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https://www.readbyqxmd.com/read/28335563/the-effects-of-sweet-foods-on-the-pharmacokinetics-of-glycyrrhizic-acid-by-icelisa
#1
Bingqian Jiang, Huihua Qu, Hui Kong, Yue Zhang, Shuchen Liu, Jinjun Cheng, Xin Yan, Yan Zhao
The effect of sweet foods, such as honey, was investigated from the perspective of pharmacokinetics on the absorption of glycyrrhizic acid (GA). Due to the unique properties of indirect competitive enzyme-linked immunosorbent assay (icELISA), namely, its: specificity, sensitivity, repeatability, simple pretreatment of samples, fast and simple operation, and because it is economic and non-polluting, it has received increased attention. In this study, we used the advantages of this method to see how honey affected the pharmacokinetics of GA...
March 21, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28335525/the-history-of-clotting-factor-concentrates-pharmacokinetics
#2
REVIEW
Massimo Morfini
Clotting factor concentrates (CFCs) underwent tremendous modifications during the last forty years. Plasma-derived concentrates made the replacement therapy feasible not only in the hospital but also at patients' home by on-demand or prophylactic regimen. Virucidal methods, implemented soon after hepatitis and AIDS outbreak, and purification by Mabs made the plasma-derived concentrates safer and purer. CFCs were considered equivalent to the other drugs and general rules and methods of pharmacokinetics (PK) were applied to their study...
March 20, 2017: Journal of Clinical Medicine
https://www.readbyqxmd.com/read/28335469/comparison-of-the-pharmacokinetic-properties-of-hemoglobin-based-oxygen-carriers
#3
REVIEW
Kazuaki Taguchi, Keishi Yamasaki, Toru Maruyama, Masaki Otagiri
Hemoglobin (Hb) is an ideal material for use in the development of an oxygen carrier in view of its innate biological properties. However, the vascular retention of free Hb is too short to permit a full therapeutic effect because Hb is rapidly cleared from the kidney via glomerular filtration or from the liver via the haptogloblin-CD 163 pathway when free Hb is administered in the blood circulation. Attempts have been made to develop alternate acellular and cellular types of Hb based oxygen carriers (HBOCs), in which Hb is processed via various routes in order to regulate its pharmacokinetic properties...
March 18, 2017: Journal of Functional Biomaterials
https://www.readbyqxmd.com/read/28335443/pharmacokinetic-and-pharmacodynamic-responses-to-clopidogrel-evidences-and-perspectives
#4
REVIEW
Yan-Jiao Zhang, Mu-Peng Li, Jie Tang, Xiao-Ping Chen
Clopidogrel has significantly reduced the incidence of recurrent atherothrombotic events in patients with acute coronary syndrome (ACS) and in those undergoing percutaneous coronary intervention (PCI). However, recurrence events still remain, which may be partly due to inadequate platelet inhibition by standard clopidogrel therapy. Genetic polymorphisms involved in clopidogrel's absorption, metabolism, and the P2Y12 receptor may interfere with its antiplatelet activity. Recent evidence indicated that epigenetic modification may also affect clopidogrel response...
March 14, 2017: International Journal of Environmental Research and Public Health
https://www.readbyqxmd.com/read/28335025/a-novel-lc-ms-ms-method-with-an-effective-antioxidant-for-the-determination-of-edaravone-a-free-radical-scavenger-in-dog-plasma-and-its-application-to-a-pharmacokinetic-study
#5
Feng Shao, Xiao-Ling Hu, Xin Liu, Mang-Ting Shan
The objective of this study was to investigate the stability of edaravone in dog plasma by using an added antioxidant stabilizer, with an ultimate goal of developing and validating a sensitive, reliable and robust LC-MS-MS method for determination of edaravone in plasma samples. Edaravone was unstable in plasma, but it presented a good stability performance in the plasma with sodium metabisulfite (SMB), an effective antioxidant. The blood sample was collected in the heparinized eppendorf tube containing SMB and plasma sample was deproteinized using acetonitrile containing 20 ng/mL of phenacetin (Internal standard)...
March 2, 2017: Journal of Chromatographic Science
https://www.readbyqxmd.com/read/28335023/qbd-driven-development-and-validation-of-liquid-chromatography-tandem-mass-spectrometric-method-for-the-quantitation-of-sildenafil-in-human-plasma
#6
M Saquib Hasnain, Shaukat Ali Ansari, Shireen Rao, Mohammad Tabish, Mukul Singh, Mohammad Syafiq Abdullah, Mohammed Tahir Ansari
The present work was employing the Quality by Design approach for the development and validation of a LC-MS-MS method to support the clinical advancement in determination of sildenafil in human plasma using lorazepam as an internal standard. Sample preparation involved solid phase extraction and calibration range observed between 3 and 1,700 ng/mL. The method was systematically optimized by employing Box-Behnken design and used mobile phase flow rate, pH and composition of mobile phase as the critical factors, and assessing the design for retention time and peak area as the responses...
February 27, 2017: Journal of Chromatographic Science
https://www.readbyqxmd.com/read/28334978/therapeutic-window-of-dopamine-d2-3-receptor-occupancy-to-treat-psychosis-in-alzheimer-s-disease
#7
Suzanne Reeves, Emma McLachlan, Julie Bertrand, Fabrizia D Antonio, Stuart Brownings, Akshay Nair, Suki Greaves, Alan Smith, David Taylor, Joel Dunn, Paul Marsden, Robert Kessler, Robert Howard
Antipsychotic drugs, originally developed to treat schizophrenia, are used to treat psychosis, agitation and aggression in Alzheimer's disease. In the absence of dopamine D2/3 receptor occupancy data to inform antipsychotic prescribing for psychosis in Alzheimer's disease, the mechanisms underpinning antipsychotic efficacy and side effects are poorly understood. This study used a population approach to investigate the relationship between amisulpride blood concentration and central D2/3 occupancy in older people with Alzheimer's disease by combining: (i) pharmacokinetic data (280 venous samples) from a phase I single (50 mg) dose study in healthy older people (n = 20, 65-79 years); (ii) pharmacokinetic, 18F-fallypride D2/3 receptor imaging and clinical outcome data on patients with Alzheimer's disease who were prescribed amisulpride (25-75 mg daily) to treat psychosis as part of an open study (n = 28; 69-92 years; 41 blood samples, five pretreatment scans, 19 post-treatment scans); and (iii) 18F-fallypride imaging of an antipsychotic free Alzheimer's disease control group (n = 10, 78-92 years), to provide additional pretreatment data...
February 4, 2017: Brain: a Journal of Neurology
https://www.readbyqxmd.com/read/28334528/why-prodrugs-and-propesticides-succeed
#8
John E Casida
What are the advantages of bioactivation in optimizing drugs and pesticides? Why are there so many prodrugs and propesticides? These questions are examined here by considering compounds selected on the basis of economic value or market success. The 100 major drugs and 90 major pesticides are divided into ones acting directly and those definitely or possibly requiring bioactivation. Established or candidate prodrugs accounted for 19% of the total drug sales with corresponding values of 20, 37 and 17% for proinsecticides, proherbicides and profungicides...
March 23, 2017: Chemical Research in Toxicology
https://www.readbyqxmd.com/read/28334510/pharmacokinetics-of-testosterone-cream-applied-to-scrotal-skin
#9
R Iyer, S F Mok, S Savkovic, L Turner, G Fraser, R Desai, V Jayadev, A J Conway, D J Handelsman
Scrotal skin is thin and has high steroid permeability, but the pharmacokinetics of testosterone via the scrotal skin route has not been studied in detail. The aim of this study was to define the pharmacokinetics of testosterone delivered via the scrotal skin route. The study was a single-center, three-phase cross-over pharmacokinetic study of three single doses (12.5, 25, 50 mg) of testosterone cream administered in random sequence on different days with at least 2 days between doses to healthy eugonadal volunteers with endogenous testosterone suppressed by administration of nandrolone decanoate...
March 23, 2017: Andrology
https://www.readbyqxmd.com/read/28334018/development-of-an-evidence-evaluation-and-synthesis-system-for-drug-drug-interactions-and-its-application-to-a-systematic-review-of-hiv-and-malaria-co-infection
#10
Kay Seden, Sara Gibbons, Catia Marzolini, Jonathan M Schapiro, David M Burger, David J Back, Saye H Khoo
BACKGROUND: In all settings, there are challenges associated with safely treating patients with multimorbidity and polypharmacy. The need to characterise, understand and limit harms resulting from medication use is therefore increasingly important. Drug-drug interactions (DDIs) are prevalent in patients taking antiretrovirals (ARVs) and if unmanaged, may pose considerable risk to treatment outcome. One of the biggest challenges in preventing DDIs is the substantial gap between theory and clinical practice...
2017: PloS One
https://www.readbyqxmd.com/read/28333661/does-your-drug-expertise-include-clinical-pharmaceutics
#11
David W Newton
Whose job is it to protect patients from harm from drug instabilities and incompatibilities and other aspects of clinical pharmaceutics? Pharmacists are better educated via multiple required general and organic chemistry prerequisite and professional curricula medicinal chemistry and pharmaceutics courses. Therefore, no healthcare professional other than pharmacists are nicknamed drug experts or are better formally educated to master drug chemistry in the bottle (i.e., injection stability and compatibility/incompatibility clinical pharmaceutics) as a prerequisite for drug administration to cause safe and effective drug chemistry in the body (i...
May 2016: International Journal of Pharmaceutical Compounding
https://www.readbyqxmd.com/read/28333546/pharmacokinetics-and-safety-of-vortioxetine-in-pediatric-patients
#12
Robert L Findling, Adelaide S Robb, Melissa DelBello, Michael Huss, Nora McNamara, Elias Sarkis, Russell Scheffer, Lis H Poulsen, Grace Chen, Ole Michael Lemming, Johan Areberg, Philippe Auby
OBJECTIVE: The primary objectives of this study were to evaluate the pharmacokinetics (PK) and tolerability of single and multiple doses of vortioxetine in children and adolescents with a depressive or anxiety disorder and to provide supportive information for appropriate dosing regimens for pediatric clinical trials. METHODS: This prospective, open-label, multinational, multisite, multiple-dose trial enrolled 48 patients (children and adolescents; 1:1 ratio) divided into 8 cohorts (4 adolescent and 4 child), with each cohort including 6 patients...
March 23, 2017: Journal of Child and Adolescent Psychopharmacology
https://www.readbyqxmd.com/read/28333443/systematic-investigation-of-ginkgo-biloba-leaves-for-treating-cardio-cerebrovascular-diseases-in-an-animal-model
#13
Yinfeng Yang, Yan Li, Jinghui Wang, Ke Sun, Weiyang Tao, Zhenzhong Wang, Wei Xiao, Yanqiu Pan, Shuwei Zhang, Yonghua Wang
Globally, cardio-cerebrovascular diseases (CCVDs) account for the leading cause of death, and thus the development of novel strategies for preventing and treating such diseases is in urgent need. Traditional Chinese Medicine (TCM), used for thousands of years in Asia and other regions, have been proven effective in certain disorders. As a medicinal herb for a long time in TCM, Ginkgo Biloba Leaves (GBLs), have been widely used to treat various diseases including CCVDs. However, the underlying molecular mechanisms of medicinal herb in treating these diseases are still unclear...
March 23, 2017: ACS Chemical Biology
https://www.readbyqxmd.com/read/28333347/polymyxin-resistant-carbapenem-resistant-acinetobacter-baumannii-is-eradicated-by-a-triple-combination-of-agents-that-lack-individual-activity
#14
Justin R Lenhard, Visanu Thamlikitkul, Fernanda P Silveira, Samira M Garonzik, Xun Tao, Alan Forrest, Beom Soo Shin, Keith S Kaye, Jürgen B Bulitta, Roger L Nation, Jian Li, Brian T Tsuji
Objectives: The emergence of polymyxin resistance threatens to leave clinicians with few options for combatting drug-resistant Acinetobacter baumannii . The objectives of the current investigation were to define the in vitro emergence of polymyxin resistance and identify a combination regimen capable of eradicating A. baumannii with no apparent drug susceptibilities. Methods: Two clonally related, paired, A. baumannii isolates collected from a critically ill patient who developed colistin resistance while receiving colistin methanesulfonate in a clinical population pharmacokinetic study were evaluated: an A...
February 28, 2017: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/28333284/revisiting-the-mutant-prevention-concentration-to-guide-dosing-in-childhood-tuberculosis
#15
Devan Jaganath, H Simon Schaaf, Peter R Donald
The mutant prevention concentration (MPC) is a well-known concept in the chemotherapy of many bacterial infections, but is seldom considered in relation to tuberculosis (TB) treatment, as the required concentrations are generally viewed as unachievable without undue toxicity. Early studies revealed single mutations conferring high MICs of first- and second-line anti-TB agents; however, the growing application of genomics and quantitative drug susceptibility testing in TB suggests a wide range of MICs often determined by specific mutations and strain type...
March 9, 2017: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/28333192/susceptibilities-of-mdr-mycobacterium-tuberculosis-isolates-to-unconventional-drugs-compared-with-their-reported-pharmacokinetic-pharmacodynamic-parameters
#16
Joseph S Cavanaugh, Ruwen Jou, Mei-Hua Wu, Tracy Dalton, Ekaterina Kurbatova, Julia Ershova, J Peter Cegielski
Background: The second-line drugs recommended to treat drug-resistant TB are toxic, expensive and difficult to procure. Given increasing resistance, the need for additional anti-TB drugs has become more urgent. But new drugs take time to develop and are expensive. Some commercially available drugs have reported anti-mycobacterial activity but are not routinely used because supporting laboratory and clinical evidence is sparse. Methods: We analysed 217 MDR M. tuberculosis isolates including 153 initial isolates from unique patients and 64 isolates from follow-up specimens during the course of treatment...
February 20, 2017: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/28332260/biological-characterization-of-novel-nitroimidazole-peptide-conjugates-in-vitro-and-in-vivo
#17
Ralf Bergmann, Katrin Splith, Jens Pietzsch, Michael Bachmann, Ines Neundorf
Recently, we reported on the design of a multimodal peptide conjugate useful as delivery platform for targeting hypoxic cells. A nitroimidazole (2-(2-nitroimidazol-1-yl)acetic acid, NIA) moiety, which is selectively entrapped in hypoxic cells, was coupled to a cell-penetrating peptide serving as the transporter. Furthermore, attachment of a bifunctional linker allowed the introduction of a diagnostic or therapeutic radiometal. However, although selective tumor accumulation could be detected in vivo, a fast renal clearance of the compound was observed...
March 23, 2017: Journal of Peptide Science: An Official Publication of the European Peptide Society
https://www.readbyqxmd.com/read/28332096/efficacy-and-safety-of-paricalcitol-in-children-with-stages-3-to-5-chronic-kidney-disease
#18
Nicholas J A Webb, Gary Lerner, Bradley A Warady, Katherine M Dell, Larry A Greenbaum, Gema Ariceta, Bernd Hoppe, Peter Linde, Ho-Jin Lee, Ann Eldred, Matthew B Dufek
BACKGROUND: Elevated intact parathyroid hormone (iPTH) levels can contribute to morbidity and mortality in children with chronic kidney disease (CKD). We evaluated the pharmacokinetics, efficacy, and safety of oral paricalcitol in reducing iPTH levels in children with stages 3-5 CKD. METHODS: Children aged 10-16 years with stages 3-5 CKD were enrolled in two phase 3 studies. The stage 3/4 CKD study characterized paricalcitol pharmacokinetics and compared the efficacy and safety of paricalcitol with placebo followed by an open-label period...
March 22, 2017: Pediatric Nephrology: Journal of the International Pediatric Nephrology Association
https://www.readbyqxmd.com/read/28332049/molecular-and-pharmacological-mechanisms-of-drug-resistance-an-evolving-paradigm
#19
Benedetta Colmegna, Lavinia Morosi, Maurizio D'Incalci
The high heterogeneity and genomic instability of malignant tumors explains why even responsive tumors contain cell clones that are resistant for many possible mechanisms involving intracellular drug inactivation, low uptake or high efflux of anticancer drugs from cancer cells, qualitative or quantitative changes in the drug target. Many tumors, however, are resistant because of insufficient exposure to anticancer drugs, due to pharmacokinetic reasons and inefficient and heterogeneous tumor drug distribution, related to a deficient vascularization and high interstitial pressure...
March 23, 2017: Handbook of Experimental Pharmacology
https://www.readbyqxmd.com/read/28331929/confirmation-of-longer-fix-activity-half-life-with-prolonged-sample-collection-after-single-doses-of-nonacog-alfa-in-patients-with-haemophilia-b
#20
Baolai Hua, Runhui Wu, FeiFei Sun, Binyu Luo, Christine Alvey, Robert Labadie, Peng Roger Qu, Joan M Korth-Bradley, Pablo Rendo
A multicentre, single-dose study enrolled 12 previously treated patients with moderately severe to severe (factor IX [FIX] levels ≤2 IU/dl) haemophilia B to assess FIX pharmacokinetics after nonacog alfa administration and to evaluate the impact of length of sampling time on half-life (t½). After refraining from FIX replacement for four days, patients received 50 IU/kg as an intravenous (IV) infusion over 10 minutes. Blood samples were collected predose and 0.25, 0.5, 1, 3, 6, 9, 24, 50, 72, and 96 h post dose...
March 23, 2017: Thrombosis and Haemostasis
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