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Pharmacologic modulation by cetirizine 2 HCl and loratadine of the histamine‐induced skin reaction in mice and in humans
Author(s) -
Coulie P.,
De Vos C.,
Ghys L.,
Rihoux J. P.
Publication year - 1989
Publication title -
drug development research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.582
H-Index - 60
eISSN - 1098-2299
pISSN - 0272-4391
DOI - 10.1002/ddr.430170303
Subject(s) - loratadine , cetirizine , histamine , pharmacology , placebo , chemistry , histamine h1 receptor , antihistamine , skin reaction , medicine , immunology , antagonist , receptor , alternative medicine , pathology
In mice, the histamine‐induced cutaneous reaction is inhibited by cetirizine with an approached ED 50 of 0.04 mg/kg and by loratadine with an approached ED 50 of 0.38 mg/kg, both drugsadministered intraperitoneally. At these doses, cetirizine' s onset of activity seems to be more rapid, although both compounds show the same duration for at least 7 hr. Nine healthy volunteers received orally either cetirizine or loratadine (10 mg single dose) or placebo in a double‐blind randomized and cross‐over study design. Both drugswere significantly more effective than placebo (except loratadine at the 2nd and 24th hr for the wheal with 1 and 10 μg histamine, and at the 2nd hr for the flare with 1 μg histamine). At all times and withboth agonists' concentrations, cetirizine was significantly more potent than loratadine (except at the 24th hr for the wheal with 1 μghistamine). Neither numerous nor marked side effects were found.