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pharmacokinetics, brain, plasma

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https://www.readbyqxmd.com/read/28549082/pharmacokinetics-and-pharmacodynamics-of-propofol-changes-in-patients-with-frontal-brain-tumours
#1
M M Sahinovic, D J Eleveld, T Miyabe-Nishiwaki, M M R F Struys, A R Absalom
Background: Models of propofol pharmacokinetics and pharmacodynamics developed in patients without brain pathology are widely used for target-controlled infusion (TCI) during brain tumour excision operations. The goal of this study was to determine if the presence of a frontal brain tumour influences propofol pharmacokinetics and pharmacodynamics and existing PK-PD model performance. Methods: Twenty patients with a frontal brain tumour and 20 control patients received a propofol infusion to achieve an induction-emergence-induction anaesthetic sequence...
May 26, 2017: British Journal of Anaesthesia
https://www.readbyqxmd.com/read/28512055/first-plasma-and-tissue-pharmacokinetic-study-of-the-ysnsg-cyclopeptide-a-new-integrin-antagonist-using-microdialysis
#2
Florian Slimano, Zoubir Djerada, Salim Bouchene, Laurence Van Gulick, Sylvie Brassart-Pasco, Sylvain Dukic
The YSNSG peptide is a synthetic peptide targeting αvβ3 integrin. This peptide exhibits promising activity in vitro and in vivo against melanoma. To determine pharmacokinetic parameters and predictive active doses in the central nervous system (CNS) and subcutaneous tissue (SC), we conducted microdialysis coupled with pharmacokinetic modeling and Monte Carlo simulation. After a recovery period of surgical procedures, a microdialysis probe was inserted in the caudate and in subcutaneous tissue. Plasma samples and dialysates collected 5h after YSNSG intravenous administration (10mg/kg) were analyzed by UPLC-MS/MS...
May 13, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28496304/evaluation-of-the-antitumor-activity-of-nov202-a-novel-microtubule-targeting-and-vascular-disrupting-agent
#3
Linda Rickardson, Emma Kutvonen, Satu Orasniemi, Marita Högberg, Marko J Kallio, Stefan Rehnmark
PURPOSE: Overall, ~65% of patients diagnosed with advanced ovarian cancer (OC) will relapse after primary surgery and adjuvant first-line platinum- and taxane-based chemotherapy. Significant improvements in the treatment of OC are expected from the development of novel compounds having combined cytotoxic and antiangiogenic properties that make them effective on refractory tumors. METHODS: Permeability of NOV202 was determined with Caco-2 monolayer assay. The compound's pharmacokinetic profile and plasma:brain distribution were assessed in male C57Bl/6 mice...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28464043/mechanistic-insights-into-the-more-potent-effect-of-kp-54-compared-to-kp-10-in-vivo
#4
Xavier d'Anglemont de Tassigny, Channa Jayasena, Kevin G Murphy, Waljit S Dhillo, William H Colledge
Kisspeptins regulate the mammalian reproductive axis by stimulating release of gonadotrophin releasing hormone (GnRH). Different length kisspeptins (KP) are found of 54, 14, 13 or 10 amino-acids which share a common C-terminal 10-amino acid sequence. KP-54 and KP-10 have been widely used to stimulate the reproductive axis but data suggest that KP-54 and KP-10 are not equally effective at eliciting reproductive hormone secretion after peripheral delivery. To confirm this, we analysed the effect of systemic administration of KP-54 or KP-10 on luteinizing hormone (LH) secretion into the bloodstream of male mice...
2017: PloS One
https://www.readbyqxmd.com/read/28445697/influence-of-maturation-on-in-vivo-tissue-to-plasma-partition-coefficients-for-cis-and-trans-permethrin
#5
Manoj Amaraneni, Jing Pang, James V Bruckner, Srinivasa Muralidhara, Tanzir B Mortuza, Darren Gullick, Shirin Hooshfar, Catherine A White, Brian S Cummings
Permethrin, the most widely used household insecticide in the U.S., is marketed as a mixture of its cis (CIS) and trans (TRANS) isomers. The major objective of this investigation was to develop and utilize a reliable approach to determine in vivo partition coefficients (PCs) for CIS and TRANS in immature and adult Sprague-Dawley rats. Adult, postnatal day (PND) 21 and PND 15 rats were infused with environmentally relevant concentrations of CIS or TRANS via a s.c. osmotic pump for 48 or 72 h. The adult and PND 21 rats also received an oral loading dose...
April 23, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28442937/simultaneous-administration-of-fluoxetine-and-simvastatin-ameliorates-lipid-profile-improves-brain-level-of-neurotransmitters-and-increases-bioavailability-of-simvastatin
#6
Abdulrahman K Al-Asmari, Zabih Ullah, Aqeel Salman Al Masoudi, Ishtiaque Ahmad
Simvastatin (STT), a 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor, is widely prescribed for dyslipidemia, whereas fluoxetine (FLX) is the first-choice drug for the treatment of depression and anxiety. A recent report suggests that selective serotonin reuptake inhibitors can interact with the cytochrome P450 3A4 substrate, and another one suggests that STT enhances the antidepressant activity of FLX. However, the data are inconclusive. The present study was designed to explore the pharmacokinetic and pharmacodynamic consequences of coadministration of STT and FLX in experimental animals...
2017: Journal of Experimental Pharmacology
https://www.readbyqxmd.com/read/28442345/characterization-of-a-recombinant-humanized-anti-cocaine-monoclonal-antibody-produced-from-multiple-clones-for-the-selection-of-a-master-cell-bank-candidate
#7
Hanna N Wetzel, Rose P Webster, Fatima O Saeed, Terence L Kirley, William J Ball, Andrew B Norman
We have generated a humanized anti-cocaine monoclonal antibody (mAb), which is at an advanced stage of pre-clinical development. We report here in vitro binding affinity studies, and in vivo pharmacokinetic and efficacy studies of the recombinant mAb. The overall aim was to characterize the recombinant antibody from each of the three highest producing transfected clones and to select one to establish a master cell bank. In mAb pharmacokinetic studies, after injection with h2E2 (120 mg/kg iv) blood was collected from the tail tip of mice over 28 days...
June 3, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28440659/alleviation-of-multiple-asthmatic-pathologic-features-with-orally-available-and-subtype-selective-gabaa-receptor-modulators
#8
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 W 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 compounds 1 and 2 decreased eosinophils in bronchoalveolar lavage fluid in ovalbumin sensitized and challenged mice, thus exhibiting anti-inflammatory properties...
May 1, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28426226/brain-uptake-of-bioactive-flavones-in-scutellariae-radix-and-its-relationship-to-anxiolytic-effect-in-mice
#9
Sophia Yui Kau Fong, Chenrui Li, Yiu Cheong Ho, Rui Li, Qian Wang, Yin Cheong Wong, Hong Xue, Zhong Zuo
Scutellariae Radix (SR) and its bioactive flavones elicit a variety of effects in the brain. However, the brain uptake of individual SR flavones and its relationship to the elicited effects after SR administration remain unknown. Moreover, previous studies seldom measured pharmacokinetic and pharmacodynamic outcomes simultaneously. In the current study, the brain uptake of six major SR flavones and the anxiolytic behavior following oral administration of a SR extract at two clinically relevant doses (600 and 1200 mg/kg twice daily) were simultaneously investigated in mice (n = 18 per group)...
May 1, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28415883/electrosteric-stealth-rivastigmine-loaded-liposomes-for-brain-targeting-preparation-characterization-ex-vivo-bio-distribution-and-in-vivo-pharmacokinetic-studies
#10
Sara Nageeb El-Helaly, Ahmed Abd Elbary, Mohamed A Kassem, Mohamed A El-Nabarawi
Being one of the highly effective drugs in treatment of Alzheimer's disease, Rivastigmine brain targeting is highly demandable, therefore liposomal dispersion of Rivastigmine was prepared containing 2 mol% PEG-DSPE added to Lecithin, Didecyldimethyl ammonium bromide (DDAB), Tween 80 in 1:0.02:0.25 molar ratio. A major challenge during the preparation of liposomes is maintaining a stable formulation, therefore the aim of our study was to increase liposomal stability by addition of DDAB to give an electrostatic stability and PEG-DSPE to increase stability by steric hindrance, yielding what we called an electrosteric stealth (ESS) liposomes...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28404688/brain-disposition-of-cis-para-methyl-4-methylaminorex-cis-4-4-dmar-and-its-potential-metabolites-after-acute-and-chronic-treatment-in-rats-correlation-with-central-behavioral-effects
#11
Jacopo Lucchetti, Claudio Marcello Marzo, Alice Passoni, Angelo Di Clemente, Federico Moro, Renzo Bagnati, Marco Gobbi, Luigi Cervo
Para-methyl-4-methylaminorex (4,4'-DMAR) is a phenethylamine derivative with psychostimulant activity, whose abuse has been associated with several deaths and a wide range of adverse effects. We recently validated an HPLC-MS/MS method to measure the compound's concentrations in plasma, and applied it to describe the pharmacokinetic properties after single dose in rats. In this study we investigated the brain disposition and metabolism of cis-4,4'-DMAR after intraperitoneal injection, and its central behavioral effects...
April 12, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28399431/determination-of-azd3759-in-rat-plasma-and-brain-tissue-by-lc-ms-ms-and-its-application-in-pharmacokinetic-and-brain-distribution-studies
#12
Shan Xiong, Mingxing Xue, Yanling Mu, Zhipeng Deng, Peilu Sun, Ruican Zhou
A simple and sensitive high performance liquid chromatography with tandem mass spectrometry (LC-MS/MS) method for determination of AZD3759, a novel epidermal growth factor receptor tyrosine kinase inhibitor, in rat plasma and brain homogenate was developed and validated over the range of 1.0-1000ng/mL. Chromatographic separation was carried out on a C18 column with acetonitrile and 0.1% formic acid in water as mobile phase with gradient elution at a flow rate of 0.4mL/min. The lower limits of quantification (LLOQs) were 1...
June 5, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28360333/detailed-characterization-of-the-in-vitro-pharmacological-and-pharmacokinetic-properties-of-n-2-hydroxybenzyl-2-5-dimethoxy-4-cyanophenylethylamine-25cn-nboh-a-highly-selective-and-brain-penetrant-5-ht2a-receptor-agonist
#13
Anders A Jensen, John D McCorvy, Sebastian Leth Petersen, Christoffer Bundgaard, Gudrun Liebscher, Terry P Kenakin, Hans Brauner-Osborne, Jan Kehler, Jesper L Kristensen
Therapeutic interest in augmentation of 5-hydroxytryptamine2A (5-HT2A) receptor signaling has been renewed by the effectiveness of psychedelic drugs in the treatment of various psychiatric conditions. In this study, we have further characterized the pharmacological properties of the recently developed 5-HT2 receptor agonist 2-hydroxybenzyl)-2,5-dimethoxy-4-cyanophenylethylamine (25CN-NBOH) and three structural analogs at recombinant 5-HT2A, 5- HT2B and 5-HT2C receptors and investigated the pharmacokinetic properties of the compound...
March 30, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28346885/plasma-and-brain-pharmacokinetics-of-ganoderic-acid-a-in-rats-determined-by-a-developed-uflc-ms-ms-method
#14
Fang-Rui Cao, Bing-Xin Xiao, Li-Sha Wang, Xue Tao, Ming-Zhu Yan, Rui-Le Pan, Yong-Hong Liao, Xin-Min Liu, Qi Chang
Ganoderic acid A (GAA), an active triterpenoid of the traditional Chinese herbal medicine Lingzhi, has been reported to exhibit antinociceptive, antioxidative, and anti-cancer activities. The present study aims to establish a sensitive and rapid UPLC-MS/MS method for studying the plasma and brain pharmacokinetics of GAA in rats. The analytes were separated on a C18 column eluted with a gradient mobile phase consisting of acetonitrile and 0.1% aqueous formic acid at 0.3mL/min. The eluate was monitored by a mass detector using an MRM (m/z, 515...
May 1, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28346882/determination-of-prodrug-treosulfan-and-its-biologically-active-monoepoxide-in-rat-plasma-liver-lungs-kidneys-muscle-and-brain-by-hplc-esi-ms-ms-method
#15
Michał Romański, Anna Kasprzyk, Artur Teżyk, Agnieszka Widerowska, Czesław Żaba, Franciszek Główka
A prodrug treosulfan (TREO) is currently investigated in clinical trials for conditioning prior to hematopoietic stem cell transplantation. Bioanalysis of TREO and its active derivatives, monoepoxide (S,S-EBDM) and diepoxide, in plasma and urine underlay the pharmacokinetic studies of these compounds but cannot explain an organ pharmacological action or toxicity. Recently, distribution of TREO and S,S-EBDM into brain, cerebrospinal fluid, and aqueous humor of the eye has been investigated in animal models and the obtained results presented clinical relevance...
June 5, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28344497/effect-of-nitazoxanide-on-albendazole-pharmacokinetics-in-cerebrospinal-fluid-and-plasma-in-rats
#16
María Isabel Ruiz-Olmedo, Iliana González-Hernández, Francisca Palomares-Alonso, Javier Franco-Pérez, María de Lourdes González F, Helgi Jung-Cook
Background: Although albendazole is the drug-of-choice for the treatment of neurocysticercosis, its efficacy is limited due to its low bioavailability. An alternative for optimizing pharmacological treatment is through drug combinations. In vitro studies have shown that nitazoxanide and tizoxanide (the active metabolite of nitazoxanide) exhibit cysticidal activity and that the combination of tizoxanide with albendazole sulfoxide (the active metabolite of albendazole) produced an additive effect. Objectives: (1) To assess the concentration profile of tizoxanide in plasma and in cerebrospinal fluid; and (2) to evaluate the influence of nitazoxanide on the pharmacokinetics of albendazole in plasma and in cerebrospinal fluid...
March 2017: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
https://www.readbyqxmd.com/read/28343895/pharmacokinetic-profile-of-promising-acetylcholinesterase-reactivators-k027-and-k203-in-experimental-pigs
#17
Jana Zdarova Karasova, Jaroslav Kvetina, Ilja Tacheci, Vera Radochova, Kamil Musilek, Kamil Kuca, Jan Bures
Standard treatment of organophosphorus compounds (OPs) poisoning includes administration of an anti-muscarinic (atropine), anticonvulsive (diazepam) and acetylcholinesterase reactivator (oxime). From a wide group of newly synthesized oximes, oxime K027 and oxime K203 seem to be perspective compounds in some specific OPs intoxication. The available in vitro and in vivo preclinical data indicate that both oximes may be considered for potential human use. The main aim of this study was to establish plasmatic concentration curves of both oximes after intramuscular (i...
May 5, 2017: Toxicology Letters
https://www.readbyqxmd.com/read/28336779/validation-of-the-semi-quantitative-static-suvr-method-for-18-f-av45-pet-by-pharmacokinetic-modeling-with-an-arterial-input-function
#18
Julie Ottoy, Jeroen Verhaeghe, Ellis Niemantsverdriet, Leonie Wyffels, Charisse Somers, Ellen De Roeck, Hanne Struyfs, Femke Soetewey, Steven Deleye, Tobi Van den Bossche, Sara Van Mossevelde, Sarah Ceyssens, Jan Versijpt, Sigrid Stroobants, Sebastiaan Engelborghs, Steven Staelens
Increased brain uptake of [(18)F]-AV45 visualized by PET is a key biomarker for Alzheimer's disease (AD). The standardized uptake value ratio (SUVR) is widely used for quantification, but is subject to variability based on choice of reference region and changes in cerebral blood flow. Here we validate the SUVR method against the gold standard volume of distribution (VT) to assess cross-sectional differences in plaque load. Methods: Dynamic 60-min [(18)F]-AV45 (291 ± 67 MBq) and 1-min [(15)O]-H2O (370 MBq) scans were obtained in 35 age-matched elderly subjects, including 10 probable AD dementia, 15 amnestic mild cognitive impairment (aMCI) and 10 cognitively healthy controls (HC)...
March 23, 2017: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/28336491/neurobehavioral-effects-of-lithium-in-the-rat-investigation-of-the-effect-concentration-relationships-and-the-contribution-of-the-poisoning-pattern
#19
Anne-Sophie Hanak, Lucie Chevillard, Rodolphe Lebeau, Patricia Risède, Jean-Louis Laplanche, Nadia Benturquia, Bruno Mégarbane
Severity of lithium poisoning depends on the ingested dose, previous treatment duration and renal function. No animal study has investigated neurobehavioral differences in relation to the lithium poisoning pattern observed in humans, while differences in lithium pharmacokinetics have been reported in lithium-pretreated rats mimicking chronic poisonings with enhanced brain accumulation in rats with renal failure. Our objectives were: 1)-to investigate lithium-related effects in overdose on locomotor activity, anxiety-like behavior, spatial recognition memory and anhedonia in the rat; 2)-to model the relationships between lithium-induced effects on locomotion and plasma, erythrocyte, cerebrospinal fluid and brain concentrations previously obtained according to the poisoning pattern...
March 20, 2017: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/28324653/evaluation-of-brain-pharmacokinetic-and-neuropharmacodynamic-attributes-of-an-antiepileptic-drug-lacosamide-in-hepatic-and-renal-impairment-preclinical-evidence
#20
Baldeep Kumar, Manish Modi, Biman Saikia, Bikash Medhi
The knowledge of pharmacokinetic and pharmacodynamic properties of antiepileptic drugs is helpful in optimizing drug therapy for epilepsy. This study was designed to evaluate the pharmacokinetic and pharmacodynamic properties of lacosamide in experimentally induced hepatic and renal impairment in seizure animals. Hepatic or renal impairment was induced by injection of carbon tetrachloride or diclofenac sodium, respectively. After induction, the animals were administered a single dose of lacosamide. At different time points, maximal electroshock (MES) seizure recordings were made followed by isolation of plasma and brain samples for drug quantification and pharmacodynamic measurements...
April 6, 2017: ACS Chemical Neuroscience
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