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Allergic rhinitis (AR) is a common debilitating disorder that can adversely affect the quality of life and the academic performance of school-age children. Symptoms during the day can hamper concentration and lead to learning problems. Nocturnal symptoms can cause sleep loss and secondary daytime fatigue, further undermining a child's ability to function well during the school day Oral antihistamines are the foundation of pharmacologic therapy, but there are important differences between the agents.
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Topical application of the antihistamines commonly leads to sensitization for patients, but skin reactions provoked by their systemic use are very rare. The antihistamines cetirizine and hydroxyzine are piperazine derivatives, on the structural basis of an ethylenediamine, but the cross-reactions between the 2 have rarely been reported. A 44-year-old man visited because of the generalized morbilliform eruptions with pruritus over his whole body, after intake of hydroxyzine (Ucerax) and azelastine (Azeptine), administered during a 2-day period for chronic urticaria. Previously, he had presented the same cutaneous reactions after oral administration of cetirizine (Lotec). Oral challenge tests performed with cetirizine and hydroxyzine led to the same cutaneous reactions. He was given the diagnosis of drug eruption from cetirizine and hydroxyzine, which suggests that there were cross-reactions among cetirizine, hydroxyzine, and ethylenediamine.
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To evaluate the effect and safety of acupuncture therapy on patients with moderate to severe allergic rhinitis.
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We are interested in understanding the pathogenesis of the cutaneous IgE-mediated late phase reaction. A double-blind, placebo-controlled, randomized cross-over study with 10 subjects of the effect of the non-sedating antihistamine, terfenadine (Selddane), on the cutaneous reaction to antigen (ragweed or mixed grass) administered intradermally and over denuded blister bases was performed. The activity of terfenadine on anti-IgE-induced mediator release from the skin mast cell, lung mast cell and basophil was also examined in vitro. Terfenadine significantly inhibited the size of the cutaneous reaction at every hour between hours 1 and 9 (hr 9, control 2250 +/- 500 mm2 vs drug 1250 +/- 250 mm2, P < 0.01, n = 10) and showed some inhibitory effect at hours 10-12. While terfenadine blocks histamine release after nasal antigen challenge the release of mediators at skin blister sites was unaffected. The infiltration of leucocytes into the blister supernatant was unaffected by terfenadine although previous studies have shown significant inhibition with another antihistamine, cetirizine. In vitro, terfenadine, like other antihistamines, was found to have inhibitory activity on anti-IgE-induced mediator release at concentrations of 10(-4)-10(-5) M in lung and skin mast cells and basophils. We conclude that the effects of the newer antihistamines on cellular movement into the skin may be diverse, that terfenadine may show organ specificity in vivo and that terfenadine significantly decreases both the early and late gross inflammatory response of the skin to antigen. We cannot, as yet, explain the mechanism(s) by which this occurs.
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Three hundred seven patients were randomized to treatment, and 299 completed 2 weeks of study treatment. The age of the population ranged from 12 to 74 years (mean, 35 years), 62.9% were female, and 69.6% were white. Over 2 weeks of treatment, both groups had significant improvements in the TNSS compared with baseline (P < 0.001). The overall change in TNSS was significantly greater with azelastine nasal spray compared with cetirizine (29.3% vs 23.0% improvement, respectively; P = 0.015). In terms of onset of action, azelastine nasal spray significantly improved the instantaneous TNSS compared with cetirizine at 60 and 240 minutes after the initial dose (both, P = 0.040). Scores on each domain of the RQLQ were significantly improved in both groups compared with baseline (P < 0.001); the overall RQLQ score was significantly improved with azelastine nasal spray compared with cetirizine (P = 0.049). Both treatments were well tolerated.
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A 5-year-old girl with insulin-dependent diabetes mellitus (IDDM) developed progressive reactions to insulin and was found to have positive intradermal skin tests to regular and NPH insulin. Addition of oral antihistamine and co-administration of subcutaneous dexamethasone along with the insulin failed to control her symptoms. The patient was therefore hospitalized and desensitized to insulin using an insulin pump and insulin lispro.
Based on the evidence that cetirizine is a commonly employed active comparator drug in AR, it is tempting to suggest that cetirizine may be a suitable benchmark in the development of novel pharmacotherapies for AR.
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Monitoring the hemodynamic responses within tissues that are associated with mast cell degranulation provides additional insight into the evolution of the acute inflammatory response and offers a unique approach to assess the effectiveness of treatment intervention.
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Recently, airway fibroblasts captured the attention of both allergists and basic scientists since they are no longer considered as mere bystanders, as far as allergic airway diseases are concerned. The aim of the present study was to assess the effects of different Cetirizine (Cet) concentrations (0.01, 0.05, 0.1 mg/ml) on human airway fibroblast proliferation and on CD54 expression. By means of flow cytometry analysis, we evaluated CD54 expression by airway fibroblasts in basal conditions or after gammaIFN stimulation in the presence of Cetirizine; we also evaluated the effect of the drug on cell proliferation by a [3H]thymidine incorporation assay. All of the tested doses of Cetirizine were able to significantly reduce CD54 upregulation induced by gammaIFN; concerning the fibroblast proliferation, we observed a dose-dependent inhibition of [3H]thymidine incorporation. These results show that Cetirizine exerts a biologic effect directly on human airway fibroblasts, suggesting a new rationale in the use of this compound.
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Twice-daily intranasal azelastine offers an effective and well tolerated alternative to other antihistamine agents currently recommended for the symptomatic relief of mild to severe SAR and PAR in adults and children (aged > or = 12 years in the US; aged > or = 6 years in some European countries including the UK). The rapid onset, confined topical activity and reduced sedation demonstrated by the intranasal formulation of azelastine may offer an advantage over other antihistamine agents, although this has yet to be confirmed.
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The aim was to determine the effect of H1- and H2-receptor blockade on histamine-induced changes in nasal airways resistance and lavage protein concentrations. Normal subjects were pretreated with oral cetirizine or ranitidine in a double-blind and randomized manner. Measurements of the concentration of total protein and albumin in nasal lavage fluid together with nasal airway resistance were made before and after challenge. Any effect of treatment was assessed by comparing the areas under the time-response curves. In all nine subjects available for analysis histamine caused an immediate increase in all measurements. Ranitidine reduced the maximum increase in nasal airway resistance, but this effect was significant only in combination with certirizine. The increase in lavage total protein and albumin concentrations was almost completely abolished by cetirizine, whereas ranitidine had less effect. We conclude that the histamine H1-receptor has the greatest effect on changes in nasal vascular permeability induced by topical histamine, whereas the H2-receptor has the greatest effect on nasal obstruction.
Two hundred seventy-four patients with perennial allergic rhinitis were tested. Quality of life was measured by using the Medical Outcome Study Short-Form Health Survey (SF-36) questionnaire. After a 2-week run-in period, cetirizine, 10 mg once daily, (136 patients) or placebo (138 patients) was given for the next 6 weeks. The SF-36 questionnaire was administered after the run-in period (at the start of treatment) and after 1 and 6 weeks of treatment. Symptom-medication scores were measured daily during the study.
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Athletes and athletic personnel associated with the National Collegiate Athletic Association (NCAA).
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A stereoselective high performance liquid chromatography method has been developed for the chiral separation of the enantiomers of six antihistamines, doxylamine, carbinoxamine, dioxopromethazine, oxomemazine, cetirizine and hydroxyzine. The effects of mobile phase additive, column temperature and flow rate on the retention time and resolution were studied. Enantiomeric separation of cetirizine, doxylamine and hydroxyzine were achieved on cellulose tris-(3,5-dichlorophenylcarbamate) immobilized on silica gel chiral stationary phase known as Chiralpak IC (RS = 3.74, RS = 1.85 and RS = 1.74, respectively).
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For quantitative use of skin prick tests (SPTs), the circumference of the wheal and/or the flare is outlined by a pen, and transferred to a paper by adhesive tape. The biological response is considered proportional to this area. We have previously developed software, the SPT-scanner, for determination of SPT areas (5-500 mm2) by a hand-held scanner and a personal computer. This study is aimed at comparing the SPT-scanner with another semiautomated system, where the outline of the wheal is followed by a digitizer pen. Comparing 2080 SPT areas from a pharmacological study of cetirizine, the two systems correlated well (r = 0.980, p < 0.001), the digitizer generally giving larger areas than the SPT-scanner. Probably, the line is considered as a part of the wheal/flare in the digitizing system, whereas the scanner only detects areas within the circumference. In conclusion, the SPT scanner is objective and reproducible for rapid SPT area determination.
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This large PMSS confirms evidence from multiple placebo-controlled trials that desloratadine is effective and well tolerated in the treatment of CIU.
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46 specialized physicians in 6 hospital clinics and 32 private outpatient clinics.
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Erythromelalgia is a clinical syndrome of which the etiology, diagnosis and management are controversial. We describe a case of a 34-month-old Egyptian child with primary erythromelalgia that manifested at an early age. We believe that this is the first Egyptian case report of this kind in the literature. Partial response of this patient to cetirizine hydrochloride may grant us a new clue to understanding this mysterious condition.
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We characterised histamine H(1) receptor antagonism by cetirizine and its enantiomers on isolated guinea pig ileum and trachea. Competitive or mixed (competitive and apparent noncompetitive) antagonism profiles were observed. The order of potency was: chlorpheniramine> or =mepyramine>levocetirizine>cetirizine> or =terfenadine>loratadine>dextrocetirizine. The inhibitory effects of cetirizine, levocetirizine, terfenadine and loratadine were slowly reversible compared to those of dextrocetirizine or mepyramine. Cetirizine and its enantiomers were inactive on L-type Ca(2+) channels. Reduction of the histamine H(1) receptor reserve by dibenamine in the ileum (100-fold higher than in the trachea) showed a gradual change from the competitive profile of dextrocetirizine and mepyramine to a mixed profile. The present results show that cetirizine and levocetirizine are selective competitive but slowly reversible histamine H(1) receptor antagonists. Their mixed antagonism profile observed in the trachea can be explained by the small receptor reserve present in this tissue compared to the ileum and their very slow dissociation rate from the histamine H(1) receptor.
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Patients with AD differ in the ability to clear S. aureus from the skin during anti-inflammatory treatment, which appears to be related to the abnormalities in immunological parameters. Local antibiotic therapy should be considered only in patients with persistent S. aureus colonization.
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Most, if not all, people are sensitized to mosquito bites in childhood. Cutaneous symptoms include immediate wheal-and-flare reactions and delayed bite papules, which tend to be more severe at the onset of the mosquito season. Systemic reactions to mosquito bites are, however, very rare. Recent immunoblot studies have demonstrated IgE antibodies to Aedes communis mosquito saliva 22 and 36 kD proteins. This confirms that specific sensitization occurs in man and indicates that mosquito-bite whealing is a classic type I allergic reaction. The delayed mosquito-bite papules seem to be cutaneous late-phase reactions mediated by eosinophils or they could also represent type IV lymphocyte-mediated immune reactions. People living in heavily infested areas such as Lapland frequently acquire tolerance to mosquito bites, and seem to have negligible levels of IgE but high amounts of IgG4 antisaliva antibodies. Desensitization treatment is a theoretical possibility but prophylactically given cetirizine, an H1-blocking antihistamine, has been shown to be helpful for people suffering from mosquito bites.
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Our results indicate a protective effect of a specific H(1)-receptor antagonist.
Using human eosinophils isolated from patients with allergic rhinitis, the cells were cultured in vitro for 48 to 72 hours with medium, cetirizine, or dexamethasone in the presence of IL-5, IL-3, or GM-CSF. Eosinophil survival was assessed by trypan blue exclusion.
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Antihistaminic drugs are widely prescribed across a multitude of medical specialties such as Allergy and Dermatology. The potentially serious sedative effect of these valuable agents has previously restricted their full use and the choice of drug has been dictated more by individual patient acceptability than by any laboratory demonstrations of comparative efficacy. Unsurprisingly therefore, there is a trend towards prescribing those newer preparations which leave the central nervous system unclouded. We have studied the most frequently prescribed non-sedating antihistamine preparations, terfenadine (Triludan, Triludan Forte), cetirizine (Zirtek) and loratadine (Clarityn) in pharmacodynamic and relative efficacy trials using a quantifiable and reproducible extension of the classic Lewis model. The results indicate that two preparations, terfenadine 120 mg (Triludan Forte) and cetirizine 10 mg (Zirtek) are superior to their immediate rivals in degree of efficacy and/or speed of action. These results should assist clinicians in the positioning of effective, rapidly acting antihistamines for the symptomatic treatment of immediate hypersensitivity reactions such as urticaria and rhinitis.