Desloratadine

IUPAC: 8-chloro- 11- ( piperidin-4- ylidene) -5,6- dihydro- 11H -benzo [ 5,6] cyclohepta [1,2- b] pyridine

R06AX27

Antihistamine

Antihistamine

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Desloratadine is a drug selected from the group of antihistamines, which is used for treatment of allergic rhinitis and chronic urticaria. Desloratadine is a metabolite of the antihistamine loratadine and descendant and was brought by the pharmaceutical company Essex Pharma with the expiry of patent protection for loratadine on the market. Desloratadine is subject to medical prescription.

Mechanism of Action

The mechanism of action of desloratadine corresponds to that of loratadine, as H1 - antihistamine that blocks the specific binding sites for histamine, the histamine H1 receptors, and thus inhibits histamine effects (eg, skin redness, itching, hypotension and bronchospasm ); Desloratadine further stabilized as well as the mast cells, whereby the release of histamine is blocked. Desloratadine also acts as FIASMA ( functional inhibitors of acid sphingomyelinase ).

Comparison with loratadine

In contrast to the desloratadine, loratadine has a three-to four-fold higher affinity for the H1 receptor. Therefore, loratadine can be formally regarded as a prodrug of desloratadine. Moreover, desloratadine has a longer plasma half-life as well as the loratadine and passes only a very small proportion of the blood- brain barrier and is thus substantially free of side effects on the central nervous system, such as sedation. A therapeutic benefit is classified as marginal, as well as loratadine in the liver is almost completely converted to desloratadine. The temporal proximity between the discontinuation of patent protection for loratadine and the marketing of desloratadine, suggests that this was also a reason for its introduction.

Trade names

Aerius (D, A, CH, I), Dasselta (D, A), Azomyr (A), Neoclarityn (A)

Aerinaze (A)