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https://www.readbyqxmd.com/read/28336160/unexpected-drug-induced-raynaud-phenomenon-analysis-from-the-french-national-pharmacovigilance-database
#1
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
https://www.readbyqxmd.com/read/28330645/design-of-fixed-dose-combination-and-physicochemical-characterization-of-enteric-coated-bilayer-tablet-with-circadian-rhythmic-variations-containing-telmisartan-and-pravastatin-sodium
#2
Daoqi Luo, Joo Hee Kim, Chulhun Park, Euichaul Oh, Jun Bum Park, Jing-Hao Cui, Qing-Ri Cao, Beom-Jin Lee
The aim of this study was to investigate a fixed dose combination (FDC) of telmisartan (TEL) and pravastatin sodium (PRA) in enteric-coated bilayer tablets, which was designed for once-daily bedtime dose in order to match circadian rhythmic variations of hypertension and cholesterol synthesis and optimize the patient friendly dosing treatment. Due to the poor aqueous solubility of TEL, a ternary solid dispersions (SD) consisting of TEL, polyethylene glycol 6000 (PEG 6000) and magnesium oxide (MgO) were designed to enhance its dissolution rate in intestinal fluid...
March 18, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28289180/beneficial-effects-of-apelin-on-vascular-function-in-patients-with-central-obesity
#3
Francesca Schinzari, Augusto Veneziani, Nadia Mores, Angela Barini, Nicola Di Daniele, Carmine Cardillo, Manfredi Tesauro
Patients with central obesity have impaired insulin-stimulated vasodilation and increased ET-1 (endothelin 1) vasoconstriction, which may contribute to insulin resistance and vascular damage. Apelin enhances insulin sensitivity and glucose disposal but also acts as a nitric oxide (NO)-dependent vasodilator and a counter-regulator of AT1 (angiotensin [Ang] II type 1) receptor-induced vasoconstriction. We, therefore, examined the effects of exogenous (Pyr(1))apelin on NO-mediated vasodilation and Ang II- or ET-1-dependent vasoconstrictor tone in obese patients...
March 13, 2017: Hypertension
https://www.readbyqxmd.com/read/28285137/functional-analysis-of-carboxylesterase-in-human-induced-pluripotent-stem-cell-derived-enterocytes
#4
Tomoki Kabeya, Wakana Matsumura, Takahiro Iwao, Masakiyo Hosokawa, Tamihide Matsunaga
Human carboxylesterase (CES) is a key esterase involved in the metabolism and biotransformation of drugs. Hydrolysis activity in the human small intestine is predominantly mediated by CES2A1 rather than CES1A. In drug development studies, Caco-2 cells are commonly used as a model to predict drug absorption in the human small intestine. However, the expression patterns of CES2A1 and CES1A in Caco-2 cells differ from those in the human small intestine. There are also species-specific differences in CES expression patterns between human and experimental animals...
April 22, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28274907/mobile-device-based-electronic-data-capture-system-used-in-a-clinical-randomized-controlled-trial-advantages-and-challenges
#5
Jing Zhang, Lei Sun, Yu Liu, Hongyi Wang, Ningling Sun, Puhong Zhang
BACKGROUND: Electronic data capture (EDC) systems have been widely used in clinical research, but mobile device-based electronic data capture (mEDC) system has not been well evaluated. OBJECTIVE: The aim of our study was to evaluate the feasibility, advantages, and challenges of mEDC in data collection, project management, and telemonitoring in a randomized controlled trial (RCT). METHODS: We developed an mEDC to support an RCT called "Telmisartan and Hydrochlorothiazide Antihypertensive Treatment (THAT)" study, which was a multicenter, double-blinded, RCT, with the purpose of comparing the efficacy of telmisartan and hydrochlorothiazide (HCTZ) monotherapy in high-sodium-intake patients with mild to moderate hypertension during a 60 days follow-up...
March 8, 2017: Journal of Medical Internet Research
https://www.readbyqxmd.com/read/28244897/comparing-the-clinical-efficacy-of-resting-and-antihypertensive-medication-in-patients-of-hypertensive-urgency-a-randomized-control-trial
#6
Sung Keun Park, Won Joong Kim, Dong-Young Lee, Sang Yoon Lee, Hyun Sun Park, Hae Won Kim, Beom Kim, Kyoung Hyoub Moon
OBJECTIVE: Hypertensive urgency is defined as a severe elevation of blood pressure (BP) without target organ damage. In emergency room, hypertensive urgency has been conventionally managed by antihypertensive medication. However, there has been increasing concern for the safety of antihypertensive medication in hypertensive urgency. Thus, this study was to compare the clinical efficacy of resting and antihypertensive medication in managing hypertensive urgency. METHODS: For 138 hypertensive urgency patients admitting in emergency room of Veterans Health Center hospital, a single-center, randomized controlled trial was conducted...
February 27, 2017: Journal of Hypertension
https://www.readbyqxmd.com/read/28244896/adjunctive-therapy-with-statins-reduces-residual-albuminuria-proteinuria-and-provides-further-renoprotection-by-downregulating-the-angiotensin-ii-at1-pathway-in-hypertensive-nephropathy
#7
Zhi Zhang, Ziqiang Li, Kaijin Cao, Dailong Fang, Fazhan Wang, Gang Bi, Jian Yang, Yingju He, Jinhui Wu, Yuquan Wei, Xiangrong Song
OBJECTIVES: Blockade of the renin-angiotensin II (Ang II) system by AT1 blockers (ARBs) and angiotensin-converting enzyme inhibitors retards the progression of chronic kidney disease (CKD) by reducing albuminuria/proteinuria. However, many patients with CKD suffer from residual albuminuria/proteinuria, which is an independent risk factor for CKD progression. The aim of the current study is to investigate the effect of pitavastatin, one of the adjunctive agents to ARBs, on the reduction of albuminuria/proteinuria and further renoprotection mediated by telmisartan in spontaneously hypertensive rats...
February 27, 2017: Journal of Hypertension
https://www.readbyqxmd.com/read/28237650/inhibition-and-inactivation-of-human-cyp2j2-implications-in-cardiac-pathophysiology-and-opportunities-in-cancer-therapy
#8
REVIEW
Aneesh Karkhanis, Yanjun Hong, Eric Chun Yong Chan
Extrahepatic cytochrome P450 enzymes (CYP450) are pivotal in the metabolism of endogenous substrates and xenobiotics. CYP2J2 is a major cardiac CYP450 and primarily metabolizes polyunsaturated fatty acids such as arachidonic acid to cardioactive epoxyeicosatrienoic acids. Due to its role in endobiotic metabolism, CYP2J2 has been actively studied in recent years with the focus on its biological functions in cardiac pathophysiology. Additionally, CYP2J2 metabolizes a number of xenobiotics such as astemizole and terfenadine and is potently inhibited by danazol and telmisartan...
February 23, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28230062/triple-combination-therapy-in-the-treatment-of-hypertension-a-review-of-the-evidence
#9
REVIEW
R Düsing, B Waeber, M Destro, C Santos Maia, P Brunel
Hypertension is a serious public health concern with inadequate control of blood pressure (BP) worldwide. Contributing factors include low efficacy of drugs, underuse of combination therapies, irrational combinations, physicians' therapeutic inertia and poor adherence to treatment. Current guidelines recommend the use of initial (dual) combination therapy in high-risk patients for immediate BP response, better short- and long-term BP control, and continued/improved patient adherence. This article aims to review the existing evidence of triple-combination therapies with respect to efficacy, safety and adherence to treatment...
February 23, 2017: Journal of Human Hypertension
https://www.readbyqxmd.com/read/28228970/comparison-of-endothelial-function-improvement-estimated-with-reactive-hyperemia-index-between-ramipril-and-telmisartan-in-hypertensive-patients
#10
You-Jeong Ki, Jae-Bin Seo, Hack-Lyoung Kim, Woo-Hyun Lim, Hye Yeon Seo, Jin Yong Lee, Woo-Young Chung
BACKGROUND: Endothelium has a function to regulate vascular tone by releasing mediators either vasodilating or vasoconstricting blood vessels. Endothelial dysfunction can be measured conveniently by Reactive Hyperemia Index (RHI) with a peripheral arterial tonometry. Angiotensin-converting enzyme inhibitors (ACEIs) and angiotensin II (AT II) receptor blockers (ARBs) are considered to have beneficial effects on endothelium through inhibition of AT II. This study was performed to compare the effect of ACEIs or ARBs on endothelial function estimated by RHI in hypertensive patients...
2017: Clinical Hypertension
https://www.readbyqxmd.com/read/28224326/treatment-with-telmisartan-a-long-acting-angiotensin-ii-receptor-blocker-prevents-migraine-attacks-in-japanese-non-responders-to-lomerizine
#11
Ken Ikeda, Sayori Hanashiro, Yuichi Ishikawa, Masahiro Sawada, Maya Kyuzen, Harumi Morioka, Junya Ebina, Junpei Nagasawa, Masaru Yanagihashi, Ken Miura, Takehisa Hirayama, Takanori Takazawa, Osamu Kano, Kiyokazu Kawabe, Yasuo Iwasaki
Lomerizine, calcium channel blocker, is the most used medication for migraine prophylaxis in Japan. The effectiveness of this drug is reported as 50-75%. Telmisartan is angiotensin II receptor blockers which plasma half-life is 24 h. We examined whether telmisartan has preventative benefits in lomerizine non-responsive migraineurs. Lomerizine non-responders received telmisartan (20 mg/day) for 3 months after the investigation period of 3 months. Blood pressure, frequency of headache days/month, headache severity, and doses of triptans and analgesics were analyzed by Wilcoxon signed rank test...
February 21, 2017: Neurological Sciences
https://www.readbyqxmd.com/read/28207015/telmisartan-induced-lichen-planus-eruption-manifested-on-vitiliginous-skin
#12
Wai P Chan, Vernon T Mackey, Diana K Sun
No abstract text is available yet for this article.
January 2017: Cutis; Cutaneous Medicine for the Practitioner
https://www.readbyqxmd.com/read/28189098/telmisartan-attenuates-diabetes-induced-depression-in-rats
#13
Urmila Aswar, Shilpa Chepurwar, Sumit Shintre, Manoj Aswar
BACKGROUND: Role of brain renin angiotensin system (RAS) is well understood and various clinical studies have proposed neuroprotective effects of ARB's. It is also assumed that diabetic depression is associated with activation of brain RAS, HPA axis dysregulation and brain inflammatory events. Therefore, the present study was designed to investigate the antidepressant effect of low dose telmisartan (TMS) in diabetes induced depression (DID) in rats. METHODS: Diabetes was induced by injecting streptozotocin...
April 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28144709/glucagon-increase-after-chronic-at1-blockade-is-more-likely-related-to-an-indirect-leptin-dependent-than-to-a-pancreatic-%C3%AE-cell-dependent-mechanism
#14
Martin Mildner, Helge Müller-Fielitz, Ines Stölting, Olaf Jöhren, Muscha Steckelings, Walter Raasch
AT1 blockers (ARB) prevent diabetes by improving pancreatic β cell function. Less is known about whether α cells are affected although they express angiotensin II (AngII) receptors. We aimed to investigate glucagon release upon AngII stimulation. We determined glucagon release after AngII stimulation (0.01-100 μM) in α cells (InR1G9) and isolated murine islets. We determined plasma glucagon in rats that were chronically treated with AngII (9 μg/h) or the ARBs telmisartan (8 mg/kg/day) and candesartan (16 mg/kg/day) and correlated glucagon with additional hormones (e...
January 31, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28128331/identification-of-a-novel-selective-ppar%C3%AE-ligand-with-a-unique-binding-mode-and-improved-therapeutic-profile-in-vitro
#15
Wei Yi, Jingjing Shi, Guanguan Zhao, X Edward Zhou, Kelly Suino-Powell, Karsten Melcher, H Eric Xu
Thiazolidinediones (TZD) function as potent anti-diabetic drugs through their direct action on the nuclear receptor peroxisome proliferator-activated receptor γ (PPARγ), but their therapeutic benefits are compromised by severe side effects. To address this concern, here we developed a potent "hit" compound, VSP-51, which is a novel selective PPARγ-modulating ligand with improved therapeutic profiles in vitro compared to the multi-billion dollar TZD drug rosiglitazone (Rosi). Unlike Rosi, VSP-51 is a partial agonist of PPARγ with improved insulin sensitivity due to its ability to bind PPARγ with high affinity without stimulating adipocyte differentiation and the expression of adipogenesis-related genes...
January 27, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28123481/effect-of-telmisartan-and-enalapril-on-ventricular-remodeling-and-kidney-prognosis-of-patients-with-coronary-artery-disease-complicated-with-diabetic-nephropathy
#16
Yuyan Hou, Fucheng Zhang, Zhiqiang Liu, Shuhong Su, Xiao Wu, Zhifang Wang
The aim of the present study was to compare the value of telmisartan and enalapril on ventricular remodeling and kidney prognosis of patients with coronary artery disease complicated with diabetic nephropathy, and provide discussion on clinical reasonably chosen medicine. A total of 60 cases of coronary artery disease complicated with diabetic nephropathy were randomly divided for telmisartan (80 mg/day) treatment (n=32), enalapril (10 mg/day) treatment (n=28), while the rest of the therapy was kept the same...
January 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28118376/urine-eicosanoids-in-the-metabolic-abnormalities-telmisartan-and-hiv-infection-math-trial
#17
Catherine N Le, Todd Hulgan, Chi-Hong Tseng, Ginger L Milne, Jordan E Lake
OBJECTIVES: Arachidonic acid metabolites (eicosanoids) reflect oxidative stress and vascular health and have been associated with anthropometric measures and sex differences in cross-sectional analyses of HIV-infected (HIV+) persons. Telmisartan is an angiotensin receptor blocker and PPAR-γ agonist with potential anti-inflammatory and metabolic benefits. We assessed telmisartan's effects on urine eicosanoids among HIV+ adults with central adiposity on suppressive antiretroviral therapy enrolled in a prospective clinical trial...
2017: PloS One
https://www.readbyqxmd.com/read/28102934/crosstalk-between-angiotensin-and-the-nonamyloidogenic-pathway-of-alzheimer-s-amyloid-precursor-protein
#18
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 the 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
#19
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
#20
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
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