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Leucocytes from healthy donors were isolated and incubated in varying concentrations of ciclosporin, ascomycin, methotrexate, diphenhydramine or hydroxyzine for 30 min prior to stimulation with serum from urticaria patients known to have functional immunoglobulin (Ig)G antibodies directed against the alpha subunit of the IgE receptor. Histamine release was then measured.
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To review the signalment, clinical characteristics, treatment, and outcome of equine EK cases in the Mid-Atlantic United States; to evaluate the effects of topical or systemic corticosteroid treatment, oral cetirizine treatment and secondary corneal infection on disease duration; and to evaluate the association between corticosteroid and cetirizine treatment and likelihood of recurrence.
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Mequitazine is a so-called 'non-sedative' second-generation antihistamine even though it has never been firmly established that this drug's sedative potential actually differs from that of the 'sedative' first-generation antihistamines.
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To compare the effectiveness of IM ketorolac with that of meperidine and hydroxyzine in the treatment of acute migraine headache.
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A total of 510 atopic children (mean +/- SEM age, 19.4 +/- 0.2 months) composed the intention-to-treat population. During the subsequent 18 months, 27.5% (70/255) of the children taking levocetirizine and 41.6% (106/255) of the children taking placebo experienced urticaria (P < .001). The mean +/- SEM number of urticaria episodes was 0.71 +/- 0.11 in those receiving levocetirizine and 1.71 +/- 0.25 in those receiving placebo (P < .001). The mean +/- SEM duration of urticaria episodes was 4.43 +/- 1.57 days in those receiving levocetirizine and 5.36 +/- 1.27 days in those receiving placebo (P < .001).
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Anaesthesia with sevoflurane leads to a high prevalence of emergence agitation in paediatric patients. This study investigates the effects of combining hydroxyzine and midazolam on sevoflurane-induced emergence agitation in paediatric patients undergoing infraumbilical surgery with a caudal block.
In the in vivo antihistaminic activity experiments, bilastine was shown to have a positive effect, similar to that of cetirizine and more potent than that of fexofenadine. The results of the in vivo antiallergic activity experiments showed that the properties of bilastine in this setting are similar to those observed for cetirizine and superior to fexofenadine in the model of passive cutaneous anaphylactic reaction. When active cutaneous anaphylactic reaction experiments were conducted, bilastine showed significant activity, less potent than that observed with cetirizine but superior to that of fexofenadine. Evaluation of the type III allergic reaction showed that of the antihistamines only bilastine was able to inhibit oedema in sensitised mice, although its effect in this respect was much less potent than that observed with dexamethasone. In terms of the type IV allergic reaction, neither bilastine, cetirizine nor fexofenadine significantly modified the effect caused by oxazolone.
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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All H(1)-antihistamines demonstrated significantly greater (P <.05) geometric mean +/- SEM AMP PC(20) values compared with that of placebo (86 +/- 29 mg/mL): desloratadine, 189 +/- 54 mg/mL; FEX, 176 +/- 57 mg/mL; and LEV, 163 +/- 48 mg/mL. Prechallenge forced expiratory flow at 25% to 75% of maximal lung volume (percent predicted) but not FEV(1) was significantly higher (P <.05) for all H(1)-antihistamines compared with that of placebo (53% +/- 4%): desloratadine, 62% +/- 4%; FEX, 62% +/- 4%; and LEV, 59% +/- 3%. There were no significant differences in either AMP PC(20) or lung function values among the H(1)-antihistamines.
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Pharmacokinetic study of a single oral dose of cetirizine 10mg in 40 patients treated for allergic conjunctivitis.
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Pain control using intramuscular analgesia is often unsatisfactory in sickle cell patients. In a pilot study, 15 patients with sickle cell anemia (SS) and one patient with SB thalassemia in vaso-occlusive crisis were treated with the Patient-Controlled Analgesia (PCA) technique using a Pharmacia Deltec Programmable pump (CADD PCA). Age range was 19-50 years (median = 27); there were nine females and seven males. The protocol consisted of 3 days of therapy using a background of continuous infusion meperidine. The starting dose was 20 mg/hr and was escalated to 30 mg/hr. The average amount given was 25.8 mg/hr. One to two boluses of 2.5-5.0 mg/dose (mode = 5.0) were also allowed each hour. In addition, patients number 8 through 16 were given hydroxyzine (Vistaril) 50 mg PO q6h. The number of days in pain prior to study entry (mean +/- SD) was 3.3 +/- 1.6. The number of pain sites per patient was 3.6 +/- 1.2. Using categorical and analog pain scales, patients' pain scores decreased only about 30%. However, most patients were fairly satisfied with the treatment and rated it overall as follows: 1 poor, 1 fair, 3 good, 6 very good, 4 excellent, 1 no comment. Patients number 8 through 16 gave higher ratings probably because a more idealized dosage regimen was being used by that time in the study. There were no adverse effects or major problems noted. It is our impression that PCA, when optimized, will be a safe and effective alternative method for providing patients with sickle cell vaso-occlusive crisis pain relief.
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This was a double-blind, placebo-controlled, parallel study. Patients were randomized to receive either cetirizine and theophylline (200 mg twice daily; group A, 67 subjects) or cetirizine and placebo for 6 months (group B, 67 subjects). Group A patients took theophylline for 6 more months. Response was assessed by visual analog scale (VAS) and treatment effectiveness score (TES). Blood theophylline levels were also determined at visit t=1 and t=7.
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We hypothesized that the objectively documented central nervous system response to antihistamines (H1-receptor antagonists) could not be predicted reliably by an individual's subjective perception of somnolence after ingestion of these medications.
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Descriptive demographic and clinical data. Odds ratios quantification of the efficacy of drug therapies administered acutely to suppress PSH episodes.
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The purpose of this prospective study was to determine the frequency of adverse events associated with supplemented and unsupplemented chloral hydrate sedation in a select group of children undergoing CT or MR imaging using the revised American Academy of Pediatrics (AAP) monitoring and management guidelines for pediatric sedation. The AAP guidelines do not recommend drug selection or dosages but define patient selection, discharge criteria, and monitoring standards for sedating children.
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Cultured keratinocytes constitutively expressed the H1 receptor mRNA and protein, which was not influenced by IFN-gamma, TNF-alpha, or IL-4. H1 but not H2 agonists induced calcium fluxes in keratinocytes. Treatment of keratinocytes with histamine (10 -7 to 10 -4 mol/L) or beta-histine increased the IFN-gamma-induced expression of membrane intercellular adhesion molecule 1 and MHC class I but not MHC class II molecules. Moreover, H1 stimulation promoted basal CC chemokine ligand (CCL)-5/RANTES and GM-CSF secretion and augmented IFN-gamma-induced release of the chemokines CCL2/monocyte chemoattractant protein 1, CCL5/RANTES, CCL20/macrophage inflammatory protein 3alpha, and CXC chemokine ligand 10/IFN-induced protein of 10 kd, as well as GM-CSF. Administration of the H1 antihistamine levocetirizine, but not of the H2 antihistamine cimetidine, abolished histamine-dependent expression of all of the investigated proinflammatory molecules in a dose-dependent manner (0.01-10 mumol/L). Levocetirizine at higher doses also reduced intercellular adhesion molecule 1, CCL5/RANTES, and GM-CSF release induced solely by IFN-gamma.
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1. Intravenous administration of ovalbumin (1 mg kg-1) to guinea-pigs that had previously been injected with 3.5 x 10(9) platelets from actively sensitized animals induced an approximately 40% decrease in the number of circulating leucocytes 30-60 min later, whereas the number of platelets was not affected. 2. In contrast, there was no change in the leucocyte number following antigen challenge of guinea-pigs that had received platelets from non-immunised animals. 3. This platelet-dependent leucopenia was inhibited by prior treatment of the recipient animal with cetirizine (10-30 mg kg-1, i.v.). Terfenadine (50 mg kg-1, p.o.) and mepyramine (2 mg kg-1, i.v.) were completely inactive in this respect. All doses of anti-histamines were used at concentrations which completely inhibited the bronchoconstriction to an i.v. injection of 5 micrograms kg-1 of histamine. 4. The site of action of cetirizine is most likely to be the platelet as leucopenia induced by the neutrophil agonists leukotriene B4 (LTB4) (30 ng kg-1) and platelet activating factor (PAF) (30 ng kg-1) were not modified by cetirizine treatment. 5. In these experiments, we failed to support a role for lipoxygenase products as mediators of the platelet-dependent leucopenia, as the selective lipoxygenase inhibitor BWA4C (50 mg kg-1, p.o.) was ineffective. 6. Our present results confirm and extend previous data demonstrating that antigen stimulated platelets can induce leucopenia in non-immunised animals and this can be inhibited by the anti-allergic agent, cetirizine, by an action which is probably unrelated to its anti-histamine properties. The precise nature of the platelet derived factor(s) and their target of action remains to be determined.
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Many solar urticaria patients may benefit from the use of antihistamines. Historically, the value of such therapy was limited by sedation. Newer agents such as terfenadine and cetirizine that are relatively non-sedating appear to be better tolerated by patients. The latter drug, in addition to its antihistamine effect, also appears to inhibit eosinophil migration, which terfenadine and other potent H1 antagonists do not significantly affect. Eosinophils have been reported as early migrating cells in induced solar urticaria, raising the possibility that the dual action of cetirizine may provide a greater potential benefit in the management of solar urticaria. Six patients with idiopathic solar urticaria were entered into a double-blind, phototest study to compare cetirizine and terfenadine. Using the minimal urticarial dose as a phototest end-point, both drugs were equally effective in raising the threshold of sensitivity in 4 patients. Two patients failed to respond to either therapy, which is in keeping with the known variable response to histamine blockade in solar urticaria. At the dosage used, cetirizine therapy appears to be no more effective than terfenadine.
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Twenty preschool-age children, with previous histories of uncooperative behavior, were randomly assigned to first receive a sedation regimen of either SM (0.5 mg/ lb), or OM (1 mg/lb), both with oral hydroxyzine (0.5 mg/lb). A cross-over design was utilized so that each child received both regimens. Safety was monitored through vital signs and side effects. Efficacy was measured with Houpt and Frankl behavior ratings.
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Hydroxyzine reduced carbachol-induced serotonin release from rat bladder in vitro through a mechanism which was unrelated to its H-1 receptor antagonistic properties. The ability of hydroxyzine to inhibit bladder mast cell activation by neurogenic stimuli along with its anticholinergic, anxiolytic and analgesic properties, may explain the clinical efficacy of this drug in reducing IC symptoms. Other, nonsedating, hydroxyzine analogues able to inhibit bladder mast cell activation may provide potentially new therapeutic approaches for IC.
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Child-caregiver dyads were enrolled from patients presenting for midazolam, meperidine, and hydroxyzine oral sedation. Children between 36 and 95 months of age, American Society of Anesthesiology (ASA) classification I or II, with diagnostic radiographs, whose parents believed he/she would swallow oral medications, were enrolled. To assess child temperament, caregivers completed the CBQ-SF. Behavior during sedation and overall sedation results were recorded using the Houpt Behavior Rating Scale. Failure was defined by Houpt overall ratings of fair or worse. The presence of disruptive behavior was also quantified.
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This case illustrates that tramadol overdose may cause refractory shock and asystole when taken in combination with CNS depressants, and reminds all physicians to be vigilant with regard to the potential toxic effects of tramadol.
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Our patients with seasonal allergic rhinoconjunctivitis usually present severe clinical symptoms. A single daily dose of cetirizine 10 mg might be insufficient for these patients. To investigate this hypothesis we compared clinical efficacy and adverse side effects between two daily doses of cetirizine, 10 and 20 mg. We designed a comparative open randomized study, including 38 patients, with hay fever sensitized to local pollens (grass, olive, parietaria judaica, chenopodium album, artemisia vulgaris and plantago lanceolata) diagnosed by clinical history and a positive skin prick test (wheal > 3 mm), 20 women and 18 men, aged 17 to 57 years (x: 31.32 +/- 9.73), living in the same geographic area. Randomly, after a week run in period, 21 subjects received a daily dose of cetirizine 10 mg during 2 weeks, and the other 17 received 10 mg twice a day. The symptomatic score used was based on: sneezes number, nasal itching, nasal secretion, nasal congestion, ocular itching, lacrimation, weight gain, sedation and additional methylprednisolone usage. All symptoms were scored on a 0-3 scale (0: absent; 1: mild; 2: moderate; 3: severe). A mean 8 points daily score during the previous week was required for recruitment. Nasal eosinophilia was determined at baseline and at the end of treatment. The study was conducted in may 1992. We did not find significant differences between the two groups, except in sneezes number and sedation. Both groups improved their symptoms, in comparison with the basal week (p < 0.01) and reduced their oral steroid use (p < 0.01).(ABSTRACT TRUNCATED AT 250 WORDS)
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This was an open-label, randomized, comparative, parallel clinical trial conducted in 315 patients, randomly allocated to 3 groups. First group received permethrin 5% cream as single application, second group received tablet ivermectin 200 mcg/kg as single dose, and third group received ivermectin 1% lotion as single application. All the patients received anti-histaminic for pruritus. The patients were followed up at intervals of 1, 2, 3, and 4 weeks. If there were no signs of cure, the same intervention was repeated at each follow up. Primary efficacy variable was clinical cure of lesions. Statistical analysis was done by chi square test and one way ANOVA test using SPSS version 12.
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Study was performed in 64 persons (aged from 17 to 43 years) suffering from rhinitis or rhinoconjunctivitis or asthma. They were diagnosed for the first time [8, 9]. None of selected persons had proven dermographism [1, 9]. Study protocol Skin prick tests were performed according to recommended protocol reviewed elsewhere . Blood samples for total and allergen-specific IgE were taken in the morning on the test-day and sera were stored until analyses. Testing was performed with in house standardized extract of grass pollens (each of 5000 AU/allergy unit per milliliter): Dactylis glomerata and Phleum pratense and Lolium perenne (produced by Torlak Institute, Belgrade). Testing was performed in selected groups of patients: a) during and out of pollen season; b) before and after allergen-specific immunotherapy, and c) with three diverse concentrations of Phleum pratense allergenic extract (5000 AU, 7500 AU and 10,000 AU/ml). During the study a medication was not allowed at least 7 days prior to the skin testing (14 days for hydroxyzine). Alergen-specific IgE in serum (RAST) Determination of serum allergen-specific IgE was performed by using commercially available Pharmacia kit (EIA RAST Phadesim). For allergen-specific IgE results were expressed in classes (1 minimal to 4-maximal concentrations) determined by manufacturer. Study was performed under approval of the Ethic Committee of our hospital. For statistical analysis we used t-test and test of variance (ANOVA). Results were considered significant if p < 0.05.
To evaluate sleep impairment in children with AR using actigraphic evaluation.
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N,N-diethyl-2-[(4 phenylmethyl)-phenoxy]-ethanamine X HCl (DPPE), a compound selective for the antiestrogen binding site, is structurally similar to the aminoethyl ether group of antihistamines. Our studies now reveal that H1-, but not H2-antagonists, also compete for this site in the order: DPPE = hydroxyzine = perchlorperazine greater than phenyltoloxamine greater than pyrilamine greater than diphenhydramine. The affinity of these compounds for the antiestrogen binding site correlates with their in vitro cytotoxicity against MCF-7 and EVSA-T human breast cancer cells. Tamoxifen, DPPE and hydroxyzine also bind to H1 receptors present in digitonin-solubilized rat liver microsomes, but with less affinity than pyrilamine, which is selective for this site; the ratio of H1 to antiestrogen binding sites in this preparation is 4:1. The data suggest that the antiestrogen binding site may be, in whole or in part, a receptor for histamine different from H1 and H2.