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Desloratadine: Wikis

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Desloratadine
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
ChemSpider 110575
Chemical data
Formula C 19H19ClN2  
Mol. mass 310.82
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability Rapidly absorbed
Protein binding 85%
Metabolism Liver
Half life 27 hours
Excretion 40% as conjugated metabolites into urine
Similar amount into the feces
Therapeutic considerations
Licence data

EU EMEA:linkUS FDA:link

Pregnancy cat. B1(AU) C(US)
Legal status POM (UK) -only (US)
Routes oral
 Yes check.svgY(what is this?)  (verify)

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.

Contents

Available forms

Desloratadine is available as tablets (including orally disintegrating and extended release) and as syrup. [1]

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.[2]

Side effects

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

Desloratadine vs. loratadine

Desloratadine is the major metabolite of loratadine. There are no head-to-head randomised controlled trials of the two drugs. A survey of patients dissatisfied with loratadine published in August 2003 reported equal or better satisfaction with desloratadine[3], concluding:

When severity of disease was controlled for in the analysis, a pattern emerged suggesting greater levels of satisfaction amongst loratadine dissatisfied patients who converted to desloratadine. Point estimates suggest a consistent pattern favoring desloratadine patient satisfaction, with statistically significant results reported for sum of adverse effects, nighttime awakening due to symptoms, symptom severity just prior to the next dose, and overall satisfaction (p < 0.05).

A November 2003 article published in the journal American Family Physician about the safety, tolerability, effectiveness, price, and simplicity of desloratadine concluded the following:[4]

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.

References

  1. ^ FDA Electronic Orange Book http://www.fda.gov/cder/ob/default.htm
  2. ^ 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. PMID 10784544. PMC 27362. http://bmj.bmjjournals.com/cgi/content/full/320/7243/1184.  
  3. ^ Glass D, Harper A (August 13, 2003). "Assessing satisfaction with desloratadine and fexofenadine in allergy patients who report dissatisfaction with loratadine". BMC Fam Pract 4: 10. doi:10.1186/1471-2296-4-10. PMID 12917016. PMC 194638. http://www.pubmedcentral.gov/articlerender.fcgi?tool=pubmed&pubmedid=12917016.  
  4. ^ See S (2003). "Desloratadine for allergic rhinitis". Am Fam Physician 68 (10): 2015–6. PMID 14655812. http://www.aafp.org/afp/20031115/steps.html.  
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