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https://www.readbyqxmd.com/read/28521025/mechanism-of-as2o3-induced-action-potential-prolongation-and-using-hips-cms-to-evaluate-the-rescue-efficacy-of-drugs-with-different-rescue-mechanism
#1
Meng Yan, Lifang Feng, Yanhui Shi, Junnan Wang, Yan Liu, Fengmei Li, Baoxin Li
Arsenic trioxide (As2O3) has been verified as a breakthrough in the management of acute promyelocytic leukemia in recent decades. However, cardiotoxicity, especially long QT syndrome (LQTS) has become the most important issue during As2O3 treatment. The characterized mechanisms behind this adverse effect are inhibition of cardiac hERG channel trafficking and increase of cardiac calcium currents. In our study, we found a new pathway underlying As2O3-induced cardiotoxicity that As2O3 accelerates lysosomal degradation of hERG on plasma membrane after using brefeldin A (BFA) to block protein trafficking...
May 17, 2017: Toxicological Sciences: An Official Journal of the Society of Toxicology
https://www.readbyqxmd.com/read/28511488/comparative-efficacy-and-safety-of-ebastine-20-mg-ebastine-10-mg-and-levocetirizine-5-mg-in-acute-urticaria
#2
Vippan Goyal, Anu Gupta, Onam Gupta, Dhruvendra Lal, Manharan Gill
INTRODUCTION: Acute and chronic urticaria can result in severely impaired quality of life from pruritus and associated sleep lessness, as well as anxiety and depression. Various treatment modalities are available out of which second generation non sedating H1 antihistamines e.g., fexofenadine, loratidine, desloratadine, cetirizine, levocetirizine, ebastine etc., are used as the first line treatment. AIM: To compare the safety and efficacy of ebastine 20 mg, ebastine 10 mg and levocetirizine 5 mg in the patients of urticaria...
March 2017: Journal of Clinical and Diagnostic Research: JCDR
https://www.readbyqxmd.com/read/28456083/microfluidic-photoinduced-chemical-oxidation-for-ru-bpy-3-3-chemiluminescence-a-comprehensive-experimental-comparison-with-on-chip-direct-chemical-oxidation
#3
Afsal Mohammed Kadavilpparampu, Haider A J Al Lawati, Fakhr Eldin O Suliman
For the first time, the analytical figures of merit in detection capabilities of the very less explored photoinduced chemical oxidation method for Ru(bpy)3(2+) CL has been investigated in detail using 32 structurally different analytes. It was carried out on-chip using peroxydisulphate and visible light and compared with well-known direct chemical oxidation approaches using Ce(IV). The analytes belong to various chemical classes such as tertiary amine, secondary amine, sulphonamide, betalactam, thiol and benzothiadiazine...
April 21, 2017: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
https://www.readbyqxmd.com/read/28437851/fexofenadine-a-putative-in-vivo-p-glycoprotein-probe-fails-to-predict-clearance-of-the-substrate-tacrolimus-in-renal-recipients
#4
Thomas Vanhove, Thomas Bouillon, Henriëtte de Loor, Pieter Annaert, Dirk R J Kuypers
Whether combined use of probe drugs for CYP3A4 and P-glycoprotein can clarify the relative contribution of these proteins to pharmacokinetic variability of a dual substrate like tacrolimus has never been assessed. Seventy renal recipients underwent simultaneous 8-hour pharmacokinetic profiles for tacrolimus, the CYP3A4 probe midazolam and the putative P-glycoprotein probe fexofenadine. Patients were genotyped for polymorphisms in CYP3A5, CYP3A4, ABCB1, ABCC2 and SLCO2B1, -1B1 and 1B3. Carriers of the ABCB1 2677G>A polymorphism displayed lower fexofenadine Cmax (-66%; P=0...
April 24, 2017: Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28414144/intestinal-drug-interactions-mediated-by-oatps-a-systematic-review-of-pre-clinical-and-clinical-findings
#5
REVIEW
Jingjing Yu, Zhu Zhou, Jessica Tay-Sontheimer, René H Levy, Isabelle Ragueneau-Majlessi
In recent years, an increasing number of clinical drug-drug interactions (DDIs) have been attributed to inhibition of intestinal organic anion transporting polypeptides (OATPs); however, only a few of these DDI results were reflected in drug labels. This review aims to provide a thorough analysis of intestinal OATP-mediated pharmacokinetic-based DDIs, using both in vitro and clinical investigations, highlighting the main mechanistic findings and discussing their clinical relevance. On the basis of pharmacogenetic and clinical DDI results, a total of 12 drugs were identified as possible clinical substrates of OATP2B1 and/or OATP1A2...
April 13, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28401798/most-frequently-reported-prescription-medications-and-supplements-in-couples-planning-pregnancy-the-life-study
#6
Kristin Palmsten, Katrina F Flores, Christina D Chambers, Lauren A Weiss, Rajeshwari Sundaram, Germaine M Buck Louis
OBJECTIVE: To identify frequently reported prescription medications and supplements among couples planning pregnancy because there is a lack of descriptive information on these agents in women and men who are trying to conceive. METHODS: Five hundred one couples enrolled in the Longitudinal Study of Infertility and the Environment, which took place between 2005 and 2009. Participants reported prescription medications as well as prescription and over-the-counter supplements used through interviews at study enrollment and through daily dairies during the 12-month follow-up...
January 1, 2017: Reproductive Sciences
https://www.readbyqxmd.com/read/28301431/cyp3a4-activity-is-markedly-lower-in-patients-with-crohn-s-disease
#7
Aze Wilson, Rommel G Tirona, Richard B Kim
BACKGROUND: Disease-dependent changes in the activity of drug metabolizing enzymes and transporters, such as Cytochrome P450 (CYP) 3A4 and P-glycoprotein (P-gp), are thought to have a major influence on the disposition of shared substrates. However, little is known regarding the in vivo relevance of these 2 proteins during drug therapy for gastrointestinal diseases. Our aim was to elucidate the activity of CYP3A4 and P-gp in subjects with Crohn's disease (CD) and to evaluate their influence on budesonide pharmacokinetics...
May 2017: Inflammatory Bowel Diseases
https://www.readbyqxmd.com/read/28188296/effect-of-garlic-gingko-and-st-john-s-wort-extracts-on-the-pharmacokinetics-of-fexofenadine-a-mechanistic-study
#8
Jasmina Turkanovic, Michael B Ward, Jacobus P Gerber, Robert W Milne
The aim of this study was to determine the effects of garlic and ginkgo herbal extracts on the pharmacokinetics of the P-glycoprotein (P-gp)/organic anion-transporting polypeptides (Oatps) substrate fexofenadine. Male rats were dosed orally with garlic (120 mg/kg), ginkgo (17 mg/kg), St. John's wort (SJW; 1000 mg/kg; positive control), or Milli-Q water for 14 days. On day 15, rats either were administered fexofenadine (orally or i.v.), had their livers isolated and perfused with fexofenadine, or had their small intestines divided into four segments (SI-SIV) and analyzed for P-gp and Oatp1a5...
May 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28102715/capsaicin-pretreatment-enhanced-the-bioavailability-of-fexofenadine-in-rats-by-p-glycoprotein-modulation-in-vitro-in-situ-and-in-vivo-evaluation
#9
Satish Kumar Bedada, Ramgopal Appani, Praveen Kumar Boga
BACKGROUND AND OBJECTIVE: Capsaicin is the main pungent principle present in chili peppers has been found to possess P-glycoprotein (P-gp) inhibition activity in vitro, which may have the potential to modulate bioavailability of P-gp substrates. Therefore, purpose of this study was to evaluate the effect of capsaicin on intestinal absorption and bioavailability of fexofenadine, a P-gp substrate in rats. METHODS: The mechanistic evaluation was determined by non-everted sac and intestinal perfusion studies to explore the intestinal absorption of fexofenadine...
June 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28090646/influence-of-p-glycoprotein-on-the-disposition-of-fexofenadine-and-its-enantiomers
#10
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...
March 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
#11
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...
February 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
#12
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
#13
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
#14
Shigeru Hishinuma, Kiyoe Kosaka, Chizuru Akatsu, Yoshihiro Uesawa, Hiroyuki Fukui, Masaru Shoji
The affinity of ligands for G-protein-coupled receptors (GPCRs) 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 100mM NaCl...
March 15, 2017: 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
#15
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
#16
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...
March 2017: 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
#17
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
#18
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
#19
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
#20
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
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