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pharmacokinetics, brain, plasma

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https://www.readbyqxmd.com/read/28710563/an-observational-study-examining-the-effects-of-a-surgically-induced-inflammatory-response-on-the-distribution-of-morphine-and-its-metabolites-into-cerebrospinal-fluid
#1
Yan Wang, Kerry B Goralski, Derek J Roberts, Kathryn Landry, Mark E Issa, Lekha Sleno, Lisa C Julien, Jeremy Wood, Richard I Hall
PURPOSE: Morphine is administered intravenously for pain management in the perioperative period. The effect of the inflammatory response to surgery on morphine distribution across the blood-brain barrier (BBB) in humans was investigated. We hypothesized that a graded surgically induced, systemic inflammatory response alters cerebrospinal fluid (CSF) levels of morphine, morphine-3-glucuronide (M3G), and morphine-6-glucuronide (M6G) through a temporary reduction in BBB drug efflux transporter function...
July 14, 2017: Canadian Journal of Anaesthesia, Journal Canadien D'anesthésie
https://www.readbyqxmd.com/read/28705616/improvement-of-the-surface-hydrophilic-properties-of-naproxen-particles-with-addition-of-hydroxypropylmethyl-cellulose-and-sodium-dodecyl-sulphate-in-vitro-and-in-vivo-studies
#2
Víctor García-Herrero, Carlos Torrado, Juan José García-Rodríguez, Alicia López-Sánchez, Susana Torrado, Santiago Torrado-Santiago
In this study, a new surface-modified naproxen was developed to enhance brain concentration in acute migraine treatment. Fast-dissolving naproxen granules were made by mixing hydroxypropylmethylcellulose (HPMC) sodium dodecyl sulphate (SDS) and sodium croscarmellose with micronized naproxen particles. The aim of this study was to evaluate the effect of adding proportions of SDS to the HPMC film caused changes in the polymer chains of the HPMC, producing a new hydrophilic HPMC-SDS structure. These formulations with different HPMC/SDS ratios were characterised using electron microscopy (SEM), powder X-ray diffraction (PXRD), and differential scanning calorimetry (DSC)...
July 10, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28702763/pharmacokinetics-of-antifungal-drugs-practical-implications-for-optimized-treatment-of-patients
#3
REVIEW
Romuald Bellmann, Piotr Smuszkiewicz
INTRODUCTION: Because of the high mortality of invasive fungal infections (IFIs), appropriate exposure to antifungals appears to be crucial for therapeutic efficacy and safety. MATERIALS AND METHODS: This review summarises published pharmacokinetic data on systemically administered antifungals focusing on co-morbidities, target-site penetration, and combination antifungal therapy. CONCLUSIONS AND DISCUSSION: Amphotericin B is eliminated unchanged via urine and faeces...
July 12, 2017: Infection
https://www.readbyqxmd.com/read/28698254/mechanism-based-pharmacokinetic-pharmacodynamic-modeling-of-the-glucagon-like-peptide-1-receptor-agonist-exenatide-to-characterize-its-anti-obesity-effects-in-diet-induced-obese-mice
#4
Shinji Iwasaki, Teruki Hamada, Ikumi Chisaki, Tomohiro Andou, Noriyasu Sano, Atsutoshi Furuta, Nobuyuki Amano
Glucagon-like peptide-1 (GLP-1) analogs lower body weight in humans in addition to their potent anti-diabetic effects. Hence, agonistic targeting of the GLP-1 receptor could be a valid approach to target obesity. However, quantitative analyses of the pharmacokinetic/pharmacodynamic (PK/PD) relationship between GLP-1 analogs and their anti-obesity effect have not been reported in either animals or humans. Therefore, the present study was performed to establish a mechanism-based PK/PD model of GLP-1 receptor agonists using the GLP-1 analog, exenatide, for the development of promising new anti-obesity drugs...
July 11, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28694087/a-mathematical-model-of-a-recombinant-humanized-anti-cocaine-monoclonal-antibody-s-effects-on-cocaine-pharmacokinetics-in-mice
#5
Hanna N Wetzel, Tongli Zhang, Andrew B Norman
AIMS: A recombinant humanized anti-cocaine monoclonal antibody (mAb), h2E2, is at an advanced stage of pre-clinical development as an immunotherapy for cocaine abuse. It is hypothesized that h2E2 binds to and sequesters cocaine in the blood. MAIN METHODS: A three-compartment model of the effects of h2E2 on cocaine's distribution was constructed. The model assumes that h2E2 binds to cocaine and that the h2E2-cocaine complex does not enter the brain but distributes between the central and peripheral compartments...
July 7, 2017: Life Sciences
https://www.readbyqxmd.com/read/28688108/a-physiologically-based-pharmacokinetic-modeling-approach-to-predict-buprenorphine-pharmacokinetics-following-intravenous-sublingual-administration
#6
Hari V Kalluri, Hongfei Zhang, Steve N Caritis, Raman Venkataramanan
INTRODUCTION: Opioid dependence is associated with high morbidity and mortality. Buprenorphine(BUP) is approved by the FDA to treat opioid dependence. There is a lack of clear consensus on appropriate dosing of BUP due to inter-patient physiological differences in absorption/disposition, subjective response assessment and other patient comorbidities. The objective of this study is to build and validate robust physiologically-based-pharmacokinetic(PBPK) models for intravenous(IV) and Sublingual(SL) BUP as a first-step to optimize BUP pharmacotherapy...
July 8, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28684900/intranasal-agomelatine-solid-lipid-nanoparticles-to-enhance-brain-delivery-formulation-optimization-and-in-vivo-pharmacokinetics
#7
Ahmed M Fatouh, Ahmed H Elshafeey, Ahmed Abdelbary
PURPOSE: Agomelatine is a novel antidepressant drug suffering from an extensive first-pass metabolism leading to a diminished absolute bioavailability. The aim of the study is: first to enhance its absolute bioavailability, and second to increase its brain delivery. METHODS: To achieve these aims, the nasal route was adopted to exploit first its avoidance of the hepatic first-pass metabolism to increase the absolute bioavailability, and second the direct nose-to-brain pathway to enhance the brain drug delivery...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28682148/pharmacokinetics-of-an-intracerebroventricularly-administered-antibody-in-rats
#8
Yuki Noguchi, Motohiro Kato, Kazuhisa Ozeki, Masaki Ishigai
The pharmacokinetics (PK) of an antibody in the brain and the spinal cord is insufficiently understood, which is an obstacle to the discovery of antibody drugs that target diseases in the central nervous system. In this study, we focused on the elimination of IgG from cerebrospinal fluid (CSF) circulating in the brain and the spinal cord in rats, and, in order to evaluate the influence of CSF bulk flow on the clearance of IgG, also examined the PK of inulin in CSF. To monitor their concentrations in CSF, IgG and inulin were co-administered into the lateral ventricle via a catheter, and CSF was collected from the cisterna magna via another catheter time-sequentially...
July 6, 2017: MAbs
https://www.readbyqxmd.com/read/28679777/efficacy-of-onalespib-a-long-acting-second-generation-hsp90-inhibitor-as-a-single-agent-and-in-combination-with-temozolomide-against-malignant-gliomas
#9
Alessandro Canella, Alessandra M Welker, Ji Young Yoo, Jihong Xu, Fazly S Abbas, Divya Kesanakurti, Prabhakaran Nagarajan, Christine E Beattie, Erik P Sulman, Joseph L Liu, Joy Gumin, Frederick F Lang, Metin Gurcan, Balveen Kaur, Deepa Sampath, Vinay K Puduvalli
HSP90, a highly conserved molecular chaperone that regulates the function of several oncogenic client proteins is altered in glioblastoma. However, HSP90 inhibitors currently in clinical trials are short-acting, have unacceptable toxicities or are unable to cross the blood brain barrier (BBB). We examined the efficacy of onalespib, a potent, long-acting novel HSP90 inhibitor as a single agent and in combination with temozolomide (TMZ) against gliomas invitro and invivo<br /><br />Experimental Design: The effect of onalespib on HSP90, its client proteins, and on the biology of glioma cell lines and patient-derived glioma-initiating cells (GSC) was determined...
July 5, 2017: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/28677844/enantioselective-analysis-of-ibuprofen-enantiomers-in-mice-plasma-and-tissues-by-high-performance-liquid-chromatography-with-fluorescence-detection-application-to-a-pharmacokinetic-study
#10
Katarzyna Przejczowska-Pomierny, Monika Włodyka, Agnieszka Cios, Elżbieta Wyska
A direct fluorometric high-performance liquid chromatography (HPLC) method was developed and validated for the analysis of ibuprofen enantiomers in mouse plasma (100 μl) and tissues (brain, liver, kidneys) using liquid-liquid extraction and 4-tertbutylphenoxyacetic acid as an internal standard. Separation of enantiomers was accomplished in a Chiracel OJ-H chiral column based on cellulose tris(4-methylbenzoate) coated on 5 μm silica-gel, 250 x 4.6 mm at 22 °C with a mobile phase composed of n-hexane, 2-propanol, and trifluoroacetic acid that were delivered in gradient elution at a flow rate of 1 ml min(-1) ...
July 5, 2017: Chirality
https://www.readbyqxmd.com/read/28664226/eribulin-shows-high-concentration-and-long-retention-in-xenograft-tumor-tissues
#11
Michiko Sugawara, Krista Condon, Earvin Liang, Christopher DesJardins, Edgar Schuck, Kazutomi Kusano, W George Lai
PURPOSE: Eribulin, a synthetic analog of the natural product halichondrin B, is a microtubule dynamics inhibitor. In this study, we report the pharmacokinetic profiles of eribulin in mice, rats, and dogs following intravenous administrations with optimized and validated bio-analytical methods. METHODS: Eribulin was administered at 0.5 and 2 mg/kg in mice, 0.5 and 1 mg/kg in rats, and 0.08 mg/kg in dogs. Tumor and brain penetration of eribulin was also evaluated in LOX human melanoma xenograft models...
June 29, 2017: Cancer Chemotherapy and Pharmacology
https://www.readbyqxmd.com/read/28662899/l-type-amino-acid-transporter-1-utilizing-prodrugs-how-to-achieve-effective-brain-delivery-and-low-systemic-exposure-of-drugs
#12
Elena Puris, Mikko Gynther, Johanna Huttunen, Aleksanteri Petsalo, Kristiina M Huttunen
L-type amino acid transporter 1 (LAT1) is selectively expressed in the blood-brain barrier (BBB) and brain parenchyma. This transporter can facilitate brain delivery of neuroprotective agents and additionally give opportunity to minimize systemic exposure. Here, we investigated structure-pharmacokinetics relationship of five newly synthesized LAT1-utilizing prodrugs of the cyclooxygenase inhibitor, ketoprofen, in order to identify beneficial structural features of prodrugs to achieve both targeted brain delivery and low peripheral distribution of the parent drug...
June 27, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/28662343/effect-of-chronic-%C3%AE-hydroxybutyrate-ghb-administration-on-ghb-toxicokinetics-and-ghb-induced-respiratory-depression
#13
Bridget L Morse, Gurkishan S Chadha, Melanie A Felmlee, Kristin E Follman, Marilyn E Morris
BACKGROUND: γ-hydroxybutyrate (GHB) has a high potential for illicit use; overdose of this compound results in sedation, respiratory depression and death. Tolerance to the hypnotic/sedative and electroencephalogram effects of GHB occurs with chronic GHB administration; however, tolerance to respiratory depression has not been evaluated. GHB toxicodynamic effects are mediated predominantly by GABAB receptors. Chronic treatment may affect monocarboxylate transporters (MCTs) and alter the absorption, renal clearance and brain uptake of GHB...
June 29, 2017: American Journal of Drug and Alcohol Abuse
https://www.readbyqxmd.com/read/28656123/determination-of-epimedin-b-in-rat-plasma-and-tissue-by-lc-ms-ms-application-in-pharmacokinetic-and-tissue-distribution-studies
#14
Qianru Feng, Shunjun Xu, Jiejing Yu, Shuai Sun, Liu Yang
A simple, sensitive, and specific liquid chromatography tandem mass-spectrometric method was developed and validated for the determination of epimedin B in rat plasma and tissue samples. After being processed with a protein precipitation method, these samples were separated on an Agilent Eclipse XDB-C18 column with an isocratic mobile phase consisting of acetonitrile and 0.1% formic acid aqueous solution (32 : 68, v/v). The calibration curve of epimedin B was linear over the concentration range from 1 to 500 ng/mL in plasma and tissue homogenate...
2017: Journal of Analytical Methods in Chemistry
https://www.readbyqxmd.com/read/28655495/tranylcypromine-in-mind-part-i-review-of-pharmacology
#15
REVIEW
Sven Ulrich, Roland Ricken, Mazda Adli
It has been over 50 years since a review has focused exclusively on the monoamine oxidase (MAO) inhibitor tranylcypromine (TCP). A new review has therefore been conducted for TCP in two parts which are written to be read preferably in close conjunction: Part I - pharmacodynamics, pharmacokinetics, drug interactions, toxicology; and Part II - clinical studies with meta-analysis of controlled studies in depression, practice of TCP treatment, place in therapy. Pharmacological data of this review part I characterize TCP as an irreversible and nonselective MAO-A/B inhibitor at low therapeutic doses of 20mg/day with supplementary norepinephrine reuptake inhibition at higher doses of 40-60mg/day...
June 24, 2017: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28648684/hbk-15-protects-mice-from-stress-induced-behavioral-disturbances-and-changes-in-corticosterone-bdnf-and-ngf-levels
#16
Karolina Pytka, Monika Głuch-Lutwin, Magdalena Kotańska, Elżbieta Żmudzka, Magdalena Jakubczyk, Anna Waszkielewicz, Paulina Janiszewska, Maria Walczak
Unlike majority of current antidepressants, HBK-15-a 5-HT1A and 5-HT7 receptor antagonist - showed memory-enhancing properties. In this study, we aimed to further characterize pharmacological profile of HBK-15 and investigate its antidepressant- and anxiolytic-like activity in the mouse model of unpredictable chronic mild stress. We used sucrose consumption test, forced swim test and elevated plus maze test as behavioral endpoints. We also evaluated the influence of HBK-15 on brain-derived neurotrophic factor (BDNF) and nerve growth factor (NGF) levels in the hippocampus and prefrontal cortex, as well as body weight, relative adrenal glands weight and plasma corticosterone level in the stressed mice...
June 23, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28617434/lispro-mitigates-%C3%AE-amyloid-and-associated-pathologies-in-alzheimer-s-mice
#17
Ahsan Habib, Darrell Sawmiller, Song Li, Yang Xiang, David Rongo, Jun Tian, Huayan Hou, Jin Zeng, Adam Smith, Shengnuo Fan, Brian Giunta, Takashi Mori, Glenn Currier, Douglas Ronald Shytle, Jun Tan
Lithium has been marketed in the United States of America since the 1970s as a treatment for bipolar disorder. More recently, studies have shown that lithium can improve cognitive decline associated with Alzheimer's disease (AD). However, the current United States Food and Drug Administration-approved lithium pharmaceutics (carbonate and citrate chemical forms) have a narrow therapeutic window and unstable pharmacokinetics that, without careful monitoring, can cause serious adverse effects. Here, we investigated the safety profile, pharmacokinetics, and therapeutic efficacy of LISPRO (ionic co-crystal of lithium salicylate and l-proline), lithium salicylate, and lithium carbonate (Li2CO3)...
June 15, 2017: Cell Death & Disease
https://www.readbyqxmd.com/read/28602600/influence-of-the-dual-combination-of-silymarin-and-epigallocatechin-gallate-natural-dietary-flavonoids-on-the-pharmacokinetics-of-oxcarbazepine-in-rats
#18
Ana Ferreira, Márcio Rodrigues, Alexandre Marques, Amílcar Falcão, Gilberto Alves
Considering the potential of flavonoids in reversing the P-glycoprotein (P-gp)-mediated multidrug resistance, this work aimed to assess the combined effects of silymarin and (-)-epigallocatechin gallate (EPG) on the pharmacokinetics of the P-gp substrates oxcarbazepine (OXC) and licarbazepine (LIC). Rats were pre-treated intraperitoneally with silymarin (25 mg/kg), EPG (25 mg/kg), silymarin/EPG (12.5/12.5 mg/kg; 6.25/18.75 mg/kg; 18.75/6.25 mg/kg) or verapamil (25 mg/kg, reference P-gp inhibitor) before the intraperitoneal administration of OXC (50 mg/kg)...
June 8, 2017: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/28595534/a-review-of-levetiracetam-in-neonates
#19
Amit Agrawal, Anita Banergee
BACKGROUND: Neonatal seizures are the most common clinical manifestation of central nervous system (CNS) dysfunction and are associated with various neurological sequelae. There are currently no evidence-based guidelines for the management of neonatal seizures and currently used drugs such as phenobarbital, and phenytoin have limited efficacy and potential toxicities. Newer second line anticonvulsant, levetiracetam, has been used in refractory neonatal seizures despite limited data and off-label use...
June 6, 2017: Current Drug Metabolism
https://www.readbyqxmd.com/read/28587251/pharmacokinetics-and-tissue-distribution-kinetics-of-puerarin-in-rats-using-indirect-competitive-elisa
#20
Hui Kong, Xueqian Wang, Rongfeng Shi, Yan Zhao, Jinjun Cheng, Xin Yan, Xiaoman Liu, Yongzhi Wang, Meiling Zhang, Qingguo Wang, Huihua Qu
Puerarin (PUE) is a compound isolated from the roots of Pueraria lobata. We studied the pharmacokinetics and tissue distribution kinetics of PUE in Sprague-Dawley rats following intraperitoneal administration of three concentrations. Indirect competitive ELISA based on an anti-PUE monoclonal antibody was used to determine the concentration of PUE in the blood, heart, liver, spleen, lung, kidney, hippocampus, cerebral cortex, and striatum. The plasma and tissue distribution kinetic characteristics following a single injection of PUE (20, 40 and 80 mg/kg) were calculated using a non-compartment model...
June 5, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
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