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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)...
October 15, 2016: European Journal of Pharmacology
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
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
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"...
August 11, 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
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
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...
August 6, 2016: British Journal of Clinical Pharmacology
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
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
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
Paroma Arefin, Ikramul Hasan, Md Selim Reza
The aim of the current study was to formulate Fexofenadine hydrochloride loaded sustained release microspheres using HPMC K100 M CR, a release retardant hydrophilic polymer by solvent evaporation method. The effect of different drug loading on drug content, drug encapsulation efficiency and release of drug was monitored. The studies on in vitro release mechanism were performed using USP paddle method with 900 ml of phosphate buffer (pH 6.8) for 10 h at 100 rpm. The mechanism of the drug release was determined by fitting in vitro release data to various release kinetic models such as the zero order, first order, Higuchi, Hixson Crowell and Korsemeyer-Peppas model and finding R(2) values for the release profile corresponding to each model...
2016: SpringerPlus
Kenji Kuwayama, Hajime Miyaguchi, Yuko T Iwata, Tatsuyuki Kanamori, Kenji Tsujikawa, Tadashi Yamamuro, Hiroki Segawa, Hiroyuki Inoue
Hair and nails are often used to prove long-term intake of drugs in forensic drug testing. The aim of this study was to evaluate the effectiveness of drug testing using hair and nails and the feasibility of determining when drugs were ingested by measuring the time-courses of drug concentrations in hair and toenails after single administrations of various drugs. Healthy subjects ingested four pharmaceutical products containing eight active ingredients in single doses. Hair and toenails were collected at predetermined intervals, and drug concentrations in hair and nails were measured for 12 months...
June 24, 2016: Drug Testing and Analysis
J Sánchez, J Zakzuk, R Cardona
BACKGROUND: Antihistamines are the first line of treatment for chronic spontaneous urticaria. However, there is no effective method to predict whether an antihistamine will have a beneficial clinical effect or not. OBJECTIVE: To assess whether the change in histamine-induced wheal and flare measurements 24 hours after administration of antihistamine can predict the efficacy of treatment. METHODS: We performed a multicenter, triple-blind, randomized study...
2016: Journal of Investigational Allergology & Clinical Immunology
Irene J Fisher, Patrick J Phillips, Kaitlyn M Colella, Shawn C Fisher, Tristen Tagliaferri, William T Foreman, Edward T Furlong
Coastal onsite wastewater disposal systems (OWDS) were inundated by Hurricane Sandy's storm tide. This study compares the shallow groundwater quality (nutrients, pharmaceuticals, and hormones) downgradient of OWDS before and after Hurricane Sandy, where available, and establishes a baseline for wastewater influence on groundwater in coastal communities inundated by Hurricane Sandy. Nutrients and contaminants of emerging concern (CECs) were detected in shallow groundwater downgradient of OWDS in two settings along the New Jersey and New York coastlines: 1) a single, centralized OWDS in a park; and 2) multiple OWDS (cesspools) in low-density residential and mixed-use/medium density residential areas...
June 30, 2016: Marine Pollution Bulletin
J Luo, H Imai, T Ohyama, S Hashimoto, T Hasunuma, Y Inoue, T Kotegawa, K Ohashi, N Uemura
Pharmacokinetic exposures to fexofenadine (FEX) are reduced by apple juice (AJ); however, the relationship between the AJ volume and the degree of AJ-FEX interaction has not been understood. In this crossover study, 10 healthy subjects received single doses of FEX 60 mg with different volumes (150, 300, and 600 mL) of AJ or water (control). To identify an AJ volume lacking clinically meaningful interaction, we tested a hypothesis that the 90% confidence interval (CI) for geometric mean ratio (GMR) of FEX AUCAJ /AUCwater is contained within a biocomparability bound of 0...
August 2016: Clinical and Translational Science
Satish Kumar Bedada, Praveen Kumar Boga, Harish Kaushik Kotakonda
1. Diosmin (DSN) has been found to possess P-glycoprotein (P-gp) inhibition activity in vitro and in vivo in rats, which may have potential to cause P-gp-mediated interactions in humans. The purpose of the present study was to investigate the effect of DSN on pharmacokinetics of fexofenadine (FEX) in healthy human volunteers. 2. An open-label, two-period, sequential study was conducted in 12 healthy male volunteers. A single dose of FEX 120 mg was administered to volunteers during control and treatment phases...
May 6, 2016: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
Xue Yan Wang, Margaret Lim-Jurado, Narayanan Prepageran, Pongsakorn Tantilipikorn, De Yun Wang
Allergic rhinitis and urticaria are common allergic diseases that may have a major negative impact on patients' quality of life. Bilastine, a novel new-generation antihistamine that is highly selective for the H1 histamine receptor, has a rapid onset and prolonged duration of action. This agent does not interact with the cytochrome P450 system and does not undergo significant metabolism in humans, suggesting that it has very low potential for drug-drug interactions, and does not require dose adjustment in renal impairment...
2016: Therapeutics and Clinical Risk Management
Laxmi N Jattinagoudar, Sharanappa T Nandibewoor, Shivamurti A Chimatadar
The binding interaction of peripheral H1 receptor antagonist drug, fexofenadine hydrochloride to bovine serum albumin is investigated by fluorescence spectroscopy in combination with UV-absorption spectroscopy under physiological conditions. The Stern-Volmer plots at different temperatures and the steady state fluorescence suggested a static type of interaction between fexofenadine and bovine serum albumin. Binding constants were determined to provide a measure of the binding affinity between fexofenadine and bovine serum albumin...
April 25, 2016: Journal of Biomolecular Structure & Dynamics
Huimin Yan, Michael A Behun, Marc D Cook, Sushant M Ranadive, Abbi D Lane-Cordova, Rebecca M Kappus, Jeffrey A Woods, Kenneth R Wilund, Tracy Baynard, John R Halliwill, Bo Fernhall
Post-exercise hypotension (PEH) is widely observed in Caucasians (CA) and is associated with histamine receptors 1- and 2- (H1R and H2R) mediated post-exercise vasodilation. However, it appears that blacks (BL) may not exhibit PEH following aerobic exercise. Hence, this study sought to determine the extent to which BL develop PEH, and the contribution of histamine receptors to PEH (or lack thereof) in this population. Forty-nine (22 BL, 27 CA) young and healthy subjects completed the study. Subjects were randomly assigned to take either a combined H1R and H2R antagonist (fexofenadine and ranitidine) or a control placebo...
2016: PloS One
Tanvi Gupta, Vijay K Garg, Rashmi Sarkar, Anjali Madan
Acute generalized exanthematous pustulosis (AGEP) is a skin eruption, frequently drug induced and characterized by the acute development of multiple sterile minute pustules on an erythematous base. There is no case of fexofenadine-induced AGEP in literature (PubMed search). A 40-year-old female presented to us with fever and sudden onset development of multiple discrete to coalescent 1-2 mm nonfollicular pustules on an erythematous base present mainly on her trunk and upper extremities for past 2 days. She had a history of use of fexofenadine 180 mg OD for rhinitis for 2 days...
March 2016: Indian Journal of Dermatology
Oksana Golovko, Olga Koba, Radka Kodesova, Ganna Fedorova, Vimal Kumar, Roman Grabic
The aim of this study was to develop a simple extraction procedure and a multiresidual liquid chromatography-tandem mass spectrometry method for determination of a wide range of pharmaceuticals from various soil types. An extraction procedure for 91 pharmaceuticals from 13 soil types, followed by liquid chromatography-tandem mass spectrometry analysis, was optimized. The extraction efficiencies of three solvent mixtures for ultrasonic extraction were evaluated for 91 pharmaceuticals. The best results were obtained using acetonitrile/water (1/1 v/v with 0...
July 2016: Environmental Science and Pollution Research International
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