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Pharmacokinetic

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https://www.readbyqxmd.com/read/28214989/exposure-response-analyses-of-blood-pressure-and-heart-rate-changes-for-methylphenidate-in-healthy-adults
#1
Liang Li, Yaning Wang, Ramana S Uppoor, Mehul U Mehta, Tiffany Farchione, Mitchell V Mathis, Hao Zhu
The aim of the study was to evaluate the exposure-response (E-R) relationships of blood pressure (BP) and heart rate (HR) changes in healthy adults taking methylphenidate (MPH). Intensive time profiles of BP and HR from healthy adults in placebo and MPH treatment arms of seven clinical trials from the FDA internal database were utilized for this analysis. The analysis model contains a circadian component for placebo effect and an E-R component to describe drug effect. Internal validation was performed using goodness-of-fit plots and visual predictive check...
February 18, 2017: Journal of Pharmacokinetics and Pharmacodynamics
https://www.readbyqxmd.com/read/28214793/evaluation-of-timing-and-route-of-epinephrine-in-a-neonatal-model-of-asphyxial-arrest
#2
Payam Vali, Praveen Chandrasekharan, Munmun Rawat, Sylvia Gugino, Carmon Koenigsknecht, Justin Helman, William J Jusko, Bobby Mathew, Sara Berkelhamer, Jayasree Nair, Myra H Wyckoff, Satyan Lakshminrusimha
BACKGROUND: Epinephrine administered by low umbilical venous catheter (UVC) or endotracheal tube (ETT) is indicated in neonates who fail to respond to positive pressure ventilation and chest compressions at birth. Pharmacokinetics of ETT epinephrine via fluid-filled lungs or UVC epinephrine in the presence of fetal shunts is unknown. We hypothesized that epinephrine administered by ETT or low UVC results in plasma epinephrine concentrations and rates of return of spontaneous circulation (ROSC) similar to right atrial (RA) epinephrine...
February 18, 2017: Journal of the American Heart Association
https://www.readbyqxmd.com/read/28214380/application-of-the-mechpeff-model-to-predict-passive-effective-intestinal-permeability-in-the-different-regions-of-the-rodent-small-intestine-and-colon
#3
D Pade, M Jamei, A Rostami-Hodjegan, D B Turner
A major component of Physiologically-Based Pharmacokinetic (PBPK) models is prediction of the rate and extent of absorption of orally dosed drugs for which knowledge of effective passive intestinal permeability (Peff ) is essential. Single pass intestinal perfusion (SPIP) studies are used to establish effective permeability in vivo but are difficult to perform in rodents while mechanistic models to predict drug Peff in rat and mouse have not been published. This work evaluates the predictive performance of the 'MechPeff' model to predict Peff in the rodent intestine based upon knowledge of regional gut physiology and drug-specific physicochemical parameters...
February 18, 2017: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/28214069/-pharmacokinetic-drug-interaction-between-miconazole-mucoadhesive-tablet-and-tacrolimus-about-3%C3%A2-case-reports-in-transplant-patients
#4
Marion Lepelley, Sophie Logerot, Xavier Fonrose, Céline Villier
Loramyc(®) is a mucoadhesive tablet of miconazole, indicated for the treatment of oropharyngeal candidiasis in immunocompromised patients. Miconazole, as others azole antifungals, is known for its potent inhibitory properties of cytochromes P450 enzymes and P-glycoprotein (P-gp). Inhibition of cytochromes P450 enzymes and P-gp can produce pharmacokinetic drug interaction. Immunosuppressive agents, such as calcineurin inhibitors (tacrolimus, cyclosporine) are substrates of cytochromes P450 3A4 and P-gp. Nevertheless, the impact of systemic absorption of miconazole mucoadhesive tablet has not been investigated by the laboratory before regulatory approval...
January 12, 2017: Thérapie
https://www.readbyqxmd.com/read/28214059/pharmacokinetic-alterations-of-rhubarb-anthraquinones-in-experimental-colitis-induced-by-dextran-sulfate-sodium-in-the-rat
#5
Wen-Jin Wu, Ru Yan, Ting Li, Ya-Ping Li, Rui-Na Zhou, Yi-Tao Wang
ETHNOPHARMACOLOGICAL RELEVANCE: Rhubarb (Rhei Rhizoma et Radix) is used for the treatment of digestive diseases in traditional medicinal practice in China. Recent studies also support its beneficial activities in alleviating ulcerative colitis (UC). AIM OF THE STUDY: This study aimed to characterize the oral pharmacokinetics of rhubarb anthraquinones, the main bioactive components of this herb, in the experimental chronic colitis rat model induced by dextran sulfate sodium (DSS) and to identify the factors causing the pharmacokinetic alterations...
February 14, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28213957/a-bosentan-pharmacokinetic-study-to-investigate-dosing-regimens-in-paediatric-patients-with-pulmonary-arterial-hypertension-future-3
#6
R M F Berger, M Gehin, M Beghetti, D Ivy, A Kusic-Pajic, P Cornelisse, S Grill, D Bonnet
AIM: To investigate whether increasing bosentan dosing frequency from 2 mg/kg twice daily (b.i.d.) to 2 mg/kg three times daily (t.i.d.) in children with pulmonary arterial hypertension (PAH) (from ≥3 months to <12 years of age) would increase exposure. METHODS: An open-label, prospective, randomised, multicentre, multiple-dose, Phase 3 study was conducted. Patients (n = 64) were randomised 1:1 to receive oral doses of bosentan of 2 mg/kg b.i...
February 18, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28213941/population-pharmacokinetic-and-exposure-simulation-analysis-for-cediranib-azd2171-in-pooled-phase-i-ii-studies-in-patients-with-cancer
#7
Jianguo Li, Nidal Al-Huniti, Anja Henningsson, Weifeng Tang, Eric Masson
AIMS: A population pharmacokinetic (PPK) model was developed for cediranib to simulate cediranib exposure for different doses, including co-medication with strong UGT/Pgp inducers such as rifampicin, in cancer patients. METHODS: Plasma concentrations and covariates from 625 cancer patients after single or multiple oral cediranib administrations ranging from 0.5 to 90 mg in 19 Phase I and II studies were included in the analysis. Stepwise covariate modelling was used to develop the PPK model...
February 18, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28213761/psychomotor-effect-differences-between-l-methamphetamine-and-d-methamphetamine-are-independent-of-murine-plasma-and-brain-pharmacokinetics-profiles
#8
Tetsuya Nishimura, Kazue Takahata, Yuri Kosugi, Takaaki Tanabe, Shizuko Muraoka
l-Methamphetamine has been occasionally referred to as a stimulant similar to d-methamphetamine, probably owing to insufficient comparative studies. Here, we directly compared psychomotor efficacies and pharmacokinetics of methamphetamine enantiomers in mice. Only d-methamphetamine, but not l-methamphetamine, induced stereotypy and sensitization at 1-10 mg/kg. However, plasma pharmacokinetic parameters of 10 mg/kg l-methamphetamine were ≥tenfold those of 1 mg/kg d-methamphetamine. These results clearly indicate that differential psychomotor efficacies of methamphetamine enantiomers are independent of their pharmacokinetic profiles...
February 17, 2017: Journal of Neural Transmission
https://www.readbyqxmd.com/read/28213593/randomised-double-blind-parallel-group-placebo-controlled-study-to-evaluate-the-analgesic-efficacy-and-safety-of-vvz-149-injections-for-postoperative-pain-following-laparoscopic-colorectal-surgery
#9
Srdjan S Nedeljkovic, Darin J Correll, Xiaodong Bao, Natacha Zamor, Jose L Zeballos, Yi Zhang, Mark J Young, Johanna Ledley, Jessica Sorace, Kristen Eng, Carlyle P Hamsher, Rajivan Maniam, Jonathan W Chin, Becky Tsui, Sunyoung Cho, Doo H Lee
INTRODUCTION: In spite of advances in understanding and technology, postoperative pain remains poorly treated for a significant number of patients. In colorectal surgery, the need for developing novel analgesics is especially important. Patients after bowel surgery are assessed for rapid return of bowel function and opioids worsen ileus, nausea and constipation. We describe a prospective, double-blind, parallel group, placebo-controlled randomised controlled trial testing the hypothesis that a novel analgesic drug, VVZ -149, is safe and effective in improving pain compared with providing opioid analgesia alone among adults undergoing laparoscopic colorectal surgery...
February 17, 2017: BMJ Open
https://www.readbyqxmd.com/read/28213532/susceptibility-and-pk-pd-relationships-of-staphylococcus-aureus-strains-from-ovine-and-caprine-with-clinical-mastitis-against-five-veterinary-fluoroquinolones
#10
J M Serrano-Rodríguez, C Cárceles-García, C M Cárceles-Rodríguez, M L Gabarda, J M Serrano-Caballero, E Fernández-Varón
Minimum inhibitory concentration (MIC) and mutant prevention concentration (MPC) of veterinary fluoroquinolones as enrofloxacin, its metabolite ciprofloxacin, danofloxacin, difloxacin and marbofloxacin against Staphylococcus aureus strains (n=24) isolated from milk of sheep and goats affected by clinical mastitis were evaluated. The authors have used the MIC and MPC, as well as the pharmacokinetic-pharmacodynamic relationships in plasma and milk. MIC values were significantly different between drugs, unlike MPC values...
February 17, 2017: Veterinary Record
https://www.readbyqxmd.com/read/28213295/determination-of-imm-h004-a-novel-neuroprotective-agent-in-rat-plasma-and-brain-tissue-by-liquid-chromatography-tandem-mass-spectrometry
#11
Ziqian Zhang, Xiangmeng Wu, Manman Zhao, Yakun Yang, Yan Wang, Jinping Hu, Baolian Wang, Li Sheng, Yan Li
A rapid and sensitive liquid chromatography-tandem mass spectrometry method for determination of IMM-H004, a novel neuroprotective agent, in rat plasma and brain was developed. Plasma and brain tissue homogenate samples containing IMM-H004 and propranolol (internal standard, IS) were prepared by using a direct protein precipitation of acetonitrile. Separation was carried out in Zorbax SB-C18 column at a flow rate of 0.3mL/min utilizing acetonitrile/water as mobile phases which contain 0.5% formic acid (v/v)...
February 6, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28213276/engineering-approaches-in-sirna-delivery
#12
Anna Angela Barba, Sara Cascone, Diego Caccavo, Gaetano Lamberti, Gianluca Chiarappa, Michela Abrami, Gabriele Grassi, Mario Grassi, Giovanna Tomaiuolo, Stefano Guido, Valerio Brucato, Francesco Carfì Pavia, Giulio Ghersi, Vincenzo La Carrubba, Roberto Andrea Abbiati, Davide Manca
siRNAs are very potent drug molecules, able to silence genes involved in pathologies development. siRNAs have virtually an unlimited therapeutic potential, particularly for the treatment of inflammatory diseases. However, their use in clinical practice is limited because of their unfavorable properties to interact and not to degrade in physiological environments. In particular they are large macromolecules, negatively charged, which undergo rapid degradation by plasmatic enzymes, are subject to fast renal clearance/hepatic sequestration, and can hardly cross cellular membranes...
February 14, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28213176/lc-ms-ms-assay-for-the-simultaneous-quantitation-of-the-atm-inhibitor-az31-and-the-atr-inhibitor-azd6738-in-mouse-plasma
#13
Brian F Kiesel, Jeffrey C Shogan, Madani Rachid, Robert A Parise, Frank P Vendetti, Christopher J Bakkenist, Jan H Beumer
The ATM kinase inhibitor AZ31 and ATR kinase inhibitor AZD6738 are in various phases of preclinical and clinical evaluation for their ability to potentiate chemoradiation. To support the preclinical evaluation of their pharmacokinetics, we developed and validated an LC-MS/MS assay for the simultaneous quantification of AZ31 and AZD6738 in mouse plasma. A "dilute and shoot" method was used to precipitate proteins from a sample volume of 50μL. Chromatographic separation was achieved using a Phenomenex Polar-RP column and a gradient mobile phase consisting of methanol-water with 0...
February 4, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28213092/prediction-of-thyroid-c-cell-carcinogenicity-after-chronic-administration-of-glp1-r-agonists-in-rodents
#14
Willem van den Brink, Annette Emerenciana, Francesco Bellanti, Oscar Della Pasqua, Jan Willem van der Laan
Increased incidence of C-cell carcinogenicity has been observed for glucagon-like-protein-1 receptor (GLP-1r) agonists in rodents. It is suggested that the duration of exposure is an indicator of carcinogenic potential in rodents of the different products on the market. Furthermore, the role of GLP-1-related mechanisms in the induction of C-cell carcinogenicity has gained increased attention by regulatory agencies. This study proposes an integrative pharmacokinetic/pharmacodynamic (PKPD) framework to identify explanatory factors and characterize differences in carcinogenic potential of the GLP-1r agonist products...
February 14, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28213088/personalized-medicine-genetic-risk-prediction-of-drug-response
#15
REVIEW
Ge Zhang, Daniel W Nebert
Pharmacogenomics (PGx), a substantial component of "personalized medicine", seeks to understand each individual's genetic composition to optimize drug therapy -- maximizing beneficial drug response, while minimizing adverse drug reactions (ADRs). Drug responses are highly variable because innumerable factors contribute to ultimate phenotypic outcomes. Recent genome-wide PGx studies have provided some insight into genetic basis of variability in drug response. These can be grouped into three categories. [a] Monogenic (Mendelian) traits include early examples mostly of inherited disorders, and some severe (idiosyncratic) ADRs typically influenced by single rare coding variants...
February 14, 2017: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/28213004/pharmacokinetic-evaluation-of-intrapleural-perfusion-with-hyperthermic-chemotherapy-using-cisplatin-in-patients-with-malignant-pleural-effusion
#16
Hirozo Sakaguchi, H Ishida, H Nitanda, N Yamazaki, K Kaneko, Kunihiko Kobayashi
OBJECTIVES: Malignant pleural effusion (MPE) has a poor prognosis. Most patients are treated with tube thoracostomy and sclerotherapy, although its success rate is around 64%. We have investigated intrapleural perfusion with hyperthermic chemotherapy (IPHC) using cisplatin in a study with a pharmacokinetic evaluation. METHODS: Patients with MPE, performance status of 0-1, possibility of good lung expansion and Cr<1.2mg/dL were treated with IPHC. The circuit was filled with 2000mL of normal saline containing cisplatin at a dose of 80mg/m(2)...
February 2017: Lung Cancer: Journal of the International Association for the Study of Lung Cancer
https://www.readbyqxmd.com/read/28212342/a-review-on-the-phytochemistry-pharmacology-and-pharmacokinetics-of-amentoflavone-a-naturally-occurring-biflavonoid
#17
REVIEW
Sheng Yu, Hui Yan, Li Zhang, Mingqiu Shan, Peidong Chen, Anwei Ding, Sam Fong Yau Li
Amentoflavone (C30H18O10) is a well-known biflavonoid occurring in many natural plants. This polyphenolic compound has been discovered to have some important bioactivities, including anti-inflammation, anti-oxidation, anti-diabetes, and anti-senescence effects on many important reactions in the cardiovascular and central nervous system, etc. Over 120 plants have been found to contain this bioactive component, such as Selaginellaceae, Cupressaceae, Euphorbiaceae, Podocarpaceae, and Calophyllaceae plant families...
February 16, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28212092/modeling-contrast-imaging-assisted-optimal-targeted-drug-delivery-a-touchable-communication-channel-estimation-and-waveform-design-perspective
#18
Yifan Chen, Yu Zhou, Ross Murch, Panagiotis Kosmas
To maximize the effect of treatment and minimize the adverse effect on patients, we propose to optimize nanorobotsassisted targeted drug delivery (TDD) for locoregional treatment of tumor from the perspective of touchable communication channel estimation and waveform design. The drug particles are the information molecules; the loading/injection and unloading of the drug correspond to the transmitting and receiving processes; the concentration-time profile of the drug particles administered corresponds to the signalling pulse...
February 15, 2017: IEEE Transactions on Nanobioscience
https://www.readbyqxmd.com/read/28212021/discovery-and-development-of-1-2-bromophenyl-sulfonyl-5-methoxy-3-4-methyl-1-piperazinyl-methyl-1h-indole-dimesylate-monohydrate-suvn-502-a-novel-potent-selective-and-orally-active-serotonin-6-5-ht6-receptor-antagonist-for-potential-treatment-of-alzheimer-s
#19
Ramakrishna Nirogi, Anil Shinde, Rama Sastry Kambhampati, Abdul Rasheed Mohammed, Sangram Keshari Saraf, Rajesh Kumar Badange, Thrinath Reddy Bandyala, Venugopalarao Bhatta, Kumar Bojja, Veena Reballi, Ramkumar Subramanian, Vijay Benade, Raghava Choudary Palacharla, Gopinadh Bhyrapuneni, Pradeep Jayarajan, Vinod Goyal, Venkat Jasti
Optimization of a novel series of 3-(piperazinylmethyl) indole derivatives as 5-hydroxytryptamine-6 receptor (5-HT6R) antagonists resulted in identification of 1-[(2-bromophenyl)sulfonyl]-5-methoxy-3-[(4-methyl-1-piperazinyl)methyl]-1H-indole dimesylate monohydrate (5al, SUVN-502) as a clinical candidate for potential treatment of cognitive disorders. It has high affinity at human 5-HT6R (Ki = 2.04 nM) and selectivity over 100 target sites which include receptors, enzymes, peptides, growth factors, ion channels, steroids, immunological factors, second messengers, and prostaglandins...
February 17, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28211963/a-parametric-model-of-the-brain-vascular-system-for-estimation-of-the-arterial-input-function-aif-at-the-tissue-level
#20
Siamak P Nejad-Davarani, Hassan Bagher-Ebadian, James R Ewing, Douglas C Noll, Tom Mikkelsen, Michael Chopp, Quan Jiang
In this paper, we introduce a novel model of the brain vascular system, which is developed based on laws of fluid dynamics and vascular morphology. This model is used to address dispersion and delay of the arterial input function (AIF) at different levels of the vascular structure and to estimate the local AIF in DCE images. We developed a method based on the simplex algorithm and Akaike information criterion to estimate the likelihood of the contrast agent concentration signal sampled in DCE images belonging to different layers of the vascular tree or being a combination of different signal levels from different nodes of this structure...
February 17, 2017: NMR in Biomedicine
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