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https://www.readbyqxmd.com/read/28441724/multiple-udp-glucuronosyltransferase-and-sulfotransferase-enzymes-are-responsible-for-the-metabolism-of-verproside-in-human-liver-preparations
#1
Ju-Hyun Kim, Deok-Kyu Hwang, Ju-Yeon Moon, Yongnam Lee, Ji Seok Yoo, Dae Hee Shin, Hye Suk Lee
Verproside, an active iridoid glycoside component of Veronica species, such as Pseudolysimachion rotundum var. subintegrum and Veronica anagallis-aquatica, possesses anti-asthma, anti-inflammatory, anti-nociceptive, antioxidant, and cytostatic activities. Verproside is metabolized into nine metabolites in human hepatocytes: verproside glucuronides (M1, M2) via glucuronidation, verproside sulfate (M3) via sulfation, picroside II (M4) and isovanilloylcatalpol (M5) via O-methylation, M4 glucuronide (M6) and M4 sulfate (M8) via further glucuronidation and sulfation of M4, and M5 glucuronide (M7) and M5 sulfate (M9) via further glucuronidation and sulfation of M5...
April 22, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28441541/molecular-interaction-of-2-4-diacetylphloroglucinol-dapg-with-human-serum-albumin-hsa-the-spectroscopic-calorimetric-and-computational-investigation
#2
Pragna Lakshmi T, Moumita Mondal, Krishna Ramadas, Sakthivel Natarajan
Drug molecule interaction with human serum albumin (HSA) affects the distribution and elimination of the drug. The compound, 2,4-diacetylphloroglucinol (DAPG) has been known for its antimicrobial, antiviral, antihelminthic and anticancer properties. However, its interaction with HSA is not yet reported. In this study, the interaction between HSA and DAPG was investigated through steady-state fluorescence, time-resolved fluorescence (TRF), circular dichroism (CD), Fourier transform infrared (FT-IR) spectroscopy, isothermal titration calorimetry (ITC), molecular docking and molecular dynamics simulation (MDS)...
April 18, 2017: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
https://www.readbyqxmd.com/read/28441481/best-practices-of-computer-aided-drug-discovery-cadd-lessons-learned-from-the-development-of-a-preclinical-candidate-for-prostate-cancer-with-a-new-mechanism-of-action
#3
Fuqiang Ban, Kush Dalal, Huifang Li, Eric LeBlanc, Paul S Rennie, Artem Cherkasov
Small-molecule drug design is a complex and iterative decision-making process relying on pre-existing knowledge and driven by experimental data. Low molecular weight chemicals represent an attractive therapeutic option as they are readily accessible to organic synthesis and can easily be characterized.1 Their potency, as well as pharmacokinetic and pharmacodynamic properties can be systematically and rationally investigated, and ultimately optimized via expert science behind medicinal chemistry and methods of computer-aided drug design (CADD)...
April 25, 2017: Journal of Chemical Information and Modeling
https://www.readbyqxmd.com/read/28441352/high-throughput-determination-of-sodium-danshensu-in-beagle-dogs-by-the-lcms-ms-method-employing-liquid-liquid-extraction-based-on-96-well-format-plates
#4
Jingjing Jiang, Xin Zhao, Xiuxiu Li, Shengyuan Wu, Shidan Yu, Yuefen Lou, Guorong Fan
Sodium Danshensu (sodium d-(+)-β-(3,4-dihydroxyphenyl) lactate), one of the water-soluble ingredients in Salvia miltiorrhiza, exhibits potent relaxation of the coronary artery and anticoagulation effection. A high-throughput, rapid, and sensitive method combining liquid chromatography with electrospray ionization tandem mass spectrometry to determine the sodium danshensu in beagle dog plasma was developed and validated, using gallic acid as an internal standard (IS). Acidified plasma samples were extracted using 96-well liquid-liquid extraction, and were eluted on a CNW Athena C18 column (3 μm, 2...
April 25, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28441162/managing-herpes-zoster-in-older-adults-prescribing-considerations
#5
Linda Beuscher, Geri Reeves, Debbie Harrell
NPs must be aware of special prescribing considerations for medication safety when managing the care of older adults with herpes zoster. Age-related physiologic changes of the body impact the pharmacokinetics and pharmacodynamics of antiviral and pain medications and can lead to potential adverse events.
April 24, 2017: Nurse Practitioner
https://www.readbyqxmd.com/read/28441076/a-novel-neuroprotective-small-molecule-for-glial-cell-derived-neurotrophic-factor-induction-and-photoreceptor-rescue
#6
Petr Baranov, Hong Lin, Kathryn McCabe, David Gale, Shenshen Cai, Burke Lieppman, Dwight Morrow, Phoebe Lei, Justin Liao, Michael Young
PURPOSE: Degenerative diseases of the retina, such as retinitis pigmentosa and age-related macular degeneration, are characterized by the irreversible loss of photoreceptors. Several growth factors, including glial cell derived neurotrophic factor (GDNF), have been shown to rescue retinal neurons. An alternative strategy to direct GDNF administration is its induction in host retina by small molecules. Here we studied the ability of a novel small molecule GSK812 to induce GDNF in vitro/in vivo and rescue photoreceptors...
April 25, 2017: Journal of Ocular Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28441044/pharmacokinetics-and-pharmacodynamics-of-midazolam-following-intravenous-and-intramuscular-administration-to-sheep
#7
Bradley T Simon, Elizabeth M Scallan, Odette O, Lisa Sams Ebner, Michelle N Cerullo, Christelle Follette, Sherry K Cox, Thomas J Doherty, Ignacio Lizarraga
OBJECTIVE To determine the pharmacokinetic and pharmacodynamic effects of midazolam following IV and IM administration in sheep. ANIMALS 8 healthy adult rams. PROCEDURES Sheep were administered midazolam (0.5 mg/kg) by the IV route and then by the IM route 7 days later in a crossover study. Physiologic and behavioral variables were assessed and blood samples collected for determination of plasma midazolam and 1-hydroxymidazolam (primary midazolam metabolite) concentrations immediately before (baseline) and at predetermined times for 1,440 minutes after midazolam administration...
May 2017: American Journal of Veterinary Research
https://www.readbyqxmd.com/read/28440955/phase-1-dose-escalation-study-of-mirvetuximab-soravtansine-imgn853-a-folate-receptor-%C3%AE-targeting-antibody-drug-conjugate-in-patients-with-solid-tumors
#8
Kathleen N Moore, Hossein Borghaei, David M O'Malley, Woondong Jeong, Shelly M Seward, Todd M Bauer, Raymond P Perez, Ursula A Matulonis, Kelli L Running, Xiaoyan Zhang, Jose F Ponte, Rodrigo Ruiz-Soto, Michael J Birrer
BACKGROUND: Mirvetuximab soravtansine (IMGN853) is an antibody-drug conjugate that selectively targets folate receptor α (FRα). In this phase 1 dose-escalation study, the authors investigated IMGN853 in patients with FRα-positive solid tumors. METHODS: Patients received IMGN853 on day 1 of a 21-day cycle (once every 3 weeks dosing), with cycles repeated until patients experienced dose-limiting toxicity or progression. Dose escalation commenced in single-patient cohorts for the first 4 planned dose levels and then followed a standard 3 + 3 scheme...
April 25, 2017: Cancer
https://www.readbyqxmd.com/read/28440827/molecular-dynamics-investigations-of-membrane-bound-cyp2c19-polymorphisms-reveal-distinct-mechanisms-for-peripheral-variants-by-long-range-effects-on-the-enzymatic-activity
#9
Ying-Lu Cui, Rong-Ling Wu
Increasing sophistication in methods used to account for human polymorphisms in susceptibility to drug metabolism has been one of the success stories in the prevention of adverse drug reactions. Genetic polymorphisms in drug-metabolizing enzymes can affect enzyme activity and cause differences in treatment response or drug toxicity. CYP2C19 is one of the most highly polymorphic CYP enzymes and acts on 10-15% of drugs in current clinical use. Despite the number of experimental analyses carried out for this system, the detailed structural basis for altered catalytic properties of polymorphic CYP2C19 variants remains unexplained at the atomic level...
April 25, 2017: Molecular BioSystems
https://www.readbyqxmd.com/read/28440713/glycinated-fullerenes-for-tamoxifen-intracellular-delivery-with-improved-anticancer-activity-and-pharmacokinetics
#10
Charu Misra, Manish Kumar, Gajanand Sharma, Rajendra Kumar, Bhupinder Singh, Om Prakash Katare, Kaisar Raza
AIM: Glycine-tethered C60-fullerenes were conjugated with N-desmethyl tamoxifen and evaluated for drug delivery benefits. MATERIALS & METHODS: C60-fullerenes were functionalized with glycine, and N-desmethyl tamoxifen was conjugated, employing a linker and characterized for micromeritics, drug loading, drug release and evaluated for cancer cell toxicity, cellular uptake and pharmacokinetics. RESULTS: The nanoconjugate with a drug entrapment efficiency of 82...
April 25, 2017: Nanomedicine
https://www.readbyqxmd.com/read/28440708/towards-in-vitro-to-in-vivo-translation-of-monoclonal-antibody-pharmacokinetics-application-of-a-neonatal-fc-receptor-mediated-transcytosis-assay-to-understand-the-interplaying-clearance-mechanisms
#11
Claudia A Castro Jaramillo, Sara Belli, Anne-Christine Cascais, Sherri Dudal, Martin R Edelmann, Markus Haak, Marie-Elise Brun, Michael B Otteneder, Mohammed Ullah, Christoph Funk, Franz Schuler, Silke Simon
Monoclonal antibodies (mAbs) are a rapidly growing drug class for which great efforts have been made to optimize certain molecular features in order to achieve the desired pharmacokinetic (PK) properties. One approach is to engineer the interactions of the mAb with the neonatal Fc receptor (FcRn) by introducing specific amino acid sequence mutations, and to assess their effect on the PK profile with in vivo studies. Indeed, FcRn protects mAbs from intracellular degradation, thereby prolongs antibody circulation time in plasma and modulates its systemic clearance...
April 25, 2017: MAbs
https://www.readbyqxmd.com/read/28440689/self-assembled-hemoglobin-nanoparticles-for-improved-oral-photosensitizer-delivery-and-oral-photothermal-therapy-in-vivo
#12
Kaikai Wang, Gang Chen, Qi Hu, Yuqian Zhen, Huipeng Li, Jiao Chen, Bin Di, Yiqiao Hu, Minjie Sun, David Oupický
AIM: The aim of the present study was to use hemoglobin (Hb) nanoparticles (NPs) to improve oral bioavailability of a near-infrared dye IR780 for in vivo antitumor application in photothermal therapy. METHODS: One-step acid-denaturing method was used to encapsulate IR780 into self-assembled Hb NPs (IR780@Hb NPs). Pharmacokinetics, biodistribution and antitumor effect were studied in vivo. RESULTS: The Hb NPs showed high stability in enzymatic and acidic conditions similar to the gastric environment, and enhanced absorption of IR780 into the blood...
April 25, 2017: Nanomedicine
https://www.readbyqxmd.com/read/28440659/alleviation-of-multiple-asthmatic-pathologic-features-with-orally-available-and-subtype-selective-gabaa-receptor-modulators
#13
Gloria S Forkuo, Amanda N Nieman, Nina Y Yuan, Revathi Kodali, Olivia B Yu, Nicolas M Zahn, Rajwana Jahan, Guanguan Li, Michael Rajesh Stephen, Margaret L Guthrie, Michael M Poe, Benjamin D Hartzler, Ted William Harris, Gene T Yocum, Charles W Emala, Douglas A Steeber, Douglas C Stafford, James M Cook, Leggy A Arnold
We describe pharmacokinetic and pharmacodynamic properties of two novel oral drug candidates for asthma. Phenolic α4β3γ2 GABAAR selective compound 1 and acidic α5β3γ2 selective GABAAR positive allosteric modulator compound 2 relaxed airway smooth muscle ex vivo and attenuated airway hyperresponsiveness (AHR) in a murine model of asthma. Importantly, compound 2 relaxed acetylcholine contracted human tracheal airway smooth muscle strips. Oral treatment of compound 1 and 2 decreased eosinophils in bronchoalveolar lavage fluid in ovalbumin sensitized and challenged mice, thus exhibiting anti-inflammatory properties...
April 25, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28440625/antischistosomal-activity-of-pyrido-1-2-a-benzimidazole-derivatives-and-correlation-with-inhibition-of-%C3%AE-haematin-formation
#14
John Okombo, Kawaljit Singh, Godfrey Mayoka, Ferdinand Ndubi, Linley Barnard, Peter M Njogu, Mathew Njoroge, Liezl Gibhard, Christel Brunschwig, Mireille Vargas, Jennifer Keiser, Timothy J Egan, Kelly Chibale
The extensive use of praziquantel against schistosomiasis raises concerns about drug resistance. New therapeutic alternatives targeting critical pathways within the parasite are therefore urgently needed. Haemozoin formation in Schistosoma presents one such target. We assessed in vitro antischistosomal activity of pyrido[1,2-a]benzimidazoles (PBIs), and investigated correlations with their ability to inhibit β-haematin formation. We further evaluated the in vivo efficacy of representative compounds in experimental mice and conducted pharmacokinetic analysis on the most potent...
April 25, 2017: ACS Infectious Diseases
https://www.readbyqxmd.com/read/28440419/different-effects-of-%C3%A2-borneol-and-%C3%A2-%C3%A2-borneol-on-the-pharmacokinetics-of-osthole-in-rats-following-oral-administration
#15
Dan-Dan Luo, Xiao-Ying Chen, Zhen-Biao Zhang, Chao-Yue Sun, Yi-Feng Zheng, Yu-Hong Liu, Xiu-Fen Wang, Qi Wang, Janis Ya-Xian Zhan, Zi-Ren Su
Osthole is the primary active component of a number of herbal plants such as the Cnidium monnieri fruit. In traditional Chinese herb medicine, osthole is commonly used in combination with borneol to obtain improved pharmacological effects. The aim of the present study was to investigate the effect of borneol enantiomers on the pharmacokinetics of osthole. An appropriate high‑performance liquid chromatography (HPLC) method was applied to determine the concentrations of osthole in plasma. Following oral administration of osthole alone or combined with borneol in rats, blood samples were collected and analyzed by HPLC...
April 21, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28440343/cyp3a4-genotype-is-associated-with-sildenafil-concentrations-in-patients-with-heart-failure-with-preserved-ejection-fraction
#16
S de Denus, J L Rouleau, D L Mann, G S Huggins, N L Pereira, S H Shah, T P Cappola, R Fouodjio, I Mongrain, M-P Dubé
Despite its established inter-individual variability, sildenafil has been the subject of only a few pharmacogenetic investigations, with limited data regarding the genetic modulators of its pharmacokinetics. We conducted a pharmacogenetic sub-study of patients randomized to sildenafil (n=85) in the RELAX trial, which investigated the impact of high-dose sildenafil in patients with heart failure with preserved left ventricular ejection fraction (HFpEF). In the overall population, the CYP3A4 inferred phenotype appeared associated with the dose-adjusted peak concentrations of sildenafil at week 12 and week 24 (adjusted P=0...
April 25, 2017: Pharmacogenomics Journal
https://www.readbyqxmd.com/read/28440204/apixaban-metabolism-pharmacologic-properties-and-drug-interaction
#17
Peter Kubisz, Lucia Stanciakova, Miroslava Dobrotova, Matej Samos, Marian Mokan, Jan Stasko
BACKGROUND: Apixaban is an oral, potent, highly selective, reversible and direct inhibitor of activated coagulation factor X, that is the end point of the intrinsic and extrinsic coagulation pathway. Additionally, apixaban has the capacity to indirectly inhibit thrombin-induced platelet aggregation. This new oral anticoagulant represents an immediate-release form of peroral drug with quick dissolution, linear pharmacokinetics, good bioavailability and rapid onset and offset of action...
April 24, 2017: Current Drug Metabolism
https://www.readbyqxmd.com/read/28440008/major-bleeding-risks-of-different-low-molecular-meight-heparin-agents-a-cohort-study-in-12-934-patients-treated-for-acute-venous-thrombosis
#18
N van Rein, J S Biedermann, F J M van der Meer, S C Cannegieter, N Wiersma, H W Vermaas, P H Reitsma, M J H A Kruip, W M Lijfering
BACKGROUND: Low-molecular-weight-heparins (LMWHs) are considered members of a class of drugs with similar anticoagulant properties. However, pharmacodynamics and pharmacokinetics between LMWHs differ, which may result in different bleeding risks. As these agents are used by many patients, small differences may lead to a large effect on numbers of major bleeding events. OBJECTIVES: To determine major bleeding risks for different LMWH agents and dosing schedules. METHODS: Cohort with acute venous thrombosis patients from four anticoagulation clinics who used a LMWH and a vitamin K antagonist...
April 25, 2017: Journal of Thrombosis and Haemostasis: JTH
https://www.readbyqxmd.com/read/28439817/developing-the-totality-of-evidence-for-biosimilars-regulatory-considerations-and-building-confidence-for-the-healthcare-community
#19
REVIEW
Richard Markus, Jennifer Liu, Monica Ramchandani, Diana Landa, Teresa Born, Primal Kaur
Biosimilars are highly similar versions of approved branded biologics. Unlike generics, they are not exact replicas of reference products. Minor differences between biosimilars and reference products in some aspects are expected; likewise, biosimilar products will differ from each other. The objective of this review is to discuss the challenges associated with the development and approval of biosimilar products that are unique because of their complex structure and specialized manufacturing processes, which can impact not only efficacy but also immunogenicity and safety...
April 24, 2017: BioDrugs: Clinical Immunotherapeutics, Biopharmaceuticals and Gene Therapy
https://www.readbyqxmd.com/read/28439684/impact-of-altered-endogenous-igg-on-unspecific-mab-clearance
#20
Saskia Fuhrmann, Charlotte Kloft, Wilhelm Huisinga
Immunodeficient mice are crucial models to evaluate the efficacy of monoclonal antibodies (mAbs). When studying mAb pharmacokinetics (PK), protection from elimination by binding to the neonatal Fc receptor (FcRn) is known to be a major process influencing the unspecific clearance of endogenous and therapeutic IgG. The concentration of endogenous IgG in immunodeficient mice, however is reduced, and this effect on the FcRn protection mechanism and subsequently on unspecific mAb clearance is unknown, yet of great importance for the interpretation of mAb PK data...
April 24, 2017: Journal of Pharmacokinetics and Pharmacodynamics
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