Desloratadine
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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 | |
| Identifiers | |
| CAS number | 100643-71-8 |
| ATC code | R06AX27 |
| PubChem | 124087 |
| DrugBank | APRD00324 |
| Chemical data | |
| Formula | C19H19ClN2 |
| Mol. weight | 310.82 |
| Pharmacokinetic data | |
| Bioavailability | rapidly absorbed |
| Protein binding | 85% |
| Metabolism | Liver |
| Half life | 50 hours |
| Excretion | 40% as conjugated metabolites into urine similar amount into the feces |
| Therapeutic considerations | |
| Licence data | |
| Pregnancy cat. | |
| Legal status |
POM(UK) |
| Routes | oral |
Desloratadine is a drug used to treat allergies. It is marketed under several trade names such as NeoClarityn®, Claramax®, Clarinex® and Aerius®. It is an active metabolite of loratadine, which is also on the market.
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[edit] Available forms
Desloratadine is available as tablets and oral suspension.
[edit] Mechanism of action
Desloratadine is a tricyclic antihistamine, which has a selective and peripheral H1-antagonist action. It has a long-lasting effect and does not cause drowsiness because it does not readily enter the central nervous system.[1]
[edit] Side effects
Most common side-effects are fatigue, drowsiness, dry mouth, headache, and gastrointestinal disturbances.
[edit] Desloratadine vs. loratadine
Desloratidine is the major metabolite of loratadine. There are no head to head randomised controlled trials of the two preparations which are expected to be therapeutically closely equivalent in those with normal drug metabolism. A survey of patients dissatisfied with loratadine reported equal or better satisfaction with desloratadine as fexofenadine.[2] This study for reasons known only to its authors did not report on how many patients who took loratadine were satisfied, and it refers to only 61 patients making the transition from loratadine to desloratidine (up to 10,023 may have been taking loratadine). There is some evidence that fexofenadine and loratadine have effectively identical clinical profiles.
A November 2003 article published in the journal American Family Physician about the safety, tolerability, effectiveness, price, and simplicity of desloratadine concluded the following:[3]
- "Desloratadine is similar in effectiveness to fexofenadine and would be expected to produce results similar to loratadine and other nonsedating antihistamines. There is no clinical advantage to switching a patient from loratadine to desloratadine. However, it may be an option for patients whose medical insurance no longer covers loratadine if the co-pay is less than the cost of the over-the-counter product."
[edit] External links
- ^ 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. PMID 10784544.
- ^ Glass D, Harper A (Aug 13, 2003). "Assessing satisfaction with desloratadine and fexofenadine in allergy patients who report dissatisfaction with loratadine.". BMC Fam Pract 4: 10. PMID 12917016.
- ^ See S (2003). "Desloratadine for allergic rhinitis.". Am Fam Physician 68 (10): 2015-6. PMID 14655812.
