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The aim of this study was to examine whether Xuesaitong, a multiherbal formulation for coronary heart disease, alters the pharmacokinetics of losartan. Adult male Sprague Dawley rats randomly received losartan (10 mg/kg) or losartan plus Xuesaitong (10 mg/kg) through an oral gavage ( = 6). Multiple blood samples were obtained for up to 36 h to determine the concentrations of losartan and its active metabolite, EXP3174, through ultraperformance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS). Pharmacokinetics were estimated using a noncompartmental model. The half-life ( ) of losartan was decreased by Xuesaitong (4.26 ± 1.51 vs. 6.35 ± 2.10 h; < 0.05). The apparent volume of distribution ( ) of losartan was also decreased by the combination of losartan and Xuesaitong (4.41 ± 1.61 vs. 7.20 ± 2.41 mL; < 0.05). The time to maximum concentration ( ) of losartan was increased by Xuesaitong (1.06 ± 1.04 vs. 0.13 ± 0.05 h; < 0.05). Xuesaitong also decreased the of EXP3174 (8.22 ± 1.41 vs. 6.29 ± 1.38 h; < 0.05). These results suggest that there is a complex interaction between losartan and Xuesaitong. In addition to enhanced elimination of losartan and EXP3174, Xuesaitong may also decrease the absorption rate and of losartan.
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http://dx.doi.org/10.1155/2019/8373476 | DOI Listing |
ACS Omega
December 2024
Beijing National Laboratory for Molecular Sciences, Molecular Reaction Dynamics Laboratory, CAS Research/Education Center for Excellence in Molecular Sciences, Institute of Chemistry, Chinese Academy of Sciences, Beijing 100190, P. R. China.
Structurally knowing the active sites of a drug is important for understanding its therapeutic functions. S086 is a novel angiotensin receptor-neprilysin inhibitor that consists of the molecular moieties of EXP3174 (the active metabolite of the angiotensin receptor blocker losartan) and sacubitril (a neprilysin inhibitor prodrug) in a 1:1 molar ratio. There are two forms of cocrystals of S086, namely, ξ-crystal and α-crystal, which were formed both via intermolecular coordination bonding to calcium ions, with the aid of internal water.
View Article and Find Full Text PDFPLoS One
December 2024
Department of Nephrology, The First Hospital, Shanxi Medical University, Taiyuan, Shanxi, China.
Renal tubular epithelial cell injury is an important manifestation of chronic kidney disease (CKD). This study aims to explore the mechanism of astragaloside IV (AS-IV) in the treatment of UII-mediated renal tubular epithelial cell injury by integrating network pharmacology and experimental validation. BATMAN, SwissTarget-Prediction and ETCM data bases were used to screen the target proteins of AS-IV.
View Article and Find Full Text PDFNaunyn Schmiedebergs Arch Pharmacol
December 2024
Department of Human Biology to the Physiology, School of Medicine, International Medical University, 57000, Kuala Lumpur, Malaysia.
Rheumatoid arthritis (RA) can cause blood pressure (BP) elevation in estrogen-deficient, post-menopausal women; however, the underlying mechanisms are not well understood. In this study, the aortic involvement and its underlying mechanisms that contribute to the BP elevation in estrogen-deficient, RA condition were identified. Ovariectomy was performed to create a state of estrogen deficiency and RA was then induced in ovariectomized rats by using incomplete Freund's adjuvant and immune-mediated collagen type-II.
View Article and Find Full Text PDFJACC Case Rep
December 2024
Indiana University School of Medicine, Indianapolis, Indiana, USA.
An 85-year-old man with recently diagnosed metastatic EGFR+ lung adenocarcinoma treated with osimertinib presented after 1 month of therapy in decompensated congestive heart failure along with atrial fibrillation, prolonged QTc and acute kidney injury. Osimertinib was held. His hemodynamic status was optimized, and he was started on cardioprotective medications (losartan and metoprolol succinate), and LVEF recovered.
View Article and Find Full Text PDFJ Biomol Struct Dyn
December 2024
Department of Pharmacy Practice, Manipal College of Pharmaceutical Sciences, Manipal, Karnataka, India.
Drug repurposing is preferred over de-novo drug discovery to unveil the therapeutic applications of existing drug candidates before investing considerable resources in unexplored novel chemical entities. This study demonstrated multifaceted stratagems to reconnoiter promising repurposable candidates against Hepatocellular Carcinoma (HCC) by amalgamating Real-World-Data (RWD) with bioinformatics algorithms corroborated with and studies. At the outset, the RWD from the Food and Drug Administration Adverse Event Reporting System (FAERS) was explored to navigate signals to retrieve repurposable drugs that are inversely associated with HCC via Disproportionality Analysis.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!