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S K Bedada, R Appani, P K Boga
Carbamazepine (CBZ) is a widely used antiepileptic drug with narrow therapeutic window and it may be prone to drug interactions. The purpose of present study was to investigate the effect of PIP on metabolism and pharmacokinetics of CBZ in healthy volunteers. An open-label, 2 period, sequential study was conducted in 12 healthy volunteers. PIP 20 mg was administered once daily for 10 days during treatment phase. A single dose of CBZ 200 mg was administered during control and after treatment phases under fasting conditions...
October 24, 2016: Drug Research
Antoun Nader, Mark C Kendall, David W Manning, Matthew Beal, Rohit Rahangdale, Robert Dekker, Gildasio S De Oliveira, Eric Kamenetsky, Robert J McCarthy
BACKGROUND AND OBJECTIVES: A single-dose adductor canal block can provide postoperative analgesia for patients undergoing total knee arthroplasty (TKA). The purpose of this study was to assess postoperative opioid consumption after ultrasound-guided single-injection bupivacaine compared with saline adductor canal block for patients undergoing TKA. METHODS: After institutional review board approval, written informed consent was obtained from patients (>18 years old) undergoing elective TKA...
November 2016: Regional Anesthesia and Pain Medicine
Jacob J Morse, Gramos Pallaska, Patrick R Pierce, Travis M Fields, Sujay S Galen, Moh H Malek
Morse, JJ, Pallaska, G, Pierce, PR, Fields, TM, Galen, SS, and Malek, MH. Acute low-dose caffeine supplementation increases electromyographic fatigue threshold in healthy men. J Strength Cond Res 30(11): 3236-3241, 2016-The purpose of this study is to determine whether consumption of a single low-dose caffeine drink will delay the onset of the electromyographic fatigue threshold (EMGFT) in the superficial quadriceps femoris muscles. We hypothesize that the EMGFT values for the caffeine condition will be significantly higher than the EMGFT values for the placebo condition...
November 2016: Journal of Strength and Conditioning Research
Andreas Gollner, Dorothea Rudolph, Heribert Arnhof, Markus Bauer, Sophia Maria Blake, Guido Boehmelt, Xiao-Ling Cockcroft, Georg Dahmann, Peter Ettmayer, Thomas Gerstberger, Jale Karolyi-Oezguer, Dirk Kessler, Christiane Kofink, Juergen Ramharter, Jörg Rinnenthal, Alexander Savchenko, Renate Schnitzer, Harald Weinstabl, Ulrike Weyer-Czernilofsky, Tobias Wunberg, Darryl B McConnell
Scaffold modification based on Wang´s pioneering MDM2-p53 inhibitors led to novel, chemically stable spiro-oxindole compounds bearing a spiro[3H-indole-3,2´-pyrrolidin]-2(1H)-one scaffold that are not prone to epimerization as observed for the initial spiro[3H-indole-3,3´-pyrrolidin]-2(1H)-one scaffold. Further structure based optimization inspired by natural product architectures led to a complex fused ring system ideally suited to bind to the MDM2 protein and to interrupt its protein-protein interaction (PPI) with TP53...
October 24, 2016: Journal of Medicinal Chemistry
Elisabeth Bezine, Yann Malaisé, Aurore Loeuillet, Marianne Chevalier, Elisa Boutet-Robinet, Bernard Salles, Gladys Mirey, Julien Vignard
The Cytolethal Distending Toxin (CDT), produced by many bacteria, has been associated with various diseases including cancer. CDT induces DNA double-strand breaks (DSBs), leading to cell death or mutagenesis if misrepaired. At low doses of CDT, other DNA lesions precede replication-dependent DSB formation, implying that non-DSB repair mechanisms may contribute to CDT cell resistance. To address this question, we developed a proliferation assay using human cell lines specifically depleted in each of the main DNA repair pathways...
October 24, 2016: Scientific Reports
Anita S Iyer, Malika Bouhenia, John Rumunu, Abdinasir Abubakar, Randon J Gruninger, Jane Pita, Richard Lako Lino, Lul L Deng, Joseph F Wamala, Edward T Ryan, Stephen Martin, Dominique Legros, Justin Lessler, David A Sack, Francisco J Luquero, Daniel T Leung, Andrew S Azman
Despite recent large-scale cholera outbreaks, little is known about the immunogenicity of oral cholera vaccines (OCV) in African populations, particularly among those at highest cholera risk. During a 2015 preemptive OCV campaign among internally displaced persons in South Sudan, a year after a large cholera outbreak, we enrolled 37 young children (1-5 years old), 67 older children (6-17 years old) and 101 adults (≥18 years old), who received two doses of OCV (Shanchol) spaced approximately 3 weeks apart...
October 24, 2016: Scientific Reports
Vaishali Yadav, Shyam Sunder Chatterjee, Muhammed Majeed, Vikas Kumar
AIM: To compare stress resistance increasing and analgesic activities of piperlongumine and a methanolic Piper longum fruit extract (PLE). METHODS: Efficacies of a single and repeated daily oral doses (1-256 mg/kg/day) of PLE, piperlongumine, and 50 mg/kg/day doxycycline against foot shock stress triggered alteration in body weights and core temperatures, and of their 11 daily doses on antidepressants like activity in tail suspension test and on pentobarbital induced sedation in male mice were compared...
October 2016: Journal of Traditional and Complementary Medicine
Venugopala Rao Konda, Ruckmani Arunachalam, Madhavi Eerike, Ramesh Rao K, Arun Kumar Radhakrishnan, Lakshmipathy Prabhu Raghuraman, Vinayak Meti, Sobita Devi
The gravity of the impact of renal failure on human health is well known and as there is no specific pharmacotherapy for renal failure, the current study was undertaken to evaluate the effect of root extract of Azima tetracantha, an ancient medicinal plant used in Siddha and Ayurvedhic systems of medicine. The experiment was done in glycerol-induced acute renal failure in Wistar albino rats. Thirty rats were divided into five groups. Group 1 was given normal saline (10 ml/kg) per oral, group 2 with single dose of hypertonic glycerol (8 ml/kg) by intramuscular injection into the hind limbs, group 3 with glycerol and ethanolic extract of A...
October 2016: Journal of Traditional and Complementary Medicine
Jeong Yeon Kang, Jieming Gao, Dae Hwan Shin, Celeste Alvarez, Weixiong Zhong, Glen S Kwon
BACKGROUND: Delivery of monomeric Amphotericin B (AmB), i.e. deaggregated AmB, has been a major tactic in the reduction of renal toxicity at a membrane level, taking advantage of the selectivity of monomeric AmB for binding ergosterol over cholesterol. OBJECTIVE: The aim of this study was to characterize the pharmacokinetic (PK) and renal toxicity of monomeric AmB in rats following a multiple dose regimen. METHOD: AmB existed primarily in a monomeric state in poly(ethylene glycol)-block-poly(N-hexyl stearate L-aspartamide) (PEG-b-PHSA) micelles (mAmB) at 2:1 ratio (mol:mol), whereas AmB as its standard formulation, Fungizone(®), was highly self-aggregated based on absorption spectroscopy...
2016: Pharm Nanotechnol
Tee Joo Yeo, Poh Shuan Daniel Yeo, Farid Abdul Hadi, Timothy Cushway, Kim Yee Lee, Bee Choo Tai, Carolyn S P Lam
AIMS: Iron deficiency (ID) is highly prevalent in patients with heart failure (HF) worldwide regardless of haemoglobin levels. Results from therapeutic trials of intermittently dosed intravenous (i.v.) iron are promising in the ambulatory Caucasian population with HF with reduced left ventricular ejection fraction, although evidence is scarce in Asia. The Pilot Randomized Controlled Trial to Assess the Role of Intravenous Ferric Carboxymaltose in Asian Patients with Heart Failure aims to assess the effect of single-dose i...
June 2016: ESC Heart Failure
Ying Liu, Yang Qi, Zhi-Hui Bai, Chen-Xu Ni, Qi-Hui Ren, Wei-Heng Xu, Jing Xu, Hong-Gang Hu, Lei Qiu, Jian-Zhong Li, Zhi-Gao He, Jun-Ping Zhang
AIM: Matrine is an alkaloid extracted from a Chinese herb Sophora flavescens Ait, which has shown chemopreventive potential against various cancers. In this study, we evaluated the anticancer efficacy of a novel derivative of matrine, (6aS, 10S, 11aR, 11bR, 11cS)-10- methylamino-dodecahydro- 3a,7a-diaza-benzo (de) (MASM), against human hepatocellular carcinoma (HCC) cells and their corresponding sphere cells in vitro and in vivo. METHODS: Human HCC cell lines (Hep3B and Huh7) were treated with MASM...
October 24, 2016: Acta Pharmacologica Sinica
Pushpa Ranjan Wijesinghe, M R Nihal Abeysinghe, Sutee Yoksan, Yafu Yao, Benli Zhou, Lei Zhang, Jessica A Fleming, Anthony A Marfin, John C Victor
BACKGROUND: The performance of live attenuated Japanese Encephalitis SA 14-14-2 vaccine (CD-JEV) among children previously given inactivated mouse brain-derived JE vaccine (IMBV) is unknown. We evaluated the safety and immunogenicity of CD-JEV administered to 2- and 5-year-old children in Sri Lanka. METHODS: In this open-label, single arm trial in the Colombo District of Sri Lanka, generally healthy children 2 and 5years of age who had previously received two and three doses of IMBV, respectively, were administered one dose of CD-JEV subcutaneously...
October 20, 2016: Vaccine
Mitiku Bajiro, Daniel Dana, Mio Ayana, Daniel Emana, Zeleke Mekonnen, Belay Zawdie, Asfaw Garbi, Ashenafi Kure, Ahmed Zeynudin
BACKGROUND: Intestinal schistosomiasis is one of the neglected tropical parasitic diseases caused by Schistosoma mansoni. Currently, the control measures for the disease are mainly based on mass drug administration (MDA) with praziquantel (PZQ) targeting the school-age children. In Ethiopia, the potential foci for schistosomiasis and therapeutic efficacy of PZQ among school-age children remain poorly explored. Therefore, we determined both the prevalence and intensity of S. mansoni infection and the therapeutic efficacy of PZQ among school children in the Manna District (new foci for S...
October 24, 2016: Parasites & Vectors
Gabriel A Knudsen, J Michael Sanders, Michael F Hughes, Ethan P Hull, Linda S Birnbaum
1. It was important to investigate the disposition of decabromodiphenyl ethane (DBDPE) based on concerns over its structural similarities to decabromodiphenyl ethane (decaBDE), high potential for environmental persistence & bioaccumulation, and high production volume. 2. In the present study, female Sprague Dawley rats were administered a single dose of [(14)C]-DBDPE by oral, topical, or IV routes. Another set of rats were administered 10 daily oral doses of [(14)C]-DBDPE. Male B6C3F1/Tac mice were administered a single oral dose...
October 24, 2016: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
Roee Admon, Roselinde H Kaiser, Daniel G Dillon, Miranda Beltzer, Franziska Goer, David P Olson, Gordana Vitaliano, Diego A Pizzagalli
OBJECTIVE: Major depressive disorder is characterized by reduced reward-related striatal activation and dysfunctional reward learning, putatively reflecting decreased dopaminergic signaling. The goal of this study was to test whether a pharmacological challenge designed to facilitate dopaminergic transmission can enhance striatal responses to reward and improve reward learning in depressed individuals. METHOD: In a double-blind placebo-controlled design, 46 unmedicated depressed participants and 43 healthy control participants were randomly assigned to receive either placebo or a single low dose (50 mg) of the D2/D3 receptor antagonist amisulpride, which is believed to increase dopamine signaling through presynaptic autoreceptor blockade...
October 24, 2016: American Journal of Psychiatry
Yoshinari Enomoto, Varuna K Gadiyaram, Carola Gianni, Rodney P Horton, Chintan Trivedi, Sanghamitra Mohanty, Luigi Di Biase, Amin Al-Ahmad, J David Burkhardt, Arvin Narula, Gwen Janczyk, Matthew J Price, Rizwan Afzal, Moustapha Atoui, Matthew Earnest, Vijay Swarup, Shephal K Doshi, Sarina van der Zee, Rebecca Fisher, Dhanunjaya R Lakkireddy, Douglas N Gibson, Andrea Natale, Vivek Reddy
BACKGROUND: In the stroke prevention trials of left atrial appendage closure (LAAC) with the Watchman device, a post-implantation anti-thrombotic regimen of 6 weeks of warfarin was employed. OBJECTIVE: Because of the clinical complexity of warfarin use, we studied the relative feasibility and safety of instead employing non-warfarin oral anticoagulants (NOACs) during the peri- and initial post-implantation period after Watchman implantation. METHODS: This is a retrospective multicenter study of consecutive patients undergoing Watchman implantation and receiving peri- and post-procedural NOACs or warfarin...
October 19, 2016: Heart Rhythm: the Official Journal of the Heart Rhythm Society
Koichi Miyamura, Toshihiro Miyamoto, Mitsune Tanimoto, Kazuhito Yamamoto, Shinya Kimura, Tatsuya Kawaguchi, Itaru Matsumura, Tomoko Hata, Hisashi Tsurumi, Shigeki Saito, Masayuki Hino, Seiji Tadokoro, Kuniaki Meguro, Hideo Hyodo, Masahide Yamamoto, Kohmei Kubo, Junichi Tsukada, Midori Kondo, Makoto Aoki, Hikaru Okada, Masamitsu Yanada, Kazuma Ohyashiki, Masafumi Taniwaki
Optimal management of patients with chronic myeloid leukemia in chronic phase with suboptimal molecular response (MR) to frontline imatinib is undefined. We report final results from SENSOR, which evaluated efficacy/safety of nilotinib in this setting. A substudy assessed whether BIM polymorphisms impacted response to nilotinib. In this single-arm, multicenter study, Japanese patients with suboptimal MR per European LeukemiaNet 2009 criteria (complete cytogenetic response, but not major MR [MMR]) after ≥18 months of frontline imatinib received nilotinib 400mg twice daily for 24 months...
September 5, 2016: Leukemia Research
Lin-Hu Ye, Ling-Ti Kong, Ming-Zhu Yan, Fang-Rui Cao, Li-Sha Wang, Yong-Hong Liao, Rui-Le Pan, Qi Chang
ETHNOPHARMACOLOGICAL RELEVANCE: The Chinese herbal medicine He-Ye, the leaves of the lotus (Nelumbo nucifera) plant, is traditionally used in China for the treatment of sunstroke, thirst, diarrhea, and fever. Currently, the leaf is used not only as an herbal tea to reduce lipid level and control body weight, but also as a major ingredient in some lipid-lowering Chinese patented medicines. Our previous study demonstrated that the alkaloid fraction (AF) of the herb has a strong inhibitory effect on CYP2D6 isoenzyme activity in vitro...
October 19, 2016: Journal of Ethnopharmacology
Elisa C Martinez, Ravendra Garg, Pratima Shrivastava, Susantha Gomis, Sylvia van Drunen Littel-van den Hurk
Respiratory syncytial virus (RSV) is the leading cause of acute lower respiratory tract infections in infants and young children. There are no licensed RSV vaccines available, and the few treatment options for high-risk individuals are either extremely costly or cause severe side effects and toxicity. Immunomodulation mediated by a novel formulation consisting of the toll-like receptor 3 agonist poly(I:C), an innate defense regulator peptide and a polyphosphazene (P-I-P) was evaluated in the context of lethal infection with pneumonia virus of mice (PVM)...
October 19, 2016: Antiviral Research
Pearlie P Chong, David van Duin, Ananta Bangdiwala, Anastasia Ivanova, William C Miller, David J Weber, Peter H Gilligan, Thomas C Shea
PURPOSE: Case reports of treatment failure with standard-dose daptomycin (6 mg/kg) have recently surfaced in vancomycin-resistant Enterococcus (VRE) bloodstream infection (BSI) episodes with daptomycin MICs of 3 to 4 mg/L. The clinical implications of daptomycin MICs of 3 to 4 mg/L in VRE BSIs have not been elucidated. METHODS: We performed a single institutional retrospective analysis of adult stem cell transplant recipients and patients with hematologic malignancies diagnosed with VRE BSI from 2006 to 2014 and compared outcomes between those with daptomycin MICs of 3 to 4 mg/L those with 2 mg/L, as determined by Etest...
October 19, 2016: Clinical Therapeutics
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