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Maximilian Wiesmann, Monica Roelofs, Robert van der Lugt, Arend Heerschap, Amanda J Kiliaan, Jurgen Ahr Claassen
Elevated angiotensin II causes hypertension and contributes to Alzheimer's disease by affecting cerebral blood flow. Angiotensin II receptor blockers may provide candidates to reduce (vascular) risk factors for Alzheimer's disease. We studied effects of two months of angiotensin II-induced hypertension on systolic blood pressure, and treatment with the angiotensin II receptor blockers, eprosartan mesylate, after one month of induced hypertension in wild-type C57bl/6j and AβPPswe/PS1ΔE9 (AβPP/PS1/Alzheimer's disease) mice...
September 5, 2016: Journal of Cerebral Blood Flow and Metabolism
Pankaj Dangre, Ritu Gilhotra, Shashikant Dhole
The present investigation is aimed to design a statistically optimized self-microemulsifying drug delivery system (SMEDDS) of eprosartan mesylate (EM). Preliminary screening was carried out to find a suitable combination of various excipients for the formulation. A 3(2) full factorial design was employed to determine the effect of various independent variables on dependent (response) variables. The independent variables studied in the present work were concentration of oil (X 1) and the ratio of S mix (X 2), whereas the dependent variables were emulsification time (s), globule size (nm), polydispersity index (pdi), and zeta potential (mV), and the multiple linear regression analysis (MLRA) was employed to understand the influence of independent variables on dependent variables...
October 2016: Drug Delivery and Translational Research
Ruirui Yang, Zhiqiang Luo, Yang Liu, Mohan Sun, Ling Zheng, Yingying Chen, Yanping Li, Hao Wang, Lingzhu Chen, Ming Wu, Huihui Zhao
BACKGROUND: Angiotensin receptor blockers (ARBs) are the most recent class of agents for the treatment of hypertension. However, ARBs may cause a low incidence of headache, upper respiratory infection, back pain, muscle cramps, fatigue, dizziness, and many other side effects. In some cases, such toxicity is associated with pharmacokinetic alterations. METHODS: The cytochrome P450 (CYP) enzyme system plays an important role in a lot of clinically important pharmacokinetic drug interactions...
2016: Current Drug Metabolism
Daan J L van Twist, Alfons J H M Houben, Peter W de Leeuw, Abraham A Kroon
BACKGROUND: Angiotensin II (Ang II) is thought to play an important role in the development of hypertension. Nevertheless, knowledge on the angiotensin II type-1-receptors (AT1Rs) in the hypertensive kidney and the influence of sodium intake and renin-angiotensin system activity on intrarenal AT1R blockade is scarce. To improve our understanding of renal AT1Rs in hypertensive patients, we studied the effects of acute, local administration of AT1R-blocker eprosartan in kidneys of patients with essential hypertension (off medication)...
August 2016: Journal of Hypertension
Young-Mi Ah, Ju-Yeun Lee, Yun-Jung Choi, Jisun Kong, Baegeum Kim, Kyung Hee Choi, Nayoung Han, Yun Mi Yu, Jung Mi Oh, Wan Gyoon Shin, Hae-Young Lee
We identified 55 504 uncomplicated, treatment-naïve hypertensive patients who started angiotensin II receptor blockers (ARBs) in 2012 from national claims data. The proportion of patients remaining on any hypertension treatment at 12 months and the adherence rate were similar between the losartan cohort (66.82% and 68.25%) and the nonlosartan ARB cohort (67.48% and 69.01%). After adjusting for confounding factors, there was no difference in persistence (aHR 0.98, 95% confidence interval (CI) 0.95-1.01) on hypertension treatment between losartan and nonlosartan ARB cohort...
2016: Clinical and Experimental Hypertension: CHE
Jelena Golubović, Ana Protić, Biljana Otašević, Mira Zečević
QSRR are mathematically derived relationships between the chromatographic parameters determined for a representative series of analytes in given separation systems and the molecular descriptors accounting for the structural differences among the investigated analytes. Artificial neural network is a technique of data analysis, which sets out to emulate the human brain's way of working. The aim of the present work was to optimize separation of six angiotensin receptor antagonists, so-called sartans: losartan, valsartan, irbesartan, telmisartan, candesartan cilexetil and eprosartan in a gradient-elution HPLC method...
April 1, 2016: Talanta
Luis Castilla-Guerra, Maria Del Carmen Fernandez-Moreno
Hypertension is the most important potentially reversible risk factor for stroke in all age groups; high blood pressure (BP) is also associated with increased risk of recurrent stroke in patients who have already had an ischemic or hemorrhagic event. Twenty-four hour ambulatory BP monitoring (ABPM) has become an important tool for improving the diagnosis and management of hypertension, and is increasingly used to assess patients with hypertension. Nevertheless, although ABPM devices are increasingly used for assessment of hypertension, their value in the chronic management of hypertension in patients with stroke has not been systematically studied...
January 2016: Journal of Stroke
Leo Akioyamen, Mitchell Levine, Diana Sherifali, Daria O'Reilly, Claudia Frankfurter, Eleanor Pullenayegum, Ron Goeree, Bernice Tsoi
Angiotensin receptor blockers (ARBs) are widely used in managing essential hypertension, with considerable evidence available on their short-term efficacy in lowering blood pressure (BP). However, there currently exists limited "pooled" data examining the long-term efficacy of ARB treatment in controlling BP or mitigating cardiovascular and cerebrovascular events. The purpose of this study was to conduct a systematic review and meta-analysis assessing the long-term effects of ARBs as a class on BP control, myocardial infarction, hospitalization for heart failure, cerebrovascular events (ie, stroke), cardiovascular mortality, and all-cause mortality...
January 2016: Journal of the American Society of Hypertension: JASH
Maximilian Wiesmann, Carmen Capone, Valerio Zerbi, Laura Mellendijk, Arend Heerschap, Jurgen A H R Claassen, Amanda J Kiliaan
AIMS: Hypertension, a risk factor for Alzheimer's disease (AD), is a treatable condition, which offers possibilities for prevention of AD. Elevated angiotensin II (AngII) is an important cause of essential hypertension. AngII has deleterious effects on endothelial function and cerebral blood flow (CBF), which may contribute to AD. AngII blocking agents can thus provide potential candidates to reduce AD risk factors in hypertensive patients. METHODS: We studied the effect of 2 months induced hypertension (AngII-infusion via osmotic micropumps) on systolic blood pressure (SBP) and CBF in 10 months-old wild-type (WT) C57bl/6j and AβPPswe/PS1ΔE9 (AβPP/PS1) mice, and treatment with two different antihypertensives, 1) eprosartan mesylate (EM, 0...
2015: Current Alzheimer Research
Cheng Wang, Min Li, Tie Yang, Xuefang Ding, Xiuli Bao, Yang Ding, Hui Xiong, Ying Wu, Wei Wang, Jianping Zhou
A new cationic polymer eprosartan-graft-PEI (ESP) containing eprosartan (ES) and polyethylenimine 1.8K was successfully developed and employed as a safe gene vector to assemble a drug (ES) and gene co-delivery complex (ESP/pDNA). Chondroitin sulfate (CS) was then used as a coating polymer to shield the surface charge of ESP/pDNA complexes, as well as a tumor targeting entity to ensure specific delivery of CS/ESP/pDNA complexes. The CS/ESP/pDNA complexes with desirable particle size and zeta potential, exhibited amidase-responsive drug release and CS-mediated endocytosis in vitro...
November 1, 2015: Materials Science & Engineering. C, Materials for Biological Applications
Thomas Letzel, Anne Bayer, Wolfgang Schulz, Alexandra Heermann, Thomas Lucke, Giorgia Greco, Sylvia Grosse, Walter Schüssler, Manfred Sengl, Marion Letzel
A large number of anthropogenic trace contaminants such as pharmaceuticals, their human metabolites and further transformation products (TPs) enter wastewater treatment plants on a daily basis. A mixture of known, expected, and unknown molecules are discharged into the receiving aquatic environment because only partial elimination occurs for many of these chemicals during physical, biological and chemical treatment processes. In this study, an array of LC-MS methods from three collaborating laboratories was applied to detect and identify anthropogenic trace contaminants and their TPs in different waters...
October 2015: Chemosphere
A A Elgarov, R M Aramisova, M A Elgarov, M A Kalmykova
AIM: To estimate effectiveness and safety of pharmacotherapy in vehicle drivers with arterial hypertension (AH). MATERIALS AND METHODS: 432 patients with grade I-III AH including 82 with cardiovascular complications largely of II and III grade were under observation during 2.5-4 months using clinical and instrumental methods (24hr AP & ECG monitoring) as well as psychophysiological testing (PPT). RESULTS: Ramipril and atenolol were efficient in 77...
2015: Klinicheskaia Meditsina
Robert Gurke, Martin Rößler, Conrad Marx, Sam Diamond, Sara Schubert, Reinhard Oertel, Joachim Fauler
The present study determines removal rates (RR) of 56 pharmaceuticals and metabolites, respectively, in an urban sewage treatment plant using mass flow analysis by comparing influent and effluent loads over a consecutive ten-day monitoring period. Besides well investigated compounds like carbamazepine and metoprolol, less researched targets, such as topiramate, pregabalin, telmisartan, and human metabolites of pharmaceuticals were included. Another aim was to determine the ratio of pharmaceuticals and corresponding metabolites in raw wastewater...
November 1, 2015: Science of the Total Environment
M Wiesmann, V Zerbi, M Roelofs, R Van Der Lugt, A Heerschap, J A H R Claassen, A J Kiliaan
OBJECTIVE: Hypertension is a risk factor for Alzheimer's disease (AD). It is a treatable condition which opens important avenues for prevention of AD. Elevated angiotensin II (AngII) is an important cause of essential hypertension and has deleterious effects on endothelial function and cerebral blood flow (CBF). In this study we therefore investigated the interaction between AngII, systolic blood pressure (SBP), and MRI-measurements in the APPswe/PS1[Delta]E9 (APP/PS1) mouse model of AD...
June 2015: Journal of Hypertension
R L Dashdamirov
The aim of the study was to evaluate results of combined therapy of stable 2-3 FC angina of effort with metabolic syndrome including metformin. Group 1 was comprised of 71 patients (38 (53.3%) men and 33 (46.5%) women), group 2 consisted of 57 patients treated with isosorbid-5 mononitrate (40 mg/d + amlodipin (5 mg/d) + eprosartan (600 mg/d) + thrombo ASS (100 mg/d) + carvedilol (25 mg/d) + atorvastatin (20 mg/d). Effects of the treatment were assessed 3, 6, and 12 months after its onset. At the end of the study, fasting blood glucose, total cholesterol, triglyceride, and low density lipoproteide levels decreased by 12...
2014: Klinicheskaia Meditsina
Hans Maier, Karlheinz Hehemann, Michael Vieth
An 83-year-old woman with hypertension received the angiotensin-II receptor type 1 blocker (ARB) eprosartan for more than 10 years. Six months ago, the dosage of the drug was doubled, and the patient reported a sudden onset of diarrhea. Duodenal biopsies showed a celiac disease-like pathology with flattened mucosa and an increase of intraepithelial lymphocytes and eosinophils, but serology of celiac disease remained negative. Celiac disease-like changes have been previously reported to be associated with other ARBs...
2015: Ceskoslovenská Patologie
Robert J Petrella, Dawn P Gill, Jean-Pascal Berrou
OBJECTIVE: As part of the Physicians' Observational Work on Patient Education According to their Vascular Risk (POWER) survey, we used Framingham methodology to examine the effect of an eprosartan-based regimen on total coronary heart disease (CHD) risk in diabetic patients recruited in Canada. METHODS: Patients with new or uncontrolled hypertension (sitting systolic blood pressure [SBP] >140 mmHg with diastolic blood pressure <110 mmHg) were identified at 335 Canadian primary care practices...
2015: Diabetes, Metabolic Syndrome and Obesity: Targets and Therapy
P A van Zwieten
A survey is presented of the registered non-peptidergic angiotensin II receptor antagonists (AT1 blockers, ARBs, sartans) and their general properties and similarities. Accordingly, their receptor profile, pharmacokinetic and therapeutic applications are discussed. In addition, attention is paid to the individual characteristics of the AT1 blockers now available. A few components of this category offer additional potentially beneficial properties, owing to their pharmacological or metabolic characteristics...
November 2006: Netherlands Heart Journal
Mohamed A Morsy, Gehan H Heeba, Magda E Mahmoud
Diabetic nephropathy becomes the single most frequent cause of end-stage renal disease. The present study aimed therefore to investigate possible protective effect of eprosartan, an angiotensin II type 1 receptor blocker, on high-fat diet/streptozotocin-induced early diabetic nephropathy in rats and various mechanisms underlie this effect. Male Wistar rats with type 2 diabetes induced by high-fat diet/streptozotocin were treated with eprosartan at the dose levels of 30 and 60mg/kg daily for 5 weeks. Eprosartan induced a nephroprotective effect as evident by the significant decrease in serum creatinine, urea, total cholesterol, triglycerides and glucose levels, urinary albumin excretion and kidney index as well as renal levels of malondialdehyde and nitric oxide products (nitrite/nitrate), in addition to angiotensin II, inducible nitric oxide synthase, transforming growth factor-β1 and collagen IV expressions with a concurrent increase in renal levels of reduced glutathione and catalase activity compared to diabetic untreated rats...
March 5, 2015: European Journal of Pharmacology
Yan Meng, Chen Chen, Cui Tian, Jie Du, Hui-Hua Li
BACKGROUND/AIMS: Angiotensin II (Ang II) plays a critical role in regulating vascular inflammatory diseases, such as atherosclerosis and hypertension. Early growth response-1 (Egr-1) is an immediate early gene that acts as a master switch for the inflammatory response. However, the role of Ang II in regulating Egr-1 expression in macrophages, and the effect of peroxisome proliferators-activated receptor-γ (PPAR-γ) ligand 15d-PGJ2 in this process remain to be investigated. METHODS AND RESULTS: We showed that Ang II significantly up-regulated the expression of Egr-1 in RAW264...
2015: Cellular Physiology and Biochemistry
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