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https://www.readbyqxmd.com/read/29038464/unveiling-some-fda-approved-drugs-as-inhibitors-of-the-store-operated-ca-2-entry-pathway
#1
Saifur Rahman, Taufiq Rahman
The store-operated calcium entry (SOCE) pathway is an important route for generating cytosolic Ca(2+) signals that regulate a diverse array of biological processes. Abnormal SOCE seem to underlie several diseases that notably include allergy, inflammation and cancer. Therefore, any modulator of this pathway is likely to have significant impact in cell biology under both normal and abnormal conditions. In this study, we screened the FDA-approved drug library for agents that share significant similarity in 3D shape and surface electrostatics with few, hitherto best known inhibitors of SOCE...
October 16, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29034101/lamotrigine-induced-sexual-dysfunction-and-non-adherence-case-analysis-with-literature-review
#2
Kenneth R Kaufman, Melissa Coluccio, Kartik Sivaraaman, Miriam Campeas
BACKGROUND: Optimal anti-epileptic drug (AED) treatment maximises therapeutic response and minimises adverse effects (AEs). Key to therapeutic AED treatment is adherence. Non-adherence is often related to severity of AEs. Frequently, patients do not spontaneously report, and clinicians do not specifically query, critical AEs that lead to non-adherence, including sexual dysfunction. Sexual dysfunction prevalence in patients with epilepsy ranges from 40 to 70%, often related to AEDs, epilepsy or mood states...
September 2017: BJPsych Open
https://www.readbyqxmd.com/read/29033425/evaluation-by-mr-enterocolonography-of-lansoprazole-induced-collagenous-colitis-accompanied-with-protein-losing-enteropathy-a-case-report
#3
Akinori Mizoguchi, Masaaki Higashiyama, Keisuke Ikeyama, Shin Nishii, Hisato Terada, Hirotaka Furuhashi, Takeshi Takajo, Koji Maruta, Yuichi Yasutake, Kazuhiko Shirakabe, Chikako Watanabe, Kengo Tomita, Shunsuke Komoto, Shigeaki Nagao, Soichiro Miura, Ryota Hokari
We herein describe a 69-year-old man suffering from chronic diarrhea caused by lansoprazole (LPZ)-induced collagenous colitis (CC) accompanied with protein-losing enteropathy (PLE), diagnosed by increased fecal alpha-1 antitrypsin clearance and the findings of leakage from the descending colon to the sigmoid colon on scintigraphy. MR enterocolonography (MREC) was also performed for differentiating digestive diseases, and inflamed findings were observed around the same portion as those on scintigraphy, suggesting that this region was responsible for protein loss in this case...
October 16, 2017: Internal Medicine
https://www.readbyqxmd.com/read/29027194/predictive-performance-of-physiologically-based-pharmacokinetic-pbpk-modeling-of-drugs-extensively-metabolized-by-major-cytochrome-p450s-in-children
#4
Wangda Zhou, Trevor N Johnson, Khanh H Bui, S Y Amy Cheung, Jianguo Li, Hongmei Xu, Nidal Al-Huniti, Diansong Zhou
The accuracy of physiologically-based pharmacokinetic (PBPK) model prediction in children, especially those younger than 2 years old has not been systematically evaluated. The aim of this study was to characterize the pediatric predictive performance of the PBPK approach for ten drugs extensively metabolized by CYP1A2 (theophylline), CYP2C8 (desloratidine, montelukast), CYP2C9 (diclofenac), CYP2C19 (esomeprazole, lansoprazole), CYP2D6 (tramadol) and CYP3A4 (itraconazole, ondansetron, sufentanil). Model performance in children was evaluated by comparing simulated plasma concentration-time profiles with observed clinical results for each drug and age group...
October 13, 2017: Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28988197/vonoprazan-prevents-ulcer-recurrence-during-long-term-nsaid-therapy-randomised-lansoprazole-controlled-non-inferiority-and-single-blind-extension-study
#5
Yuji Mizokami, Kazunori Oda, Nobuo Funao, Akira Nishimura, Satoshi Soen, Takashi Kawai, Kiyoshi Ashida, Kentaro Sugano
OBJECTIVE: To assess the non-inferiority of vonoprazan to lansoprazole for secondary prevention of non-steroidal anti-inflammatory drug (NSAID)-induced peptic ulcer (PU) and the safety of vonoprazan during extended use. DESIGN: A phase 3, 24-week, multicenter, randomised, double-blind (DB), active-controlled study, followed by a phase 3, ≥28 week, multicenter, single-blind, parallel-group extension study (EXT) in outpatients (n=642) receiving long-term NSAID therapy who are at risk of PU recurrence...
October 7, 2017: Gut
https://www.readbyqxmd.com/read/28964908/interchageable-use-of-proton-pump-inhibitors-based-on-relative-potency
#6
David Y Graham, Aylin Tansel
Although proton pump inhibitors (PPIs) are widely used, their relative potency and ideal dosing regimens remain unclear. We analyzed data from randomized clinical trials that performed pH testing in patients receiving solid-dose PPI formulations (omeprazole, esomeprazole, lansoprazole, pantoprazole, rabeprazole) for a minimum of 5 days. We used omeprazole equivalency and the surrogate biomarker, pH4time (percentage time pH>4 over 24-hour period), to compare PPI effectiveness for different PPIs given once, twice or three times daily...
September 28, 2017: Clinical Gastroenterology and Hepatology
https://www.readbyqxmd.com/read/28953640/comparative-effectiveness-and-acceptability-of-the-fda-licensed-proton-pump-inhibitors-for-erosive-esophagitis-a-prisma-compliant-network-meta-analysis
#7
Mei-Juan Li, Qing Li, Min Sun, Li-Qin Liu
BACKGROUND: This study compared the effectiveness and acceptability of all Food and Drug Administration (FDA)-recommended dose proton pump inhibitors (PPIs) in erosive esophagitis (EE): Dexlansoprazole 60 mg, Esomeprazole 40 mg, Esomeprazole 20 mg, Pantoprazole 40 mg, Lansoprazole 30 mg, Rabeprazole 20 mg, Omeprazole 20 mg. METHODS: A systematic literature search was performed using PubMed, Embase, and Cochrane Library. Totally, 25 randomized controlled trials (RCTs) met study selection criteria and were incorporated in this network meta-analysis (NMA) study...
September 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/28889052/a-rapid-fourier-transform-infrared-spectroscopic-method-for-analysis-of-certain-proton-pump-inhibitors-in-binary-and-ternary-mixtures
#8
Pakinaz Y Khashaba, Hassan Refat H Ali, Mohamed M El-Wekil
A simple and non-destructive FTIR method was used to determine certain proton pump inhibitors (PPIs) in binary and ternary mixtures. Proton pump inhibitors (PPIs); omeprazole (OMZ), esomeprazole (EZM), lansoprazole (LAN), pantoprazole sodium (PAN sodium) and rabeprazole sodium (RAB sodium) in binary mixture with domperidone (DOM) and ternary mixture of OMZ, clarithromycin (CLM) and tinidazole (TNZ) were determined in the solid-state by FTIR spectroscopy for the first time. The method was validated according to ICH-guidelines where linearity was ranged from 20 to 850μg/g and 20-360μg/g for PPIs and DOM, respectively in binary mixtures and 10-400, 100-8000 and 150-14,000μg/g for OMZ, CLM and TNZ, respectively...
September 5, 2017: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
https://www.readbyqxmd.com/read/28872126/application-and-methodology-of-the-non-destructive-19f-time-domain-nmr-technique-to-measure-the-content-in-fluorine-containing-drug-products
#9
Maria Victoria Silva Elipe, Lan Li, Karthik Nagapudi, Alan M Kook, Carlos Cobas, Isaac Iglesias, Chen Peng
Here, we describe a protocol developed by our group that uses low-field fluorine-19 ((19)F) time-domain (TD) nuclear magnetic resonance (NMR) to measure the average content of fluorinated drugs in their formulated drug product forms: tablets or capsules. This method is specific to fluorinated drugs because it detects only the content of fluorine, avoiding interference from the excipients that lack fluorine. The advantages of measuring the active content of fluorinated drugs using low-field (19)F TD-NMR versus high-field (19)F solid-state (SS) NMR are the simplicity of the method; the low cost; and the non-destructive nature of the technique, with all samples recoverable in intact forms (e...
August 22, 2017: Journal of Visualized Experiments: JoVE
https://www.readbyqxmd.com/read/28822783/the-expression-induction-and-pharmacological-activity-of-cyp1a2-are-post-transcriptionally-regulated-by-microrna-hsa-mir-132-5p
#10
Yinting Chen, Linjuan Zeng, Yong Wang, William H Tolleson, Bridgett Knox, Si Chen, Zhen Ren, Lei Guo, Nan Mei, Feng Qian, Kaihong Huang, David Liu, Weida Tong, Dianke Yu, Baitang Ning
Cytochrome P450 1A2 (CYP1A2) is one of the most abundant and important drug metabolizing enzymes in human liver. However, little is known about the post-transcriptional regulation of CYP1A2, especially the mechanisms involving microRNAs (miRNAs). This study applied a systematic approach to investigate the post-transcriptional regulation of CYP1A2 by miRNAs. Candidate miRNAs targeting the 3'-untranslated region (3'-UTR) of CYP1A2 were screened in silico, resulting in the selection of sixty-two potential miRNAs for further analysis...
August 16, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28801980/effects-of-proton-pump-inhibitors-and-famotidine-on-elimination-of-plasma-methotrexate-evaluation-of-drug-drug-interactions-mediated-by-organic-anion-transporter-3
#11
Katsuya Narumi, Yu Sato, Masaki Kobayashi, Ayako Furugen, Kumiko Kasashi, Takehiro Yamada, Takanori Teshima, Ken Iseki
Methotrexate (MTX) is an antifolate agent used in the treatment of numerous types of cancer, and eliminated by active tubular secretion via organic anion transporter 3 (OAT3). Gastric antisecretory drugs, such as proton pump inhibitors (PPIs) and histamine H2 receptor antagonists, are widely used among patients with cancer in clinical practice. The aim of the present study was to analyze the potential drug-drug interactions between MTX and gastric antisecretory drugs in high-dose MTX (HD-MTX) therapy. We retrospectively analyzed the impact of PPIs on the plasma MTX concentration on 73 cycles of HD-MTX therapy performed in 43 patients...
August 12, 2017: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/28797990/marked-improvement-in-gastric-involvement-in-beh%C3%A3-et-s-disease-with-adalimumab-treatment
#12
Akira Sonoda, Ryo Ogawa, Kazuhiro Mizukami, Kensuke Fukuda, Mitsutaka Shuto, Kazuhisa Okamoto, Osamu Matsunari, Tadayoshi Okimoto, Kazunari Murakami
Gastric involvement is the least frequent manifestation of Behçet's disease, and effective treatment for it unknown. Here the case of a patient with gastric involvement in Behçet's disease that was markedly improved with adalimumab therapy is presented. A 68-year-old man developed an oral ulcer, erythema, folliculitis, and arthralgia. Behçet's disease was suspected; then, prednisolone and colchicine were administered. Esophagogastroduodenoscopy showed a punched-out ulcer in the posterior wall of the gastric antrum...
August 9, 2017: Turkish Journal of Gastroenterology: the Official Journal of Turkish Society of Gastroenterology
https://www.readbyqxmd.com/read/28766240/determination-of-s-lansoprazole-in-dexlansoprazole-preparation-by-capillary-zone-electrophoresis
#13
Hyun Kyu Chung, Quoc-Ky Truong, Xuan-Lan Mai, Yusung Choi, Jong-Seong Kang, Woongchon Mar, Kyeong Ho Kim
Capillary zone electrophoresis was successfully applied to the enantiomeric purity determination of dexlansoprazole using sulfobutyl ether-β-cyclodextrin and methyl-β-cyclodextrin as chiral selectors. Separations were carried out in a 50 μm, 64/56 cm fused-silica capillary. The optimized conditions included 90 mM phosphate buffer, pH 6.0, containing 30 mM sulfobutyl ether-β-cyclodextrin, 20 mM methyl-β-cyclodextrin as background electrolyte, an applied voltage of 25 kV and a temperature of 16 °C, detection was at 280 nm...
August 1, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28713440/investigating-the-physical-stability-of-repackaged-medicines-stored-into-commercially-available-multicompartment-compliance-aids-mcas
#14
Bahijja Tolulope Raimi-Abraham, Alba Garcia Del Valle, Carlota Varon Galcera, Susan Anne Barker, Mine Orlu
BACKGROUND: Compliance aids are devices which have been developed and are currently used to assist individuals in their medicines management. The use of compliance aids involves the transfer of medicines from the manufacturers' original packaging and repackaged into an multicompartment compliance aid (MCA). MCAs do not guarantee the same level of protection compared to manufacturer's original packaging. OBJECTIVE: The aim of this study was to investigate the stability profile of atenolol, aspirin and lansoprazole dosage forms repackaged together in two different commercially available MCAs...
June 2017: Journal of Pharmaceutical Health Services Research
https://www.readbyqxmd.com/read/28699491/a-case-of-pantoprazole-anaphylaxis-with-cross-reactivity-to-all-proton-pump-inhibitors-finding-a-safe-alternative
#15
Özlem Türedi, Zeynep Çelebi Sözener, Reşat Kendirlinan, Sevim Bavbek
BACKGROUND: Hypersensitivity reactions due to Proton pump inhibitors (PPIs ) are rare, and further anaphylaxis to a PPI with cross-reactivity to all commercially available PPIs is very rare Objective: To present a case of anaphylaxis to pantoprazole with cross-reactivity to all commercially available PPIs Method: Skin prick tests (SPTs), intradermal tests (IDTs) and oral provocation tests (OPTs) were performed with available PPIs according to the method described in previous studies. RESULTS: All tested PPIs except lansoprazole were positive on skin tests either SPT or IDT...
July 11, 2017: Current Drug Safety
https://www.readbyqxmd.com/read/28680717/effect-of-a-proton-pump-inhibitor-on-tumor-bleeding-prevention-in-unresectable-gastric-cancer-patients-a-double-blind-randomized-placebo-controlled-trial
#16
Young-Il Kim, Mi-Jung Kim, Sook Ryun Park, Hark Kyun Kim, Soo-Jeong Cho, Jong Yeul Lee, Chan Gyoo Kim, Gwang Ha Kim, Moo In Park, Byung-Ho Nam, Young Iee Park, Il Ju Choi
PURPOSE: Tumor bleeding is a major complication in inoperable gastric cancer. The study aim was to investigate the effects of proton pump inhibitor (PPI) treatment for the prevention of gastric tumor bleeding. MATERIALS AND METHODS: This study was a prospective double-blind, randomized, placebo-controlled trial. Patients with inoperable gastric cancer were randomly assigned to receive oral lansoprazole (30 mg) or placebo daily. The primary endpoint was the occurrence of tumor bleeding, and the secondary endpoints were transfusion requirement and overall survival (OS)...
June 2017: Journal of Gastric Cancer
https://www.readbyqxmd.com/read/28659302/higher-dietary-cholesterol-and-%C3%AF-3-fatty-acid-intakes-are-associated-with-a-lower-success-rate-of-helicobacter-pylori-eradication-therapy-in-japan
#17
Hiroaki Ikezaki, Norihiro Furusyo, Paul F Jacques, Motohiro Shimizu, Masayuki Murata, Ernst J Schaefer, Yoshihisa Urita, Jun Hayashi
Background:Helicobacter pylori infection is a known risk factor for duodenal ulcers, gastritis, and gastric cancer. The eradication of H. pylori is successful in treating these disorders; however, the success rate of eradication therapy is declining. There may be an interaction with nutrient intake to account for this decline.Objective: We investigated the influence of food and nutrient intake on H. pylori eradication therapy.Design: In this study, 4014 subjects underwent endoscopy, were tested for serum antibodies to H...
August 2017: American Journal of Clinical Nutrition
https://www.readbyqxmd.com/read/28629736/kfp-h008-blocks-gastric-acid-secretion-through-inhibiting-h-k-atpase
#18
Cheng-Yuan Li, Mei Su, Yun-Yi Yan, Lin Zhou, Lu-Yao Ao, Wei-Rong Fang, Yun-Man Li
1-(5-(1H-indol-5-yl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl)-N-methylmethanamine (KFP-H008),a novel and potent potassium-competitive acid blocker for the treatment of acid secretion related diseases, has not been reported previously. In this study, we demonstrated that KFP-H008 inhibits basal acid secretion, 2-deoxy-D-glucose- (2DG-) stimulated gastric acid secretion in rats. KFP-H008 blocked histamine-stimulated acid secretion in rats and heidenhain pouch dogs and reversed acid output in isolated gastric perfusion under histamine stimulation...
September 5, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28623874/lansoprazole-sulfide-pharmacokinetics-of-this-promising-anti-tuberculous-agent
#19
Sipho Mdanda, Sooraj Baijnath, Adeola Shobo, Sanil D Singh, Glenn E M Maguire, Hendrik G Kruger, Per I Arvidsson, Tricia Naicker, Thavendran Govender
Lansoprazole (LPZ) is a commercially available proton-pump inhibitor whose primary metabolite, lansoprazole sulfide (LPZS) was recently reported to have in vitro and in vivo activity against Mycobacterium tuberculosis. It was also reported that a 300 mg kg(-1) oral administration of LPZS was necessary to reach therapeutic levels in the lung, with the equivalent human dose being unrealistic. A validated liquid chromatography-tandem mass spectrometric method (LC-MS/MS) for the simultaneous quantification LPZ and LPZS in rat plasma and lung homogenates was developed...
June 17, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/28599440/identification-of-candidate-drugs-for-the-treatment-of-metastatic-osteosarcoma-through-a-subpathway-analysis-method
#20
Xin Li, Ming-Lan Yan, Qian Yu
Osteosarcoma (OS) is the third most frequent type of cancer in adolescents and represents >56% of all bone tumors. In addition, metastatic OS frequently demonstrates resistance to conventional chemotherapy; thus, the development of novel therapeutic agents for the treatment of patients with metastatic OS is warranted. In the present study, the metabolic mechanisms underlying OS metastasis were investigated using a subpathway analysis method and lead to the identification of candidate drugs for the treatment of metastatic OS...
June 2017: Oncology Letters
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