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https://www.readbyqxmd.com/read/28805311/mechanistic-model-for-blood-pressure-and-heart-rate-changes-produced-by-telmisartan-in-humans
#1
Dong Woo Chae, Mijeong Son, Yukyung Kim, Hankil Son, Kyungsoo Park
Telmisartan, an angiotensin receptor blocker (ARB), is indicated for the treatment of essential hypertension. This study aimed to develop a mechanistic model of telmisartan drug effect in human using non-invasive markers. Data were acquired from a previous study where telmisartan 80 mg was given once daily for 6 days. Systolic (SBP) and diastolic blood pressure (DBP) and heart rate (HR) were measured before dosing for day 1 to 5 and serially after the last dose. Mean arterial pressure (MAP) and pulse pressure (PP) were calculated from SBP and DBP...
August 14, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28798804/sinomenine-hydrochloride-attenuates-renal-fibrosis-by-inhibiting-excessive-autophagy-induced-by-adriamycin-an-experimental-study
#2
Ming-Ming Zhao, Bin Yang, Qiu Zhang, Jin-Hu Wang, Jin-Ning Zhao, Yu Zhang
The objective of this study is to investigate if sinomenine hydrochloride (SIN-HCl) could be effective against adriamycin-induced renal fibrosis by regulating autophagy in a rat model. Forty male Sprague-Dawley (SD) rats were randomly divided into control group, model group, telmisartan group, and SIN-HCl group; rat model was induced by adriamycin; all rats were given intragastric administration for 6 weeks. Urine was collected from rats in metabolic cages to determine 24 h protein level. This was done after intragastric administration for the first two weeks and then once for every two weeks...
2017: Evidence-based Complementary and Alternative Medicine: ECAM
https://www.readbyqxmd.com/read/28791353/telmisartan-improves-vascular-remodeling-through-ameliorating-prooxidant-and-profibrotic-mechanisms-in-hypertension-via-the-involvement-of-transforming-growth-factor-%C3%AE-1
#3
Peijin Shang, Tianlong Liu, Wenxing Liu, Yuwen Li, Fang Dou, Yikai Zhang, Lijuan Sun, Tiejun Zhang, Zhihui Zhu, Fei Mu, Yi Ding, Aidong Wen
Vascular remodeling is a common complication and pathological basis of hypertension. Transforming growth factor‑β1 (TGF‑β1)/small mothers against decapentaplegic 3 (Smad3) is considered a potential therapeutic target for vascular remodeling in hypertension. The present study aimed to demonstrate the antifibrotic effects of telmisartan and examined the potential mechanisms associated with its prevention of vascular remodeling. Spontaneously hypertensive rats (SHRs) were treated with telmisartan (20 mg/kg), and vascular contractility, reactivity and oxidative stress were preliminarily evaluated...
August 4, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28754590/telmisartan-mitigates-hyperglycemia-induced-vascular-inflammation-by-increasing-gsk3%C3%AE-ser-9-phosphorylation-in-endothelial-cells-and-mouse-aortas
#4
Kee-Ho Song, Sun-Ju Bae, Jiyeon Chang, Jung-Hyun Park, Inho Jo, Kae Won Cho, Du-Hyong Cho
Telmisartan, an angiotensin II type 1 receptor blocker (ARB), attenuates hyperglycemia-aggravated vascular inflammation by decreasing IκB kinase β (IKKβ) expression in endothelial cells. Because glycogen synthase 3β (GSK3β) is involved in inflammatory process by regulating nuclear factor-κB (NF-κB) activity, we investigated whether GSK3β mediates telmisartan-ameliorated vascular inflammation in hyperglycemia-treated endothelial cells and high-fat diet (HFD)-fed mice. Telmisartan remarkably induced GSK3β-Ser(9) phosphorylation in hyperglycemia-treated endothelial cells that accompanied a decrease in hyperglycemia-induced NF-κB p65-Ser(536) phosphorylation, vascular cell adhesion molecule-1 (VCAM-1) expression, and THP-1 monocyte adhesion...
July 25, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28747068/a-dual-ampk-nrf2-activator-reduces-brain-inflammation-after-stroke-by-enhancing-microglia-m2-polarization
#5
Yunjie Wang, Yun Huang, Yazhou Xu, Wenchen Ruan, Haojie Wang, Yihua Zhang, Juan M Saavedra, Luyong Zhang, Zhangjian Huang, Tao Pang
AIMS: Microglia-mediated neuroinflammation plays an important role in focal ischemic stroke, a disorder with no effective therapeutic agents. Since microglial polarization to the M2 phenotype and reduction of oxidative stress are mediated through AMPK and Nrf2 activation, we assessed the dual therapeutic effect of AMPK and Nrf2 activation by a novel neuroprotectant HP-1c in the treatment of ischemic stroke. RESULTS: We developed a novel class of hybrids (HP-1a-HP-1f) of telmisartan and 2-(1-hydroxypentyl)-benzoate (HPBA) as a ring-opening derivative of NBP...
July 26, 2017: Antioxidants & Redox Signaling
https://www.readbyqxmd.com/read/28745698/-telmisartan-in-the-treatment-of-hypertensive-patients
#6
REVIEW
V I Podzolkov, A I Tarzimanova
The paper highlights the use of telmisartan, one of the currently available angiotensin receptor blockers, for the treatment of patients with hypertension, metabolic syndrome, and those at high cardiovascular risk. Telmisartan treatment allows blood pressure control, provides organ protection at different stages of the cardiovascular continuum, and reduces the risk of cardiovascular diseases and death. The additional properties and pleiotropic activity of the drug determines its wide range of applications in cardiology...
2017: Terapevticheskiĭ Arkhiv
https://www.readbyqxmd.com/read/28733707/angiotensin-ii-type-1-receptor-blockers-inhibit-kat-ii-activity-in-the-brain-its-possible-clinical-applications
#7
Izabela Zakrocka, Katarzyna M Targowska-Duda, Artur Wnorowski, Tomasz Kocki, Krzysztof Jóźwiak, Waldemar A Turski
Angiotensin II receptor blockers (ARBs) are one of the most frequently recommended antihypertensive drugs. Apart from their activity towards the circulatory system, ARBs also penetrate the blood-brain barrier and display neuroprotective effects. Kynurenic acid (KYNA) is an endogenous metabolite of tryptophan produced by kynurenine aminotransferase II (KAT II) in the brain. Antagonism towards all ionotropic glutamate (GLU) receptors is the main mechanism of KYNA action. An elevated brain level of KYNA is linked with memory impairment and psychotic symptoms...
July 21, 2017: Neurotoxicity Research
https://www.readbyqxmd.com/read/28727906/potential-of-telmisartan-in-the-treatment-of-benign-prostatic-hyperplasia
#8
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
#9
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
#10
(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
#11
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
#12
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
#13
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
#14
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
#15
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
#16
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
#17
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
#18
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 COX-2, which has been suggested to promote the progression of endometriosis. Accordingly, in the present study we analysed whether a combination therapy with telmisartan and a COX-2 inhibitor may be more effective in the treatment of endometriotic lesions than the application of telmisartan alone. EXPERIMENTAL APPROACH: Endometriotic lesions were induced in the peritoneal cavity of C57BL/6 mice, which were treated daily with an i...
August 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
#19
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/organic-anion-transporting-polypeptide-and-efflux-transporter-mediated-hepatic-uptake-and-biliary-excretion-of-cilostazol-and-its-metabolites-in-rats-and-humans
#20
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
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