Aroled Mechanism of Action

Pharmacology: Desloratadine is a major metabolite of loratadine, antagonist with selective peripheral H1-receptor antagonist activity.
Pharmacodynamics: After oral administration, Desloratadine selectively blocks peripheral histamine H1-receptor. It does not cross the blood-brain barrier to any great extent. Desloratadine has demonstrated in addition to antihistamine activity, anti-allergic and anti-inflammatory activity from numerous in vitro (mainly conducted on cells of human origin) and in vivo studies. These studies have shown that Desloratadine inhibits the broad cascade of events that initiate and propagate allergic inflammation.
Pharmacokinetics: Film-coated tablet: Desloratadine plasma concentrations can be detected within 30 minutes of Desloratadine administration. Desloratadine is well absorbed with maximum concentration achieved after approximately 3 hours; the terminal phase half-life is approximately 27 hours. The degree of accumulation of Desloratadine is consistent with its half-life (approximately 27 hours) and a once daily dosing frequency. The bioavailability of Desloratadine is dose proportional over the range of 5 mg-20 mg.
Syrup: Desloratadine plasma concentrations can be detected within 30 mins of Desloratadine administration.
Desloratadine is well absorbed with maximum concentration achieved after approximately 3 hours; the terminal phase half-life is approximately 27 hours and once daily dosing frequency. The bioavailability of Desloratadine is dose proportional over the range of 5mg-20mg. Desloratadine is moderately bound (83%-87%) to plasma proteins. There is no evidence of clinically relevant drug accumulation following once daily dosing of Desloratadine (5 mg-20 mg) for 14 days.