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Pharmacology: Pharmacodynamics: Desloratadine is the major active metabolite of loratadine. Similar to loratadine, desloratadine is a non-sedating antihistamine. Desloratadine is a long-acting tricyclic antihistamine with selective peripheral histamine H1 receptor antagonistic activity.
Pharmacokinetics: Absorption: Peak plasma concentrations in children occur in about 2 hours after a single oral 1.25 mg and 5 mg of desloratadine syrup. These values are similar to what was measure in adults who receives 5 mg oral desloratadine. Food has no effect on the extent of absorption.
Distribution: Desloratadine is 82% to 87% bound to plasma proteins. An active metabolite (3-Hydroxydesloratadine) is 85% to 89% bound to plasma proteins. Total protein binding of desloratadine is 73% to 76%. Volume of distribution of desloratadine in children is 686 L to 1565 L.
Metabolism: Desloratadine is metabolized via liver. Metabolism of desloratadine to major active metabolite 3-Hydroxydesloratadine and its associated O-glucuronide was mediated by CYP2C8 in conjunction with UGT2B10. Desloratadine is rapidly metabolized via hydroxylation. Metabolism decrease in slow metabolizers of desloratadine.
Excretion: Desloratadine is excreted in the urine 40.6% and 46.5% was excreted in feces. Total body clearance in adults, approximately 150 L/hr and 31.4 to 64.5 L/hr in children. The mean half-life elimination of desloratadine in children 2-5 years is 16.4 hours, 6-11 years is 19.4 hours and about 27 hours in adults.
