Desloratadine
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| 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 | |
| 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  |
| ATC code | R06AX27 |
| PubChem | CID 124087 |
| IUPHAR/BPS | 7157 |
| DrugBank |
DB00967 |
| ChemSpider |
110575 |
| UNII |
FVF865388R |
| KEGG |
D03693 |
| ChEBI |
CHEBI:291342 |
| ChEMBL |
CHEMBL1172 |
| Chemical data | |
| Formula | C19H19ClN2 |
| Molar mass | 310.82 |
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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
- 1 2 3 See S (2003). "Desloratadine for allergic rhinitis". Am Fam Physician 68 (10): 2015–6. PMID 14655812.
- ↑ 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. doi:10.1097/WOX.0b013e3182093e19. PMC 3500039. PMID 23268457.
- ↑ 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. doi:10.1136/bmj.320.7243.1184. PMC 27362. PMID 10784544.
- ↑ Drugs.com Desloratadine entry at drugs.com international Page accessed May 4, 2015
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