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https://www.readbyqxmd.com/read/28102934/crosstalk-between-angiotensin-and-the-non-amyloidogenic-pathway-of-alzheimer-s-amyloid-precursor-protein
#1
Anna Maria Kanarek, Annika Wagner, Jim Küppers, Michael Gütschow, Rolf Postina, Elzbieta Kojro
The association between hypertension and an increased risk for Alzheimer's disease (AD) and dementia is well established. Many data suggest that modulation of the renin-angiotensin system may be meaningful for the prevention and therapy of neurodegenerative disorders, in particular AD. Proteolytic cleavage of the amyloid precursor protein (APP) by α-secretase precludes formation of neurotoxic Aβ peptides and is expected to counteract the development of AD. An established approach for the up-regulation of α-secretase cleavage is activation of G protein-coupled receptors (GPCRs)...
January 19, 2017: FEBS Journal
https://www.readbyqxmd.com/read/28101724/drug-drug-multicomponent-solid-forms-cocrystal-coamorphous-and-eutectic-of-three-poorly-soluble-antihypertensive-drugs-using-mechanochemical-approach
#2
Jamshed Haneef, Renu Chadha
The present study deals with the application of mechanochemical approach for the preparation of drug-drug multicomponent solid forms of three poorly soluble antihypertensive drugs (telmisartan, irbesartan and hydrochlorothiazide) using atenolol as a coformer. The resultant solid forms comprise of cocrystal (telmisartan-atenolol), coamorphous (irbesartan-atenolol) and eutectic (hydrochlorothiazide-atenolol). The study emphasizes that solid-state transformation of drug molecules into new forms is a result of the change in structural patterns, diminishing of dimers and creating new facile hydrogen bonding network based on structural resemblance...
January 18, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28090225/efficacy-and-safety-of-combination-therapy-consisting-of-angiotensin-ii-type-1-receptor-blocker-calcium-channel-blocker-and-hydrochlorothiazide-in-patients-with-hypertension
#3
Yuhei Shiga, Shin-Ichiro Miura, Kota Motozato, Yuka Yoshimine, Kenji Norimatsu, Tadaaki Arimura, Rie Koyoshi, Joji Morii, Takashi Kuwano, Ken Inoue, Tetsuro Shirotani, Kazuaki Fujisawa, Eiyu Matsunaga, Keijiro Saku
BACKGROUND: Many patients continue to have high blood pressure (BP) even after treatment with high-dose (H)-angiotensin II type 1 receptor blocker (ARB)/calcium channel blocker (CCB) or middle-dose (M)-ARB/CCB/hydrochlorothiazide (HCTZ). METHODS: Thirty-two hypertensive patients who had the use of H-ARB/CCB or M-ARB/CCB/HCTZ were enrolled in this study. We applied a changeover with a switch to H-ARB (telmisartan 80 mg/day)/CCB (amlodipine 5 mg/day or nifedipine CR 40 mg/day)/HCTZ (12...
February 2017: Journal of Clinical Medicine Research
https://www.readbyqxmd.com/read/28065235/a-clinical-multicenter-randomized-controlled-study-on-jianpiqinghua-decoction-in-treating-stage-3-chronic-kidney-disease-with-a-syndrome-type-of-dampness-heat-due-to-spleen-deficiency
#4
Ke-Na Yu, Zhao-Hui Ni, Nian-Song Wang, Wen Peng, Yi Wang, Chang-Ming Zhang, Li-Qun He
Objective To evaluate the clinical effectiveness of JianpiQinghua decoction in treating stage 3 chronic kidney disease (CKD3) with syndrome type of dampness-heat due to spleen deficiency. Methods A multicenter, randomized, controlled, prospective, double-blind, and double-simulation study was undertaken. A total of 270 CKD3 patients with syndrome type of dampness-heat due to spleen deficiency from the outpatient departments of six general hospitals were randomly divided into telmisartan+analog traditional Chinese medicine (TA) group, traditional Chinese medicine+analog telmisartan (TCMA) group, and telmisartan+traditional Chinese medicine (TTCM) group, in which the corresponding treatment was applied in addition to basic treatment...
December 20, 2016: Zhongguo Yi Xue Ke Xue Yuan Xue Bao. Acta Academiae Medicinae Sinicae
https://www.readbyqxmd.com/read/28052030/the-angiotensin-ii-type-1-receptor-antagonist-telmisartan-inhibits-cell-proliferation-and-tumor-growth-of-esophageal-adenocarcinoma-via-the-ampk%C3%AE-mtor-pathway-in-vitro-and-in-vivo
#5
Shintaro Fujihara, Asahiro Morishita, Kana Ogawa, Tomoko Tadokoro, Taiga Chiyo, Kiyohito Kato, Hideki Kobara, Hirohito Mori, Hisakazu Iwama, Tsutomu Masaki
Telmisartan, a widely used antihypertensive drug, is an angiotensin II type 1 (AT1) receptor blocker (ARB). This drug inhibits cancer cell proliferation, but the underlying mechanisms in various cancers, including esophageal cancer, remain unknown. The aim of the present study was to evaluate the effects of telmisartan on human esophageal cancer cell proliferation in vitro and in vivo. We assessed the effects of telmisartan on human esophageal adenocarcinoma (EAC) cells using the cell lines OE19, OE33, and SKGT-4...
December 28, 2016: Oncotarget
https://www.readbyqxmd.com/read/28041700/a-comparison-study-of-the-echocardiographic-changes-in-hypertensive-patients-treated-with-telmisartan-vs-enalapril
#6
Najah R Hadi, Mohammad S Abdulzahra, Laith M Al-Huseini, Hayder A Al-Aubaidy
BACKGROUND: Hypertension-induced cardiac dysfunction is variable among different anti-hypertensive medications. This study compares the effects of telmisartan and enalapril on echocardiographic parameters in hypertensive patients. MATERIALS AND METHODS: This was a randomised single blinded study. Eighty hypertensive patients were included in this study and they were randomly allocated into two study groups: Group 1 included 40 patients who took telmisartan 80mg once daily for six months...
December 22, 2016: International Journal of Cardiology
https://www.readbyqxmd.com/read/28040266/angiotensin-ii-at1-receptor-signaling-is-necessary-for-cyclooxygenase-2-dependent-postnatal-nephron-generation
#7
Stefanie Frölich, Patrick Slattery, Dominique Thomas, Itamar Goren, Nerea Ferreiros, Boye L Jensen, Rolf M Nüsing
Deletion of cyclooxygenase-2 (COX-2) causes impairment of postnatal kidney development. Here we tested whether the renin angiotensin system contributes to COX-2-dependent nephrogenesis in mice after birth and whether a rescue of impaired renal development and function in COX-2(-/-) mice was achievable. Plasma renin concentration in mouse pups showed a birth peak and a second peak around day P8 during the first 10 days post birth. Administration of the angiotensin II receptor AT1 antagonist telmisartan from day P1 to P3 did not result in cortical damage...
December 28, 2016: Kidney International
https://www.readbyqxmd.com/read/28027398/physiologically-based-pharmacokinetic-predictions-of-intestinal-bcrp-mediated-effect-of-telmisartan-on-the-pharmacokinetics-of-rosuvastatin-in-humans
#8
Soo Hyeon Bae, Wan-Su Park, Seunghoon Han, Gab-Jin Park, Jongtae Lee, Taegon Hong, Sangil Jeon, Dong-Seok Yim
It was recently reported that the Cmax and AUC of rosuvastatin increases when it is coadministered with telmisartan. The aim of this study was to explore the mechanism of the interaction of telmisartan and rosuvastatin. A full-PBPK model of telmisartan was developed, and the rosuvastatin model in Simcyp (version 15)'s drug library was modified to reflect ethnic differences in rosuvastatin exposure. PK characteristics, including intestinal and hepatic transporter / enzyme specificities of telmisartan and rosuvastatin, were incorporated into the PBPK models to simulate a rosuvastatin (20 mg) - telmisartan (80 mg) multiple dose drug interaction study...
December 27, 2016: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/28025969/quantitative-analysis-of-valsartan-by-two-dimensional-liquid-chromatography-2d-hplc-method-and-its-application-in-a-bioequivalence-study-in-chinese-volunteers%C3%A2
#9
Min Zhang, Yang Deng, Hua-Lin Cai, Ping-Fei Fang, Miao Yan, Bi-Kui Zhang, Yan-Qin Wu
PURPOSE: To develop a sensitive, two-dimensional liquid chromatography (2D-LC) method for determination of valsartan, applied to investigate bioequivalence of two valsartan tablets in Chinese volunteers under fasting condition. METHODS: A full automatic 2D-HPLC system was used to quantify valsartan in human plasma. The analytes were extracted by protein precipitation, using telmisartan as internal standard. The analytical method was applied in a randomized, crossover bioequivalence study of valsartan tablets; the study enrolled 18 Chinese volunteers (12 were men and 6 were women)...
December 27, 2016: International Journal of Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28024639/soluble-telmisartan-bearing-poly-ethylene-glycol-conjugated-chitosan-nanoparticles-augmented-drug-delivery-cytotoxicity-apoptosis-and-cellular-uptake-in-human-cervical-cancer-cells
#10
Anjali Sharma, Kiran Jyoti, Vikas Bansal, Upendra Kumar Jain, Bharat Bhushan, Jitender Madan
Soluble telmisartan and telmisartan were loaded in to poly (ethylene-glycol) grafted chitosan nanoparticles (S-TEL-PEG-CNPs and TEL-PEG-CNPs) for targeting cervical cancer through non-invasive, intravaginal route. The mean particle size of S-TEL-PEG-CNPs was measured to be 23.4±5.9-nm significantly (P<0.05) higher than 16.2±3.2-nm of TEL-PEG-CNPs. In contrast, the zeta-potential (-21.5±4.6-mV) of S-TEL-PEG-CNPs was insignificantly (P>0.05) different from -23.8±3.7-mV of TEL-PEG-CNPs. In addition, S-TEL-PEG-CNPs exhibited higher percent mucoadhesiveness (40...
March 1, 2017: Materials Science & Engineering. C, Materials for Biological Applications
https://www.readbyqxmd.com/read/27994942/effect-of-telmisartan-on-kidney-function-in-patients-with-chronic-kidney-disease-an-observational-study
#11
Ashish Agrawal, Shibnath Kamila, Swetha Reddy, Joyal Lilly, Ms Sadhguna Mariyala
Background: Globally the burden of chronic kidney disease (CKD) is rising, an important cause of death and loss of disability-adjusted life years. Activation of the renin-angiotensin-aldosterone system is involved in its pathogenesis. The aim of the present study was to examine the effects of telmisartan (40 mg/day), an angiotensin receptor blocker (ARB) in Indian patients with CKD in real-life setting. Method: This was a prospective observational study. Fifty-six patients (>18 years) diagnosed with CKD were enrolled into the study...
2016: Journal of drug assessment
https://www.readbyqxmd.com/read/27966230/method-development-and-validation-quantitation-of-telmisartan-bulk-drug-and-its-tablet-formulation-by-1-h-nmr-spectroscopy
#12
Yashwantsinh Jadeja, Bhagyawanti Chomal, Madhavi Patel, Hetal Jebaliya, Ranjan Khunt, Anamik Shah
The quantitative NMR (qNMR) spectroscopy is nowadays a new tool for the determination of pharmaceutical potent biologically active molecules in bulk drug and its tablet formulation than the other analytical techniques. Herein, qNMR method was developed for an anti-hypertensive drug, telmisartan in bulk drug and its tablet formulation. The precise method was developed by using malononitrile as an internal standard. The methylene signal of telmisartan appeared at δ = 5.46 ppm (singlet) relative to the signal of malononitrile at δ = 3...
December 14, 2016: Magnetic Resonance in Chemistry: MRC
https://www.readbyqxmd.com/read/27927602/acute-change-in-glomerular-filtration-rate-with%C3%A2-inhibition-of-the-renin-angiotensin-system-does-not%C3%A2-predict-subsequent-renal-and-cardiovascular%C3%A2-outcomes
#13
Catherine M Clase, Joshua Barzilay, Peggy Gao, Andrew Smyth, Roland E Schmieder, Sheldon Tobe, Koon K Teo, Salim Yusuf, Johannes F E Mann
Initiation of blockade of the renin-angiotensin system may cause an acute decrease in glomerular filtration rate (GFR): the prognostic significance of this is unknown. We did a post hoc analysis of patients with, or at risk for, vascular disease, in two randomized controlled trials: Ongoing Telmisartan Alone and in combination with Ramipril Global Endpoint Trial (ONTARGET) and the Telmisartan Randomized AssessmeNt Study in ACE iNtolerant participants with cardiovascular Disease (TRANSCEND), whose median follow-up was 56 months...
December 4, 2016: Kidney International
https://www.readbyqxmd.com/read/27920497/efficacy-and-safety-of-two-fixed-dose-combinations-of-s-amlodipine-and-telmisartan-ckd-828-versus-s-amlodipine-monotherapy-in-patients-with-hypertension-inadequately-controlled-using-s-amlodipine-monotherapy-an-8-week-multicenter-randomized-double-blind-phase
#14
Sang-Hyun Ihm, Hui-Kyung Jeon, Tae-Joon Cha, Taek-Jong Hong, Sang-Hyun Kim, Nae-Hee Lee, Jung Han Yoon, Namsik Yoon, Kyung-Kuk Hwang, Sang-Ho Jo, Ho-Joong Youn
PURPOSE: To evaluate the blood pressure (BP) lowering efficacy and safety of CKD-828, a fixed-dose combination of S-amlodipine (the more active isomer of amlodipine besylate, which is calcium channel blocker) and telmisartan (long acting angiotensin receptor blocker), in patients with hypertension inadequately controlled with S-amlodipine monotherapy. PATIENTS AND METHODS: Eligible patients (N=187) who failed to respond after 4-week S-amlodipine 2.5 mg monotherapy (sitting diastolic blood pressure [sitDBP] ≥90 mmHg) to receive CKD-828 2...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27918994/importance-of-5-6-aryl-substitution-on-the-pharmacological-profile-of-4-2-propyl-1h-benzo-d-imidazol-1-yl-methyl-1-1-biphenyl-2-carboxylic-acid-derived-ppar%C3%AE-agonists
#15
Victoria Obermoser, Robert Mauersberger, Daniela Schuster, Monika Czifersky, Marina Lipova, Monika Siegl, Ulrich Kintscher, Ronald Gust
In this structure-activity relationship study, the influence of aryl substituents at position 5 or 6 on the pharmacological profile of the partial PPARγ agonist 4'-((2-propyl-1H-benzo[d]imidazol-1-yl)methyl)-[1,1'-biphenyl]-2-carboxylic acid was investigated. This lead was previously identified as the essential part of telmisartan to induce PPARγ activation. Para-OCH3-phenyl substitution strongly increased potency and efficacy independent of the position. Both compounds represent full agonists because of strong hydrophobic contacts with the amino acid Phe363 in the ligand binding domain...
November 25, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27881888/effects-of-ramipril-and-telmisartan-on-plasma-concentrations-of-low-molecular-weight-and-protein-thiols-and-carotid-intima-media-thickness-in-patients-with-chronic-kidney-disease
#16
Angelo Zinellu, Salvatore Sotgia, Arduino A Mangoni, Elisabetta Sotgiu, Sara Ena, Dionigia Arru, Stefano Assaretti, Angela Baralla, Andrea E Satta, Ciriaco Carru
Hypertension, a common feature in chronic kidney disease (CKD), is an independent risk factor for CKD progression and cardiovascular disease. Although inhibitors of the renin-angiotensin system (RAS) exert salutary effects on blood pressure control and proteinuria in CKD patients, their activity towards traditional and novel oxidative markers is largely unknown. We studied the effects of 6-month treatment with telmisartan versus a combination of telmisartan and ramipril on plasma concentrations of low molecular mass (LMW, including homocysteine and cysteine) and protein thiols (PSH) plasma concentration and their relationships with carotid intima media thickness (IMT), in 24 hypertensive CKD patients (age 60 ± 12 years, 8 females and 16 males)...
2016: Disease Markers
https://www.readbyqxmd.com/read/27881849/are-diuretic-additives-fit-for-uncontrolled-hypertensive-patients-receiving-telmisartan-and-amlodipine-treatment
#17
Yoshiaki Taniyama, Ryuichi Morishita
No abstract text is available yet for this article.
November 24, 2016: Hypertension Research: Official Journal of the Japanese Society of Hypertension
https://www.readbyqxmd.com/read/27834982/telmisartan-decreases-microalbuminuria-in-patients-with-type-2-diabetes-mellitus-following-coronary-artery-bypass-grafting
#18
Cevdet Furat, Riza Dogan, Gokhan Ilhan, Ekrem Bayar, Berkan Ozpak, Hakan Kara, Şahin Bozok
OBJECTIVE: This prospective study aimed to investigate the effects of the selective angiotensin receptor antagonist, telmisartan, on microalbuminuria after coronary artery bypass surgery in patients with diabetes mellitus. METHODS: Patients were divided into two groups with block randomisation, using the sealed envelope technique: group T (telmisartan group) consisted of patients who received the angiotensin receptor blocking agent telmisartan 80 mg daily for at least six months in the pre-operative period; group N-T (non-telmisartan group) consisted of patients who received no telmisartan treatment...
November 10, 2016: Cardiovascular Journal of Africa
https://www.readbyqxmd.com/read/27821063/high-fat-diet-induced-atherosclerosis-is-accompanied-with-low-colonic-bacterial-diversity-and-altered-abundances-that-correlates-with-plaque-size-plasma-a-fabp-and-cholesterol-a-pilot-study-of-high-fat-diet-and-its-intervention-with-lactobacillus-rhamnosus
#19
Yee Kwan Chan, Manreetpal Singh Brar, Pirkka V Kirjavainen, Yan Chen, Jiao Peng, Daxu Li, Frederick Chi-Ching Leung, Hani El-Nezami
BACKGROUND: Atherosclerosis appears to have multifactorial causes - microbial component like lipopolysaccharides (LPS) and other pathogen associated molecular patterns may be plausible factors. The gut microbiota is an ample source of such stimulants, and its dependent metabolites and altered gut metagenome has been an established link to atherosclerosis. In this exploratory pilot study, we aimed to elucidate whether microbial intervention with probiotics L. rhamnosus GG (LGG) or pharmaceuticals telmisartan (TLM) could improve atherosclerosis in a gut microbiota associated manner...
November 8, 2016: BMC Microbiology
https://www.readbyqxmd.com/read/27791151/targeting-cyp2j-to-reduce-paclitaxel-induced-peripheral-neuropathic-pain
#20
Marco Sisignano, Carlo Angioni, Chul-Kyu Park, Sascha Meyer Dos Santos, Holger Jordan, Maria Kuzikov, Di Liu, Sebastian Zinn, Stephan W Hohman, Yannick Schreiber, Béla Zimmer, Mike Schmidt, Ruirui Lu, Jing Suo, Dong-Dong Zhang, Stephan M G Schäfer, Martine Hofmann, Ajay S Yekkirala, Natasja de Bruin, Michael J Parnham, Clifford J Woolf, Ru-Rong Ji, Klaus Scholich, Gerd Geisslinger
Chemotherapy-induced peripheral neuropathic pain (CIPNP) is a severe dose- and therapy-limiting side effect of widely used cytostatics that is particularly difficult to treat. Here, we report increased expression of the cytochrome-P450-epoxygenase CYP2J6 and increased concentrations of its linoleic acid metabolite 9,10-EpOME (9,10-epoxy-12Z-octadecenoic acid) in dorsal root ganglia (DRGs) of paclitaxel-treated mice as a model of CIPNP. The lipid sensitizes TRPV1 ion channels in primary sensory neurons and causes increased frequency of spontaneous excitatory postsynaptic currents in spinal cord nociceptive neurons, increased CGRP release from sciatic nerves and DRGs, and a reduction in mechanical and thermal pain hypersensitivity...
November 1, 2016: Proceedings of the National Academy of Sciences of the United States of America
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