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Bosentan

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https://www.readbyqxmd.com/read/28237536/early-experience-of-macitentan-for-pulmonary-arterial-hypertension-in-adult-congenital-heart-disease
#1
S Herbert, W Gin-Sing, L Howard, R M R Tulloh
BACKGROUND: Endothelin receptor antagonists (ERA) have been recognised as effective therapy for pulmonary arterial hypertension in congenital heart disease (CHD-PH), and Eisenmenger syndrome (ES) since the Breathe 5 study. A new dual receptor antagonist - Macitentan - is currently undergoing trials to determine its efficacy in simple ES. To date there is little information on this therapy in CHD and we report our first experience, some with more complex diseases. METHODS: Data was collected prospectively from September 2014...
February 6, 2017: Heart, Lung & Circulation
https://www.readbyqxmd.com/read/28223322/eta-receptors-blockade-by-activating-etb-receptors-increases-vascular-permeability-and-induces-exaggerated-fluid-retention
#2
Magali Vercauteren, Frederic Trensz, Anne Pasquali, Christophe Cattaneo, Daniel S Strasser, Patrick Hess, Marc Iglarz, Martine Clozel
Endothelin receptor antagonists have been associated with fluid retention. It has been suggested that, of the two endothelin receptor subtypes, ETB receptors should not be blocked, because of their involvement in natriuresis and diuresis. Surprisingly, clinical data suggest that ETA-selective antagonists pose a greater risk of fluid overload than dual antagonists. The purpose of this study was to evaluate the contribution of each endothelin receptor to fluid retention and vascular permeability in rats. Sitaxentan and ambrisentan as ETA-selective antagonists, bosentan and macitentan as dual antagonists were used as representatives of each class, respectively...
February 21, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28214014/controlling-the-digital-ulcerative-disease-in-systemic-sclerosis-is-associated-with-improved-hand-function
#3
Luc Mouthon, Patrick H Carpentier, Catherine Lok, Pierre Clerson, Virginie Gressin, Eric Hachulla, Alice Bérezné, Elisabeth Diot, Aurélie Khau Van Kien, Patrick Jego, Christian Agard, Anne-Bénédicte Duval-Modeste, Agnès Sparsa, Eve Puzenat, Marie-Aleth Richard
OBJECTIVES: Ischemic digital ulcers (DU) represent a major complication of systemic sclerosis (SSc). We investigated the impact of controlling the ulcerative disease on disability, pain, and quality of life in SSc patients receiving bosentan. METHODS: ECLIPSE (Study AC-052-517) is a 2-year prospective, multicenter, and observational study. Patients with SSc who experienced at least 1 DU in the previous year and received bosentan were included between October 2009 and March 2011...
January 13, 2017: Seminars in Arthritis and Rheumatism
https://www.readbyqxmd.com/read/28213957/a-bosentan-pharmacokinetic-study-to-investigate-dosing-regimens-in-paediatric-patients-with-pulmonary-arterial-hypertension-future-3
#4
R M F Berger, M Gehin, M Beghetti, D Ivy, A Kusic-Pajic, P Cornelisse, S Grill, D Bonnet
AIM: To investigate whether increasing bosentan dosing frequency from 2 mg/kg twice daily (b.i.d.) to 2 mg/kg three times daily (t.i.d.) in children with pulmonary arterial hypertension (PAH) (from ≥3 months to <12 years of age) would increase exposure. METHODS: An open-label, prospective, randomised, multicentre, multiple-dose, Phase 3 study was conducted. Patients (n = 64) were randomised 1:1 to receive oral doses of bosentan of 2 mg/kg b.i...
February 18, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28173639/bosentan-and-rifampin-interactions-modulate-influx-transporter-and-cytochrome-p450-expression-and-activities-in-primary-human-hepatocytes
#5
Kyoung-Moon Han, Sun-Young Ahn, Hyewon Seo, Jaesuk Yun, Hye Jin Cha, Ji-Soon Shin, Young-Hoon Kim, Hyungsoo Kim, Hye-Kyung Park, Yong-Moon Lee
The incidence of polypharmacy-which can result in drug-drug interactions-has increased in recent years. Drug-metabolizing enzymes and drug transporters are important polypharmacy modulators. In this study, the effects of bosentan and rifampin on the expression and activities of organic anion-transporting peptide (OATP) and cytochrome P450 (CYP450) 2C9 and CYP3A4 were investigated in vitro. HEK293 cells and primary human hepatocytes overexpressing the target genes were treated with bosentan and various concentrations of rifampin, which decreased the uptake activities of OATP transporters in a dose-dependent manner...
February 6, 2017: Biomolecules & Therapeutics
https://www.readbyqxmd.com/read/28156176/respirable-controlled-release-polymeric-colloid-rcrpc-of-bosentan-for-the-management-of-pulmonary-hypertension-in-vitro-aerosolization-histological-examination-and-in-vivo-pulmonary-absorption
#6
COMPARATIVE STUDY
Lydia A Hanna, Emad B Basalious, Omaima N ELGazayerly
Bosentan is an endothelin receptor antagonist (ERA) prescribed for patients with pulmonary arterial hypertension (PAH). The oral delivery of bosentan possesses several drawbacks such as low bioavailability (about 50%), short duration of action, frequent administration, hepatotoxicity and systemic hypotension. The pulmonary administration would circumvent the pre-systemic metabolism thus improving the bioavailability and avoids the systemic adverse effects of oral bosentan. However, the short duration of action and the frequent administration are the major drawbacks of inhalation therapy...
November 2016: Drug Delivery
https://www.readbyqxmd.com/read/28138822/drug-reaction-with-eosinophilia-and-systemic-symptoms-dress-syndrome-and-the-rheumatologist
#7
REVIEW
Marwan H Adwan
PURPOSE OF THE REVIEW: The purpose of the review is to summarise the various drugs used in rheumatology practice implicated in the causation of DRESS syndrome. RECENT FINDINGS: The most commonly reported drugs are allopurinol, sulfasalazine and minocycline, which pose a very high risk for DRESS syndrome development, followed by strontium ranelate and dapsone. Other, less commonly reported, drugs include leflunomide, hydroxychloroquine, non-steroidal anti-inflammatory drugs, febuxostat, bosentan and solcitinib...
January 2017: Current Rheumatology Reports
https://www.readbyqxmd.com/read/28134077/dual-endothelin-receptor-antagonists-contrast-the-effects-induced-by-endothelin-1-on-cultured-human-microvascular-endothelial-cells
#8
Stefano Soldano, Sabrina Paolino, Carmen Pizzorni, Amelia Chiara Trombetta, Paola Montagna, Renata Brizzolara, Claudio Corallo, Nicola Giordano, Alberto Sulli, Maurizio Cutolo
OBJECTIVES: To evaluate the ability of dual endothelin (ET) receptor antagonists (ETA/ETB -ETA/BRAs) to contrast the ET-1-induced effects on cultured human microvascular endothelial cells (HMVECs). METHODS: Some cultured HMVECs were untreated, or treated with ET-1 (100nM) or transforming growth factor β1 (TGFβ1, 10ng/mL) alone for 6 days, in order to induce the endothelial-to-mesenchymal transition (EndoMT). Other cultured HMVECs were pre-treated for 1hr with ETA/BRAs bosentan (10μM) or macitentan (1μM, 10μM) before the stimulation with ET-1 for 6 days...
January 27, 2017: Clinical and Experimental Rheumatology
https://www.readbyqxmd.com/read/28121194/in-vitro-characterization-studies-of-self-microemulsified-bosentan-systems
#9
Harini Chowdary Vadlamudi, Prasanna Raju Yalavarthi, M V Basaveswara Rao, Arun Rasheed, Tejeswari N
CONTEXT: Bosentan is a poorly soluble drug and pose challenges in design delivery systems. OBJECTIVE: To enhance the solubility, dissolution and shelf-life of bosentan by formulating it as S-SMEDDS capsules. MATERIALS AND METHODS: Solubility of bosentan was tested in various liquid vehicles such as oils (rice bran and sunflower), surfactants (span 20 and tween 80) and co-surfactants (PEG 400 and propylene glycol) and microemulsions were developed...
January 25, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28119496/treatment-of-pulmonary-arterial-hypertension-using-initial-combination-therapy-of-bosentan-and-iloprost
#10
Xinpeng Han, Yuhai Zhang, Liang Dong, Liying Fang, Yaqin Chai, Mengjie Niu, Yongping Yu, Lingli Liu, Xuemin Yang, Shuoyao Qu, Shengqing Li
BACKGROUND: Monotherapy and sequential combination therapy have been widely used in the treatment of pulmonary arterial hypertension (PAH). There is limited evidence for initial combination therapy in patients with PAH, particularly those with World Health Organization (WHO) functional class III or IV. METHODS: Twenty-seven consecutive treatment-naive PAH subjects with WHO functional class III or IV PAH were randomized into 3 groups with a 1:1:1 ratio: a combination therapy group with 125 mg of bosentan twice daily plus 10 μg of iloprost 4-6 times/d; a bosentan monotherapy group with 125 mg of bosentan twice daily; and a iloprost monotherapy group with 10 μg of iloprost 4-6 times/d...
January 24, 2017: Respiratory Care
https://www.readbyqxmd.com/read/28078552/pediatric-development-of-bosentan-facilitated-by-modeling-and-simulation
#11
Jochen Zisowsky, Martine Géhin, Andjela Kusic-Pajic, Andreas Krause, Maurice Beghetti, Jasper Dingemanse
BACKGROUND: Bosentan is approved for use in adult patients with pulmonary arterial hypertension. The primary aim of the pharmacokinetic modeling was the provision of a systematic guidance for study design and enhanced understanding of pharmacokinetics across the entire pediatric age range. METHODS: A physiologically based pharmacokinetic model was developed for the pediatric population; starting from an adult model, the effects of body weight, age, and maturation of relevant metabolizing enzymes were incorporated to extrapolate the pharmacokinetics to children...
January 11, 2017: Paediatric Drugs
https://www.readbyqxmd.com/read/28053559/systemic-lupus-erythematosus-and-pulmonary-arterial-hypertension-links-risks-and-management-strategies
#12
REVIEW
Konstantinos Tselios, Dafna D Gladman, Murray B Urowitz
Systemic lupus erythematosus (SLE) is characterized by the second highest prevalence of pulmonary arterial hypertension (PAH), after systemic sclerosis, among the connective tissue diseases. SLE-associated PAH is hemodynamically defined by increased mean pulmonary artery pressure at rest (≥25 mmHg) with normal pulmonary capillary wedge pressure (≤15 mmHg) and increased pulmonary vascular resistance. Estimated prevalence ranges from 0.5% to 17.5% depending on the diagnostic method used and the threshold of right ventricular systolic pressure in studies using transthoracic echocardiogram...
2017: Open Access Rheumatology: Research and Reviews
https://www.readbyqxmd.com/read/28030574/endothelin-regulates-porphyromonas-gingivalis-induced-production-of-inflammatory-cytokines
#13
Ga-Yeon Son, Eun-Jung Bak, Ji-Hye Kim, Dong Eun Lee, Si-Mook Kang, So Yun Lee, Lin Choi, Ji Su Sun, Seul Ki Kim, Wonse Park, Baek Il Kim, Yun-Jung Yoo, Inik Chang, Dong Min Shin
Periodontitis is a very common oral inflammatory disease that results in the destruction of supporting connective and osseous tissues of the teeth. Although the exact etiology is still unclear, Gram-negative bacteria, especially Porphyromonas gingivalis in subgingival pockets are thought to be one of the major etiologic agents of periodontitis. Endothelin (ET) is a family of three 21-amino acid peptides, ET-1, -2, and -3, that activate G protein-coupled receptors, ETA and ETB. Endothelin is involved in the occurrence and progression of various inflammatory diseases...
2016: PloS One
https://www.readbyqxmd.com/read/28018840/hand-impairment-in-systemic-sclerosis-various-manifestations-and-currently-available-treatment
#14
Amber Young, Rajaie Namas, Carole Dodge, Dinesh Khanna
Systemic sclerosis (SSc) is an autoimmune disease initially recognized by hand involvement due to characteristic Raynaud's phenomenon (RP), puffy hands, skin thickening, and contractures resembling claw deformities. SSc contributes to hand impairment through inflammatory arthritis, joint contractures, tendon friction rubs (TFRs), RP, digital ulcers (DU), puffy hands, skin sclerosis, acro-osteolysis, and calcinosis. These manifestations, which often co-exist, can contribute to difficulty with occupational activities and activities of daily living (ADL), which can result in impaired quality of life...
September 2016: Current Treatment Options in Rheumatology
https://www.readbyqxmd.com/read/28008226/preparation-and-physicochemical-characterization-of-spray-dried-and-jet-milled-microparticles-containing-bosentan-hydrate-for-dry-powder-inhalation-aerosols
#15
Hyo-Jung Lee, Ji-Hyun Kang, Hong-Goo Lee, Dong-Wook Kim, Yun-Seok Rhee, Ju-Young Kim, Eun-Seok Park, Chun-Woong Park
The objectives of this study were to prepare bosentan hydrate (BST) microparticles as dry powder inhalations (DPIs) via spray drying and jet milling under various parameters, to comprehensively characterize the physicochemical properties of the BST hydrate microparticles, and to evaluate the aerosol dispersion performance and dissolution behavior as DPIs. The BST microparticles were successfully prepared for DPIs by spray drying from feeding solution concentrations of 1%, 3%, and 5% (w/v) and by jet milling at grinding pressures of 2, 3, and 4 MPa...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27994906/swift-and-complete-healing-of-digital-ulcers-after-macitentan-treatment
#16
Emilio Giner Serret
Digital ulcers are a burdensome and painful condition with sparse options of treatment. We report the case of a 78-year-old female patient with limited cutaneous systemic sclerosis that sequentially developed digital ulcers. After the appearance of digital ulcers in the soles of her feet she was successfully treated with bosentan. The report of two new digital ulcers in her hands 9 months later alongside with elevated transaminase levels led to a switch to macitentan treatment. A swift and complete healing of both digital ulcers was observed after 3 months, with the restoration of normal biochemical values...
2016: Case Reports in Rheumatology
https://www.readbyqxmd.com/read/27986807/effects-of-4-multitargeted-receptor-tyrosine-kinase-inhibitors-on-regional-hemodynamics-in-conscious-freely-moving-rats
#17
Joanne J Carter, Laurice V Fretwell, Jeanette Woolard
VEGF inhibitors, including receptor tyrosine kinase inhibitors, are used as adjunct therapies in a number of cancer treatments. An emerging issue with these drugs is that most cause hypertension. To gain insight into the physiological mechanisms involved, we evaluated their regional hemodynamic effects in conscious rats. Male Sprague Dawley rats (350-450 g) were chronically implanted with pulsed Doppler flow probes (renal and mesenteric arteries, and the descending abdominal aorta) and catheters (jugular vein, peritoneal cavity, and distal abdominal aorta)...
December 16, 2016: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/27971684/a-budget-impact-analysis-of-the-introduction-of-generic-bosentan-for-the-treatment-of-pulmonary-arterial-hypertension-in-greece
#18
K Athanasakis, F Tarantilis, C Tsakalogiannis, M Ollandezos, J Kyriopoulos
No abstract text is available yet for this article.
November 2016: Value in Health: the Journal of the International Society for Pharmacoeconomics and Outcomes Research
https://www.readbyqxmd.com/read/27912207/clinical-adverse-effects-of-endothelin-receptor-antagonists-insights-from-the-meta-analysis-of-4894-patients-from-24-randomized-double-blind-placebo-controlled-clinical-trials
#19
Anhua Wei, Zhichun Gu, Juan Li, Xiaoyan Liu, Xiaofan Wu, Yi Han, Jun Pu
BACKGROUND: Evidence of the clinical safety of endothelin receptor antagonists (ERAs) is limited and derived mainly from individual trials; therefore, we conducted a meta-analysis. METHODS AND RESULTS: After systematic searches of the Medline, Embase, and Cochrane Library databases and the ClinicalTrials.gov website, randomized controlled trials with patients receiving ERAs (bosentan, macitentan, or ambrisentan) in at least 1 treatment group were included. All reported adverse events of ERAs were evaluated...
October 26, 2016: Journal of the American Heart Association
https://www.readbyqxmd.com/read/27906839/endothelin-contributes-to-the-blood-pressure-rise-triggered-by-hypoxia-in-severe-obstructive-sleep-apnea
#20
Christophe Janssen, Atul Pathak, Guido Grassi, Philippe van de Borne
BACKGROUND: Obstructive sleep apnea (OSA) is strongly correlated with an increased risk of systemic hypertension. However, the link between systemic hypertension and nocturnal apneas remains incompletely understood. Animal studies suggest an implication of the endothelin system. The aim of the present study is to determine if endogenous endothelin plays a role in the increase in blood pressure observed during hypoxic episodes in OSA patients, in addition to peripheral chemoreflex and neural sympathetic activation...
January 2017: Journal of Hypertension
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