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https://www.readbyqxmd.com/read/29036802/pharmacosimulation-of-interruptions-and-its-solution-in-intravenous-administration-of-cangrelor
#1
Maryna Masyuk, Nadia Heramvand, Johanna M Muessig, Amir M Nia, Amin Polzin, Markus Kollmann, Malte Kelm, Christian Jung
BACKGROUNDCangrelor is an intravenous adenosine diphosphate (ADP) P2Y12 receptor antagonist, which has to be administered as a bolus followed by immediate infusion. Nevertheless, in clinical routine deviations from the correct practice, such as delayed infusion onset or interruptions during infusion, may occur. OBJECTIVE: The objective of the present study was to investigate the impact of administration delays on cangrelor concentration in a pharmacological simulation setting and to give possible solutions for the clinical practice...
October 7, 2017: Clinical Hemorheology and Microcirculation
https://www.readbyqxmd.com/read/29036723/converting-from-transdermal-to-buccal-formulations-of-buprenorphine-a-pharmacokinetic-meta-model-simulation-in-healthy-volunteers
#2
Tony Priestley, Arvind K Chappa, Diane R Mould, Richard N Upton, Neil Shusterman, Steven Passik, Vicente J Tormo, Stephen Camper
OBJECTIVE:  To develop a model to predict buprenorphine plasma concentrations during transition from transdermal to buccal administration. DESIGN:  Population pharmacokinetic model-based meta-analysis of published data. METHODS:  A model-based meta-analysis of available buprenorphine pharmacokinetic data in healthy adults, extracted as aggregate (mean) data from published literature, was performed to explore potential conversion from transdermal to buccal buprenorphine...
September 29, 2017: Pain Medicine: the Official Journal of the American Academy of Pain Medicine
https://www.readbyqxmd.com/read/29036256/pharmacokinetic-comparison-of-once-daily-topical-minocycline-foam-4-vs-oral-minocycline-for-moderate-to-severe-acne
#3
Terry M Jones, Herman Ellman, Tina deVries
OBJECTIVE: To characterize minocycline pharmacokinetics and relative bioavailability following multiple-dose topical administration of minocycline hydrochloride (HCl) foam 4% (FMX101 4%) as compared with single-dose oral administration of minocycline HCl extended-release tablets (Solodyn®) in subjects with moderate-to-severe acne. METHODS: A Phase 1, single-center, nonrandomized, open-label, active-controlled, 2-period, 2-treatment crossover clinical study. The study included 30 healthy adults (mean age, 22...
October 1, 2017: Journal of Drugs in Dermatology: JDD
https://www.readbyqxmd.com/read/29035675/practical-considerations-in-clinical-strategy-to-support-the-development-of-injectable-drug-device-combination-products-for-biologics
#4
Zhaoyang Li, Rachael Easton
The development of an injectable drug-device combination (DDC) product for biologics is an intricate and evolving process that requires substantial investments of time and money. Consequently, the commercial dosage form(s) or presentation(s) are often not ready when pivotal trials commence, and it is common to have drug product changes (manufacturing process or presentation) during clinical development. A scientifically sound and robust bridging strategy is required in order to introduce these changes into the clinic safely...
October 16, 2017: MAbs
https://www.readbyqxmd.com/read/29035637/design-and-characterization-of-mp0250-a-tri-specific-anti-hgf-anti-vegf-darpin%C3%A2-drug-candidate
#5
H Kaspar Binz, Talitha R Bakker, Douglas J Phillips, Andreas Cornelius, Christof Zitt, Thomas Göttler, Gabriel Sigrist, Ulrike Fiedler, Savira Ekawardhani, Ignacio Dolado, Johan Abram Saliba, Gaby Tresch, Karl Proba, Michael T Stumpp
MP0250 is a multi-domain drug candidate currently being tested in clinical trials for the treatment of cancer. It comprises one anti-vascular endothelial growth factor-A (VEGF-A), one anti-hepatocyte growth factor (HGF), and two anti-human serum albumin (HSA) DARPin® domains within a single polypeptide chain. While there is first clinical validation of a single-domain DARPin® drug candidate, little is known about DARPin® drug candidates comprising multiple domains. Here, we show that MP0250 can be expressed at 15 g/L in soluble form in E...
October 16, 2017: MAbs
https://www.readbyqxmd.com/read/29035574/a-6-month-open-label-extension-study-of-vortioxetine-in-pediatric-patients-with-depressive-or-anxiety-disorders
#6
Robert L Findling, Adelaide S Robb, Melissa P DelBello, Michael Huss, Nora K McNamara, Elias H Sarkis, Russell E Scheffer, Lis H Poulsen, Grace Chen, Ole M Lemming, Philippe Auby
OBJECTIVES: In this 6-month open-label extension (OLE) of NCT01491035 (a 14-day, open-label, pharmacokinetic/safety lead-in study), the long-term safety and tolerability of vortioxetine (5-20 mg/day) were investigated in children and adolescents with a DSM-IV-TR™ diagnosis of depressive or anxiety disorder in the United States or Germany. The study also was designed to provide data to inform dose selection and titration in future pediatric studies with vortioxetine. METHODS: Safety evaluations included spontaneously reported adverse events (AEs), the Columbia Suicide Severity Rating Scale (C-SSRS), and the Pediatric Adverse Events Rating Scale (PAERS; clinician administered)...
October 16, 2017: Journal of Child and Adolescent Psychopharmacology
https://www.readbyqxmd.com/read/29035547/pharmacokinetics-and-pharmacodynamics-of-the-triterpenoid-ursolic-acid-in-regulating-the-anti-oxidant-anti-inflammatory-and-epigenetic-gene-responses-in-rat-leukocytes
#7
Chengyue Zhang, Chao Wang, Wenji Li, Renyi Wu, Yue Guo, David Cheng, Yuqing Yang, Ioannis P Androulakis, Ah-Ng Kong
The triterpenoid ursolic acid (UA) has been proposed as a potential cancer chemopreventive agent in many preclinical and clinical studies. In the present work, we aimed to characterize the pharmacokinetics (PK) of UA and to quantitatively assess the anti-oxidative and anti-inflammatory effects of UA, which are potentially linked to its chemopreventive efficacy. UA was administered intravenously (i.v., 20 mg/kg) or by oral gavage (100 mg/kg) to male Sprague-Dawley rats, and blood samples were collected at a series of designated time points...
October 16, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/29035537/discovery-of-a-novel-piperidine-based-inhibitor-of-cholesteryl-ester-transfer-protein-cetp-that-retains-activity-in-hypertriglyceridemic-plasma
#8
Ken Yamada, Margaret Brousseau, Wataru Honma, Akiko Iimura, Hidetomo Imase, Yuki Iwaki, Toshio Kawanami, Daniel LaSala, Guiqing Liang, Hironobu Mitani, Kazuhiko Nonomura, Osamu Ohmori, Meihui Pan, Dean F Rigel, Ichiro Umemura, Kayo Yasoshima, Guoming Zhu, Muneto Mogi
Herein we describe the discovery and characterization of a novel, piperidine-based inhibitor of cholesteryl ester transfer protein (CETP) with a core structure distinct from other reported CETP inhibitors. A versatile synthesis starting from 4-methoxypyridine enabled an efficient exploration of the SAR, giving a lead molecule with potent CETP inhibition in human plasma. The subsequent optimization focused on improvement of pharmacokinetics and mitigation of off-target liabilities, such as CYP inhibition, whose improvement correlated with increased lipophilic efficiency...
October 16, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29035509/positron-emission-tomography-assessment-of-the-intranasal-delivery-route-for-orexin-a
#9
Genevieve C Van de Bittner, Kyle C Van de Bittner, Hsiao-Ying Wey, Wayne Rowe, Ramalinga Dharanipragada, Xiaoyou Ying, William Hurst, Andrew Giovanni, Kim Alving, Anurag Gupta, John Hoekman, Jacob M Hooker
Intranasal drug delivery is a non-invasive drug delivery route that can enhance systemic delivery of therapeutics with poor oral bioavailability by exploiting the rich microvasculature within the nasal cavity. The intranasal delivery route has also been targeted as a method for improved brain uptake of neurotherapeutics, with a goal of harnessing putative, direct nose-to-brain pathways. Studies in rodents, non-human primates and humans have pointed to the efficacy of intranasally delivered neurotherapeutics, while radiolabeling studies have analyzed brain uptake following intranasal administration...
October 16, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29035325/advanced-prodrug-strategies-in-nucleoside-and-non-nucleoside-antiviral-agents-a-review-of-the-recent-five-years
#10
REVIEW
Hanadi Sinokrot, Tasneem Smerat, Anas Najjar, Rafik Karaman
Background: Poor pharmacokinetic profiles and resistance are the main two drawbacks from which currently used antiviral agents suffer, thus make them excellent targets for research, especially in the presence of viral pandemics such as HIV and hepatitis C. Methods: The strategies employed in the studies covered in this review were sorted by the type of drug synthesized into ester prodrugs, targeted delivery prodrugs, macromolecular prodrugs, other nucleoside conjugates, and non-nucleoside drugs. Results: Utilizing the ester prodrug approach a novel isopropyl ester prodrug was found to be potent HIV integrase inhibitor...
October 16, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29034951/a-nanocrystal-based-formulation-improves-the-pharmacokinetic-performance-and-therapeutic-response-of-albendazole-in-dogs
#11
Alejandro Javier Paredes, Nicolás Litterio, Alicia Dib, Daniel Alberto Allemandi, Carlos Lanusse, Sergio Sánchez Bruni, Santiago Daniel Palma
OBJECTIVES: Here, we aimed to assess the pharmacokinetic performance and therapeutic response (anthelmintic efficacy) of an albendazole (ABZ) nano-sized formulation in dogs. METHODS: In the pharmacokinetic study, ABZ self-dispersible nanocrystals (SDNCS) and a control formulation were administered orally to healthy dogs (n = 6). The concentrations of the sulphoxide metabolite in plasma were determined by high-performance liquid chromatography. For the anthelmintic efficacy trial, SDNCS and a commercially available formulation of ABZ were given to naturally parasitised dogs...
October 16, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29034832/new-advances-in-atrial-fibrillation-management-the-role-of-apixaban
#12
Giuseppe Mc Rosano, Ilaria Spoletini, Walter Gianni, Cristiana Vitale
Prevention of stroke is a pivotal intervention in the management of patients with atrial fibrillation (AF) at increased risk of systemic embolism. Because of the difficulties of safely implementing Vitamin K Antagonists in all patients, there has been a growing interest in improving the pharmacological management of AF, with newer antithrombotic agents. The new oral anticoagulants (NOACs) have been developed to overcome the limitations and improve the efficacy of the conventional oral anticoagulant drugs. Among the NOACs, apixaban - a very specific antagonist of activated factor Xa - has pharmacokinetic and pharmacodynamic properties that allow significant efficacy in AF management...
October 12, 2017: Current Drug Targets
https://www.readbyqxmd.com/read/29034770/association-with-polymorphic-marmoset-cytochrome-p450-2c19-of-in-vivo-hepatic-clearances-of-chirally-separated-r-omeprazole-and-s-warfarin-using-individual-marmoset-physiologically-based-pharmacokinetic-models
#13
Takashi Kusama, Akiko Toda, Makiko Shimizu, Shotaro Uehara, Takashi Inoue, Yasuhiro Uno, Masahiro Utoh, Erika Sasaki, Hiroshi Yamazaki
1. Simulated clearances of R-warfarin and efavirenz were recently reported for individual cynomolgus monkeys genotyped for cytochrome P450 2C19 and 2C9, respectively. To expand and verify this modeling procedure, simulations of R/S-omeprazole and R/S-warfarin clearances after oral administrations in individual marmosets were performed using individual simplified physiologically based pharmacokinetic (PBPK) modeling consisting of gut, liver, and central compartments. 2. Pharmacokinetics of R/S-omeprazole were chirally determined using the previously reported plasma microsamples in this study...
October 16, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/29034063/targeting-orthotopic-gliomas-with-renal-clearable-luminescent-gold-nanoparticles
#14
Chuanqi Peng, Xiaofei Gao, Jing Xu, Bujie Du, Xuhui Ning, Shaoheng Tang, Robert M Bachoo, Mengxiao Yu, Woo-Ping Ge, Jie Zheng
A major clinical translational challenge in nanomedicine is the potential of toxicity associated with the uptake and long-term retention of non-degradable nanoparticles (NPs) in major organs. The development of inorganic NPs that undergo renal clearance could potentially resolve this significant biosafety concern. However, it remains unclear whether inorganic NPs that can be excreted by the kidneys remain capable of targeting tumors with poor permeability. Glioblastoma multiforme, the most malignant orthotopic brain tumor, presents a unique challenge for NP delivery because of the blood-brain barrier and robust blood-tumor barrier of reactive microglia and macroglia in the tumor microenvironment...
April 2017: Nano Research
https://www.readbyqxmd.com/read/29033901/monte-carlo-simulations-suggest-current-chlortetracycline-drug-residue-based-withdrawal-periods-would-not-control-antimicrobial-resistance-dissemination-from-feedlot-to-slaughterhouse
#15
Casey L Cazer, Lucas Ducrot, Victoriya V Volkova, Yrjö T Gröhn
Antimicrobial use in beef cattle can increase antimicrobial resistance prevalence in their enteric bacteria, including potential pathogens such as Escherichia coli. These bacteria can contaminate animal products at slaughterhouses and cause food-borne illness, which can be difficult to treat if it is due to antimicrobial resistant bacteria. One potential intervention to reduce the dissemination of resistant bacteria from feedlot to consumer is to impose a withdrawal period after antimicrobial use, similar to the current withdrawal period designed to prevent drug residues in edible animal meat...
2017: Frontiers in Microbiology
https://www.readbyqxmd.com/read/29033841/pharmacodynamic-evaluation-and-pk-pd-based-dose-prediction-of-tulathromycin-a-potential-new-indication-for-streptococcus-suis-infection
#16
Yu-Feng Zhou, Hui-Min Peng, Ming-Xiao Bu, Ya-Hong Liu, Jian Sun, Xiao-Ping Liao
Tulathromycin is the first member of the triamilide antimicrobial drugs that has been registered in more than 30 countries. The goal of this study is to provide a potential new indication of tulathromycin for Streptococcus suis infections. We investigated the pharmacokinetic and ex vivo pharmacodynamics of tulathromycin against experimental S. suis infection in piglets. Tulathromycin demonstrated a relatively long elimination half-life (74.1 h) and a mean residence time of 97.6 h after a single intramuscular administration...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29033568/in-vivo-evaluation-of-cetuximab-conjugated-poly-%C3%AE-glutamic-acid-docetaxel-nanomedicines-in-egfr-overexpressing-gastric-cancer-xenografts
#17
Maya Sreeranganathan, Saji Uthaman, Bruno Sarmento, Chethampadi Gopi Mohan, In-Kyu Park, Rangasamy Jayakumar
Epidermal growth factor receptor (EGFR), upregulated in gastric cancer patients, is an oncogene of interest in the development of targeted cancer nanomedicines. This study demonstrates in silico modeling of monoclonal antibody cetuximab (CET MAb)-conjugated docetaxel (DOCT)-loaded poly(γ-glutamic acid) (γ-PGA) nanoparticles (Nps) and evaluates the in vitro/in vivo effects on EGFR-overexpressing gastric cancer cells (MKN-28). Nontargeted DOCT-γ-PGA Nps (NT Nps: 110±40 nm) and targeted CET MAb-DOCT-γ-PGA Nps (T Nps: 200±20 nm) were prepared using ionic gelation followed by 1-Ethyl-3-(3-dimethyl aminopropyl)carbodiimide-N-Hydoxysuccinimide (EDC-NSH) chemistry...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/29033547/new-tablet-formulation-of-tacrolimus-with-smaller-interindividual-variability-may-become-a-better-treatment-option-than-the-conventional-capsule-formulation-in-organ-transplant-patients
#18
Yu Kyong Kim, Anhye Kim, Shin Jung Park, Howard Lee
To evaluate the pharmacokinetic (PK) and tolerability profiles of a new tablet formulation of tacrolimus and its interindividual variability (IIV) in the systemic exposure, and to compare them with those of the conventional capsule formulation, a randomized, open-label, two-treatment, two-period, two-sequence, crossover study was performed in 47 healthy males. The capsule or tablet formulation of tacrolimus was orally administered, and serial blood samples were collected up to 96 hours after dosing. Whole-blood tacrolimus concentration was determined using liquid chromatography-tandem mass spectrometry...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29032907/pharmaceuticals-in-water-fish-and-osprey-nestlings-in-delaware-river-and-bay
#19
Thomas G Bean, Barnett A Rattner, Rebecca S Lazarus, Daniel D Day, S Rebekah Burket, Bryan W Brooks, Samuel P Haddad, William W Bowerman
Exposure of wildlife to Active Pharmaceutical Ingredients (APIs) is likely to occur but studies of risk are limited. One exposure pathway that has received attention is trophic transfer of APIs in a water-fish-osprey food chain. Samples of water, fish plasma and osprey plasma were collected from Delaware River and Bay, and analyzed for 21 APIs. Only 2 of 21 analytes exceeded method detection limits in osprey plasma (acetaminophen and diclofenac) with plasma levels typically 2-3 orders of magnitude below human therapeutic concentrations (HTC)...
October 9, 2017: Environmental Pollution
https://www.readbyqxmd.com/read/29032696/impact-of-improving-postprandial-glycemic-control-with-intensifying-insulin-therapy-in-type-2-diabetes
#20
Tamer Yacoub
Worldwide, many people with type 2 diabetes are not at recommended glycemic targets and remain at increased risk of microvascular and macrovascular complications. Reaching recommended glycemic targets requires normalizing both fasting and postprandial glucose (PPG). For some patients, this will require addition of a prandial insulin delivered by injection to control PPG excursions. Evidence from epidemiological studies suggests an association between postprandial hyperglycemia and cardiovascular disease, and thus, expert guidelines recommend that treatment for elevated PPG not be delayed...
October 14, 2017: Postgraduate Medicine
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