PMID: 9541729May 9, 1998Paper

Anti-inflammatory properties of mizolastine after oral administration on arachidonic acid-induced cutaneous reaction in the rat

Arzneimittel-Forschung
P PichatS Arbilla

Abstract

The anti-inflammatory effect of mizolastine (CAS 108612-45-9, SL85.0324-00), a new non-sedative histamine H1-receptor antagonist, was assessed in comparison to loratadine, terfenadine and pyrilamine. Intraplantar injection of arachidonic acid (AA) into the rat paw was followed by a rapid and sustained (> or = 4h) inflammatory oedema. Mizolastine (0.1 to 10 mg/ kg p.o.) inhibited in a dose-dependent manner the time course of the AA-induced paw inflammation as from the dose of 0.1 mg/kg p.o. This effect was maintained for at least the 4 h of observation (-44% at 0.3 mg/kg p.o.) suggesting a long lasting action of mizolastine. Although with higher maximal effect, a similar time course of response was observed with dexamethasone at 0.1 mg/kg p.o. In contrast, at anti-histamine, doses, the histamine H1-receptor antagonists terfenadine (1 to 30 mg/kg p.o.), loratadine (10 mg/kg p.o.), and pyrilamine (10 mg/kg p.o.) failed to inhibit significantly the inflammatory action of AA. Moreover, under conditions of H1-receptors blockade (e.g. when co-administered with pyrilamine or loratadine (10 mg/kg p.o.), the inhibition by mizolastine (0.3 mg/kg) of AA-induced inflammation was unchanged. This suggests that the anti-inflammatory effect of ...Continue Reading

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