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midazolam effects

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https://www.readbyqxmd.com/read/29160125/effects-of-paeoniflorin-on-the-activities-and-mrna-expression-of-rat-cyp1a2-cyp2c11-and-cyp3a1-enzymes-in-vivo
#1
Sicong Li, Xuting Li, Dingsheng Yuan, Bin Wang, Rui Yang, Min Zhang, Jinliang Li, Fuqiang Zeng
1. Paeoniflorin is the major constituent in extracts of the peony root, the purpose of the present study was to assess the effects of paeoniflorin on the activities and mRNA expression of the rat hepatic drug-metabolizing enzymes cytochrome P450 (CYP1A2), CYP2C11 and CYP3A1 in vivo. 2. Sprague-Dawley (SD) male rats were treated with paeoniflorin at the dosage of 25, 50 and 100 mg/kg or 0.9% sodium chloride solution by intragastric administration for 7 days, then were given probe drugs phenacetin (CYP1A2), tolbutamide (CYP2C11), or midazolam (CYP3A1) orally on the eighth day...
November 21, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/29156621/influence-of-shenxiong-glucose-injection-on-the-activities-of-six-cyp-isozymes-and-metabolism-of-warfarin-in-rats-assessed-using-probe-cocktail-and-pharmacokinetic-approaches
#2
Jia Sun, Yuan Lu, Yueting Li, Jie Pan, Chunhua Liu, Zipeng Gong, Jing Huang, Jiang Zheng, Lin Zheng, Yongjun Li, Ting Liu, Yonglin Wang
Shenxiong glucose injection (SGI), a traditional Chinese medicine (TCM) preparation, has been widely used for the treatment of various cardiovascular and cerebrovascular diseases for many years. We assessed the potential influences of SGI on the activities of six CYP enzymes (CYP1A2, CYP2C11, CYP2C19, CYP2D4, CYP2E1, and CYP3A2) and on the pharmacokinetics of warfarin in rats. We compared plasma pharmacokinetics of six probe drugs (caffeine/CYP1A2, tolbutamide/CYP2C11, omeprazole/CYP2C19, metoprolol/CYP2D4, chlorzoxazone/CYP2E1, and midazolam/CYP3A2) and of warfarin between control and SGI-pretreated groups, to estimate the effect on the relative activities of the six isozymes and warfarin metabolism...
November 20, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29151416/-short-term-deep-sedation-strategy-in-patients-with-spontaneous-intracerebral-hemorrhage-a-randomized-controlled-trial
#3
Zhuheng Wang, Chunzhi Shi, Liping Sun, Qinghua Guo, Wei Qiao, Guanhua Zhou
OBJECTIVE: To evaluate the efficacy and safety of short-term deep sedation strategy in patients with spontaneous intracerebral hemorrhage (ICH) after surgery. METHODS: A perspective, randomized, parallel-group study was conducted. Adult patients with spontaneous ICH and undergoing craniotomy admitted to Daxing Teaching Hospital of Capital Medical University from December 2015 to November 2016 were enrolled. The patients who received surgery were randomly divided into a short-term deep sedation and a slight and middle sedation group...
November 2017: Zhonghua Wei Zhong Bing Ji Jiu Yi Xue
https://www.readbyqxmd.com/read/29147790/-etomidate-for-intravenous-induction-of-anaesthesia
#4
C Dumps, D Bolkenius, E Halbeck
The pharmacological and historical knowledge about the currently available intravenous induction hypnotics form the basis for the daily work of anesthetists. Side effects of using hypnotic induction agents must be anticipated and adequately treated. Decades of experience with using intravenous induction hypnotics have led to theoretical requirements for an ideal narcotic agent with a best possible side effect profile. In the absence of this optimal hypnotic induction agent, a careful selection of one or a combination of narcotic drugs is necessary to meet the needs of the respective risk constellation of the patient...
November 16, 2017: Der Anaesthesist
https://www.readbyqxmd.com/read/29137494/trh-receptor-mobility-in-the-plasma-membrane-is-strongly-affected-by-agonist-binding-and-by-interaction-with-some-cognate-signaling-proteins
#5
Radka Moravcova, Barbora Melkes, Jiri Novotny
OBJECTIVES: Extensive research has been dedicated to elucidating the mechanisms of signal transduction through different G protein-coupled receptors (GPCRs). However, relatively little is known about the regulation of receptor movement within the cell membrane upon ligand binding. In this study we focused our attention on the thyrotropin-releasing hormone (TRH) receptor that typically couples to Gq/11 proteins. METHODS: We monitored receptor diffusion in the plasma membrane of HEK293 cells stably expressing yellow fluorescent protein (YFP)-tagged TRH receptor (TRHR-YFP) by fluorescence recovery after photobleaching (FRAP)...
November 14, 2017: Journal of Receptor and Signal Transduction Research
https://www.readbyqxmd.com/read/29132458/-efficacy-of-analgesic-and-sedative-treatments-in-children-with-mechanical-ventilation-in-the-pediatric-intensive-care-unit
#6
Xiao-Fang Cai, Fu-Rong Zhang, Long Zhang, Ji-Min Sun, Wen-Bin Li
OBJECTIVE: To compare the efficacy and safety of different analgesic and sedative treatments in children with mechanical ventilation in the pediatric intensive care unit (PICU). METHODS: Eighty children with mechanical ventilation in the PICU who needed analgesic and sedative treatments were equally and randomly divided into midazolam group and remifentanil+midazolam group. The sedative and analgesic effects were assessed using the Ramsay Scale and the Face, Legs, Activity, Cry and Consolability (FLACC) Scale...
November 2017: Zhongguo Dang Dai Er Ke za Zhi, Chinese Journal of Contemporary Pediatrics
https://www.readbyqxmd.com/read/29130583/endoscopic-retrograde-cholangio-pancreatography-in-the-management-of-biliary-complications-after-paediatric-liver-transplantation
#7
Sivaramakrishnan Venkatesh Karthik, Seng-Hock Quak, Marion M Aw
BACKGROUND: The published paediatric experience with Endoscopic retrograde cholangio-pancreatography (ERCP) in the diagnosis and management of biliary complications following liver transplantation (LT) is limited. AIMS: We describe our experience with ERCP in the management of children following LT who presented with biliary complications, over a 20 year period (1995-2014). METHODS: The retrospectively reviewed data is summarized descriptively...
November 11, 2017: Transplant International: Official Journal of the European Society for Organ Transplantation
https://www.readbyqxmd.com/read/29121108/spatio-temporal-dynamics-of-multimodal-eeg-fnirs-signals-in-the-loss-and-recovery-of-consciousness-under-sedation-using-midazolam-and-propofol
#8
Seul-Ki Yeom, Dong-Ok Won, Seong In Chi, Kwang-Suk Seo, Hyun Jeong Kim, Klaus-Robert Müller, Seong-Whan Lee
On sedation motivated by the clinical needs for safety and reliability, recent studies have attempted to identify brain-specific signatures for tracking patient transition into and out of consciousness, but the differences in neurophysiological effects between 1) the sedative types and 2) the presence/absence of surgical stimulations still remain unclear. Here we used multimodal electroencephalography-functional near-infrared spectroscopy (EEG-fNIRS) measurements to observe electrical and hemodynamic responses during sedation simultaneously...
2017: PloS One
https://www.readbyqxmd.com/read/29119733/administration-of-fentanyl-via-a-slow-intravenous-fluid-line-compared-with-rapid-bolus-alleviates-fentanyl-induced-cough-during-general-anesthesia-induction
#9
Min-Qiang Liu, Feng-Xian Li, Ya-Kun Han, Jun-Yong He, Hao-Wen Shi, Li Liu, Ren-Liang He
OBJECTIVE: Fentanyl-induced cough (FIC) is a common complication with a reported incidence from 18.0% to 74.4% during general anesthesia induction. FIC increases the intrathoracic pressure and risks of postoperative nausea and vomiting, yet available treatments are limited. This study was designed to investigate whether administering fentanyl via a slow intravenous fluid line can effectively alleviate FIC during induction of total intravenous general anesthesia. METHODS: A total number of 1200 patients, aged 18-64 years, were enrolled, all of whom were American Society of Anesthesiologists (ASA) grade I or II undergoing scheduled surgeries...
2017: Journal of Zhejiang University. Science. B
https://www.readbyqxmd.com/read/29117990/simultaneous-physiologically-based-pharmacokinetic-pbpk-modeling-of-parent-and-active-metabolites-to-investigate-complex-cyp3a4-drug-drug-interaction-potential-a-case-example-of-midostaurin
#10
Helen Gu, Catherine Dutreix, Sam Rebello, Taoufik Ouatas, Lai Wang, Dung Yu Chun, Heidi J Einolf, Handan He
Midostaurin (PKC412) is being investigated for the treatment of acute myeloid leukemia (AML) and advanced systemic mastocytosis (advSM). It is extensively metabolized by cytochrome P450 (CYP) 3A4 to form 2 major active metabolites, CGP52421 and CGP62221. In vitro and clinical drug-drug interaction (DDI) studies indicated that midostaurin and its metabolites are substrates, reversible and time-dependent inhibitors, and inducers of CYP3A4. A simultaneous pharmacokinetic model of parent and active metabolites was initially developed by incorporating data from in vitro, preclinical, and clinical pharmacokinetic studies in healthy volunteers and in patients with AML or advSM...
November 8, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/29115994/exploring-venlafaxine-pharmacokinetic-variability-with-a-phenotyping-approach-a-multicentric-french-swiss-study-marvel-study
#11
Célia Lloret-Linares, Youssef Daali, Sylvie Chevret, Isabelle Nieto, Fanny Molière, Philippe Courtet, Florence Galtier, Raphaëlle-Marie Richieri, Sophie Morange, Pierre-Michel Llorca, Wissam El-Hage, Thomas Desmidt, Frédéric Haesebaert, Philippe Vignaud, Jerôme Holtzmann, Jean-Luc Cracowski, Marion Leboyer, Antoine Yrondi, Fabienne Calvas, Liova Yon, Philippe Le Corvoisier, Olivier Doumy, Kyle Heron, Damien Montange, Siamak Davani, Julien Déglon, Marie Besson, Jules Desmeules, Emmanuel Haffen, Frank Bellivier
BACKGROUND: It is well known that the standard doses of a given drug may not have equivalent effects in all patients. To date, the management of depression remains mainly empirical and often poorly evaluated. The development of a personalized medicine in psychiatry may reduce treatment failure, intolerance or resistance, and hence the burden and costs of mood depressive disorders. The Geneva Cocktail Phenotypic approach presents several advantages including the "in vivo" measure of different cytochromes and transporter P-gp activities, their simultaneous determination in a single test, avoiding the influence of variability over time on phenotyping results, the administration of low dose substrates, a limited sampling strategy with an analytical method developed on DBS analysis...
November 7, 2017: BMC Pharmacology & Toxicology
https://www.readbyqxmd.com/read/29112329/in-vitro-and-in-vivo-investigation-of-potential-for-complex-cyp3a-interaction-for-pf-00251802-dagrocorat-a-novel-dissociated-agonist-of-the-glucocorticoid-receptor
#12
Sharon L Ripp, Arnab Mukherjee, Heather Eng, Thomas Stock, Dona Fleishaker, Tina Checchio, Brinda Tammara
The dissociated agonists of the glucocorticoid receptor are a novel class of agents in clinical development for rheumatoid arthritis. PF-04171327 (fosdagrocorat) is a phosphate ester prodrug of PF-00251802 (dagrocorat), a selective high-affinity partial agonist of the glucocorticoid receptor, which is further metabolized to PF-04015475. This study evaluated the cytochrome P450 (CYP)-mediated drug-drug interaction (DDI) potential of PF-00251802 and PF-04015475 in vitro and used model-based prediction approaches to estimate clinical impact...
November 7, 2017: Clinical Pharmacology in Drug Development
https://www.readbyqxmd.com/read/29104056/taste-evaluation-of-a-novel-midazolam-tablet-for-pediatric-patients-in-vitro-drug-dissolution-in-vivo-animal-taste-aversion-and-clinical-taste-perception-profiles
#13
Laurence C Cheung, Minh Nguyen, Edith Tang, Britta S von Ungern Sternberg, Sam Salman, Catherine Tuleu, Abeer H A Mohamed Ahmed, Jessica Soto, Lee Yong Lim
Harmonized methodologies are urgently required for the taste evaluation of novel pediatric medicines. This study utilized in vitro, in vivo and clinical data to evaluate the palatability of a novel midazolam chocolate tablet. In vitro dissolution experiments showed the crushed tablet to release within 5 min 1.68 mg of midazolam into simulated saliva. This translated to a drug level of 0.84 mg/ml in the oral cavity, which would be higher than the midazolam bitterness detection threshold concentration of 0...
November 11, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29104018/the-influence-of-midazolam-on-heart-rate-arises-from-cardiac-autonomic-tones-alterations-in-burmese-pythons-python-molurus
#14
Ivã Guidini Lopes, Vinicius Araújo Armelin, Victor Hugo da Silva Braga, Luiz Henrique Florindo
The GABAA receptor agonist midazolam is a compound widely used as a tranquilizer and sedative in mammals and reptiles. It is already known that this benzodiazepine produces small to intermediate heart rate (HR) alterations in mammals, however, its influence on reptiles' HR remains unexplored. Thus, the present study sought to verify the effects of midazolam on HR and cardiac modulation in the snake Python molurus. To do so, the snakes' HR, cardiac autonomic tones, and HR variability were evaluated during four different experimental stages...
October 28, 2017: Autonomic Neuroscience: Basic & Clinical
https://www.readbyqxmd.com/read/29099769/influence-of-amlodipine-enantiomers-on-human-microsomal-cytochromes-p450-stereoselective-time-dependent-inhibition-of-cyp3a-enzyme-activity
#15
Kristyna Krasulova, Ondrej Holas, Pavel Anzenbacher
Amlodipine (AML) is available as a racemate, i.e., a mixture of R- and S-enantiomers. Its inhibitory potency towards nine cytochromes P450 (CYP) was studied to evaluate the drug-drug interactions between the enantiomers. Enzyme inhibition was evaluated using specific CYP substrates in human liver microsomes. With CYP3A, both enantiomers exhibited reversible and time-dependent inhibition. S-AML was a stronger reversible inhibitor of midazolam hydroxylation: the Ki values of S- and R-AML were 8.95 µM, 14.85 µM, respectively...
November 3, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29099542/chloral-hydrate-as-a-sedating-agent-for-neurodiagnostic-procedures-in-children
#16
REVIEW
Choong Yi Fong, Chee Geap Tay, Lai Choo Ong, Nai Ming Lai
BACKGROUND: Paediatric neurodiagnostic investigations, including brain neuroimaging and electroencephalography (EEG), play an important role in the assessment of neurodevelopmental disorders. The use of an appropriate sedative agent is important to ensure the successful completion of the neurodiagnostic procedures, particularly in children, who are usually unable to remain still throughout the procedure. OBJECTIVES: To assess the effectiveness and adverse effects of chloral hydrate as a sedative agent for non-invasive neurodiagnostic procedures in children...
November 3, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/29098381/the-effects-of-lapatinib-on-cyp3a-metabolism-of-midazolam-in-patients-with-advanced-cancer
#17
Kevin M Koch, E Claire Dees, Shodeinde A Coker, Nandi J Reddy, Shelby D Gainer, Nikita Arya, Andrew P Beelen, Lionel D Lewis
PURPOSE: The potential inhibition of CYP3A4 by lapatinib was studied using midazolam as a probe substrate in patients with cancer. METHODS: This was a partially randomized, 4-period, 4-sequence, 4-treatment, cross-over study in 24 patients with advanced cancer. Single 1-mg IV and 3-mg oral doses of midazolam were given 2 days apart, in a partially random order, on study days 1, 3, 9, and 11. Lapatinib 1500-mg was administered orally once daily on study days 4 through 11...
November 2, 2017: Cancer Chemotherapy and Pharmacology
https://www.readbyqxmd.com/read/29081581/xylazine-infusion-in-isoflurane-anesthetized-and-ventilated-healthy-horses-effects-on-cardiovascular-parameters-and-intestinal-perfusion
#18
Klaus Hopster, Liza Wittenberg-Voges, Sabine B R Kästner
To investigate the effects of a xylazine infusion during isoflurane anesthesia on global perfusion parameters and gastrointestinal oxygenation and microperfusion, 8 adult warmblood horses were sedated with xylazine and anesthesia induced with midazolam and ketamine. Horses were mechanically ventilated during anesthesia. After 3 h of stable isoflurane anesthesia (FEIso 1.3 Vol %), a xylazine infusion with 1 mg/kg body weight (BW) per hour was started for 1 h and then stopped. Before, during, and after xylazine infusion, heart rate (HR), arterial blood pressure (MAP), cardiac output (CO), central venous pressure (CVP), and pulmonary artery pressure (PAP) were measured and systemic vascular resistance (SVR) was calculated...
October 2017: Canadian Journal of Veterinary Research, Revue Canadienne de Recherche Vétérinaire
https://www.readbyqxmd.com/read/29080097/hydromorphone-hydrochloride-use-during-various-interventional-radiology-procedures-pain-control-and-adverse-events-a-case-series-audit-analysis
#19
Thea Moran, Amit Prabhakar, James H Diaz, Alan David Kaye
INTRODUCTION: This project studied pain control and the development of adverse events before, during, and after the administration of hydromorphone hydrochloride for various interventional radiology (IR) procedures. METHODS: We performed a retrospective analysis of 100 patients (men = 58; women = 42) sedated with peri-procedural intravenous (IV) hydromorphone in association with various IR procedures. We stratified the procedures as follows: abscess drainages (M = 8; F = 8), arteriograms (M = 1; F = 0), biliary interventions (M = 3; F = 2), bone biopsies (M = 2; F = 2), non-bone biopsies (M = 26; F = 19), non-tunneled venous catheters (M = 1; F = 1), tunneled venous catheters (M = 7; F = 5), embolization (M = 4; F = 0), IVC filter placement (M = 1; F = 1), nephrostomy tube placement (M = 1; F = 4), and percutaneous nephrolithotomy tube placements (M = 4; F = 0)...
December 2017: Pain and Therapy
https://www.readbyqxmd.com/read/29079070/pharmacologic-interventions-for-intractable-and-persistent-hiccups-a-systematic-review
#20
Nick B Polito, Shawn E Fellows
BACKGROUND: Chlorpromazine is the only drug approved by the US Food and Drug Administration for the treatment of hiccups; however, many other pharmacologic treatments have been proposed for intractable and persistent hiccups. Currently, there is little evidence to support the use of one agent over another. OBJECTIVE: This review aims to identify literature concerning the use of pharmacologic treatments for intractable and persistent hiccups with the goal of evaluating therapies in terms of their level of evidence, mechanism of action, efficacy, dosing, onset of action, and adverse effects...
October 2017: Journal of Emergency Medicine
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