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https://www.readbyqxmd.com/read/28914858/-bosentan-use-in-pulmonary-arterial-hypertension-russian-and-foreign-experience
#1
Z S Valieva, T V Martynyuk, I E Chazova
The results of evaluating the efficacy and safety of bosentan in patients with pulmonary arterial hypertension (PAH), as shown by the data of foreign randomized controlled trials and the authors' own experience, convincingly demonstrate that the introduction of the drug into clinical practice has led to a significant improvement of the possibilities of drug therapy in patients with this serious illness. Bosentan substantially improves physical activity in patients, reduces the severity of clinical symptoms, slows down the rates of disease progression, and prolongs survival in patients with different forms of PAH...
2017: Terapevticheskiĭ Arkhiv
https://www.readbyqxmd.com/read/28891448/a-special-focus-on-selexipag-treatment-of-pulmonary-arterial-hypertension
#2
Louise Marqvard Sørensen, Markus Wehland, Marcus Krüger, Ulf Simonsen, Mohamed Zakaria Nassef, Manfred Infanger, Daniela Grimm
BACKGROUND: This review focuses on the treatment of pulmonary arterial hypertension (PAH) with selexipag and compares its drug-related therapeutic effects with those of prostacyclin analogues. METHODS: We searched the relevant literature and summarized the current clinical trials concerning selexipag and PAH. RESULTS: With only few cases per million, PAH is a rare disease, but when untreated it can be life threatening. PAH is linked to elevated levels of endothelin (ET-1) and decreased levels of nitric oxide (NO) and prostacyclin (PGI2)...
September 7, 2017: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/28874133/sildenafil-dosed-concomitantly-with-bosentan-for-adult-pulmonary-arterial-hypertension-in-a-randomized-controlled-trial
#3
Carmine Dario Vizza, Pavel Jansa, Simon Teal, Theresa Dombi, Duo Zhou
BACKGROUND: Few controlled clinical trials exist to support oral combination therapy in pulmonary arterial hypertension (PAH). METHODS: Patients with PAH (idiopathic [IPAH] or associated with connective tissue disease [APAH-CTD]) taking bosentan (62.5 or 125 mg twice daily at a stable dose for ≥3 months) were randomized (1:1) to sildenafil (20 mg, 3 times daily; n = 50) or placebo (n = 53). The primary endpoint was change from baseline in 6-min walk distance (6MWD) at week 12, assessed using analysis of covariance...
September 6, 2017: BMC Cardiovascular Disorders
https://www.readbyqxmd.com/read/28871941/-elevated-expression-of-endothelin-2-in-lung-tissues-of-asthmatic-rats-after-exposed-to-cigarette-smoke-and-its-mechanism
#4
Fangfang Han, Shuyang Zhu, Bi Chen, Jingjing Li
Objective To study the effect of cigarette smoke exposure on the expression of endothelin 2 (ET-2) in bronchial epithelium of asthmatic rats. Methods Asthma models were established through intraperitoneal injection of 1 mL chicken ovalbumin (OVA)/Al(OH)3 mixture (asthma model group, n=6); based on the asthma models, exposure to smoking gas lasted four weeks with 10 cigarettes per day (smoke-exposed asthma group, n=6); based on the smoke-exposed asthma models, the rats were treated with intraperitoneal injection of dexamethasone 2 mg/(kg...
August 2017: Xi Bao Yu Fen Zi Mian Yi Xue za Zhi, Chinese Journal of Cellular and Molecular Immunology
https://www.readbyqxmd.com/read/28855090/effects-of-liquid-post-column-addition-in-electrospray-ionization-performance-in-supercritical-fluid-chromatography-mass-spectrometry
#5
Laura Akbal, Gérard Hopfgartner
In supercritical fluid chromatography coupled to atmospheric pressure ionization mass spectrometry (SFC-MS), the use of a make-up post-column is almost mandatory to avoid analyte precipitation, especially when using low percentage of modifier (<5%) in the mobile phase. Due to the specific nature of gaseous CO2, the tuning of the make-up conditions in electrospray becomes an important factor and can be used to tune analyte sensitivity. Neither a dilution effect (loss of signal) nor a relevant degradation of chromatographic performances is observed with the addition of a make-up at various flow-rates, up to 0...
August 19, 2017: Journal of Chromatography. A
https://www.readbyqxmd.com/read/28819231/in-vitro-micropatterned-human-pluripotent-stem-cell-test-%C3%A2%C2%B5p-hpst-for-morphometric-based-teratogen-screening
#6
Jiangwa Xing, Yue Cao, Yang Yu, Huan Li, Ziwei Song, Hanry Yu
Exposure to teratogenic chemicals during pregnancy may cause severe birth defects. Due to high inter-species variation of drug responses as well as financial and ethical burdens, despite the widely use of in vivo animal tests, it's crucial to develop highly predictive human pluripotent stem cell (hPSC)-based in vitro assays to identify potential teratogens. Previously we have shown that the morphological disruption of mesoendoderm patterns formed by geometrically-confined cell differentiation and migration using hPSCs could potentially serve as a sensitive morphological marker in teratogen detection...
August 17, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28805809/x-ray-structures-of-endothelin-etb-receptor-bound-to-clinical-antagonist-bosentan-and-its-analog
#7
Wataru Shihoya, Tomohiro Nishizawa, Keitaro Yamashita, Asuka Inoue, Kunio Hirata, Francois Marie Ngako Kadji, Akiko Okuta, Kazutoshi Tani, Junken Aoki, Yoshinori Fujiyoshi, Tomoko Doi, Osamu Nureki
Endothelin receptors (ETRs) have crucial roles in vascular control and are targets for drugs designed to treat circulatory-system diseases and cancer progression. The nonpeptide dual-ETR antagonist bosentan is the first oral drug approved to treat pulmonary arterial hypertension. Here we report crystal structures of human endothelin ETB receptor bound to bosentan and to the ETB-selective analog K-8794, at 3.6-Å and 2.2-Å resolution, respectively. The K-8794-bound structure reveals the detailed water-mediated hydrogen-bonding network at the transmembrane core, which could account for the weak negative allosteric modulation of ETB by Na(+) ions...
September 2017: Nature Structural & Molecular Biology
https://www.readbyqxmd.com/read/28794135/pulmonary-vasodilator-therapy-is-associated-with-greater-survival-in-eisenmenger-syndrome
#8
Clare Arnott, Geoff Strange, Andrew Bullock, Adrienne C Kirby, Clare O'Donnell, Dorothy J Radford, Leeanne E Grigg, David S Celermajer
OBJECTIVE: Eisenmenger syndrome (ES) is a severe form of pulmonary hypertension in adults with congenital heart disease (CHD) and has a poor prognosis. We aimed to understand factors associated with survival in ES and particularly to assess the potential benefits of advanced pulmonary vasodilator therapy (AT). METHODS: From January 2004, when AT became generally available for patients with ES, we followed 253 ES adults from 12 adult congenital heart disease centres across Australia and New Zealand...
August 9, 2017: Heart: Official Journal of the British Cardiac Society
https://www.readbyqxmd.com/read/28782712/effects-of-fasudil-on-pulmonary-hypertension-in-clinical-practice
#9
REVIEW
Yiqing Zhang, Shangjie Wu
Pulmonary hypertension (PH) is a pathophysiologic disorder that may involve multiple clinical conditions and can complicate the majority of cardiovascular and respiratory diseases. The presence of PH is associated with worse outcomes, but the efficacy of current therapy is still unsatisfactory. Because Rho-kinase (ROCK) plays an important role in the pathogenesis of PH, the ROCK inhibitor fasudil is expected to contribute to PH treatment. In animal models of PH, fasudil reduced pulmonary artery pressure (PAP) and improved survival...
August 4, 2017: Pulmonary Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/28779766/the-discovery-of-macitentan-a-standard-medicinal-chemistry-program
#10
Martin H Bolli
A plethora of properties are typically studied during a medicinal chemistry program and many of these parameters may shape the cascade of compound selection. Given the task to discover a molecule with a profile superior to that of the dual endothelin receptor antagonist bosentan, we tailored our compound profiling cascade to the specific properties that were not optimal in bosentan, namely in vivo efficacy and safety. Contrary to conventional thinking, we therefore focused on corresponding in vivo experiments...
August 9, 2017: Chimia
https://www.readbyqxmd.com/read/28735030/effect-of-bosentan-therapy-in-persistent-pulmonary-hypertension-of-the-newborn
#11
Gunlawadee Maneenil, Anucha Thatrimontrichai, Waricha Janjindamai, Supaporn Dissaneevate
BACKGROUND: Persistent pulmonary hypertension of the newborn (PPHN) contributes to neonatal hypoxemia and is associated with a high mortality. Some PPHN patients are unresponsive to inhaled nitric oxide (iNO). Bosentan, an oral endothelin-1 receptor antagonist, reduces pulmonary vascular resistance and hence may play a role in the treatment of PPHN. METHODS: A retrospective medical records review was performed in newborns who received oral bosentan as an adjunctive therapy for treatment of PPHN between January 2013 and February 2016 at the neonatal intensive care unit of Songklanagarind Hospital...
July 11, 2017: Pediatrics and Neonatology
https://www.readbyqxmd.com/read/28724039/treatment-of-digital-ulcers-in-systemic-sclerosis-case-series-study-of-thirteen-patients-and-discussion-on-outcome
#12
Yahia Abuowda, Raquel Sousa Almeida, Ana Alves Oliveira, Petra Pego, Cristina Santos, João Matos-Costa
Introduction: In systemic sclerosis (SSc), digital ulcers (DU) are debilitating and recurrent. They are markers of prognosis and are associated with disability and mortality. Treatment strategies have been developed to block the proposed mechanisms of this complication. Objective: Clinical description of a population of SSc patients with DU, treatment, complications and outcome. Method: Analysis of 48 SSc patients meeting 2013 ACR-EULAR criteria, followed between 1999-2015; 13 patients had DU...
May 2017: Revista da Associação Médica Brasileira
https://www.readbyqxmd.com/read/28707522/the-effect-of-endothelin-receptor-antagonists-in-the-endotoxin-induced-uveitis-rabbit-model
#13
Emine Esra Karaca, Feyzahan Uzun, Ergin Dileköz, Gökçe Sevim Öztürk Fincan, Sevim Ercan, Oğuz Kul, Emin Ümit Bağrıaçık, Meral Or
PURPOSE: To investigate the effect of Bosentan (non-selective endothelin receptor antagonist) and BQ123 (ETA receptor antagonist) on intraocular inflammation in an endotoxin-induced uveitis (EIU) rabbit model METHODS: Uveitis was induced by intravitreal injection of lipopolysaccharide (LPS). The animals were divided into 7 groups and there were 6 rabbits in each group (saline, saline and ethanol, Bosentan, BQ123, Lipopolysaccharide(LPS), Bosentan and LPS, BQ123 and LPS injected groups)...
July 14, 2017: Cutaneous and Ocular Toxicology
https://www.readbyqxmd.com/read/28660556/the-effect-of-endothelin-receptor-antagonists-in-patients-with-eisenmenger-syndrome-a-systematic-review
#14
REVIEW
Abdelrahman Elshafay, Duy Hieu Truong, Mohamed M AboElnas, Hossam Idrees, Hatem G Metwali, Nguyen Lam Vuong, Omar Ahmed Saad, Kenji Hirayama, Nguyen Tien Huy
INTRODUCTION: The efficacy of endothelin receptor antagonists (ERAs) in the management of Eisenmenger syndrome (ES) remains controversial. The aim of this study is to systemically review the safety and effects of ERAs in improving the quality of life and basic cardiac functions of these patients. METHODS: Twelve databases were searched, including PubMed, Web of Science, Scopus, Virtual Health Library, World Health Organization (WHO) Global Health Library, Google Scholar, POPLINE, Systems for Information of Grey Literature in Europe, New York Academy of Medicine, ClinicalTrials...
June 28, 2017: American Journal of Cardiovascular Drugs: Drugs, Devices, and Other Interventions
https://www.readbyqxmd.com/read/28655665/effect-of-amphiphilic-graft-co-polymer-carrier-on-physical-stability-of-bosentan-nanocomposite-assessment-of-solubility-dissolution-and-bioavailability
#15
Prakash N Kendre, Pravin D Chaudhari
Bosentan is a dual endothelin receptor antagonist used in the treatment of pulmonary arterial hypertension (PAH). But the solubility and bioavailability of this drug are poor, which has restricted the design and development of dosage forms for efficient and successful therapy. The present study was carried out to develop nanocomposites using an amphiphilic graft co-polymer (Soluplus®) as a carrier to enhance the solubility and bioavailability of bosentan. The graft co-polymer-based nanocomposite formulation was prepared using the single-emulsion technique...
June 24, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28640077/improvement-of-peripheral-artery-disease-with-sildenafil-and-bosentan-combined-therapy-in-a-patient-with-limited-cutaneous-systemic-sclerosis-a-case-report
#16
Loukman Omarjee, Cedric Fontaine, Guillaume Mahe, Vincent Jaquinandi
RATIONALE: Sildenafil, a phosphodiesterase-5-inhibitor and Bosentan, an endothelin-1-receptor antagonist combined therapy could have beneficial effect in systemic sclerosis (SSc) patients with peripheral artery disease. PATIENT CONCERNS: We report a case of a 48-year-old Black woman, who developed severe left limb claudication and walking limitation following a left femoropopliteal bypass occlusion in 2014. She was a heavy smoker and had a history of right middle cerebral artery ischemic stroke and bilateral Raynaud phenomenon...
June 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/28628863/simultaneous-quantification-of-endothelin-receptor-antagonists-and-phosphodiesterase-5-inhibitors-currently-used-in-pulmonary-arterial-hypertension
#17
Yeliz Enderle, Lukas Witt, Heinrike Wilkens, Ekkehard Grünig, Walter E Haefeli, Jürgen Burhenne
Combination treatment with endothelin receptor antagonists (ERA) and phosphodiesterase 5 inhibitors (PDE5I) improved efficacy of pulmonary arterial hypertension (PAH) therapy. However, drug-drug interactions, variable exposure, non-adherence can influence plasma levels. For these reasons, drug quantification may be advantageous particularly in patients with poor treatment responses. We developed, validated, and applied an assay for the simultaneous quantification of ambrisentan, bosentan, macitentan, sildenafil, and tadalafil as well as their main (and partly active) metabolites in human plasma...
September 5, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28618763/comparison-of-endothelin-and-nitric-oxide-synthase-blockers-on-hemorheological-parameters-in-endotoxemic-rats
#18
Neslihan H Dikmenoğlu Falkmarken, Okan Arihan, Alper B Iskit
BACKGROUND/AIM: Septic shock is an important health problem that vastly alters cardiovascular and hemodynamic status. Increased production of nitric oxide (NO) and endothelin is a counterpart of this endotoxemic state. This study was conducted to test the hypothesis that nonselective NO synthesis blocker (L-NAME), inducible NO synthesis blocker (L-canavanine), or endothelin receptor antagonist (bosentan) will reverse the effects of sepsis on hemorheological parameters. MATERIALS AND METHODS: Forty-eight male Sprague-Dawley rats were used in 8 groups: saline (control), endotoxin, bosentan, L-NAME, L-canavanine, endotoxin + bosentan, endotoxin + L-NAME, and endotoxin + L-canavanine...
June 12, 2017: Turkish Journal of Medical Sciences
https://www.readbyqxmd.com/read/28616089/severe-pulmonary-arterial-hypertension-associated-with-congenital-cardiac-shunts-evolution-under-specific-treatment
#19
R I Negoi, I Ghiorghiu, F Filipoiu, M Hostiuc, I Negoi, C Ginghina
Objective: The aim of this study was to compare the effects of Sildenafil, Bosentan and combined therapy in patients with congenital cardiac shunts associated pulmonary artery hypertension (CCS-PAH). Design: Prospective observational study (February 2011 - January 2014) with a historical control group (January 2009 - January 2011). Setting: "CC Iliescu" Institute for Emergency Cardiovascular Diseases of Bucharest, a tertiary university-affiliated center. Patients: All cases with CCS-PAH. Interventions: Specific vasodilatory therapy: Sildenafil, Bosentan or combined therapy...
April 2017: Journal of Medicine and Life
https://www.readbyqxmd.com/read/28597771/first-in-child-use-of-the-oral-selective-prostacyclin-ip-receptor-agonist-selexipag-in-pulmonary-arterial-hypertension
#20
Lianne M Geerdink, Harald Bertram, Georg Hansmann
Pulmonary arterial hypertension (PAH) is a complex disease with a poor prognosis. Selexipag is a selective prostacyclin receptor agonist with vasodilatory, anti-proliferative, anti-inflammatory, and pro-angiogenic properties. However, no clinical data on its therapeutic use in children with PAH are currently available. Here, we report the case of a 12-year-old girl who presented in World Health Organization (WHO) functional class III and right ventricular (RV) failure with recurrent syncope, dizziness, and progressive fatigue for two years...
April 2017: Pulmonary Circulation
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