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https://www.readbyqxmd.com/read/27922185/relaxin-family-peptides-structure-activity-relationship-studies
#1
REVIEW
Nitin A Patil, K Johan Rosengren, Frances Separovic, John D Wade, Ross A D Bathgate, Mohammed Akhter Hossain
The human relaxin peptide family consists of seven cystine-rich peptides, four of which are known to signal through relaxin family peptide receptors, RXFP1-4. Considering the vital roles these peptides play in physiology and various diseases, they are of considerable importance for drug discovery and development. Detailed structure-activity relationship (SAR) studies towards understanding the role of important residues in each of these peptides have been reported over the years and utilised for design of antagonists and minimised agonist variants...
December 6, 2016: British Journal of Pharmacology
https://www.readbyqxmd.com/read/27913306/effect-of-bradykinin-receptor-antagonism-on-ace-inhibitor-associated-angioedema
#2
Brittany T Straka, Claudia E Ramirez, James B Byrd, Elizabeth Stone, Alencia Woodard-Grice, Hui Nian, Chang Yu, Aleena Banerji, Nancy J Brown
BACKGROUND: The B2 receptor antagonist icatibant is approved for treatment of attacks of hereditary angioedema. Icatibant has been reported to decrease time-to-resolution of angiotensin-converting enzyme (ACE) inhibitor-associated angioedema in one study of European patients. METHODS: Patients with ACE inhibitor-associated angioedema (defined as swelling of lips, tongue, pharynx or face during ACE inhibitor use and no swelling in the absence of ACE inhibitor use) were enrolled at Vanderbilt University Medical Center from October 2007 through September 2015 and at Massachusetts General Hospital in 2012...
November 29, 2016: Journal of Allergy and Clinical Immunology
https://www.readbyqxmd.com/read/27895933/influence-of-proton-pump-inhibitors-and-histamine-h2-receptor-antagonists-on-serum-phosphorus-level-control-by-calcium-carbonate-in-patients-undergoing-hemodialysis-a-retrospective-medical-chart-review
#3
Masaomi Tatsuzawa, Ryuichi Ogawa, Atsushi Ohkubo, Kazuyo Shimojima, Kunimi Maeda, Hirotoshi Echizen, Akihisa Miyazaki
BACKGROUND: Hyperphosphatemia is one of the common complications in patients undergoing hemodialysis. Although calcium carbonate (CaC) is often used to control serum inorganic phosphorus level in dialysis patients, co-administration of gastric acid reducers (ARs) may interfere with the phosphate binding effect of CaC. We performed a retrospective medical chart review to study whether ARs attenuate the hypophosphatemic effect of CaC in patients undergoing hemodialysis. METHODS: One hundred and eight chronic hemodialysis patients receiving either CaC alone or CaC concomitant with one of the ARs (proton pump inhibitors and histamine H2-receptor antagonists) were retrieved from the medical charts in Juntendo University Nerima Hospital...
2016: Journal of Pharmaceutical Health Care and Sciences
https://www.readbyqxmd.com/read/27884335/pneumonia-prevention-in-intubated-patients-given-sucralfate-versus-proton-pump-inhibitors-and-or-histamine-ii-receptor-blockers
#4
Gene A Grindlinger, Sarah B Cairo, Carole B Duperre
BACKGROUND: Ventilator-associated pneumonia (VAP) is a common cause of infectious morbidity and mortality in the intensive care unit (ICU). The type of stress-ulcer prophylaxis (SUP) given to ventilated patients may, in part, be responsible. We observed an increase in VAP as ventilator bundle compliance increased and a decrease in VAP when bundle compliance decreased. We reasoned that SUP which raises gastric pH such as proton-pump inhibitors (PPIs) and histamine II (H2) receptor antagonists as opposed to SUP which does not raise pH such as sucralfate (S) may be responsible and also may alter the causative bacteria...
December 2016: Journal of Surgical Research
https://www.readbyqxmd.com/read/27871467/the-effect-of-diabetes-and-hypertension-on-the-placental-permeation-of-the-hydrophilic-drug-ranitidine
#5
Mladena Lalic-Popovic, Jovana Paunkovic, Zorica Grujic, Svetlana Golocorbin-Kon, Velibor Vasovic, Hani Al-Salami, Momir Mikov
INTRODUCTION: Ranitidine is a hydrophilic weak base and an H2-receptor antagonist which is commonly used for gastroesophageal reflux, including during pregnancy. It has limited placental permeation and can be used as a pre-anesthetic antacid to prevent aspiration of acidic stomach contents. Recent studies suggest that diabetes and hypertension may influence placental permeation of hydrophilic drugs. Thus, this study aimed to investigate the influence of diabetes and hypertension on ranitidine's placental permeation in pregnant women...
December 2016: Placenta
https://www.readbyqxmd.com/read/27855401/systematic-review-and-net-work-meta-analysis-of-upper-gastrointestinal-hemorrhage-interventions
#6
Mengyuan Jiang, Pan Chen, Qiang Gao
BACKGROUND/AIMS: Upper gastrointestinal hemorrhage (UGH) is a serious medical condition which affects a large number of individuals. Endoscopic therapy accompanied by medication is a standard approach that is used to improve the prognosis of UGH patients and a few medications have been developed including proton pump inhibitors (PPIs), histamine H2 receptor antagonist (H2RA), somatostatin analogues and tranexamic acid. This study is set to compare the efficacy and safety of various medical interventions that are used to manage upper gastrointestinal bleeding...
2016: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/27822777/critical-role-of-endogenous-histamine-in-promoting-end-organ-tissue-injury-in-sepsis
#7
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/27787718/histamine-and-histamine-receptors-in-allergic-dermatitis
#8
Hiroshi Ohtsu, Masahiro Seike
In this chapter we will first introduce the pathophysiological process of several skin diseases including allergic dermatitis, a common skin disease, including chronic allergic contact dermatitis (CACD), and atopic dermatitis (AD). In CACD and AD patients, repeated skin exposure to antigens contributes to the development of chronic eczematous lesions. Repeated application of haptens on mice allows emulation of the development of CACD in humans. Further, we will focus on H1, H2, and H4 histamine receptors and their effects on CACD and AD...
October 28, 2016: Handbook of Experimental Pharmacology
https://www.readbyqxmd.com/read/27787717/role-of-the-histamine-h3-receptor-in-the-central-nervous-system
#9
Eberhard Schlicker, Markus Kathmann
The Gi/o protein-coupled histamine H3 receptor is distributed throughout the central nervous system including areas like cerebral cortex, hippocampus and striatum with the density being highest in the posterior hypothalamus, i.e. the area in which the histaminergic cell bodies are located. In contrast to the other histamine receptor subtypes (H1, H2 and H4), the H3 receptor is located presynaptically and shows a constitutive activity. In detail, H3 receptors are involved in the inhibition of histamine release (presynaptic autoreceptor), impulse flow along the histaminergic neurones (somadendritic autoreceptor) and histamine synthesis...
October 28, 2016: Handbook of Experimental Pharmacology
https://www.readbyqxmd.com/read/27784575/the-appropriate-use-of-proton-pump-inhibitors-ppis-need-for-a-reappraisal
#10
REVIEW
Vincenzo Savarino, Pietro Dulbecco, Nicola de Bortoli, Andrea Ottonello, Edoardo Savarino
The advent of powerful acid-suppressive drugs, such as proton pump inhibitors (PPIs), has revolutionized the management of acid-related diseases and has minimized the role of surgery. The major and universally recognized indications for their use are represented by treatment of gastro-esophageal reflux disease, eradication of Helicobacter pylori infection in combination with antibiotics, therapy of H. pylori-negative peptic ulcers, healing and prophylaxis of non-steroidal anti-inflammatory drug-associated gastric ulcers and control of several acid hypersecretory conditions...
October 23, 2016: European Journal of Internal Medicine
https://www.readbyqxmd.com/read/27742625/state-of-the-art-of-chronic-spontaneous-urticaria-in-italy-a-multicentre-survey-to-evaluate-physicians-and-patients-perspectives
#11
Marco Rimoldi, Oliviero Rossi, Nadia Rota
OBJECTIVE: To assess the clinical status of chronic spontaneous urticaria (CSU) and understand treatment approaches in Italy through specialists who treat CSU (dermatologists and allergy specialists) and CSU patients' experience. DESIGN: Multicentre survey. SETTING: Online structured questionnaires (one for physicians and one for patients). PARTICIPANTS: Physicians and patients with CSU in Italy. INTERVENTIONS: None...
October 14, 2016: BMJ Open
https://www.readbyqxmd.com/read/27723909/-stress-ulcer-prophylaxis-are-ppis-truly-superior-compared-to-h2-receptor-antagonists
#12
H M Steffen
The S2k-Guideline "Helicobacter pylori and gastroduodenal ulcer disease" offers a statement and comment on the subject of stress ulcer prophylaxis that need a critical response.
October 2016: Zeitschrift Für Gastroenterologie
https://www.readbyqxmd.com/read/27693797/the-role-of-histamine-h1-h2-and-h3-receptors-of-ventral-posteromedial-nucleus-of-thalamus-in-modulation-of-trigeminal-pain
#13
Esmaeal Tamaddonfard, Amir Erfanparast, Hamid Ghasemi, Farzin Henareh-Chareh, Mansoor Hadidi, Navideh Mirzakhani, Sahar Seyedin, Mina Taati, Reza Salighedar, Sara Salimi, Farshad Safaei
Histamine receptors are involved in supraspinal modulation of pain. In the present study, we investigated the effects of microinjection of histamine H1, H2 and H3 receptor antagonists and agonists into the ventral posteromedial (VPM) nucleus of the thalamus on two models of trigeminal pain. Right and left sides of VPM were implanted with two guide cannulas. Corneal pain was induced by local corneal surface application of hypertonic saline and the number of eye wipes was recorded. The duration of face rubbing, as an orofacial pain measure, was recorded after subcutaneous (s...
September 29, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27693316/selective-scavenging-of-intra-mitochondrial-superoxide-corrects-diclofenac-induced-mitochondrial-dysfunction-and-gastric-injury-a-novel-gastroprotective-mechanism-independent-of-gastric-acid-suppression
#14
Somnath Mazumder, Rudranil De, Souvik Sarkar, Asim Azhar Siddiqui, Shubhra Jyoti Saha, Chinmoy Banerjee, Mohd Shameel Iqbal, Shiladitya Nag, Subhashis Debsharma, Uday Bandyopadhyay
Non-steroidal anti-inflammatory drugs (NSAIDs) are widely used to treat multiple inflammatory diseases and pain but severe gastric mucosal damage is the worst outcome of NSAID-therapy. Here we report that mitoTEMPO, a mitochondrially targeted superoxide (O2(-)) scavenger protected as well as healed gastric injury induced by diclofenac (DCF), the most commonly used NSAID. Common existing therapy against gastric injury involves suppression of gastric acid secretion by proton pump inhibitors and histamine H2 receptor antagonists; however, dyspepsia, vitamin B12 deficiency and gastric microfloral dysbalance are the major drawbacks of acid suppression...
September 28, 2016: Biochemical Pharmacology
https://www.readbyqxmd.com/read/27659672/age-and-prevalence-of-esophageal-reflux-disease-in-japanese-patients-with-type-2-diabetes-mellitus-the-dogo-study
#15
Yoshio Ikeda, Shinya Furukawa, Takenori Sakai, Tetsuji Niiya, Hiroaki Miyaoka, Teruki Miyake, Shin Yamamoto, Hidenori Senba, Yasunori Yamamoto, Eiji Arimitsu, Sen Yagi, Hiroki Utsunomiya, Keiko Tanaka, Eiji Takeshita, Bunzo Matsuura, Yoshihiro Miyake, Yoichi Hiasa
BACKGROUND: Only limited epidemiological evidence exists regarding the relationship between age and gastroesophageal reflux disease (GERD) among Japanese patients with type 2 diabetes mellitus. AIM: The purpose of the present study is to investigate this issue among Japanese patients with type 2 diabetes mellitus. METHODS: A multicenter cross-sectional study was conducted in 847 Japanese patients with type 2 diabetes mellitus. Subjects were divided into quartiles according to age: (1) 19 ≤ age < 56, (2) 56 ≤ age < 64, (3) 64 ≤ age < 71, and (4) 71 ≤ age < 89...
September 22, 2016: Digestive Diseases and Sciences
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
#16
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...
September 15, 2016: Gastroenterology
https://www.readbyqxmd.com/read/27625037/current-knowledge-and-perspectives-on-histamine-h1-and-h2-receptor-pharmacology-functional-selectivity-receptor-crosstalk-and-repositioning-of-classic-histaminergic-ligands
#17
Federico Monczor, Natalia Fernandez
H1 and H2 histamine receptor antagonists, although developed many decades ago, are still effective for the treatment of allergic and gastric acid-related conditions. This article focuses on novel aspects of the pharmacology and molecular mechanisms of histamine receptors that should be contemplated for optimizing current therapies, repositioning histaminergic ligands for new therapeutic uses, or even including agonists of the histaminergic system in the treatment of different pathologies such as leukemia or neurodegenerative disorders...
November 2016: Molecular Pharmacology
https://www.readbyqxmd.com/read/27622015/ranitidine-modifies-myeloid-cell-populations-and-inhibits-breast-tumor-development-and-spread-in-mice
#18
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
#19
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
https://www.readbyqxmd.com/read/27603551/effects-of-commonly-used-chronic-medications-on-the-outcomes-of-ipilimumab-therapy-in-patients-with-metastatic-melanoma
#20
Jarrett J Failing, Heidi D Finnes, Lisa A Kottschade, Jacob B Allred, Svetomir N Markovic
Ipilimumab can induce long-term survival in 20% of patients with metastatic melanoma. Concurrent chronic medications may impact the patient's immune system, possess antimelanoma properties, and potentially affect clinical outcomes. This retrospective study sought to describe the efficacy and toxicity effects of 12 classes of chronic medications in metastatic melanoma patients treated with ipilimumab. A total of 159 adults who received ipilimumab for metastatic melanoma at Mayo Clinic (Rochester, Minnesota, USA) from 1 March 2011 through 31 December 2014 were included...
September 3, 2016: Melanoma Research
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