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https://www.readbyqxmd.com/read/29211350/the-angiotensin-ii-receptors-type-1-blockage-affects-the-urinary-bladder-activity-in-hyperosmolar-induced-detrusor-overactivity-in-rats-preliminary-results
#1
Kajetan Juszczak, Piotr Maciukiewicz
BACKGROUND: Angiotensin II receptors play a role in the pathogenesis of urinary bladder dysfunction, especially in the case of bladder outlet obstruction. The function of these receptors in the detrusor overactivity (DO) still remains unclear. OBJECTIVES: The study aims to investigate some of the mechanisms through which hyperosmolarity induces urinary bladder overactivity. The effect of angiotensin II receptor type 1 - AT1 (telmisartan) on urinary bladder function in physiological state and in hyperosmolar-induced DO in rat model was explored...
October 2017: Advances in Clinical and Experimental Medicine: Official Organ Wroclaw Medical University
https://www.readbyqxmd.com/read/29187367/oxidative-stress-increases-megalin-expression-in-the-renal-proximal-tubules-during-the-normoalbuminuric-stage-of-diabetes-mellitus
#2
Yoshifumi Kurosaki, Akemi Imoto, Fumitaka Kawakami, Masanori Yokoba, Tsuneo Takenaka, Takafumi Ichikawa, Masato Katagiri, Naohito Ishii
Megalin, an endocytic receptor expressed in proximal tubule cells, plays a critical role in renal tubular protein reabsorption and is associated with in the albuminuria observed in diabetic nephropathy. We have previously reported increased oxidant production in the renal cortex during the normoalbuminuric stage of diabetes mellitus (DM); however, the relationship between oxidative stress and renal megalin expression during the normoalbuminuric stage of DM remains unclear. In the present study, we evaluated whether oxidative stress affects megalin expression in the normoalbuminuric stage of DM in a streptozotocin-induced diabetic rat model and in immortalized human proximal tubular cells (HK-2)...
November 29, 2017: American Journal of Physiology. Renal Physiology
https://www.readbyqxmd.com/read/29163738/a-case-of-moderate-sprue-like-enteropathy-associated-with-telmisartan
#3
Aurelio Negro, Loredana De Marco, Valentina Cesario, Rosaria Santi, Maria Chiara Boni, Magda Zanelli
Sprue-like enteropathy associated with olmesartan medoxomil use has been recently reported. Its clinical manifestations include diarrhea, weight loss and malabsorption. Duodenal biopsies show villous atrophy (VA) with or without intraepithelial lymphocytosis and inflammation of the lamina propria. Serology for celiac disease (CD) is negative and gluten-free diet does not result in clinical improvement. Symptoms resolve after olmesartan discontinuation. Follow-up biopsies show recovery/improvement of the duodenum...
December 2017: Journal of Clinical Medicine Research
https://www.readbyqxmd.com/read/29159410/use-of-health-care-databases-to-support-supplemental-indications-of-approved-medications
#4
Michael Fralick, Aaron S Kesselheim, Jerry Avorn, Sebastian Schneeweiss
Importance: Manufacturers of US Food and Drug Administration-approved prescription drugs often apply for additional indications based on randomized clinical trials. Real-world database analyses on a medication's use and outcomes in routine settings of care might help to inform decision making regarding such supplemental indications. Objective: To examine whether longitudinal data from a health care database can support the results of a randomized clinical trial that led to a supplemental indication for telmisartan...
November 20, 2017: JAMA Internal Medicine
https://www.readbyqxmd.com/read/29159401/comparison-of-observational-data-and-the-ontarget-results-for-telmisartan-treatment-of-hypertension-bull-s-eye-or-painting-the-target-around-the-arrow
#5
Robert M Califf
No abstract text is available yet for this article.
November 20, 2017: JAMA Internal Medicine
https://www.readbyqxmd.com/read/29107617/assessment-of-preclinical-pharmacokinetics-and-acute-toxicity-of-pioglitazone-and-telmisartan-combination
#6
Pinaki Sengupta, Bappaditya Chatterjee, Tapan Kumar Pal
The prevalence of hypertension is very common amongst the diabetic patients and is reported as the major cause of mortality in diabetes. Pioglitazone reported to have an ability to alter the blood cholesterol level and cardioprotective efficiency along with its antidiabetic activity. Telmisartan, through activation of PPAR-γ receptor exerts insulin sensitizing property in addition to its primary cardioprotective efficiency. Theoretically, a combination of pioglitazone and telmisartan may be beneficial to effectively control the high blood glucose level and management of coexisting cardiovascular complication in diabetes...
October 28, 2017: Regulatory Toxicology and Pharmacology: RTP
https://www.readbyqxmd.com/read/29105958/additivity-of-nebivolol-valsartan-single-pill-combinations-versus-other-single-pill-combinations-for-hypertension
#7
Jack Ishak, Michael Rael, Henry Punzi, Alan Gradman, Lynn M Anderson, Mehul Patel, Sanjida Ali, William Ferguson, Joel Neutel
The single-pill combination (SPC) comprising nebivolol (5 mg), a vasodilatory β1 -selective antagonist/β3 -agonist, and valsartan (80 mg), a renin-angiotensin-aldosterone system inhibitor, is the only Food and Drug Administration-approved β-blocker/renin-angiotensin-aldosterone system inhibitor SPC for hypertension. Additive effects of four nebivolol/valsartan SPC doses (5 mg/80 mg, 5/160 mg, 10/160 mg, 10/320 mg nebivolol/valsartan) were compared with five Food and Drug Administration-approved non-β-blocker/renin-angiotensin-aldosterone system inhibitor SPCs (aliskiren/hydrochlorothiazide, aliskiren/amlodipine, valsartan/amlodipine, aliskiren/valsartan, and telmisartan/amlodipine)...
November 5, 2017: Journal of Clinical Hypertension
https://www.readbyqxmd.com/read/29081650/edaravone-inhibits-pressure-overload-induced-cardiac-fibrosis-and-dysfunction-by-reducing-expression-of-angiotensin-ii-at1-receptor
#8
Wei-Wei Zhang, Feng Bai, Jin Wang, Rong-Hua Zheng, Li-Wang Yang, Erskine A James, Zhi-Qing Zhao
Angiotensin II (Ang II) is known to be involved in the progression of ventricular dysfunction and heart failure by eliciting cardiac fibrosis. The purpose of this study was to demonstrate whether treatment with an antioxidant compound, edaravone, reduces cardiac fibrosis and improves ventricular function by inhibiting Ang II AT1 receptor. The study was conducted in a rat model of transverse aortic constriction (TAC). In control, rats were subjected to 8 weeks of TAC. In treated rats, edaravone (10 mg/kg/day) or Ang II AT1 receptor blocker, telmisartan (10 mg/kg/day) was administered by intraperitoneal injection or gastric gavage, respectively, during TAC...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29081617/efficacy-and-tolerability-of-olmesartan-telmisartan-and-losartan-in-patients-of-stage-i-hypertension-a-randomized-open-label-study
#9
Mrunalini Kalikar, Kundan S Nivangune, Ganesh N Dakhale, Chaitali S Bajait, Smita D Sontakke, Vijay M Motghare, Ritu Budania
OBJECTIVES: To compare the efficacy and tolerability of losartan, telmisartan, and olmesartan as antihypertensive agents and evaluate and compare their effects on lipid profile and blood glucose. MATERIALS AND METHODS: This was a randomized, open-label, parallel-group, comparative study conducted in sixty patients of Stage I hypertension. The eligible patients were randomly allocated into three treatment groups: (1) Tablet olmesartan (20 mg), (2) Tablet telmisartan (40 mg), and (3) Tablet losartan (50 mg)...
July 2017: Journal of Pharmacology & Pharmacotherapeutics
https://www.readbyqxmd.com/read/29075786/angiotensin-receptor-blocker-telmisartan-inhibits-cell-proliferation-and-tumor-growth-of-cholangiocarcinoma-through-cell-cycle-arrest
#10
Eri Samukawa, Shintaro Fujihara, Kyoko Oura, Hisakazu Iwama, Yoshimi Yamana, Tomoko Tadokoro, Taiga Chiyo, Kiyoyuki Kobayashi, Asahiro Morishita, Mai Nakahara, Hideki Kobara, Hirohito Mori, Keiichi Okano, Yasuyuki Suzuki, Takashi Himoto, Tsutomu Masaki
Cholangiocarcinoma (CCA) is at an advanced stage at the time of its diagnosis, and developing a more effective treatment of CCA would be desirable. Angiotensin II type 1 (AT1) receptor blocker (ARB), telmisartan may inhibit cancer cell proliferation, but the mechanisms by which telmisartan affects various cancers remain unknown. In this study, we evaluated the effects of telmisartan on human CCA cells and to assess the expression of microRNAs (miRNAs). We studied the effects of telmisartan on CCA cells using two cell lines, HuCCT-1 and TFK-1...
December 2017: International Journal of Oncology
https://www.readbyqxmd.com/read/29070884/telmisartan-activates-ppar%C3%AE-to-improve-symptoms-of-unpredictable-chronic-mild-stress-induced-depression-in-mice
#11
Yingxiao Li, Kai-Chun Cheng, Keng-Fan Liu, Wen-Huang Peng, Juei-Tang Cheng, Ho-Shan Niu
Major depression is a common mental disorder that has been established to be associated with a decrease in serotonin and/or serotonin transporters in the brain. Peroxisome proliferator-activated receptor δ (PPARδ) has been introduced as a potential target for depression treatment. Telmisartan was recently shown to activate PPARδ expression; therefore, the effectiveness of telmisartan in treating depression was investigated. In unpredictable chronic mild stress (UCMS) model, treatment with telmisartan for five weeks notably decrease in the time spent in the central and the reduced frequency of grooming and rearing in open filed test (OFT) and the decreased sucrose consumption in sucrose preference test (SPT) compared with the paradigms...
October 25, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29048654/telmisartan-inhibits-hepatocellular-carcinoma-cell-proliferation-in-vitro-by-inducing-cell-cycle-arrest
#12
Kyoko Oura, Tomoko Tadokoro, Shintaro Fujihara, Asahiro Morishita, Taiga Chiyo, Eri Samukawa, Yoshimi Yamana, Koji Fujita, Teppei Sakamoto, Takako Nomura, Hirohito Yoneyama, Hideki Kobara, Hirohito Mori, Hisakazu Iwama, Keiichi Okano, Yasuyuki Suzuki, Tsutomu Masaki
Hepatocellular carcinoma (HCC) is the most common primary malignancy of the liver and the third leading cause of cancer-related death. Telmisartan, a widely used antihypertensive drug, is an angiotensin II type 1 (AT1) receptor blocker (ARB) that might inhibit cancer cell proliferation, but the mechanisms through which telmisartan affects various cancers remain unknown. The aim of the present study was to evaluate the effects of telmisartan on human HCC and to assess the expression of microRNAs (miRNAs). We studied the effects of telmisartan on HCC cells using the HLF, HLE, HepG2, HuH-7 and PLC/PRF/5 cell lines...
September 20, 2017: Oncology Reports
https://www.readbyqxmd.com/read/29031980/quality-by-design-qbd-approach-to-optimize-the-formulation-of-a-bilayer-combination-tablet-telmiduo-%C3%A2-manufactured-via-high-shear-wet-granulation
#13
Ah Ram Lee, Seok Young Kwon, Du Hyung Choi, Eun Seok Park
A bilayer tablet, which consisted of telmisartan and amlodipine besylate, was formulated based on a Quality by Design (QbD) approach. The control and response factors were determined based on primary knowledge and the target values of the control tablet (Twynsta(®)). A D-optimal mixture design was used to obtain the optimal formulations in terms of D-mannitol, crospovidone, and MCC for the telmisartan layer, and CCM-Na, PVP K25, and Prosolv for the amlodipine layer. The quantitative effects of the different formulation factors on the response factors were accurately predicted using the equations of best fit and a strong linearity was observed between the predicted and actual values of the response factors...
October 12, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28979698/stachydrine-ameliorates-pressure-overload-induced-diastolic-heart-failure-by-suppressing-myocardial-fibrosis
#14
Hui-Hua Chen, Pei Zhao, Wen-Xia Zhao, Jing Tian, Wei Guo, Ming Xu, Chen Zhang, Rong Lu
Stachydrine (Sta), a major constituent of Leonurus japonicus Houtt, has been reported to possess numerous cardioprotective effects. In this study, we evaluated the effect of Sta on pressure overload-induced diastolic heart failure in rats and investigated the mechanisms underlying the effect. Wistar rats were randomized to transverse aortic constriction (TAC) or sham operation. After 3 days, the rats that underwent TAC were randomized to treatment for a total of four experimental groups (n=10 each group): sham operation, TAC only, TAC + telmisartan (Tel), and TAC + stachydrine (Sta)...
2017: American Journal of Translational Research
https://www.readbyqxmd.com/read/28974567/relative-and-combined-prognostic-importance-of-on-treatment-mean-and-visit-to-visit-blood-pressure-variability-in-ontarget-and-transcend-patients
#15
RANDOMIZED CONTROLLED TRIAL
Giuseppe Mancia, Helmut Schumacher, Michael Böhm, Josep Redon, Roland E Schmieder, Paolo Verdecchia, Peter Sleight, Koon Teo, Salim Yusuf
In 28 790 patients recruited for the ONTARGET (Ongoing Treatment Alone and in Combination With Ramipril Global End Point Trials) and TRANSCEND (Telmisartan Randomized Assessment Study in ACE Intolerant Subjects With Cardiovascular Disease) trials, we investigated the prognostic value for cardiovascular events (primary outcome) of (1)on-treatment visit-to-visit systolic blood pressure (SBP) variability versus mean SBP and (2) the 2 measures together. SBP variability was measured by the coefficient of variation (CV) of mean SBP to which it was unrelated...
November 2017: Hypertension
https://www.readbyqxmd.com/read/28962213/effects-of-telmisartan-on-improving-leptin-resistance-and-inhibiting-hepatic-fibrosis-in-rats-with-non-alcoholic-fatty-liver-disease
#16
Qiu-Zan Zhang, Ying-Li Liu, Yan-Rong Wang, Li-Na Fu, Jing Zhang, Xiu-Ru Wang, Bang-Mao Wang
The present study aimed to investigate the impacts of telmisartan (TEL) on hepatic fibrosis, serum leptin, leptin protein in liver tissue and its mRNA expression level in rats with non-alcoholic fatty liver disease (NAFLD). Male Sprague Dawley rats were randomly divided into the control (N), model (M), polyene phosphatidylcholine (P) and TEL (T) groups. Group M and the intervention groups were given a high-fat diet for 12 weeks to induce NAFLD, followed by 4 weeks of intragastric administration of normal saline (1...
September 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28955302/temporal-changes-in-cortical-and-hippocampal-expression-of-genes-important-for-brain-glucose-metabolism-following-controlled-cortical-impact-injury-in-mice
#17
June Zhou, Mark P Burns, Linda Huynh, Sonia Villapol, Daniel D Taub, Juan M Saavedra, Marc R Blackman
Traumatic brain injury (TBI) causes transient increases and subsequent decreases in brain glucose utilization. The underlying molecular pathways are orchestrated processes and poorly understood. In the current study, we determined temporal changes in cortical and hippocampal expression of genes important for brain glucose/lactate metabolism and the effect of a known neuroprotective drug telmisartan on the expression of these genes after experimental TBI. Adult male C57BL/6J mice (n = 6/group) underwent sham or unilateral controlled cortical impact (CCI) injury...
2017: Frontiers in Endocrinology
https://www.readbyqxmd.com/read/28933256/combined-effect-of-telmisartan-and-fluvastatin-on-arachidonic-acid-metabolism-in-human-liver-microsomes
#18
Yuka Kato, Yuji Mukai, Anders Rane, Nobuo Inotsume, Takaki Toda
Epoxyeicosatrienoic acids (EETs), metabolites of arachidonic acid (AA) via cytochrome P450s, have a protective effect on the cardiovascular system involving vasodilation. We have previously demonstrated that telmisartan (TEL) inhibits EETs production from AA in vitro. The objectives of the study were to examine the inhibitory effect of fluvastatin (FLU), an inhibitor of CYP2C9, and the combined effect of TEL and FLU on the production of EETs using human liver microsomes. The combined effect of TEL and FLU was evaluated using two methods, the fixed concentration method and the fixed ratio method...
September 21, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/28904053/cardiovascular-biomarkers-in-hypertensive-patients-with-medical-treatment-results-from-the-randomized-teamsta-protect-i-trial
#19
Annika Jagodzinski, Johannes Tobias Neumann, Francisco Ojeda, Nils Arne Sörensen, Philipp Wild, Thomas Münzel, Tanja Zeller, Dirk Westermann, Stefan Blankenberg
BACKGROUND: High blood pressure (BP) is associated with an increased rate of cardiovascular events and mortality. Cardiovascular biomarkers are able to predict long-term risk in the general population, particularly in diseased cohorts. We undertook an investigation of the effect of 2 different antihypertensive treatments on cardiovascular biomarkers in a randomized trial. METHODS: The TEAMSTA study included 481 hypertensive patients. They were randomized to either 80-mg telmisartan + 5-mg amlodipine (TA) or 40-mg olmesartan + 12...
September 13, 2017: Clinical Chemistry
https://www.readbyqxmd.com/read/28868047/in-premature-newborns-intraventricular-hemorrhage-causes-cerebral-vasospasm-and-associated-neurodisability-via-heme-induced-inflammasome-mediated-interleukin-1-production-and-nitric-oxide-depletion
#20
Michael Eisenhut, Samyami Choudhury
BACKGROUND: Intraventricular hemorrhage (IVH) occurs in 60-70% of neonates weighing 500-750 g and 10-20% of those weighing 1,000-1,500 g. All forms of IVH have been associated with neurocognitive deficits. Both subarachnoid and IVHs have been associated with delayed vasospasm leading to neurological deficits. Pathways linking hemoglobin release from blood clots to vasospasm include heme-induced activation of inflammasomes releasing interleukin-1 (IL-1) that can cause calcium dependent and independent vasospasm...
2017: Frontiers in Neurology
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