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telmisartan

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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
#1
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
#2
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
#3
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
#4
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
#5
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
#6
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
#7
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
#8
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
#9
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
#10
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
#11
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
https://www.readbyqxmd.com/read/28434702/inhibition-or-deletion-of-angiotensin-ii-type-1-receptor-suppresses-elastase-induced-experimental-abdominal-aortic-aneurysms
#12
Haojun Xuan, Baohui Xu, Wei Wang, Hiroki Tanaka, Naoki Fujimura, Masaaki Miyata, Sara A Michie, Ronald L Dalman
OBJECTIVE: Angiotensin (Ang) II type 1 receptor (AT1) activation is essential for the development of exogenous Ang II-induced abdominal aortic aneurysms (AAAs) in hyperlipidemic animals. Experimental data derived from this modeling system, however, provide limited insight into the role of endogenous Ang II in aneurysm pathogenesis. Consequently, the potential translational value of AT1 inhibition in clinical AAA disease management remains incompletely understood on the basis of the existing literature...
April 20, 2017: Journal of Vascular Surgery
https://www.readbyqxmd.com/read/28421141/excess-of-aminopeptidase-a-in-the-brain-elevates-blood-pressure-via-the-angiotensin-ii-type-1-and-bradykinin-b2-receptors-without-dipsogenic-effect
#13
Takuto Nakamura, Masanobu Yamazato, Akio Ishida, Yusuke Ohya
Aminopeptidase A (APA) cleaves angiotensin (Ang) II, kallidin, and other related peptides. In the brain, it activates the renin angiotensin system and causes hypertension. Limited data are available on the dipsogenic effect of APA and pressor effect of degraded peptides of APA such as bradykinin. Wistar-Kyoto rats received intracerebroventricular (icv) APA in a conscious, unrestrained state after pretreatment with (i) vehicle, (ii) 80 μg of telmisartan, an Ang II type-1 (AT1) receptor blocker, (iii) 800 nmol of amastatin, an aminopeptidase inhibitor, and (iv) 1 nmol of HOE-140, a bradykinin B2 receptor blocker...
2017: International Journal of Hypertension
https://www.readbyqxmd.com/read/28415046/cost-benefit-effectiveness-of-angiotensin-ii-receptor-blockers-in-patients-with-uncomplicated-hypertension-a-comparative-analysis
#14
Alberto Mazza, Antonella Paola Sacco, Danyelle M Townsend, Gianni Bregola, Edgardo Contatto, Isabella Cappello, Laura Schiavon, Emilio Ramazzina, Domenico Rubello
OBJECTIVE: The treatment of hypertensive patients (HTs) requires a long-term commitment of compliance for the patient and resources by the healthcare system. This poses an economic dilemma in countries where universal healthcare is standard. The aim of this study was to evaluate the costs/health benefit and effectiveness of treatment with angiotensin-II receptor blockers (ARBs) in uncomplicated essential hypertension. DESIGN AND METHODS: The daily and annual economic commitment for treating patients with ARBs was estimated using pharmacy dispensing records and the BP-lowering effects of candesartan, irbesartan, losartan, olmesartan, telmisartan and valsartan was evaluated retrospectively...
June 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28393446/copper-mediated-late-stage-functionalization-of-heterocycle-containing-molecules
#15
Ming Shang, Ming-Ming Wang, Tyler G Saint-Denis, Ming-Hong Li, Hui-Xiong Dai, Jin-Quan Yu
One long-standing issue in directed C-H functionalization is that either nitrogen or sulfur atoms present in heterocyclic substrates may bind preferentially to a transition-metal catalyst rather than to the desired directing group. This competitive binding has largely hindered the application of C-H functionalization in late-stage heterocycle drug discovery. Reported here is the use of an oxazoline-based directing group capable of overriding the poisoning effect of a wide range of heterocycle substrates. The potential use of this directing group in pharmaceutical drug discovery is illustrated by diversification of Telmisartan (an antagonist for the angiotensin II receptor) through copper-mediated C-H amination, hydroxylation, thiolation, arylation, and trifluoromethylation...
May 2, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28390695/achieved-blood-pressure-and-cardiovascular-outcomes-in-high-risk-patients-results-from-ontarget-and-transcend-trials
#16
Michael Böhm, Helmut Schumacher, Koon K Teo, Eva M Lonn, Felix Mahfoud, Johannes F E Mann, Giuseppe Mancia, Josep Redon, Roland E Schmieder, Karen Sliwa, Michael A Weber, Bryan Williams, Salim Yusuf
BACKGROUND: Studies have challenged the appropriateness of accepted blood pressure targets. We hypothesised that different levels of low blood pressure are associated with benefit for some, but harm for other outcomes. METHODS: In this analysis, we assessed the previously reported outcome data from high-risk patients aged 55 years or older with a history of cardiovascular disease, 70% of whom had hypertension, from the ONTARGET and TRANSCEND trials investigating ramipril, telmisartan, and their combination, with a median follow-up of 56 months...
June 3, 2017: Lancet
https://www.readbyqxmd.com/read/28388365/protective-effects-of-telmisartan-and-tempol-on-lipopolysaccharide-induced-cognitive-impairment-neuroinflammation-and-amyloidogenesis-possible-role-of-brain-derived-neurotrophic-factor
#17
Waleed A I Khallaf, Basim A S Messiha, Amira M H Abo-Youssef, Nesrine S El-Sayed
Angiotensin II has pro-inflammatory and pro-oxidant potentials. We investigated the possible protective effects of the Angiotensin II receptor blocker telmisartan, compared with the superoxide scavenger tempol, on lipopolysaccharide (LPS)-induced cognitive decline and amyloidogenesis. Briefly, mice were allocated into a normal control group, an LPS control group, a tempol treatment group, and 2 telmisartan treatment groups. A behavioral study was conducted followed by a biochemical study via assessment of brain levels of beta amyloid (Aβ) and brain-derived neurotropic factor (BDNF) as amyloidogenesis and neuroplasticity markers, tumor necrosis factor alpha (TNF-α), nitric oxide end products (NOx), neuronal and inducible nitric oxide synthase (nNOS and iNOS) as inflammatory markers, and superoxide dismutase (SOD), malondialdehyde (MDA), glutathione reduced (GSH), and nitrotyrosine (NT) as oxido-nitrosative stress markers...
April 7, 2017: Canadian Journal of Physiology and Pharmacology
https://www.readbyqxmd.com/read/28385651/intranasal-telmisartan-ameliorates-brain-pathology-in-five-familial-alzheimer-s-disease-mice
#18
Nofar Torika, Keren Asraf, Hagit Cohen, Sigal Fleisher-Berkovich
The renin-angiotensin system (RAS) is a major circulative system engaged in homeostasis modulation. Angiotensin II (Ang II) serves as its main effector hormone upon binding to its primary receptor, Ang II receptor type 1 (AT1R). It is well established that an intrinsic independent brain RAS exists. Abnormal AT1R activation both in the periphery and in the brain probably contributes to the development of Alzheimer's disease (AD) pathology that is characterized, among others, by brain inflammation. Moreover, treatment with drugs that block AT1R (AT1R blockers, ARBs) ameliorates most of the clinical risk factors leading to AD...
April 3, 2017: Brain, Behavior, and Immunity
https://www.readbyqxmd.com/read/28374982/angiotensin-ii-receptor-blockers-inhibit-the-generation-of-epoxyeicosatrienoic-acid-from-arachidonic-acid-in-recombinant-cyp2c9-cyp2j2-and-human-liver-microsomes
#19
Asuna Senda, Yuji Mukai, Toru Hayakawa, Yuka Kato, Erik Eliasson, Anders Rane, Takaki Toda, Nobuo Inotsume
Cytochrome P450 (CYP) 2C9, CYP2C8 and CYP2J2 enzymes, which metabolize arachidonic acid to epoxyeicosatrienoic acids (EETs), have cardioprotective effects including anti-inflammation and vasodilation. We have recently shown that some angiotensin II receptor blockers (ARBs) may inhibit AA metabolism via CYP2C8. Using recombinant CYP2C9, CYP2J2, and human liver microsomes (HLMs), the aim was now to compare the ability of six different clinically used ARBs to inhibit AA metabolism in vitro. The rank order of the ARBs for the 50% inhibitory concentration (IC50 ) of AA metabolism was losartan < telmisartan < irbesartan < candesartan < olmesartan < valsartan via CYP2C9, and telmisartan < irbesartan < olmesartan < losartan < candesartan and valsartan via CYP2J2...
April 4, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28336160/unexpected-drug-induced-raynaud-phenomenon-analysis-from-the-french-national-pharmacovigilance-database
#20
Émilie Bouquet, Geoffrey Urbanski, Christian Lavigne, Pascale Lainé-Cessac
OBJECTIVE: To estimate the association between exposure to medicinal products and Raynaud phenomenon. METHODS: The study used the data of all adverse drug reactions notified to the French national pharmacovigilance database. All cases reported between 1st January 1995 and 10th December 2012 were selected. A case/non-case method was used to measure disproportionality of the association between drug exposure and Raynaud phenomenon. The cases concerned all observations involving Raynaud phenomenon...
February 22, 2017: Thérapie
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