Desloratadine

Desloratadine

Clinical data
Trade names	Clarinex
AHFS/Drugs.com	Monograph
MedlinePlus	a602002
License data	EU EMA: Aerius US FDA: Desloratadine
Pregnancy category	AU: B1 US: C (Risk not ruled out)
Routes of administration	Oral
ATC code	R06AX27 (WHO)
Legal status
Legal status	AU: S2 (Pharmacy only) CA: OTC UK: POM (Prescription only) US: ℞-only
Pharmacokinetic data
Bioavailability	Rapidly absorbed
Protein binding	85%
Metabolism	Hepatic
Biological half-life	27 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 Y
PubChem CID	124087
IUPHAR/BPS	7157
DrugBank	DB00967 Y
ChemSpider	110575 Y
UNII	FVF865388R
KEGG	D03693 Y
ChEBI	CHEBI:291342 Y
ChEMBL	CHEMBL1172 Y
ECHA InfoCard	100.166.554
Chemical and physical data
Formula	C19H19ClN2
Molar mass	310.82
3D model (Jmol)	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 Y Key:JAUOIFJMECXRGI-UHFFFAOYSA-N Y

Desloratadine is a tricyclic H₁-antihistamine that is used to treat allergies. It is an active metabolite of loratadine.

Desloratadine is used to treat allergic rhinitis and nasal congestion. It is the major metabolite of loratadine and the two drugs are similar in safety and effectiveness. Desloratadine is available in many dosage forms and under many trade names worldwide.

An emerging indication for desloratadine is in the treatment of acne, as an inexpensive adjuvant to isotretinoin and possibly as maintenance therapy or monotherapy.

Most common side-effects are fatigue, dry mouth, headache, and gastrointestinal disturbances.

Desloratadine is a selective H₁-antihistamine which functions as an inverse agonist at the histamine H₁ receptor;

It is also an antagonist at all subtypes of the muscarinic acetylcholine receptors.

It exhibits only peripheral activity since it does not readily cross the blood-brain barrier; hence, it does not cause drowsiness because it does not readily enter the central nervous system.

It has a long-lasting effect and is effective in moderate and low doses.