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Takanobu Takezako, Hamiyet Unal, Sadashiva S Karnik, Koichi Node
BACKGROUND AND PURPOSE: Diseases such as hypertension and renal-allograft rejection are accompanied by chronic agonist-independent signaling by the angiotensin II (Ang II) type 1 receptor (AT1R). The current treatment paradigm for these diseases embraces the preferred use of inverse agonist AT1R blockers (ARBs). However, variability in the inverse agonist activities of common biphenyl-tetrazole ARBs for the active state of AT1R often leads to treatment failure. Therefore, characterization of robust inverse agonist ARBs for the active state of AT1R is necessary...
March 23, 2018: British Journal of Pharmacology
Abdul Ahad, Abdulmohsen A Al-Saleh, Abdullah M Al-Mohizea, Fahad I Al-Jenoobi, Mohammad Raish, Alaa Eldeen B Yassin, Mohd Aftab Alam
The objective of the present work was to formulate, optimize and evaluate the potential of novel soft nanovesicles i.e. nano-transfersomes, containing eprosartan mesylate (EM) for transdermal delivery. Nano-transfersomes of EM were developed using Phospholipon 90G, Span 80 (SP) and sodium deoxycholate (SDC) and characterized for vesicle size, shape, entrapment efficiency, in vitro skin permeation study and confocal laser scanning microscopy. The optimized nano-transfersomes formulation showed vesicles size of 108...
November 2017: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
Abdul Ahad, Mohammad Raish, Ajaz Ahmad, Fahad I Al-Jenoobi, Abdullah M Al-Mohizea
The objective of the present study was to formulate eprosartan mesylate loaded nano-bilosomes and investigates its potential for controlling streptozotocin induced diabetes nephropathy in Wistar rats. The eprosartan mesylate loaded nano-bilosomes comprising of various ratios of soybean phosphatidylcholine/sodium deoxycholate were prepared by thin film hydration technique. The prepared formulations were evaluated for vesicles size, polydispersity index, zeta potential and entrapment efficiency. Further the optimized formulation was characterized for vesicles morphology, and its efficacy for the management of diabetic nephropathy in Wistar rats...
October 10, 2017: European Journal of Pharmaceutical Sciences
Harshal Surendra Mandavdhare, Vishal Sharma, Kaushal K Prasad, Amit Kumar, Manish Rathi, Surinder S Rana
Recent studies have identified sprue-like illness associated with the use of the antihypertensive agent olmesartan medoxomil. However, whether this condition is specific to the use of olmesartan or is associated with the use of drugs belonging to the class of "sartans" remains to be clarified. A 45-year-old woman with chronic kidney disease along with hypothyroidism and hypertension presented with chronic diarrhea and significant weight loss. Endoscopy of the upper gastrointestinal tract showed scalloping and grooving of the duodenum, and histopathological examination showed subtotal villous atrophy...
July 2017: Intestinal Research
Yunseo Woo, Yu-Jin Jung
Angiotensin II receptor blockers (ARBs) are anti-hypertensive drugs that competitively inhibit the binding of angiotensin II to its receptor, resulting in blood vessel dilation and the reduction of blood pressure. These antagonists are also known as sartans, and are a group of pharmaceuticals that possess tetrazole or imidazole groups. In the present study, the anticancer and antimetastatic effects of the ARBs fimasartan, losartan, eprosartan and valsartan on the human prostate cancer PC-3, DU-145 and LNCap-LN3 cell lines were investigated in vitro...
May 2017: Oncology Letters
Abdul Ahad, Abdulmohsen A Al-Saleh, Abdullah M Al-Mohizea, Fahad I Al-Jenoobi, Mohammad Raish, Alaa Eldeen B Yassin, Mohd Aftab Alam
The objective of the current study was to formulate the eprosartan mesylate loaded transfersomes using different proportions of Phospholipon(®) 90 G and Tween(®) 80 (95-75:5-25% w/w). The prepared transfersomes were characterized for their vesicles size, shape, polydispersity index, zeta potential, entrapment efficiency, in vitro skin permeation, confocal laser scanning microscopy, and in vivo skin irritation. Results revealed that the formulated transfersomes were negatively charged, spherical unilamellar structure of 71...
May 26, 2017: Pharmaceutical Development and Technology
O D Ostroumova, E I Pervichko, Y P Zinchenko
GOAL: The study of emotional and personality characteristics of patients with hypertension in the workplace (HW) and comparative assessment of the effectiveness of antihypertensive therapy in these patients. MATERIAL AND METHODS: The study included 170 patients c hypertensive disease stage II, 1-2-th degree, aged 32-52 years, including 85 patients with and 85 patients without WAH, and 82 healthy subjects matched for age and sex. To carry out simulation of the situation of emotional intensity (level of claims assessment process - UE) and a modified version of the test Rosenzweig...
September 2016: Kardiologiia
Abdul Ahad, Abdulmohsen A Al-Saleh, Abdullah M Al-Mohizea, Fahad I Al-Jenoobi, Mohammad Raish, Alaa Eldeen B Yassin, Mohd Aftab Alam
The objective of present study was to prepare eprosartan mesylate (EM)-loaded transfersomes Carbopol(®) gel and characterized for various parameters, including in vitro skin permeation, in vivo antihypertensive study, skin irritation, and histological study. Furthermore, effect of transfersomes gel on angiotensin II type-1 receptor (AT1R) mRNA and protein expressions on smooth vascular muscles of aorta was determined by real-time polymerase chain reaction (RT-PCR) and western blot analysis. The physical evaluation parameters were detected to be in correspondence with reference marketed gel formulation...
May 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
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...
July 2017: 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
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