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Levocetirizine, the active enantiomer of cetirizine, is more potent and consistent than other popular H1 antihistamines for blocking the cutaneous response to histamine. These findings may predict the efficacy of this drug in treating allergic disorders.
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Leukotriene receptor antagonists are recommended for the treatment of asthma, and have proved anecdotally successful even in atopic dermatitis. Standard treatments of atopic dermatitis are often unsatisfactory. Accordingly, we compared montelukast, 10 mg/day, with a combined regimen (orally administered cetirizine and clarythromycin, topical corticosteroids and hydrating preparations) for treatment of moderate-to-severe atopic dermatitis of adults. The trial was designed as a randomized single-blind study. SCORAD, eosinophilic cationic protein (ECP), eosinophilic protein X (EPX) serum levels were assessed at baseline and after 6 weeks in 32 adult patients with atopic dermatitis (16 treated with montelukast; 16 treated with the combined regimen). Similar improvements, evaluated in term of SCORAD reductions, were detected in both groups (Mann-Whitney, p < 0.05), while ECP and EPX levels significantly reduced within each group (Welch's approximate t, p < 0.05). We conclude that montelukast is as effective as the comparison combined regimen to treat atopic dermatitis of adults.
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The pharmaceutical products are emerging pollutants continuously released into the environment, because they cannot be effectively removed by the wastewater treatment plants. In recent years, questions have been raised concerning the environmental risks related to these pollutants. The goal of this research was to evaluate the responses in Lemna minor after 7 days and in Corbicula fluminea after differing durations (1, 3, 7, and 19 days) of exposure to the psychoactive drug mixture (valproic acid, citalopram, carbamazepine, cyamemazine, hydroxyzine, oxazepam, norfluoxetine, lorazepam, fluoxetine, and sertraline) in different concentrations (0, 0 + ethanol, drug concentration (DC) 1 = river water concentration, DC2 = effluent concentration, and DC3 = 10× effluent concentration). In this aim, growth parameters of L. minor, gluthathione S-transferase (GSTs), catalase (CAT), ethoxyresorufin-O-deethylase (EROD) and/or gene expressions (pi-gst, cat, cytochrome P450 4 (cyp4), multidrug resistant 1 (mdr1), and superoxide dismutase (sod)) were measured. GST activities increased significantly in L. minor exposed to DC3, but no changes were found in CAT activity. In C. fluminea, EROD activity was induced significantly in both gill and digestive gland tissues after 3 days' exposure to DC3, while a GST increase was observed only in digestive gland tissues, suggesting that these pharmaceuticals induced an oxidative effect. Gene expression analysis revealed transient transcriptomic responses of cyp4, sod, and mdr1 under drug concentrations 2 or 3 and no change of expression for the other genes (cat and pi-gst) or condition (environmental drug concentration) tested. Finally, the data reported in this study represent important ecotoxicological information, confirming that this enzyme family (cyp4, sod, and mdr1) may be considered as a sensible and early indicator of exposure to drugs and emphasizing the involvement of selected genes in detoxification pathways.
The purpose of this prospective, pilot study was to investigate postsedation events during the first 24 hours after discharge from the treatment facility in children sedated for dental treatment.
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2, 5 and 7 h after intake of the antihistaminic drug, there were significant differences between both drugs. Concerning LDF recordings, we noted at the histamine administration site an increase in perfusion unit (PU) values which is an effect known to be in proportion to the degree of inhibition of wheal reaction, and at 1 cm distal to the histamine administration site, there was a decrease in PU values. These changes were more marked under cetirizine. A greater suppressive effect of cetirizine on the wheal and flare reaction was consistently observed at all time points during the study, demonstrating its superior efficacy.
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This study sample consisted of thirty children aged 24-72 months (mean = 41.1) exhibiting definitely negative behavior. Three sedative regimens including: Oral meperidine/hydroxyzine, oral midazolam/hydroxyzine and submucosal meperidine/oral hydroxyzine were administered randomly during three consecutive appointments with a crossover design. Houpt behavioral scale was employed for evaluating the sedation effect of each regimen by a calibrated independent Pediatric dentist. Physiologic parameters were also recorded including blood oxygen saturation and pulse rate. Data was analyzed using Wilcoxon-signed ranked test, Mc-Nemar, GEE Logistic regression, Friedman, Fisher exact and Cochran tests for significance.
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We assessed the effectiveness of five in vitro assays in predicting in vivo tumor growth stimulation by the H1-antihistamines loratadine, astemizole, cetirizine, hydroxyzine, and doxylamine.
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Tachyphylaxis phenomenon for antihistamine effect of 10 mg/day cetirizine and 5 mg/day levocetirizine was not observed during the whole 180-days treatment.
Painful bladder syndrome/interstitial cystitis (PBS/IC) is a disease of unknown aetiology, characterised by severe pressure and pain in the bladder area or lower pelvis that is frequently or typically relieved by voiding, along with urgency or frequency of urination in the absence of urinary tract infections. PBS/IC occurs primarily in women, is increasingly recognised in young adults, and may affect as many as 0.1-1% of adult women. PBS/IC is often comorbid with allergies, endometriosis, fibromyalgia, irritable bowel syndrome and panic syndrome, all of which are worsened by stress. As a result, patients may visit as many as five physicians, including family practitioners, internists, gynaecologists, urologists and pain specialists, leading to confusion and frustration. There is no curative treatment; intravesical dimethyl sulfoxide, as well as oral amitriptyline, pentosan polysulfate and hydroxyzine have variable results, with success more likely when these drugs are given together. Pilot clinical trials suggest that the flavonoid quercetin may be helpful. Lack of early diagnosis and treatment can affect outcomes and leads to the development of hyperalgesia/allodynia.
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There were no significant differences between overall inhibitions of wheal or flare by 20 mg bilastine and 10 mg cetirizine. Bilastine was faster in onset than cetirizine, inhibitions of wheal and flare at 1.5 h being 89 ± 3 versus 44 ± 14% (P = 0.011) and 85 ± 4 versus 45 ± 14% (P = 0.016), respectively (Student's t test). At 1.5 h, both wheals and flares were inhibited by >70% in 11/12 volunteers taking bilastine and 3/11 taking cetirizine (P = 0.003, Fisher's exact test). There were no significant differences between the drugs at later times. Bilastine 50 mg had a longer duration of action than bilastine 20 mg.
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Patients with chronic idiopathic urticaria were randomly assigned to relieve either 10 mg of cetirizine, 10 mg of astemizole, or placebo for 4 weeks in a multicenter double-blind trial. Patients rated symptom severity each night, and investigators rated symptoms weekly.
Reactions between active drug substances and excipients are of interest in the drug formulation process and should also be considered in the following storage of final preparations. Some excipients react more readily with certain chemical groups in drug substances and in the present paper the ester formation between a drug substance having a carboxylic acid moiety and some polyols are described. The drug substance cetirizine was chosen as the model substance as it is already marketed and used as a common drug for treatment of allergic reactions. Among the marketed products are oral solutions and oral drops containing excipients like sorbitol and glycerol. It was found that the carboxylic acid cetirizine readily reacts with sorbitol and glycerol to form monoesters. At a temperature as low as 40 degrees C, more than 1% of the cetirizine content was transformed into a monoester within 1 week using concentrations similar to those used in marketed preparations. The kinetic studies of the reaction performed at 40, 60 and 80 degrees C also revealed that the esters were unstable and they degraded especially at higher temperatures. Analysis of two marketed preparations having expiry dates in 2011 showed content of the cetirizine esters corresponding to a range from 0.1 to 0.3% of the declared cetirizine content.
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Nasal congestion is the most troublesome symptom of allergic rhinitis (AR). First-generation and older second-generation antihistamines, while effective against nasal itching, sneezing, and rhinorrhea, have limited efficacy in relieving nasal congestion.
To explore risk factors for the yawning response induced by the intravenous administration of thiopental during the induction of general anesthesia.
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This cross-sectional database study identified older patients receiving drugs included in the HEDIS 2006 criteria using national data from the Veterans Health Administration. Patients aged 65 years or older on October 1, 1999, with at least 2 outpatient visit days during fiscal year 2000, ending September 30, or outpatient visits in fiscal years 1999 and 2000 were included (N=1,096,361). Multivariable logistic regression analyses stratified by gender identified patient characteristics associated with increased risk of HEDIS 2006 drug exposure. Since oral estrogens were considered appropriate at the time of this study, they were excluded from the list of HEDIS 2006 drugs.
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87 with a history of urticaria following the administration of multiple, chemically unrelated NSAID underwent 250 oral tolerance tests with alternative drugs exerting little or no COX-1 inhibition (paracetamol, coxibs, nimesulide, tramadol). Twenty-eight challenges scored positive in 21 subjects: 8, 5, 9, and 6 reactions were induced by paracetamol, tramadol, coxibs, and nimesulide, respectively. Thirteen of 21 underwent a new oral challenge with the offending drug(s) 2-6 hours after taking cetitrizine 10 mg.
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Both eosinophils and mast cells have been implicated in the generation of abdominal pain. The purposes of this retrospective study were to determine the prevalence of duodenal eosinophilia in pediatric dyspepsia and to determine the clinical response rate of these patients to combined H1 and H2 receptor antagonist and mast cell stabilizer therapy. Fifty-nine patients (ages 3.5-17.7 years) with dyspepsia undergoing endoscopy were evaluated. All patients had a minimum of 2 forceps biopsies obtained from each of the esophagus, antrum, and duodenal bulb. Routine histologic evaluation was performed and duodenal biopsies were additionally evaluated to determine eosinophil counts. Patients with > 10 eosinophils/hpf were treated with ranitidine and hydroxyzine (H1/H2). Nonresponders were then treated with oral cromolyn. Patients were followed up and response recorded in an abdominal pain database and/or medical chart, which were reviewed for this study. Forty-two patients (71%) had duodenal eosinophilia. Twenty-one (50%) of these were responders to H1/H2. The response rate did not differ between patients with and without noneosinophilic esophagitis, gastritis, or duodenitis, respectively. Two patients were lost to follow-up and considered nonresponders. Seventeen of the remaining 19 (89%) were responders to cromolyn. Overall, the response rate to this treatment pathway was 90%. Duodenal eosinophilia is common in pediatric patients with dyspepsia. These patients appear to be clinically amenable to combination H1/H2 therapy and/or oral cromolyn.
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We characterized the histamine H(1) receptor agonism of various histaprodifen derivatives in guinea pig isolated ileum and trachea in comparison with histamine. Based on their affinity (calculated pK(A) values for ileum and trachea, respectively), the compounds were ranked as follows: suprahistaprodifen (8.31/8.08) > N(alpha)-(4-phenylbutyl)histaprodifen (7.22/5.93) >or= histamine (5.79/5.19) approximately methylhistaprodifen (5.57/6.07). Based on their efficacy (calculated tau values for ileum and trachea, respectively), the compounds were ranked as follows: methylhistaprodifen (37.67/2.50) > histamine (5.64/1.80) > suprahistaprodifen (1.63/1.42) >or= N(alpha)-(4-phenylbutyl)histaprodifen (0.083/1.54). In the ileum, histamine and methylhistaprodifen showed a high histamine H(1) receptor reserve while suprahistaprodifen and N(alpha)-(4-phenylbutyl)histaprodifen are devoid of any histamine H(1 )receptor reserve. On the trachea, no histamine H(1 )receptor reserve was demonstrable with the four tested agonists. The kinetic of contraction/relaxation of the ileum was faster with histamine and methylhistaprodifen than with suprahistaprodifen and N(alpha)-(4-phenylbutyl)histaprodifen. Histamine contracted the trachea faster than histaprodifen derivatives. Levocetirizine antagonized contractions induced by histamine and histaprodifen derivatives in both tissues. The differences observed in the calculated pA(2) (7.60-8.29) and/or pD'(2) values (6.28-7.90) depending on the tissue and/or the agonist are discussed.