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Nelly Frossard - One of the best experts on this subject based on the ideXlab platform.
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Activity of Ebastine (10 and 20 mg) and cetirizine at 24 hours of a steady state treatment in the skin of healthy volunteers
Fundamental & clinical pharmacology, 2000Co-Authors: Nelly Frossard, O. Benabdesselam, Ashok Purohit, Nadjat Mounedji, Gabrielle PauliAbstract:We have compared the inhibitory effects of Ebastine (10 mg), Ebastine (20 mg) and cetirizine (10 mg) on histamine-induced wheal and flare skin reactions 24 h following a 6-day-long treatment. This was a double-blind, randomised, crossover, placebo-controlled study involving 24 healthy volunteers (18-65 years) with negative skin prick tests and the absence of specific IgEs to common allergens. Subjects were randomised to receive each of the following treatments once daily for 6 days: Ebastine (10 mg), Ebastine (20 mg), cetirizine (10 mg) or placebo with a washout period of 5 days. Twenty-four hours after the last dose of each treatment, histamine skin prick tests were performed (0, 0.5, 1, 2.5, 5, 10, 20, 50, 100 and 200 mg/mL), and wheal and flare responses were measured. All active treatments produced significant inhibition of the wheal responses compared to placebo (P < 0.001). Wheal response inhibition was significantly better with 20 mg of Ebastine compared with 10 mg of Ebastine and 10 mg of cetirizine. In a comparison to histamine concentrations required to produce a wheal surface area of 10 mm2, 20 mg of Ebastine was also significantly better than Ebastine 10 mg and cetirizine (P < 0.001), and 10 mg Ebastine was significantly better than cetirizine (P < 0.05). Highly significant (P < 0.001) effects on the flare response were observed with each active treatment compared to placebo, with no difference between groups. The frequency of adverse events, primarily somnolence, was similar among the four treatment groups. Our results clearly indicate that Ebastine, at either recommended dosage of 10 and 20 mg, and cetirizine produced significant inhibition of the histamine-induced wheal and flare reaction compared to placebo for up to 24 h. A superior efficacy of 20 mg of Ebastine is observed compared with 10 mg of Ebastine and 10 mg of cetirizine on the skin wheal response 24 h after the last dose of a 6-day-long treatment. This study clearly proves Ebastine to be an effective, truly once-daily antihistamine.
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Consistency and efficacy of cetirizine (10 mg) versus Ebastine (20 mg) at 4 h on skin reactivity
European journal of clinical pharmacology, 1999Co-Authors: Ashok Purohit, O. Benabdesselam, Gabrielle Pauli, Catherine Duvernelle, M Melac, Nelly FrossardAbstract:Objective: We compared the consistency and efficacy of the two antihistamines, cetirizine (10 mg) and Ebastine (20 mg) on histamine skin reactivity 4 h after treatment. Methods: Twenty-four healthy volunteers participated in a randomised double-blind cross-over study. The areas of wheals and flares induced by increasing (0, 5, 10, 50, 100, 200, 300 mg/ml) histamine concentrations, administered by prick tests, were measured before and 4 h after intake of cetirizine or Ebastine. Results: Before treatment, concentration–response curves were similar and threshold concentrations identical (0.57 mg/ml and 0.57 mg/ml for cetirizine and Ebastine, respectively). Both treatments exerted a significant effect. However, cetirizine was significantly more efficient than Ebastine 20 mg (P
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consistency and efficacy of cetirizine 10 mg versus Ebastine 20 mg at 4 h on skin reactivity
European Journal of Clinical Pharmacology, 1999Co-Authors: A Purohit, O. Benabdesselam, Gabrielle Pauli, Catherine Duvernelle, M Melac, Nelly FrossardAbstract:Objective: We compared the consistency and efficacy of the two antihistamines, cetirizine (10 mg) and Ebastine (20 mg) on histamine skin reactivity 4 h after treatment. Methods: Twenty-four healthy volunteers participated in a randomised double-blind cross-over study. The areas of wheals and flares induced by increasing (0, 5, 10, 50, 100, 200, 300 mg/ml) histamine concentrations, administered by prick tests, were measured before and 4 h after intake of cetirizine or Ebastine. Results: Before treatment, concentration–response curves were similar and threshold concentrations identical (0.57 mg/ml and 0.57 mg/ml for cetirizine and Ebastine, respectively). Both treatments exerted a significant effect. However, cetirizine was significantly more efficient than Ebastine 20 mg (P < 0.01 both for wheals and flares). After cetirizine, the threshold concentration inducing a 3-mm2 wheal was significantly higher (266 mg/ml) than after Ebastine (77 mg/ml) (P < 0.01), and total inhibition of the wheal was obtained in 18 of 24 patients for cetirizine and in 4 of 24 for Ebastine (P < 0.001). The variation coefficient for the wheal reaction was 31% for cetirizine and 159% for Ebastine, indicating a much lower variability after cetirizine. Conclusion: Our study shows clearly that the efficacy of a single therapeutic dosage of cetirizine is greater and consistently better than that of Ebastine for suppression of cutaneous reactivity to histamine 4 h after treatment in healthy volunteers. The need for Ebastine to metabolise into the active carEbastine might explain this difference.
Joel Morganroth - One of the best experts on this subject based on the ideXlab platform.
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Effects of supratherapeutic doses of Ebastine and terfenadine on the QT interval
British journal of clinical pharmacology, 2001Co-Authors: Michael S Gillen, Philip Chaikin, Barry M. Miller, Joel MorganrothAbstract:Aims The objective of this study was to compare the effects of high doses of Ebastine with terfenadine and placebo on QTc. Methods Thirty-two subjects were randomly assigned to four treatments (Ebastine 60 mg day−1, Ebastine 100 mg day−1, terfenadine 360 mg day−1, placebo) administered for 7 days. Serial ECGs were performed at baseline and day 7 of each period. QT interval was analysed using both Bazett (QTcB) and Fridericia (QTcF) corrections. Results Ebastine 60 mg (+ 3.7 ms) did not cause a statistically significant change in QTcB compared with placebo (+ 1.4 ms). The mean QTcB for Ebastine 100 mg was increased by + 10.3 ms which was significantly greater than placebo but was significantly less (P
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effects of supratherapeutic doses of Ebastine and terfenadine on the qt interval
British Journal of Clinical Pharmacology, 2001Co-Authors: Michael S Gillen, Barry Miller, Philip Chaikin, Joel MorganrothAbstract:Aims The objective of this study was to compare the effects of high doses of Ebastine with terfenadine and placebo on QTc. Methods Thirty-two subjects were randomly assigned to four treatments (Ebastine 60 mg day−1, Ebastine 100 mg day−1, terfenadine 360 mg day−1, placebo) administered for 7 days. Serial ECGs were performed at baseline and day 7 of each period. QT interval was analysed using both Bazett (QTcB) and Fridericia (QTcF) corrections. Results Ebastine 60 mg (+ 3.7 ms) did not cause a statistically significant change in QTcB compared with placebo (+ 1.4 ms). The mean QTcB for Ebastine 100 mg was increased by + 10.3 ms which was significantly greater than placebo but was significantly less (P < 0.05) than with terfenadine 360 mg (+ 18.0 ms). There were no statistically significant differences in QTcF between Ebastine 60 mg (−3.2 ms) or Ebastine 100 mg (1.5 ms) and placebo (−2.1 ms); although terfenadine caused a 14.1 ms increase which was significantly different from the other three treatments. The increase in QTcB with Ebastine most likely resulted from overcorrection of the small drug-induced increase in heart rate. Conclusions Ebastine at doses up to five times the recommended therapeutic dose did not cause clinically relevant changes in QTc interval.
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Cardiac Effects of Ebastine and Other Antihistamines in Humans
Drug Safety, 1999Co-Authors: Arthur J. Moss, Joel MorganrothAbstract:The electrocardiographic effects of Ebastine and its active metabolite, carEbastine, have been studied alone and in relevant drug-interaction studies in various patient populations. The overall cardiac tolerability of Ebastine is excellent. In Ebastine dose-ranging studies in adults and children, there were no meaningful dose-related changes in the QTc interval. At high doses of Ebastine (5 to 10 times the recommended dose), a modest 10.3 msec increase in QTc was observed. Recommended doses of Ebastine had no meaningful effect on QTc in the elderly or in patients with renal or hepatic insufficiency. Interaction studies involving Ebastine with ketoconazole revealed a significant increase in the serum Ebastine concentration and in the elimination half-life of Ebastine, with a modest 18.1 msec increase in QTc (approximately 10 msec above ketoconazole alone) and a plateau QTc-Ebastine relationship at higher Ebastine levels. Similar, though more minor, QTc findings were observed during coadministration of Ebastine with erythro-mycin. No QTc effects were noted when Ebastine was administered with theo-phylline, and the QTc was similar when Ebastine was administered with or without food. These findings indicate that Ebastine is well tolerated and, in contrast to terfenadine and astemizole, has no clinically meaningful effect on the QTc interval even at high serum concentrations. As with other ‘safe’ antihistamines, which have shown similar modest increases in QTc when coadministered with ketoconazole, caution should be exercised when administering Ebastine to patients having the long QT syndrome or hypokalaemia, and in patients receiving azole antifungals or macrolide antibacterials.
Gabrielle Pauli - One of the best experts on this subject based on the ideXlab platform.
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Activity of Ebastine (10 and 20 mg) and cetirizine at 24 hours of a steady state treatment in the skin of healthy volunteers
Fundamental & clinical pharmacology, 2000Co-Authors: Nelly Frossard, O. Benabdesselam, Ashok Purohit, Nadjat Mounedji, Gabrielle PauliAbstract:We have compared the inhibitory effects of Ebastine (10 mg), Ebastine (20 mg) and cetirizine (10 mg) on histamine-induced wheal and flare skin reactions 24 h following a 6-day-long treatment. This was a double-blind, randomised, crossover, placebo-controlled study involving 24 healthy volunteers (18-65 years) with negative skin prick tests and the absence of specific IgEs to common allergens. Subjects were randomised to receive each of the following treatments once daily for 6 days: Ebastine (10 mg), Ebastine (20 mg), cetirizine (10 mg) or placebo with a washout period of 5 days. Twenty-four hours after the last dose of each treatment, histamine skin prick tests were performed (0, 0.5, 1, 2.5, 5, 10, 20, 50, 100 and 200 mg/mL), and wheal and flare responses were measured. All active treatments produced significant inhibition of the wheal responses compared to placebo (P < 0.001). Wheal response inhibition was significantly better with 20 mg of Ebastine compared with 10 mg of Ebastine and 10 mg of cetirizine. In a comparison to histamine concentrations required to produce a wheal surface area of 10 mm2, 20 mg of Ebastine was also significantly better than Ebastine 10 mg and cetirizine (P < 0.001), and 10 mg Ebastine was significantly better than cetirizine (P < 0.05). Highly significant (P < 0.001) effects on the flare response were observed with each active treatment compared to placebo, with no difference between groups. The frequency of adverse events, primarily somnolence, was similar among the four treatment groups. Our results clearly indicate that Ebastine, at either recommended dosage of 10 and 20 mg, and cetirizine produced significant inhibition of the histamine-induced wheal and flare reaction compared to placebo for up to 24 h. A superior efficacy of 20 mg of Ebastine is observed compared with 10 mg of Ebastine and 10 mg of cetirizine on the skin wheal response 24 h after the last dose of a 6-day-long treatment. This study clearly proves Ebastine to be an effective, truly once-daily antihistamine.
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Consistency and efficacy of cetirizine (10 mg) versus Ebastine (20 mg) at 4 h on skin reactivity
European journal of clinical pharmacology, 1999Co-Authors: Ashok Purohit, O. Benabdesselam, Gabrielle Pauli, Catherine Duvernelle, M Melac, Nelly FrossardAbstract:Objective: We compared the consistency and efficacy of the two antihistamines, cetirizine (10 mg) and Ebastine (20 mg) on histamine skin reactivity 4 h after treatment. Methods: Twenty-four healthy volunteers participated in a randomised double-blind cross-over study. The areas of wheals and flares induced by increasing (0, 5, 10, 50, 100, 200, 300 mg/ml) histamine concentrations, administered by prick tests, were measured before and 4 h after intake of cetirizine or Ebastine. Results: Before treatment, concentration–response curves were similar and threshold concentrations identical (0.57 mg/ml and 0.57 mg/ml for cetirizine and Ebastine, respectively). Both treatments exerted a significant effect. However, cetirizine was significantly more efficient than Ebastine 20 mg (P
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consistency and efficacy of cetirizine 10 mg versus Ebastine 20 mg at 4 h on skin reactivity
European Journal of Clinical Pharmacology, 1999Co-Authors: A Purohit, O. Benabdesselam, Gabrielle Pauli, Catherine Duvernelle, M Melac, Nelly FrossardAbstract:Objective: We compared the consistency and efficacy of the two antihistamines, cetirizine (10 mg) and Ebastine (20 mg) on histamine skin reactivity 4 h after treatment. Methods: Twenty-four healthy volunteers participated in a randomised double-blind cross-over study. The areas of wheals and flares induced by increasing (0, 5, 10, 50, 100, 200, 300 mg/ml) histamine concentrations, administered by prick tests, were measured before and 4 h after intake of cetirizine or Ebastine. Results: Before treatment, concentration–response curves were similar and threshold concentrations identical (0.57 mg/ml and 0.57 mg/ml for cetirizine and Ebastine, respectively). Both treatments exerted a significant effect. However, cetirizine was significantly more efficient than Ebastine 20 mg (P < 0.01 both for wheals and flares). After cetirizine, the threshold concentration inducing a 3-mm2 wheal was significantly higher (266 mg/ml) than after Ebastine (77 mg/ml) (P < 0.01), and total inhibition of the wheal was obtained in 18 of 24 patients for cetirizine and in 4 of 24 for Ebastine (P < 0.001). The variation coefficient for the wheal reaction was 31% for cetirizine and 159% for Ebastine, indicating a much lower variability after cetirizine. Conclusion: Our study shows clearly that the efficacy of a single therapeutic dosage of cetirizine is greater and consistently better than that of Ebastine for suppression of cutaneous reactivity to histamine 4 h after treatment in healthy volunteers. The need for Ebastine to metabolise into the active carEbastine might explain this difference.
George Georges - One of the best experts on this subject based on the ideXlab platform.
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a double blind placebo controlled study of the efficacy and safety of Ebastine 20 mg once daily given with and without food in the treatment of seasonal allergic rhinitis
The Journal of Clinical Pharmacology, 2002Co-Authors: Frank Hampel, Shashank Rohatagi, Michael Gillen, Janet Lim, George GeorgesAbstract:The efficacy and safety of Ebastine 20 mg once daily given with and without food were compared in patients ages 12 to 70 years with seasonal allergic rhinitis (SAR) caused by mountain cedar allergen. This double-blind, placebo-controlled study was conducted at six centers in Texas. Efficacy and safety analyses were performed on the intent-to-treat population, which comprised 652 patients; 540 patients completed the study. Following 2 weeks' treatment, no significant differences (p > or = 0.91) were found between the Ebastine with and without food groups in the percentage change from baseline of daily "reflective" total rhinitis symptom scores (i.e., patients' assessment of severity over the previous 12 h), but both Ebastine groups exhibited significantly greater reductions versus patients receiving placebo (p < 0.0001). There were also no significant differences in the percentages of patients experiencing adverse events between the Ebastine with and without food groups. Mean steady-state plasma concentrations of Ebastine and its active metabolite carEbastine were, respectively, 5.5% (ns) and 15.1% (p < 0.05) higher when Ebastine was given with food versus its administration without food. Overall, these results indicate that in clinical practice, Ebastine does not need to be administered with reference to food.
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Comparison of once-daily Ebastine 20 mg, Ebastine 10 mg, loratadine 10 mg, and placebo in the treatment of seasonal allergic rhinitis
Journal of Allergy and Clinical Immunology, 2000Co-Authors: Paul H. Ratner, Janet Lim, George GeorgesAbstract:Abstract Background: Ebastine and loratadine are 2 nonsedating second-generation H 1 antihistamines with once-daily dosing. Objective: We compared the efficacy and safety of Ebastine 20 mg and 10 mg, loratadine 10 mg, and placebo administered once daily for 4 weeks in controlling the symptoms of seasonal allergic rhinitis (SAR). Methods: In a double-blind, placebo-controlled, randomized, parallel-group study, 565 patients with ragweed SAR, ages 12 to 70 years, received either Ebastine 20 mg, Ebastine 10 mg, loratadine 10 mg, or placebo once daily for 4 weeks. Patients recorded morning and evening reflective scores (past 12 hours) as well as snapshot scores (at time of recording) for nasal discharge, congestion, sneezing, itching, and total eye symptoms. Total symptom score (TSS) is the sum of these 5 scores. Results: Ebastine 20 mg produced significantly greater ( P P P = .78). Conclusion: Ebastine 20 mg given once daily was significantly superior to loratadine 10 mg given once daily at improving the rhinitis total symptom score throughout the day and at awakening over a 4-week period. Ebastine 20 mg and 10 mg doses were both efficacious and well tolerated in the treatment of SAR. (J Allergy Clin Immunol 2000;105:1101-7.)
Michael S Gillen - One of the best experts on this subject based on the ideXlab platform.
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Effects of supratherapeutic doses of Ebastine and terfenadine on the QT interval
British journal of clinical pharmacology, 2001Co-Authors: Michael S Gillen, Philip Chaikin, Barry M. Miller, Joel MorganrothAbstract:Aims The objective of this study was to compare the effects of high doses of Ebastine with terfenadine and placebo on QTc. Methods Thirty-two subjects were randomly assigned to four treatments (Ebastine 60 mg day−1, Ebastine 100 mg day−1, terfenadine 360 mg day−1, placebo) administered for 7 days. Serial ECGs were performed at baseline and day 7 of each period. QT interval was analysed using both Bazett (QTcB) and Fridericia (QTcF) corrections. Results Ebastine 60 mg (+ 3.7 ms) did not cause a statistically significant change in QTcB compared with placebo (+ 1.4 ms). The mean QTcB for Ebastine 100 mg was increased by + 10.3 ms which was significantly greater than placebo but was significantly less (P
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effects of supratherapeutic doses of Ebastine and terfenadine on the qt interval
British Journal of Clinical Pharmacology, 2001Co-Authors: Michael S Gillen, Barry Miller, Philip Chaikin, Joel MorganrothAbstract:Aims The objective of this study was to compare the effects of high doses of Ebastine with terfenadine and placebo on QTc. Methods Thirty-two subjects were randomly assigned to four treatments (Ebastine 60 mg day−1, Ebastine 100 mg day−1, terfenadine 360 mg day−1, placebo) administered for 7 days. Serial ECGs were performed at baseline and day 7 of each period. QT interval was analysed using both Bazett (QTcB) and Fridericia (QTcF) corrections. Results Ebastine 60 mg (+ 3.7 ms) did not cause a statistically significant change in QTcB compared with placebo (+ 1.4 ms). The mean QTcB for Ebastine 100 mg was increased by + 10.3 ms which was significantly greater than placebo but was significantly less (P < 0.05) than with terfenadine 360 mg (+ 18.0 ms). There were no statistically significant differences in QTcF between Ebastine 60 mg (−3.2 ms) or Ebastine 100 mg (1.5 ms) and placebo (−2.1 ms); although terfenadine caused a 14.1 ms increase which was significantly different from the other three treatments. The increase in QTcB with Ebastine most likely resulted from overcorrection of the small drug-induced increase in heart rate. Conclusions Ebastine at doses up to five times the recommended therapeutic dose did not cause clinically relevant changes in QTc interval.
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A review of the cardiac systemic side-effects of antihistamines: Ebastine.
Clinical & Experimental Allergy, 1999Co-Authors: A. J. Moss, Michael S Gillen, Philip Chaikin, J. D. Garcia, D. J. Roberts, J. MorganrothAbstract:The cardiac safety of Ebastine, a long-acting, non-sedating antihistamine, has been thoroughly assessed in phase I-III clinical studies. Ebastine alone at the recommended doses of 10 mg and 20 mg has no clinically relevant effect on QTc interval in adults and in special patient populations (elderly, children or subjects with hepatic or renal impairment). Ebastine administered at 60 and 100 mg/day (3-5 times the maximum recommended dose) for 1 week had statistically significantly smaller effects (3.7 and 10.3 msec, respectively) on the QTc interval than terfenadine (18 msec) at three times the recommended dose (360 mg/day). The mean QTc interval prolongation observed with Ebastine 100 mg/day was small and not clinically meaningful, although the results were statistically significant vs. placebo. The effect of Ebastine 60 mg/day was not statistically different from placebo. Steady-state drug interaction studies demonstrated that the co-administration of Ebastine 20 mg with ketoconazole or erythromycin produced significant increases in systemic exposure for Ebastine, which were accompanied by small increases in QTc (approximately 10 msec above ketoconazole or erythromycin alone). Results from individual studies suggest that, when coadministered with ketoconazole, Ebastine produces similar changes in QTc interval measurements compared to loratadine and cetirizine. Pooled data from clinical efficacy trials of Ebastine 1-30 mg/day administered for 2-3 weeks showed no clinically relevant cardiac effects as assessed by serial electrocardiographs and Holter monitoring. The overall cardiac safety profile based on currently available information suggests that Ebastine, like loratadine and cetirizine, has a lower potential for causing adverse cardiovascular effects than terfenadine.