Desloratadine

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Desloratadine
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222px
Systematic (IUPAC) name
8-chloro-6,11-dihydro-11-(4-piperdinylidene)- 5H-benzo[5,6]cyclohepta[1,2-b]pyridine
Clinical data
Trade names Clarinex
AHFS/Drugs.com monograph
MedlinePlus a602002
Licence data EMA:Link, US FDA:link
Pregnancy
category
  • AU: B1
  • US: C (Risk not ruled out)
Legal status
Routes of
administration
Oral
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
CAS Number 100643-71-8 YesY
ATC code R06AX27 (WHO)
PubChem CID: 124087
IUPHAR/BPS 7157
DrugBank DB00967 YesY
ChemSpider 110575 YesY
UNII FVF865388R YesY
KEGG D03693 YesY
ChEBI CHEBI:291342 YesY
ChEMBL CHEMBL1172 YesY
Chemical data
Formula C19H19ClN2
Molecular mass 310.82
  • Clc4cc2c(C(/c1ncccc1CC2)=C3/CCNCC3)cc4
  • 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 YesY
  • Key:JAUOIFJMECXRGI-UHFFFAOYSA-N YesY
  (verify)

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

Use

Desloratadine is used to treat allergic rhinitis and nasal congestion.[1] It is the major metabolite of loratadine and the two drugs are similar in safety and effectiveness.[1]

Side effects

Most common side-effects are fatigue, dry mouth, headache, and gastrointestinal disturbances.[1]

Mechanism of action

Desloratadine is a selective H1-antihistamine which functions as an inverse agonist at the histamine H1 receptor;[2] it is also an antagonist at all subtypes of the muscarinic acetylcholine receptors. It has a long-lasting effect and in moderate and low doses. 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.[3]

Society and culture

Desloratadine is available in many dosage forms and under many trade names worldwide.[4]

See also

References

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  4. Drugs.com Desloratadine entry at drugs.com international Page accessed May 4, 2015