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Pharmacodynamic

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https://www.readbyqxmd.com/read/28549082/pharmacokinetics-and-pharmacodynamics-of-propofol-changes-in-patients-with-frontal-brain-tumours
#1
M M Sahinovic, D J Eleveld, T Miyabe-Nishiwaki, M M R F Struys, A R Absalom
Background: Models of propofol pharmacokinetics and pharmacodynamics developed in patients without brain pathology are widely used for target-controlled infusion (TCI) during brain tumour excision operations. The goal of this study was to determine if the presence of a frontal brain tumour influences propofol pharmacokinetics and pharmacodynamics and existing PK-PD model performance. Methods: Twenty patients with a frontal brain tumour and 20 control patients received a propofol infusion to achieve an induction-emergence-induction anaesthetic sequence...
May 26, 2017: British Journal of Anaesthesia
https://www.readbyqxmd.com/read/28547774/population-pharmacokinetics-pharmacodynamics-and-exploratory-exposure-response-analyses-of-apixaban-in-subjects-treated-for-venous-thromboembolism
#2
W Byon, K Sweeney, C Frost, R A Boyd
Apixaban is approved for treatment of venous thromboembolism (VTE) and prevention of recurrence. Population pharmacokinetics, pharmacokinetics-pharmacodynamics (anti-FXa activity), and exposure-response (binary bleeding and thromboembolic endpoints) of apixaban in VTE treatment subjects were characterized using data from phase I-III studies. Apixaban pharmacokinetics were adequately characterized by a two-compartment model with first-order absorption and elimination. Age, sex, and Asian race had less than 25% impact on exposure, while subjects with severe renal impairment were predicted to have 56% higher exposure than the reference subject (60-year-old non-Asian male weighing 85 kg with creatinine clearance of 100 mL/min)...
May 2017: CPT: Pharmacometrics & Systems Pharmacology
https://www.readbyqxmd.com/read/28546950/genetic-polymorphisms-of-multidrug-and-toxin-extrusion-proteins-mate1-and-mate2-in-south-indian-population
#3
Gerard Marshall Raj, Jayanthi Mathaiyan, Mukta Wyawahare, Katiboina Srinivasa Rao, Rekha Priyadarshini
Introduction: Drug transporters are key determinants of pharmacokinetic and pharmacodynamic profiles of certain drugs. SLC47A1 (MATE1) and SLC47A2 (MATE2) are major efflux transporters involved in the hepatic and renal excretion of many cationic drugs including metformin. Our study was proposed to determine the normative frequencies of the single nucleotide polymorphisms (SNPs) rs2289669 and rs12943590 in the SLC47A1 and SLC47A2 genes, respectively, in South Indian population and also to compare those with those of the HapMap populations...
2017: BioImpacts: BI
https://www.readbyqxmd.com/read/28544992/pharmacokinetics-pharmacodynamics-and-tolerability-of-usl261-midazolam-nasal-spray-randomized-study-in-healthy-geriatric-and-non-geriatric-adults
#4
Alexander K Berg, Michael J Myrvik, Peter J Van Ess
AIM: Characterize pharmacokinetics, pharmacodynamics, and safety/tolerability of USL261 in geriatric adults to inform its potential for treating bouts of increased seizure activity. METHODS: Phase 1, randomized, double-blind, 2-way crossover study in healthy geriatric (≥65years; n=18) and non-geriatric (18-40years; n=12) adults evaluated single USL261 doses (2.5 and 5.0mg) administered intranasally. Pharmacokinetic parameters were estimated for midazolam and 1-hydroxymidazolam (active metabolite), including area under the plasma concentration-time curve (AUC), maximum plasma concentration (Cmax), time to Cmax (Tmax), and half-life (t1/2)...
May 22, 2017: Epilepsy & Behavior: E&B
https://www.readbyqxmd.com/read/28544774/safety-pharmacokinetics-and-pharmacodynamics-of-hetrombopag-olamine-a-novel-tpo-r-agonist-in-healthy-subjects
#5
Li Zheng, Mao-Zhi Liang, Xiao-Ling Zeng, Cai-Zheng Li, Yi-Fan Zhang, Xiao-Yan Chen, Xi Zhu, An-Bo Xiang
Hetrombopag olamine (hetrombopag) is a novel small-molecule, orally bioavailable, non-peptide thrombopoietin (TPO) receptor agonist that is being developed as the treatment for thrombocytopenia. Two randomized, placebo-controlled phase I studies were conducted in 72 healthy subjects to assess the safety, tolerability, pharmacokinetics and pharmacodynamics of hetrombopag. Hetrombopag was orally administered with a single dose in 5 dose cohorts (5 mg, 10 mg, 20 mg, 30 mg or 40 mg) in the first study, and given once daily for 10 days in 3 dose cohorts (2...
May 24, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28544589/methionine-tumor-starvation-by-erythrocyte-encapsulated-methionine-gamma-lyase-activity-controlled-with-per-os-vitamin-b6
#6
Fabien Gay, Karine Aguera, Karine Sénéchal, Angie Tainturier, Willy Berlier, Delphine Maucort-Boulch, Jérôme Honnorat, Françoise Horand, Yann Godfrin, Vanessa Bourgeaux
Erymet is a new therapy resulting from the encapsulation of a methionine gamma-lyase (MGL; EC number 4.4.1.11) in red blood cells (RBC). The aim of this study was to evaluate erymet potential efficacy in methionine (Met)-dependent cancers. We produced a highly purified MGL using a cGMP process, determined the pharmacokinetics/pharmacodynamics (PK/PD) properties of erymet in mice, and assessed its efficacy on tumor growth prevention. Cytotoxicity of purified MGL was tested in six cancer cell lines. CD1 mice were injected with single erymet product supplemented or not with vitamin B6 vitamer pyridoxine (PN; a precursor of PLP cofactor)...
May 23, 2017: Cancer Medicine
https://www.readbyqxmd.com/read/28544475/thiazole-based-sigma-1-receptor-ligands-diversity-by-late-stage-c-h-arylation-of-thiazoles-structure-affinity-and-selectivity-relationships-and-molecular-interactions
#7
Bernhard Wünsch, Artur Kokornaczyk, Dirk Schepmann, Junichiro Yamaguchi, Kenichiro Itami, Erik Laurini, Maurizio Fermeglia, Sabrina Pricl
Spirocyclic thiophene derivatives represent promising sigma-1 ligands with high sigma-1 affinity and selectivity over the sigma-2 subtype. In order to increase ligand efficiency, the thiophene ring was replaced bioisosterically by a thiazole ring and the pyran ring was opened. Late-stage diversification by regioselective C-H arylation of thiazoles 9a-c resulted in a set of 53 compounds with high diversity. This set of compounds was analyzed with respect to sigma-1 affinity, sigma-1/sigma-2 selectivity, lipophilicity (logD7...
May 24, 2017: ChemMedChem
https://www.readbyqxmd.com/read/28543601/influence-of-meals-and-glycemic-changes-on-qt-interval-dynamics
#8
Brenda Cirincione, Philip T Sager, Donald E Mager
Thorough QT/QTc studies have become an integral part of early drug development programs, with major clinical and regulatory implications. This analysis expands on existing pharmacodynamic models of QT interval analysis by incorporating the influence of glycemic changes on the QT interval in a semimechanistic manner. A total of 21 healthy subjects enrolled in an open-label phase 1 pilot study and provided continuous electrocardiogram monitoring and plasma glucose and insulin concentrations associated with a 24-hour baseline assessment...
May 22, 2017: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28543360/relationship-between-the-uplc-q-tof-ms-fingerprinted-constituents-from-daphne-genkwa-and-their-anti-inflammatory-anti-oxidant-activities
#9
Wen-Juan Du, Jun Ji, Ling Wang, Xin-Yi Lan, Jia Li, Jun-Qiu Lei, Xin He, Chun-Feng Zhang, Wen-Ze Huang, Zhen-Zhong Wang, Wei Xiao, Chong-Zhi Wang, Chun-Su Yuan
Daphne genkwa Sieb.et Zucc. is a well-known medicinal plant. This study was designed to apply the ultra-high performance liquid chromatography (UPLC) system to establish a quality control method of Daphne genkwa. Data revealed that there were fifteen common peaks in ten batches of D. genkwa Sieb. Et Zucc.(Thymelaeaceae) from different provinces of China. On this basis, the fingerprint chromatogram was established to provide references for quality control. Afterwards, the chemical constitutions of these common peaks were analyzed using the UPLC-Q-TOF-MS system and nine of them were identified primarily...
May 22, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/28543183/a-novel-k-competitive-acid-blocker-yh4808-sustains-inhibition-of-gastric-acid-secretion-with-a-faster-onset-than-esomeprazole-randomised-clinical-study-in-healthy-volunteers
#10
S Yi, H Lee, S B Jang, H M Byun, S H Yoon, J-Y Cho, I-J Jang, K-S Yu
BACKGROUND: YH4808, a K(+) -competitive acid blocker, is under clinical development for the treatment of acid-related disorders, such as gastroesophageal reflux disease. AIMS: We aimed to determine the safety, tolerability, pharmacokinetics (PK), and pharmacodynamics (PD) of YH4808, compared to placebo and esomeprazole. METHODS: This double-blind, randomised, placebo- and active comparator (esomeprazole)-controlled study was conducted with 123 healthy male volunteers...
May 21, 2017: Alimentary Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/28542866/pharmacokinetic-pharmacodynamic-evaluation-of-marbofloxacin-as-a-single-injection-for-pasteurellaceae-respiratory-infections-in-cattle-using-population-pharmacokinetics-and-monte-carlo-simulations
#11
A Paulin, M Schneider, F Dron, F Woehrle
Population pharmacokinetic of marbofloxacin was investigated with 52 plasma concentration-time profiles obtained after intramuscular administration of Forcyl® in cattle. Animal's status, pre-ruminant, ruminant, or dairy cow, was retained as a relevant covariate for clearance. Monte Carlo simulations were performed using a stratification by status, and 1000 virtual disposition curves were generated in each bovine subpopulation for the recommended dosage regimen of 10 mg/kg as a single injection. The probability of target attainment (PTA) of pharmacokinetic/pharmacodynamic (PK/PD) ratios associated with clinical efficacy and prevention of resistance was determined in each simulated subpopulation...
May 19, 2017: Journal of Veterinary Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28541510/optimization-of-linezolid-therapy-in-the-critically-ill-the-effect-of-adjusted-infusion-regimens
#12
Max Taubert, Johannes Zander, Sebastian Frechen, Christina Scharf, Lorenz Frey, Michael Vogeser, Uwe Fuhr, Michael Zoller
Objectives: Insufficient linezolid levels, which are associated with a poorer outcome, are often observed in ICU patients who receive standard dosing. Although strategies to overcome these insufficient levels have been discussed, appropriate alternative dosing regimens remain to be identified. Methods: Various infusion regimens (1200-3600 mg/day; q6h, q8h, q12h and continuous) were simulated in 67 000 ICU patients. The probability of attaining pharmacodynamic targets ( T >MIC ≥85%, AUC/MIC ≥100, cumulative fraction of response for Staphylococcus aureus and Enterococcus spp...
May 24, 2017: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/28541145/pharmacokinetics-of-butorphanol-tartrate-in-a-long-acting-poloxamer-407-gel-formulation-administered-to-hispaniolan-amazon-parrots-amazona-ventralis
#13
Delphine Laniesse, David Sanchez-Migallon Guzman, Heather K Knych, Dale A Smith, Cornelia Mosley, Joanne R Paul-Murphy, Hugues Beaufrère
OBJECTIVE To determine pharmacokinetics of butorphanol tartrate incorporated into poloxamer 407 (P407) after SC administration to Hispaniolan Amazon parrots (Amazona ventralis). ANIMALS 11 adult Hispaniolan Amazon parrots (6 males and 5 females; 11 to 27 years old). PROCEDURES A sterile formulation of butorphanol in P407 (But-P407) 25% (percentage determined as [weight of P407/weight of diluent] × 100]) was created (8.3 mg/mL). Five preliminary experiments (2 birds/experiment) were performed to determine the ideal dose for this species...
June 2017: American Journal of Veterinary Research
https://www.readbyqxmd.com/read/28541144/in-vitro-characterization-of-a-formulation-of-butorphanol-tartrate-in-a-poloxamer-407-base-intended-for-use-as-a-parenterally-administered-slow-release-analgesic-agent
#14
Delphine Laniesse, Dale A Smith, Heather K Knych, Cornelia Mosley, David Sanchez-Migallon Guzman, Hugues Beaufrère
OBJECTIVE To assess rheological properties and in vitro diffusion of poloxamer 407 (P407) and butorphanol-P407 (But-P407) hydrogels and to develop a sustained-release opioid formulation for use in birds. SAMPLE P407 powder and a commercially available injectable butorphanol tartrate formulation (10 mg/mL). PROCEDURES P407 and But-P407 gels were compounded by adding water or butorphanol to P407 powder. Effects of various concentrations of P407 (20%, 25% and 30% [{weight of P407/weight of diluent} × 100]), addition of butorphanol, and sterilization through a microfilter on rheological properties of P407 were measured by use of a rheometer...
June 2017: American Journal of Veterinary Research
https://www.readbyqxmd.com/read/28540640/a-population-pharmacokinetic-and-pharmacodynamic-analysis-of-abemaciclib-in-a-phase-i-clinical-trial-in-cancer-patients
#15
Sonya C Tate, Amanda K Sykes, Palaniappan Kulanthaivel, Edward M Chan, P Kellie Turner, Damien M Cronier
BACKGROUND AND OBJECTIVES: Abemaciclib, a dual inhibitor of cyclin-dependent kinases 4 and 6, has demonstrated clinical activity in a number of different cancer types. The objectives of this study were to characterize the pharmacokinetics of abemaciclib in cancer patients using population pharmacokinetic (popPK) modeling, and to evaluate target engagement at clinically relevant dose levels. METHODS: A phase I study was conducted in cancer patients which incorporated intensive pharmacokinetic sampling after single and multiple oral doses of abemaciclib...
May 24, 2017: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/28539174/drug-metabolism-in-the-elderly-a-multifactorial-problem
#16
REVIEW
R H Waring, R M Harris, S C Mitchell
Whether or not an individual's drug metabolising capacity declines with advancing age is a vexing question. There is no clear evidence that drug metabolism itself ('the biologically-assisted chemical alteration of the administered parent molecule') is less efficient in healthy old age than at younger ages, whereas a decreased capacity may be associated with ill-health and frailty. However, elderly individuals do show a reduced enzyme induction capability and are less able to tolerate overdoses. It appears that the majority of deleterious clinical outcomes related to drug therapy in an elderly (usually ill or frail) population may be ascribed to various anatomical and physiological age-related changes...
June 2017: Maturitas
https://www.readbyqxmd.com/read/28538836/establishment-of-patient-derived-tumor-xenograft-pdtx-models-using-samples-from-ct-guided-percutaneous-biopsy
#17
Y-P Zhuang, Y-P Zhu, H-Y Wang, L Sun, J Zhang, Y-P Hao, L Wang
This study aimed to investigate the feasibility of the establishment of a human cancer xenograft model using samples from computed tomography (CT)-guided percutaneous biopsy. Fresh tumor tissues obtained from 10 cancer patients by CT-guided percutaneous biopsy were subcutaneously inoculated into NOD-Prkdcem26Il2rgem26Nju (NCG) mice to establish human patient-derived tumor xenograft (PDTX) models. The formation of first and second generation xenografts was observed, and tumor volume was recorded over time. Tumor tissue consistency between the PDTX model and primary tumors in patients was compared using H&E staining and immunohistochemistry...
May 18, 2017: Brazilian Journal of Medical and Biological Research, Revista Brasileira de Pesquisas Médicas e Biológicas
https://www.readbyqxmd.com/read/28538111/cardiovascular-and-metabolic-effects-of-angptl3-antisense-oligonucleotides
#18
Mark J Graham, Richard G Lee, Teresa A Brandt, Li-Jung Tai, Wuxia Fu, Raechel Peralta, Rosie Yu, Eunju Hurh, Erika Paz, Bradley W McEvoy, Brenda F Baker, Nguyen C Pham, Andres Digenio, Steven G Hughes, Richard S Geary, Joseph L Witztum, Rosanne M Crooke, Sotirios Tsimikas
Background Epidemiologic and genomewide association studies have linked loss-of-function variants in ANGPTL3, encoding angiopoietin-like 3, with low levels of plasma lipoproteins. Methods We evaluated antisense oligonucleotides (ASOs) targeting Angptl3 messenger RNA (mRNA) for effects on plasma lipid levels, triglyceride clearance, liver triglyceride content, insulin sensitivity, and atherosclerosis in mice. Subsequently, 44 human participants (with triglyceride levels of either 90 to 150 mg per deciliter [1...
May 24, 2017: New England Journal of Medicine
https://www.readbyqxmd.com/read/28537878/biological-characterization-of-sn32976-a-selective-inhibitor-of-pi3k-and-mtor-with-preferential-activity-to-pi3k%C3%AE-in-comparison-to-established-pan-pi3k-inhibitors
#19
Gordon W Rewcastle, Sharada Kolekar, Christina M Buchanan, Swarna A Gamage, Anna C Giddens, Kit Y Tsang, Jackie D Kendall, Ripudaman Singh, Woo-Jeong Lee, Greg C Smith, Weiping Han, David J Matthews, William A Denny, Peter R Shepherd, Stephen M F Jamieson
Multiple therapeutic agents have been developed to target the phosphatidylinositol 3-kinase (PI3K) signaling pathway, which is frequently dysregulated in cancer promoting tumor growth and survival. These include pan PI3K inhibitors, which target class Ia PI3K isoforms and have largely shown limited single agent activity with narrow therapeutic windows in clinical trials. Here, we characterize SN32976, a novel pan PI3K inhibitor, for its biochemical potency against PI3K isoforms and mTOR, kinase selectivity, cellular activity, pharmacokinetics, pharmacodynamics and antitumor efficacy relative to five clinically-evaluated pan PI3K inhibitors: buparlisib, dactolisib, pictilisib, omipalisib and ZSTK474...
May 9, 2017: Oncotarget
https://www.readbyqxmd.com/read/28537449/understanding-how-pharmacokinetic-and-pharmacodynamic-differences-of-basal-analog-insulins-influence-clinical-practice
#20
Jennifer Goldman, Christoph Kapitza, Jeremy Pettus, Tim Heise
This article reviews pharmacokinetic (PK) and pharmacodynamic (PD) concepts relating to the pharmacology of basal insulin analogs. Understanding the pharmacology of currently available long-acting basal insulins and the techniques used to assess PK and PD parameters (e.g. the euglycemic clamp method) is important when considering the efficacy and safety of these agents, and can help in understanding the rationale for specific dosing strategies when tailoring therapy for a specific patient. Basal insulins such as insulin glargine 100 units (U)/mL and insulin detemir show improved PK/PD characteristics compared with the intermediate-acting NPH insulin, with a longer duration of action, a more consistent glucose-lowering effect and less prominent concentration peaks...
May 24, 2017: Current Medical Research and Opinion
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