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https://www.readbyqxmd.com/read/28727906/potential-of-telmisartan-in-the-treatment-of-benign-prostatic-hyperplasia
#1
Ismail Ogunbayode Ishola, Charles C Anunobi, Kehinde Habeeb Tijani, Olasunmbo Afolayan, Victoria U Udokwu
Benign prostatic hyperplasia (BPH) is a common health problem in aging men. This study was carried out to investigate the protective effect of telmisartan on testosterone induced-BPH in rats. Fifty-four male Wistar rats (200 - 250g) were randomly divided into 9 groups (n =6) and orally treated for 28 consecutive days: group 1- vehicle normal, olive oil (10 ml/kg); group 2- BPH model control (10 ml/kg); groups 3-5 - telmisartan (5, 10 or 20 mg/kg, respectively); group 6- pioglitazone (20 mg/kg); group 7- celecoxib (20 mg/kg); group 8- combination of telmisartan (5 mg/kg) and pioglitazone (20 mg/kg); group 9- combination of telmisartan (5 mg/kg) and celecoxib (20 mg/kg)...
July 20, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28711865/enhanced-mitochondrial-transient-receptor-potential-channel-canonical-type-3-mediated-calcium-handling-in-the-vasculature-from-hypertensive-rats
#2
Bin Wang, Shiqiang Xiong, Shaoyang Lin, Weijie Xia, Qiang Li, Zhigang Zhao, Xing Wei, Zongshi Lu, Xiao Wei, Peng Gao, Daoyan Liu, Zhiming Zhu
BACKGROUND: Mitochondrial Ca(2+) homeostasis is fundamental to the regulation of mitochondrial reactive oxygen species (ROS) generation and adenosine triphosphate production. Recently, transient receptor potential channel, canonical type 3 (TRPC3), has been shown to localize to the mitochondria and to play a role in maintaining mitochondrial calcium homeostasis. Inhibition of TRPC3 attenuates vascular calcium influx in spontaneously hypertensive rats (SHRs). However, it remains elusive whether mitochondrial TRPC3 participates in hypertension by increasing mitochondrial calcium handling and ROS production...
July 15, 2017: Journal of the American Heart Association
https://www.readbyqxmd.com/read/28699721/comparison-of-pre-and-post-ischemic-treatment-of-telmisartan-and-nimodipine-combination-in-experimentally-induced-cerebral-ischemia
#3
(no author information available yet)
Time dependent intervention plays a crucial role in preventing neurodegeneration after ischemic insult. The intensity of excitotoxicity is greater in the secondary reperfusion phase (2-4 h) compared to the primary occlusion phase (2 h), which could be attributed to secondary elevation of excitatory amino acids (EAA) in cerebral ischemia. In the present study, we tried to assess the neuroprotective effects of telmisartan and nimodipine (TM-NM) combination on the secondary reperfusion phase. The drug treatments were made immediately after reperfusion and their effects were compared with pre-treatment...
September 2016: Indian Journal of Experimental Biology
https://www.readbyqxmd.com/read/28674251/co-administration-of-fluvastatin-and-cyp3a4-and-cyp2c8-inhibitors-may-increase-the-exposure-to-fluvastatin-in-carriers-of-cyp2c9-genetic-variants
#4
Yuji Mukai, Masayuki Narita, Erika Akiyama, Kanami Ohashi, Yasutaka Horiuchi, Yuka Kato, Takaki Toda, Anders Rane, Nobuo Inotsume
Fluvastatin, which is one of the hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitors (statins), is primarily metabolized by CYP2C9 and to a lesser extent by CYP3A4 and CYP2C8. Predictions of drug-drug interactions (DDI) are important for the safety of combination therapies with statins, in particular drugs that are metabolized by CYP3A4. Little information is available regarding drug interactions with fluvastatin. Since CYP2C9 is a polymorphic enzyme, we investigated the effect of DDI via CYP2C9, CYP3A4, and CYP2C8 on fluvastatin pharmacokinetics by using a validated prediction method in relation to CYP2C9 variants...
2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28670240/telmisartan-induced-sprue-like-enteropathy-a-case-report-and-a-review-of-patients-using-non-olmesartan-angiotensin-receptor-blockers
#5
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
https://www.readbyqxmd.com/read/28656677/author-s-response-to-letter-to-the-editor-on-physiologically-based-pharmacokinetic-predictions-of-intestinal-bcrp-mediated-effect-of-telmisartan-on-the-pharmacokinetics-of-rosuvastatin-in-humans
#6
https://www.readbyqxmd.com/read/28656296/the-ace2-ang%C3%A2-1-7-mas-receptor-axis-attenuates-cardiac-remodeling-and-fibrosis-in-post-myocardial-infarction
#7
Juan Wang, Wen He, Liping Guo, Yin Zhang, Hui Li, Suxia Han, Difei Shen
Myocardial remodeling serves an important role in the pathophysiology of coronary heart disease. The angiotensin-converting enzyme (ACE)2-angiotensin-(1-7) [Ang (1‑7)]‑Mas receptor (MasR) axis is a key regulator in myocardial remodeling and development of heart failure. To investigate how ACE2‑Ang‑(1‑7)‑MasR axis function on myocardial remodeling and cardiac fibrosis in post‑myocardial infarction (MI), male Sprague‑Dawley rats (weight, 200±20 g) were used to establish the model of myocardial infarction by ligating the left coronary artery...
August 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28646121/at1-receptor-blockade-attenuates-outward-aortic-remodeling-associated-with-diet-induced-obesity-in-mice
#8
Friedrich Krueger, Kai Kappert, Anna Foryst-Ludwig, Frederike Kramer, Markus Clemenz, Aleksandra Grzesiak, Manuela Sommerfeld, Jan Paul Bernhard Frese, Andreas Greiner, Ulrich Kintscher, Thomas Unger, Elena Kaschina
The renin-angiotensin-system and obesity have been implicated in vascular outward remodeling, including aneurysms, but the precise mechanisms are yet not understood. We investigated the effect of the angiotensin AT1-receptor antagonist telmisartan on aortic outward remodeling in a diet-induced obesity-model in mice. C57/Black6J mice were fed with either a low-fat diet (LFD), or a high-fat diet (HFD) for 14 weeks. One group of HFD-mice was additionally exposed to telmisartan (3mg/kg/d) for the last 4 weeks. HFD led to aortic outward remodeling, characterized by increased proteolysis, along with structural changes, such as fragmentation of elastic fibres, and decreased elastin content...
June 23, 2017: Clinical Science (1979-)
https://www.readbyqxmd.com/read/28640647/influence-of-prkch-gene-polymorphism-on-antihypertensive-response-to-amlodipine-and-telmisartan
#9
Zan-Ling Zhang, Miao-Miao Zhu, Hui-Lan Li, Li-Hong Shi, Xiao-Ping Chen, Jia Luo, Jin-Feng Zhao
This study aimed to evaluate the effect of PRKCH rs2230500 genetic polymorphism on efficacy of amlodipine and telmisartan for patients with hypertension. A total of 136 essential hypertension (EH) patients were treated with amlodipine (70 patients) or telmisartan (66 patients), respectively. Genetic polymorphism was genotyped by Sanger sequencing. Both baseline and post-treatment blood pressure (BP) and heart rate were measured to evaluate the influence of genetic polymorphism on the antihypertensive response...
June 22, 2017: Clinical and Experimental Hypertension: CHE
https://www.readbyqxmd.com/read/28584018/renin-angiotensin-aldosterone-system-is-not-involved-in-the-arterial-stiffening-induced-by-acute-and-prolonged-exposure-to-high-altitude
#10
Miriam Revera, Paolo Salvi, Andrea Faini, Andrea Giuliano, Francesca Gregorini, Grzegorz Bilo, Carolina Lombardi, Giuseppe Mancia, Piergiuseppe Agostoni, Gianfranco Parati
This randomized, double-blind, placebo-controlled study was designed to explore the effects of exposure to very high altitude hypoxia on vascular wall properties and to clarify the role of renin-angiotensin-aldosterone system inhibition on these vascular changes. Forty-seven healthy subjects were included in this study: 22 randomized to telmisartan (age, 40.3±10.8 years; 7 women) and 25 to placebo (age, 39.3±9.8 years; 7 women). Tests were performed at sea level, pre- and post-treatment, during acute exposure to 3400 and 5400-m altitude (Mt...
July 2017: Hypertension
https://www.readbyqxmd.com/read/28548231/combination-therapy-with-telmisartan-and-parecoxib-induces-regression-of-endometriotic-lesions
#11
Anca Nenicu, Yuan Gu, Christina Körbel, Michael D Menger, Matthias W Laschke
BACKGROUND AND PURPOSE: Telmisartan suppresses the development of endometriotic lesions. However, the drug also up-regulates the expression of cyclooxygenase (COX)-2, which has been suggested to promote the progression of endometriosis. Accordingly, we herein analysed whether a combination therapy with telmisartan and a COX-2 inhibitor may be more effective in the treatment of endometriotic lesions than application of telmisartan alone. EXPERIMENTAL APPROACH: Endometriotic lesions were induced in the peritoneal cavity of C57BL/6 mice, which were daily treated with an intraperitoneal (i...
May 26, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28538203/uhplc-ms-ms-method-with-sample-dilution-to-test-therapeutic-adherence-through-quantification-of-ten-antihypertensive-drugs-in-urine-samples
#12
Amedeo De Nicolò, Valeria Avataneo, Franco Rabbia, Mauro Sciandra, Francesco Tosello, Jessica Cusato, Elisa Perlo, Paolo Mulatero, Franco Veglio, Giovanni Di Perri, Antonio D'Avolio
Nowadays, hypertension represents an important health problem, particularly in developed countries. In some cases the standard therapeutic approaches are not able to reestablish the normal blood pressure values: this condition is called "resistant hypertension". However, a fraction of cases of resistant hypertension are actually due to poor adherence to the prescribed therapy. Therapeutic Drug Monitoring could represent a direct and useful tool to correctly identify non-compliant patients. Nevertheless, high throughput methods for the simultaneous monitoring of a wide panel of drugs in the same analysis are lacking and, furthermore, there is not a generally acknowledged "standard" matrix for this test (plasma or urine)...
May 13, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28535976/oatp-and-efflux-transporter-mediated-hepatic-uptake-and-biliary-excretion-of-cilostazol-and-its-metabolites-in-rats-and-humans
#13
Chong Wang, Xiaokui Huo, Changyuan Wang, Qiang Meng, Zhihao Liu, Pengyuan Sun, Jian Cang, Huijun Sun, Kexin Liu
Cilostazol undergoes extensive liver metabolism. However, the transporter-mediated hepatic disposition of cilostazol remains unknown. The present study was performed to investigate the hepatic uptake and biliary excretion of cilostazol and its metabolites (OPC-13015 and OPC-13213) using rat liver and human transporter-transfected cells in vitro. Cilostazol uptake by rat liver slices and isolated rat hepatocytes exhibited time-, concentration-, and temperature-dependency and was decreased by Oatp inhibitors, which suggested that Oatp was involved in the hepatic uptake of cilostazol...
May 20, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28521674/sorbitane-monostearate-and-cholesterol-based-niosomes-for-oral-delivery-of-telmisartan-from-bench-to-preclinical-implementation-in-wistar-albino-rats
#14
Abdul Ahad, Mohammad Raish, Fahad I Al-Jenoobi, Abdullah M Al-Mohizea
BACKGROUND: Niosomes are non-ionic surfactant vesicles used as drug carriers for encapsulating both hydrophobic and hydrophilic drugs. The aim of the present study was to prepare and characterize niosomes formulations for oral delivery of telmisartan and evaluated for its antihypertensive activity. METHOD: Telmisartan loaded niosomes were prepared using thin film hydration method by varying the Span 60 and cholesterol at several molar ratios and characterized for vesicles size, polydispersity index, zeta potential, entrapment efficiency...
May 18, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/28518053/effects-of-genetic-variants-in-ugt1a1-slco1b3-abcb1-abcc2-abcg2-orm1-on-pk-pd-of-telmisartan-in-chinese-patients-with-mild-to-moderate-essential-hypertension%C3%A2
#15
Qi Pei, Liu Yang, Hong-Yi Tan, Shi-Kun Liu, Yang Liu, Lu Huang, Rong-Hui Li, Qian Wan, Jie Huang, Cheng-Xian Guo, Xiao-Cong Zuo, Jingle Li, Guo-Ping Yang
PURPOSE: This study aimed to understand the effects of single nucleotide polymorphisms (SNPs) in UGT1A1, SLCO1B3, ABCB1, ABCC2, ABCG2, and ORM1 on the pharmacokinetics (PK) (plasma concentration) and pharmacodynamics (PD) (blood pressure) of telmisartan in Chinese patients. METHODS: 58 Han Chinese patients (aged 45 - 72 years) with mild to moderate essential hypertension were included and received 80 mg/day telmisartan for 4 weeks. The plasma concentration and genetic variants were determined by LC/MS/MS and MALDI-TOF mass spectrometry, respectively...
May 18, 2017: International Journal of Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28509725/telmisartan-and-hydrochlorothiazide-antihypertensive-treatment-in-high-sodium-intake-population-a-randomized-double-blind-trial
#16
Puhong Zhang, Hongyi Wang, Lei Sun, Jing Zhang, Yang Xi, Yangfeng Wu, Lijing L Yan, Xian Li, Ningling Sun
OBJECTIVES: To compare the blood pressure (BP)-lowering effects of telmisartan 40 mg/day and hydrochlorothiazide (HCTZ) 25 mg/day in high sodium intake patients with mild-to-moderate hypertension in China. METHODS: In this randomized, double-blind trial, eligible patients were randomly divided into telmisartan and HCTZ groups with three follow-ups scheduled on days 15, 30, and 60 after enrollment to compare BP decrease, hypokalemia, and other adverse events after intervention...
May 13, 2017: Journal of Hypertension
https://www.readbyqxmd.com/read/28490219/recruitment-of-macrophages-from-the-spleen-contributes-to-myocardial-fibrosis-and-hypertension-induced-by-angiotensin-ii
#17
Ning-Ping Wang, James Erskine, Wei-Wei Zhang, Rong-Hua Zheng, Li-Hui Zhang, Garret Duron, Julian Gendreau, Zhi-Qing Zhao
INTRODUCTION: The purpose of this study was to determine whether macrophages migrated from the spleen are associated with angiotensin II-induced cardiac fibrosis and hypertension. METHODS: Sprague-Dawley rats were subjected to angiotensin II infusion in vehicle (500 ng/kg/min) for up to four weeks. In splenectomy, the spleen was removed before angiotensin II infusion. In the angiotensin II AT1 receptor blockade, telmisartan was administered by gastric gavage (10 mg/kg/day) during angiotensin II infusion...
April 2017: Journal of the Renin-angiotensin-aldosterone System: JRAAS
https://www.readbyqxmd.com/read/28456626/compound-21-and-telmisartan-combination-mitigates-type-2-diabetic-nephropathy-through-amelioration-of-caspase-mediated-apoptosis
#18
Anuradha Pandey, Anil Bhanudas Gaikwad
The current study aimed to understand the role of novel, highly selective, orally active, non-peptide Angiotensin II type 2 receptor (AT2R) agonist, Compound 21 and its potential additive effect with Telmisartan on apoptosis and underlying posttranslational modifications in a non-genetic murine model for type 2 diabetic nephropathy (T2DN). An experimental model for T2DN was developed by administering low dose Streptozotocin in high fat diet fed male Wistar rats, followed by their treatment with Telmisartan, C21 or their combination...
June 10, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28447738/telmisartan-suppresses-cardiac-hypertrophy-by-inhibiting-cardiomyocyte-apoptosis-via-the-nfat-anp-bnp-signaling-pathway
#19
Xiurong Li, Yuhuai Lan, Yan Wang, Minghao Nie, Yanhong Lu, Eryang Zhao
Telmisartan, a type of angiotensin II (Ang II) receptor inhibitor, is a common agent used to treat hypertension in the clinic. Hypertension increases cardiac afterload and promotes cardiac hypertrophy. However, the ventricular Ang II receptor may be activated in the absence of hypertension. Therefore, telmisartan may reduce cardiac hypertrophy by indirectly ameliorating hypertensive symptoms and directly inhibiting the cardiac Ang II receptor. Nuclear factor of activated T‑cells (NFAT) contributes to cardiac hypertrophy via nuclear translocation, which induces a cascade of atrial natriuretic peptide (ANP) and brain/B‑type natriuretic peptide (BNP) expression and cardiomyocyte apoptosis...
May 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28445965/molecular-docking-3d-qsar-and-structural-optimization-on-imidazo-pyridine-derivatives-dually-targeting-at1-and-pparg
#20
Jun Zhang, Qing-Qing Hao, Xin Liu, Zhi Jing, Wen-Qing Jia, Shu-Qing Wang, Wei-Ren Xu, Xian-Chao Cheng, Run-Ling Wang
Telmisartan, a bifunctional agent of blood pressure lowering and glycemia reduction, was previously reported to antagonize angiotensin II type 1 (AT1) receptor and partially activate peroxisome proliferator-activated receptor γ (PPARγ) simultaneously. Through the modification to telmisartan, researchers designed and obtained imidazo-\pyridine derivatives with the IC50s of 0.49~94.1 nM against AT1 and EC50s of 20~3640 nM towards PPARγ partial activation. For minutely inquiring the interaction modes with the relevant receptor and analyzing the structure-activity relationships, molecular docking and 3D-QSAR (Quantitative structure-activity relationships) analysis of these imidazo-\pyridines on dual targets were conducted in this work...
April 11, 2017: Oncotarget
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