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https://www.readbyqxmd.com/read/29764826/systemic-sclerosis-severe-pulmonary-arterial-hypertension-and-pericardial-effusion-at-diagnosis
#1
Patricia Moniz, Daniel Rei, Joana Rodrigues, Arturo Botella
A 51-year-old female patient with a recent hospital admission reported to the emergency room (ER) with progressive worsening of fatigue, dyspnoea and chest discomfort. She had been recently admitted and discharged with the diagnosis of pericarditis and medicated with non-steroidal anti-inflammatory drugs and diuretics. She returned to the ER with persisting symptoms. Echocardiography was repeated and showed signs of elevated right ventricular systolic pressure and a slightly increased moderate/severe pericardial effusion without signs of cardiac tamponade...
May 14, 2018: BMJ Case Reports
https://www.readbyqxmd.com/read/29761207/omics-based-responses-induced-by-bosentan-in-human-hepatoma-heparg-cell-cultures
#2
Robim M Rodrigues, Laxmikanth Kollipara, Umesh Chaudhari, Agapios Sachinidis, René P Zahedi, Albert Sickmann, Annette Kopp-Schneider, Xiaoqi Jiang, Hector Keun, Jan Hengstler, Marlies Oorts, Pieter Annaert, Eef Hoeben, Eva Gijbels, Joery De Kock, Tamara Vanhaecke, Vera Rogiers, Mathieu Vinken
Bosentan is well known to induce cholestatic liver toxicity in humans. The present study was set up to characterize the hepatotoxic effects of this drug at the transcriptomic, proteomic, and metabolomic levels. For this purpose, human hepatoma-derived HepaRG cells were exposed to a number of concentrations of bosentan during different periods of time. Bosentan was found to functionally and transcriptionally suppress the bile salt export pump as well as to alter bile acid levels. Pathway analysis of both transcriptomics and proteomics data identified cholestasis as a major toxicological event...
May 14, 2018: Archives of Toxicology
https://www.readbyqxmd.com/read/29750649/cardiac-examination-in-children-with-laron-syndrome-undergoing-mecasermin-therapy
#3
Nurdan Erol, Metin Yıldız, Ayla Güven, Ayse Yıldırım
BACKGROUND: Laron syndrome (LS), which can be defined as primary growth hormone resistance or insensitivity, is a rare genetic disease inherited by an autosomal recessive trait. Although it is undistinguishable from growth hormone deficiency, LS has high levels of growth hormone, but insulin-like growth factor (IGF-1) cannot be synthesized. Mecasermin treatment is the only option for the patients who suffer from LS. This study aims to research cardiac findings of children with LS, who receive treatment with mecasermin...
May 11, 2018: Journal of Pediatric Endocrinology & Metabolism: JPEM
https://www.readbyqxmd.com/read/29746136/relative-activity-factor-raf-based-scaling-of-uptake-clearance-mediated-by-organic-anion-transporting-polypeptide-oatp-1b1-and-oatp1b3-in-human-hepatocytes
#4
Saki Izumi, Yoshitane Nozaki, Hiroyuki Kusuhara, Koichiro Hotta, Toshiki Mochizuki, Takafumi Komori, Kazuya Maeda, Yuichi Sugiyama
In vitro-in vivo extrapolation based on uptake clearance determined in human hepatocytes has been used to predict in vivo hepatic clearance of organic anion transporting polypeptide (OATP) substrates. This study evaluated the relative activity factor (RAF) approach to extrapolate active uptake clearance in transporter-transfected cell systems (CLuptake ) to that in human hepatocyte suspensions (PSinf,act ). RAF values for OATP1B1 and OATP1B3 were determined in two batches of cryopreserved human hepatocytes using estrone-3-sulfate and cholecystokinin octapeptide as reference substrates, respectively...
May 10, 2018: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/29720472/predicting-human-clearance-of-oatp-substrates-using-cynomolgus-monkey-in-vitro-in-vivo-scaling-of-hepatic-uptake-clearance
#5
Tom de Bruyn, Ayse Ufuk, Carina Cantrill, Rachel E Kosa, Yi-An Bi, Mark Niosi, Sweta Modi, A David Rodrigues, Larry M Tremaine, Manthena Vs Varma, Aleksandra Galetin, J Brian Houston
This work explores the utility of the cynomolgus monkey as a preclinical model to predict hepatic uptake clearance mediated by organic anion transporting polypeptide (OATP) transporters. Nine OATP substrates (rosuvastatin, pravastatin, repaglinide, fexofenadine, cerivastatin, telmisartan, pitavastatin, bosentan and valsartan) were investigated in plated cynomolgus monkey and human hepatocytes. Total uptake clearance and passive diffusion were measured in vitro from initial rates in the absence and presence of the OATP inhibitor rifamycin SV, respectively...
May 2, 2018: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/29719121/a-focus-on-macitentan-in-the-treatment-of-pulmonary-arterial-hypertension
#6
Martin Bedan, Daniela Grimm, Markus Wehland, Ulf Simonsen, Manfred Infanger, Marcus Krüger
The approval of macitentan has increased the number of pharmacological treatments of pulmonary arterial hypertension (PAH). Here, we review the effect on PAH of macitentan compared to other endothelin receptor antagonists (ERAs). Drugs targeting the endothelin (ET) pathway include the selective ETA receptor antagonist ambrisentan, the ETA /ETB receptor antagonists bosentan and macitentan which were recently approved for PAH treatment. This article is protected by copyright. All rights reserved.
May 2, 2018: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/29692255/juvenile-scleroderma-what-has-changed-in-the-meantime
#7
Amra Adrovic, Sezgin Sahin, Kenan Barut, Ozgur Kasapcopur
BACKGROUND: Juvenile scleroderma is a rarely seen chronic connective tissue disorder characterized by stiffening of the skin. The frequency of the disease was reported as one per million. According to organ involvement, the disease is divided into two main forms: systemic and localized scleroderma. OBJECTIVES: Since it is uncommon in children, many aspects of the disease remain discussable. With this review, we aimed to revise recent findings and new developments in this rare condition...
April 22, 2018: Current Rheumatology Reviews
https://www.readbyqxmd.com/read/29692180/a-validated-uplc-ms-ms-method-for-flibanserin-in-plasma-and-its-pharmacokinetic-interaction-with-bosentan-in-rats
#8
Muzaffar Iqbal, Essam Ezzeldin, Naser L Rezk, Amal A Bajrai, Khalid A Al-Rashood
AIM: The purpose of this study was development, validation and application of ultra-performance liquid chromatography (UPLC)-ESI-MS/MS method for quantitation of flibanserin in plasma samples. METHOD & RESULTS: After extraction of analyte from plasma by diethyl ether, separation was performed on UPLC C18 column using mobile phase composition of 10 mM ammonium formate-acetonitrile (30:70, v/v) by isocratic elution of 0.3 ml/min. The multiple reaction monitoring transitions of m/z 391...
April 25, 2018: Bioanalysis
https://www.readbyqxmd.com/read/29602480/-tunnelled-central-venous-catheter-infection-during-treatment-with-epoprostenol
#9
M Koszutski, M Faure, A Guillaumot, E Gomez, M Mercy, F Chabot, A Chaouat
INTRODUCTION: Pulmonary arterial hypertension is a pulmonary vascular disease with a poor prognosis. Continuous intravenous treatment with prostacyclin analogues requires the placement of a tunnelled catheter. The occurrence of catheter-related infections in this context is unusual due to the alkaline pH of the prostacyclin analogue solutions. OBSERVATION: A 50-year-old patient with inherited pulmonary artery hypertension, treated with bosentan, sildenafil and epoprostenol, experienced generalized malaise associated with a weight loss of 9kg over a 12-month period without evidence of a source of infection or malignancy...
March 28, 2018: Revue des Maladies Respiratoires
https://www.readbyqxmd.com/read/29557420/bosentan-inducing-autoimmune-hepatitis-in-a-patient-with-idiopathic-pulmonary-arterial-hypertension
#10
Alexandre de Araujo, Augusto Mantovani, Carlos Thadeu Schmidt Cerski, Antonio Barros Lopes, Luiza Cristina Bortoncello, Marcelo Basso Gazzana, Hugo Cheinquer
A 41-year-old woman diagnosed with idiopathic pulmonary hypertension presented symptoms despite the use of vasodilators, requiring treatment with bosentan. Previously, the patient had no signs of autoimmunity and had normal liver function. After three years of bosentan use, aminotransferase levels increased, without improvement after bosentan suspension, leading to complementary investigation. The diagnosis of autoimmune hepatitis was confirmed by biopsy, already in the stage of cirrhosis. In conclusion, in case of aminotransferase levels that remain persistently elevated, despite the reduction in doses and/or suspension of bosentan, autoimmune hepatitis must be investigated and treated urgently due to possibly rapid progression to cirrhosis...
March 2018: Journal of Gastrointestinal and Liver Diseases: JGLD
https://www.readbyqxmd.com/read/29549081/correction-to-a-study-on-pharmacokinetics-of-bosentan-with-systems-modeling-part-2-prospectively-predicting-systemic-and-liver-exposure-in-healthy-subjects
#11
(no author information available yet)
No abstract text is available yet for this article.
April 2018: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/29549080/correction-to-a-study-on-pharmacokinetics-of-bosentan-with-systems-modeling-part-1-translating-systemic-plasma-concentration-to-liver-exposure-in-healthy-subjects
#12
(no author information available yet)
No abstract text is available yet for this article.
April 2018: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/29546917/-the-role-of-pulmonary-hypertension-on-bronchopulmonary-dysplasia
#13
D Valenzuela, F Moya, M Luco, J L Tapia
50 years ago, Northway described Broncopulmonary Dysplasia (BPD) in preterm infants exposed to mechanical ventilation. Since then, their survival has increased, nevertheless a "new BPD" has appeared and its incidence has not diminished. One of the characteristics of this pathology is the the abnormal vascular remodeling, which in its most severe expression is known as Pulmonary Hyper tension (PH); with an incidence of 17% in patients with BPD, which is proportional to the severity of the disease (33% in severe BPD), and as mortality factor (up to 48% 2-year mortality in PH-BPD)...
December 2017: Revista Chilena de Pediatría
https://www.readbyqxmd.com/read/29517668/the-efficiency-of-endothelin-receptor-antagonist-bosentan-for-pulmonary-arterial-hypertension-associated-with-congenital-heart-disease-a-systematic-review-and-meta-analysis
#14
REVIEW
Hong-Yu Kuang, Yu-Hao Wu, Qi-Jian Yi, Jie Tian, Chun Wu, We Nian Shou, Tie-Wei Lu
BACKGROUND: Oral bosentan has been widely applied in pulmonary arterial hypertension associated with congenital heart disease (PAH-CHD). A systemic review and meta-analysis was conducted for a therapeutic evaluation of oral bosentan in both adult and pediatric patients with PAH-CHD. The acute responses and a long-term effect were respectively assessed in a comparison with baseline characteristics, and the improvement of exercise tolerance was analyzed. METHODS: PubMed, Medline, Embase, and Cochrane Central Register of clinical controlled trails or observational studies have been searched for a recording of bosentan effects on the PAH-CHD participants...
March 2018: Medicine (Baltimore)
https://www.readbyqxmd.com/read/29510172/the-role-of-lactose-carrier-on-the-powder-behavior-and-aerodynamic-performance-of-bosentan-microparticles-for-dry-powder-inhalation
#15
Hyo-Jung Lee, Hong-Goo Lee, Yong-Bin Kwon, Ju-Young Kim, Yun-Seok Rhee, Jinmann Chon, Eun-Soek Park, Dong-Wook Kim, Chun-Woong Park
In this study, we prepared carrier-based formulations for dry powder inhalers by mixing bosentan microparticles with carrier, prepared in three separate types of lactose. Spray-dried, milled and sieved lactose resulted in formulations with various shapes, surface morphology and particle size distributions. In the spray-dried lactose, the micronized bosentan particles were trapped and strongly interlocked in the rugged surface of spray-dried lactose, whereas in the milled and sieved lactose they exhibited lower binding affinity onto the smooth surface of carrier...
May 30, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29475833/physiologically-based-pharmacokinetic-modeling-of-bosentan-identifies-the-saturable-hepatic-uptake-as-a-major-contributor-to-its-nonlinear-pharmacokinetics
#16
Masanobu Sato, Kota Toshimoto, Atsuko Tomaru, Takashi Yoshikado, Yuta Tanaka, Akihiro Hisaka, Wooin Lee, Yuichi Sugiyama
Bosentan is a substrate of hepatic uptake transporter organic anion-transporting polypeptides (OATPs), and undergoes extensive hepatic metabolism by cytochrome P450 (P450), namely, CYP3A4 and CYP2C9. Several clinical investigations have reported a nonlinear relationship between bosentan doses and its systemic exposure, which likely involves the saturation of OATP-mediated uptake, P450-mediated metabolism, or both in the liver. Yet, the underlying causes for the nonlinear bosentan pharmacokinetics are not fully delineated...
May 2018: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/29467212/intravital-multiphoton-microscopy-with-fluorescent-bile-salts-in-rats-as-an-in-vivo-biomarker-for-hepatobiliary-transport-inhibition
#17
Jennifer Ryan, Ryan E Morgan, Yuan Chen, Laurie P Volak, Robert T Dunn, Kenneth W Dunn
The bile salt export pump (BSEP) is expressed at the canalicular domain of hepatocytes, where it mediates the elimination of monovalent bile salts into the bile. Inhibition of BSEP is considered a susceptibility factor for drug-induced liver injury that often goes undetected during nonclinical testing. Although in vitro assays exist for screening BSEP inhibition, a reliable and specific method for confirming Bsep inhibition in vivo would be a valuable follow up to a BSEP screening strategy, helping to put a translatable context around in vitro inhibition data, incorporating processes such as metabolism, protein binding, and other exposure properties that are lacking in most in vitro BSEP models...
May 2018: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/29455195/sildenafil-bosentan-drug-drug-interaction-a-word-of-caution-regarding-the-most-common-combination-therapy-in-children-with-advanced-pulmonary-arterial-hypertension
#18
Christian Apitz, Dietmar Schranz
No abstract text is available yet for this article.
February 16, 2018: Respiration; International Review of Thoracic Diseases
https://www.readbyqxmd.com/read/29453947/evaluation-of-the-effects-of-rp5063-a-novel-multimodal-serotonin-receptor-modulator-as-single-agent-therapy-and-co-administrated-with-sildenafil-bosentan-and-treprostinil-in-a-monocrotaline-induced-pulmonary-arterial-hypertension-rat-model
#19
Laxminarayan Bhat, Jon Hawkinson, Marc Cantillon, Dasharatha G Reddy, Seema R Bhat, Charles-E Laurent, Annie Bouchard, Marzena Biernat, Dany Salvail
Pulmonary arterial hypertension (PAH), a condition that is defined by pulmonary vasculature constriction and remodeling, involves dysfunctional signaling of the serotonin (5-HT) receptors, 5-HT2A/2B/7 . In a rat model of monocrotaline (MCT)-induced PAH, the effectiveness of RP5063 (RP), a dopamine and 5-HT receptor modulator, was evaluated as monotherapy and as an adjunct to standard PAH treatments. After a single 60 mg/kg dose of MCT, rats received vehicle (MCT+Veh; gavage twice-daily [b.i.d.]), RP (10 mg/kg; gavage b...
May 15, 2018: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29436381/subcutaneous-treprostinil-in-congenital-heart-disease-related-pulmonary-arterial-hypertension
#20
Nika Skoro-Sajer, Christian Gerges, Olga Hajnalka Balint, Dora Kohalmi, Monika Kaldararova, Iveta Simkova, Johannes Jakowitsch, Harald Gabriel, Helmut Baumgartner, Mario Gerges, Roela Sadushi-Kolici, David S Celermajer, Irene Marthe Lang
OBJECTIVE: To assess the efficacy and safety of subcutaneous treprostinil in adult patients with congenital heart disease (CHD)-associated pulmonary arterial hypertension (PAH) after 12 months of treatment. METHODS: Consecutive adult patients with CHD-PAH received subcutaneous treprostinil to maximum tolerated doses in an observational study. RESULTS: Advanced CHD-PAH patients with WHO class III or IV disease (n=32, age 40±10 years, 20 females) received treprostinil for suboptimal response to bosentan (n=12), WHO functional class IV disease (FC, n=7) or prior to bosentan approval (n=13)...
February 7, 2018: Heart: Official Journal of the British Cardiac Society
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