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Irina Pereira, Patrícia Severino, Ana C Santos, Amélia M Silva, Eliana B Souto
The medicinal properties of essential oils from aromatic plants are known since antiquity. Currently, the technological innovation enabled the reinvention of the ancient plant knowledge leading to the identification and extraction of organic compounds present in essential oils. These organic compounds belong mainly to the terpene group and are accountable for the wide range of bioactive properties attributed to essential oils. Linalool (C10 H18 O), so-called 3,7-dimethyl-1,6-octadien-3-ol, is a monoterpene alcohol broadly present as a major constituent of plant essential oils, particularly lavender and coriander...
August 3, 2018: Colloids and Surfaces. B, Biointerfaces
Robin Guibal, Sophie Lissalde, Yoann Brizard, Gilles Guibaud
Pharmaceutical monitoring (37 pharmaceuticals and 3 human tracers) was conducted in a headwater streams in southwest France, an area characterized by a low population density with an elderly population (30% > 60 years old) and extensive agriculture (cow cattle breeding). Polar Organic Chemical Integrative Sampler (POCIS) were exposed for 14-day consecutive periods in 2016 at three sampling points. Three human wastewater tracers and 20 pharmaceuticals commonly used for human and/or cattle were quantified in headwaters...
July 31, 2018: Journal of Hazardous Materials
C M Bowman, L Z Benet
As explained by the free drug theory, the unbound fraction of drug has long been thought to drive the efficacy of a molecule. Thus, the fraction unbound term, or fu , appears in equations for fundamental pharmacokinetic parameters such as clearance, and is used when attempting in vitro to in vivo extrapolation (IVIVE). In recent years though, it has been noted that IVIVE does not always yield accurate predictions, and that some highly protein bound ligands have more efficient uptake than can be explained by their unbound fractions...
August 8, 2018: European Journal of Pharmaceutical Sciences
Birendra Chaurasiya, Muye Zhou, Jiasheng Tu, Chunmeng Sun
Delivery of inhalational dry powders (DPs) to the lung of mice is pivotal for pre-clinical pharmacokinetic and pharmacodynamic investigations. Although several devices have been reported, their application is always limited by many factors, including complicated design, high price, commercially discontinued status, as well as requirement of special skills. Here, we have introduced a simple device for non-invasive and precise delivery of DPs in mice. We set up the self-made device using a 20 G cannula tube and a 1 mL syringe...
August 9, 2018: European Journal of Pharmaceutical Sciences
Kausar Jahan, Krishna K Pillai, Divya Vohora
The central neurotransmitters assume a noteworthy part in the pathophysiology of epilepsy, noradrenaline is one of them. However, its role in 6 Hz induced psychomotor seizures is not known. The present study was, therefore, designed to investigate the role of noradrenaline (NA) in 6 Hz-induced psychomotor seizures in Swiss albino mice using N-2-Chloroethyl-N-ethyl-2-bromobenzylamine hydrochloride (DSP-4), a well-known depletor of NA. The vehicle and DSP-4 treated mice were given 6 Hz stimulation. A sham treatment was utilized as a comparator and sodium valproate (SVP) was utilized as a reference anti-epileptic medication...
August 8, 2018: Brain Research Bulletin
Thamara C Coutinho, Mayerlenis J Rojas, Paulo W Tardioli, Elaine C Paris, Cristiane S Farinas
β-Glucosidase is an enzyme of great industrial interest that is used in biorefineries and in the pharmaceutical, food, and beverage sectors, among others. These industrial processes would benefit from the use of immobilized enzyme systems that allow several reuses of the enzyme. A promising inorganic and nontoxic material for such application is hydroxyapatite (HA), which can be synthesized at nanometric scale, hence providing good accessibility of the substrate to the catalyst. Here, we carried out a systematic study to evaluate the feasibility of immobilizing β-glucosidase on HA nanoparticles...
August 8, 2018: International Journal of Biological Macromolecules
Patricia Rivera, María Del Mar Fernández-Arjona, Daniel Silva-Peña, Eduardo Blanco, Antonio Vargas, María Dolores López-Ávalos, Jesús M Grondona, Antonia Serrano, Francisco Javier Pavón, Fernando Rodríguez de Fonseca, Juan Suárez
Changes in endogenous cannabinoid homeostasis are associated with both ethanol-related neuroinflammation and memory decline. Extensive research is still required to unveil the role of endocannabinoid signaling activation on hippocampal microglial cells after ethanol exposure. Either microglial morphology, phenotype and recruitment may become notably altered after chronic alcohol-related neurodegeneration. Here, we evaluated the pharmacological effects of fatty-acid amide-hydrolase (FAAH) inhibitor URB597 (0...
August 8, 2018: Biochemical Pharmacology
Rose Cairns, Andrea L Schaffer, Nicole Ryan, Sallie-Anne Pearson, Nicholas A Buckley
BACKGROUND AND AIMS: Pregabalin is a gamma-aminobutyric acid (GABA) analogue, used to treat neuropathic pain and epilepsy. Pregabalin was registered in Australia in 2005, and publically subsidised in 2013. We aimed to describe Australian patterns of pregabalin use and intentional poisoning, and identify people potentially at high risk of misuse. DESIGN AND SETTING: Population-based retrospective cohort study of dispensings in the 10% sample of Australian Pharmaceutical Benefits Scheme (July 2012-February 2017); intentional poisoning calls to New South Wales Poisons Information Centre (NSWPIC) (2004-2016); intentional poisonings in two Australian toxicology service databases; poisoning fatalities in NSW coronial records (2005-2016)...
August 11, 2018: Addiction
François Montastruc, Justine Benevent, Vanessa Rousseau, Geneviève Durrieu, Agnès Sommet, Jean-Louis Montastruc
In contrast to statins, the risk of diabetes with fibrates was not clearly studied. The present study investigates a putative signal of diabetes associated with the use of fibrates using the World Health Organization (WHO) global individual case safety reports database, VigiBase® . We included all reports registered until the 31st December 2017 in VigiBase® to measure the risk of reporting "hyperglycemia or new onset of diabetes" (SMQ term) compared with all other reports [as a Reporting Odds Ratio (ROR 95%CI)] for fibrates, statins and the combination fibrates + statins...
August 11, 2018: Fundamental & Clinical Pharmacology
Min-Ho Shin, Gi-Won Song, Sung-Gyu Lee, Shin Hwang, Ki-Hun Kim, Chul-Soo Ahn, Deok-Bog Moon, Tae-Yong Ha, Dong-Hwan Jung, Gil-Chun Park, Young-In Yun, Wan-Jun Kim, Woo-Hyoung Kang, Seok-Hwan Kim, Hongsi Jiang, Sungmin Lee, Eun-Young Tak
Randomized, open-label, comparative, single-center, Phase 4, 24-week study comparing pharmacokinetics (PK), safety, and efficacy of once-daily, prolonged-release tacrolimus (PR-T) with twice-daily, immediate-release tacrolimus (IR-T) in adult de novo living-donor liver transplant (LDLT) recipients in Korea. All patients received intravenous tacrolimus from Day 0 (transplantation) for 4 days and were randomized (1:1) to receive oral PR-T or IR-T from Day 5. PK profiles taken on Days 6 and 21. Primary endpoint: area-under-the-concentration-time curve over 24h (AUC0-24 )...
August 11, 2018: Clinical Transplantation
Sofie Deleu, Thomas N Kakuda, Kurt Spittaels, Jurgen J Vercauteren, Vera Hillewaert, Amy Lwin, Lorant Leopold, Richard M W Hoetelmans
AIM: Evaluate the drug-drug interaction between pimodivir, a novel, non-nucleoside polymerase basic protein 2 (PB2) subunit inhibitor of the influenza A virus polymerase complex, and oseltamivir, to assess the feasibility of this combination therapy. Furthermore, single- and multiple-dose pharmacokinetics and safety of pimodivir in healthy volunteers were assessed. METHODS: In Part 1 of this open-label phase 1 study, healthy volunteers (n=18) were randomized to 1 of 6 cross-over treatment sequences, each comprising of oseltamivir 75-mg or pimodivir 600-mg or combination administered twice-daily on days 1-4, followed by a single morning dose on day 5...
August 11, 2018: British Journal of Clinical Pharmacology
Andrew Young Chang, Mariam Askari, Jun Fan, Paul A Heidenreich, P Michael Ho, Kenneth W Mahaffey, Aditya Jathin Ullal, Alexander Carroll Perino, Mintu Pravin Turakhia
BACKGROUND: Atrial fibrillation (AF) is treated by many types of physician specialists, including primary care physicians (PCPs). Health plans have different policies for how patients encounter these providers, and these may affect selection of AF treatment strategy. HYPOTHESIS: We hypothesized that healthcare plans with PCP-gatekeeping to specialist access may be associated with different pharmacologic treatments for AF. METHODS: We performed a retrospective cohort study using a commercial pharmaceutical claims database...
August 11, 2018: Clinical Cardiology
Otavio Berwanger, Magdy Abdelhamid, Thomas Alexander, Abdulmajeed Alzubaidi, Oleg Averkov, Philip Aylward, Eduardo Contreras Zúñiga, Sigrun Halvorsen, Ricardo Iglesias, Muhamad A Sk Abdul Kader, Mohammad Zubaid, Khalid F AlHabib
Primary percutaneous coronary intervention (PCI) is the preferred reperfusion method in patients with ST-segment elevation myocardial infarction (STEMI). In patients with STEMI who cannot undergo timely primary PCI, pharmacoinvasive treatment is recommended, comprising immediate fibrinolytic therapy with subsequent coronary angiography and rescue PCI if needed. Improving clinical outcomes following fibrinolysis remains of great importance for the many patients globally for whom rapid treatment with primary PCI is not possible...
August 11, 2018: Clinical Cardiology
Zhen Li, Tongli Zheng, Miao Li, Xiang Liu
The effluents of wastewater treatment plants (WWTPs) are the important sources for pollutants. These pollutants may entry into surface water, groundwater, and soil by recharging and irrigation then pose risk to human beings. Using reports from the past 20 years (n = 58), we conducted this review of organic contaminants (OCs) in the effluent of Chinese WWTPs. All the studies were during 2005 to 2017 and more than two papers were conducted in every year. Nineteen provinces (20 cities) were covered and most of the studies were located in the eastern part of China, especially the most developed and highest density of population areas...
August 10, 2018: Environmental Science and Pollution Research International
Nicole Berndt, Ralf Bergmann, Michael Bachmann
Protein-based preparations for biomedical research, and radiolabeled pharmaceuticals for nuclear medical diagnostics and therapy require highest chemical, radiochemical, and in particular protein purity. For detection of contaminations most commonly size exclusion high-performance liquid chromatography and polyacrylamide gel analysis in combination with silver staining is used. Here we describe a by far more sensitive radiolabeling method for the detection of traces of contaminating proteins.
2018: Methods in Molecular Biology
Adrian Wagg
Overactive bladder (OAB) is a common, troublesome condition affecting the lives of many older people. When pharmacotherapy is considered, antimuscarinics remain the mainstay for treatment. Bladder antimuscarinics are effective in the relief of symptoms for OAB and treatment leads to significant improvements in quality of life for those with the condition. However, many older people (> 65 years) with OAB are in later life (> 75 years) and a proportion of these will either be medically complex, with multiple comorbid conditions, or frail...
August 10, 2018: Drugs & Aging
Henry J Woodford
Urinary incontinence (UI) is a common and disabling problem among older people. Anticholinergic drugs (ADs) are a pharmacological option recommended for overactive bladder or mixed UI when non-pharmacological approaches have failed. However, UI is a more prevalent and complex condition in frail older people and to simply assume that AD actions are the same across all age groups would be wrong. This article reviews evidence for the efficacy and safety of these drugs, especially when prescribed for frail older people...
August 10, 2018: Drugs & Aging
Valentina Shakhnovich, P Brian Smith, Jeffrey T Guptill, Laura P James, David N Collier, Huali Wu, Chad E Livingston, Jian Zhao, Gregory L Kearns, Michael Cohen-Wolkowiez
BACKGROUND AND AIMS: Pharmacokinetic data for proton pump inhibitors (PPIs), acid-suppression drugs commonly prescribed to children, are lacking for obese children who are at greatest risk for acid-related disease. In a recent multi-center investigation, we demonstrated decreased, total body weight adjusted, apparent clearance (CL/F) of the PPI pantoprazole for obese children compared with their non-obese peers. Subsequently, we developed a population-based pharmacokinetic (PopPK) model to characterize pantoprazole disposition and evaluated appropriate pantoprazole dosing strategies for obese pediatric patients, using simulation...
August 11, 2018: Paediatric Drugs
Dan-Dan Xiong, Yue Qin, Wen-Qing Xu, Rong-Quan He, Hua-Yu Wu, Dan-Min Wei, Jing-Jing Zeng, Yi-Wu Dang, Gang Chen
BACKGROUND AND OBJECTIVES: Pharmacological control against ovarian serous cystadenocarcinoma has received increasing attention. The purpose of this study was to investigate multi-drug treatments as synergetic therapy for ovarian serous cystadenocarcinoma and to explore their mechanisms of action by the network pharmacology method. METHODS: Genes acting on ovarian serous cystadenocarcinoma were first collected from GEPIA and DisGeNET. Gene Ontology annotation, Kyoto Encyclopedia of Genes and Genomes pathway, Reactome pathway, and Disease Ontology analyses were then conducted...
August 10, 2018: Clinical Drug Investigation
Sherwin K B Sy, Luning Zhuang, Serubbabel Sy, Hartmut Derendorf
Avibactam is a non-β-lactam, β-lactamase inhibitor of the diazabicyclooctane class that covalently acylates its β-lactamase targets, encompassing extended spectrum of activities that cover serine β-lactamases but not metallo-β-lactamases. Ceftazidime and avibactam have complementary pharmacokinetic (PK) profiles. Both drugs have a half-life of approximately 2 h, making them suitable to be combined in a fixed-dose combination ratio of 4:1 (ceftazidime:avibactam). Renal clearance is the primary elimination pathway of both ceftazidime and avibactam, and dose adjustment is required in patients with moderate and severe renal impairment...
August 11, 2018: Clinical Pharmacokinetics
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