The Experts below are selected from a list of 252 Experts worldwide ranked by ideXlab platform
Keith J. Simons - One of the best experts on this subject based on the ideXlab platform.
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Hydroxyzine from topical phospholipid liposomal formulations: Evaluation of peripheral antihistaminic activity and systemic absorption in a rabbit model
AAPS PharmSci, 2003Co-Authors: Abeer A W Elzainy, F. Estelle R. Simons, Xiaochen Gu, Keith J. SimonsAbstract:Hydroxyzine, an effective but sedating H_1-antihistamine is given orally to treat allergic skin disorders. This study was performed to assess the peripheral H_1-antihistaminic activity and extent of systemic absorption of Hydroxyzine from liposomes applied to the skin. Using L-α-phosphatidylcholine (PC), small unilamellar vesicles (SUVs) and multilamellar vesicles (MLVs) containing Hydroxyzine were prepared. Hydroxyzine in Glaxal Base (GB) was used as the control. Using a randomized, crossover design, each formulation, containing 10 mg of Hydroxyzine, was applied to the shaved backs of 6 rabbits (3.08±0.05 kg). Histamine-induced wheal tests and blood sampling were performed at designated time intervals up to 24 hours. Compared with baseline, Hydroxyzine from all formulations significantly suppressed histamine-induced wheal formation by 75% to 95% for up to 24 hours. Mean maximum suppression, 85% to 94%, occurred from 2 to 6 hours, with no differences among the formulations. The areas of plasma Hydroxyzine concentration versus time area under the curve (AUCs) from PC-SUV and PC-MLV, 80.1±20.8 and 78.4±33.9 ng/mL/h, respectively, were lower than that from GB, 492±141 ng/mL/h ( P
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Hydroxyzine from topical phospholipid liposomal formulations evaluation of peripheral antihistaminic activity and systemic absorption in a rabbit model
Aaps Pharmsci, 2003Co-Authors: Abeer A W Elzainy, Xiaochen Gu, Estelle F R Simons, Keith J. SimonsAbstract:Hydroxyzine, an effective but sedating H1-antihistamine is given orally to treat allergic skin disorders. This study was performed to assess the peripheral H1-antihistaminic activity and extent of systemic absorption of Hydroxyzine from liposomes applied to the skin. Using L-α-phosphatidylcholine (PC), small unilamellar vesicles (SUVs) and multilamellar vesicles (MLVs) containing Hydroxyzine were prepared. Hydroxyzine in Glaxal Base (GB) was used as the control. Using a randomized, crossover design, each formulation, containing 10 mg of Hydroxyzine, was applied to the shaved backs of 6 rabbits (3.08±0.05 kg). Histamine-induced wheal tests and blood sampling were performed at designated time intervals up to 24 hours. Compared with baseline, Hydroxyzine from all formulations significantly suppressed histamine-induced wheal formation by 75% to 95% for up to 24 hours. Mean maximum suppression, 85% to 94%, occurred from 2 to 6 hours, with no differences among the formulations. The areas of plasma Hydroxyzine concentration versus time area under the curve (AUCs) from PC-SUV and PC-MLV, 80.1±20.8 and 78.4±33.9 ng/mL/h, respectively, were lower than that from GB, 492±141 ng/mL/h (P<.05) over 24 hours. Plasma concentrations of cetirizine arising in-vivo as the active metabolite of Hydroxyzine, from PC-SUV, PC-MLV, and GB, were similar with AUCs of 765±50, 1035±202, and 957±227 ng/mL/h, respectively (P<.05). Only 0.02% to 0.06% of the initial Hydroxyzine dose remained on the skin after 24 hours. In this model, Hydroxyzine from SUV and MLV had excellent topical H1-antihistaminic activity, and minimal systemic exposure occurred. Cetirizine formed in-vivo contributed to some of H1-antihistaminic activity.
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effect of the h2 antagonist cimetidine on the pharmacokinetics and pharmacodynamics of the h1 antagonists Hydroxyzine and cetirizine in patients with chronic urticaria
The Journal of Allergy and Clinical Immunology, 1995Co-Authors: Estelle F R Simons, Gordon Sussman, Keith J. SimonsAbstract:Abstract Background: Concomitant administration of an H 1 -receptor antagonist with an H 2 -receptor antagonist may enhance the wheal and flare suppression produced by the H 1 -antagonist. This synergism may be due, at least in part, to a pharmacokinetic effect. Methods: In a randomized, double-blind, parallel-group study in 16 patients with chronic urticaria, we investigated the pharmacokinetics and suppressive effect on the histamine-induced wheal and flare of a single dose of Hydroxyzine 25 mg or cetirizine 10 mg, given before and after treatment with cimetidine 600 mg every 12 hours for 10 days. Results: When Hydroxyzine was administered with cimetidine, the partial Hydroxyzine area under the curve increased significantly ( p 0.05). When cetirizine was administered with cimetidine, the pharmacokinetics of cetirizine did not change significantly, and no enhancement of wheal and flare suppression was observed. Conclusions: In this study co-administration of Hydroxyzine with cimetidine resulted in significantly increased serum Hydroxyzine concentrations and increased wheal and flare suppression, thus confirming the rationale for a trial of concomitant administration of these medications in some patients with chronic urticaria unresponsive to treatment with an H 1 -antagonist alone. We found no therapeutic rationale for co-administration of cetirizine with cimetidine in urticaria treatment. These medications may be co-administered safely without fear of medication interaction. (J ALLERGY CLIN IMMUNOL 1995;95:685-93.)
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Effect of the H2-receptor antagonist cimetidine, on the pharmacokinetics and pharmacodynamics of the H1-receptor antagonists Hydroxyzine and cetirizine in rabbits.
Pharmaceutical Research, 1994Co-Authors: Xueyu Chen, F. Estelle R. Simons, Keith J. SimonsAbstract:The effects of coadministration of the H2-receptor antagonist cimetidine on the pharmacokinetics and pharmacodynamics of the H1 receptor antagonists Hydroxyzine and cetirizine were studied in rabbits. A single dose of Hydroxyzine, 10 mg (Experiment A), or cetirizine, 10 mg (Experiment B), was given intravenously on three occasions: 2 weeks before cimetidine administration, after cimetidine, 100 mg/kg, had been given every 12 hr for 1 week, and 2 weeks after the cimetidine was discontinued. Serum concentrations of Hydroxyzine and cetirizine, the active metabolite of Hydroxyzine arising in vivo (Experiment A), or cetirizine (Experiment B) were measured by HPLC. The pharmacologic effects of Hydroxyzine and cetirizine were monitored by measuring the suppression of histamine-induced wheals, using an IBM-PC and digitizer. The Hydroxyzine and cetrizine half-life and AUG0→∞ values were significantly increased and the systemic clearance rates were significantly decreased in the presence of cimetidine. Similar results were obtained when cetirizine was administered de novo. Wheal suppression produced by Hydroxyzine or cetirizine was increased and prolonged in the presence of cimetidine. The synergism observed between Hydroxyzine or cetirizine and cimetidine in suppression of the histamine-induced cutaneous response may be due to a pharmacokinetic interaction.
Michael Bigby - One of the best experts on this subject based on the ideXlab platform.
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urticaria clinical efficacy of cetirizine in comparison with Hydroxyzine and placebo
The Journal of Allergy and Clinical Immunology, 1990Co-Authors: James Kalivas, Debra L Breneman, Michael D Tharp, Suzanne Bruce, Michael BigbyAbstract:Chronic urticaria is a problem for both physician and patient. In an effort to avoid the risks associated with corticosteroid treatment, many first-generation H 1 -receptor antagonists have been tried and found to induce undesirable levels of sedation when given in amounts sufficient to control urticaria. Cetirizine, a pharmacologically active oxidized metabolite of Hydroxyzine, was developed to provide selective H 1 -receptor inhibition without depression of the central nervous system. In a 4-week, multicenter, double-blind, placebo-controlled safety and efficacy study, cetirizine, in a once-a-day dose (5 to 20 mg), was equivalent in efficacy to Hydroxyzine in divided doses (25 to 75 mg/day). The incidence of somnolence in the cetirizine group was not significantly different from that of the placebo group. However, in the Hydroxyzine group, the incidence of somnolence was significantly higher than that in the placebo group ( p =0.001). The results of this study demonstrate that cetirizine has a greater safety margin over the older parent drug Hydroxyzine.
James Kalivas - One of the best experts on this subject based on the ideXlab platform.
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relative efficacy and safety of loratadine Hydroxyzine and placebo in chronic idiopathic urticaria
Drug Research, 1992Co-Authors: E W Monroe, James Kalivas, D I Bernstein, S V Grabiec, R W Honsinger, H I Katz, F Cuss, M R Danzig, P R GarvinAbstract:Abstract The efficacy and safety of a new non-sedating antihistamine, loratadine (Clarityn, CAS 79794-75-5) 10 mg q.d., was compared to the classical antihistamine, Hydroxyzine 25 mg t.i.d. and placebo in a 4-week (optional 12 week) randomized, double-blind, multi-center study in 203 patients with chronic idiopathic urticaria. Efficacy evaluations included weekly physician and patient assessments of pruritus, overall disease condition, and therapeutic response to treatment. Loratadine and Hydroxyzine were significantly more effective than placebo and clinically comparable to each other as measured by all efficacy evaluations at each visit. Loratadine was safe and well tolerated with sedation and dry mouth similar to placebo and significantly less than Hydroxyzine.
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urticaria clinical efficacy of cetirizine in comparison with Hydroxyzine and placebo
The Journal of Allergy and Clinical Immunology, 1990Co-Authors: James Kalivas, Debra L Breneman, Michael D Tharp, Suzanne Bruce, Michael BigbyAbstract:Chronic urticaria is a problem for both physician and patient. In an effort to avoid the risks associated with corticosteroid treatment, many first-generation H 1 -receptor antagonists have been tried and found to induce undesirable levels of sedation when given in amounts sufficient to control urticaria. Cetirizine, a pharmacologically active oxidized metabolite of Hydroxyzine, was developed to provide selective H 1 -receptor inhibition without depression of the central nervous system. In a 4-week, multicenter, double-blind, placebo-controlled safety and efficacy study, cetirizine, in a once-a-day dose (5 to 20 mg), was equivalent in efficacy to Hydroxyzine in divided doses (25 to 75 mg/day). The incidence of somnolence in the cetirizine group was not significantly different from that of the placebo group. However, in the Hydroxyzine group, the incidence of somnolence was significantly higher than that in the placebo group ( p =0.001). The results of this study demonstrate that cetirizine has a greater safety margin over the older parent drug Hydroxyzine.
Serge Brand - One of the best experts on this subject based on the ideXlab platform.
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comparing the effect of prazosin and Hydroxyzine on sleep quality in patients suffering from posttraumatic stress disorder
Neuropsychobiology, 2014Co-Authors: Mohammad Ahmadpanah, Parasto Sabzeiee, Seyed Mohammad Hosseini, Saadat Torabian, Mohammad Haghighi, Leila Jahangard, Hafez Bajoghli, Edith Holsboertrachsler, Serge BrandAbstract:Objectives: In light of the high prevalence of sleep disorders in patients suffering from posttraumatic stress disorder (PTSD), this study sought to compare the effect of prazosin and Hydroxyzine on sleep quality in this patient group. Methods: A total of 100 patients suffering from PTSD were assessed (mean age = 35.51 years, SD = 6.41; 28% females). Next, they were randomly assigned to one of three treatment groups: prazosin (33 patients), Hydroxyzine (34 patients) or placebo (33 patients). The trial lasted for 8 weeks. The patients' sleep quality was assessed using the Pittsburgh Sleep Quality Index. Items taken from the Mini International Neuropsychiatric Interview were used to operationalize PTSD. Results: Compared to controls, patients treated with prazosin and Hydroxyzine reported improved sleep and less nightmares. Improvement was greatest in patients treated with prazosin compared to Hydroxyzine and placebo. Improvement in sleep was associated with an amelioration of their PTSD symptoms. Conclusion: Both prazosin and Hydroxyzine can be used to treat psychopharmacological sleep disorders and nightmares in patients suffering from PTSD, also leading to reductions in PTSD symptoms.
E W Monroe - One of the best experts on this subject based on the ideXlab platform.
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relative efficacy and safety of loratadine Hydroxyzine and placebo in chronic idiopathic urticaria
Drug Research, 1992Co-Authors: E W Monroe, James Kalivas, D I Bernstein, S V Grabiec, R W Honsinger, H I Katz, F Cuss, M R Danzig, P R GarvinAbstract:Abstract The efficacy and safety of a new non-sedating antihistamine, loratadine (Clarityn, CAS 79794-75-5) 10 mg q.d., was compared to the classical antihistamine, Hydroxyzine 25 mg t.i.d. and placebo in a 4-week (optional 12 week) randomized, double-blind, multi-center study in 203 patients with chronic idiopathic urticaria. Efficacy evaluations included weekly physician and patient assessments of pruritus, overall disease condition, and therapeutic response to treatment. Loratadine and Hydroxyzine were significantly more effective than placebo and clinically comparable to each other as measured by all efficacy evaluations at each visit. Loratadine was safe and well tolerated with sedation and dry mouth similar to placebo and significantly less than Hydroxyzine.
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relative efficacy and safety of loratadine Hydroxyzine and placebo in chronic idiopathic urticaria and atopic dermatitis
Clinical Therapeutics, 1992Co-Authors: E W MonroeAbstract:The subjects of this double-blind study were 59 patients with chronic idiopathic urticaria or atopic dermatitis randomly assigned to receive 10 mg of loratadine once daily and placebo twice daily (n = 20), 25 mg of Hydroxyzine thrice daily (n = 20), or placebo thrice daily (n = 19). The patients (15 men, 44 women) were aged 18 to 65 years. Among the 18 patients with urticaria and 41 with atopic dermatitis, daily symptom scores decreased 43% and 57% in those receiving loratadine, 47% and 38% in those receiving Hydroxyzine, and 0% and 33% in the placebo patients. The difference between the treated and placebo patients was significant among the urticaria patients. According to a global evaluation of treatment effects, more treated than placebo patients reported marked or complete symptom relief; among the patients with atopic dermatitis, the difference was significant between the loratadine and placebo patients. Somnolence or sedation during treatment was reported by one of the patients receiving loratadine, by eight of the Hydroxyzine patients, and by two of the placebo patients; the difference between the loratadine and Hydroxyzine patients was significant. It was concluded that loratadine is as effective as Hydroxyzine in the treatment of urticaria and demonstrates a significant antipruritic effect in atopic dermatitis, but does not have the central nervous system effects of Hydroxyzine.