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Pharmacodynamic

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https://www.readbyqxmd.com/read/29782406/population-pharmacokinetics-and-pharmacodynamics-of-dexmedetomidine-in-children-undergoing-ambulatory-surgery
#1
María-Gabriela Pérez-Guillé, Alejandra Toledo-López, Liliana Rivera-Espinosa, Radames Alemon-Medina, Chiharu Murata, Ismael Lares-Asseff, Juan Luis Chávez-Pacheco, Josefina Gómez-Garduño, Ana-Lilia Zamora Gutiérrez, Claudia Orozco-Galicia, Karina Ramírez-Morales, Gustavo Lugo-Goytia
BACKGROUND: Dexmedetomidine (DEX) is an α-2 adrenergic agonist with sedative and analgesic properties. Although not approved for pediatric use by the Food and Drug Administration, DEX is increasingly used in pediatric anesthesia and critical care. However, very limited information is available regarding the pharmacokinetics of DEX in children. The aim of this study was to investigate DEX pharmacokinetics and pharmacodynamics (PK-PD) in Mexican children 2-18 years of age who were undergoing outpatient surgical procedures...
May 17, 2018: Anesthesia and Analgesia
https://www.readbyqxmd.com/read/29782261/-chronic-kidney-disease-as-basis-of-high-thrombotic-and-bleeding-risk-in-patients-with-atrial-fibrillation-place-of-oral-anticoagulants
#2
A G Obrezan, A Y Zemchenkov
Chronic kidney disease (CKD) aggravates course of practically all diseases by worsening outcomes and hindering adequate treatment. Specificities of renal excretion of various drugs, changes of parameters of their pharmacokinetics and pharmacodynamics, nephrotoxic effects of drugs, tactics of drug therapy in conditions of CKD, terminal stage of kidney failure and dialysis are in the focus of attention of internists. To a greatest degree difficulties of drug therapy in CKD and associated clinical states refer to the group of anticoagulants...
April 2018: Kardiologiia
https://www.readbyqxmd.com/read/29780866/molecular-imaging-what-is-right-and-what-is-an-illusion
#3
William E Klunk
Over the past 40 years, brain molecular imaging has evolved from measuring cerebral metabolism with fluorodeoxyglucose, to neuroreceptor imaging, to imaging pathological protein deposits. In the early going, the characteristics of successful molecular imaging radiotracers were defined, and a detailed "Process" was developed for the collection of basic pharmacodynamic and pharmacokinetic data. These data are essential for the interpretation of in vivo imaging data and for defining the strengths, weaknesses, and limitations of new tracers...
2018: Alzheimer's & Dementia: Diagnosis, Assessment & Disease Monitoring
https://www.readbyqxmd.com/read/29780587/development-of-a-vancomycin-dosing-approach-for-critically-ill-patients-receiving-hybrid-hemodialysis-using-monte-carlo-simulation
#4
Susan J Lewis, Bruce A Mueller
Objectives: Prolonged intermittent renal replacement therapy is an increasingly popular treatment for acute kidney injury in critically ill patients that runs at different flow rates and durations than conventional hemodialysis or continuous renal replacement therapies. Pharmacokinetic studies conducted in patients receiving prolonged intermittent renal replacement therapy are scarce; consequently, clinicians are challenged to dose antibiotics effectively. The purpose of this study was to develop vancomycin dosing recommendations for patients receiving prolonged intermittent renal replacement therapy...
2018: SAGE Open Medicine
https://www.readbyqxmd.com/read/29779975/design-and-synthesis-of-a-series-of-bioavailable-fatty-acid-synthase-fasn-kr-domain-inhibitors-for-cancer-therapy
#5
Tianbao Lu, Carsten Schubert, Maxwell D Cummings, Gilles Bignan, Peter J Connolly, Karine Smans, Donald Ludovici, Michael H Parker, Christophe Meyer, Christian Rocaboy, Richard Alexander, Bruce Grasberger, Sabine De Breucker, Norbert Esser, Erwin Fraiponts, Ron Gilissen, Boudewijn Janssens, Danielle Peeters, Luc Van Nuffel, Peter Vermeulen, James Bischoff, Lieven Meerpoel
We designed and synthesized a new series of fatty acid synthase (FASN) inhibitors with potential utility for the treatment of cancer. Extensive SAR studies led to highly active FASN inhibitors with good cellular activity and oral bioavailability, exemplified by compound 34. Compound 34 is a potent inhibitor of human FASN (IC50  = 28 nM) that effectively inhibits proliferation of A2780 ovarian cells (IC50  = 13 nM) in lipid-reduced serum (LRS). This cellular activity can be rescued by addition of palmitate, consistent with an on-target effect...
May 8, 2018: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29779485/tgn-1412-and-bia-2474-trials-with-tragic-end-lessons-learnt-to-make-clinical-trials-safer
#6
Rimple Jeet Kaur, Surjit Singh, Preeti Sidhu, Pramod Kumar Sharma
BACKGROUND: Globally, there have been tremendous efforts by regulatory authorities to make clinical trials safer by making stringent clinical trial regulations. Despite this, we witnessed several tragic events. TGN1412 and BIA 10-2474 phase I trials are infamous trails in which healthy volunteers either succumbed to severe adverse effects or faced irreversible impairments of the test drug. Such afflictions in clinical trials are not only turbulent to the image of pharmaceutical industry but it also conveys dispiriting message for clinical trial participants...
May 20, 2018: Reviews on Recent Clinical Trials
https://www.readbyqxmd.com/read/29779330/-tolerance-and-pharmacodynamics-phase-%C3%A2-clinical-trial-study-of-chimeric-anti-cd20-monoclonal-antibody-ibi301-in-chinese-patients-with-cd20-positive-non-hodgkin-s-lymphoma
#7
B Jiang, J Y Qi, M Y Sun, Z J Li, W Liu, L J Liu, F K Zhang, L G Qiu
Objective: To evaluate the tolerance and safety of a human-mouse chimeric anti-CD20 monoclonal antibody IBI301 in Chinese patients achieved objective response with CD20(+) B-cell non-Hodgkin's lymphoma (NHL). Methods: Nine patients with CD20(+) B-cell NHL received dose-escalating IBI301 infusions (250 mg/m(2), n =3; 375 mg/m(2), n =3; 500 mg/m(2), n =3, respectively). The data of all patients were collected for safety analyses. The median exposures of 125 mg/m(2), 375 mg/m(2), 500 mg/m(2) dose groups were 243, 690 and 980 mg, respectively...
April 14, 2018: Zhonghua Xue Ye Xue za Zhi, Zhonghua Xueyexue Zazhi
https://www.readbyqxmd.com/read/29778180/pharmacokinetic-pharmacodynamic-assessment-of-cefquinome-against-actinobacillus-pleuropneumoniae-in-a-piglet-tissue-cage-infection-model
#8
Longfei Zhang, Xun Wu, Zilong Huang, Nan Zhang, Yuzhi Wu, Qinren Cai, Xiangguang Shen, Huanzhong Ding
To evaluate the relationship between the pharmacokinetic/pharmacodynamic (PK/PD) parameters and the antibacterial effect of cefquinome against Actinobacillus pleuropneumoniae, a tissue cage infection model was established in piglets. In this model, an initial count of A. pleuropneumoniae of approximately 106 CFU/mL was exposed to different concentrations of cefquinome after multiple administration at dosages of 0.2, 0.4, 0.8, 1, 2, 4 mg/kg body weight once a day for 3 days. Concentration of cefquinome and bacterial numbers of A...
June 2018: Veterinary Microbiology
https://www.readbyqxmd.com/read/29777683/probing-the-binding-site-of-novel-selective-positive-allosteric-modulators-at-the-m-1-machr
#9
Elham Khajehali, Celine Valant, Manuela Jörg, Andrew B Tobin, P Jeffrey Conn, Craig W Lindsley, Patrick M Sexton, Peter J Scammells, Arthur Christopoulos
Subtype-selective allosteric modulation of the M1 muscarinic acetylcholine (ACh) receptor (M1 mAChR) is an attractive approach for the treatment of numerous disorders, including cognitive deficits. The discovery of benzyl quinolone carboxylic acid, BQCA, a selective M1 mAChR positive allosteric modulator (PAM), spurred the subsequent development of newer generation M1 PAMs representing diverse chemical scaffolds, different pharmacodynamic properties and, in some instances, improved pharmacokinetics. Key exemplar molecules from such efforts include PF-06767832 (N-((3R,4S)-3-hydroxytetrahydro-2H-pyran-4-yl)-5-methyl-4-(4-(thiazol-4-yl)benzyl)pyridine-2-carboxamide), VU6004256 (4,6-difluoro-N-(1S,2S)-2-hydroxycyclohexyl-1-((6-(1-methyl-1H-pyrazol-4-yl)pyridine-3-yl)methyl)-1H-indole-3-carboxamide) and MIPS1780 (3-(2-hydroxycyclohexyl)-6-(2-((4-(1-methyl-1H-pyrazol-4-yl)-benzyl)oxy)phenyl)pyrimidin-4(3H)-one)...
May 16, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/29777528/state-of-the-art-review-on-physiologically-based-pharmacokinetic-modeling-in-pediatric-drug-development
#10
REVIEW
Venkata Yellepeddi, Joseph Rower, Xiaoxi Liu, Shaun Kumar, Jahidur Rashid, Catherine M T Sherwin
Physiologically based pharmacokinetic modeling and simulation is an important tool for predicting the pharmacokinetics, pharmacodynamics, and safety of drugs in pediatrics. Physiologically based pharmacokinetic modeling is applied in pediatric drug development for first-time-in-pediatric dose selection, simulation-based trial design, correlation with target organ toxicities, risk assessment by investigating possible drug-drug interactions, real-time assessment of pharmacokinetic-safety relationships, and assessment of non-systemic biodistribution targets...
May 18, 2018: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/29777407/modelling-the-delay-between-pharmacokinetics-and-eeg-effects-of-morphine-in-rats-binding-kinetic-versus-effect-compartment-models
#11
Wilhelmus E A de Witte, Vivi Rottschäfer, Meindert Danhof, Piet H van der Graaf, Lambertus A Peletier, Elizabeth C M de Lange
Drug-target binding kinetics (as determined by association and dissociation rate constants, k on and k off ) can be an important determinant of the kinetics of drug action. However, the effect compartment model is used most frequently instead of a target binding model to describe hysteresis. Here we investigate when the drug-target binding model should be used in lieu of the effect compartment model. The utility of the effect compartment (EC), the target binding kinetics (TB) and the combined effect compartment-target binding kinetics (EC-TB) model were tested on either plasma (ECPL , TBPL and EC-TBPL ) or brain extracellular fluid (ECF) (ECECF , TBECF and EC-TBECF ) morphine concentrations and EEG amplitude in rats...
May 18, 2018: Journal of Pharmacokinetics and Pharmacodynamics
https://www.readbyqxmd.com/read/29776710/pharmacokinetics-pharmacodynamics-computer-decision-support-technologies-and-antimicrobial-stewardship-the-compass-and-rudder
#12
REVIEW
Robert C Owens, Catharine C Bulik, David R Andes
The first guidelines for conducting antimicrobial stewardship in the hospitalized setting were published in 2007. These guidelines recommend that stewardship programs employ the science of pharmacokinetics-pharmacodynamics (PK-PD) as well as adopting computerized decision support technologies when possible. The United States Food and Drug Administration have adopted PK-PD as a cornerstone in the evaluation of antimicrobial agents during clinical development. The core principles of PK-PD center around describing the relationship between drug exposure indexed to the susceptibility of the infecting bacterial pathogen and patient response...
April 13, 2018: Diagnostic Microbiology and Infectious Disease
https://www.readbyqxmd.com/read/29776017/pharmacokinetics-and-c-reactive-protein-modelling-of-anti-il-6-antibody-pf-04236921-in-healthy-volunteers-and-patients-with-autoimmune-disease
#13
Cheryl Li, Satoshi Shoji, Jean Beebe
AIMS: The purpose of this study was to characterize pharmacokinetics (PK) of PF-04236921, a novel anti-IL-6 monoclonal antibody, and its pharmacokinetics/pharmacodynamics (PK/PD) relationship on serum C-Reactive Protein (CRP) in healthy volunteers and patients with rheumatoid arthritis (RA), systemic lupus erythematosus (SLE), and Crohn's disease (CD) METHODS: Population modelling analyses were conducted using nonlinear mixed effects modelling. Data from 2 phase 1 healthy volunteer studies, a phase 1 RA study, a Phase 2 CD study, and a Phase 2 SLE study were included...
May 18, 2018: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29774062/-in-vivo-imaging-biomarkers-of-neuroinflammation-in-the-development-and-assessment-of-stroke-therapies-towards-clinical-translation
#14
REVIEW
Bastian Zinnhardt, Maximilian Wiesmann, Lisa Honold, Cristina Barca, Michael Schäfers, Amanda J Kiliaan, Andreas H Jacobs
Modulation of the inflammatory microenvironment after stroke opens a new avenue for the development of novel neurorestorative therapies in stroke. Understanding the spatio-temporal profile of (neuro-)inflammatory imaging biomarkers in detail thereby represents a crucial factor in the development and application of immunomodulatory therapies. The early integration of quantitative molecular imaging biomarkers in stroke drug development may provide key information about (i) early diagnosis and follow-up, (ii) spatio-temporal drug-target engagement (pharmacodynamic biomarker), (iii) differentiation of responders and non-responders in the patient cohort (inclusion/exclusion criteria; predictive biomarkers), and (iv) the mechanism of action...
2018: Theranostics
https://www.readbyqxmd.com/read/29774052/therapeutic-drug-monitoring-of-vedolizumab-in-inflammatory-bowel-disease-current-data-and-future-directions
#15
REVIEW
Mark G Ward, Miles P Sparrow, Xavier Roblin
The introduction of vedolizumab, a lymphocyte adhesion inhibitor, has expanded the relatively limited therapeutic armamentarium available for Crohn's disease and ulcerative colitis. Despite its effectiveness, both primary nonresponse and secondary loss of response to vedolizumab do occur, as is observed with the use of anti-tumour necrosis factor (TNF) therapy. Further, in a proportion, onset of efficacy may be relatively slow. A large body of data support an exposure-response relationship with anti-TNF drug levels, which has led to therapeutic drug monitoring becoming incorporated into everyday clinical management...
2018: Therapeutic Advances in Gastroenterology
https://www.readbyqxmd.com/read/29773891/assessing-the-feasibility-of-neutralizing-osteopontin-with-various-therapeutic-antibody-modalities
#16
Vahid Farrokhi, Jeffrey R Chabot, Hendrik Neubert, Zhiyong Yang
Osteopontin is a secreted glycophosphoprotein that is highly implicated in many physiological and pathological processes such as biomineralization, cell-mediated immunity, inflammation, fibrosis, cell survival, tumorigenesis and metastasis. Antibodies against osteopontin have been actively pursued as potential therapeutics for various diseases by pharmaceutical companies and academic laboratories. Many studies have demonstrated the efficacy of osteopontin inhibition in a variety of preclinical models of diseases such as rheumatoid arthritis, cancer, nonalcoholic steatohepatitis, but clinical utility has not yet been demonstrated...
May 17, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29773888/antitumor-effect-of-axitinib-combined-with-dopamine-and-pk-pd-modeling-in-the-treatment-of-human-breast-cancer-xenograft
#17
Yuan-Heng Ma, Si-Yuan Wang, Yu-Peng Ren, Jian Li, Ting-Jie Guo, Wei Lu, Tian-Yan Zhou
Rising evidence has shown the development of resistance to vascular endothelial growth factor receptor (VEGFR) inhibitors in the practices of cancer therapy. It is reported that the efficacy of axitinib (AX), a VEGFR inhibitor, is limited in the treatment of breast cancer as a single agent or in combination with other chemotherapeutic drugs due to the probability of rising population of cancer stem-like cells (CSCs) caused by AX. The present study evaluated the effect of dopamine (DA) improving AX's efficacy on MCF-7/ADR breast cancer in vitro and in vivo, and developed a pharmacokinetic-pharmacodynamic (PK-PD) model describing the in vivo experimental data and characterizing the interaction of effect between AX and DA...
May 17, 2018: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29773500/an-analysis-on-distribution-and-inter-relationships-of-biomarkers-under-rivaroxaban-in-japanese-patients-with-non-valvular-atrial-fibrillation-cvi-aro-1
#18
Shinya Suzuki, Takeshi Yamashita, Hidefumi Kasai, Takayuki Otsuka, Koichi Sagara
Prothrombin time (PT) has been widely used for measuring anticoagulation intensity under rivaroxaban therapy, but precise information has not been well established yet. Consecutive 96 non-valvular atrial fibrillation (NVAF) under rivaroxaban between Jan/June, 2015 were recruited. Serum concentration (SC) and PT with 5 representative reagents available in Japan (Neoplastin Plus®, Thromborel S®, Thrombocheck PT®, Thrombocheck PT Plus®, and Recombiplastin®) at 2-4 hours after (peak) and before intake of rivaroxaban (trough) were measured at outpatient clinic in the cardiovascular institute (CVI ARO study 1)...
March 15, 2018: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/29773381/cd44-targeted-hyaluronic-acid-curcumin-prodrug-protects-renal-tubular-epithelial-cell-survival-from-oxidative-stress-damage
#19
Jing-Bo Hu, Shu-Juan Li, Xu-Qi Kang, Jing Qi, Jia-Hui Wu, Xiao-Juan Wang, Xiao-Ling Xu, Xiao-Ying Ying, Sai-Ping Jiang, Jian You, Yong-Zhong Du
Based on the abnormally increased expression of CD44 receptors on renal tubule epithelial cells during ischemia/reperfusion-induced acute kidney injury (AKI), we developed a hyaluronic acid-curcumin (HA-CUR) polymeric prodrug targeting to epithelial cells and then relieving oxidative stress damages. The water solubility of HA-CUR was significantly enhanced and approximately 27-fold higher than that of CUR. Cellular uptake test showed HA-CUR was preferably internalized by H2 O2 -pretreated tubular epithelial (HK-2) cells compared with free CUR benefiting from the specific binding between HA and CD44 receptors...
August 1, 2018: Carbohydrate Polymers
https://www.readbyqxmd.com/read/29773068/pharmacokinetic-and-pharmacodynamic-relationship-of-blinatumomab-in-patients-with-non-hodgkin-lymphoma
#20
Youssef Hijazi, Matthias Klinger, Andrea Kratzer, Benjamin Wu, Patrick A Baeuerle, Peter Kufer, Andreas Wolf, Dirk Nagorsen, Min Zhu
OBJECTIVE: We describe the relationship between pharmacokinetics (PK) of blinatumomab and pharmacodynamic (PD) changes in peripheral lymphocytes, serum cytokines, and tumor size in patients with non-Hodgkin lymphoma (NHL). METHODS: In a phase 1 study, 76 patients with relapsed/refractory NHL received blinatumomab by continuous intravenous infusion at various doses (0.5 to 90 µg/m2/day). PD changes were analyzed with respect to dose, blinatumomab concentration at steady state (Css), and cumulative area under the concentration-versus-time curve (AUCcum)...
May 17, 2018: Current Clinical Pharmacology
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