{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,7,18]],"date-time":"2026-07-18T14:56:25Z","timestamp":1784386585655,"version":"3.55.0"},"reference-count":25,"publisher":"Wiley","issue":"1","license":[{"start":{"date-parts":[[2008,9,23]],"date-time":"2008-09-23T00:00:00Z","timestamp":1222128000000},"content-version":"vor","delay-in-days":2822,"URL":"http:\/\/onlinelibrary.wiley.com\/termsAndConditions#vor"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Allergy"],"published-print":{"date-parts":[[2001,1]]},"abstract":"<jats:p> <jats:bold>Background:<\/jats:bold> Cetirizine is a highly efficacious and long\u2010acting second\u2010generation H<jats:sub>1<\/jats:sub>\u2010receptor antagonist for the treatment of allergic diseases, such as allergic rhinitis and chronic idiopathic urticaria, in adults and children. Pharmacologic studies have demonstrated that cetirizine, a racemate mixture composed of equal amounts of two enantiomers, does not undergo hepatic metabolism to any significant level. The enantiomers are excreted mainly unchanged, predominantly in the urine and to a lesser extent in the faeces.<\/jats:p><jats:p> <jats:bold>Methods:<\/jats:bold> The pharmacologic activity and potency of the two enantiomers of cetirizine in the management of allergic skin conditions were investigated by studying the effect of treatment with 5.0\u2003mg cetirizine; 2.5\u2003mg levocetirizine, the (<jats:italic>R<\/jats:italic>)\u2010enantiomer; and 2.5\u2003mg ucb 28557, the (<jats:italic>S<\/jats:italic>)\u2010enantiomer, on histamine\u2010induced wheal and flare response in 18 healthy volunteers. Each treatment was administered as a single oral dose in randomized, double\u2010blind, and crossover manner, and the efficacy of treatment was assessed over a period of 32\u2003h, as per cent inhibition of the histamine\u2010induced wheal and flare areas before treatment. Blood and urine samples were collected in a time\u2010dependent manner and analyzed for the total amounts of each study drug, to elucidate their pharmacokinetic profiles.<\/jats:p><jats:p> <jats:bold>Results: <\/jats:bold>Both cetirizine and levocetirizine caused a marked inhibition of histamine\u2010induced wheal and flare, whereas ucb 28557 was inactive in this model. Inhibition of the wheal response observed for cetirizine and levocetirizine was apparent by 1\u2003h after dosage and lasted for mean durations of 24.4 and 28.4\u2003h, respectively. In addition, the response for cetirizine and levocetirizine became maximal by 6\u2003h after treatment, rising to 79.5% and 83.8%. Similarly, cetirizine and levocetirizine also markedly inhibited the histamine\u2010induced flare response. This effect was evident for both drugs by 1 h after dosage and lasted over a mean period of 28.4 and 26.0 h, respectively, for cetirizine and levocetirizine. The inhibitory effect of these compounds on histamine\u2010induced flare response was also maximal by approximately 6\u2003h after dosage, peaking at 88.5% and 83.6%, respectively. Statistical evaluation showed that cetirizine and levocetirizine were equivalent for maximum inhibition of histamine\u2010induced wheal and flare. However, levocetirizine was found to be superior to cetirizine when area under the curve was compared. In contrast, ucb 28557 was not found to inhibit histamine\u2010induced wheal and flare responses at any time during the study period. Plasma concentrations of levocetirizine were found to be approximately double those of ucb 28557 at 4 and 8\u2003h after dosing, and 50\u201360% of the drugs were excreted unchanged in urine over a period of 32\u2003h.<\/jats:p><jats:p> <jats:bold>Conclusions: <\/jats:bold>The finding that, in this model, levocetirizine 2.5\u2003mg has comparable antihistaminic activity to cetirizine 5\u2003mg, whereas its other enantiomer ucb 28557 has no pharmacodynamic effect, suggests that the antihistaminic properties of cetirizine observed in the management of allergic skin conditions are likely to be attributable to levocetirizine.<\/jats:p>","DOI":"10.1034\/j.1398-9995.2001.00726.x","type":"journal-article","created":{"date-parts":[[2003,3,11]],"date-time":"2003-03-11T01:45:05Z","timestamp":1047347105000},"page":"50-57","source":"Crossref","is-referenced-by-count":121,"title":["A randomized, double\u2010blind, crossover comparison among cetirizine, levocetirizine, and ucb 28557 on histamine\u2010induced cutaneous responses in healthy adult volunteers"],"prefix":"10.1111","volume":"56","author":[{"given":"J. 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