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Benzydamine

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https://www.readbyqxmd.com/read/28819071/genetic-and-non-genetic-factors-associated-with-protein-abundance-of-flavin-containing-monooxygenase-3-in-human-liver
#1
Meijuan Xu, Deepak Kumar Bhatt, Catherine K Yeung, Katrina G Claw, Amarjit S Chaudhry, Andrea Gaedigk, Robin E Pearce, Ulrich Broeckel, Roger Gaedigk, Debbie Nickerson, Erin Schuetz, Allan E Rettie, Steven Leeder, Kenneth E Thummel, Bhagwat Prasad
Hepatic flavin-containing monooxygenase 3 (FMO3) metabolizes a broad array of nucleophilic heteroatom (e.g., N or S)-containing xenobiotics (e.g., amphetamine, sulindac, benzydamine, ranitidine, tamoxifen, nicotine, and ethioniamide), as well as endogenous compounds (e.g., catecholamine and trimethylamine). To predict the effect of genetic and non-genetic factors on the hepatic metabolism of FMO3 substrates, we quantified FMO3 protein abundance in human liver microsomes (HLM; n=445) by LC-MS/MS proteomics. Genotyping/gene-resequencing, mRNA expression, and functional activity (with benzydamine as a probe substrate) of FMO3 were also performed...
August 17, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28760731/differential-nitric-oxide-derived-protein-modifications-of-flavin-containing-monooxygenases-in-type-1-allergic-mice
#2
Tadatoshi Tanino, Toru Bando, Akira Komada, Yukie Nojiri, Yuna Okada, Yukari Ueda, Eiichi Sakurai
Flavin-containing monooxygenases (FMOs) are major mammalian non-cytochrome P450 oxidative enzymes. T Helper2 cell-activated allergic diseases produce excess levels of nitric oxide (NO) that modify the functions of proteins. However, it remains unclear whether allergy-induced NO affects the pharmacokinetics of drugs metabolized by FMOs. This study investigated alterations of hepatic microsomal FMO1 and FMO3 activities in type 1 allergic mice, and further examined the interaction of FMO1 and FMO3 with allergy-induced NO...
July 31, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28442642/vaginal-delivery-of-benzydamine-hydrochloride-through-liposomes-dispersed-in-mucoadhesive-gels
#3
Fatmanur Tuğcu-Demiröz
Liposomal vaginal drug delivery systems are important strategy in the treatment of both topical and systemic diseases. The aim of this study was to develop a vaginal delivery system for benzydamine hydrochloride (BNZ) loaded liposomes dispersed into mucoadhesive gels. The delivery system was also designed for a once a day dosage and to obtain controlled release of the BNZ. For this purpose BNZ containing gel formulations using hydroxypropyl methylcellulose (HPMC) K100M and Carbopol(®) 974P, which are composed of polymers that show promising potential as mucoadhesive vaginal delivery systems, were developed...
July 1, 2017: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28429885/intravenous-self-administration-of-benzydamine-a-non-steroidal-anti-inflammatory-drug-with-a-central-cannabinoidergic-mechanism-of-action
#4
Riccardo Avvisati, Maria Meringolo, Emiliana Stendardo, Elisa Malavasi, Silvia Marinelli, Aldo Badiani
Benzydamine (BZY) is a non-steroidal anti-inflammatory drug used for the topical treatment of inflammations of the oral and vaginal mucosae. Virtually nothing is known about the central pharmacological actions of BZY. Yet there are reports of voluntary systemic overdosage of BZY in drug addicts, resulting in a euphoric, hallucinatory state. In the present study, we investigated the reinforcing properties of BZY in a rat self-administration paradigm. We found that BZY has a powerful reinforcing effect and that this effect is greatly facilitated in animals that already had substance experience, having previously self-administered heroin and cocaine, indicating cross sensitization between BZY and other common drugs of abuse...
April 21, 2017: Addiction Biology
https://www.readbyqxmd.com/read/28352949/from-prescription-only-rx-to-over-the-counter-otc-status-in-germany-2006-2015-pharmacological-perspectives-on-regulatory-decisions
#5
Eva Barrenberg, Edeltraut Garbe
PURPOSE: Little is known about the extent of switches from prescription-only (Rx) to over-the-counter (OTC) status in Europe and about the pharmacological properties of the switched substances. The objectives of this study were to provide an overview of the substances that were switched from Rx to OTC status in Germany between 2006 and 2015 and to assess their pharmacological properties. METHODS: Session minutes of the German Expert Advisory Committee for Prescription-Only Issues, changes to the German Ordinance on Prescription-Only Medicines and the Summary of Product Characteristics of the switched substances were analysed...
July 2017: European Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28258069/marmoset-flavin-containing-monooxygenase-3-in-the-liver-is-a-major-benzydamine-and-sulindac-sulfide-oxygenase
#6
Shotaro Uehara, Makiko Shimizu, Yasuhiro Uno, Takashi Inoue, Erika Sasaki, Hiroshi Yamazaki
Common marmosets (Callithrix jacchus) are potentially primate models for preclinical drug metabolism studies because there are similarities in the molecular characteristics of cytochrome P450 enzymes between this species and humans. However, characterization of non-cytochrome P450 enzymes has not been clarified in marmosets. Here, we report characterization of flavin-containing monooxygenases FMO1-FMO5 identified in marmoset tissues. Marmoset FMO forms shared high amino acid sequence identities (93%-95%) and phylogenetic closeness with human homologous FMO forms...
May 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28247977/burning-mouth-syndrome-a-systematic-review-of-treatments
#7
REVIEW
Y F Liu, Y Kim, T Yoo, P Han, J C Inman
Burning mouth syndrome (BMS) is a chronic oral pain syndrome that primarily affects peri- and postmenopausal women. It is characterized by oral mucosal burning and may be associated with dysgeusia, paresthesia, dysesthesia, and xerostomia. The etiology of the disease process is unknown, but is thought to be neuropathic in origin. The goal of this systematic review was to assess the efficacy of the various treatments for BMS. Literature searches were conducted through PubMed, Web of Science, and Cochrane Library databases, which identified 22 randomized controlled trials...
March 1, 2017: Oral Diseases
https://www.readbyqxmd.com/read/28195065/effect-of-econazole-and-benzydamine-on-sensory-neurons-in-culture
#8
S Mathivanan, R de la Torre-Martinez, C Wolf, G Mangano, L Polenzani, C Milanese, A Ferrer-Montiel
Econazole is an anti-mycotic agent widely used for the treatment of cutaneous fungal infections, and for the therapy of vaginal candidiasis. Topical application of this azole is generally safe, although some patients have complained of mild burning sensation/cutaneous irritation and itching, especially when administered intravaginally. The underlying mechanisms responsible of these adverse effects are poorly understood, though they suggest excitation of cutaneous nociceptor terminals. We report that exposure of primary cultures of rat nociceptors to econazole augments neuronal excitability...
December 2016: Journal of Physiology and Pharmacology: An Official Journal of the Polish Physiological Society
https://www.readbyqxmd.com/read/28145791/human-plasma-metabolic-profiles-of-benzydamine-a-flavin-containing-monooxygenase-probe-substrate-simulated-with-pharmacokinetic-data-from-control-and-humanized-liver-mice
#9
Miho Yamazaki-Nishioka, Makiko Shimizu, Hiroshi Suemizu, Megumi Nishiwaki, Marina Mitsui, Hiroshi Yamazaki
1. Benzydamine is used clinically as a nonsteroidal anti-inflammatory drug in oral rinses and is employed in preclinical research as a flavin-containing monooxygenase (FMO) probe substrate. In this study, plasma concentrations of benzydamine and its primary N-oxide and N-demethylated metabolites were investigated in control TK-NOG mice, in humanized-liver mice, and in mice whose liver cells had been ablated with ganciclovir. 2. Following oral administration of benzydamine (10 mg/kg) in humanized-liver TK-NOG mice, plasma concentrations of benzydamine N-oxide were slightly higher than those of demethyl benzydamine...
February 1, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/28137602/identification-of-human-flavin-containing-monooxygenase-3-substrates-by-a-colorimetric-screening-assay
#10
Gianluca Catucci, Isabelle Polignano, Debora Cusumano, Claudio Medana, Gianfranco Gilardi, Sheila J Sadeghi
Human hepatic flavin-containing monooxygenase 3 is a phase I drug-metabolizing enzyme that is responsible for the oxidation of a variety of drugs and xenobiotics. This work reports on a high throughput rapid colorimetric assay for the screening of substrates or inhibitors of this enzyme. The method is based on the competition of two substrates for access to the active site of hFMO3 whereby the enzymatic product of the first drug converts nitro-5-thiobenzoate (TNB, yellow) to 5,5'-dithiobis (2-nitrobenzoate) (DTNB, colourless)...
April 1, 2017: Analytical Biochemistry
https://www.readbyqxmd.com/read/28054999/interaction-between-dna-and-drugs-having-protonable-basic-groups-characterization-through-affinity-constants-drug-release-kinetics-and-conformational-changes
#11
Liliana P Alarcón, Yolima Baena, Rubén H Manzo
This paper reports the in vitro characterization of the interaction between the phosphate groups of DNA and the protonated species of drugs with basic groups through the determination of the affinity constants, the reversibility of the interaction, and the effect on the secondary structure of the macromolecule. Affinity constants of the counterionic condensation DNA-drug were in the order of 10⁶. The negative electrokinetic potential of DNA decreased with the increase of the proportion of loading drugs. The drugs were slowly released from the DNA-drug complexes and had release kinetics consistent with the high degree of counterionic condensation...
January 4, 2017: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/27987094/role-of-benzydamine-hydrochloride-in-the-prevention-of-oral-mucositis-in-head-and-neck-cancer-patients-treated-with-radiotherapy-50%C3%A2-gy-with-or-without-chemotherapy
#12
Madhup Rastogi, Rohini Khurana, Swaroop Revannasiddaiah, Isha Jaiswal, Sambit S Nanda, Pooja Gupta, Kundan S Chufal, M L Bhatt
PURPOSE: Benzydamine is recommended for prophylaxis of oral mucositis (OM) in head and neck cancer (HNC) patients for radiation doses (<50 Gy). This study evaluates role of benzydamine for higher radiation doses (>50 Gy) with or without chemotherapy. METHODS: One hundred twenty patients of HNC with planned radiation doses of ≥60 Gy were randomized to group A (control radiotherapy alone), group B (study radiotherapy alone), group C (control chemoradiotherapy), or to group D (study chemoradiotherapy)...
December 16, 2016: Supportive Care in Cancer: Official Journal of the Multinational Association of Supportive Care in Cancer
https://www.readbyqxmd.com/read/27918734/protocols-for-management-of-oral-complications-of-chemotherapy-and-or-radiotherapy-for-oral-cancer-systematic-review-and-meta-analysis-current
#13
J-N Carneiro-Neto, J-D-S de-Menezes, L-B Moura, E-M-S Massucato, C-R de-Andrade
BACKGROUND AND OBJECTIVE: Considering the high possibility of dentist consult a patient with oral complications of chemotherapy and/or radiotherapy for oral cancer because of the advances in this area, this study aims to systematically review the literature to identify and suggest effective and safe protocols for the managements of oral complications in oncology patients. MATERIAL AND METHODS: The systematic review was designed by PICO and PRISMA including eligibility and exclusion criteria; the source of information and search strategy in PubMed according MeSH: "Mouth Neoplasms and Radiotherapy" and "Mouth Neoplasms and Drug Therapy" the period from 2010 to 2015; selection and data collection of study was carried form blind and independently by two researchers; risk of bias and methodological quality: ensured by the PEDro scale; synthesis of data: of oral complications were evaluated by adapted version of associative direction classification proposed by Costigan and collaborators; and data analysis was performed by the meta-analysis of BioEstat program (5...
January 1, 2017: Medicina Oral, Patología Oral y Cirugía Bucal
https://www.readbyqxmd.com/read/27644912/management-of-radiation-and-chemotherapy-related-acute-toxicity-in-gastrointestinal-cancer
#14
REVIEW
Gerhard G Grabenbauer, Göbel Holger
Possible toxic effects following radiation and chemotherapy of gastrointestinal tumours may cause a depletion of the mucosal barrier within the radiation volumes with severe mucositis. Diarrhoea, nausea, emesis and severe malabsorption followed by infections with dehydration and electrolyte disorders have to be encountered. For prevention and treatment of oropharyngeal mucositis an oral care protocol, oral cryotherapy together with benzydamine mouthwash may be recommended. Lower gastrointestinal diarrhoea is best treated by Octreotide (>100 μg s...
August 2016: Best Practice & Research. Clinical Gastroenterology
https://www.readbyqxmd.com/read/27523475/human-flavin-containing-monooxygenase-3-structural-mapping-of-gene-polymorphisms-and-insights-into-molecular-basis-of-drug-binding
#15
Chongliang Gao, Gianluca Catucci, Giovanna Di Nardo, Gianfranco Gilardi, Sheila J Sadeghi
Human hepatic flavin-containing monooxygenase 3 (hFMO3) catalyses the monooxygenation of carbon-bound reactive heteroatoms and plays an important role in the metabolism of drugs and xenobiotics. Although numerous hFMO3 allelic variants have been identified in patients and their biochemical properties well-characterised in vitro, the molecular mechanisms underlying loss-of-function mutations have still not been elucidated due to lack of detailed structural information of hFMO3. Therefore, in this work a 3D structural model of hFMO3 was generated by homology modeling, evaluated by a variety of different bioinformatics tools, refined by molecular dynamics simulations and further assessed based on in vitro biochemical data...
November 15, 2016: Gene
https://www.readbyqxmd.com/read/27344198/misuse-of-otc-drugs-in-poland
#16
Tomasz Zaprutko, Dorota Koligat, Michał Michalak, Marta Wieczorek, Malwina Józiak, Monika Ratajczak, Kinga Szydłowska, Joanna Miazek, Krzysztof Kus, Elżbieta Nowakowska
INTRODUCTION: The misuse of over-the-counter (OTC) drugs became a global public health concern. Although abuse with dextrometorphan (DXM), pseudoefedrine (PSD), codeine (COD) or benzydamine (BND) may lead even to psychosis, drugs containing these substances are relatively cheap and freely available. In Poland the Act on Counteracting Drug Addiction was amended in 2015, however it seems that there are still some points which could be improved. METHODS: Study was conducted between October 2014 and June 2015 using a specially designed questionnaire delivered to pharmacists from the Greater Poland region...
August 2016: Health Policy
https://www.readbyqxmd.com/read/27108819/comparative-study-between-benzydamine-hydrochloride-gel-lidocaine-5-gel-and-lidocaine-10-spray-on-endotracheal-tube-cuff-as-regards-postoperative-sore-throat
#17
COMPARATIVE STUDY
Nashwa Abdallah Mekhemar, Ahmed Samy El-Agwany, Wafaa Kamel Radi, Sherif Mohammed El-Hady
Postoperative sore throat is a common complication after endotracheal intubation. After tracheal intubation, the incidence of sore throat varies from 14.4% to 50%. The aim of the study was to compare between benzydamine hydrochloride gel, lidocaine 5% gel and lidocaine 10% spray on the endotracheal tube cuff as regards postoperative sore throat. The present study was carried out on 124 patients admitted to Alexandria university hospitals for lumbar fixation surgery requiring general anesthesia. Patients were randomly allocated into 4 groups...
May 2016: Brazilian Journal of Anesthesiology
https://www.readbyqxmd.com/read/26993406/-comparative-study-between-benzydamine-hydrochloride-gel-lidocaine-5-gel-and-lidocaine-10-spray-on-endotracheal-tube-cuff-as-regards-postoperative-sore-throat
#18
Nashwa Abdallah Mekhemar, Ahmed Samy El-Agwany, Wafaa Kamel Radi, Sherif Mohammed El-Hady
Postoperative sore throat is a common complication after endotracheal intubation. After tracheal intubation, the incidence of sore throat varies from 14.4% to 50%. The aim of the study was to compare between benzydamine hydrochloride gel, lidocaine 5% gel and lidocaine 10% spray on the endotracheal tube cuff as regards postoperative sore throat. The present study was carried out on 124 patients admitted to Alexandria university hospitals for lumbar fixation surgery requiring general anesthesia. Patients were randomly allocated into 4 groups...
May 2016: Revista Brasileira de Anestesiologia
https://www.readbyqxmd.com/read/26786266/does-type-of-pharyngeal-packing-during-sinonasal-surgery-have-an-effect-on-ponv-and-throat-pain
#19
RANDOMIZED CONTROLLED TRIAL
Basak Ceyda Meco, Menekse Ozcelik, Cigdem Yildirim Guclu, Suha Beton, Yuce Islamoglu, Aysegul Turgay, Cem Meco, Yesim Batislam
OBJECTIVE: Postoperative nausea and vomiting (PONV) is a common problem that affects up to 30% of all surgical patients after general anaesthesia, which increases in sinonasal surgery due the very potent emetic effect of ingested blood that is swallowed during the procedures. Therefore, a hypo/oropharyngeal packing is commonly placed in an effort to prevent blood ingestion. The primary aim of this study was to compare the efficacy of 3 packing types in preventing PONV and to compare the results with patients who received no packing...
April 2016: Otolaryngology—Head and Neck Surgery
https://www.readbyqxmd.com/read/26745781/burning-mouth-syndrome
#20
Joanna Zakrzewska, John A G Buchanan
INTRODUCTION: Burning mouth syndrome mainly affects women, particularly after the menopause, when its prevalence may be 18% to 33%. METHODS AND OUTCOMES: We conducted a systematic overview, aiming to answer the following clinical question: What are the effects of selected treatments for burning mouth syndrome? We searched: Medline, Embase, The Cochrane Library, and other important databases up to January 2015 (Clinical Evidence overviews are updated periodically; please check our website for the most up-to-date version of this overview)...
January 7, 2016: Clinical Evidence
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