[Fis2006-8] Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 549. ISBN 9783527607495.

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