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https://www.readbyqxmd.com/read/29909577/population-pharmacokinetic-model-for-tumescent-lidocaine-in-women-undergoing-breast-cancer-surgery
#1
Camille Riff, Aurélie Bourgoin, Amelie Marsot, Laurent Allanioux, Marc Leone, Olivier Blin, Romain Guilhaumou
PURPOSE: Tumescent lidocaine anesthesia (TLA) is an opportunity to perform mastectomy for breast cancer without general anesthesia in elderly women. Few reports are available on the pharmacokinetics of lidocaine in a context of TLA during a unilateral mastectomy. The aim of this study was to describe lidocaine pharmacokinetics in elderly women undergoing breast cancer surgery after TLA and to explore the risk of the toxicity of this technique. METHODS: A prospective study was conducted to examine the pharmacokinetics of lidocaine in women undergoing TLA...
June 16, 2018: European Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29909549/pharmacokinetics-of-ombitasvir-paritaprevir-ritonavir-and-dasabuvir-in-healthy-chinese-subjects-and-hcv-gt1b-infected-chinese-south-korean-and-taiwanese-patients
#2
Jiuhong Zha, Bifeng Ding, Haoyu Wang, Weihan Zhao, Chen Yu, Katia Alves, Niloufar Mobashery, Yan Luo, Rajeev M Menon
BACKGROUND/PURPOSE: The 3 direct-acting antiviral (3D) regimen of ombitasvir/paritaprevir/ritonavir plus dasabuvir has recently been approved in several Asian geographic regions for the treatment of hepatitis C virus (HCV) genotype (GT) 1 infection. The pharmacokinetics of the components of the 3D regimen with or without ribavirin were evaluated in healthy Chinese subjects and HCV GT1b-infected Chinese, South Korean, and Taiwanese patients, with or without cirrhosis, to determine how the drug exposures in Asian populations compare with historical data in Western populations...
June 16, 2018: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/29909433/pharmacokinetics-of-fentanyl-sublingual-spray-in-opioid-na%C3%A3-ve-participants-results-of-a-phase-1-multiple-ascending-dose-study
#3
Richard L Rauck, D Alexander Oh, Neil Singla, Christian Koch, Neha Parikh, Srinivas Nalamachu, Jin Yu, Steven James
BACKGROUND AND OBJECTIVES: Fentanyl sublingual spray may be a viable alternative to intravenous (IV) opioids for the treatment of acute pain. As patients with acute pain may include those who have limited prior exposure to opioids, this phase 1, open-label, randomized, multiple ascending-dose study was conducted to assess the pharmacokinetics, pharmacodynamics, safety, and tolerability of multiple doses of fentanyl sublingual spray in opioid-naïve participants. This article primarily reports the pharmacokinetics results...
June 16, 2018: Clinical Drug Investigation
https://www.readbyqxmd.com/read/29909432/pharmacokinetics-of-a-novel-sildenafil-orodispersible-film-administered-by-the-supralingual-and-the-sublingual-route-to-healthy-men
#4
Luca Loprete, Chiara Leuratti, Valeria Frangione, Milko Radicioni
BACKGROUND: Sildenafil was the first selective drug available on the market as oral therapy for erectile dysfunction (ED). A novel sildenafil orodispersible film (ODF) for ED treatment, containing sildenafil citrate, has recently been marketed. OBJECTIVES: Study objective was to investigate sildenafil bioavailability of the novel ODF formulation after sublingual and supralingual administration. METHODS: In this randomised, two-way cross-over study, 12 healthy male volunteers received a single 50 mg sildenafil dose by the sublingual and supralingual administration routes...
June 16, 2018: Clinical Drug Investigation
https://www.readbyqxmd.com/read/29909029/investigation-of-drug-delivery-in-rats-via-subcutaneous-injection-case-study-of-pharmacokinetic-modeling-of-suspension-formulations
#5
Po-Chang Chiang, Karthik Nagapudi, Peter W Fan, Jia Liu
With the rising cost of drug research, "do more with less" has become a new emphasis in the pharmaceutical industry. Consequently, the early analysis of PK/PD, efficacy, and safety parameters for a new drug target is critical for ensuring informed decision-making as soon as possible during the drug discovery process. When ADME properties of compounds are suboptimalwhich is especially true during the early stages of drug discovery, obtaining the desired exposure can be challenging via the most common routes (oral, IV)...
June 14, 2018: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29908917/potential-effectiveness-of-long-acting-injectable-pre-exposure-prophylaxis-for-hiv-prevention-in-men-who-have-sex-with-men-a-modelling-study
#6
Brandon D L Marshall, William C Goedel, Maximilian R F King, Alyson Singleton, David P Durham, Philip A Chan, Jeffrey P Townsend, Alison P Galvani
BACKGROUND: Oral pre-exposure prophylaxis (PrEP) prevents HIV infection in men who have sex with men (MSM); however, adherence is an ongoing concern. Long-acting injectable PrEP is being tested in phase 3 trials and could address challenges associated with adherence. We examined the potential effectiveness of long-acting injectable PrEP compared with oral PrEP in MSM. METHODS: We used an agent-based model to simulate HIV transmission in a dynamic network of 11 245 MSM in Atlanta, GA, USA...
June 13, 2018: Lancet HIV
https://www.readbyqxmd.com/read/29908846/suspect-and-untargeted-screening-of-bisphenol-s-metabolites-produced-by-in-vitro-human-liver-metabolism
#7
Celine Gys, Ana Kovačič, Carolin Huber, Foon Yin Lai, Ester Heath, Adrian Covaci
Bisphenol S (BPS) is increasingly used as substitute for bisphenol A, resulting in higher potential of human exposure to this compound. Yet, information on the human metabolism of BPS is limited. Hence, current biomonitoring studies rely only on the measurement of BPS itself, leading to a potential underestimation of assessing human exposure to this emerging contaminant. The aims of this study were to investigate the in vitro metabolic pathways of BPS using human liver microsomes and cytosol fractions and propose in vitro metabolites for evaluation in pharmacokinetics studies...
June 14, 2018: Toxicology Letters
https://www.readbyqxmd.com/read/29908755/characterization-of-butyrylcholinesterase-from-porcine-milk
#8
Ashima Saxena, Tatyana Belinskaya, Lawrence M Schopfer, Oksana Lockridge
Human butyrylcholinesterase (HuBChE) is under development for use as a pretreatment antidote against nerve agent toxicity. Animals are used to evaluate the efficacy of HuBChE for protection against organophosphorus nerve agents. Pharmacokinetic studies of HuBChE in minipigs showed a mean residence time of 267 h, similar to the half-life of HuBChE in humans, suggesting a high degree of similarity between BChE from 2 sources. Our aim was to compare the biochemical properties of PoBChE purified from porcine milk to HuBChE purified from human plasma...
June 14, 2018: Archives of Biochemistry and Biophysics
https://www.readbyqxmd.com/read/29908469/simultaneous-determination-of-six-bioactive-saponins-from-rhizoma-panacis-japonici-in-rat-plasma-by-uhplc-ms-ms-application-to-a-pharmacokinetic-study
#9
Hong Zheng, Feng Qiu, Hui Zhao, Jie Chen, Lei Wang, Haiyan Zou
A specific, sensitive and rapid ultra high performance liquid chromatography-tandem mass spectrometric (UHPLC-MS/MS) method was developed and validated for simultaneous determination of six major bioactive constituents in Rhizoma Panacis Japonici (RPJ), including oleanolic acid-type chikusetsusaponin V, IV, hemsgiganoside B, damarane-type ginsenoside Rb1, Rg1 and Re in rat plasma, using estazolam as the internal standard (IS). Plasma samples were pretreated with methanol/acetonitrile (1:1, V/V) for protein precipitation...
June 7, 2018: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/29908468/first-report-on-the-pharmacokinetic-profile-of-nimbolide-a-novel-anticancer-agent-in-oral-and-intravenous-administrated-rats-by-lc-ms-method
#10
Shandilya Mahamuni Baira, Amit Khurana, Jaganmohan Somagoni, R Srinivas, Chandraiah Godugu, M V N Kumar Talluri
Nimbolide is a novel, natural compound with promising potential as a drug candidate for anticancer activity. It is isolated from the Indian traditional medicinal plant Azadirachta indica popularly known as neem. The present study was undertaken to explore the oral bioavailability and pharmacokinetic characteristics of nimbolide in rats using the LC/QTOF/MS method. A simple protein precipitation method using acetonitrile was employed for extracting nimbolide from rat plasma. The chromatographic separation of nimbolide and the internal standard (regorafenib) was attained on an Aquity BEH C18 column (100 × 2...
June 2, 2018: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/29908443/novel-pyrimidinic-selenourea-induces-dna-damage-cell-cycle-arrest-and-apoptosis-in-human-breast-carcinoma
#11
Flavio A R Barbosa, Tâmila Siminski, Rômulo F S Canto, Gabriela M Almeida, Nádia S R S Mota, Fabiana Ourique, Rozangela Curi Pedrosa, Antonio Luiz Braga
Novel pyrimidinic selenoureas were synthesized and evaluated against tumour and normal cell lines. Among these, the compound named 3j initially showed relevant cytotoxicity and selectivity for tumour cells. Three analogues of 3j were designed and synthesized keeping in view the structural requirements of this compound. Almost all the tested compounds displayed considerable cytotoxicity. However, 8a, one of the 3j analogues, was shown to be highly selective and cytotoxic, especially for breast carcinoma cells (MCF-7) (IC50  = 3...
June 11, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29908439/recent-advances-in-the-rational-design-and-development-of-lim-kinase-inhibitors-are-not-enough-to-enter-clinical-trials
#12
REVIEW
Fabrizio Manetti
LIM kinases are involved in various pathophysiological processes that depend on actin organization. Alteration of microtubule dynamics by LIMK dysregulation is in fact related to tumor progression and metastasis, viral infection, and ocular diseases, such as glaucoma. As a consequence, many efforts have been done in recent years to rationally design small molecules able to inhibit LIMK activity selectively, without affecting other kinases. As a result, compounds optimized in terms of binding affinity and pharmacokinetic parameters have been discovered, that however failed to access clinical trials...
June 8, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29908424/high-dispersed-phyto-phospholipid-complex-tpgs-1000-with-mesoporous-silica-to-enhance-oral-bioavailability-of-tanshinol
#13
Mengmeng Yang, Ting Chen, Lingchong Wang, Lihua Chen, Junsong Li, Liuqing Di
Phenolic acids are widely distributed in the plant kingdom and possess a broad spectrum of pharmacological activity. However, low oral bioavailability restricts their application. In this study, a high dispersed phyto- phospholipid complex with mesoporous silica containing TPGS 1000 (TPC-SD) was fabricated using Tanshinol (Tan) as model drug. Phospholipid complex (PC) was employed to improve the n-octanol/water partition coefficient (log P) and apparent permeability coefficients (Papp ) of Tan. Mesoporous silica was used to compensate for the negative effects of phospholipid on drug's dispersion and dissolution owing to its viscosity and poor water-solubility...
June 9, 2018: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/29908414/synthesis-and-photophysical-properties-of-deuteration-of-pirfenidone
#14
Qiuju Yin, Yujie Chen, Meng Zhou, Xiangsheng Jiang, Junjun Wu, Yang Sun
In order to improve the metabolism of pirfenidone (5-methyl-1-phenylpyridin-2-one, PFD), the methyl-deuterated version of pirfenidone via the substitution of hydrogen (H) at C-5 by its isotope deuterium (D, 5D-PFD) was synthesized and its photophysical properties were investigated. The negative solvatochrom was observed in absorption and fluorescence spectra with increasing solvent polarity, which implied that intermolecular charge transfer (ICT) involved n → π* transition for both of PFD and 5D-PFD...
June 7, 2018: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
https://www.readbyqxmd.com/read/29908332/enhanced-nanoparticle-uptake-into-virus-infected-cells-could-nanoparticles-be-useful-in-antiviral-therapy
#15
Yasmin Abo-Zeid, Richard A Urbanowicz, Brian J Thomson, William L Irving, Alexander W Tarr, Martin C Garnett
Virus infections cause diseases of different severity ranged from mild infection e.g. common cold into life threating diseases e.g. Human Immunodeficiency virus (HIV), Hepatitis B. Virus infections represent 44% of newly emerging infections. Although there are many efficient antiviral agents, they still have drawbacks due to accumulation at off target organs and developing of virus resistance due to virus mutation. Therefore, developing a delivery system that can selectively target drug into affected organs and avoid off target accumulation would be a highly advantageous strategy to improve antiviral therapy...
June 13, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29908331/all-atomistic-molecular-dynamics-aa-md-studies-and-pharmacokinetic-performance-of-pamam-dendrimer-furosemide-delivery-systems
#16
Daniel P Otto, Melgardt M de Villiers
Improvement of problematic dissolution and solubility properties of a model drug, furosemide, was investigated for poly(amidoamine) (PAMAM) dendrimer complexes of the drug. Full and half generation dendrimers with amino and ester terminals respectively, were studied. In vitro release performance of these complexes was investigated at drug loads ranging 5-60% using simulated gastric fluids. Full generation dendrimers accommodated higher drug loads, outperformed half-generation complexes, and free drug. Pharmacokinetic studies in rats indicated that the dendrimer complexes markedly improved in the bioavailability of the drug compared to the unformulated drug...
June 13, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29908205/real-time-and-in-vivo-pharmaceutical-and-environmental-studies-with-spidermass-instrument
#17
B Fatou, P Saudemont, M Duhamel, M Ziskind, C Focsa, M Salzet, I Fournier
Remote Infrared Matrix Assisted Laser Desorption Ionization (Remote IR MALDI) system (SpiderMass) with endogenous water as matrix allows to perform real-time DMPK in vivo. In this work, SpiderMass was used to analyze the impact on metabolite production or release of invalidated pro-protein PC1/3 macrophages by Short RNA (shRNA) versus scramble shRNA with Paclitaxel. Time course in vivo experiments were then performed on the inner and outer faces of patients' forearms or comedo treated with Melascreen (Ducray) containing ascorbyl glucoside...
June 13, 2018: Journal of Biotechnology
https://www.readbyqxmd.com/read/29908155/pharmacokinetics-of-continuous-infusion-beta-lactams-in-the-treatment-of-acute-pulmonary-exacerbations-in-adult-cystic-fibrosis-patients
#18
Lisa T Hong, Theodore G Liou, Rishi Deka, Jordan B King, Vanessa Stevens, David C Young
BACKGROUND: Several clinical trials have demonstrated the efficacy of continuous infusion (CI) beta-lactam (BL) antibiotics in cystic fibrosis (CF) patients; however, little is known regarding pharmacokinetic changes during treatment of an acute pulmonary exacerbation (APE). Identifying and understanding these changes may assist in optimizing antibiotic dosing during APE treatment. METHODS: This study is a retrospective cohort study of 162 adult CF patients admitted to the University of Utah Hospital between January 1, 2008 and May 15, 2014 for treatment of an APE with both a CI BL and intravenous tobramycin...
June 13, 2018: Chest
https://www.readbyqxmd.com/read/29908138/interaction-of-pirenzepine-with-bovine-serum-albumin-and-effect-of-%C3%AE-cyclodextrin-on-binding-a-biophysical-and-molecular-docking-approach
#19
Yusra Rahman, Shumaila Afrin, Mohammad Tabish
Studying the interaction of therapeutic molecules with serum albumin is important to understand their biopharmaceutics, pharmacokinetics and toxicity as well as their relation with the structure and function of protein. The biomolecular interaction of an anti-spasmodic drug, pirenzepine with bovine serum albumin (BSA) was investigated using multi-spectroscopic, calorimetric and docking studies. Fluorescence quenching of BSA on interaction with pirenzepine revealed the static mode of quenching. Pirenzepine exhibited a moderate binding to serum albumin with the binding constant value in the order of 104  M-1 ...
June 13, 2018: Archives of Biochemistry and Biophysics
https://www.readbyqxmd.com/read/29908131/low-body-mass-index-is-a-risk-factor-for-hyperkalaemia-associated-with-angiotensin-converting-enzyme-inhibitors-and-angiotensin-ii-receptor-blockers-treatments
#20
T Hirai, R Yamaga, A Fujita, T Itoh
WHAT IS KNOWN AND OBJECTIVE: Angiotensin converting enzyme inhibitors (ACEI) and angiotensin II receptor blockers (ARB) represent the cornerstones of hypertension and congestive heart failure treatment. Risk factors for hyperkalaemia associated with ACEI and ARB are chronic kidney disease and concomitant medications which increase serum potassium level. Body mass index (BMI) also affects pharmacokinetics of ACEI and ARB and potassium disposition. We evaluated the relationship between BMI and hyperkalaemia associated with ACEI and ARB treatments...
June 16, 2018: Journal of Clinical Pharmacy and Therapeutics
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