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Basic & Clinical Pharmacology & Toxicology

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https://www.readbyqxmd.com/read/28229534/letter-to-the-editor
#1
LETTER
Adriana Oller
No abstract text is available yet for this article.
February 22, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28218988/toxicological-effects-during-and-following-persistent-insulin-induced-hypoglycaemia-in-healthy-euglycaemic-rats
#2
Vivi F H Jensen, Anne-Marie Mølck, Line O Berthelsen, Lene Alifrangis, Lene Andersen, Melissa Chapman, Jens Lykkesfeldt, Ingrid B Bøgh
New insulin analogues with a longer duration of action and a "peakless" pharmacokinetic profile have been developed to improve efficacy, safety and convenience for diabetic patients. During non-clinical development, according to regulatory guidelines, these analogues are tested in healthy euglycaemic rats rendering them persistently hypoglycaemic. Little is known about the effect of persistent (24 hr/day) insulin-induced hypoglycaemia (IIH) in rats, complicating interpretation of results in pre-clinical studies with new longer-acting insulin analogues...
February 20, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28212463/efficacy-and-tolerability-of-an-inhaled-selective-glucocorticoid-receptor-modulator-azd5423-in-copd-patients-phase-ii-study-results
#3
Piotr Kuna, Magnus Aurivillius, Carin Jorup, Susanne Prothon, Ziad Taib, Staffan Edsbäcker
AZD5423 is a novel, inhaled, selective glucocorticoid receptor modulator (SGRM), which in an allergen challenge model in asthmatics improved lung function and airway hyper-reactivity. In the current trial, AZD5423 was for the first time tested in patients with chronic obstructive pulmonary disease (COPD). In this double-blind, randomised and parallel group study, we examined airway and systemic effects of two doses of AZD5423, inhaled via Turbuhaler for 12 weeks, in 353 symptomatic COPD patients (average pre-bronchodilator forced expiratory volume in one second (FEV1) at screening was 50-52% of predicted normal)...
February 17, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28208233/neonatal-exposure-to-endocrine-disrupting-chemicals-impair-learning-behaviour-by-disrupting-hippocampal-organization-in-male-swiss-albino-mice
#4
Rakesh Bhaskar, Ashish K Mishra, Banalata Mohanty
Hippocampus is highly susceptible to endocrine disrupting chemicals exposure particularly during the critical phase of brain development. In the present study, mice offspring were exposed to endocrine disruptors mancozeb (MCZ) and imidacloprid (IMI) individually (40 mg MCZ and 0.65 mg IMI/kg/day) as well as to their equimixture (40 mg MCZ + 0.65 mg IMI/kg/day) through the diet of lactating mothers from post-natal day (PND) 1 to PND 28. Half of the randomly selected male offspring were killed at PND 29 and the rest half were left unexposed and killed at PND 63...
February 16, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28165667/use-of-moderate-intensity-statins-for-low-density-lipoprotein-cholesterol-level-above-190-mg-dl-at-baseline-in-koreans
#5
Hun-Sung Kim, Hyeseon Lee, Sue Hyun Lee, Yoo Jin Jeong, Tong Min Kim, So Jung Yang, Sun Jung Baik, Hyunah Kim, Seung-Hwan Lee, Jae Hyoung Cho, In-Young Choi, Kun-Ho Yoon, Ju Han Kim
The ACC/AHA 2013 guideline recommends high-intensity statin therapy for a decrease in low-density lipoprotein cholesterol (LDL-C) level by >50% among patients with baseline values of ≥190 mg/dL (approximately 4.872 mmol/L); however, this value should be modified before applying it to Korean populations. We investigated the statin-specific LDL-C-lowering effects in Korean patients with baseline LDL-C value ≥ 4.872 mmol/L. Data of patients prescribed a statin for the first time from January 2009 to December 2013 were assessed...
February 6, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28164442/odense-pharmacoepidemiological-database-oped-a-review-of-use-and-content
#6
Jesper Hallas, Maja Hellfritzsch, Morten Rix, Morten Olesen, Mette Reilev, Anton Pottegård
The Odense University Pharmacoepidemiological Database (OPED) is a prescription database established in 1990 by the University of Southern Denmark, covering reimbursed prescriptions from the county of Funen in Denmark and the region of Southern Denmark (1.2 million inhabitants). It is still active and thereby has more than 25 years' of continuous coverage. In this MiniReview, we review its history, content, quality, coverage, governance and some of its uses. OPED's data include the Danish Civil Registration Number (CPR), which enables unambiguous linkage with virtually all other health-related registers in Denmark...
February 5, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28135763/the-cyp2c19-2-and-cyp2c19-17-polymorphisms-play-a-vital-role-in-clopidogrel-responsiveness-after-percutaneous-coronary-intervention-a-pharmacogenomics-study
#7
Faruk Saydam, İrfan Değirmenci, Alparslan Birdane, Mahmut Özdemir, Taner Ulus, Cansu Özbayer, Ertuğrul Çolak, Necmi Ata, Hasan Veysi Güneş
Clopidogrel inhibits platelet activation and aggregation by blocking the P2Y12 receptor. Dual antiplatelet therapy with clopidogrel and aspirin is recommended treatment by current guidelines for patients undergoing percutaneous interventions. Recurrent ischaemic cardiac events after this treatment showed lack of clopidogrel responsiveness. We aimed to investigate the most noticeable variants in the genes involved in clopidogrel pharmacokinetics and pharmacodynamics. 347 Turkish patients who underwent percutaneous coronary interventions with stent implantation were included in our study...
January 30, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28132418/switching-adverse-effects-and-use-of-over-the-counter-analgesics-among-users-of-oral-anticoagulants-a-pharmacy-based-survey
#8
Maja Hellfritzsch, Lea Maria Rønneberg Hyllested, Line Meegaard, Alexander Wiberg-Hansen, Erik Lerkevang Grove, Anton Pottegård
Oral anticoagulants are widely used but information on important aspects in that respect is not available from medical registers or clinical databases. Therefore, we conducted a survey including patients filling a prescription for oral anticoagulants at two large Danish community pharmacies. We collected information concerning the patients' knowledge of their anticoagulant treatment including prior drug switching. Further, patients were asked about use of over-the-counter analgesics, adverse effects, and how the treatment affected their everyday life...
January 28, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28132416/modification-of-the-fc-region-of-a-human-anti-oncostatin-m-monoclonal-antibody-for-higher-affinity-to-fcrn-and-extension-of-half-life-in-cynomolgus-monkeys
#9
Ivo P Nnane, Chao Han, Qun Jiao, Susan Tam, Hugh M Davis, Zhenhua Xu
The purpose of this study was to evaluate the pharmacokinetics (PK) of anti-oncostatin M (OSM) IgG1 monoclonal antibodies, CNTO 1119 and its Fc variant (CNTO 8212), which incorporates the LS(Xtend) mutation to extend terminal half-life (T1/2 ), after a single intravenous (IV) or subcutaneous (SC) administration in cynomolgus monkeys, and to predict human PK. In study 1, single doses of CNTO 1119 and CNTO 8212 were administered IV or SC at 3 mg/kg to cynomolgus monkeys (n=3). In study 2, single doses of CNTO 8212 were administered IV at 1, 5 or 20 mg/kg, or SC at 5 mg/kg to cynomolgus monkeys (n=5)...
January 28, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28084056/genetic-influences-of-oprm1-oprd1-and-comt-on-morphine-analgesia-in-a-multi-modal-multi-tissue-human-experimental-pain-model
#10
Lecia Møller Nielsen, Lona Louring Christrup, Hiroe Sato, Asbjørn Mohr Drewes, Anne Estrup Olesen
Human studies on experimentally induced pain are of value to elucidate the genetic influence on morphine analgesia under controlled conditions. The aim of this study was to investigate if genetic variants of mu, kappa and delta opioid receptor genes (OPRM1, OPRK1 and OPRD1) and catechol-O-methyltransferase gene (COMT) are associated with the morphine analgesia. The study was a randomised, double-blind, two-way, cross-over, single-dose study conducted in 40 healthy participants, where morphine was compared with placebo...
January 13, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28064463/global-research-trends-in-lithium-toxicity-from-1913-to-2015-a-bibliometric-analysis
#11
Sa'ed H Zyoud, W Stephen Waring, Waleed M Sweileh, Samah W Al-Jabi
Lithium salts have been used to treat psychiatric disorders since the 1940s and are currently used in prophylaxis and treatment of depression and bipolar disorder. Therefore, we conducted this study to assess lithium toxicity-related publications using bibliometric approaches from a health point of view to assess global research trends in the lithium toxicity field to offer guidance to future research in this field. The data were retrieved from the online version of Scopus database on 6 August 2016. All records with the term "lithium" in the title were retrieved, and those related to lithium toxicity were evaluated...
January 8, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28064437/clinical-pharmacology-research-internships-at-the-interface-of-academia-and-industry-students-perceptions-and-scientific-output
#12
Sebastiaan C Goulooze, Kari L Franson, Adam F Cohen, Robert Rissmann
The Centre for Human Drug Research (CHDR) is a non-profit clinical research institute at the interface between academia and the pharmaceutical industry. CHDR hosts a research internship program for undergraduate (bio)medical students. The aim of this study was i) to investigate the student perceptions of the undergraduate research internship ii) quantify the scientific output related to these internships. We surveyed former interns at the CHDR from the years 2007 - 2014 and quantified their scientific output with a PubMed search...
January 8, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28054752/opposite-modulatory-effects-of-selective-and-non-selective-cyclooxygenase-inhibition-on-cardiovascular-and-autonomic-consequences-of-cyclosporine-in-female-rats
#13
Karim S Ibrahim, Ahmed F El-Yazbi, Hanan M El-Gowelli, Mahmoud M El-Mas
Non-steroidal anti-inflammatory drugs (NSAIDs) and the immunosuppressant drug cyclosporine (CSA) are concurrently administered in arthritis. Here, we investigated whether diclofenac (non-selective inhibitor of cyclooxygenase-1 and 2, COX-1/COX-2), celecoxib (selective COX-2 inhibitor) or SC560 (selective COX-1 inhibitor) interact variably with hemodynamic effects of CSA in conscious female rats. Changes caused by CSA (10 mg/kg i.v.) in blood pressure (BP), heart rate (HR), HR variability (HRV) and myocardial contractility were assessed in absence and presence of individual NSAIDs (10 mg/kg each)...
January 5, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28054742/evaluation-of-dna-damage-in-hepg2-cells-and-mutagenicity-of-garcinielliptone-fc-a-bioactive-benzophenone
#14
Lismare da Silva Prado, Juliana da Silva, Ana Letícia Hilario Garcia, Fernanda Brião Menezes Boaretto, Ivana Grivicich, Lucas Umpierre Conter, Aguisson de Oliveira Salvi, Flávio Henrique Reginatto, Suele Bierhals Vencato, Alexandre de Barros Falcão Ferraz, Jaqueline Nascimento Picada
Garcinielliptone FC (GFC) is a polyprenylated benzophenone isolated from the hexanic extract of Platonia insignis seeds with potential pharmacological effects on the central nervous system. In a pre-clinical study, this compound showed anticonvulsant action, becoming a candidate to treat epilepsy disorders. However, genotoxicological aspects of GFC should be known to ensure its safe use. This study investigated the cytotoxic, genotoxic and mutagenic effects of GFC. Cytotoxicity was evaluated using the colourimetric assay of MTT (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide) in human hepatoma cells (HepG2) (2 - 100 μg/mL) for 3, 6 and 24 hr...
January 5, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28052578/ticagrelor-increased-adenosine-and-cyclic-adenosine-monophosphate-plasma-concentration-compared-with-clopidogrel-in-acute-coronary-syndromes-patients
#15
Xiao-Ye Li, Qi-Bing Wang, Ying Xue, Jia-Hui Chen, Qian-Zhou Lv
Ticagrelor produces a more potent antiplatelet effect than clopidogrel, and inhibits cellular uptake of adenosine, which is associated with several cardiovascular consequences. We aimed to explore the correlation between adenosine and cyclic adenosine monophosphate (cAMP) plasma concentration and antiplatelet effect by clopidogrel or ticagrelor in acute coronary syndrome (ACS) patients receiving dual antiplatelet therapy (DAPT). We conducted a prospective, observational and single-centre cohort study enrolling 68 patients with non-ST-segment elevation ACS from January 2016 to May 2016...
January 4, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28032943/mass-spectrometry-based-tools-to-characterize-dna-protein-cross-linking-by-bis-electrophiles
#16
Arnold Groehler, Amanda Degner, Natalia Y Tretyakova
DNA-protein cross-links (DPCs) are unusually bulky DNA adducts that form in cells as a result of exposure to endogenous and exogenous agents including reactive oxygen species, ultraviolet light, ionizing radiation, environmental agents (e.g. transition metals, formaldehyde, 1,2-dibromoethane, 1,3-butadiene) and common chemotherapeutic agents. Covalent DPCs are cytotoxic and mutagenic due to their ability to interfere with faithful DNA replication and prevent accurate gene expression. Key to our understanding of the biological significance of DPC formation is identifying the proteins most susceptible to forming these unusually bulky and complex lesions and quantifying the extent of DNA-protein cross-linking in cells and tissues...
December 29, 2016: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28032440/magnolol-attenuates-concanavalin-a-induced-hepatic-fibrosis-inhibits-cd4-t-helper-17-th17-cell-differentiation-and-suppresses-hepatic-stellate-cell-activation-blockade-of-smad3-smad4-signalling
#17
Hongjun Zhang, Baoling Ju, Xiaoli Zhang, Yanfei Zhu, Ying Nie, Yuanhong Xu, Qiuxia Lei
Magnolol is a pharmacological biphenolic compound extracted from Chinese herb Magnolia officinalis, which displays anti-inflammatory and antioxidant effects. This study was aimed at exploring the potential effect of magnolol on immune-related liver fibrosis. Herein, BALB/c mice were injected with concanavalin A (ConA, 8 mg/kg/week) up to 6 weeks to establish hepatic fibrosis, and magnolol (10, 20, 30 mg/kg/day) was given to these mice orally throughout the whole experiment. We found that magnolol preserved liver function and attenuated liver fibrotic injury in vivo...
December 29, 2016: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28027430/pharmacological-properties-of-melanin-and-its-function-in-health
#18
Adila Salih ElObeid, Afaf Kamal-Eldin, Mohamed Anwar K Abdelhalim, Adil M Haseeb
The biological pigment melanin is present in most of the biological systems. It manifests a host of biological and pharmacological properties. Its role as a molecule with special properties and functions affecting general health, including photo-protective and immunological action are well recognised. Its antioxidant, anti-inflammatory, immuno-modulatory, radio-protective, hepatic, gastrointestinal and hypoglycaemic benefits have only recently been recognised and studied. It is also associated with certain disorders of the nervous system...
December 27, 2016: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28001342/triggering-mechanisms-and-inflammatory-effects-of-combustion-exhaust-particles-with-implication-for-carcinogenesis
#19
J Øvrevik, M Refsnes, M Låg, B Brinchmann, P E Schwarze, J A Holme
A number of biological responses may contribute to the carcinogenic effects of combustion-derived particulate matter (CPM). Here, we focus on mechanisms that trigger CPM-induced pro-inflammatory responses. Inflammation has both genotoxic as well as non-genotoxic implications and is considered to play a central role in development of various health outcomes associated with CPM exposure, including cancer. Chronic, low-grade inflammation may cause DNA damage through a persistent increased level of reactive oxygen species (ROS) produced and released by activated immune cells...
December 21, 2016: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28000392/the-antinociceptive-activity-of-geraniol
#20
LETTER
Salvatore Chirumbolo, Geir Bjørklund
No abstract text is available yet for this article.
December 20, 2016: Basic & Clinical Pharmacology & Toxicology
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