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https://www.readbyqxmd.com/read/29241109/pharmacokinetic-studies-of-naproxen-amides-of-some-amino-acid-esters-with-promising-colorectal-cancer-chemopreventive-activity
#1
Tarek Aboul-Fadl, Soliman S Al-Hamad, Ehab A Fouad
Naproxen (nap) is belonging to Non-steriodal anti-inflammatory drugs (NSAIDs) group of drugs that characterized by their free carboxylic group. The therapeutic activity of nap is usually accompanied by GI untoward side effects. Recently synthesized naproxen amides of some amino acid esters prodrugs to mask the free carboxylic group were reported. Those prodrugs showed a promising colorectal cancer chemopreventive activity. The current study aims to investigate the fate and hydrolysis of the prodrugs kinetically in different pH conditions, simulated gastric and intestinal fluids with pHs of 1...
December 2, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29241059/moxidectin-residues-in-lamb-tissues-development-and-validation-of-analytical-method-by-uhplc-ms-ms
#2
Michelle Del Bianchi A Cruz, Maria A M Fernandes, Patricia A de C Braga, Alda L G Monteiro, Daniela Daniel, Felix G R Reyes
The development and validation of a throughput method for the quantitation of moxidectin residues in lamb target tissues (muscle, kidney, liver and fat) was conducted using ultra-high-performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS). To achieve higher recovery of the analyte from the matrices, a modified QuEChERS method was used for sample preparation. The chromatographic separation was achieved using a Zorbax Eclipse Plus C18 RRHD column with a mobile phase comprising 5mM ammonium formate solution +0...
December 11, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/29240650/oxytocin-use-in-labor-legal-implications
#3
Susan Drummond
Oxytocin is one of the most commonly used medications in obstetrics and has been associated with claims of negligence in cases of adverse outcomes. Errors involving intravenous oxytocin administration for induction or augmentation of labor are most commonly dose related and include failure to avoid or treat tachysystole or failure to asses or treat a fetal heart rate pattern indicative of disruption in oxygenation. Clinicians should be knowledgeable regarding pharmacokinetics of oxytocin and the effect of uterine contractions on fetal oxygenation as well as safe titration of oxytocin to achieve the desired effect while minimizing harm...
December 13, 2017: Journal of Perinatal & Neonatal Nursing
https://www.readbyqxmd.com/read/29240409/from-experiments-to-a-fast-easy-to-use-computational-methodology-to-predict-human-aldehyde-oxidase-selectivity-and-metabolic-reactions
#4
Gabriele Cruciani, Nicolò Milani, Paolo Benedetti, Susan Lepri, Lucia Cesarini, Massimo Baroni, Francesca Spyrakis, Sara Tortorella, Edoardo Mosconi, Laura Goracci
Aldehyde oxidase (AOX) is a molibdo-flavoenzyme that raised great interest in recent years, since its contribution in xenobiotics metabolism has not always been identified before clinical trials, with consequent negative effects on the fate of new potential drugs. The fundamental role of AOX in metabolizing xenobiotics is also due to the attempt of medicinal chemists to stabilize candidates toward cytochrome P450 activity, which increases the risk for new compounds to be susceptible to AOX nucleophile attack...
December 14, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29240266/posaconazole-oral-dose-and-plasma-levels-in-pediatric-hematology-oncology-patients
#5
Edoardo Bruno Vicenzi, Elisabetta Calore, Nunzia Decembrino, Massimo Berger, Katia Perruccio, Francesca Carraro, Sara Rossin, Maria Caterina Putti, Mariadelfina Molinaro, Gloria Tridello, Simone Cesaro
BACKGROUND: Posaconazole is a triazole with limited pharmacokinetic information in children. This study assessed the correlation between posaconazole-oral-solution daily dosage/kg/body weight and trough plasma level. METHODS: 97 hematology-oncology pediatric patients with > 1 posaconazole plasma level (PPC) assessment in the first 6 weeks after the start of posaconazole treatment were included. RESULTS: Posaconazole was used as prophylaxis in 84 of 97 (87%) patients and as therapy in 13 of 97 (13%)...
December 14, 2017: European Journal of Haematology
https://www.readbyqxmd.com/read/29239784/new-perspectives-for-natural-triterpene-glycosides-as-potential-adjuvants
#6
Marie-Aleth Lacaille-Dubois, Hildebert Wagner
BACKGROUND: Triterpene glycosides are a vast group of secondary metabolites widely distributed in plants including a high number of biologically active compounds. The pharmacological potential is evaluated by using many bioassays particularly in the field of cancerology, immunology, and microbiology. The adjuvant concept is well known for these molecules in vaccines, but there is little preclinical evidence to support this concept in the management of cancer, infections and inflammation...
November 7, 2017: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/29239601/preparation-and-pharmaceutical-characterizations-of-lipidated-dimeric-xenopus-glucagon-like-peptide-1-conjugates
#7
Jing Han, Feng Zhou, Yingying Fei, Xinyu Chen, Junjie Fu, Hai Qian
Two glucagon-like peptide-1 (GLP-1) analogs (1 and 2) were synthesized by hybridizing the key sequences of GLP-1, exendin-4, lixisenatide and xenGLP-1B (Xenopus GLP-1 analog). To achieve long-acting hypoglycemic effects and to further improve their antidiabetic potencies, lipidization and dimerization strategies were used to afford two lipidated dimeric conjugates (9 and 11). Conjugates 9 and 11 showed stronger receptor activation potency than GLP-1 and exendin-4 in vitro. Moreover, 9 and 11 exhibited superior hypoglycemic and insulinotropic activities to liraglutide in db/db mice...
December 14, 2017: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/29239156/do-patients-require-escorts-or-carers-for-discharge-following-day-surgery-and-office-based-anesthesia-both-sides-of-the-debate-explored
#8
Keira P Mason, Christopher M Burkle
Over the past few years, there has been a rapid rise in office-based procedures, out of hospital and day surgery procedures, particularly as an effort to combat the escalating costs of hospital- based services. Coincident with this burgeoning demand for office based anesthesia, is the accompanying increased risk of anesthesia and sedation-related complications. In the 1990's and 2000's, the risk of mortality was higher for anesthetics and sedations performed outside of the operating theater setting. Although guidelines exist for ambulatory and office based anesthesia, they are being continuously reviewed and reconsidered...
December 13, 2017: Minerva Anestesiologica
https://www.readbyqxmd.com/read/29239016/intestinal-and-hepatic-contributions-to-the-pharmacokinetic-interaction-between-gamithromycin-and-rifampicin-after-single-dose-and-multiple-dose-administration-in-healthy-foals
#9
S Berlin, S Wallstabe, E Scheuch, S Oswald, M Hasan, D Wegner, M Grube, M Venner, A Ullrich, W Siegmund
BACKGROUND: Standard treatment of foals with severe abscessing lung infection caused by Rhodococcus equi using rifampicin and a macrolide antibiotic can be compromised by extensive inhibition and/or induction of drug metabolising enzymes (e.g. CYP3A4) and transport proteins (e.g. P-glycoprotein), as has been shown for rifampicin and clarithromycin. The combination of rifampicin with the new, poorly metabolised gamithromycin, a long-acting analogue of azithromycin and tulathromycin with lower pharmacokinetic interaction potential, might be a suitable alternative...
December 14, 2017: Equine Veterinary Journal
https://www.readbyqxmd.com/read/29239002/pharmacokinetics-of-osimertinib-in-chinese-patients-with-advanced-nsclc-a-phase-1-study
#10
Hongyun Zhao, Junning Cao, Jianhua Chang, Zhenxian Zhang, Li Yang, Jia Wang, Mireille Cantarini, Li Zhang
Osimertinib is an oral, irreversible, central nervous system active epidermal growth factor receptor (EGFR)-tyrosine kinase inhibitor (TKI) selective for both EGFR-TKI sensitizing and T790M resistance mutations. The study's (NCT02529995) primary objective was to characterize the pharmacokinetics (PK) of osimertinib and its metabolites in Chinese patients enrolled in China. PK was assessed following single and multiple doses of 40 or 80 mg osimertinib once daily. Patients were aged ≥ 18 years with locally advanced or metastatic EGFR-TKI-sensitizing (EGFRm) non-small cell lung cancer and World Health Organization performance status of 0/1, who had progressed following prior EGFR-TKI...
December 14, 2017: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29239000/minimal-physiologically-based-pharmacokinetic-and-drug-drug-disease-interaction-model-of-rivaroxaban-and-verapamil-in-healthy-and-renally-impaired-subjects
#11
Mohamed Ismail, Vincent H Lee, Christina R Chow, Christopher M Rubino
Current dosing recommendations for rivaroxaban advocate dosage reduction in patients with moderate to severe renal impairment and avoidance of concomitant strong inhibitors of CYP3A or P-glycoprotein. However, rivaroxaban dosing in patients with mild renal impairment taking concomitant moderate inhibitors of CYP3A and P-glycoprotein is not addressed. To quantify the impacts of concomitant verapamil administration and renal impairment on rivaroxaban pharmacokinetics, a minimal physiologically based pharmacokinetic model system was developed and used to evaluate potential increases in rivaroxaban exposure and the consequent increase in risk of major bleeding...
December 14, 2017: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29238995/test-dose-pharmacokinetics-in-pediatric-patients-receiving-once-daily-iv-busulfan-conditioning-for-hematopoietic-stem-cell-transplant-a-reliable-approach
#12
Kristina M Brooks, Paul Jarosinski, Thomas Hughes, Elizabeth Kang, Nirali N Shah, John B Le Gall, Dennis D Hickstein, Suk See De Ravin, Jomy M George, Parag Kumar
Intravenous (IV) busulfan test dose pharmacokinetics (PK) has been shown to accurately predict once-daily dose requirements and improve outcomes in adult transplant patients, but there are limited data to support this approach in children. Test doses of busulfan ∼0.8 mg/kg were infused over 2 to 3 hours, followed by serial sampling to 4-6 hours postinfusion in pediatric hematopoietic stem cell transplant recipients (n = 5). Once-daily busulfan doses were calculated based on a myelosuppressive area under the concentration-time curve (AUC) target of ∼3700 to 4000 μmol·min/L and assumed dose-proportionality to the test dose...
December 14, 2017: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29238994/intestinal-p-glycoprotein-inhibitors-benzoxanthone-analogues
#13
Song Wha Chae, Jaeok Lee, Jung Hyun Park, Youngjoo Kwon, Younghwa Na, Hwa Jeong Lee
OBJECTIVES: The inhibitors of P-glycoprotein (P-gp) which limits an access of exogenous compounds in the luminal membrane of the intestine have been studied to enhance the intestinal P-gp-mediated absorption of anticancer drugs. METHODS: Inhibition of the efflux pump by synthesized benzoxanthone derivatives was investigated in vitro and in vivo. MCF-7/ADR cell line was used for cytotoxicity assay and [3 H]-daunomycin (DNM) accumulation/efflux study. Eight benzoxanthone analogues were tested for their effects on DNM cytotoxicity...
December 13, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29238984/differing-disintegration-and-dissolution-rates-pharmacokinetic-profiles-and-gastrointestinal-tolerability-of-over-the-counter-ibuprofen-formulations
#14
Ingvar Bjarnason, Ozgur Sancak, Anne Crossley, Andrew Penrose, Angel Lanas
OBJECTIVES: Formulations of over the counter (OTC) NSAIDs differ substantially, but information is lacking on whether this alters their gastrointestinal profiles. To assess disintegration and dissolution rates and pharmacokinetics of four preparations of OTC ibuprofen and relate these with spontaneously reported gastrointestinal adverse events. METHODS: Disintegration and dissolution rates of ibuprofen tablets as (a) acid, (b) sodium salt, (c) lysine salt, and (d) as a liquid gelatine capsule were assessed...
December 13, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29238962/population-pharmacokinetics-of-polymyxin-b
#15
Pooja Manchandani, Visanu Thamlikitkul, Yanina Dubrovskaya, Jessica T Babic, David C Lye, Lawrence S Lee, Vincent H Tam
Polymyxin B is used as a last treatment resort for multidrug-resistant Gram-negative bacterial infections. The objectives of this study were to examine the population pharmacokinetics of polymyxin B and investigate factor(s) influencing pharmacokinetic variability. Four serial blood samples each were collected from 35 adult patients at steady state. The concentrations of individual polymyxin B components were analyzed using a validated LCMS/MS assay and combined to derive total concentrations. A maximum likelihood expectation maximization approach was used to fit the data...
December 14, 2017: Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29238223/the-effect-of-medication-nonadherence-on-progression-free-survival-among-patients-with-renal-cell-carcinoma
#16
Jason Shafrin, Jeffrey Sullivan, Jacquelyn W Chou, Michael N Neely, Justin F Doan, J Ross Maclean
Objective: To examine how observed medication nonadherence to 2 second-line, oral anticancer medications (axitinib and everolimus) affects progression-free survival (PFS) among patients with renal cell carcinoma. Methods: We used an adherence-exposure-outcome model to simulate the impact of adherence on PFS. Using a pharmacokinetic/pharmacodynamic (PK/PD) population model, we simulated drug exposure measured by area under the plasma concentration-time curve (AUC) and minimum blood or trough concentration (Cmin) under 2 scenarios: 1) optimal adherence and 2) real-world adherence...
2017: Cancer Management and Research
https://www.readbyqxmd.com/read/29238169/bioequivalence-study-of-two-formulations-of-flupirtine-maleate-capsules-in-healthy-male-chinese-volunteers-under-fasting-and-fed-conditions
#17
Yanfang Liu, Hua Huo, Zhibo Zhao, Wenli Hu, Yujia Sun, Yunbiao Tang
Aim: This study developed a high-performance liquid chromatography-tandem mass spectrometry method to simultaneously determine the concentrations of flupirtine and its major active metabolite D-13223 in human plasma in order to assess the bioequivalence (BE) of two flupirtine maleate capsules among healthy male Chinese volunteers under fasting and fed conditions. Materials and methods: There were two single-center, randomized, single-dose, open-label, laboratory-blinded, two-period, cross-over studies which included 24 healthy male Chinese volunteers under fasting and fed conditions, respectively...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29237680/personalized-anticoagulation-optimizing-warfarin-management-using-genetics-and-simulated-clinical-trials
#18
Kourosh Ravvaz, John A Weissert, Christian T Ruff, Chih-Lin Chi, Peter J Tonellato
BACKGROUND: Clinical trials testing pharmacogenomic-guided warfarin dosing for patients with atrial fibrillation have demonstrated conflicting results. Non-vitamin K antagonist oral anticoagulants are expensive and contraindicated for several conditions. A strategy optimizing anticoagulant selection remains an unmet clinical need. METHODS AND RESULTS: Characteristics from 14 206 patients with atrial fibrillation were integrated into a validated warfarin clinical trial simulation framework using iterative Bayesian network modeling and a pharmacokinetic-pharmacodynamic model...
December 2017: Circulation. Cardiovascular Genetics
https://www.readbyqxmd.com/read/29237390/chronopharmacokinetic-evaluation-of-budesonide-multiparticulate-systems
#19
Sowjanya Battu, Prasanna Raju Yalavarthi, G V Subbareddy, Uma Maheswara Rao, Jyothshna Devi Katamreddy, Harini Cowdary Vadlamudi
Poor oral absorption of budesonide limits design of its solid oral dosage form. With this context, multiparticulate pulsatile system of budesonide for chronotherapy of nocturnal asthma was aimed in this study. Initially, solid dispersions of budesonide (BD) using sodium starch glycolate (SSG) and guar gum (GG) were developed and characterized. Uniform sized non-pariel seeds (~400 µm) were coated with solid dispersions to obtain immediate (BMP) and controlled release pellets by solution layering technique. Pulsatile drug release pellets (BMPP) were obtained by coating the controlled release pellets with Eudragit L100 and RS 100...
December 12, 2017: Recent Patents on Drug Delivery & Formulation
https://www.readbyqxmd.com/read/29237296/pharmacokinetic-evaluation-of-besifovir-for-the-treatment-of-hbv-infection
#20
Lung-Yi Mak, Wai-Kay Seto, Ching-Lung Lai, Man-Fung Yuen
Besifovir (LB80380) is a relatively new oral acyclic nucleotide phosphonate. We reviewed the pharmacokinetic characteristics of LB80380 and discussed its role in the treatment of chronic hepatitis B infection. Areas covered: LB80380 is a prodrug of LB80331 and LB8031. It is rapidly absorbed when taken orally. Escalating doses of besifovir produce linear increase of the plasma concentration. Doses above 60mg are effective for inhibiting HBV in human. Using 60mg as an example, the maximal concentration of LB80331 in plasma is 397 ng/mL...
December 13, 2017: Expert Opinion on Drug Metabolism & Toxicology
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