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https://www.readbyqxmd.com/read/28213943/a-phase-2-safety-study-of-accelerated-elotuzumab-infusion-over-less-than-1-hour-in-combination-with-lenalidomide-and-dexamethasone-in-patients-with-multiple-myeloma
#1
James Berenson, Robert Manges, Suprith Badarinath, Alan Cartmell, Kristi McIntyre, Roger Lyons, Wael Harb, Hesham Mohamed, Ali Nourbakhsh, Robert Rifkin
Elotuzumab, an immunostimulatory SLAMF7-targeting monoclonal antibody, induces myeloma cell death with minimal effects on normal tissue. In a previous phase 3 study in patients with relapsed/refractory multiple myeloma (RRMM), elotuzumab (10 mg/kg, ∼3-hour infusion), combined with lenalidomide and dexamethasone, demonstrated durable efficacy and acceptable safety; 10% (33/321) of patients had infusion reactions (IRs; Grade 1/2: 29; Grade 3: 4). This phase 2 study (NCT02159365) investigated an accelerated infusion schedule in 70 patients with newly diagnosed multiple myeloma or RRMM...
February 18, 2017: American Journal of Hematology
https://www.readbyqxmd.com/read/28185047/histaminergic-h1-and-h2-receptors-mediate-the-effects-of-propofol-on-the-noradrenalin-inhibited-neurons-in-rat-ventrolateral-preoptic-nucleus
#2
Yang Liu, Yu Zhang, Kun Qian, Lin Zhang, Tian Yu
The ventrolateral preoptic nucleus is a sleep-promoting nucleus located in the basal forebrain. A commonly used intravenous anesthetic, propofol, had been reported to induce sleep spindles and augment the firing rate of neurons in ventrolateral preoptic nucleus, but the underlining mechanism is yet to be known. By using patch clamp recording on neuron in acute brain slice, present study tested if histaminergic H1 and H2 receptors play a role in the effect of propofol on the noradrenalin-inhibited neurons in ventrolateral preoptic nucleus...
February 9, 2017: Neurochemical Research
https://www.readbyqxmd.com/read/28178593/the-role-of-histamine-in-the-regulation-of-the-viability-proliferation-and-transforming-growth-factor-%C3%AE-1-secretion-of-rat-wound-fibroblasts
#3
Monika Wolak, Ewa Bojanowska, Teresa Staszewska, Joanna Ciosek, Marlena Juszczak, Jacek Drobnik
BACKGROUND: Inflammation mediators play a regulatory role in repair processes. The study will examine the influence of histamine on wound fibroblast metabolic activity, viability, proliferation, and TGFβ1 secretion. The study also will identify the histamine receptor involved in regulation of the tested repair processes. METHODS: Fibroblasts were obtained from the granulation tissue of wounds or intact dermis of rats. The MTT and BrdU assays were used to examine the effect of histamine (10(-8)M-10(-4)M) on the viability and metabolic activity of fibroblasts, and on their proliferative capacity...
November 15, 2016: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28177773/gastroprotective-and-antielastase-effect-of-protein-inhibitors-from-erythrina-velutina-seeds-in-an-experimental-ulcer-model
#4
Vanessa Cristina Oliveira de Lima, Richele Janaína de Araújo Machado, Norberto Monteiro, Christina da Silva Camillo, Alexandre Coelho Serquiz, Adeliana Silva de Oliveira, Fabiola Rufino, Bruna Leal Lima Maciel, Adriana Ferreira Uchôa, Elizeu Antunes Santos, Ana Heloneida de Araújo Morais
Trypsin and chymotrypsin inhibitors from Erythrina velutina seeds have been previously isolated by our group. In previous studies using a sepsis model, we demonstrated the anti-tumor and anti-inflammatory action of these compounds. This study aimed to evaluate the gastroprotective and antielastase effect of protein inhibitors from Erythrina velutina seeds in an experimental stress induced ulcer model. Two protein isolates from E. velutina seeds, with antitrypsin (PIAT) and anti-chymotrypsin (PIAQ) activities were tested...
September 12, 2016: Biochemistry and Cell Biology, Biochimie et Biologie Cellulaire
https://www.readbyqxmd.com/read/28176470/effect-of-sustained-elevated-gastric-ph-levels-on-gefitinib-exposure
#5
Weifeng Tang, Helen Tomkinson, Eric Masson
This open-label, randomized, phase 1 crossover study investigated the effect of elevated gastric pH level (>5) on the relative bioavailability and pharmacokinetic profile of the epidermal growth factor receptor tyrosine kinase inhibitor gefitinib. Healthy male volunteers (n = 26) were randomized to gefitinib 250 mg (fasted), either alone on day 1 (unmodified gastric pH) or 1 hour following the second of 2 oral doses of the H2 -receptor antagonist ranitidine 450 mg (elevated gastric pH). After a 3-week washout period, volunteers crossed to the other treatment...
February 8, 2017: Clinical Pharmacology in Drug Development
https://www.readbyqxmd.com/read/28166080/stress-induced-gastric-ulcers-presenting-as-massive-rectal-bleeding-in-a-newborn
#6
A Joshi, P S Shrestha, S Dangol, N C Shrestha, P Poudyal, A Shrestha A
Severe gastrointestinal bleeding in newborn period is a serious but uncommon phenomenon that has a broad differential diagnosis. Primary duodenal ulcers are rare in children but stress induced ulceration in stomach occurs more often in neonatal period due to birth asphyxia, prolonged labour, cesarean deliveries, instrumentations, respiratory distress syndrome and sepsis. These present as acute onset of gastrointestinal bleeding commonly as altered gastric aspirate, hematemesis or malena. We report a case of a neonate with stress induced gastric bleeding following birth asphyxia who presented with massive gastrointestinal bleed manifesting as hematemesis and massive rectal bleeding...
April 2016: Kathmandu University Medical Journal (KUMJ)
https://www.readbyqxmd.com/read/28159802/ranitidine-forgotten-drug-of-delayed-gastric-emptying
#7
Abbie E Veevers, Stephen G Oxberry
Delayed gastric emptying in the presence or absence of mechanical bowel obstruction can cause distressing symptoms in palliative care patients. We present two patients, both with vomiting due to delayed gastric emptying and gastric outlet obstruction secondary to pancreatic cancer, treated with subcutaneous ranitidine resulting in a symptomatic response. We hypothesise that ranitidine is a useful adjunct to standard treatment with prokinetic agents or octreotide in such patients and potentially those with proximal mechanical bowel obstruction from other malignancies with associated delayed gastric emptying...
February 3, 2017: BMJ Supportive & Palliative Care
https://www.readbyqxmd.com/read/28144167/evaluation-of-anti-ulcer-activity-of-the-leaf-extract-of-osyris-quadripartita-decne-santalaceae-in-rats
#8
Mastewal Abebaw, Bharat Mishra, Dessalegn Asmelashe Gelayee
Osyris quadripartita (OQ) Salzm. ex Decne. has been used to treat peptic ulcer disease in Ethiopian folk medicine, but its efficacy has not been validated. The present study was therefore carried out to evaluate the anti-ulcer activity of 80% methanol leaf extract of OQ in rats. The effect of OQ extract on gastric ulcer in rats in pylorus ligation-induced and ethanol-induced models was studied using single dosing (100, 200, 400 mg/kg) and repeated dosing (200 mg/kg for 10 and 20 days) approaches. Ranitidine (50 mg/kg) and sucralfate (100 mg/kg) were used as the standard drugs...
2017: Journal of Experimental Pharmacology
https://www.readbyqxmd.com/read/28092180/n-acetylcysteine-a-possible-protector-against-indomethacin-induced-peptic-ulcer-crosstalk-between-antioxidant-anti-inflammatory-and-antiapoptotic-mechanisms
#9
Nema Ali Soliman, Doaa Hussein Zineldeen, Mohamed Alaa Katary, Darin Abd Ali
This study investigated the gastroprotective effects of N-acetylcysteine (NAC) against indomethacin-induced gastric ulcer in rats. Ulceration was induced by a single oral administration of indomethacin (30 mg/kg). 50 male albino rats were allocated into 5 equal groups: control group received normal saline orally, indomethacin group rats received normal saline orally for 5 days and indomethacin (50 mg/kg) on the last day, ranitidine group received ranitidine (reference drug) orally for 5 days (50 mg/kg) before receiving indomethacin (50 mg/kg) on the last day, and NAC groups received NAC orally at 300 and 500 mg/kg, respectively, for 5 days before receiving indomethacin (50 mg/kg) on the last day...
November 14, 2016: Canadian Journal of Physiology and Pharmacology
https://www.readbyqxmd.com/read/28042359/non-prescription-proton-pump-inhibitors-for-self-treating-frequent-heartburn-the-role-of-the-canadian-pharmacist
#10
David Armstrong, Nardine Nakhla
Heartburn and acid regurgitation are the cardinal symptoms of gastroesophageal reflux and occur commonly in the Canadian population. Multiple non-prescription treatment options are available for managing these symptoms, including antacids, alginates, histamine-H2 receptor antagonists (H2RAs), and proton-pump inhibitors (PPIs). As a result, pharmacists are ideally positioned to recommend appropriate treatment options based upon an individual's needs and presenting symptoms, prior treatment response, comorbid medical conditions, and other relevant factors...
October 2016: Pharmacy Practice
https://www.readbyqxmd.com/read/28013186/ponciretin-attenuates-ethanol-induced-gastric-damage-in-mice-by-inhibiting-inflammatory-responses
#11
Geum-Dan Kang, Dong-Hyun Kim
BACKGROUND: Poncirin (PO) and isosakuranetin (or ponciretin [PT]) are compounds found in fruits of the genus Citrus. They are frequently used in traditional Chinese medicine for the treatment of inflammation and asthma. Therefore, we examined their anti-gastritis effects in vitro and in vivo. METHODS: The anti-inflammatory effects of PO and PT were examined using ethanol- or LPS-stimulated KATO III cells. Gastritis was induced in ICR mice via intragastric injection of absolute ethanol...
February 2017: International Immunopharmacology
https://www.readbyqxmd.com/read/27990166/morbidity-and-mortality-in-preterm-infants-following-antacid-use-a-retrospective-audit
#12
Natasha Singh, Aparna Dhayade, Abdel-Latif Mohamed, Tejasvi Vasant Chaudhari
Background and Objectives. Antacids are often prescribed to preterm infants due to misdiagnosis of gastro-oesophageal reflux. This suppresses gastric acidity, a major defence mechanism against infection. This study aims to determine if ranitidine and omeprazole use in very low birth weight (VLBW) neonates, <1500 grams, is associated with increased risk of late onset sepsis, necrotising enterocolitis (NEC), and mortality. Methods. Retrospective analysis was conducted on neonates, <1500 grams, born and admitted into the Neonatal Intensive Care Unit at The Canberra Hospital during the period from January 2008 to December 2012...
2016: International Journal of Pediatrics
https://www.readbyqxmd.com/read/27871467/the-effect-of-diabetes-and-hypertension-on-the-placental-permeation-of-the-hydrophilic-drug-ranitidine
#13
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/27858108/effects-of-ranitidine-antacid-food-and-formulation-on-the-pharmacokinetics-of-fostamatinib-results-from-five-phase-i-clinical-studies
#14
Talia Flanagan, Paul Martin, Michael Gillen, David Mathews, Eleanor Lisbon, Martin Kruusmägi
PURPOSE: Fostamatinib is an orally dosed phosphate prodrug that is cleaved by intestinal alkaline phosphatase to the active metabolite R406. Clinical studies were performed to assess the effect of food and ranitidine on exposure, to support in vitro-in vivo relationships (IVIVR) understanding and formulation transitions and to investigate absolute oral bioavailability. METHODS: A series of in vitro dissolution and clinical pharmacokinetic studies were performed to support the design and introduction of a new formulation, understand the impact of changes in in vitro dissolution on in vivo performance for two fostamatinib formulations, to characterize the effects of food and ranitidine on exposure, and determine the absolute oral bioavailability...
November 17, 2016: European Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/27799040/optimal-pre-treatment-for-acute-exposure-to-the-organophosphate-dicrotophos
#15
Dietrich Ernst Lorke, Syed M Nurulain, Mohamed Y Hasan, Kamil Kuča, Georg A Petroianu
BACKGROUND: Reversible cholinesterase inhibitors, when given prophylactically before exposure to organophosphates, are able to decrease organophosphate-induced mortality. However, the efficacy of pyridostigmine, the only pre-treatment substance approved by the US Federal Drug Administration, is unsatisfactory. METHODS: In search of a better prophylactic compound, we determined in vivo the protection conferred by five cholinesterase inhibitors (ranitidine, physostigmine, tacrine, K-27 and pyridostigmine), which were administered in equitoxic dosage (1/4 of LD01) 30 minutes before exposure to the organophosphate dicrotophos...
October 27, 2016: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/27795221/-acute-generalized-exanthematous-pustulosis-induced-by-piroxicam
#16
Ingrid Bissinger, Gustavo Matute-Turizo, María Natalia Mejía-Barreneche
BACKGROUND: Between 62 and 90% of cases of acute generalized exanthematous pustulosis are caused by drugs. Its onset is rapid with generalized pustules, fever, and blood neutrophil count over 7000; pustules resolve spontaneously in less than 15 days. A case associated with piroxicam described. CASE REPORT: A 36-year-old with initial erythema of the thorax and abdomen, accompanied by burning, without fever, which later spread to his forearms, upper arms, and thighs, with face edema...
October 2016: Revista Alergia Mexico: Organo Oficial de la Sociedad Mexicana de Alergia e Inmunología, A.C
https://www.readbyqxmd.com/read/27790462/antiulcer-activity-of-ethanolic-extract-of-salvadora-indica-w-leaves-on-albino-rats
#17
Saroj Kumar Sahoo, Himanshu Bhusan Sahoo, D Priyadarshini, G Soundarya, Ch Kishore Kumar, K Usha Rani
BACKGROUND: Ulcer can be developed inside the inner lining of the stomach (gastric ulcer) or the small intestine (duodenal ulcer). Both the ulcers are also cumulatively referred as peptic ulcers. It affects nearly 10% of world population. AIM: To investigate the antiulcer activity of ethanolic extract of Salvadora indica W. leaves (ESIL) on albino rats. MATERIALS AND METHODS: The present study was carried by pylorus ligation, ethanol and cysteamine induced ulcer models in albino rats...
September 2016: Journal of Clinical and Diagnostic Research: JCDR
https://www.readbyqxmd.com/read/27769620/synthesis-and-biological-evaluation-of-ranitidine-analogs-as-multiple-target-directed-cognitive-enhancers-for-the-treatment-of-alzheimer-s-disease
#18
Jie Gao, Narasimha Midde, Jun Zhu, Alvin V Terry, Campbell McInnes, James M Chapman
Using molecular modeling and rationally designed structural modifications, the multi-target structure-activity relationship for a series of ranitidine analogs has been investigated. Incorporation of a variety of isosteric groups indicated that appropriate aromatic moieties provide optimal interactions with the hydrophobic and π-π interactions with the peripheral anionic site of the AChE active site. The SAR of a series of cyclic imides demonstrated that AChE inhibition is increased by additional aromatic rings, where 1,8-naphthalimide derivatives were the most potent analogs and other key determinants were revealed...
November 15, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27759759/human-immunodeficiency-virus-in-institutionalized-elderly-people
#19
Milton Luiz Gorzoni, Sueli Luciano Pires, Lilian de Fátima Costa Faria, Márcia Regina Valadares Aguado, Miriam Carmen Santana
CONTEXT AND OBJECTIVE: A search in the SciELO and PubMed databases showed few studies on human immunodeficiency virus (HIV) positive individuals in long-term care institutions (LTCIs), thus prompting the present study. The aim of this study was to ascertain whether there were any HIV-positive individuals in LTCIs for the elderly. DESIGN AND SETTING: Cross-sectional study in which the Hospital Infection Control Committee (HICC) of a 405-bed LTCI was consulted. METHODS: The medical records of 405 individuals interned in the LTCI who had been tested for HIV infection were requested for analysis of the following variables: [1] age and gender; [2] length of stay at LTCI (months); [3] causes and diagnoses on admission to LTCI according to International Classification of Diseases, 10th edition; [4] date of HIV diagnosis; [5] seropositivity for syphilis and hepatitis B and C viruses; [6] medications used at last prescription in medical file; and [7] mean CD4 lymphocyte count based on: total lymphocyte count/6 and total lymphocyte count x 0...
October 13, 2016: São Paulo Medical Journal, Revista Paulista de Medicina
https://www.readbyqxmd.com/read/27730681/novel-compounds-with-new-anti-ulcergenic-activity-from-convolvulus-pilosellifolius-using-bio-guided-fractionation
#20
Amani S Awaad, Asmaa Al-Refaie, Reham El-Meligy, Mohamed Zain, Hesham Soliman, Mohamed S Marzoke, Nabil El-Sayed
Oral administration of the total alcohol extract of Convolvulus pilosellifolius Desr. (250 and 500 md/kg) showed potent anti-ulcerogenic activity in absolute ethanol-induced ulcer model in rats; it showed percent protection of control ulcer by 69.2 and 84.6%, respectively, while standard ranitidine (100 mg/kg) exhibited 46.2%. Bio-guided work leads to isolation of two novel compounds (1 and 2), which were identified through (1) H, (13) C NMR, HMPC, HMQC and DEPT as: methyl 2-(hydroxymethyl) octanoate, named as amanitate, and 16-amino-9,13-dimethyl-17-(prop-1-en-2-yl)-hexadecahydro-1H-cyclopenta[a] phenanthren-3-ol, named as asmatol...
December 2016: Phytotherapy Research: PTR
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