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https://www.readbyqxmd.com/read/28231276/alterations-in-cellular-pharmacokinetics-and-pharmacodynamics-of-elvitegravir-in-response-to-ethanol-exposure-in-hiv-1-infected-monocytic-u1-cells
#1
Narasimha M Midde, Namita Sinha, Pradeep B Lukka, Bernd Meibohm, Santosh Kumar
Ethanol consumption is negatively associated with antiretroviral therapy (ART) adherence and general health in HIV positive individuals. Previously, we demonstrated ethanol-mediated alterations to metabolism of elvitegravir (EVG) in human liver microsomes. In the current study, we investigated ethanol influence on the pharmacokinetic and pharmacodynamic interactions of EVG in HIV infected monocytic (U1) cells. U1 cells were treated with 5 μM EVG, 2 μM Cobicistat (COBI), a booster drug, and 20 mM ethanol for up to 24 hours...
2017: PloS One
https://www.readbyqxmd.com/read/28231247/favipiravir-pharmacokinetics-in-ebola-infected-patients-of-the-jiki-trial-reveals-concentrations-lower-than-targeted
#2
Thi Huyen Tram Nguyen, Jérémie Guedj, Xavier Anglaret, Cédric Laouénan, Vincent Madelain, Anne-Marie Taburet, Sylvain Baize, Daouda Sissoko, Boris Pastorino, Anne Rodallec, Géraldine Piorkowski, Sara Carazo, Mamoudou N Conde, Jean-Luc Gala, Joseph Akoi Bore, Caroline Carbonnelle, Frédéric Jacquot, Hervé Raoul, Denis Malvy, Xavier de Lamballerie, France Mentré
BACKGROUND: In 2014-2015, we assessed favipiravir tolerance and efficacy in patients with Ebola virus (EBOV) disease (EVD) in Guinea (JIKI trial). Because the drug had never been used before for this indication and that high concentrations of the drugs were needed to achieve antiviral efficacy against EBOV, a pharmacokinetic model had been used to propose relevant dosing regimen. Here we report the favipiravir plasma concentrations that were achieved in participants in the JIKI trial and put them in perspective with the model-based targeted concentrations...
February 23, 2017: PLoS Neglected Tropical Diseases
https://www.readbyqxmd.com/read/28231003/utilization-of-gastrointestinal-simulator-gis-an-in-vivo-predictive-dissolution-methodology-coupled-with-computational-approach-to-forecast-oral-absorption-of-dipyridamole
#3
Kazuki Matsui, Yasuhiro Tsume, Susumu Takeuchi, Amanda Searls, Gordon L Amidon
Weakly basic drugs exhibit a pH-dependent dissolution profile in the gastrointestinal (GI) tract, making it difficult to predict their oral absorption profile. The aim of this study was to investigate the utility of the Gastrointestinal Simulator (GIS), a novel in vivo predictive dissolution (iPD) methodology, in predicting the in vivo behavior of the weakly basic drug, dipyridamole, when coupled with in silico analysis. The GIS is a multi-compartmental dissolution apparatus, which represents physiological gastric emptying in the fasted state...
February 23, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28230619/population-pharmacokinetics-of-topiramate-in-japanese-pediatric-and-adult-patients-with-epilepsy-using-routinely-monitored-data
#4
Masato Takeuchi, Ikuko Yano, Satoko Ito, Mitsuhiro Sugimoto, Shota Yamamoto, Atsushi Yonezawa, Akio Ikeda, Kazuo Matsubara
BACKGROUND: Topiramate is a second-generation antiepileptic drug used as monotherapy and adjunctive therapy in adults and children with partial seizures. A population pharmacokinetic analysis was performed to improve the topiramate dosage adjustment for individualized treatment. METHODS: Patients whose steady-state serum concentration of topiramate was routinely monitored at Kyoto University Hospital from April 2012 to March 2013 were included in the model-building data...
February 20, 2017: Therapeutic Drug Monitoring
https://www.readbyqxmd.com/read/28230618/biopharmaceuticals-reference-products-and-biosimilars-to-treat-inflammatory-diseases
#5
Ann Gils, Antonio Bertolotto, Denis Mulleman, Theodora Bejan-Angoulvant, Paul J Declerck
Biopharmaceuticals are primarily therapeutic proteins developed to perform specific functions by acting on the disease pathophysiology. Compared to low molecular chemically synthesized drugs, production of biopharmaceuticals is much more complex and routes of administration and pharmacokinetics differ. Biopharmaceuticals are blockbusters in the treatment of inflammatory diseases such as psoriasis, multiple sclerosis, rheumatic diseases, and inflammatory bowel diseases, and the introduction of these drugs has revolutionized treatment...
February 20, 2017: Therapeutic Drug Monitoring
https://www.readbyqxmd.com/read/28230617/acute-kidney-injury-following-efavirenz-tenofovir-disoproxil-fumarate-emtricitabine-atripla%C3%A2-overdose
#6
Thomas Havenith, David Burger, Maarten Visschers, Jolanda Schippers, Astrid Oude Lashof
We describe a patient with acute renal failure and irreversible kidney damage after an overdose with the fixed dose combination of efavirenz/tenofovir disoproxil fumarate/emtricitabine (Atripla). The acute kidney injury was most probably caused by tenofovir. Efavirenz and emtricitabine seemed relatively safe in overdose. The pharmacokinetics in overdose of all three drugs and the effect of hemodialysis on the tenofovir clearance were studied by measuring the plasma concentrations and by the use of clinical pharmacokinetic software...
February 20, 2017: Therapeutic Drug Monitoring
https://www.readbyqxmd.com/read/28230269/antigenic-burden-and-serum-igg-concentrations-influence-rituximab-pharmacokinetics-in-rheumatoid-arthritis-patients
#7
Bertrand Lioger, Soujanya Ratna Edupuganti, Denis Mulleman, Christophe Passot, Céline Desvignes, Théodora Bejan-Angoulvant, Gilles Thibault, Valérie Gouilleux-Gruart, Julien Mélet, Gilles Paintaud, David Ternant
AIMS: Rituximab is a monoclonal antibody directed against CD20, which is approved in rheumatoid arthritis (RA). This study aimed at assessing the influence of CD19+ cell counts as target-antigen amount, and of immunoglobulin G (IgG) serum concentrations on rituximab pharmacokinetics in RA patients. METHODS: In a cohort of 64 RA patients who had received repetitive courses of rituximab, the influence of CD19+ cell count, IgG serum concentration, body surface area (BSA), sex, and disease activity score in 28 joints (DAS28) on rituximab pharmacokinetic parameters was assessed using a population pharmacokinetic analysis...
February 23, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28230262/evaluation-of-the-immunogenicity-of-the-dabigatran-reversal-agent-idarucizumab-during-phase-i-studies
#8
Stephen Norris, Steven Ramael, Ippei Ikushima, Wouter Haazen, Akiko Harada, Viktoria Moschetti, Susumu Imazu, Paul A Reilly, Benjamin Lang, Joachim Stangier, Stephan Glund
AIMS: Idarucizumab, a humanized monoclonal anti-dabigatran antibody fragment, is effective in emergency reversal of dabigatran anticoagulation. Pre-existing and treatment-emergent anti-idarucizumab antibodies (antidrug antibodies; ADA) may affect the safety and efficacy of idarucizumab. This analysis characterized the pre-existing and treatment-emergent ADA and assessed their impact on the pharmacokinetics and pharmacodynamics (PK/PD) of idarucizumab. METHODS: Data were pooled from three phase I, randomized, double-blind idarucizumab studies in healthy Caucasian; elderly, renally impaired subjects; and healthy Japanese subjects...
February 23, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28229809/pharmacokinetic-profiles-of-meloxicam-and-sustained-release-buprenorphine-in-prairie-dogs-cynomys-ludovicianus
#9
Cynthia D Cary Nicole L Lukovsky-Akhsanov Nadia F Gallardo-Romero Cassandra M Tansey Sharon D Ostergaard Willie D Taylor Jr Clint N Morgan Nathaniel Powell George W Lathrop And Christina L Hutson
In this study, we evaluated the pharmacokinetic profiles of meloxicam and sustained-release (SR) buprenorphine in prairiedogs. The 4 treatment groups were: low-dose meloxicam (0.2 mg/kg SC), high-dose meloxicam (4 mg/kg SC), low-dosebuprenorphine SR (0.9 mg/kg SC), and high-dose buprenorphine SR (1.2 mg/kg SC). The highest plasma concentrationsoccurred within 4 h of administration for both meloxicam treatment groups. The therapeutic range of meloxicam in prairiedogs is currently unknown. However, as compared with the therapeutic range documented in other species (0...
February 22, 2017: Journal of the American Association for Laboratory Animal Science: JAALAS
https://www.readbyqxmd.com/read/28229443/-desvenlafaxine-and-neuropathic-pain-additional-clinical-benefits-of-a-second-generation-serotonin-noradrenaline-reuptake-inhibitor
#10
REVIEW
A Alcantara-Montero
INTRODUCTION: Desvenlafaxine is the third antidepressant within the group of serotonin-norepinephrine reuptake inhibitors. The latest clinical practice guidelines consulted agree that tricyclic antidepressants, dual (venlafaxine/duloxetine) and gabapentin/pregabalin antiepileptics, are the first-line drugs in the treatment of neuropathic pain, being tramadol, lidocaine 5% patches and capsaicin 8% patches of second-line drugs, while strong opioids constitute a third line treatment. The interaction between the binomial pain and depression is very frequent, being the psychological complication more frequent in patients with chronic pain...
March 1, 2017: Revista de Neurologia
https://www.readbyqxmd.com/read/28229437/pharmacokinetic-modeling-of-11-c-flumazenil-kinetics-in-the-rat-brain
#11
Isadora Lopes Alves, David Vállez García, Andrea Parente, Janine Doorduin, Rudi Dierckx, Ana Maria Marques da Silva, Michel Koole, Antoon Willemsen, Ronald Boellaard
BACKGROUND: Preferred models for the pharmacokinetic analysis of [(11)C]flumazenil human studies have been previously established. However, direct translation of these models and settings to animal studies might be sub-optimal. Therefore, this study evaluates pharmacokinetic models for the quantification of [(11)C]flumazenil binding in the rat brain. Dynamic (60 min) [(11)C]flumazenil brain PET scans were performed in two groups of male Wistar rats (tracer dose (TD), n = 10 and pre-saturated (PS), n = 2)...
December 2017: EJNMMI Research
https://www.readbyqxmd.com/read/28229434/preclinical-pharmacokinetics-and-pharmacodynamics-of-pinometostat-epz-5676-a-first-in-class-small-molecule-s-adenosyl-methionine-competitive-inhibitor-of-dot1l
#12
Nigel J Waters
Acute leukemias bearing mixed lineage leukemia (MLL) rearrangements are aggressive diseases characterized by a poor overall prognosis despite multi-agent chemotherapy. Aberrant fusion proteins involving the MLL histone methyltransferase (HMT) lead to recruitment of DOT1L, to a multi-protein complex resulting in aberrant methylation of histone H3 lysine 79 at MLL target genes, and ultimately enhanced expression of critical genes for hematopoietic differentiation, including HOXA9 and MEIS1, and as such defines the established mechanism for leukemogenesis in MLL-rearrangement (MLL-r) leukemias...
February 22, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28229376/the-pharmacogenetics-of-tacrolimus-in-corticosteroid-sparse-pediatric-and-adult-kidney-transplant-recipients
#13
Mads Juul Madsen, Troels K Bergmann, Kim Brøsen, Helle Charlotte Thiesson
INTRODUCTION: Tacrolimus is a calcineurin inhibitor used as an immunosuppressant drug in solid organ transplantation, and is mainly metabolized by cytochrome P450 (CYP) 3A4 and CYP3A5. Studies have shown an association between the CYP3A5 genotype and tacrolimus dose-adjusted trough concentrations. Variants in the genes PPARA, POR and CYP3A4 have recently been shown to influence tacrolimus metabolism. Furthermore, pharmacokinetic interaction between corticosteroid treatment and tacrolimus has been shown...
February 22, 2017: Drugs in R&D
https://www.readbyqxmd.com/read/28229375/clinical-pharmacokinetics-of-ombitasvir
#14
REVIEW
Prajakta S Badri, Diana L Shuster, Sandeep Dutta, Rajeev M Menon
Ombitasvir is a potent, nonstructural protein 5A inhibitor of the hepatitis C virus (HCV) that is used in combination with other direct-acting antivirals for the treatment of chronic HCV infection. Ombitasvir is predominantly metabolized by amide hydrolysis followed by oxidative metabolism and is a substrate of P-glycoprotein. Ombitasvir displays linear pharmacokinetics with minimal accumulation and is eliminated via metabolism and biliary excretion. A negligible amount of unchanged drug is excreted in urine...
February 22, 2017: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/28229374/effect-of-short-term-fasting-on-systemic-cytochrome-p450-mediated-drug-metabolism-in-healthy-subjects-a-randomized-controlled-crossover-study-using-a-cocktail-approach
#15
Laureen A Lammers, Roos Achterbergh, Ron H N van Schaik, Johannes A Romijn, Ron A A Mathôt
BACKGROUND AND OBJECTIVE: Short-term fasting can alter drug exposure but it is unknown whether this is an effect of altered oral bioavailability and/or systemic clearance. Therefore, the aim of our study was to assess the effect of short-term fasting on oral bioavailability and systemic clearance of different drugs. METHODS: In a randomized, controlled, crossover trial, 12 healthy subjects received a single administration of a cytochrome P450 (CYP) probe cocktail, consisting of caffeine (CYP1A2), metoprolol (CYP2D6), midazolam (CYP3A4), omeprazole (CYP2C19) and warfarin (CYP2C9), on four occasions: an oral (1) and intravenous (2) administration after an overnight fast (control) and an oral (3) and intravenous (4) administration after 36 h of fasting...
February 22, 2017: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/28229162/pharmacokinetics-of-recombinant-human-soluble-thrombomodulin-in-disseminated-intravascular-coagulation-patients-with-acute-renal-dysfunction
#16
Mineji Hayakawa, Shigeki Kushimoto, Eizo Watanabe, Koji Goto, Yasushi Suzuki, Toru Kotani, Takeyuki Kiguchi, Tomoaki Yatabe, Jun Tagawa, Fumiyo Komatsu, Satoshi Gando
Recombinant human soluble thrombomodulin (ART-123) is a novel anticoagulant for patients with disseminated intravascular coagulation (DIC). It is widely used in clinical settings throughout Japan. Furthermore, a global Phase 3 study is currently being conducted. In healthy subjects, ART-123 is excreted mainly via the kidneys. Therefore, ART-123 dose decrease was recommended in DIC patients with severe renal dysfunction. However, the pharmacokinetics of ART-123 in DIC patients with severe acute renal dysfunction has not been elucidated...
February 23, 2017: Thrombosis and Haemostasis
https://www.readbyqxmd.com/read/28228617/silkworm-fungal-infection-model-for-identification-of-virulence-genes-in-pathogenic-fungus-and-screening-of-novel-antifungal-drugs
#17
Masaki Ishii, Yasuhiko Matsumoto, Ikuko Nakamura, Kazuhisa Sekimizu
The silkworm infection model has the potential to replace conventional animal models for evaluation of the efficacy and toxicity of investigational antifungal agents. Silkworms are relatively inexpensive, can be simply grown in large numbers and can be easily infected with pathogenic fungi, including mutant strains. Antifungal agents can then be injected into the silkworm either via the hemolymph to mimic intravenous administration or directly into the gut for oral administration, and their antifungal effect can be evaluated...
February 21, 2017: Drug Discoveries & Therapeutics
https://www.readbyqxmd.com/read/28228413/determination-of-human-hepatic-cyp2c8-and-cyp1a2-age-dependent-expression-to-support-human-health-risk-assessment-for-early-ages
#18
Gina Song, Xueying Sun, Ronald N Hines, D Gail McCarver, Brian G Lake, Thomas G Osimitz, Moire R Creek, Harvey J Clewell, Miyoung Yoon
Predicting age-specific metabolism is important for evaluating age-related drug and chemical sensitivity. Multiple cytochrome P450s (CYP) and carboxylesterase (CES) enzymes are responsible for human pyrethroid metabolism. Complete ontogeny data for each enzyme is needed to support in vitro to in vivo extrapolation (IVIVE). This study was designed to determine age-dependent human hepatic CYP2C8 expression, for which only limited ontogeny data are available, and to further define CYP1A2 ontogeny. CYP2C8 and 1A2 protein levels were measured by quantitative Western blotting using liver microsomal samples prepared from 222 subjects with ages ranging from 8 weeks gestation to 18 years after birth...
February 22, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28228362/development-of-mbri-001-a-deuterium-substituted-plinabulin-derivative-as-a-potent-anti-cancer-agent
#19
Zhongpeng Ding, Hejuan Cheng, Shixiao Wang, Yingwei Hou, Jianchun Zhao, Huashi Guan, Wenbao Li
Plinabulin, a drug targeting microtubule of cancer cells, has been currently tried in its phase III clinical study. However, low efficacy caused by poor pharmacokinetic (PK) properties has been considered to be the main obstacle to approved by the Food and Drug Administration. Herein, we introduced a deuterium atom as an isostere in its structure to become a new compound named (MBRI-001, No. 9 in a series of deuterium-substituted compounds). The structure of MBRI-001 was characterized by HRMS, NMR, IR and a single crystal analysis...
February 3, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28228077/antioxidant-nanoplatforms-for-dermal-delivery-melatonin
#20
Aroha Belen Sánchez Milán, Ana C Calpena Campmany, Beatriz Clares Naveros
Melatonin (MLT) is emerging as a promising therapeutic agent, mainly due to its role as antioxidant. Substantial evidences show that melatonin is potentially effective on a variety of diseases as cancer, inflammation and neurodegenerative diseases. The excellent antioxidant capacity with pharmacokinetics characteristics and the emerging search for new pharmaceutical nanotechnology based systems, make it particularly attractive to elaborate nanoplatforms based on MLT for biomedical or cosmetic dermal applications...
February 22, 2017: Current Drug Metabolism
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