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Anne K Ellis - One of the best experts on this subject based on the ideXlab platform.
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onset of action for Loratadine tablets for the symptomatic control of seasonal allergic rhinitis in adults challenged with ragweed pollen in the environmental exposure unit a post hoc analysis of total symptom score
Allergy Asthma & Clinical Immunology, 2018Co-Authors: Anne K Ellis, Mark W. Tenn, Lisa M. Steacy, Charlene C NgAbstract:Loratadine is a second-generation, non-sedating antihistamine used for the relief of allergic rhinitis symptoms. Previous studies reported that when Loratadine was encapsulated, the onset of action for symptom relief was 180 min. However, unmodified Loratadine tablets were not evaluated at that time. Using data from a previously published Environmental Exposure Unit (EEU) study comparing azelastine nasal spray with Loratadine tablets, cetirizine tablets, and placebo, this post hoc analysis determines the onset of action of Loratadine tablets (i.e. unmodified) by analyzing the total symptom score for the relief of nasal and ocular seasonal allergic rhinitis (SAR) symptoms. A Phase IV, randomized, single-center, double-blind, placebo-controlled, double-dummy, four-way crossover study was conducted in the EEU. Seventy participants were randomized sequentially into one of the four treatments during ragweed pollen exposure. Nasal and ocular symptom scores were self-reported by the participants and recorded. The original study analysis was carried out by evaluating the nasal symptom scores only. For this post hoc analysis, both nasal and ocular data from the Loratadine and placebo treatment arms were analyzed. The primary endpoint for this analysis was the onset of action of Loratadine as measured by the change in total symptom score (TSS) from baseline in comparison to placebo. The onset of ocular symptom relief using the total ocular symptom score (TOSS) was also reported. Loratadine tablets demonstrated a significant and durable improvement in both TSS (P = .005) and TOSS (P = .013) at 75 min post-treatment administration compared to placebo. The mean proportion of participants reporting none or mild for all component symptoms of TSS and TOSS at 75 min and thereafter was significantly higher in the Loratadine (TSS, P = .0005; TOSS, P ≤ .0001) vs. placebo treatment arm. The onset of action of Loratadine tablets was 75 min for the relief of nasal and ocular symptoms in adults with SAR. These results suggest a faster onset of action for Loratadine tablets (75 min) compared to previously reported studies which were conducted with modified (i.e. gelatin-encapsulated) Loratadine tablets (180 min). Trial registration Clinicaltrials.gov identifier NCT00561717
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Onset of action for Loratadine tablets for the symptomatic control of seasonal allergic rhinitis in adults challenged with ragweed pollen in the Environmental Exposure Unit: a post hoc analysis of total symptom score
BMC, 2018Co-Authors: Mark W. Tenn, Lisa M. Steacy, Anne K EllisAbstract:Abstract Background Loratadine is a second-generation, non-sedating antihistamine used for the relief of allergic rhinitis symptoms. Previous studies reported that when Loratadine was encapsulated, the onset of action for symptom relief was 180 min. However, unmodified Loratadine tablets were not evaluated at that time. Using data from a previously published Environmental Exposure Unit (EEU) study comparing azelastine nasal spray with Loratadine tablets, cetirizine tablets, and placebo, this post hoc analysis determines the onset of action of Loratadine tablets (i.e. unmodified) by analyzing the total symptom score for the relief of nasal and ocular seasonal allergic rhinitis (SAR) symptoms. Methods A Phase IV, randomized, single-center, double-blind, placebo-controlled, double-dummy, four-way crossover study was conducted in the EEU. Seventy participants were randomized sequentially into one of the four treatments during ragweed pollen exposure. Nasal and ocular symptom scores were self-reported by the participants and recorded. The original study analysis was carried out by evaluating the nasal symptom scores only. For this post hoc analysis, both nasal and ocular data from the Loratadine and placebo treatment arms were analyzed. The primary endpoint for this analysis was the onset of action of Loratadine as measured by the change in total symptom score (TSS) from baseline in comparison to placebo. The onset of ocular symptom relief using the total ocular symptom score (TOSS) was also reported. Results Loratadine tablets demonstrated a significant and durable improvement in both TSS (P = .005) and TOSS (P = .013) at 75 min post-treatment administration compared to placebo. The mean proportion of participants reporting none or mild for all component symptoms of TSS and TOSS at 75 min and thereafter was significantly higher in the Loratadine (TSS, P = .0005; TOSS, P ≤ .0001) vs. placebo treatment arm. Conclusions The onset of action of Loratadine tablets was 75 min for the relief of nasal and ocular symptoms in adults with SAR. These results suggest a faster onset of action for Loratadine tablets (75 min) compared to previously reported studies which were conducted with modified (i.e. gelatin-encapsulated) Loratadine tablets (180 min). Trial registration Clinicaltrials.gov identifier NCT0056171
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a four way double blind randomized placebo controlled study to determine the efficacy and speed of azelastine nasal spray versus Loratadine and cetirizine in adult subjects with allergen induced seasonal allergic rhinitis
Allergy Asthma & Clinical Immunology, 2013Co-Authors: James H Day, Anne K Ellis, Lisa M. Steacy, Yifei Zhu, Terry WalkerAbstract:Azelastine has been shown to be effective against seasonal allergic rhinitis (SAR). The Environmental Exposure Unit (EEU) is a validated model of experimental SAR. The objective of this double-blind, four-way crossover study was to evaluate the onset of action of azelastine nasal spray, versus the oral antihistamines Loratadine 10 mg and cetirizine 10 mg in the relief of the symptoms of SAR. 70 participants, aged 18-65, were randomized to receive azelastine nasal spray, cetirizine, Loratadine, or placebo after controlled ragweed pollen exposure in the EEU. Symptoms were evaluated using the total nasal symptom score (TNSS). The primary efficacy parameter was the onset of action as measured by the change from baseline in TNSS. Azelastine displayed a statistically significant improvement in TNSS compared with placebo at all time points from 15 minutes through 6 hours post dose. Azelastine, cetirizine, and Loratadine reduced TNSS compared to placebo with an onset of action of 15 (p < 0.001), 60 (p = 0.015), and 75 (p = 0.034) minutes, respectively. The overall assessment of efficacy was rated as good or very good by 46% of the participants for azelastine, 51% of the participants for cetirizine, and 30% of the participants for Loratadine compared to 18% of the participants for placebo. Azelastine’s onset of action for symptom relief was faster than that of cetirizine and Loratadine. The overall participant satisfaction in treatment with azelastine is comparable to cetirizine and statistically superior to Loratadine. These results suggest that azelastine may be preferential to oral antihistamines for the rapid relief of SAR symptoms.
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onset of action and efficacy of terfenadine astemizole cetirizine and Loratadine for the relief of symptoms of allergic rhinitis
Annals of Allergy Asthma & Immunology, 1997Co-Authors: Maureen P Briscoe, Reginald H Clark, Anne K Ellis, Pierre GervaisAbstract:BACKGROUND: Terfenadine, astemizole, cetirizine, and Loratadine are compared in their abilities to produce relief of symptoms of allergic rhinitis. OBJECTIVE: The aim of this study was to compare the onset of action and efficacy of the study medications. METHODS: 111 ragweed-sensitive subjects were primed with pollen in the Environmental Exposure Unit. Study entry required adequate symptoms over a 3 hour exposure to 5000 +/- 300 grains/m3 of ragweed pollen. On the test day, subjects were given a single dose of either terfenadine 60 mg (22), astemizole 10 mg (22), cetirizine 10 mg (23), Loratadine 10 mg (22), or placebo (22) when sufficiently symptomatic after a 60-minute exposure. Allergen levels were maintained and symptoms recorded every 30 minutes. RESULTS: Proportions of subjects with clinically important relief were cetirizine, 69.6%; terfenadine, 54.5%; Loratadine, 50.0%; astemizole, 40.9%; and placebo, 31.8% but differences weren't significant between treatment groups (P = .119). Survival curves for times to onset of clinically important relief for the four treatment groups were not different (P = .119). Subjects realizing definitive relief were cetirizine, 65.2%; terfenadine, 45.5%; Loratadine, 31.8%; placebo, 27.3%; and astemizole, 22.7% (P = .023). Survival analysis of onset time for definitive relief found significant differences (P = .010). The ranking was cetirizine --> terfenadine --> Loratadine --> astemizole (quickest to slowest). Global evaluation based on subject willingness to take the medication again yielded percentages: cetirizine, 82.6%; terfenadine, 66.7%; astemizole, 63.6%; Loratadine, 40.9%; and placebo, 36.4% (P = .036). CONCLUSION: Cetirizine and terfenadine continuously ranked higher in terms of onset of action and efficacy, while Loratadine and astemizole ranked lower. Significance was detected in definitive relief and relative efficacy.
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onset of action and efficacy of terfenadine astemizole cetirizine and Loratadine for the relief of symptoms of allergic rhinitis
Annals of Allergy Asthma & Immunology, 1997Co-Authors: James H Day, Maureen P Briscoe, Reginald H Clark, Anne K Ellis, Pierre GervaisAbstract:Background Terfenadine, astemizole, cetirizine, and Loratadine are compared in their abilities to produce relief of symptoms of allergic rhinitis. Objective The aim of this study was to compare the onset of action and efficacy of the study medications. Methods One hundred eleven ragweed-sensitive subjects were primed with pollen in the Environmental Exposure Unit. Study entry required adequate symptoms over a 3-hour exposure to 5,000 ± 300 grains/m 3 of ragweed pollen. On the test day, subjects were given a single dose of either terfenadine 60 mg (22), astemizole 10 mg (22), cetirizine 10 mg (23), Loratadine 10 mg (22), or placebo (22) when sufficiently symptomatic after a 60-minute exposure. Allergen levels were maintained and symptoms recorded every 30 minutes. Results Proportions of subjects with clinically important relief were cetirizine, 69.6%; terfenadine, 54.5%; Loratadine, 50.0% astemizole, 40.9%; and placebo, 31.8% but differences weren't significant between treatment groups (P = .119). Survival curves for times to onset of clinically important relief for the four treatment groups were not different ( P = .119). Subjects realizing definitive relief were cetiriazine, 65.2%; terfenadine, 45.5%; Loratadine, 31.8%; placebo, 27.3%; and astemizole, 22.7% (P = .023). Survival analysis of onset time for definitive relief found significant differences ( P = .010). The ranking was cetirizine to terfenadine to Loratadine to astemizole (quickest to slowest). Global evaluation based on subject willingness to take the medication again yielded percentages: cetirizine, 82.6%; terfenadine, 66.7%; astemizole, 63.6%; Loratadine, 40.9%; and placebo, 36.4% ( P = .036). Conclusion Cetirizine and terfenadine continuously ranked higher in terms of onset of action and efficacy, while Loratadine and astemizole ranked lower. Significance was detected in definitive relief and relative efficacy.
James H Day - One of the best experts on this subject based on the ideXlab platform.
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a four way double blind randomized placebo controlled study to determine the efficacy and speed of azelastine nasal spray versus Loratadine and cetirizine in adult subjects with allergen induced seasonal allergic rhinitis
Allergy Asthma & Clinical Immunology, 2013Co-Authors: James H Day, Anne K Ellis, Lisa M. Steacy, Yifei Zhu, Terry WalkerAbstract:Azelastine has been shown to be effective against seasonal allergic rhinitis (SAR). The Environmental Exposure Unit (EEU) is a validated model of experimental SAR. The objective of this double-blind, four-way crossover study was to evaluate the onset of action of azelastine nasal spray, versus the oral antihistamines Loratadine 10 mg and cetirizine 10 mg in the relief of the symptoms of SAR. 70 participants, aged 18-65, were randomized to receive azelastine nasal spray, cetirizine, Loratadine, or placebo after controlled ragweed pollen exposure in the EEU. Symptoms were evaluated using the total nasal symptom score (TNSS). The primary efficacy parameter was the onset of action as measured by the change from baseline in TNSS. Azelastine displayed a statistically significant improvement in TNSS compared with placebo at all time points from 15 minutes through 6 hours post dose. Azelastine, cetirizine, and Loratadine reduced TNSS compared to placebo with an onset of action of 15 (p < 0.001), 60 (p = 0.015), and 75 (p = 0.034) minutes, respectively. The overall assessment of efficacy was rated as good or very good by 46% of the participants for azelastine, 51% of the participants for cetirizine, and 30% of the participants for Loratadine compared to 18% of the participants for placebo. Azelastine’s onset of action for symptom relief was faster than that of cetirizine and Loratadine. The overall participant satisfaction in treatment with azelastine is comparable to cetirizine and statistically superior to Loratadine. These results suggest that azelastine may be preferential to oral antihistamines for the rapid relief of SAR symptoms.
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comparative onset of action and symptom relief with cetirizine Loratadine or placebo in an environmental exposure unit in subjects with seasonal allergic rhinitis confirmation of a test system
Annals of Allergy Asthma & Immunology, 2001Co-Authors: James H Day, Maureen P Briscoe, Elizabeth Rafeiro, Douglass Chapman, Benjamin KramerAbstract:Background The environmental exposure unit (EEU) is an instrument designed to determine onset of action of antiallergic treatment. Confirmation of test results would be useful in defining its role. Objective This study was intended to confirm a previous study comparing cetirizine, Loratadine, and placebo in the EEU using an identical protocol design (randomized, double-blind, parallel-group comparison having the same symptom scoring system, endpoints, and statistical analyses), thus demonstrating reproducibility of studies conducted in the EEU. Methods Onset of action and symptom relief with once-daily cetirizine 10 mg, Loratadine 10 mg, and placebo (n = 120 each group) were evaluated replicating a previous study design. Subjects meeting inclusion and exclusion criteria and qualifying symptom scores were randomized to 2 days' exposure (6 to 7 hours daily) with treatment. Changes in total and major symptom complex (TSC, MSC) scores based on 14 symptoms evaluated at 30-minute intervals served as primary efficacy variables. Results Onset of action again was earlier with cetirizine (at 1 hour, P ≤ 0.001) versus Loratadine (at 3 hours, P ≤ 0.01). Cetirizine produced a 25.4% least-square mean reduction in TSC scores overall versus an 11.2% decrease with Loratadine ( P = 0.006) and a 4.8% increase with placebo ( P P = 0.002). Similar changes were also noted in MSC scores. Cetirizine consistently reduced TSC and MSC scores after the first dose versus placebo ( P ≤ 0.001) and at most time points versus Loratadine ( P ≤ 0.05). Adverse events were reported in 1.7% of patients in each active-treatment group and in 2.5% on placebo. Conclusions Cetirizine acted earlier and was more effective than Loratadine or placebo in reducing symptoms of seasonal allergic rhinitis in subjects undergoing a controlled pollen challenge, replicating results from an earlier, identically designed study, demonstrating reproducibility of these assessments by the EEU.
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onset of action and efficacy of terfenadine astemizole cetirizine and Loratadine for the relief of symptoms of allergic rhinitis
Annals of Allergy Asthma & Immunology, 1997Co-Authors: James H Day, Maureen P Briscoe, Reginald H Clark, Anne K Ellis, Pierre GervaisAbstract:Background Terfenadine, astemizole, cetirizine, and Loratadine are compared in their abilities to produce relief of symptoms of allergic rhinitis. Objective The aim of this study was to compare the onset of action and efficacy of the study medications. Methods One hundred eleven ragweed-sensitive subjects were primed with pollen in the Environmental Exposure Unit. Study entry required adequate symptoms over a 3-hour exposure to 5,000 ± 300 grains/m 3 of ragweed pollen. On the test day, subjects were given a single dose of either terfenadine 60 mg (22), astemizole 10 mg (22), cetirizine 10 mg (23), Loratadine 10 mg (22), or placebo (22) when sufficiently symptomatic after a 60-minute exposure. Allergen levels were maintained and symptoms recorded every 30 minutes. Results Proportions of subjects with clinically important relief were cetirizine, 69.6%; terfenadine, 54.5%; Loratadine, 50.0% astemizole, 40.9%; and placebo, 31.8% but differences weren't significant between treatment groups (P = .119). Survival curves for times to onset of clinically important relief for the four treatment groups were not different ( P = .119). Subjects realizing definitive relief were cetiriazine, 65.2%; terfenadine, 45.5%; Loratadine, 31.8%; placebo, 27.3%; and astemizole, 22.7% (P = .023). Survival analysis of onset time for definitive relief found significant differences ( P = .010). The ranking was cetirizine to terfenadine to Loratadine to astemizole (quickest to slowest). Global evaluation based on subject willingness to take the medication again yielded percentages: cetirizine, 82.6%; terfenadine, 66.7%; astemizole, 63.6%; Loratadine, 40.9%; and placebo, 36.4% ( P = .036). Conclusion Cetirizine and terfenadine continuously ranked higher in terms of onset of action and efficacy, while Loratadine and astemizole ranked lower. Significance was detected in definitive relief and relative efficacy.
Anna Puigdemont - One of the best experts on this subject based on the ideXlab platform.
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in vitro inhibitory effect of rupatadine on histamine and tnf alpha release from dispersed canine skin mast cells and the human mast cell line hmc 1
Inflammation Research, 2000Co-Authors: Mireia Queralt, Manuel Merlos, Pilar Brazis, F De Mora, Anna PuigdemontAbstract:Objective and design: To examine the inhibitory potential of rupatadine, a new H1-antihistamine and anti-PAF agent, on histamine and TNF-α release. Comparison with an H1-antihistamine (Loratadine) and a PAF-antagonist (SR-27417A).¶Material: Dispersed canine skin mast cells were used to assess the effect of the drugs tested on FceRI-dependent and -independent histamine release; the human HMC-1 cell line was used to study TNF-α release.¶Treatment and methods: Before stimulation mast cell populations were treated with increasing concentrations of rupatadine, Loratadine and SR-27417A. Histamine and TNF-α release were measured following 15-30 min and 3 h activation, respectively.¶Results: The IC50 for rupatadine in A23187, concanavalin A and anti-IgE induced histamine release was 0.7 ± 0.4 μM, 3.2 ± 0.7μM and 1.5 ± 0.4 μM, respectively whereas for Loratadine the IC50 was 2.1 ± 0.9 μM, 4.0 ± 1.3 M and 1.7 ± 0.5 μM. SR-27417A exhibited no inhibitory effect. Rupatadine, Loratadine and SR-27417A inhibited TNF-α release with IC50 2.0 ± 0.9 μM, 2.1 ± 1.1 M and 4.3 ± 0.6 μM, respectively.¶Conclusions: Rupatadine and Loratadine showed similar inhibitory effect on histamine and TNF-α release, whereas SR-27417A only exhibited inhibitory effect against TNF-α.
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in vitro inhibitory effect of rupatadine on histamine and tnf α release from dispersed canine skin mast cells and the human mast cell line hmc 1
Inflammation Research, 2000Co-Authors: Mireia Queralt, Manuel Merlos, Pilar Brazis, F De Mora, Anna PuigdemontAbstract:Objective and design: To examine the inhibitory potential of rupatadine, a new H1-antihistamine and anti-PAF agent, on histamine and TNF-α release. Comparison with an H1-antihistamine (Loratadine) and a PAF-antagonist (SR-27417A).¶Material: Dispersed canine skin mast cells were used to assess the effect of the drugs tested on FceRI-dependent and -independent histamine release; the human HMC-1 cell line was used to study TNF-α release.¶Treatment and methods: Before stimulation mast cell populations were treated with increasing concentrations of rupatadine, Loratadine and SR-27417A. Histamine and TNF-α release were measured following 15-30 min and 3 h activation, respectively.¶Results: The IC50 for rupatadine in A23187, concanavalin A and anti-IgE induced histamine release was 0.7 ± 0.4 μM, 3.2 ± 0.7μM and 1.5 ± 0.4 μM, respectively whereas for Loratadine the IC50 was 2.1 ± 0.9 μM, 4.0 ± 1.3 M and 1.7 ± 0.5 μM. SR-27417A exhibited no inhibitory effect. Rupatadine, Loratadine and SR-27417A inhibited TNF-α release with IC50 2.0 ± 0.9 μM, 2.1 ± 1.1 M and 4.3 ± 0.6 μM, respectively.¶Conclusions: Rupatadine and Loratadine showed similar inhibitory effect on histamine and TNF-α release, whereas SR-27417A only exhibited inhibitory effect against TNF-α.
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inhibitory effects of rupatadine on mast cell histamine release and skin wheal development induced by ascaris suum in hypersensitive dogs
Drug Development Research, 1998Co-Authors: Mireia Queralt, Manuel Merlos, Pilar Brazis, Anna PuigdemontAbstract:The present studies were performed to compare the cutaneous antiallergic effects of rupatadine, a new potent dual antagonist of histamine and platelet-activating factor (PAF), with those of Loratadine (an H1-antihistamine) and SR-27417A (a PAF antagonist). Two experimental models were used: an in vivo skin challenge by Ascaris suum extract administered intradermically in conscious hypersensitive dogs and an in vitro assay of Asc S 1 antigen-induced histamine release from isolated canine skin mast cells. In antigen-induced skin inflammation, both rupatadine and Loratadine administered orally inhibited wheal formation in a dose-dependent manner at the studied doses. At the 0.1 mg/kg dose, maximum inhibition values for rupatadine and Loratadine were similar, but the effect of rupatadine lasted 24 h, whereas Loratadine's effect disappeared after 8 h. At the 1 mg/kg dose, the two compounds behaved similarly, with maximum effects of about 65% (4 h after treatment) and activity lasting more than 24 h in both cases. At the 10 mg/kg dose, rupatadine and Loratadine exhibited maximum effects of 84 and 64% in wheal inhibition 2 and 4 h after drug administration, respectively. SR-27417A did not inhibit ascaris-induced wheal at the doses studied (1 and 10 mg/kg p.o.). In isolated canine skin mast cells, rupatadine and Loratadine inhibited antigen-induced histamine release in a concentration-dependent manner. Rupatadine was more potent than Loratadine at each concentration studied (100 nM–30 μM). Maximum inhibitory effects were 83 and 67% for rupatadine and Loratadine, respectively, after a 30 μM concentration. Rupatadine, with an IC50 value of 5.3 μM, was about fourfold more potent than Loratadine, with an IC50 value of 19 μM. SR-27417A exhibited no effect in our experimental model. Moreover, neither Loratadine or rupatadine showed cytotoxic or prodegranulating effects at any concentration, whereas SR-27417A was cytotoxic at the highest concentration (30 μM). Thus, rupatadine is effective in controlling inflammatory reactions in dog skin and the effect may be partly due to its modulation of mast cell degranulation, but not to its PAF-antagonist properties. Drug Dev. Res. 44:49–55, 1998. © 1998 Wiley-Liss, Inc.
Mark W. Tenn - One of the best experts on this subject based on the ideXlab platform.
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onset of action for Loratadine tablets for the symptomatic control of seasonal allergic rhinitis in adults challenged with ragweed pollen in the environmental exposure unit a post hoc analysis of total symptom score
Allergy Asthma & Clinical Immunology, 2018Co-Authors: Anne K Ellis, Mark W. Tenn, Lisa M. Steacy, Charlene C NgAbstract:Loratadine is a second-generation, non-sedating antihistamine used for the relief of allergic rhinitis symptoms. Previous studies reported that when Loratadine was encapsulated, the onset of action for symptom relief was 180 min. However, unmodified Loratadine tablets were not evaluated at that time. Using data from a previously published Environmental Exposure Unit (EEU) study comparing azelastine nasal spray with Loratadine tablets, cetirizine tablets, and placebo, this post hoc analysis determines the onset of action of Loratadine tablets (i.e. unmodified) by analyzing the total symptom score for the relief of nasal and ocular seasonal allergic rhinitis (SAR) symptoms. A Phase IV, randomized, single-center, double-blind, placebo-controlled, double-dummy, four-way crossover study was conducted in the EEU. Seventy participants were randomized sequentially into one of the four treatments during ragweed pollen exposure. Nasal and ocular symptom scores were self-reported by the participants and recorded. The original study analysis was carried out by evaluating the nasal symptom scores only. For this post hoc analysis, both nasal and ocular data from the Loratadine and placebo treatment arms were analyzed. The primary endpoint for this analysis was the onset of action of Loratadine as measured by the change in total symptom score (TSS) from baseline in comparison to placebo. The onset of ocular symptom relief using the total ocular symptom score (TOSS) was also reported. Loratadine tablets demonstrated a significant and durable improvement in both TSS (P = .005) and TOSS (P = .013) at 75 min post-treatment administration compared to placebo. The mean proportion of participants reporting none or mild for all component symptoms of TSS and TOSS at 75 min and thereafter was significantly higher in the Loratadine (TSS, P = .0005; TOSS, P ≤ .0001) vs. placebo treatment arm. The onset of action of Loratadine tablets was 75 min for the relief of nasal and ocular symptoms in adults with SAR. These results suggest a faster onset of action for Loratadine tablets (75 min) compared to previously reported studies which were conducted with modified (i.e. gelatin-encapsulated) Loratadine tablets (180 min). Trial registration Clinicaltrials.gov identifier NCT00561717
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Onset of action for Loratadine tablets for the symptomatic control of seasonal allergic rhinitis in adults challenged with ragweed pollen in the Environmental Exposure Unit: a post hoc analysis of total symptom score
BMC, 2018Co-Authors: Mark W. Tenn, Lisa M. Steacy, Anne K EllisAbstract:Abstract Background Loratadine is a second-generation, non-sedating antihistamine used for the relief of allergic rhinitis symptoms. Previous studies reported that when Loratadine was encapsulated, the onset of action for symptom relief was 180 min. However, unmodified Loratadine tablets were not evaluated at that time. Using data from a previously published Environmental Exposure Unit (EEU) study comparing azelastine nasal spray with Loratadine tablets, cetirizine tablets, and placebo, this post hoc analysis determines the onset of action of Loratadine tablets (i.e. unmodified) by analyzing the total symptom score for the relief of nasal and ocular seasonal allergic rhinitis (SAR) symptoms. Methods A Phase IV, randomized, single-center, double-blind, placebo-controlled, double-dummy, four-way crossover study was conducted in the EEU. Seventy participants were randomized sequentially into one of the four treatments during ragweed pollen exposure. Nasal and ocular symptom scores were self-reported by the participants and recorded. The original study analysis was carried out by evaluating the nasal symptom scores only. For this post hoc analysis, both nasal and ocular data from the Loratadine and placebo treatment arms were analyzed. The primary endpoint for this analysis was the onset of action of Loratadine as measured by the change in total symptom score (TSS) from baseline in comparison to placebo. The onset of ocular symptom relief using the total ocular symptom score (TOSS) was also reported. Results Loratadine tablets demonstrated a significant and durable improvement in both TSS (P = .005) and TOSS (P = .013) at 75 min post-treatment administration compared to placebo. The mean proportion of participants reporting none or mild for all component symptoms of TSS and TOSS at 75 min and thereafter was significantly higher in the Loratadine (TSS, P = .0005; TOSS, P ≤ .0001) vs. placebo treatment arm. Conclusions The onset of action of Loratadine tablets was 75 min for the relief of nasal and ocular symptoms in adults with SAR. These results suggest a faster onset of action for Loratadine tablets (75 min) compared to previously reported studies which were conducted with modified (i.e. gelatin-encapsulated) Loratadine tablets (180 min). Trial registration Clinicaltrials.gov identifier NCT0056171
Mireia Queralt - One of the best experts on this subject based on the ideXlab platform.
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in vitro inhibitory effect of rupatadine on histamine and tnf alpha release from dispersed canine skin mast cells and the human mast cell line hmc 1
Inflammation Research, 2000Co-Authors: Mireia Queralt, Manuel Merlos, Pilar Brazis, F De Mora, Anna PuigdemontAbstract:Objective and design: To examine the inhibitory potential of rupatadine, a new H1-antihistamine and anti-PAF agent, on histamine and TNF-α release. Comparison with an H1-antihistamine (Loratadine) and a PAF-antagonist (SR-27417A).¶Material: Dispersed canine skin mast cells were used to assess the effect of the drugs tested on FceRI-dependent and -independent histamine release; the human HMC-1 cell line was used to study TNF-α release.¶Treatment and methods: Before stimulation mast cell populations were treated with increasing concentrations of rupatadine, Loratadine and SR-27417A. Histamine and TNF-α release were measured following 15-30 min and 3 h activation, respectively.¶Results: The IC50 for rupatadine in A23187, concanavalin A and anti-IgE induced histamine release was 0.7 ± 0.4 μM, 3.2 ± 0.7μM and 1.5 ± 0.4 μM, respectively whereas for Loratadine the IC50 was 2.1 ± 0.9 μM, 4.0 ± 1.3 M and 1.7 ± 0.5 μM. SR-27417A exhibited no inhibitory effect. Rupatadine, Loratadine and SR-27417A inhibited TNF-α release with IC50 2.0 ± 0.9 μM, 2.1 ± 1.1 M and 4.3 ± 0.6 μM, respectively.¶Conclusions: Rupatadine and Loratadine showed similar inhibitory effect on histamine and TNF-α release, whereas SR-27417A only exhibited inhibitory effect against TNF-α.
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in vitro inhibitory effect of rupatadine on histamine and tnf α release from dispersed canine skin mast cells and the human mast cell line hmc 1
Inflammation Research, 2000Co-Authors: Mireia Queralt, Manuel Merlos, Pilar Brazis, F De Mora, Anna PuigdemontAbstract:Objective and design: To examine the inhibitory potential of rupatadine, a new H1-antihistamine and anti-PAF agent, on histamine and TNF-α release. Comparison with an H1-antihistamine (Loratadine) and a PAF-antagonist (SR-27417A).¶Material: Dispersed canine skin mast cells were used to assess the effect of the drugs tested on FceRI-dependent and -independent histamine release; the human HMC-1 cell line was used to study TNF-α release.¶Treatment and methods: Before stimulation mast cell populations were treated with increasing concentrations of rupatadine, Loratadine and SR-27417A. Histamine and TNF-α release were measured following 15-30 min and 3 h activation, respectively.¶Results: The IC50 for rupatadine in A23187, concanavalin A and anti-IgE induced histamine release was 0.7 ± 0.4 μM, 3.2 ± 0.7μM and 1.5 ± 0.4 μM, respectively whereas for Loratadine the IC50 was 2.1 ± 0.9 μM, 4.0 ± 1.3 M and 1.7 ± 0.5 μM. SR-27417A exhibited no inhibitory effect. Rupatadine, Loratadine and SR-27417A inhibited TNF-α release with IC50 2.0 ± 0.9 μM, 2.1 ± 1.1 M and 4.3 ± 0.6 μM, respectively.¶Conclusions: Rupatadine and Loratadine showed similar inhibitory effect on histamine and TNF-α release, whereas SR-27417A only exhibited inhibitory effect against TNF-α.
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inhibitory effects of rupatadine on mast cell histamine release and skin wheal development induced by ascaris suum in hypersensitive dogs
Drug Development Research, 1998Co-Authors: Mireia Queralt, Manuel Merlos, Pilar Brazis, Anna PuigdemontAbstract:The present studies were performed to compare the cutaneous antiallergic effects of rupatadine, a new potent dual antagonist of histamine and platelet-activating factor (PAF), with those of Loratadine (an H1-antihistamine) and SR-27417A (a PAF antagonist). Two experimental models were used: an in vivo skin challenge by Ascaris suum extract administered intradermically in conscious hypersensitive dogs and an in vitro assay of Asc S 1 antigen-induced histamine release from isolated canine skin mast cells. In antigen-induced skin inflammation, both rupatadine and Loratadine administered orally inhibited wheal formation in a dose-dependent manner at the studied doses. At the 0.1 mg/kg dose, maximum inhibition values for rupatadine and Loratadine were similar, but the effect of rupatadine lasted 24 h, whereas Loratadine's effect disappeared after 8 h. At the 1 mg/kg dose, the two compounds behaved similarly, with maximum effects of about 65% (4 h after treatment) and activity lasting more than 24 h in both cases. At the 10 mg/kg dose, rupatadine and Loratadine exhibited maximum effects of 84 and 64% in wheal inhibition 2 and 4 h after drug administration, respectively. SR-27417A did not inhibit ascaris-induced wheal at the doses studied (1 and 10 mg/kg p.o.). In isolated canine skin mast cells, rupatadine and Loratadine inhibited antigen-induced histamine release in a concentration-dependent manner. Rupatadine was more potent than Loratadine at each concentration studied (100 nM–30 μM). Maximum inhibitory effects were 83 and 67% for rupatadine and Loratadine, respectively, after a 30 μM concentration. Rupatadine, with an IC50 value of 5.3 μM, was about fourfold more potent than Loratadine, with an IC50 value of 19 μM. SR-27417A exhibited no effect in our experimental model. Moreover, neither Loratadine or rupatadine showed cytotoxic or prodegranulating effects at any concentration, whereas SR-27417A was cytotoxic at the highest concentration (30 μM). Thus, rupatadine is effective in controlling inflammatory reactions in dog skin and the effect may be partly due to its modulation of mast cell degranulation, but not to its PAF-antagonist properties. Drug Dev. Res. 44:49–55, 1998. © 1998 Wiley-Liss, Inc.
