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https://www.readbyqxmd.com/read/28430398/impact-of-acid-reducing-agents-on-the-pharmacokinetics-of-palbociclib-a-weak-base-with-ph-dependent-solubility-with-different-food-intake-conditions
#1
Wan Sun, Karen J Klamerus, Lisa M Yuhas, Sylvester Pawlak, Anna Plotka, Melissa O'Gorman, Leonid Kirkovsky, Maha Kosa, Diane Wang
Palbociclib free base capsule is a weak base drug with highly pH-dependent solubility. In vitro and in vivo studies evaluated the impact of acid-reducing agents on exposure of palbociclib and determined whether the impact, if any, can be mitigated by food. A drug-drug interaction study (study 1) was conducted first under fasted conditions and showed that coadministration of multiple doses of the proton-pump inhibitor rabeprazole substantially reduced palbociclib mean area under the concentration-time curve from time 0 to infinity and maximum observed plasma concentration by 62% and 80%, respectively...
April 21, 2017: Clinical Pharmacology in Drug Development
https://www.readbyqxmd.com/read/28423916/pegfilgrastim-induced-bone-pain-a-review-on-incidence-risk-factors-and-evidence-based-management
#2
Donald C Moore, Annie E Pellegrino
OBJECTIVE: To review the incidence, risk factors, and management of pegfilgrastim-induced bone pain (PIBP). DATA SOURCES: PubMed was searched from 1980 to March 31, 2017, using the terms pegfilgrastim and bone pain. STUDY SELECTION AND DATA EXTRACTION: English-language, human studies and reviews assessing the incidence, risk factors, and management of PIBP were incorporated. DATA SYNTHESIS: A total of 3 randomized, prospective studies and 2 retrospective studies evaluated pharmacological management of PIBP...
April 1, 2017: Annals of Pharmacotherapy
https://www.readbyqxmd.com/read/28367296/famotidine-induced-reversal-of-meperidine-related-serotonin-syndrome-a-case-report
#3
Soohyun Joe, Eunju Kim, Junyi Park, Dongwon Lee, Jongchul Son, Hyun Kim
Serotonin syndrome is an unexpected fatal adverse event related to serotonergic medication. This case report is the first report describing the possible treatment effect of famotidine on serotonin syndrome. Furthermore, this is the first case report of serotonin syndrome induced by meperidine alone in a patient with no previous history suggesting a susceptibility to serotonin syndrome. A 70-year-old male with no recent history of serotonergic drug use presented with severe serotonin syndrome following ureteroscopy, possibly due to postoperative meperidine administration...
April 2017: Korean Journal of Anesthesiology
https://www.readbyqxmd.com/read/28199788/development-of-fluorescence-surrogates-to-predict-the-photochemical-transformation-of-pharmaceuticals-in-wastewater-effluents
#4
Shuwen Yan, Bo Yao, Lushi Lian, Xinchen Lu, Shane A Snyder, Rui Li, Weihua Song
The photochemical transformation of pharmaceutical and personal care products (PPCPs) in wastewater effluents is an emerging concern for environmental scientists. In the current study, the photodegradation of 29 PPCPs was examined in effluents under simulated solar irradiation. Direct photodegradation, triplet state effluent organic matter ((3)EfOM*)-mediated and hydroxyl radical (HO(•))-mediated degradation are three major pathways in the removal process. With the photodegradation of trace levels of PPCPs, the excitation-emission matrix (EEM) fluorescence intensities of the effluents were also gradually reduced...
February 24, 2017: Environmental Science & Technology
https://www.readbyqxmd.com/read/28153970/a-rare-case-of-famotidine-induced-delirium-in-a-peritoneal-dialysis-patient
#5
Gary C W Chan, K M Lee, Lorraine P Y Kwan, Maggie M Y Mok, Maggie K M Ma, Desmond Y H Yap, Sydney C W Tang
H2 receptor antagonists are commonly employed to manage gastro-esophageal reflux and peptic ulcer diseases with a very low incidence of side effects. Herein, we report an extremely rare incidence of famotidine-induced acute confusion in a patient with end-stage renal failure. We also discuss the pharmacokinetic properties of famotidine and its interplay with compromised renal function to result in neuropsychiatric manifestations, highlighting the importance of dosage ad ustment in individuals with renal insufficiency...
January 2017: Peritoneal Dialysis International: Journal of the International Society for Peritoneal Dialysis
https://www.readbyqxmd.com/read/28151040/design-of-peg-grafted-pla-nanoparticles-as-oral-permeability-enhancer-for-p-gp-substrate-drug-model-famotidine
#6
Mohamed Mokhtar, Patrick M Gosselin, François Lacasse, Patrice Hildgen
Bioavailability of oral drugs can be limited by an intestinal excretion process mediated by P-glycoprotein (P-gp). Polyethylene glycol (PEG) is a known P-gp inhibitor. Dispersion of Famotidine (a P-gp substrate) within PEGylated nanoparticles (NPs) was used to improve its oral bioavailability. In this work, we evaluated the potential impact of NPs prepared from a grafted copolymer of polylactic acid and PEG on P-gp function by studying in vitro permeability of Famotidine across Caco-2 cells. Copolymers of PEG grafted on polylactic acid a (PLA) backbone (PLA-g-PEG) were synthesized with 1 mol% and 5 mol% PEG vs...
February 2, 2017: Journal of Microencapsulation
https://www.readbyqxmd.com/read/28027824/protective-effect-of-chamomile-matricaria-recutita-l-decoction-extract-against-alcohol-induced-injury-in-rat-gastric-mucosa
#7
Mohamed-Amine Jabri, Nadhem Aissani, Haifa Tounsi, Mohsen Sakly, Lamjed Marzouki, Hichem Sebai
BACKGROUND: Matricaria recutita L. (Asteraceae), German chamomile, has been widely used in the traditional Tunisian medicine because of having the powerful health benefits. the current study was conducted to determine the protective effect of chamomile (Matricaria recutita L.) decoction extract (CDE) in ethanol-induced ulcer and oxidative stress on gastric mucosa in rat. METHODS: Adult male wistar rats were used and divided into seven groups: Control, EtOH, EtOH+various doses of CDE (25, 50 and 100mg/kg, b...
December 21, 2016: Pathophysiology: the Official Journal of the International Society for Pathophysiology
https://www.readbyqxmd.com/read/27975177/involvement-of-histaminergic-and-noradrenergic-receptors-in-the-oxytocin-induced-food-intake-in-neonatal-meat-type-chicks
#8
Seyed Vahid Mirnaghizadeh, Morteza Zendehdel, Vahab Babapour
Oxytocin neurons have a physiological role in food intake and energy balance. Several studies have shown that central histaminergic and adrenergic systems synapse on oxytocin neurons but there is no information for their interaction on food intake regulation in birds. The purpose of this study was to examine the effects of intracerebroventricular (ICV) injection of α-fluoromethylhistidine (α-FMH, histidine decarboxylase inhibitor), chlorpheniramine (histamine H1 receptors antagonist), famotidine (histamine H2 receptors antagonist), thioperamide (histamine H3 receptors antagonist), prazosin (α1 receptor antagonist), yohimbine (α2 receptor antagonist), metoprolol (β1 adrenergic receptor antagonist), ICI 118,551 (β2 adrenergic receptor antagonist) and SR59230R (β3 adrenergic receptor antagonist) on oxytocin-induced hypophagia in 3-h food-deprived (FD3) neonatal broiler chicken...
March 2017: Veterinary Research Communications
https://www.readbyqxmd.com/read/27922030/histamine-2-receptor-antagonist-cannot-prevent-recurrent-peptic-ulcers-in-patients-with-atherosclerotic-diseases-who-receive-platelet-adp-receptor-antagonist-monotherapy-a-randomized-controlled-double-blind-and-double-dummy-trial
#9
Ping-I Hsu, Deng-Chyang Wu, Feng-Woei Tsay, Jin-Shiung Cheng, Chun-Peng Liu, Kwok-Hung Lai, Wen-Chi Chen, Huay-Min Wang, Tzung-Jiun Tsai, Kuo-Wang Tsai, Sung-Shuo Kao
OBJECTIVES: Proton pump inhibitor can effectively prevent recurrent peptic ulcers among atherosclerotic patients receiving clopidogrel monotherapy. However, the interaction between proton pump inhibitors and clopidogrel has raised concerns over the safety of combined use of the two medicines in clinical practice. The aims of this randomized-controlled, double-blind and double-dummy trial were to investigate the efficacy of histamine-2 receptor antagonist (H2RA) in the prevention of recurrent peptic ulcer in patients undergoing thienopyridine monotherapy...
February 2017: American Journal of Gastroenterology
https://www.readbyqxmd.com/read/27906465/repeated-famotidine-administration-results-in-a-diminished-effect-on-intragastric-ph-in-dogs
#10
M K Tolbert, A Graham, A Odunayo, J Price, J M Steiner, K Newkirk, S Hecht
BACKGROUND: Famotidine is an acid suppressant commonly administered to dogs. Prolonged famotidine use in people results in decreased efficacy, but the effect in dogs is unknown. HYPOTHESIS/OBJECTIVES: To compare the effect of repeated oral administration of famotidine or placebo on intragastric pH and serum gastrin in dogs. We hypothesized that famotidine would have a diminished effect on intragastric pH on day 13 compared to day 1. ANIMALS: Six healthy adult colony Beagles...
January 2017: Journal of Veterinary Internal Medicine
https://www.readbyqxmd.com/read/27888865/advances-in-gastrointestinal-bleeding
#11
Ángel Lanas
The main innovations of the latest meeting of the Gastroenterological Association (2016) concerning upper gastrointestinal bleeding from the clinician's perspective can be summarised as follows: a) The Glasgow-Blatchford scale has the best accuracy in predicting the need for surgical intervention and hospital mortality; b) Prognostic scales for non-variceal upper gastrointestinal bleeding are also useful for lower gastrointestinal bleeding; c) Preliminary data suggest that treatment with hemospray does not seem to be superior to current standard treatment in controlling active peptic ulcer bleeding; d) Either famotidine or a proton pump inhibitor may be effective in preventing haemorrhagic recurrence in patients taking aspirin, but this finding needs to be confirmed in further studies; e) There was confirmation of the need to re-introduce antiplatelet therapy as early as possible in patients with antiplatelet-associated gastrointestinal bleeding in order to prevent cardiovascular mortality; f) Routine clinical practice suggests that gastrointestinal or cardiovascular complications with celecoxib or traditional NSAIDs are very low; g) Dabigatran is associated with an increased incidence of gastrointestinal bleeding compared with apixaban or warfarin...
September 2016: Gastroenterología y Hepatología
https://www.readbyqxmd.com/read/27822777/critical-role-of-endogenous-histamine-in-promoting-end-organ-tissue-injury-in-sepsis
#12
Mizuki Hattori, Mitsuaki Yamazaki, Wakana Ohashi, Satoshi Tanaka, Kohshi Hattori, Kenichiro Todoroki, Toshio Fujimori, Hiroshi Ohtsu, Naoyuki Matsuda, Yuichi Hattori
BACKGROUND: Histamine assumes an important role as a major mediator in various pathologic disorders associated with inflammation and immune reactions. However, the involvement of histamine in the pathological conditions and symptoms of sepsis remains entirely unknown. In this study, we establish that histamine is identified as a contributory mediator to promoting the development of organ injury in sepsis. METHODS: Histidine decarboxylase (HDC) gene knockout (HDC(-/-)) mice, histamine H1-/H2-receptor gene-double knockout (H1R(-/-)/H2R(-/-)) mice, and their littermate wild-type (WT) C57BL/6J mice underwent cecal ligation and puncture (CLP) or sham operation...
December 2016: Intensive Care Medicine Experimental
https://www.readbyqxmd.com/read/27817104/prevention-of-granulocyte-colony-stimulating-factor-g-csf-induced-bone-pain-using-double-histamine-blockade
#13
Elizabeth Gavioli, Misty Abrams
PURPOSE: Febrile neutropenia (FN) is an oncological emergency that may reduce patient survival due to chemotherapy dose delays or reductions. It is recommended that patients at risk for FN receive prophylaxis with granulocyte-colony stimulating factor (G-CSF). Bone pain is a common side effect through a mechanism not fully understood. It is thought to be due to histamine release from an inflammatory response. METHODS: This was a retrospective cohort from January to November 2015...
March 2017: Supportive Care in Cancer: Official Journal of the Multinational Association of Supportive Care in Cancer
https://www.readbyqxmd.com/read/27813628/quercetin-attenuates-indomethacin-induced-acute-gastric-ulcer-in-rats
#14
Abdullah Glil Rada Alkushi, Naser Ahmed Mahmoud Elsawy
BACKGROUND: Peptic ulcer diseases are common and are induced by many factors, including stress, smoking, and ingestion of non-steroidal anti-inflammatory drugs. Quercetin is considered to be an anti-oxidant with healing effects on many experimental toxic injuries. MATERIALS AND METHODS: The present study aimed to explore the possible effect of quercetin on acute gastric ulcer induced by indomethacin in rats. Three groups received indomethacin (30mg/kg body weight) orally by orogastric gavage on two consecutive days...
November 4, 2016: Folia Morphologica (Warsz)
https://www.readbyqxmd.com/read/27773524/the-slow-relaxation-dynamics-in-the-amorphous-pharmaceutical-drugs-cimetidine-nizatidine-and-famotidine
#15
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...
December 2016: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27723808/time-to-onset-analysis-of-drug-induced-long-qt-syndrome-based-on-a-spontaneous-reporting-system-for-adverse-drug-events
#16
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
https://www.readbyqxmd.com/read/27645307/inhibiting-renin-angiotensin-system-in-rate-limiting-step-by-aliskiren-as-a-new-approach-for-preventing-indomethacin-induced-gastric-ulcers
#17
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
https://www.readbyqxmd.com/read/27641510/similar-efficacy-of-proton-pump-inhibitors-vs-h2-receptor-antagonists-in-reducing-risk-of-upper-gastrointestinal-bleeding-or-ulcers-in-high-risk-users-of-low-dose-aspirin
#18
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 GI bleeding and ulcers in high-risk aspirin users. METHODS: We studied 270 users of low-dose aspirin (≤325 mg/day) with a history of endoscopically confirmed ulcer bleeding at 8 sites in Hong Kong and Japan...
January 2017: Gastroenterology
https://www.readbyqxmd.com/read/27622015/ranitidine-modifies-myeloid-cell-populations-and-inhibits-breast-tumor-development-and-spread-in-mice
#19
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
https://www.readbyqxmd.com/read/27618417/histamine-induced-dilation-of-isolated-porcine-retinal-arterioles-role-of-endothelium-derived-hyperpolarizing-factor
#20
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
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