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M Teresa Viciosa, Joaquim J Moura Ramos, Hermínio P Diogo
The slow molecular mobility in the amorphous solid state of 3 active pharmaceutical drugs (cimetidine, nizatidine, and famotidine) has been studied using differential scanning calorimetry and the 2 dielectric-related techniques of dielectric relaxation spectroscopy and thermally stimulated depolarization currents. The glass-forming ability, the glass stability, and the tendency for crystallization from the equilibrium melt were investigated by differential scanning calorimetry, which also provided the characterization of the main relaxation of the 3 glass formers...
October 20, 2016: Journal of Pharmaceutical Sciences
Sayaka Sasaoka, Toshinobu Matsui, Yuuki Hane, Junko Abe, Natsumi Ueda, Yumi Motooka, Haruna Hatahira, Akiho Fukuda, Misa Naganuma, Shiori Hasegawa, Yasutomi Kinosada, Mitsuhiro Nakamura
Long QT syndrome (LQTS) is a disorder of the heart's electrical activity that infrequently causes severe ventricular arrhythmias such as a type of ventricular tachycardia called torsade de pointes (TdP) and ventricular fibrillation, which can be fatal. There have been no previous reports on the time-to-onset for LQTS based on data from spontaneous reporting systems. The aim of this study was to assess the time-to-onset of LQTS according to drug treatment. We analyzed the association between 113 drugs in 37 therapeutic categories and LQTS including TdP using data obtained from the Japanese Adverse Drug Event Report database...
2016: PloS One
Zekai Halici, Beyzagul Polat, Elif Cadirci, Atilla Topcu, Emre Karakus, Duygu Kose, Abdulmecit Albayrak, Yasin Bayir
PURPOSE: Previously blocking the renin angiotensin system (RAAS) has been effective in the prevention of gastric damage. Therefore, the aim of this study was to investigate the effects of aliskiren, and thus, direct renin blockage, in indomethacin-induced gastric damage model. METHODS: Effects of aliskiren were evaluated in indomethacin-induced gastric damage model on Albino Wistar rats. Effects of famotidine has been investigated as standard antiulcer agent. Stereological analyses for ulcer area determination, biochemical analyses for oxidative status determination and molecular analyses for tissue cytokine and cyclooxygenase determination were performed on stomach tissues...
October 25, 2016: Chemico-biological Interactions
Francis K L Chan, Moe Kyaw, Tetsuya Tanigawa, Kazuhide Higuchi, Kazuma Fujimoto, Pui Kuan Cheong, Vivian Lee, Yoshikazu Kinoshita, Yuji Naito, Toshio Watanabe, Jessica Y L Ching, Kelvin Lam, Angeline Lo, Heyson Chan, Rashid Lui, Raymond S Y Tang, Yasuhisa Sakata, Yee Kit Tse, Toshihisa Takeuchi, Osamu Handa, Hiroko Nebiki, Justin C Y Wu, Takashi Abe, Tsuyoshi Mishiro, Siew C Ng, Tetsuo Arakawa
BACKGROUND & AIMS: It is not clear whether H2-receptor antagonists (H2RAs) reduce the risk of gastrointestinal (GI) bleeding in aspirin users at high risk. We performed a double-blind randomized trial to compare the effects of a proton pump inhibitor (PPI) vs a H2RA antagonist in preventing recurrent upper gastrointestinal (GI) bleeding and ulcers in high-risk aspirin users. METHODS: We studied 270 users of low-dose aspirin (325 mg or less per day) with a history of endoscopically confirmed ulcer bleeding at 8 sites in Hong Kong and Japan...
September 15, 2016: Gastroenterology
Ava Vila-Leahey, Sharon A Oldford, Paola A Marignani, Jun Wang, Ian D Haidl, Jean S Marshall
Histamine receptor 2 (H2) antagonists are widely used clinically for the control of gastrointestinal symptoms, but also impact immune function. They have been reported to reduce tumor growth in established colon and lung cancer models. Histamine has also been reported to modify populations of myeloid-derived suppressor cells (MDSCs). We have examined the impact of the widely used H2 antagonist ranitidine, on both myeloid cell populations and tumor development and spread, in three distinct models of breast cancer that highlight different stages of cancer progression...
July 2016: Oncoimmunology
Shinichi Otani, Taiji Nagaoka, Tsuneaki Omae, Ichiro Tanano, Takayuki Kamiya, Shinji Ono, Travis W Hein, Lih Kuo, Akitoshi Yoshida
PURPOSE: Although endothelium-dependent nitric oxide (NO)-mediated dilation of retinal arterioles has been well described, the role of endothelium-derived hyperpolarizing factor (EDHF) in the retinal arteriolar response remains unclear. In the current study, we examined the contribution of EDHF to the retinal arteriolar dilation to the inflammatory agent histamine and investigated the signaling mechanisms underlying this vasomotor activity. METHODS: Porcine retinal arterioles were isolated, cannulated, and pressurized without flow for functional study by using video microscopic techniques...
September 1, 2016: Investigative Ophthalmology & Visual Science
Hang Yin, Runmiao Wang, Jianbo Wan, Ying Zheng, Defang Ouyang, Ruibing Wang
The histamine H₂-receptor antagonists cimetidine, famotidine and nizatidine are individually encapsulated by macrocyclic cucurbit[7]uril (CB[7]), with binding affinities of 6.57 (±0.19) × 10³ M(-1), 1.30 (±0.27) × 10⁴ M(-1) and 1.05 (±0.33) × 10⁵ M(-1), respectively. These 1:1 host-guest inclusion complexes have been experimentally examined by ¹H-NMR, UV-visible spectroscopic titrations (including Job plots), electrospray ionization mass spectrometry (ESI-MS), and isothermal titration calorimetry (ITC), as well as theoretically by molecular dynamics (MD) computation...
2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Heiko Schenk, Detlef Neumann, Christina Kloth
OBJECTIVE AND DESIGN: The modulation of antigen uptake and activation of dendritic cells (DCs) by histamine may function as a regulator of inflammation. Therefore, we sought to determine the impact of histamine on antigen uptake by and activation of murine DCs. MATERIAL AND METHODS: DCs from spleen and lung were either identified by flow cytometry or were immunomagnetically enriched. Cells were stimulated with histamine, and the regulation of MHC-II and co-stimulatory molecule expression (CD80, CD86, and ICOS-L) and antigen uptake were quantified by flow cytometry...
October 2016: Immunopharmacology and Immunotoxicology
Y KalantarMotamedi, M Peymani, H Baharvand, M H Nasr-Esfahani, A Bender
Small molecules are being increasingly used for inducing the targeted differentiation of stem cells to different cell types. However, until now no systematic method for selecting suitable small molecules for this purpose has been presented. In this work, we propose an integrated and general bioinformatics- and cheminformatics-based approach for selecting small molecules which direct cellular differentiation in the desired way. The approach was successfully experimentally validated for differentiating stem cells into cardiomyocytes...
2016: Cell Death Discovery
Sneh Verma, Vijay L Kumar
A number of factors like alcohol consumption, stress, use of non steroidal anti-inflammatory drugs and acidity are well known to increase the risk of development of gastric ulcers. The present study was carried out to investigate the protective effect of artesunate against gastric injury induced in rats by oral administration of ethanol and by pylorus ligation in independent sets of experiments. The groups included in each set (n = 6 per group) were normal control, experimental control and drug treated groups: artesunate 50 and 150 mg/kg (ART 50 and ART 150) and famotidine 20 mg/kg (FAM 20)...
September 25, 2016: Chemico-biological Interactions
Feng Zhao, Sheng Wang, Lin Liu, Yijuan Wang
To evaluate the efficacy of members of the H2RA family for the treatment of gastro-esophageal reflux disease (GERD). We performed a thorough electronic search on PubMed, EMBASE, and the Cochrane Central Register of Controlled Trials (CENTRAL) for eligible randomized clinical trials that investigated H2RAs and the treatment of GERD up to July 28, 2015. A comprehensive network meta-analysis was conducted to compare the effects of each subset of H2RAs. A total of 13 randomized controlled trials (RCTs) were included in our network meta-analysis...
October 2016: International Journal of Clinical Pharmacology and Therapeutics
Hye Kyung Kim, Myung-Gyou Kim, Kang-Hyun Leem
OBJECTIVE: To investigate the gastroprotective effects of Acanthopanax senticosus leaves (ASLs) extrusion on acute gastric mucosal lesion in rats induced by compound 48/80 (C48/80). METHODS: Rats were divided into six groups: normal; C48/80-induced gastric lesion control; gastric lesion positive control (famotidine 4 mg/kg); gastric lesion administered with two levels of extruded ASLs (ASLE, 40 and 200 mg/kg); and gastric lesion treated with ASLs (ASL 200 mg/kg)...
April 2016: Journal of Traditional Chinese Medicine, Chung i Tsa Chih Ying Wen Pan
Sylwia Smolinska, David Groeger, Noelia Rodriguez Perez, Elisa Schiavi, Ruth Ferstl, Remo Frei, Patrycja Konieczna, Cezmi A Akdis, Marek Jutel, Liam OʼMahony
BACKGROUND: Histamine is a key immunoregulatory mediator in immediate-type hypersensitivity reactions and chronic inflammatory responses, in particular histamine suppresses proinflammatory responses to bacterial ligands, through histamine receptor 2 (H2R). The aim of this study was to investigate the effects of histamine and H2R on bacteria-induced inflammatory responses in patients with IBD. METHODS: Peripheral blood mononuclear cells (PBMCs) were obtained from patients with Crohn's disease, patients with ulcerative colitis, and healthy controls...
July 2016: Inflammatory Bowel Diseases
Lesley Pahs, Chris Droege, Hilary Kneale, Arthur Pancioli
Orolingual angioedema is a rare adverse effect of tissue plasminogen activator (tPA), with an incidence of 1% to 5%. There are currently no published reports describing resolution of tPA-induced orolingual angioedema with complement inhibitor therapy. A 72-year-old man receiving home angiotensin-converting enzyme inhibitor therapy presented to the emergency department with newly developed orolingual angioedema after treatment with tPA for acute ischemic stroke. Therapy was initiated with intravenous methylprednisolone 125 mg, famotidine 20 mg, and diphenhydramine 50 mg, without significant improvement...
September 2016: Annals of Emergency Medicine
Chara Litou, Maria Vertzoni, Constantinos Goumas, Vassilis Vasdekis, Wei Xu, Filippos Kesisoglou, Christos Reppas
OBJECTIVE: Evaluate the impact of reduced gastric acid secretion after administration of two acid-reducing agents on the physicochemical characteristics of contents of upper gastrointestinal lumen of fasted adults. MATERIALS AND METHODS: Eight healthy male adults, fasted from food for 12 h, participated in a three-phase crossover study. Phase 1: No drug treatment prior to aspirations. Phase 2: Oral administration of 40 mg pantoprazole at ~9 am the last 3 days prior to aspirations and at ~7 am on aspiration day...
June 2016: Pharmaceutical Research
M Zendehdel, A Baghbanzadeh, P Aghelkohan, S Hassanpour
The aim of the current study was to investigate the interaction of the lipopolysaccharide (LPS) and histaminergic systems on appetite regulation in broilers. Effects of intracerebroventricular (ICV) injection of α-fluoromethylhistidine (α-FMH, histidine decarboxylase inhibitor), chlorpheniramine (histamine H1 receptor antagonist), famotidine (histamine H2 receptor antagonist) and thioperamide (histamine H3 receptor antagonist) on LPS-induced hypophagia in broilers were studied. A total of 128 broilers were randomly allocated into 4 experiments (4 groups and 8 replications in each experiment)...
April 2016: British Poultry Science
Fumiaki Kitazawa, Yoko Kado, Kumi Ueda, Takatoshi Kokufu, Shin-Ichi Fuchida, Akira Okano, Mayumi Hatsuse, Satoshi Murakami, Yuko Nakayama, Kohji Takara, Chihiro Shimazaki
The aim of the present study was to clarify whether gastric antisecretory drugs affect the clinical efficacy and toxicity of orally administered melphalan in patients with multiple myeloma. A total of 10 patients receiving bortezomib plus oral melphalan and prednisolone (VMP) therapy between December 2011 and November 2014 were analyzed retrospectively. The patients were divided into a control group (seven patients) and a concomitant group (three patients, who were also administered with gastric antisecretory drugs)...
February 2016: Molecular and Clinical Oncology
Jing Liu, Dan Sun, Jinfeng He, Chengli Yang, Tingting Hu, Lijing Zhang, Hua Cao, Ai-Ping Tong, Xiangrong Song, Yongmei Xie, Gu He, Gang Guo, Youfu Luo, Ping Cheng, Yu Zheng
Ibuprofen is the first line of treatment for osteoarthritis and arthritis. The main side effects of ibuprofen especially in long-term treatment include gastric ulcer, duodenal ulcer and indigestion etc. Therefore, screening drugs with effective gastric protective effects and low toxicity for combination therapy with ibuprofen is necessary. The mechanism of gastric damage induced by ibuprofen is still unclear, however, cell damage caused by reactive oxygen species (ROS) is considered as the main reason. Preliminary screening of literature with the criteria of low toxicity led to four histamine-2 receptor antagonists (H2RAs): nizatidine, famotidine, lafutidine, and roxatidine acetate, which were selected for further investigation...
March 15, 2016: Life Sciences
Mohamed-Amine Jabri, Haifa Tounsi, Kais Rtibi, Lamjed Marzouki, Mohsen Sakly, Hichem Sebai
Context Myrtle, Myrtus communis L. (Myrtaceae), is a medicinal plant well known for its richness in phenolic compounds and its beneficial effects for the treatment of gastrointestinal disorders. Objective In the present work, the protective effect of the myrtle berry seed aqueous extract (MBSAE) against esophageal reflux (ER)-induced damage in esophagus mucosa as well as the mechanisms implicated was determined. Materials and methods In this respect, adult male Wistar rats were used and divided into seven groups: Control, ER, ER + various doses of MBSAE, ER + famotidine or ER + gallic acid...
January 25, 2016: Pharmaceutical Biology
Debasis Das, Papiya Sikdar, Moumita Bairagi
The 2-aminothiazole (2-AT) core is an active pharmacophore and used in medicinal chemistry and drug discovery research. A number of drugs with 2-AT core are in the market, e.g. Famotidine, Cefdinir, Meloxcam etc. Recently, 2-AT core has been explored for many more important therapeutic areas and identified new 2-aminothiazoles with anticancer, antitumor, antidiebatic and anticonvulsant activity. In this review, we discuss the newly identified and developed 2-aminothiazoles in recent years and their use in medicinal chemistry and pharmacology...
February 15, 2016: European Journal of Medicinal Chemistry
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