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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...
October 6, 2016: Bioorganic & Medicinal Chemistry Letters
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
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...
October 12, 2016: Phytotherapy Research: PTR
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
Keisuke Goda, Tadakazu Takahashi, Akio Kobayashi, Toshiyuki Shoda, Hideyuki Kuno, Shoichiro Sugai
Drug-induced liver injury (DILI) is one of the serious and frequent drug-related adverse events. This adverse event is a main reason for regulatory action pertaining to drugs, including restrictions in clinical indications and withdrawal from clinical trials or the marketplace. Idiosyncratic DILI especially has become a major clinical concern because of its unpredictable nature, frequent hospitalization, need for liver transplantation and high mortality. The estimation of the potential for compounds to induce idiosyncratic DILI is very difficult in non-clinical studies because the precise mechanism of idiosyncratic DILI is still unknown...
2016: Journal of Toxicological Sciences
Arezoo Saberi, Elham Abbasloo, Gholamreza Sepehri, Mahnaz Yazdanpanah, Ehsan Mirkamandari, Vahid Sheibani, Zohreh Safi
BACKGROUND: Melissa officinalis (MO) has potent antioxidant activity. Recent research has demonstrated the anti-ulcer properties of some medicinal plants through their antioxidant properties. OBJECTIVES: The aim of this study was to evaluate the effects of methanolic extracts of MO on experimental gastric ulcers in rats. MATERIALS AND METHODS: Male Wistar rats (200 - 250 g) were starved for 24 hours prior to the induction of gastric ulceration by either indomethacin (48 mg/kg/oral) or water immersion restraint (WIR) stress...
July 2016: Iranian Red Crescent Medical Journal
Ramesh Devkota, G M Khan, Kadir Alam, Amisha Regmi, Binaya Sapkota
BACKGROUND: Drugs used during pregnancy can adversely affect the health and life of the mother and unborn child. However, the fact that drugs are needed to mitigate complications during pregnancy cannot be avoided. The present study was designed to identify the common complications during pregnancy and assess the medications that have been used to mitigate those complications in an attempt to improve drug prescribing during pregnancy. METHODS: A hospital based cross sectional study was conducted at Manipal Teaching Hospital, Nepal in 275 pregnant women presenting with at least one complication and the drugs prescribed for the management of those complications were analyzed...
2016: BMC Pregnancy and Childbirth
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
Justin T Jasper, Oliver S Shafaat, Michael R Hoffmann
Solar-powered electrochemical systems have shown promise for onsite wastewater treatment in regions where basic infrastructure for conventional wastewater treatment is not available. To assess the applicability of these systems for trace organic contaminant treatment, test compound electrolysis rate constants were measured in authentic latrine wastewater using mixed-metal oxide anodes coupled with stainless steel cathodes. Complete removal of ranitidine and cimetidine was achieved within 30 min of electrolysis at an applied potential of 3...
September 20, 2016: Environmental Science & Technology
Stina Paulsson, Staffan Eksborg, Åsa Andersson, Per Nydert, Lena Grahnquist
OBJECTIVE: The aim of this retrospective study was to investigate the clinical practice, i.e. the frequency of use and the treatment strategies, for acid reducing drugs to neonates in a Swedish hospital. METHODS: Retrospective reviews of charts and interviews with nurses at the neonatal wards of Karolinska University Hospital were performed to identify difficulties that might occur with drug administration. All patients admitted over a 2-month period were included...
2012: J Drug Assess
Yusuke Endo, Yoshitaka Ishihara, Satoshi Tsuno, Akiko Matsuda, Weibin Qian, Norimasa Miura, Junichi Hasegawa
BACKGROUND: Ranitidine is a histamine 2 receptor antagonist, and daijokito is a Kampo (Chinese herbal medicine as practiced in Japan) formula, which is traditionally used for treating constipation and digestive trouble. Previous study demonstrated that daijokito significantly affected the pharmacokinetics of ranitidine in rats; however, the doses of ranitidine and daijokito in that study were higher than in clinical practice. Therefore, we examined the pharmacokinetic interaction between ranitidine and daijokito in clinical practice doses in healthy volunteers...
June 2016: Yonago Acta Medica
Matthew R Ely, Steven A Romero, Dylan C Sieck, Joshua E Mangum, Meredith J Luttrell, John R Halliwill
Histamine contributes to elevations in skeletal muscle blood flow following exercise, which raises the possibility that histamine is an important mediator of the inflammatory response to exercise. We examined the influence of antihistamines on post-exercise blood flow, inflammation, muscle damage, and delayed onset muscle soreness (DOMS) in a model of moderate exercise-induced muscle damage. Subjects consumed either a combination of fexofenadine and ranitidine (blockade, n=12) or nothing (control, n=12) before 45 min of downhill running (-10% grade)...
August 4, 2016: Journal of Applied Physiology
Carolina Garrido Zinn, Nicolas Clairis, Lorena Evelyn Silva Cavalcante, Cristiane Regina Guerino Furini, Jociane de Carvalho Myskiw, Ivan Izquierdo
Social recognition memory (SRM) is crucial for reproduction, forming social groups, and species survival. Despite its importance, SRM is still relatively little studied. Here we examine the participation of the CA1 region of the dorsal hippocampus (CA1) and the basolateral amygdala (BLA) and that of dopaminergic, noradrenergic, and histaminergic systems in both structures in the consolidation of SRM. Male Wistar rats received intra-CA1 or intra-BLA infusions of different drugs immediately after the sample phase of a social discrimination task and 24-h later were subjected to a 5-min retention test...
August 16, 2016: Proceedings of the National Academy of Sciences of the United States of America
Lincy Lawrence, Seema Menon, Sheka Vincent, Vipin P Sivaram, Jose Padikkala
BACKGROUND: Gmelina arborea (GA) is widely used in traditional medicine for treating a number of ailments including gastrointestinal tract disorders. OBJECTIVE: To evaluate the gastroprotective effect of GA stem bark against ethanol-induced gastric ulcer in Wistar rats. MATERIALS AND METHODS: All animals were fasted for 36 h and received GA extract 250 and 500 mg/kg body weight (bw), 1 h before the administration of ethanol. The animals received ranitidine 50 mg/kg bw which served as the standard...
April 2016: Journal of Ayurveda and Integrative Medicine
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
Francesca Bartoli, Cosimo Bruni, Laura Cometi, Jelena Blagojevic, Ginevra Fiori, Lorenzo Tofani, Felice Galluccio, Daniel E Furst, Marco Matucci Cerinic
Infliximab (IFX) is an anti-tumor necrosis factor-alpha antibody used to treat inflammatory joint diseases. Infusion reactions (IR) can occur during and after intravenous administration and often require discontinuation of IFX therapy. This retrospective study aimed at evaluating the incidence of IR in patients with joint inflammatory diseases receiving IFX with and without premedication. Clinical charts of rheumatoid arthritis, psoriatic arthritis, and ankylosing spondylitis patients receiving IFX from January 2002 to December 2014 were reviewed...
November 2016: Clinical Rheumatology
Nathalie Vernaz, Victoria Rollason, Liene Adlere, Christophe Combescure, Antoine Poncet, Pascal Bonnabry, Jules Desmeules
The antiplatelet clopidogrel and the proton pump inhibitor esomeprazole demonstrate a pharmacokinetic interaction through CYP2C19 that could translate into clinical inefficacy of clopidogrel. No medical consensus as to their coprescription has been reached, and different guidelines are available. We evaluated the prescribing practices at the Geneva University Hospitals (HUG) by measuring whether the coprescription was staggered as suggested by experts. We estimated the financial impact of different implementation guidelines...
June 2016: Pharmacology Research & Perspectives
Ismael Lares Asseff, Graciela Benitez Gaucin, Hugo Juárez Olguín, Jose Antonio Godinez Nájera, Alejandra Toledo López, Gabriela Pérez Guillé, Fausto Zamura Torres
BACKGROUND: The aim of this study was to determine the effect of gestational age on pharmacokinetics of ranitidine in newborns with gastroesophageal reflux. METHODS: A prospective, descriptive and pharmacokinetic study was carried out in 30 pre-term and 20 full-term babies. 3 mg/kg of ranitidine was administered intravenously to all the babies and at 0.25, 0.5, 1, 2, 4, and 8 h following the administration, samples of blood were drawn to assess ranitidine levels using high performance liquid chromatographic technique...
2016: BMC Pediatrics
Lokesh Verma, Nishant S Jain
Intrigued by the report demonstrating an increase in brain histamine levels by ethanol administration and central histamine transmission to affect the anxiety related behaviors, the present study examined the permissive role of central histaminergic transmission in the acute anxiolytic-like effect of the ethanol on elevated plus maze (EPM) in mice. Results demonstrated that prior administration of the agents that are known to enhance the brain histamine transmission, i.e. low dose of histamine (0.1μg/mouse, i...
October 15, 2016: Behavioural Brain Research
Julian Mamo, Sara Insa, Hèctor Monclús, Ignasi Rodríguez-Roda, Joaquim Comas, Damià Barceló, Maria José Farré
The removal of N-nitrosodimethylamine (NDMA) formation potential through a membrane bioreactor (MBR) coupled to a nanofiltration (NF) pilot plant that treats urban wastewater is investigated. The results are compared to the fate of the individual NDMA precursors detected: azithromycin, citalopram, erythromycin, clarithromycin, ranitidine, venlafaxine and its metabolite o-desmethylvenlafaxine. Specifically, the effect of dissolved oxygen in the aerobic chamber of the MBR pilot plant on the removal of NDMA formation potential (FP) and individual precursors is studied...
October 1, 2016: Water Research
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