Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0042109 (urticaria)
 6,569 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Antihistamines are frequently employed in the treatment of allergic rhinitis and urticaria-angioedema syndrome. We analyzed the in vitro effects of cetirizine on the immune response. To this end the proliferation of peripheral mononuclear cells induced by mitogen and by -CD3, -CD2, or -CD28 monoclonal antibodies has been studied. Since the plasma peak of cetirizine following ingestion of 10 mg is about 1 microgram/mL, the drug was tested in the cultures at the concentration of 0.1, 1, or 10 micrograms/mL. No influence of cetirizine on T cell proliferation was detected. We also evaluated the effect of cetirizine on the expression of the following markers expressed by T cells upon activation: lymphocyte markers ICAM-1, HLA-DR, and CD25 surface expression, alpha-1-acid glycoprotein has been also studied. There was no effect of cetirizine on the investigated immunologic parameters; these data acquire clinical relevance when related to previous reports showing a depression of the immunologic response exerted by other compounds such as ketotifen and theophylline and when related to the recent data about the modulation of ICAM-1 expression on eosinophils by cetirizine. Cetirizine does not affect ICAM-1 expression of lymphocyte membrane.
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PMID:Cetirizine does not influence the immune response. 134 75

The recent development of selective H1-antagonists that minimally cross the blood-brain barrier has greatly improved the management of allergic rhinitis and chronic urticaria. These new agents have much reduced anticholinergic and sedative side effects, which were the major drawbacks of the classic H1-antihistamines. Cetirizine, a new second-generation H1-antagonist, offers several properties that may further improve the treatment of allergic rhinitis and chronic urticaria. Cetirizine is the only antihistamine known to possess activity against both the histamine-mediated early phase of the allergic response and the late-phase response of immediate hypersensitivity characterized by migration of inflammatory cells to the site of the reaction. Its efficacy has been demonstrated in clinical trials of patients with seasonal rhinitis and urticaria. The most common side effects associated with cetirizine, such as sedation, are similar to those of other second-generation antihistamines. These properties, combined with a once-daily dosage regimen, should help improve patient compliance and optimize antihistamine therapy.
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PMID:Cetirizine: a unique second-generation antihistamine for treatment of rhinitis and chronic urticaria. 167 32

Cetirizine, a peripheral H1 antagonist, was administered to patients with delayed pressure urticaria in a double-blind, placebo-controlled, crossover study. Efficacy in reducing pressure-induced wheals and flares was evaluated. Histologic changes were also assessed with the skin window technique in weight-induced wheals. Results showed a statistically significant reduction in weight-induced wheal area (p less than 0.01) after cetirizine therapy; this improvement was accompanied by a concomitant reduction in eosinophil recruitment as demonstrated by the skin window technique (p = 0.0029). Subsequently, 14 patients with delayed pressure urticaria underwent biopsy before and after 3 weeks of cetirizine therapy to evaluate the drug's histologic effects. A blinded observer performed the histologic studies. Weight-induced lesions showed a mixed inflammatory infiltrate, primarily polymorphonuclear (neutrophils and eosinophils), whereas the unchallenged skin sites were normal. Cell counts from pressure-induced lesions showed a significant reduction in eosinophils after cetirizine treatment.
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PMID:Therapeutic effects of cetirizine in delayed pressure urticaria: clinicopathologic findings. 167 12

Cetirizine, an H1 antihistamine, has properties in addition to H1 blockade that may be useful in the treatment of seasonal rhinitis and urticaria. For example, cetirizine has been shown to block the influx of eosinophils into the site of antigen-stimulated skin blisters. Studies with other antihistamines suggest that this is not a universal property of this type of drug. Pretreatment with cetirizine also has been found to block the augmented sensitivity to methacholine that occurs 24 hours after antigen provocation of the nasal mucosa. This reduction takes place despite the absence of an effect on eosinophil influx into this area, and suggests another action of cetirizine. Our study of allergic rhinitis patients examined the effect of cetirizine on early response to nasal challenge with antigen. Cetirizine, although it did not block the release into nasal secretions of histamine, significantly reduced sneezing and decreased levels of albumin and TAME-esterase activity, which are indicators of vascular permeability. Cetirizine also blocked the generation of leukotriene C4. In vitro studies have shown that cetirizine does not block the release of leukotriene from anti-IgE stimulated mast cells, raising the possibility that cells in the nasal mucosa in addition to mast cells generate leukotrienes.
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PMID:Additional properties of cetirizine, a new H1 antagonist. 168 95

The efficacy of cetirizine dihydrochloride, a new H1-antagonist claimed to have minimal sedative property was evaluated in 28 patients with chronic idiopathic urticaria. Cetirizine 10 mg and placebo were compared in a double-blind cross-over trial. Response was measured by patients with daily charts on itch and wheals. Response was also assessed by patients and investigators while on cetirizine and placebo on an analogue scale. The mean analogue score by the investigator while on cetirizine (64.6 mm) was better than while on placebo (47.0 mm) (p = 0.008). Reduction of itch with cetirizine was significantly greater than with placebo. The mean itch scores for placebo and cetirizine were 21.2 and 14.5 respectively (p = 0.01) showing a significant improvement of itch by cetirizine. The mean score for wheal response for placebo and cetirizine were 21.0 and 16.16 respectively (p = 0.07 NS) showing a reduction of wheal from cetirizine was greater than placebo but the difference was not statistically significant. The patients' mean visual analogue score for placebo was 38.4 and for cetirizine was 57.5 (p = 0.006). Cetirizine was significantly better in controlling symptoms of chronic urticaria than placebo. Five of the 28 (17.9%) patients reported mild drowsiness while taking cetirizine. Two patients reported drowsiness while on placebo. Tolerance was reported as good in 85%, moderate in 10% and bad in 5% according to patients' assessment, while tolerance was excellent and good in 80%, moderate in 15% of patients according to investigator's assessment.
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PMID:Cetirizine vs placebo in chronic idiopathic urticaria--a double blind randomised cross-over study. 168 78

Although the action of H1 antagonists in the early phase of IgE-mediated, allergic skin reactions is well established, the effect of these antihistamines on the ensuing late-phase reaction has only recently been investigated. The eosinophilic late-phase reaction, sometimes associated with the tissue damage that occurs in chronic idiopathic urticaria, is important in allergic responses. Cetirizine is a new H1 antagonist with potent inhibitory action against the infiltration of eosinophils into involved tissue, thereby affecting the late-phase reaction. No other antihistamine has yet been reported to possess this antieosinophilic property. The mechanisms by which cetirizine acts against eosinophils, although not thoroughly understood, seem to involve direct action against these cells.
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PMID:Cetirizine: a new H1 antagonist with antieosinophilic activity in chronic urticaria. 168 39

The effects of oral cetirizine on spontaneous and provoked urticaria were evaluated in two studies. In a double-blind crossover trial, 30 patients with idiopathic urticaria received 10 or 20 mg of cetirizine or placebo. Cetirizine was significantly more effective than placebo in reducing the incidence of erythema, wheals, and pruritus. No serious side effects were reported. In the second study of ten patients with chronic urticaria, immediate and delayed reactions to injected autologous serum, histamine, kallikrein, and synthetic platelet-activating factor (PAF)-acether were inhibited by 10 mg of cetirizine. These results suggest that the mechanism of action of cetirizine may involve inhibition of PAF-induced influx of eosinophils.
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PMID:Cetirizine in the treatment of chronic urticaria. 182 14

The protective efficacy of oral cetirizine, a selective and potent H1-receptor antagonist, against the immediate bronchoconstrictive response to allergen inhalation and exercise challenge was evaluated in 16 subjects with stable, predominantly mild asthma. The subjects underwent double-blind, crossover pretreatments in randomized order in two separate protocols with (1) three daily oral doses of 20 mg of cetirizine and placebo, followed by allergen inhalation, and (2) single oral doses of cetirizine (5, 10, and 20 mg), albuterol (4 mg), and placebo, followed by exercise with cold-air inhalation. Cetirizine failed to decrease bronchial sensitivity to inhaled allergen in eight of 10 subjects. Neither cetirizine nor albuterol uniformly inhibited exercise-induced bronchoconstriction. Serum concentrations of cetirizine were consistent with systemic H1-blocking activity. Modest bronchodilation occurred after administration of cetirizine and albuterol before exercise but not after the third dose of cetirizine in the allergen protocol. One subject developed moderate drowsiness during multiple dosing with cetirizine. Thus, cetirizine, in the doses studied, is not uniformly effective in preventing allergen- or exercise-induced bronchoconstriction. Histamine is one of many mediators participating in immediate asthmatic responses, and selective H1 antagonists do not completely block these airway events. However, cetirizine may still clinically benefit some patients with asthma, such as patients with allergic rhinitis or urticaria.
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PMID:Effects of oral cetirizine, a selective H1 antagonist, on allergen- and exercise-induced bronchoconstriction in subjects with asthma. 196 19

The effects of oral administration of the antihistamine cetirizine on the weal and flare caused by intradermal injection of platelet activating factor (PAF-acether), kallikrein, histamine and the patient's own serum were investigated in 10 patients with chronic urticaria. Cetirizine markedly reduced the weal and flare induced by all these agents as measured 12 min after the injections. The delayed reactions observed after injection of PAF, kallikrein and serum were also inhibited by cetirizine at 6 hours. In addition, reactions which were present 20 h after injection of the agent before administration of cetirizine were found to be inhibited at the same point in time after cetirizine treatment. These effects might explain the good inhibitory clinical effect of cetirizine on the patients' urticaria. No side-effects were noted during the treatment.
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PMID:Effect of cetirizine on cutaneous reactions to PAF, kallikrein and serum in patients with chronic urticaria. 196 2

Chronic urticaria is a problem for both physician and patient. In an effort to avoid the risks associated with corticosteroid treatment, many first-generation H1-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 H1-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.
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PMID:Urticaria: clinical efficacy of cetirizine in comparison with hydroxyzine and placebo. 197 96


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