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BMC Pharmacology & Toxicology

Melissa Palmer, Lee Jennings, Debra G Silberg, Caleb Bliss, Patrick Martin
BACKGROUND: Accumulation of toxic free cholesterol in hepatocytes may cause hepatic inflammation and fibrosis. Volixibat inhibits bile acid reuptake via the apical sodium bile acid transporter located on the luminal surface of the ileum. The resulting increase in bile acid synthesis from cholesterol could be beneficial in patients with non-alcoholic steatohepatitis. This adaptive dose-finding study investigated the safety, tolerability, pharmacodynamics, and pharmacokinetics of volixibat...
March 16, 2018: BMC Pharmacology & Toxicology
Tinchou Li, Mingcheng Lee, Fuming Tsai, Yunhsiang Chen, Yiyin Lin, Maoliang Chen
BACKGROUND: Based on accumulating evidence, the regulation of protein expression by antipsychotic drugs (APDs) might be closely related to the control of psychotic symptoms when these drugs are used to treat mental disorders. The low quantity of nuclear proteins in the cell hinders their detection because signal for rare proteins are masked in most proteomic detection systems. METHODS: Nuclear proteins fractionated from APD-treated B35 cells were labeled with iTRAQ and detected by LC/MS/MS to investigate APD-induced alterations in nuclear protein expression...
March 7, 2018: BMC Pharmacology & Toxicology
Kamil Kuca, Kamil Musilek, Daniel Jun, Jana Zdarova-Karasova, Eugenie Nepovimova, Ondrej Soukup, Martina Hrabinova, John Mikler, Tanos C C Franca, Elaine F F Da Cunha, Alexandre A De Castro, Martin Valis, Teodorico C Ramalho
BACKGROUND: Based on in vitro and in vivo rat experiments, the newly developed acetylcholinesterase (AChE) reactivator, K203, appears to be much more effective in the treatment of tabun poisonings than currently fielded oximes. METHODS: To determine if this reactivating efficacy would extend to humans, studies were conducted in vitro using human brain homogenate as the source of AChE. The efficacy of K203 was compared with commercially available oximes; pralidoxime, obidoxime and asoxime (HI-6)...
February 21, 2018: BMC Pharmacology & Toxicology
Isabelle Guay, Simon Boulanger, Charles Isabelle, Eric Brouillette, Félix Chagnon, Kamal Bouarab, Eric Marsault, François Malouin
BACKGROUND: Tomatidine (TO) is a plant steroidal alkaloid that possesses an antibacterial activity against the small colony variants (SCVs) of Staphylococcus aureus. We report here the spectrum of activity of TO against other species of the Bacillales and the improved antibacterial activity of a chemically-modified TO derivative (FC04-100) against Listeria monocytogenes and antibiotic multi-resistant S. aureus (MRSA), two notoriously difficult-to-kill microorganisms. METHODS: Bacillus and Listeria SCVs were isolated using a gentamicin selection pressure...
February 13, 2018: BMC Pharmacology & Toxicology
Alexander J Sandweiss, Christopher M Morrison, Anne Spichler, John Rozich
BACKGROUND: Clonidine is an imidazoline sympatholytic, acting on both α2 -adrenergic and imidazoline receptors in the brainstem to induce antihypertensive and negative chronotropic effects in the vasculature and heart respectively. CASE PRESENTATION: A 69-year-old gentleman with hypertension presented to the emergency department after multiple syncopal episodes over the past 12 months. Electrocardiogram demonstrated sinus bradycardia with a heart rate of 42 beats per minute...
February 13, 2018: BMC Pharmacology & Toxicology
I-Yun Lee, Yin-Yin Lin, Yao-Hsu Yang, Yu-Shin Lin, Chun-Liang Lin, Wei-Yu Lin, Yu-Ching Cheng, Li-Hsin Shu, Ching-Yuan Wu
BACKGROUND: Radiotherapy plays an important role in the treatment of prostate cancer. Despite that sophisticated techniques of radiotherapy and radiation combined with chemotherapy were applied to the patients, some tumors may recur. Therefore, the study investigated the effect of dihydroisotanshinone I (DT) and the combination treatment of 5 μM DT and 5Gy irradiation (IR) against the migration ability of prostate cancer cells. METHODS: DT and the combination treatment were studied for its biological activity against migration ability of prostate cancer cells with transwell migration assay...
January 31, 2018: BMC Pharmacology & Toxicology
Hyun-Moon Back, Byungjeong Song, Sudeep Pradhan, Jung-Woo Chae, Nayoung Han, Wonku Kang, Min Jung Chang, Jiao Zheng, Kwang-Il Kwon, Mats O Karlsson, Hwi-Yeol Yun
BACKGROUND: Oral administration of drugs is convenient and shows good compliance but it can be affected by many factors in the gastrointestinal (GI) system. Consumption of food is one of the major factors affecting the GI system and consequently the absorption of drugs. The aim of this study was to develop a mechanistic GI absorption model for explaining the effect of food on fenofibrate pharmacokinetics (PK), focusing on the food type and calorie content. METHODS: Clinical data from a fenofibrate PK study involving three different conditions (fasting, standard meals and high-fat meals) were used...
January 25, 2018: BMC Pharmacology & Toxicology
Reem Ali Shaker, Samer Hassan Abboud, Hayder Chasib Assad, Najah Hadi
BACKGROUND: Doxorubicin (DOX) is commonly used in the treatment of many types of cancers but its cardiotoxicity is limiting its clinical use. Beyond its anticoagulant action, enoxaparin (ENX), a low molecular weight heparin, has been shown to exert multiple pharmacological actions including antioxidant, anti-inflammatory and antiapoptotic effects. Therefore, the current study aimed to assess if ENX could ameliorate cardiotoxicity induced by DOX. METHODS: Twenty-one adult male Wistar albino rats were randomly allocated into three groups (n = 7 each) of control, receiving 0...
January 10, 2018: BMC Pharmacology & Toxicology
Nana Tsiklauri, Natia Pirkulashvili, Ivliane Nozadze, Marina Nebieridze, Gulnaz Gurtskaia, Elene Abzianidze, Merab G Tsagareli
BACKGROUND: In the past decade several studies have reported that in some brain areas, particularly, in the midbrain periaqueductal gray matter, rostral ventro-medial medulla, central nucleus of amygdala, nucleus raphe magnus, and dorsal hippocampus, microinjections of non-steroidal anti-inflammatory drugs (NSAIDs) induce antinociception with distinct development of tolerance. Given this evidence, in this study we investigated the development of tolerance to the analgesic effects of NSAIDs diclofenac, ketorolac and xefocam microinjected into the rostral part of anterior cingulate cortex (ACC) in rats...
January 6, 2018: BMC Pharmacology & Toxicology
Marisa Boff Costa, Paulo Dornelles Picon, Guilherme Becker Sander, Hugo Nodarse Cuni, Carmen Valenzuela Silva, Rolando Páez Meireles, Ana Carolina Magalhães Andrade Góes, Nadia Maria Batoreu, Maria de Lourdes de Sousa Maia, Elizabeth Maciel Albuquerque, Denise Cristina de Souza Matos, Pedro Lopez Saura
BACKGROUND: Several countries have used pegylation technology to improve the pharmacokinetic properties of essential drugs. Recently, a novel interferon alfa-2b protein conjugated to four-branched 12 kDa polyethylene glycol molecules was developed jointly between Cuba and Brazil. The aim of this study was to compare the pharmacokinetic properties of BIP48 (pegylated interferon alfa-2b from Bio-Manguinhos/Fiocruz, Brazil) to those of PEGASYS® (commercially available pegylated interferon alfa-2a from Roche Pharmaceutical)...
January 4, 2018: BMC Pharmacology & Toxicology
Arnold Donkor Forkuo, Charles Ansah, David Pearson, Werner Gertsch, Amanda Cirello, Adam Amaral, Jaimie Spear, Colin W Wright, Caroline Rynn
BACKGROUND: This study aims at characterizing the in vitro metabolism of cryptolepine using human and rat hepatocytes, identifying metabolites in rat plasma and urine after a single cryptolepine dose, and evaluating the single-dose oral and intravenous pharmacokinetics of cryptolepine in male Sprague Dawley (SD) rats. METHODS: The in vitro metabolic profiles of cryptolepine were determined by LC-MS/MS following incubation with rat and human hepatocytes. The in vivo metabolic profile of cryptolepine was determined in plasma and urine samples from Sprague Dawley rats following single-dose oral administration of cryptolepine...
December 22, 2017: BMC Pharmacology & Toxicology
Omar Babateen, Sergiy V Korol, Zhe Jin, Amol K Bhandage, Aikeremu Ahemaiti, Bryndis Birnir
BACKGROUND: γ-Aminobutyric acid (GABA) is the main inhibitory neurotransmitter in the brain where it regulates activity of neuronal networks. The receptor for glucagon-like peptide-1 (GLP-1) is expressed in the hippocampus, which is the center for memory and learning. In this study we examined effects of liraglutide, a GLP-1 analog, on GABA signaling in CA3 hippocampal pyramidal neurons. METHODS: We used patch-clamp electrophysiology to record synaptic and tonic GABA-activated currents in CA3 pyramidal neurons in rat hippocampal brain slices...
December 16, 2017: BMC Pharmacology & Toxicology
Chih-Jen Yang, Ming-Ju Tsai, Jen-Yu Hung, Mei-Hsuan Lee, Ying-Ming Tsai, Yu-Chen Tsai, Jui-Feng Hsu, Ta-Chih Liu, Ming-Shyan Huang, Inn-Wen Chong
BACKGROUND: Afatinib is a second-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI). Compared to cytotoxic chemotherapy, afatinib has been shown to have better efficacy in the treatment of non-small cell lung cancer harboring EGFR mutations. However, 40 mg daily as the initial dose is often accompanied by serious adverse drug reactions (ADRs) and 28 to 53.3% of patients required a dose reduction. No previous study has compared the clinical efficacy and ADRs of different initial doses (40 mg vs...
December 13, 2017: BMC Pharmacology & Toxicology
Stefanie Geith, Bertold Renner, Christian Rabe, Jochen Stenzel, Florian Eyer
BACKGROUND: Inquiries relating to ibuprofen overdose have more than tripled in the last ten years in our poison control center. Although the vast majority of cases have a benign clinical course, there are few severe or even fatal cases present with refractory circulatory failure. CASE PRESENTATION: We describe a case of a 48 year-old male with suicidal mono-ingestion of approximately 72 g ibuprofen. Despite an initial rapid spontaneous drop in the total ibuprofen plasma concentration (IPC) from 550 to 275 mcg/mL within the first 5 h after admission, the patient developed a circulatory failure, refractory to aggressive fluid resuscitation and high doses of vasopressors...
December 12, 2017: BMC Pharmacology & Toxicology
Pravesh Kumar Bundhun, Jia-Xin Shi, Feng Huang
BACKGROUND: Prasugrel and Ticagrelor are emerging antiplatelet drugs that might have the potential to replace currently used antiplatelet agents. Previous analyses comparing prasugrel with ticagrelor mainly focused on an indirect comparison whereas direct comparison was reported only in a few recently published trials. We aimed to systematically carry out a head to head comparison of the adverse clinical outcomes which were associated with prasugrel versus ticagrelor in patients with acute coronary syndrome (ACS)...
December 12, 2017: BMC Pharmacology & Toxicology
Alan O Vázquez-Alvarez, Lorena Michele Brennan-Bourdon, Ana Rosa Rincón-Sánchez, María Cristina Islas-Carbajal, Selene G Huerta-Olvera
BACKGROUND: The aim of this study was to detect and analyze Adverse Drug Reactions (ADRs) through Intensive Pharmacovigilance (IPV) in hospitalized pediatric patients to improve drug safety. METHODS: A prospective 6-month cross-sectional study was performed in the pediatric service of a regional hospital in Mexico in order to assess hospitalized children from 1 day to 18 years old. The inclusion criteria were: both genders, all hospitalization causes, and at least one prescribed medication (indistinct drug group)...
December 8, 2017: BMC Pharmacology & Toxicology
Muhammad M Hammami, Sophia J S De Padua, Rajaa Hussein, Eman Al Gaai, Nesrine A Khodr, Reem Al-Swayeh, Syed N Alvi, Nada Binhashim
BACKGROUND: The extents of generic-reference and generic-generic average bioequivalence and intra-subject variation of on-market drug products have not been prospectively studied on a large scale. METHODS: We assessed bioequivalence of 42 generic products of 14 immediate-release oral drugs with the highest number of generic products on the Saudi market. We conducted 14 four-sequence, randomized, crossover studies on the reference and three randomly-selected generic products of amlodipine, amoxicillin, atenolol, cephalexin, ciprofloxacin, clarithromycin, diclofenac, ibuprofen, fluconazole, metformin, metronidazole, paracetamol, omeprazole, and ranitidine...
December 8, 2017: BMC Pharmacology & Toxicology
Manuela Malsy, Bernhard Graf, Anika Bundscherer
BACKGROUND: Adenocarcinoma of the pancreas is one of the most aggressive cancer diseases affecting the human body. Recent research has shown the importance of the perioperative phase in disease progression. Particularly during this vulnerable phase, substances such as metamizole and paracetamol are given as general anesthetics and postoperative analgesics. Therefore, the effects of metamizole and paracetamol on tumor progression should be investigated in more detail because the extent to which these substances influence the carcinogenesis of pancreatic carcinoma is still unclear...
December 6, 2017: BMC Pharmacology & Toxicology
Inken Arnold, Kati Straube, Wolfgang Himmel, Stephanie Heinemann, Vivien Weiss, Laura Heyden, Eva Hummers-Pradier, Roland Nau
BACKGROUND: Many elderly patients receive psychotropic drugs. Treatment with psychotropic agents is associated with serious side effects including an increased risk of falls and fractures. Several psychotropic drugs are considered potentially inappropriate for treatment of the elderly. METHODS: A retrospective chart review was conducted covering all patients aged ≥ 65 years who were admitted to Evangelisches Krankenhaus Göttingen-Weende between 01/01/2013 and 03/31/2013...
December 4, 2017: BMC Pharmacology & Toxicology
Qasim Khan, Mohammad Ismail, Sehrash Khan
BACKGROUND: Cancer patients may receive a high number of medications with the potential to prolong QT interval and subsequent TdP (torsades de pointes). This study aimed to identify the prevalence of QT prolonging drugs, their TdP risk, QT prolonging drug-drug interactions (QT-DDIs), levels, predictors, and TdP risk of drugs involved in QT-DDIs. METHODS: This multicenter study included cancer patients from three major tertiary care hospitals of Khyber-Pakhtunkhwa, Pakistan...
December 1, 2017: BMC Pharmacology & Toxicology
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