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Pharmacodynamic

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https://www.readbyqxmd.com/read/28092108/pharmacokinetics-and-pharmacodynamics-of-the-injectable-formulation-of-methadone-hydrochloride-and-methadone-in-lipid-nanocarriers-administered-orally-to-horses
#1
N Crosignani, S P Luna, T Dalla Costa, E L Pimenta, C B Detoni, S S Guterres, J N Puoli Filho, J C Pantoja, M C Pigatto
We investigated the thermal, electrical and mechanical antinociceptive and physiological effects (heart rate, respiratory rate, arterial blood pressure, head height and abdominal auscultation score), and pharmacokinetics, of 0.5 mg/kg of the injectable formulation (ORAL) or nanoparticulated methadone (NANO) given orally, in six adult mares, using a crossover, blind and prospective design. Repeated-measure models were used to compare parametric data between and within treatments, followed by Tukey's test. Nonparametric data were analysed with Wilcoxon signed-rank, adjusted by Bonferroni tests...
January 16, 2017: Journal of Veterinary Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28091703/bolus-application-of-landiolol-and-esmolol-comparison-of-the-pharmacokinetic-and-pharmacodynamic-profiles-in-a-healthy-caucasian-group
#2
Günther Krumpl, Ivan Ulc, Michaela Trebs, Pavla Kadlecová, Juri Hodisch
PURPOSE: The aim of this prospective study was to compare in non-Asian subjects the pharmacokinetics (PK), pharmacodynamics (PD), safety, and tolerability of two short-acting cardioselective β1-adrenergic antagonists, landiolol and esmolol, after administration of three different bolus dosages. MATERIALS AND METHODS: We conducted a single-center, prospective, double-blinded, randomized study in three cross-over periods with 12 healthy subjects (7 women and 5 men, mean age of 24...
January 13, 2017: European Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28090673/pharmacokinetic-pharmacodynamic-integration-and-modelling-of-oxytetracycline-for-the-porcine-pneumonia-pathogens-actinobacillus-pleuropneumoniae-and-pasteurella-multocida
#3
L Dorey, L Pelligand, Z Cheng, P Lees
Pharmacokinetic-pharmacodynamic (PK/PD) integration and modelling were used to predict dosage schedules of oxytetracycline for two pig pneumonia pathogens, Actinobacillus pleuropneumoniae and Pasteurella multocida. Minimum inhibitory concentration (MIC) and mutant prevention concentration (MPC) were determined in broth and porcine serum. PK/PD integration established ratios of average concentration over 48 h (Cav0-48 h )/MIC of 5.87 and 0.27 μg/mL (P. multocida) and 0.70 and 0.85 μg/mL (A. pleuropneumoniae) for broth and serum MICs, respectively...
January 16, 2017: Journal of Veterinary Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28090323/high-thioredoxin-1-levels-in-rheumatoid-arthritis-patients-diminish-binding-and-signalling-of-the-monoclonal-antibody-tregalizumab
#4
Katharina Heim, Benjamin Dälken, Stefanie Faust, Faiza Rharbaoui, Andre Engling, Holger Wallmeier, Theodor Dingermann, Heinfried H Radeke, Jörg Schüttrumpf, Marcus Gutscher
The humanized non-depleting anti-CD4 monoclonal antibody Tregalizumab (BT-061) is able to selectively activate the suppressive function of regulatory T cells and has been investigated up to phase IIb in clinical trials in patients suffering from rheumatoid arthritis (RA). A pharmacokinetic-pharmacodynamic model based on clinical data from RA and healthy volunteers, which used the cell surface CD4 downmodulation as marker of activity, confirmed a stronger effect in healthy volunteers compared with RA patients...
December 2016: Clinical & Translational Immunology
https://www.readbyqxmd.com/read/28089180/enteric-coating-and-aspirin%C3%A2-nonresponsiveness-in-patients%C3%A2-with-type%C3%A2-2%C3%A2-diabetes-mellitus
#5
Deepak L Bhatt, Tilo Grosser, Jing-Fei Dong, Douglas Logan, Walter Jeske, Dominick J Angiolillo, Andrew L Frelinger, Lanyu Lei, Juan Liang, Jason E Moore, Byron Cryer, Upendra Marathi
BACKGROUND: A limitation of aspirin is that some patients, particularly those with diabetes, may not have an optimal antiplatelet effect. OBJECTIVES: The goal of this study was to determine if oral bioavailability mediates nonresponsiveness. METHODS: The rate and extent of serum thromboxane generation and aspirin pharmacokinetics were measured in 40 patients with diabetes in a randomized, single-blind, triple-crossover study. Patients were exposed to three 325-mg aspirin formulations: plain aspirin, PL2200 (a modified-release lipid-based aspirin), and a delayed-release enteric-coated (EC) aspirin...
January 5, 2017: Journal of the American College of Cardiology
https://www.readbyqxmd.com/read/28088883/candesartan-cilexetil-loaded-nanodelivery-systems-for-improved-oral-bioavailability
#6
Narendar Dudhipala, Kishan Veerabrahma
Candesartan cilexetil (CC), an antihypertensive drug, has low oral bioavailability due to poor solubility and hepatic first-pass metabolism. These are major limitations in oral delivery of CC. Several approaches are known to reduce the problems of solubility and improve the bioavailability of CC. Among various approaches, nanotechnology-based delivery of CC has potential to overcome the challenges associated with the oral administration. This review focuses on various nano-based delivery systems available and tried for improving the aqueous solubility, dissolution and consequently bioavailability of CC upon oral administration...
February 2017: Therapeutic Delivery
https://www.readbyqxmd.com/read/28088839/pharmacokinetic-pharmacodynamic-modeling-of-the-pde4-inhibitor-tak-648-in-type-2-diabetes-early-translational-approaches-for-human-dose-prediction
#7
N Plock, S Vollert, M Mayer, G Hanauer, G Lahu
TAK-648 is a PDE4 inhibitor with demonstrated preclinical antidiabetic properties. Our objective was to develop a translational pharmacokinetic/pharmacodynamic (PK/PD) model for human type 2 diabetes (T2D) dose prediction using HbA1c results from a db/db mouse study. Estimated parameters in combination with tPDE4i values calculated for the clinical roflumilast dose of 500 μg were used to translate preclinical effects of TAK-648 to required exposure in humans. A first-in-human study with single TAK-648 doses of 0...
January 15, 2017: Clinical and Translational Science
https://www.readbyqxmd.com/read/28088332/manipulation-of-tumor-oxygenation-and-radiosensitivity-through-modification-of-cell-respiration-a-critical-review-of-approaches-and-imaging-biomarkers-for-therapeutic-guidance
#8
REVIEW
Bernard Gallez, Marie-Aline Neveu, Pierre Danhier, Bénédicte F Jordan
Tumor hypoxia has long been considered as a detrimental factor for the response to irradiation. In order to improve the sensitivity of tumors cells to radiation therapy, tumor hypoxia may theoretically be alleviated by increasing the oxygen delivery or by decreasing the oxygen consumption by tumor cells. Mathematical modelling suggested that decreasing the oxygen consumption should be more efficient than increasing oxygen delivery in order to alleviate tumor hypoxia. In this paper, we review several promising strategies targeting the mitochondrial respiration for which alleviation of tumor hypoxia and increase in sensitivity to irradiation have been demonstrated...
January 11, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28087972/lack-of-effect-of-oral-cabotegravir-on-the-pharmacokinetics-of-a-levonorgestrel-ethinyl-estradiol-containing-oral-contraceptive-in-healthy-adult-females
#9
C Trezza, S L Ford, E Gould, Y Lou, C Huang, J M Ritter, A M Buchanan, W Spreen, P Patel
AIM(S): This study aimed to investigate whether cabotegravir (CAB), an integrase inhibitor in development for treatment and prevention of HIV-1, influences the pharmacokinetics (PK) of a levonorgestrel (LNG) and ethinyl estradiol (EE)-containing oral contraceptive (OC) in healthy women. METHODS: In this open-label, fixed-sequence crossover study, healthy female subjects received LNG 0.15 mg/EE 0.03 mg tablet once daily Days 1-10 alone and with oral CAB 30 mg once daily Days 11-21...
January 14, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28081041/a-systematic-literature-review-approach-to-estimate-the-therapeutic-index-of-selected-immunosuppressant-drugs-after-renal-transplantation
#10
Jessica E Ericson, Kanecia O Zimmerman, Daniel Gonzalez, Chiara Melloni, Jeffrey T Guptill, Kevin D Hill, Huali Wu, Michael Cohen-Wolkowiez
BACKGROUND: Drugs that exhibit close margins between therapeutic and toxic blood concentrations are considered to have a narrow therapeutic index (NTI). The Food and Drug Administration has proposed that NTI drugs should have more stringent bioequivalence standards for approval of generic formulations. However, many immunosuppressant drugs do not have a well-defined therapeutic index (TI). METHODS: We sought to determine whether safety, efficacy, and pharmacokinetic data obtained from the medical literature through a comprehensive literature search could be used to estimate the TI of cyclosporine, tacrolimus, and sirolimus...
February 2017: Therapeutic Drug Monitoring
https://www.readbyqxmd.com/read/28079589/in-vogue-ketamine-for-neuroprotection-in-acute-neurologic-injury
#11
Josh D Bell
Neurologic deterioration following acute injury to the central nervous system may be amenable to pharmacologic intervention, although, to date, no such therapy exists. Ketamine is an anesthetic and analgesic emerging as a novel therapy for a number of clinical entities in recent years, including refractory pain, depression, and drug-induced hyperalgesia due to newly discovered mechanisms of action and new application of its known pharmacodynamics. In this focused review, the evidence for ketamine as a neuroprotective agent in stroke, neurotrauma, subarachnoid hemorrhage, and status epilepticus is highlighted, with a focus on its applications for excitotoxicity, neuroinflammation, and neuronal hyperexcitability...
January 10, 2017: Anesthesia and Analgesia
https://www.readbyqxmd.com/read/28079463/influence-of-abcb1-polymorphisms-and-serum-concentrations-on-venlafaxine-response-in-patients-with-major-depressive-disorder
#12
Gul Ozbey, Feryal Cam Celikel, Birgul Elbozan Cumurcu, Derya Kan, Berna Yucel, Ekrem Hasbek, Ferda Percin, Ismail Cüneyt Guzey, Canan Uluoglu
BACKGROUND: The pharmacokinetics and the pharmacodynamics of antidepressants show large inter-individual variations which result in unpredictable clinical responses. AIM: The aim of the study was to examine the effect of ABCB1 polymorphisms and the serum concentrations on the efficacy and tolerability of venlafaxine in patients with major depressive disorder (MDD). METHODS: Fifty-two outpatients who met the Diagnostic and Statistical Manual of Mental Disorders Fourth Edition (DSM-IV) criteria for MDD were recruited for the study...
January 12, 2017: Nordic Journal of Psychiatry
https://www.readbyqxmd.com/read/28079057/functional-mri-of-the-reserpine-induced-putative-rat-model-of-fibromyalgia-reveals-discriminatory-patterns-of-functional-augmentation-to-acute-nociceptive-stimuli
#13
Jack A Wells, Sayaka Shibata, Akihiko Fujikawa, Masayasu Takahashi, Tsuneo Saga, Ichio Aoki
Functional neuroimaging, applied to pre-clinical models of chronic pain, offers unique advantages in the drive to discover new treatments for this prevalent and oppressive condition. The high spatial and temporal resolution of fMRI affords detailed mapping of regional pharmacodynamics that underlie mechanisms of pain suppression by new analgesics. Despite evidence supporting the translational relevance of this approach, relatively few studies have investigated fMRI abnormalities in rodent models of chronic pain...
January 12, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28077672/potentiation-of-ceftazidime-by-avibactam-against-%C3%AE-lactam-resistant-pseudomonas-aeruginosa-in-an-in-vitro-infection-model
#14
Sherwin K B Sy, Luning Zhuang, Marie-Eve Beaudoin, Philipp Kircher, Maria A M Tabosa, Noely C T Cavalcanti, Christian Grunwitz, Sebastian Pieper, Virna J Schuck, Wright W Nichols, Hartmut Derendorf
OBJECTIVES: This study evaluated the in vitro pharmacodynamics of combinations of ceftazidime and the non-β-lactam β-lactamase inhibitor, avibactam, against ceftazidime-, piperacillin/tazobactam- and meropenem-multiresistant Pseudomonas aeruginosa by a quantitative time-kill method. METHODS: MICs of ceftazidime plus 0-16 mg/L avibactam were determined against eight isolates of P. aeruginosa Single-compartment, 24 h time-kill kinetics were investigated for three isolates at 0-16 mg/L avibactam with ceftazidime at 0...
January 10, 2017: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/28076702/lasmiditan-for-the-treatment-of-migraine
#15
Matilde Capi, Fernando de Andrés, Luana Lionetto, Giovanna Gentile, Fabiola Cipolla, Marina Borro, Paolo Martelletti, Martina Curto
Migraine is one of the most common diseases in the world, with high economical and subjective burden. Migraine acute therapy is nowadays based on specific and non-specific drugs but up to 40% of episodic migraineurs still have unmet treatment needs and over 35% do not benefit from triptans administration. Serotonin-1F receptors have been identified in trigeminal system and became an ideal target for anti-migraine drug development as potential trigeminal neural inhibitors. Lasmiditan, a novel serotonin1F receptor agonist, showed specific affinity in vitro for the receptor with any vasoconstrictive action and inhibited markers associated with electrical stimulation of trigeminal ganglion in migraine animal models...
January 11, 2017: Expert Opinion on Investigational Drugs
https://www.readbyqxmd.com/read/28074875/from-an-indirect-response-pharmacodynamic-model-towards-a-secondary-signal-model-of-dose-response-relationship-between-exercise-training-and-physical-performance
#16
Thierry Busso
The aim of this study was to test the suitability of using indirect responses for modeling the effects of physical training on performance. We formulated four different models assuming that increase in performance results of the transformation of a signal secondary to the primary stimulus which is the training dose. The models were designed to be used with experimental data with daily training amounts ascribed to input and performance measured at several dates ascribed to output. The models were tested using data obtained from six subjects who trained on a cycle ergometer over a 15-week period...
January 11, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28074489/a-novel-nf-%C3%AE%C2%BAb-inhibitor-edasalonexent-cat-1004-in-development-as-a-disease-modifying-treatment-for-patients-with-duchenne-muscular-dystrophy-phase-1-safety-pharmacokinetics-and-pharmacodynamics-in-adult-subjects
#17
Joanne M Donovan, Michael Zimmer, Elliot Offman, Toni Grant, Michael Jirousek
In Duchenne muscular dystrophy (DMD), NF-κB is activated in skeletal muscle from infancy regardless of the underlying dystrophin mutation and drives inflammation and muscle degeneration while inhibiting muscle regeneration. Edasalonexent (CAT-1004) is a bifunctional orally administered small molecule that covalently links 2 compounds known to inhibit NF-κB, salicylic acid and docosahexaenoic acid (DHA). Edasalonexent is designed to inhibit activated NF-κB upon intracellular cleavage to these bioactive components...
January 11, 2017: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28074152/optimal-dosage-of-cefmetazole-for-intraoperative-antimicrobial-prophylaxis-in-patients-undergoing-surgery-for-colorectal-cancer
#18
Atsushi Tomizawa, Takatoshi Nakamura, Toshiaki Komatsu, Hiroshi Inano, Rumiko Kondo, Masahiko Watanabe, Koichiro Atsuda
BACKGROUND: Few studies have reported the dosage of cefmetazole (CMZ) for intraoperative antimicrobial prophylaxis in patients underwent surgery for colorectal cancer. We therefore examined the optimal intraoperative dosage of CMZ according to pharmacokinetic/pharmacodynamic (PK/PD) theory in patients who undergoing surgery for colorectal cancer. METHODS: The study group comprised 23 patients with colorectal cancer who underwent surgery, using CMZ as antimicrobial treatment to prevent postoperative infection...
2017: Journal of Pharmaceutical Health Care and Sciences
https://www.readbyqxmd.com/read/28073964/single-dose-pharmacokinetics-and-pharmacodynamics-of-oral-tenofovir-and-emtricitabine-in-blood-saliva-and-rectal-tissue-a-sub-study-of-the-anrs-ipergay-trial
#19
Julien Fonsart, Sentob Saragosti, Milad Taouk, Gilles Peytavin, Lane Bushman, Isabelle Charreau, Allan Hance, Lauriane Goldwirt, Stéphane Morel, Fabrizio Mammano, Bénédicte Loze, Catherine Capitant, François Clavel, Nadia Mahjoub, Laurence Meyer, Peter L Anderson, Constance Delaugerre, Jean-Michel Molina
OBJECTIVES: In the ANRS IPERGAY pre-exposure prophylaxis (PrEP) trial, a single dose of tenofovir disoproxil fumarate and emtricitabine was taken orally 2-24 h before sexual intercourse. A sub-study was conducted to assess the pharmacokinetics of tenofovir and emtricitabine in blood, saliva and rectal tissue following this initial oral intake. METHODS: Plasma, PBMC, saliva and rectal tissue sampling was performed over 24 h in 12 seronegative men before enrolment in the ANRS IPERGAY trial, following a single dose of 600 mg tenofovir disoproxil fumarate/400 mg emtricitabine...
September 28, 2016: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/28073847/identification-of-ccr2-and-cd180-as-robust-pharmacodynamic-tumor-and-blood-biomarkers-for-clinical-use-with-brd4-bet-inhibitors
#20
Tammie C Yeh, Greg O'Connor, Philip Petteruti, Austin Dulak, Maureen Hattersley, J Carl Barrett, Huawei Chen
PURPOSE: AZD5153 is a novel BRD4/BET inhibitor with a distinctive bivalent bromodomain binding mode. To support its clinical development, we identified pharmacodynamic (PD) biomarkers for use in clinical trials to establish target engagement. EXPERIMENTAL DESIGN: CCR2 and CD180 mRNAs, initially identified from whole transcriptome profiling, were further evaluated by quantitative PCR in hematologic cell lines, xenografts, and whole blood from rat, healthy volunteers, and patients with cancer...
January 10, 2017: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
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