Desloratadine

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

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Desloratadine.png
Chemical structure of desloratadine.


Descarboethoxyloratadine
8-chloro-6,11-dihydro-11-(4-piperdinylidene)- 5H-benzo[5,6]cyclohepta[1,2-b]pyridine
Molecular Weight 310.82
Empiric Formula C19H19ClN2
ATC code R06AX27
Metabolism Liver
Pregnancy category C (USA)
B1 (Aus)
Contents

Available forms

Desloratadine is available as tablets and oral suspension.

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. It is 10-20 times more potent as an antihistamine than loratadine.

Pharmacokinetics

Desloratadine is rapidly absorbed from the gastro-intestinal tract. Desloratadine is moderately bound to plasma proteins (85%). The half-life of desloratadine is on average 28 hours. About 40% is excreted as conjugated metabolites into the urine and similar amount into the feces. Traces of unmetabolised desloratadine can be found in the urine.

Side effects

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

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