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https://www.readbyqxmd.com/read/28090646/influence-of-p-glycoprotein-on-the-disposition-of-fexofenadine-and-its-enantiomers
#1
Fei Li, Karyn D Howard, Michael J Myers
OBJECTIVES: P-glycoprotein (P-gp) is responsible for the efflux of a broad variety of human and veterinary drugs. Canine P-gp polymorphisms alter drug disposition and toxicity, but their impact on the disposition of enantiomeric drugs is unknown. Using fexofenadine as a model compound, we developed and validated HPLC-fluorescence methods to determine the effect of P-gp on the disposition of fexofenadine and its enantiomers. METHODS: A chiral CD-Ph column was used for the separation of (R) and (S)-fexofenadine...
January 16, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28070872/sedative-effects-of-levocetirizine-a-systematic-review-and-meta-analysis-of-randomized-controlled-studies
#2
REVIEW
Kornkiat Snidvongs, Kachorn Seresirikachorn, Likhit Khattiyawittayakun, Wirach Chitsuthipakorn
INTRODUCTION: As a substrate of P-glycoprotein, levocetirizine should not cause sedative effects. However, while cetirizine, a mixture of levocetirizine and dextrocetirizine, can slightly penetrate the blood brain barrier, the sedative effects of levocetirizine are still under study. OBJECTIVES: The aim of this study was to investigate the sedative effects of levocetirizine. METHODS: An electronic literature search was performed using Medline and EMBASE from January 01, 2001 through August 6, 2015...
January 9, 2017: Drugs
https://www.readbyqxmd.com/read/28066101/comparison-of-efficacy-safety-and-cost-effectiveness-of-montelukast-levocetirizine-and-montelukast-fexofenadine-in-patients-of-allergic-rhinitis-a-randomized-double-blind-clinical-trial
#3
Mohini Sachin Mahatme, Ganesh Natthuji Dakhale, Kanchan Tadke, Sachin Keshaorao Hiware, S D Dudhgaonkar, Sumit Wankhede
OBJECTIVES: Allergic rhinitis (AR) is a global health problem. Almost 10%-25% of population worldwide is affected by AR. Oral/intranasal H1-antihistamine, decongestants, leukotriene receptor antagonists, and intranasal corticosteroids are the pillars in the management of AR. The combination therapy of montelukast with antihistaminic provides enhancing and complimentary effects, thereby reducing the symptoms effectively, but there are scanty data regarding the comparisons of combinations...
November 2016: Indian Journal of Pharmacology
https://www.readbyqxmd.com/read/28058761/d-optimal-mixture-design-optimization-of-a-hplc-method-for-simultaneous-determination-of-commonly-used-antihistaminic-parent-molecules-and-their-active-metabolites-in-human-serum-and-urine
#4
Selvakumar Kanthiah, Kannappan Valliappan
This present study describes a specific, precise, sensitive and accurate method for simultaneous determination of hydroxyzine, loratadine, terfenadine, rupatadine and their main active metabolites cetirizine, desloratadine and fexofenadine in serum and urine by using meclizine as an internal standard. Solid phase extraction method for sample clean-up and preconcentration of analytes was carried out by using Phenomenex Strata-X-C and Strata X polymeric cartridges. Chromatographic analysis was performed on a Phenomenex cyano (150 mm x 4...
January 6, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/28040476/asp73-dependent-and-independent-regulation-of-the-affinity-of-ligands-for-human-histamine-h1-receptors-by-na
#5
Shigeru Hishinuma, Kiyoe Kosaka, Chizuru Akatsu, Yoshihiro Uesawa, Hiroyuki Fukui, Masaru Shoji
The affinity of ligands for G-protein-coupled receptors (GPCR) is allosterically regulated by Na(+) via a highly conserved aspartate residue (Asp(2.50)) in the second transmembrane domain of GPCRs. In the present study, we examined the Na(+)-mediated regulation of the affinity of ligands for Gq/11-protein-coupled human histamine H1 receptors in Chinese hamster ovary cells. The affinities of 3 agonists and 20 antihistamines were evaluated by their displacement curves against the binding of [(3)H]-mepyramine to membrane preparations in the presence or absence of 100 mM NaCl...
December 28, 2016: Biochemical Pharmacology
https://www.readbyqxmd.com/read/27983859/reply-to-comment-on-in-silico-modeling-of-gastrointestinal-drug-absorption-predictive-performance-of-three-physiologically-based-absorption-models
#6
Erik Sjögren, Helena Thörn, Christer Tannergren
This is a reply to the comment on "In Silico Modeling of Gastrointestinal Drug Absorption: Predictive Performance of Three Physiologically Based Absorption Models" by Turner and other Simcyp associates. In the reply we address the major concerns raised by Turner et al. regarding the methodology to compare the predictive performance of the different absorption models and at the same time ensure that the systemic pharmacokinetic input was exactly the same for the different models; the selection of the human effective permeability value of fexofenadine; the adoption of model default values and settings; and how supersaturation/precipitation was handled...
January 3, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/27981349/the-influence-of-piperine-on-the-pharmacokinetics-of-fexofenadine-a-p-glycoprotein-substrate-in-healthy-volunteers
#7
Satish Kumar Bedada, Praveen Kumar Boga
PURPOSE: Piperine (PIP) has been found to inhibit P-glycoprotein (P-gp) function in rats, suggesting that it may have the potential to modulate P-gp-mediated drug efflux in humans. The aim of this study was to evaluate the effect of PIP on the pharmacokinetics of fexofenadine (FEX), a P-gp substrate, in healthy volunteers. METHODS: An open-label, two-period, sequential study involving 12 healthy volunteers was conducted. A single oral dose of FEX 120 mg was given to volunteers during the control phase and after the treatment phase...
December 15, 2016: European Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/27919212/investigating-drug-repositioning-approach-to-design-novel-prodrugs-for-colon-specific-release-of-fexofenadine-for-ulcerative-colitis
#8
Suneela S Dhaneshwar, Priyanka Singh
BACKGROUND: Recent immunologic data implicates involvement of mucosal immune cells of the intestine like eosinophils and mast cells to be functionally involved in the pathogenesis of UC. Mast cell activation is followed by increased secretion and elevated tissue concentration of histamine. Inhibition of mucosal histamine release in colon may be an effective therapeutic approach to treat UC. Some studies report that intestinal inflammation associated with acute and chronic colitis has been ameliorated by fexofenadine in mice...
December 5, 2016: Current Drug Delivery
https://www.readbyqxmd.com/read/27891350/hypersensitivity-with-inhalational-budesonide-an-under-recognised-entity
#9
Pramod Kumar Sharma, Neeraj Gupta, Najmul Hasan, Bhaskar Krishnamurthy, Surjit Singh
Hypersensitivity reactions are commonly encountered with drugs such as beta lactams, sulphonamides, allopurinol etc., Corticosteroids are frequently employed in the treatment of drug induced allergic reactions. Therefore, it is highly unlikely that a corticosteroid itself may cause such a reaction as an adverse effect. We had encountered a rare case of hypersensitivity reaction with inhalational budesonide in an eight-year-old boy. The patient developed maculopapular rashes over the back, buttocks and legs accompanied with pruritus within four hours of administration of the first dose...
October 2016: Journal of Clinical and Diagnostic Research: JCDR
https://www.readbyqxmd.com/read/27864798/pharmacokinetic-drug-interactions-with-panax-ginseng
#10
REVIEW
Meenakshi R Ramanathan, Scott R Penzak
Panax ginseng is widely used as an adaptogen throughout the world. The major active constituents of P. ginseng are ginsenosides. Most naturally occurring ginsenosides are deglycosylated by colonic bacteria to intestinal metabolites. Ginsenosides along with these metabolites are widely accepted as being responsible for the pharmacologic activity and drug interaction potential of ginseng. Numerous preclinical studies have assessed the influence of various ginseng components on cytochrome P450 (CYP), glucuronidation, and drug transport activity...
November 18, 2016: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27843000/changes-in-gene-expression-induced-by-histamine-fexofenadine-and-osthole-expression-of-histamine-h1-receptor-cox-2-nf-%C3%AE%C2%BAb-ccr1-chemokine-ccl5-rantes-and-interleukin-1%C3%AE-in-pbmc-allergic-and-non-allergic-patients
#11
Natalia Karolina Kordulewska, Elżbieta Kostyra, Anna Cieślińska, Michał Matysiewicz, Ewa Fiedorowicz, Edyta Sienkiewicz-Szłapka
INTRODUCTION: Fexofenadine (FXF) is a third-generation antihistamine drug and osthole is assumed as a natural antihistamine alternative. This paper compares results of histamine, FXF and osthole impact on HRH-1, COX-2, NF-κB-p50, CCR1 mRNA expression. We also measured mRNA expression of IL-1β and CCL5/RANTES in incubated peripheral blood mononuclear cells (PBMC) to compared how histamine, FXF and osthole had influence on expression level and interacts on product secretion. OBJECTIVE: The purpose was to investigate expression pattern in asthma PBMC...
November 10, 2016: Immunobiology
https://www.readbyqxmd.com/read/27756601/cytokine-production-by-pbmc-and-serum-from-allergic-and-non-allergic-subjects-following-in-vitro-histamine-stimulation-to-test-fexofenadine-and-osthole-anti-allergic-properties
#12
Natalia Karolina Kordulewska, Elżbieta Kostyra, Anna Cieślińska, Ewa Fiedorowicz, Beata Jarmołowska
FXF is a third-generation antihistamine drug and osthole is assumed a natural antihistamine alternative. This paper compares peripheral blood mononuclear cell (PBMC) incubation with FXF and osthole, by studying FXF, osthole and histamine cytokine secretion in PBMC in vitro cultures. Mabtech kits determined the interleukins IL-1β, IL-4, IL-10, IL-13 and TNF-α. The influence of the above active substances on cytokine secretion in PBMC's and serum was assessed: cytokines were IL-1β, IL-4, IL-10, IL-13 and TNF-α; and cytokine levels secreted by untreated PBMCs in pure culture medium formed the absolute control (ctrl)...
November 15, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27746690/effect-of-red-ginseng-on-cytochrome-p450-and-p-glycoprotein-activities-in-healthy-volunteers
#13
Dal-Sik Kim, Yunjeong Kim, Ji-Young Jeon, Min-Gul Kim
BACKGROUND: We evaluated the drug interaction profile of Red Ginseng (RG) with respect to the activities of major cytochrome P450 (CYP) enzymes and the drug transporter P-glycoprotein (P-gp) in healthy Korean volunteers. METHODS: This article describes an open-label, crossover study. CYP probe cocktail drugs, caffeine, losartan, dextromethorphan, omeprazole, midazolam, and fexofenadine were administered before and after RG supplementation for 2 wk. Plasma samples were collected, and tolerability was assessed...
October 2016: Journal of Ginseng Research
https://www.readbyqxmd.com/read/27631194/mapping-slco1b1-genetic-variation-for-global-precision-medicine-in-understudied-regions-in-africa-a-focus-on-zulu-and-cape-admixed-populations
#14
Nisreen Hoosain, Brendon Pearce, Clifford Jacobs, Mongi Benjeddou
The U.S. President Barack Obama has announced, in his State of the Union address on January 20, 2015, the Precision Medicine Initiative, a US$215-million program. For global precision medicine to become a reality, however, biological and environmental "variome" in previously understudied populations ought to be mapped and catalogued. Chief among the molecular targets that warrant global mapping is the organic anion-transporting polypeptide 1B1 (OATP1B1), encoded by solute carrier organic anion transporter family member 1B1 (SLCO1B1), a hepatic uptake transporter predominantly expressed in the basolateral side of hepatocytes...
September 2016: Omics: a Journal of Integrative Biology
https://www.readbyqxmd.com/read/27522261/the-efficacy-and-safety-of-h1-antihistamine-versus-montelukast-for-allergic-rhinitis-a-systematic-review-and-meta-analysis
#15
Chunhui Wei
PURPOSE: In order to verify the differences of effectiveness and safety between SAHs and Montelukast, and to find out potential uncared-for problems, we performed a systematic review and Meta-analysis to proceed a qualitative describe and quantitative assessment. METHODS: We searched the databases of Pubmed, the Cochrane Library, Nature and Science as well as Wanfang data and CNKI from 2000 to March 2016, using key words "Montelukast SAH" or "H1-antihistamine Montelukast", or "Loratadine Montelukast", or "Desloratadine Montelukast", or "Levocetirizine Montelukast", or "Cetirizen Montelukast", or "Fexofenadine Montelukast"...
October 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/27512204/treatment-of-chronic-spontaneous-urticaria-with-a-single-dose-of-omalizumab-a-study-of-four-cases
#16
Radhakrishnan Subramaniyan, Ajay Chopra
BACKGROUND: Chronic spontaneous urticaria (CSU) has a detrimental effect on patients' emotional and physical quality of life. Omalizumab, an anti-immunoglobulin E humanized monoclonal antibody, has been shown to be very effective in the treatment of refractory chronic urticaria patients but may not be an economically viable option for all CSU patients. However, we present a case series where a single dose of omalizumab gave sustained relief of symptoms in patients with CSU, which may be an economical option...
July 2016: Indian Journal of Dermatology
https://www.readbyqxmd.com/read/27495955/effect-of-fermented-red-ginseng-on-cytochrome-p450-and-p-glycoprotein-activity-in-healthy-subjects-as-evaluated-using-the-cocktail-approach
#17
Min-Gul Kim, Yunjeong Kim, Ji-Young Jeon, Dal-Sik Kim
AIMS: We assessed the drug interaction profile of fermented red ginseng with respect to the activity of major cytochrome (CYP) P450 enzymes and of a drug transporter protein, P-glycoprotein (P-gp), in healthy volunteers. METHODS: This study was an open-label crossover study. The CYP probe cocktail drugs caffeine, losartan, dextromethorphan, omeprazole, midazolam and fexofenadine were administered before and after 2 weeks of fermented red ginseng administration. Plasma samples were collected, and tolerability was assessed...
December 2016: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/27493198/a-single-dose-of-histamine-receptor-antagonists-prior-to-downhill-running-alters-markers-of-muscle-damage-and-delayed-onset-muscle-soreness
#18
Matthew R Ely, Steven A Romero, Dylan C Sieck, Joshua E Mangum, Meredith J Luttrell, John R Halliwill
Histamine contributes to elevations in skeletal muscle blood flow following exercise, which raises the possibility that histamine is an important mediator of the inflammatory response to exercise. We examined the influence of antihistamines on post-exercise blood flow, inflammation, muscle damage, and delayed onset muscle soreness (DOMS) in a model of moderate exercise-induced muscle damage. Subjects consumed either a combination of fexofenadine and ranitidine (blockade, n=12) or nothing (control, n=12) before 45 min of downhill running (-10% grade)...
August 4, 2016: Journal of Applied Physiology
https://www.readbyqxmd.com/read/27475625/therapeutic-effect-of-bilastine-in-japanese-cedar-pollinosis-using-an-artificial-exposure-chamber-ohio-chamber
#19
Kazuhiro Hashiguchi, Ken-Ichiro Wakabayashi, Michinori Togawa, Akihiro Saito, Kimihiro Okubo
BACKGROUND: Environmental exposure chambers have been used to expose subjects to aeroallergens to investigate the efficacy of prophylactic treatment with symptomatic agents in Japan. We first examined the therapeutic effect of bilastine (BIL), a novel non-sedative second-generation H1-antihistamine, in subjects with Japanese cedar pollinosis using an artificial exposure chamber (OHIO Chamber). METHODS: This was a randomized, double-blind, four-way crossover, placebo- and active-controlled phase II study (trial registration number JapicCTI-132213)...
July 27, 2016: Allergology International: Official Journal of the Japanese Society of Allergology
https://www.readbyqxmd.com/read/27421817/efficacy-and-safety-of-bilastine-in-japanese-patients-with-perennial-allergic-rhinitis-a-multicenter-randomized-double-blind-placebo-controlled-parallel-group-phase-iii-study
#20
Kimihiro Okubo, Minoru Gotoh, Mikiya Asako, Yasuyuki Nomura, Michinori Togawa, Akihiro Saito, Takayuki Honda, Yoshihiro Ohashi
BACKGROUND: Bilastine, a novel non-sedating second-generation H1 antihistamine, has been approved in most European countries since 2010. This study aimed to evaluate the superiority of bilastine over placebo in Japanese patients with perennial allergic rhinitis (PAR). METHODS: This randomized, double-blind, placebo-controlled, parallel-group, phase III study (trial registration number JapicCTI-142600) evaluated the effect of a 2-week treatment period with bilastine (20 mg once daily), fexofenadine (60 mg twice daily), or a matched placebo (double dummy) in patients with PAR...
July 12, 2016: Allergology International: Official Journal of the Japanese Society of Allergology
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