Desloratadine

Desloratadine

Desloratadine
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
MedlinePlus
Licence data EMA:, US FDA:
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 Liver
Biological half-life 27 hours
Excretion 40% as conjugated metabolites into urine
Similar amount into the feces
Identifiers
CAS Registry Number  Y
ATC code R06
PubChem CID:
IUPHAR/BPS
DrugBank  Y
ChemSpider  Y
UNII  Y
KEGG  Y
ChEBI  Y
ChEMBL  Y
Chemical data
Formula C19H19ClN2
Molecular mass 310.82
 Y   

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

Contents

  • Use 1
  • Side effects 2
  • Mechanism of action 3
  • Society and culture 4
  • References 5

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]

References

  1. ^ a b c See S (2003). "Desloratadine for allergic rhinitis". Am Fam Physician 68 (10): 2015–6.  
  2. ^ Canonica GW, Blaiss M (2011). "Antihistaminic, anti-inflammatory, and antiallergic properties of the nonsedating second-generation antihistamine desloratadine: a review of the evidence". World Allergy Organ J 4 (2): 47–53.  
  3. ^ Mann R, Pearce G, Dunn N, Shakir S (2000). "Sedation with "non-sedating" antihistamines: four prescription-event monitoring studies in general practice". BMJ 320 (7243): 1184–6.  
  4. ^ Drugs.com Desloratadine entry at drugs.com international Page accessed May 4, 2015