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Pharmacodynamics

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https://www.readbyqxmd.com/read/28813419/vaccine-driven-pharmacodynamic-dissection-and-mitigation-of-fenethylline-psychoactivity
#1
Cody J Wenthur, Bin Zhou, Kim D Janda
Fenethylline, also known by the trade name Captagon, is a synthetic psychoactive stimulant that has recently been linked to a substance-use disorder and 'pharmacoterrorism' in the Middle East. Although fenethylline shares a common phenethylamine core with other amphetamine-type stimulants, it also incorporates a covalently linked xanthine moiety into its parent structure. These independently active pharmacophores are liberated during metabolism, resulting in the release of a structurally diverse chemical mixture into the central nervous system...
August 16, 2017: Nature
https://www.readbyqxmd.com/read/28812389/evolocumab-for-the-treatment-of-hypercholesterolemia
#2
Brian Tomlinson, Miao Hu, Yuzhen Zhang, Paul Chan, Zhong-Min Liu
Evolocumab is a fully human monoclonal immunoglobulin G2 directed against human proprotein convertase subtilisin/kexin type 9 (PCSK9). It is administered by subcutaneous injection every 2 weeks or once monthly. Area covered: Herein, the authors discuss the rationale for inhibiting PCSK9 and describe the pharmacodynamics, pharmacokinetics and clinical trials with evolocumab. Evolocumab reduces low density lipoprotein cholesterol (LDL-C) levels by 50 to 60% in most patients with and without background treatment with statins or other lipid lowering agents...
August 16, 2017: Expert Opinion on Biological Therapy
https://www.readbyqxmd.com/read/28811827/pharmacodynamics-and-medicinal-chemistry-of-an-external-chinese-herbal-formula-for-mammary-precancerous-lesions
#3
Ruixue Chen, Guijuan Zhang, Yi Ma, Fengjie Bie, Hongxia Fan, Min Ma
Ruyan Neixiao Cream (RYNXC) is a traditional Chinese herbal formula for treating mammary precancerous disease. This study was carried out to investigate in vivo anticancer effect of RYNXC and multiple constituents. 32 virginal Sprague-Dawley rats were randomly divided into blank control group (BC), mammary precancer models group (MODEL), tamoxifen group (TAM), and Ruyan Neixiao Cream group (RYNXC). TAM was intervened by tamoxifen; RYNXC was intervened by Ruyan Neixiao Cream. The chromatographic separation was performed by high performance liquid chromatography (HPLC) coupled with mass spectrometry (MS)...
2017: Evidence-based Complementary and Alternative Medicine: ECAM
https://www.readbyqxmd.com/read/28811125/pharmacokinetics-and-pharmacodynamics-of-thiopurines-in-an-in-vitro-model-of-human-hepatocytes-insights-from-an-innovative-mass-spectrometry-assay
#4
Marco Pelin, Elena Genova, Laura Fusco, Monzer Marisat, Ute Hofmann, Diego Favretto, Marianna Lucafò, Andrea Taddio, Stefano Martelossi, Alessandro Ventura, Gabriele Stocco, Matthias Schwab, Giuliana Decorti
AIM: To apply an innovative LC-MS/MS method to quantify thiopurine metabolites in human hepatocytes and to associate them to cytotoxicity. METHODS: Immortalized human hepatocytes (IHH cells) were treated for 48 and 96 h, with 1.4 × 10(-4) M azathioprine and 1.1 × 10(-3) M mercaptopurine, concentrations corresponding to the IC50 values calculated after 96 h exposure in previous cytotoxicity analysis. After treatments, cells were collected for LC-MS/MS analysis to quantify 11 thiopurine metabolites with different level of phosphorylation and viable cells were counted by Trypan blue exclusion assay to determine thiopurines in vitro effect on cell growth and survival...
August 12, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28811111/cell-cultures-in-drug-discovery-and-development-the-need-of-reliable-in-vitro-in-vivo-extrapolation-for-pharmacodynamics-and-pharmacokinetics-assessment
#5
REVIEW
Karol Jaroch, Alina Jaroch, Barbara Bojko
For ethical and cost-related reasons, use of animals for the assessment of mode of action, metabolism and/or toxicity of new drug candidates has been increasingly scrutinized in research and industrial applications. Implementation of the 3 "Rs"(1); rule (Reduction, Replacement, Refinement) through development of in silico or in vitro assays has become an essential element of risk assessment. Physiologically based pharmacokinetic (PBPK(2)) modeling is the most potent in silico tool used for extrapolation of pharmacokinetic parameters to animal or human models from results obtained in vitro...
July 27, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28810520/studies-on-the-regulation-of-lipid-metabolism-and-the-mechanism-of-the-aqueous-and-ethanol-extracts-of-usnea
#6
Jiali Zhu, Xuemei Zhang, Xiu Chen, Yong Sun, Yaolan Dai, Chang Chen, Tiane Zhang, Zhiyong Yan
OBJECTIVES: Usnea is a lichen of Usnea diffracta Vain and Usnea longissima Ach, which belongs to the genus Usnea Adans of Usneaceae. Usnea exerts numerous pharmacological activities, while its lipid regulatory activities remain unreported. This study aims to evaluate the effects of aqueous and ethanol extracts of Usnea on the regulation of lipid metabolism and to explore the possible mechanism. METHODS: Hyperlipidemia rat model was established by feeding with high-fat diet for 45days...
August 10, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28809448/improved-pharmacokinetic-and-pharmacodynamic-attributes-of-artemether-lumefantrine-loaded-solid-smedds-for-oral-administration
#7
Sameer Bhandari, Vikram Bhandari, Jatin Sood, Sunil Jaswal, Vikas Rana, Neena Bedi, Rakesh Sehgal, Ashok K Tiwary
OBJECTIVES: To evaluate the in-vivo efficacy of solid SMEDDS containing combination of artemether and lumefantrine. METHODS: Formulation development of solid SMEDDS containing combination of artemether and lumefantrine was carried out using spray drying technique. These S-SMEDDS were evaluated for reduction in parasitemia and mortality as well as subacute toxicity in mice. Haematology, biochemical parameters and histopathology were performed for evaluating safety of formulation...
August 15, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28808915/cost-effectiveness-of-posaconazole-tablets-for-invasive-fungal-infections-prevention-in-acute-myelogenous-leukemia-or-myelodysplastic-syndrome-patients-in-spain
#8
Rafael Cámara, Irmina Gozalbo, Manuel Jurado, Jaime Sanz, Belén Aragón, Santiago Grau
INTRODUCTION: Posaconazole is superior to fluconazole (FLU) and itraconazole (ITRA) in the prevention of invasive fungal diseases (IFDs) in neutropenic patients with acute myelogenous leukemia (AML) and myelodysplastic syndrome (MDS). A new tablet formulation of posaconazole with improved pharmacokinetic and pharmacodynamic properties compared to posaconazole oral solution has recently been approved. The objective of this study is to estimate the cost-effectiveness of the newly developed posaconazole tablets versus FLU oral suspension or ITRA oral solution for preventing IFDs in high-risk neutropenic patients with AML or MDS and from the perspective of the Spanish National Health System (NHS)...
August 14, 2017: Advances in Therapy
https://www.readbyqxmd.com/read/28808886/assessment-of-pharmacokinetic-interactions-between-obeticholic-acid-and-caffeine-midazolam-warfarin-dextromethorphan-omeprazole-rosuvastatin-and-digoxin-in-phase-1-studies-in-healthy-subjects
#9
Jeffrey E Edwards, Lise Eliot, Andrew Parkinson, Sharon Karan, Leigh MacConell
INTRODUCTION: Obeticholic acid (OCA), a potent and selective farnesoid X receptor agonist, is indicated for the treatment of primary biliary cholangitis (PBC). We investigated the potential drug-drug interaction effect of OCA on metabolic CYP450 enzymes and drug transporters. METHODS: Five phase 1 single-center, open-label, fixed-sequence, inpatient studies were conducted in healthy adult subjects to evaluate the effect of oral daily doses of 10 or 25 mg OCA on single-dose plasma pharmacokinetics of specific probe substrates for enzymes CYP1A2 (caffeine, R-warfarin), CYP3A (midazolam, R-warfarin), CYP2C9 (S-warfarin), CYP2D6 (dextromethorphan), CYP2C19 (omeprazole), and drug transporters, BCRP/OATP1B1/OATP1B3 (rosuvastatin), and P-gp (digoxin)...
August 14, 2017: Advances in Therapy
https://www.readbyqxmd.com/read/28808833/long-acting-ionically-paired-embonate-based-nanocrystals-of-donepezil-for-the-treatment-of-alzheimer-s-disease-a-proof-of-concept-study
#10
Naresh Mittapelly, Maharshi Thalla, Gitu Pandey, Venkatesh Teja Banala, Shweta Sharma, Abhishek Arya, Sandeep Mishra, Kalyan Mitra, Shubha Shukla, Prabhat Ranjan Mishra
PURPOSE: The aim of the present study was to prepare a patient friendly long acting donepezil (D) nanocrystals (NCs) formulation, with a high payload for i.m administration. As the native D hydrochloride salt has high aqueous solubility it is necessary to increase its hydrophobicity prior to the NCs formation. METHODS: D was ionically paired with embonic acid (E) in aqueous media and was successfully characterized using techniques like DSC, PXRD, FT-IR, NMR etc...
August 14, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28807911/systematic-review-and-meta-analyses-of-the-effect-of-chemotherapy-on-pulmonary-mycobacterium-abscessus-outcomes-and-disease-recurrence
#11
Jotam G Pasipanodya, Deborah Ogbonna, Beatriz E Ferro, Gesham Magombedze, Shashikant Srivastava, Devyani Deshpande, Tawanda Gumbo
Background. In pharmacokinetic/pharmacodynamics models of pulmonary Mycobacterium abscessus complex, the recommended macrolide-containing combination therapy has poor kill rates. However, clinical outcomes are unknown.Methods We searched the literature for studies published between 1990-2017 that reported microbial outcomes in patients treated for pulmonary M. abscessus disease. Good outcome was defined as sustained sputum culture conversion (SSCC) without relapse. Random effects models were used to pool studies and estimate proportions of patients with good outcomes...
August 14, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28807910/24-hour-pharmacokinetic-relationships-for-vancomycin-and-novel-urinary-biomarkers-of-acute-kidney-injury
#12
J Nicholas O'Donnell, Nathaniel J Rhodes, Thomas P Lodise, Walter C Prozialeck, Cristina M Miglis, Medha Joshi, Natarajan Venkatesan, Gwendolyn Pais, Cameron Cluff, Peter C Lamar, Seema Briyal, John Z Day, Anil Gulati, Marc H Scheetz
Introduction: Vancomycin has been associated with acute kidney injury in preclinical and clinical settings, however the precise exposure profiles associated with vancomycin induced acute kidney injury has not been defined. We sought to determine pharmacokinetic/pharmacodynamics indices associated with the development of acute kidney injury using sensitive urinary biomarkers.Methods: Male Sprague-Dawley rats received clinical grade vancomycin or normal saline as an intraperitoneal injection. Total daily doses between 0 and 400 mg/kg/day were administered as single or 2 divided doses over a 24-hour period...
August 14, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28807904/no-clinically-relevant-drug-drug-interactions-between-methadone-or-buprenorphine-naloxone-and-anti-viral-combination-glecaprevir-and-pibrentasvir
#13
Matthew Kosloski, Weihan Zhao, Armen Asatryan, Jens Kort, Pierre Geoffroy, Wei Liu
The combination of glecaprevir (formerly ABT-493), a nonstructural (NS) protein 3/4A protease inhibitor, and pibrentasvir (formerly ABT-530), a NS5A protein inhibitor, is being developed as treatment for HCV genotype 1-6 infection. The pharmacokinetics, pharmacodynamics, safety, and tolerability of methadone or buprenorphine/naloxone when coadministered with the glecaprevir and pibrentasvir combination in HCV-negative subjects on stable opioid maintenance therapy were investigated in a Phase 1, single-center, two-arm, multiple-dose, open-label sequential study...
August 14, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28807873/neurophysiologically-informed-markers-of-individual-variability-and-pharmacological-manipulation-of-human-cortical-gamma
#14
A D Shaw, R J Moran, S D Muthukumaraswamy, J Brealy, D E Linden, K J Friston, K D Singh
The ability to quantify synaptic function at the level of cortical microcircuits from non-invasive data would be enormously useful in the study of neuronal processing in humans and the pathophysiology that attends many neuropsychiatric disorders. Here, we provide proof of principle that one can estimate inter-and intra-laminar interactions among specific neuronal populations using induced gamma responses in the visual cortex of human subjects - using dynamic causal modelling based upon the canonical microcircuit (CMC; a simplistic model of a cortical column)...
August 11, 2017: NeuroImage
https://www.readbyqxmd.com/read/28807643/-use-of-subcutaneous-route-for-comfort-care%C3%A2-in-neonatal-palliative-population-systematic-review-and-survey-of-practices-in-france
#15
N Pouvreau, J Tandonnet, O Tandonnet, L Renesme
INTRODUCTION: Subcutaneous hydration (hypodermoclysis) and drug administration is a widely used method of analgesic therapy in adult palliative care medicine. Very little is known about its use in neonatal medicine. Evidence-based guidelines do not exist due to a lack of data. In this study, the advantages of subcutaneous analgesic therapy in terms of comfort in neonatal palliative care situations were investigated. METHODS: This report details the results of a systematic review associated with a survey in neonatal intensive care units (NICUs) and pediatric palliative care departments (PPCTs) in France...
August 11, 2017: Archives de Pédiatrie: Organe Officiel de la Sociéte Française de Pédiatrie
https://www.readbyqxmd.com/read/28807159/herb-drug-interactions-of-commonly-used-chinese-medicinal-herbs
#16
Amrinder Singh, Kaicun Zhao
With more and more popular use of traditional herbal medicines, in particular Chinese herbal medicines, herb-drug interactions have become a more and more important safety issue in the clinical applications of the conventional drugs. Researches in this area are increasing very rapidly. Herb-drug interactions are complicated due to the fact that multiple chemical components are involved, and these compounds may possess diverse pharmacological activities. Interactions can be in both pharmacokinetics and pharmacodynamics...
2017: International Review of Neurobiology
https://www.readbyqxmd.com/read/28807037/selepressin-a-novel-selective-vasopressin-v1a-agonist-is-an-effective-substitute-for-norepinephrine-in-a-phase-iia-randomized-placebo-controlled-trial-in-septic-shock-patients
#17
James A Russell, Jean-Louis Vincent, Anne Louise Kjølbye, Håkan Olsson, Allan Blemings, Herbert Spapen, Peder Carl, Pierre-Francois Laterre, Lars Grundemar
BACKGROUND: Vasopressin is widely used for vasopressor support in septic shock patients, but experimental evidence suggests that selective V1A agonists are superior. The initial pharmacodynamic effects, pharmacokinetics, and safety of selepressin, a novel V1A-selective vasopressin analogue, was examined in a phase IIa trial in septic shock patients. METHODS: This was a randomized, double-blind, placebo-controlled multicenter trial in 53 patients in early septic shock (aged ≥18 years, fluid resuscitation, requiring vasopressor support) who received selepressin 1...
August 15, 2017: Critical Care: the Official Journal of the Critical Care Forum
https://www.readbyqxmd.com/read/28806782/the-use-of-18f-fluoro-deoxy-glucose-positron-emission-tomography-18f-fdg-pet-as-a-non-invasive-pharmacodynamic-biomarker-to-determine-the-minimally-pharmacologically-active-dose-of-azd8835-a-novel-pi3k%C3%AE-inhibitor
#18
Juliana Maynard, Sally-Ann Emmas, Francois-Xavier Ble, Herve Barjat, Emily Lawrie, Urs Hancox, Urszula M Polanska, Alison Pritchard, Kevin Hudson
BACKGROUND: The phosphatidyl inositol 3 kinase (PI3K), AKT and mammalian target of rapamycin (mTOR) signal transduction pathway is frequently de-regulated and activated in human cancer and is an important therapeutic target. AZD8835 is a PI3K inhibitor, with selectivity against PI3K α and δ isoforms, which is currently in Phase 1 clinical trials. 18F-Fluoro-deoxy-glucose positron emission tomography (18F-FDG PET) is a non-invasive pharmacodynamic imaging biomarker that has become an integral part of drug development...
2017: PloS One
https://www.readbyqxmd.com/read/28806704/chiral-pharmaceuticals-a-review-on-their-environmental-occurrence-and-fate-processes
#19
REVIEW
Edmond Sanganyado, Zhijiang Lu, Qiuguo Fu, Daniel Schlenk, Jay Gan
More than 50% of pharmaceuticals in current use are chiral compounds. Enantiomers of the same pharmaceutical have identical physicochemical properties, but may exhibit differences in pharmacokinetics, pharmacodynamics and toxicity. The advancement in separation and detection methods has made it possible to analyze trace amounts of chiral compounds in environmental media. As a result, interest on chiral analysis and evaluation of stereoselectivity in environmental occurrence, phase distribution and degradation of chiral pharmaceuticals has grown substantially in recent years...
August 5, 2017: Water Research
https://www.readbyqxmd.com/read/28805299/dissociation-between-the-pharmacokinetics-and-pharmacodynamics-of-once-daily-rivaroxaban-and-twice-daily-apixaban-a-randomized-crossover-study
#20
Reinhold Kreutz, Pontus B Persson, Dagmar Kubitza, Kirstin Thelen, Stefan Heitmeier, Stephan Schwers, Michael Becka, Melanie Hemmrich
BACKGROUND: The anticoagulant actions of the oral direct factor Xa inhibitors, rivaroxaban and apixaban, have not previously been directly compared. OBJECTIVES: To compare directly the steady-state pharmacokinetics and anticoagulant effects of rivaroxaban and apixaban at doses approved for stroke prevention in nonvalvular atrial fibrillation. METHODS: Twenty-four healthy Caucasian male volunteers were included in this open-label, two-period crossover, phase 1 study (EudraCT number: 2015-002612-32)...
August 14, 2017: Journal of Thrombosis and Haemostasis: JTH
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