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https://www.readbyqxmd.com/read/29458233/pharmacokinetic-modelling-to-predict-fviii-c-response-to-desmopressin-and-its-reproducibility-in-nonsevere-haemophilia-a-patients
#1
L M Schütte, R M van Hest, S C M Stoof, F W G Leebeek, M H Cnossen, M J H A Kruip, R A A Mathôt
BACKGROUND: Nonsevere haemophilia A (HA) patients can be treated with desmopressin. Response of factor VIII activity (FVIII:C) differs between patients and is difficult to predict. OBJECTIVES: Our aims were to describe FVIII:C response after desmopressin and its reproducibility by population pharmacokinetic (PK) modelling. PATIENTS AND METHODS: Retrospective data of 128 nonsevere HA patients (age 7-75 years) receiving an intravenous or intranasal dose of desmopressin were used...
February 19, 2018: Thrombosis and Haemostasis
https://www.readbyqxmd.com/read/29458194/differential-effects-of-acute-versus-chronic-stress-on-ethanol-sensitivity-evidence-for-interactions-on-both-behavioral-and-neuroimmune-outcomes
#2
Tamara L Doremus-Fitzwater, Jacqueline E Paniccia, Anny Gano, Andrew Vore, Terrence Deak
Acute alcohol intoxication induces significant alterations in brain cytokines. Since stress challenges also profoundly impact central cytokine expression, these experiments examined the influence of acute and chronic stress on ethanol-induced brain cytokine responses. In Experiment 1, adult male rats were exposed to acute footshock. After a post-stress recovery interval of 0, 2, 4, or 24 h, rats were administered ethanol (4 g/kg; intragastric), with trunk blood and brains collected 3 h later. In non-stressed controls, acute ethanol increased expression of Il-6 and IκBα in the hippocampus...
February 16, 2018: Brain, Behavior, and Immunity
https://www.readbyqxmd.com/read/29458138/pharmacokinetic-and-pharmacodynamic-evaluation-of-5-methoxy-2-aminoindane-meai-a-new-binge-mitigating-agent
#3
Jakob A Shimshoni, Eyal Sobol, Ezekiel Golan, Yulius Ben Ari, Orit Gal
5-Methoxy-2-aminoindane (MEAI) is a novel psychoactive aminoindane derivative, exerting euphoric, alcohol-like tipsy experience and reduced desire to consume alcoholic beverages. Our previous toxicological evaluation of MEAI in rats, clearly indicated MEAI's potential to be further evaluated as a promising binge mitigating agent due to its favorable safety profile. In the light of these observations, we have determined MEAI's pharmacokinetic (PK) profile in rats and evaluated in-vitro its pharmacodynamics (PD) profile...
February 16, 2018: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/29458132/therapeutic-drug-monitoring-in-treatment-experienced-hiv-infected-patients-receiving-darunavir-based-salvage-regimens-a-case-series
#4
Sébastien Landry, Chi-Nan Chen, Nimish Patel, Alice Tseng, Richard G Lalonde, Denis Thibeault, Steven Sanche, Nancy L Sheehan
Therapeutic drug monitoring (TDM) constitutes a compelling approach for the optimization of antiretroviral therapy in treatment-experienced HIV-1 patients. While various inhibitory indices have been proposed to predict virologic outcome, there is a lack of consensus on the clinical value of TDM. Here, we report the comparative results of TDM in 14 HIV-1-infected patients who had previously received at least two different PI-based regimens and who initiated darunavir (DRV)-based salvage therapy. Pharmacokinetic/pharmacodynamics (PK/PD) parameters were calculated for each subject...
February 16, 2018: Antiviral Research
https://www.readbyqxmd.com/read/29458047/effects-of-cytochrome-p450-single-nucleotide-polymorphisms-on-methadone-metabolism-and-pharmacodynamics
#5
REVIEW
Taha Ahmad, Monica A Valentovic, Gary O Rankin
Methadone is a synthetic, long-acting opioid with a single chiral center forming two enantiomers, (R)-methadone and (S)-methadone, each having specific pharmacological actions. Concentrations of (R)- and (S)-methadone above therapeutic levels have the ability to cause serious, life-threatening, and fatal side effects. This toxicity can be due in part to the pharmacogenetics of an individual, which influences the pharmacokinetic and pharmacodynamic properties of the drug. Methadone is primarily metabolized in the liver by cytochrome P450 (CYP) enzymes, predominately by CYP2B6, followed by CYP3A4, 2C19, 2D6, and to a lesser extent, CYP2C18, 3A7, 2C8, 2C9, 3A5, and 1A2...
February 16, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/29457982/discovery-of-gdc-0853-a-potent-selective-and-non-covalent-bruton-s-tyrosine-kinase-inhibitor-in-early-clinical-development
#6
James J Crawford, Adam R Johnson, Dinah L Misner, Lisa D Belmont, Georgette M Castanedo, Regina Choy, Melis Coraggio, Liming Dong, Charles Eigenbrot, Rebecca Erickson, Nico Ghilardi, Jonathan Hau, Arna Katewa, Pawan Bir Kohli, Wendy Lee, Joseph W Lubach, Brent S McKenzie, Daniel Fred Ortwine, Leah Schutt, Suzanne Tay, Binqing Wei, Karin Reif, Lichuan Liu, Harvey Wong, Wendy B Young
Btk is a non-receptor cytoplasmic tyrosine kinase involved in B-cell and myeloid cell activation, downstream of B-cell and Fcγ receptors, respectively. Pre-clinical studies have indicated that inhibition of Btk activity might offer a potential therapy in autoimmune diseases such as rheumatoid arthritis and systemic lupus erythematosus. Here we disclose the discovery and pre-clinical characterization of a potent, selective, and non-covalent Btk inhibitor currently in clinical development. GDC-0853 (29) suppresses B cell- and myeloid cell-mediated components of disease, and demonstrates dose-dependent activity in an in vivo rat model of inflammatory arthritis...
February 19, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29457876/pharmacokinetics-of-metformin-in-patients-with-gastrointestinal-intolerance
#7
L McCreight, T B Stage, P Connelly, M Lonergan, F Nielsen, C Prehn, J Adamski, K Brosen, E R Pearson
AIMS: Metformin intolerance symptoms are gastrointestinal in nature, but the underlying mechanism is poorly understood. The aim of this study was to assess potential causes of metformin intolerance including: altered metformin uptake from the intestine; increased anaerobic glucose utilisation and subsequent lactate production; altered serotonin uptake; and altered bile acid pool. METHODS: This pharmacokinetic study recruited ten severely intolerant and ten tolerant individuals matched for age, sex and BMI...
February 19, 2018: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/29457840/population-pharmacokinetics-and-pharmacogenomics-of-apixaban-in-japanese-adult-patients-with-atrial-fibrillation
#8
Satoshi Ueshima, Daiki Hira, Yuuma Kimura, Ryo Fujii, Chiho Tomitsuka, Takuya Yamane, Yohei Tabuchi, Tomoya Ozawa, Hideki Itoh, Seiko Ohno, Minoru Horie, Tomohiro Terada, Toshiya Katsura
AIMS: This study aimed to analyse the effects of genetic polymorphisms in drug transporters and metabolising enzymes, and clinical laboratory data on the pharmacokinetic parameters of apixaban. METHODS: Data were collected from 81 Japanese patients with atrial fibrillation. Pharmacogenomic data were stratified by ABCB1, ABCG2, and CYP3A5 polymorphisms. The pharmacokinetic profile of apixaban was described by a one-compartment model with first-order absorption. Population pharmacokinetic analysis was conducted using non-linear mixed effect modelling (NONMEM™) program...
February 19, 2018: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29457349/impact-of-glutathione-modulation-on-stability-and-pharmacokinetic-profile-of-redox-sensitive-nanogels
#9
Natascha Drude, Oliver H Winz, Felix M Mottaghy, Marion Roller, Hiltrud Königs, Martin Möller, Smriti Singh, Agnieszka Morgenroth
Nanoparticles degradable upon external stimuli combine pharmacokinetic features of both small molecules as well as large nanoparticles. However, despite promising preclinical results, several redox responsive disulphide-linked nanoparticles failed in clinical translation, mainly due to their unexpected in vivo behavior. Glutathione (GSH) is one of the most evaluated antioxidants responsible for disulfide degradation. Herein, the impact of GSH on the in vivo behavior of redox-sensitive nanogels under physiological and modulated conditions is investigated...
February 19, 2018: Small
https://www.readbyqxmd.com/read/29457257/pharmacokinetics-pharmacodynamics-and-metabolism-of-acepromazine-following-intravenous-oral-and-sublingual-administration-to-exercised-thoroughbred-horses
#10
H K Knych, K Seminoff, D S McKemie, P H Kass
Acepromazine is a tranquilizer used commonly in equine medicine. This study describes serum and urine concentrations and the pharmacokinetics and pharmacodynamics of acepromazine following intravenous, oral, and sublingual (SL) administration. Fifteen exercised adult Thoroughbred horses received a single intravenous, oral, and SL dose of 0.09 mg/kg of acepromazine. Blood and urine samples were collected at time 0 and at various times for up to 72 hr and analyzed for acepromazine and its two major metabolites (2-(1-hydroxyethyl) promazine and 2-(1-hydroxyethyl) promazine sulfoxide) using liquid chromatography-tandem mass spectrometry...
February 18, 2018: Journal of Veterinary Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29457247/development-of-a-multiroute-physiologically-based-pharmacokinetic-model-for-orbifloxacin-in-rabbits
#11
F Yang, F Yang, W Shi, H Si, T Kong, G Wang, J Zhang
To predict the orbifloxacin concentrations in rabbits after multiple routes of administration, a flow-limited multiroute physiologically based pharmacokinetic (PBPK) model was developed. Three routes of administration (IV, IM, and PO) were incorporated into this model. Physiological parameters including tissue weights and blood flows through different tissues were obtained from the literature. The tissue/plasma partition coefficients (PX s) for noneliminating tissues were calculated according to the area method, while the PX s for kidney and the rest of the body compartment, together with other parameters for absorption and elimination, were optimized based on the published concentrations...
February 18, 2018: Journal of Veterinary Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29456791/nonacidic-chemotype-possessing-n-acylated-piperidine-moiety-as-potent-farnesoid-x-receptor-fxr-antagonists
#12
Naoki Teno, Yukiko Yamashita, Yusuke Iguchi, Ko Fujimori, Mizuho Une, Tomoko Nishimaki-Mogami, Takie Hiramoto, Keigo Gohda
Farnesoid X receptor (FXR) plays a major role in the control of cholesterol metabolism. Antagonizing transcriptional activity of FXR is an effective means to treat the relevant metabolic syndrome. Some of antagonists so far have the charged functions; however, they may negatively affect the pharmacokinetics. We describe herein a structure-activity relationship (SAR) exploration of nonacidic FXR antagonist 6 focusing on two regions in the structure and biological evaluation of nonacidic 10 with the characteristic N -acylated piperidine group obtained from SAR studies...
February 8, 2018: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29456504/a-review-on-central-nervous-system-effects-of-gastrodin
#13
REVIEW
Yuan Liu, Jialiang Gao, Min Peng, Hongyan Meng, Hongbo Ma, Pingping Cai, Yuan Xu, Qiong Zhao, Guomin Si
Rhizoma Gastrodiae (also known as Tian ma ), the dried rhizome of Gastrodia elata Blume, is a famous Chinese herb that has been traditionally used for the treatment of headache, dizziness, spasm, epilepsy, stoke, amnesia and other disorders for centuries. Gastrodin, a phenolic glycoside, is the main bioactive constituent of Rhizoma Gastrodiae . Since identified in 1978, gastrodin has been extensively investigated on its pharmacological properties. In this article, we reviewed the central nervous system (CNS) effects of gastrodin in preclinical models of CNS disorders including epilepsy, Alzheimer's disease, Parkinson's disease, affective disorders, cerebral ischemia/reperfusion, cognitive impairment as well as the underlying mechanisms involved and, where possible, clinical data that support the pharmacological activities...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29456381/evaluation-of-teaching-clinical-pharmacology-of-antiarrhythmic-drugs-to-first-year-mbbs-students-through-worksheet-based-small-group-discussion
#14
Ameya A Hasamnis, Aditya Arya
Cardiac arrhythmias are a major cause of morbidity and mortality across the world. Learning the science behind the use of antiarrhythmic drugs is essential for all medical graduates. However, many antiarrhythmic drugs are available, and most of them have complex pharmacodynamic and pharmacokinetic profiles. We tried to improvise our teaching by conducting interactive, worksheet-based, small-group discussion on antiarrhythmic drugs with preclinical students of School of Medicine, Taylor's University, Malaysia...
October 2017: Journal of Pharmacy & Bioallied Sciences
https://www.readbyqxmd.com/read/29455730/enhancement-of-oral-bioavailability-and-immune-response-of-ginsenoside-rh2-by-co-administration-with-piperine
#15
Zhao-Hui Jin, Wen Qiu, Hui Liu, Xue-Hua Jiang, Ling Wang
Ginsenoside Rh2 (Rh2) is one of the major bioactive ginsenosides in Panax ginseng. However, the oral bioavailability of Rh2 is low, with P-glycoprotein (P-gp) and CYP3A4 being reported to be the main factors. The purpose of the present study was to determine the enhancing effect of piperine on the oral bioavailability as well as bioactivity of Rh2. The inhibitory effect of piperine on P-gp and CYP3A4 was determined using a Caco-2 monolayer model and a recombinant CYP3A4 metabolic system, respectively. The pharmacokinetics of oral Rh2 (10 mg·kg-1 ) administered alone or in combination with piperine (10 and 20 mg·kg-1 ) was performed in rats...
February 2018: Chinese Journal of Natural Medicines
https://www.readbyqxmd.com/read/29455535/antioxidative-nanoparticles-significantly-enhance-therapeutic-efficacy-of-an-antibacterial-therapy-against-listeria-monocytogenes-infection
#16
Yutaka Ikeda, Kazuhiro Shoji, Chitho P Feliciano, Shinji Saito, Yukio Nagasaki
Acute inflammatory conditions such as sepsis lead to fatal conditions, including multiple organ failure. Several treatments such as steroidal anti-inflammatory drugs are currently being investigated in order to decrease the blood cytokine level, which increases remarkably. However, any of these therapeutic treatments are not always reliable and effective; none have drastically improved survival rates, and some have mostly ended with failure. Reactive oxygen species (ROS) are signaling molecules responsible for the production of cytokines and chemokines that can mediate hyperactivation of the immune response called cytokine storm...
February 20, 2018: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/29455429/predictive-performance-of-physiologically-based-pharmacokinetic-models-in-predicting-drug-drug-interactions-involving-enzyme-modulation
#17
Chia-Hsiang Hsueh, Vicky Hsu, Yuzhuo Pan, Ping Zhao
BACKGROUND: Physiologically-based pharmacokinetic (PBPK) modeling in predicting metabolic drug-drug interactions (mDDIs) is routinely used in drug development. Currently, the US FDA endorses the use of PBPK to potentially support dosing recommendations for investigational drugs as enzyme substrates of mDDIs, and to inform a lack of mDDIs for investigational drugs as enzyme modulators. METHODS: We systematically evaluated the performance of PBPK modeling in predicting mDDIs published in the literature...
February 17, 2018: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/29455032/sevoflurane-for-procedural-sedation-in-critically-ill-patients-a-pharmacokinetic-comparative-study-between-burn-and-non-burn-patients
#18
Sebastien Perbet, Daniel Bourdeaux, Alexandre Lenoire, Claire Biboulet, Bruno Pereira, Malha Sadoune, Benoit Plaud, Jean-Marie Launay, Jean-Etienne Bazin, Valerie Sautou, Alexandre Mebazaa, Pascal Houze, Jean-Michel Constantin, Matthieu Legrand
BACKGROUND: Sevoflurane has anti-inflammatory proprieties and short lasting effects making it of interest for procedural sedation in critically ill patients. We evaluated the pharmacokinetics of sevoflurane and metabolites in severely ill burn patients and controls. The secondary objective was to assess potential kidney injury. METHODS: prospective interventional study in a burn and a surgical intensive care unit 24 mechanically ventilated critically ill patients (12 burns, 12 controls) were included,...
February 15, 2018: Anaesthesia, Critical Care & Pain Medicine
https://www.readbyqxmd.com/read/29454920/design-synthesis-and-identification-of-silicon-containing-hcv-ns5a-inhibitors-with-pan-genotype-activity
#19
Baomin Liu, Kuo Gai, Hui Qin, Xushi Liu, Yuan Cao, Qin Lu, Dandan Lu, Deyang Chen, Hengqiao Shen, Wei Song, Yang Zhang, Xiaojin Wang, Hongjiang Xu, Yinsheng Zhang
Modification of a HCV NS5A inhibitor, ombitasvir, led to the identification of 10d with improved pan-genotype NS5A inhibition and better pharmacokinetic properties. The key structural changes to ombitasvir include bioisosteric replacement of carbon with silicon atom. Compared with ombitasvir, the activity of anti-HCV genotypes (GT 1 to 6) of 10d is increased to some extent, especially the inhibitory activity against genotype 3a and 6a is increased by more than seven times, and the dog's in vivo pharmacokinetics properties were also superior to ombitasvir...
February 10, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29454888/bioequivalence-decision-for-nanoparticular-iron-complex-drugs-for-parenteral-administration-based-on-their-disposition
#20
Julia Schnorr, Sören Fütterer, Karsten Spicher, Maria Catarinolo, Christoph Schlösser, Harald Enzmann, Peter Langguth
Although parenteral iron products have been established to medicinal use decades before, their structure and pharmacokinetic properties are not fully characterized yet. With its' second reflection paper on intravenous iron-based nano-colloidal products (EMA/CHMP/SWP/620008/2012) the European Medicine Agency provided an extensive catalogue of methods for quality, non-clinical and pharmacokinetic studies for the comparison of nano-sized iron products to an originator (EMA, 2015). For iron distribution studies, the reflection paper assumed the use of rodents...
February 15, 2018: Regulatory Toxicology and Pharmacology: RTP
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