Desloratadine

Desloratadine

File:Desloratadine.svg
File:Desloratadine2.png
Systematic (IUPAC) name
8-chloro-6,11-dihydro-11-(4-piperdinylidene)- 5H-benzo[5,6]cyclohepta[1,2-b]pyridine
Clinical data
[[Regulation of therapeutic goods |Template:Engvar data]]	EU EMA: Aerius US FDA: Desloratadine
Pregnancy category	AU: B1 US: C (Risk not ruled out)
Routes of administration	oral
Legal status
Legal status	UK: POM (Prescription only) US: ℞-only
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 Number	100643-71-8
ATC code	R06AX27 (WHO)
PubChem	CID 124087
DrugBank	APRD00324
ChemSpider	110575
Chemical data
Formula	C19H19ClN2
Molar mass	310.82[[]]
(verify)

Desloratadine is a drug used to treat allergies. It is marketed under several trade names such as NeoClarityn, Claramax, Clarinex, Larinex, Aerius and Delot. It is an active metabolite of loratadine, which is also on the market.

Available forms

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

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.

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, 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:

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.

In Canada, desloratadine is available without a prescription, and as a generic. Prices are comparable to those of loratadine.

References

de:Desloratadin