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https://www.readbyqxmd.com/read/29314090/development-and-validation-of-lc-ms-ms-method-for-simultaneous-determination-of-sofosbuvir-and-daclatasvir-in-human-plasma-application-to-pharmacokinetic-study
#1
Ola M Abdallah, Ahmed M Abdel-Megied, Amira S Gouda
The first simple and highly sensitive Liquid chromatography-tandem mass spectrometry (LC-MS/MS) bioanalytical method was developed and fully validated for the simultaneous determination of newly discovered antiviral drugs namely, Sofosbuvir (SOF) and Daclatasvir (DAC) in human plasma. Tadalafil (TAD) was used as internal standard (IS). SOF, DAC and TAD (IS) were extracted from plasma using liquid-liquid extraction technique with methyl tert-butyl ether. The chromatographic separation was carried out using ZorbaxSB-C18 column (4...
January 3, 2018: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/29277884/penile-glans-necrosis-developing-after-internal-pudendal-arterial-embolization-a-case-report
#2
Tae Nam Kim, Chan Ho Lee, Seung Ryong Baek, Kyung Min Lee, Sangmin Choe, Nam Cheol Park, Hyun Jun Park
Penile glans ischemia or necrosis developing after internal pudendal arterial embolization is very rare; no relevantreport has yet appeared. A 53-year-old male who visited our emergency room because of massive urethral bleedingwas diagnosed with an internal pudendal artery-urethral fistula; he underwent selective embolization of the internalpudendal artery. However, unexpected penile glans ischemic necrosis developed after embolization. We successfullytreated the patients with intravenous infusion of alprostadil, oral pentoxifylline and tadalafil...
December 26, 2017: Urology Journal
https://www.readbyqxmd.com/read/29275134/comparative-safety-of-drugs-targeting-the-nitric-oxide-pathway-in-pulmonary-hypertension-a-mixed-approach-combining-a-meta-analysis-of-clinical-trials-and-a-disproportionality-analysis-from-the-who-pharmacovigilance-database
#3
C Khouri, M Lepelley, M Roustit, F Montastruc, M Humbert, J L Cracowski
BACKGROUND: Recent guidelines recommend riociguat, a soluble guanylate cyclase (sGC) stimulator, as well as the type 5 phosphodiesterase inhibitor (PDE5i) tadalafil or sildenafil as treatments for pulmonary arterial hypertension. We compared the safety profiles of sildenafil, tadalafil and riociguat in pulmonary hypertension. METHODS: We combined two approaches: First, we performed a meta-analysis of safety data extracted from randomized controlled trials. Secondly, we conducted a disproportionality analysis of data from VigiBase, the WHO global database of individual case safety reports, to compare the safety profiles with real life data...
December 21, 2017: Chest
https://www.readbyqxmd.com/read/29251556/express-the-impact-of-ambrisentan-and-tadalafil-upfront-combination-therapy-on-cardiac-function-in-patients-with-scleroderma-associated-pulmonary-arterial-hypertension-cardiac-magnetic-resonance-feature-tracking-study
#4
https://www.readbyqxmd.com/read/29236802/tadalafil-protector-effect-during-ischemia-reperfusion-in-rats
#5
Eduardo Gabriel Gerber Wietzikoski, Julio Cesar Foiatto, Nicolau Gregori Czeczko, Osvaldo Malafaia, Fernando Cesar Koleski, Tiago Cesar Mierzwa, Regina de Paula Xavier Gomes
PURPOSE: To evaluate histological parameters in rat renal tissue after tadalafil use during hot ischemia for 45 minutes and reperfusion for 24 hours. METHODS: Twenty rats were divided into 2 groups. In the experimental group 10 mg/kg of tadalafil was used per gavage before the procedure. All cases underwent left partial nephrectomy, followed by 45 minutes of warm ischemia. Left nephrectomy of the remaining kidney was performed after 24 hours from the initial procedure...
November 2017: Acta Cirúrgica Brasileira
https://www.readbyqxmd.com/read/29233027/effects-of-phosphodiestrase-type-5-inhibitors-in-epinephrine-induced-arrhythmia-in-rats-involvement-of-lactate-dehydrogenase-and-creatine-kinase-downregulation-and-adiponectin-expression
#6
Aaa Salama, R E Mostafa, E A Omara
Cardiac arrhythmia is a common cause of mortality, and its progression may be due to abnormal sympathetic nerve activity and catecholamine release. Besides, lactate dehydrogenase (LDH) and creatine kinase (CK) downregulation and adiponectin expression play important roles in promoting coronary artery disease. The study aimed to examine the possible cardioprotective effect of members of phosphodiesterase type 5 (PDE-5) inhibitors in epinephrine-induced arrhythmia in rats. Arrhythmia was induced by cumulative boluses of epinephrine (4, 8, 16, 32, 64, and 128 mg/kg) given at 10-min intervals...
January 1, 2017: Human & Experimental Toxicology
https://www.readbyqxmd.com/read/29220595/dose-dependent-effects-of-tadalafil-and-roflumilast-on-ovalbumin-induced-airway-hyperresponsiveness-in-guinea-pigs
#7
Anna Urbanova, Ivana Medvedova, Martin Kertys, Pavol Mikolka, Petra Kosutova, Daniela Mokra, Juraj Mokrý
INTRODUCTION: Chronic obstructive diseases of airways associated with cough and/or airway smooth muscle hyperresponsiveness are usually treated with bronchodilating and anti-inflammatory drugs. Recently, selective phosphodiesterase (PDE) 4 inhibitors have been introduced into the therapy of chronic obstructive pulmonary disease. Several studies have demonstrated their ability to influence the airway reactivity and eosinophilic inflammation by increasing the intracellular cAMP concentrations also in bronchial asthma...
December 8, 2017: Experimental Lung Research
https://www.readbyqxmd.com/read/29215546/initial-tadalafil-and-ambrisentan-combination-therapy-in-pulmonary-arterial-hypertension-clinical-and-haemodynamic-long-term-efficacy-italy-study
#8
Michele D'Alto, Emanuele Romeo, Paola Argiento, Giuseppe Paciocco, Renato Prediletto, Stefano Ghio, Michele Correale, Francesco Lo Giudice, Roberto Badagliacca, Alessandra Greco, Carmine Dario Vizza
AIMS: Initial combination therapy with ambrisentan and tadalafil (upfront therapy) offers clinical benefits in pulmonary arterial hypertension (PAH) and reduces the risk of clinical failure compared with monotherapy in naïve patients. The aim of study is to assess the efficacy of a 12-month upfront therapy with ambrisentan and tadalafil in improving haemodynamics in incident PAH patients. METHODS: This is a multicentre retrospective analysis of real-world Italian clinical data in 56 patients with newly diagnosed PAH...
January 2018: Journal of Cardiovascular Medicine
https://www.readbyqxmd.com/read/29202488/acute-tadalafil-administration-increases-plasma-fatty-acids-without-changes-in-the-inflammatory-response-in-healthy-men
#9
Roberta Ceci, Guglielmo Duranti, Paolo Sgrò, Stefania Sabatini, Luigi Di Luigi
PURPOSE: Tadalafil, the phosphodiesterase type 5 inhibitor (PDE5I), has been shown to reduce visceral adipose tissue in rabbit and to improve lean mass content in non-obese men. In order to clarify this effect in humans, in the present study we determined the impact of an acute oral tadalafil administration on lipolysis by evaluating plasma free fatty acids (FFAs) and glycerol. FFAs are potential modulator of inflammation response that we evaluated through tumor necrosis factor alpha (TNFα), interleukin 6 (IL6), interleukin 8 (IL8) and interleukin 10 (IL10) plasma levels...
December 5, 2017: Acta Biochimica Polonica
https://www.readbyqxmd.com/read/29201512/safety-and-efficacy-of-silodosin-and-tadalafil-in-ease-of-negotiation-of-large-ureteroscope-in-the-management-of-ureteral-stone-a-prosective-randomized-trial
#10
Rohit Bhattar, Vipin Jain, Vinay Tomar, Sher Singh Yadav
Objective: To evaluate the safety and efficacy of silodosin and tadalafil in ease of negotiation of large size ureteroscope (8/9.8 Fr) in the management of ureteral stone. Material and methods: Between June 2015 and May 2016, 86 patients presented with ureteral stone of size 6-15 mm were on consent randomly assigned to 1 of 3 outpatient treatment arms: silodosin (Group A), tadalafil (Group B), and placebo (Group C). After two weeks of therapy 67 patients underwent ureteroscopy, and ureteral orifice configuration, ureteroscopic negotiation, ureteral dilatation, operating time, procedural complication and drug related side effects were noted in each group...
December 2017: Turkish Journal of Urology
https://www.readbyqxmd.com/read/29194814/how-sildenafil-viagra%C3%A2-may-cause-melanoma-a-histopathologic-study-providing-a-potential-physiological-etiopathological-mechanism
#11
W Clark Lambert, Muriel W Lambert, Christina M Ring, Claude E Gagna, Jose D Espinal-Mariotte, Robert A Schwartz
The potential role of phosphodiesterase type 5 inhibitors (PDE5-Is) sildenafil (Viagra® ), vardenafil (Levitra® ), and tadalafil (Cialis® ) in development of malignant melanoma is controversial. Four observational studies have examined the association of PDE5-Is) and melanoma (1-4). While a conclusion regarding causality is challenging, the biological basis for an association between PDE5-I exposure and melanoma remains compelling. Melanoma lines expressing the BRAF oncogene downregulate PDE5, leading to vasodilation, invasion and metastasis of melanoma cells (5)...
December 1, 2017: Journal of the European Academy of Dermatology and Venereology: JEADV
https://www.readbyqxmd.com/read/29171944/-central-serous-chorioretinopathy-following-the-use-of-phosphodiesterase-5-inhibitors
#12
C Smal, G Lepièce, S Bonnet
Central serous chorioretinopathy occurs primarily in young caucasian men. It is characterized by the development of a serous detachment of the sensory retina with the apparition of a relative central scotomata. An association with phosphodiesterase 5 inhibitors is reported in some articles. We described two cases of central serous chorioretinopathy following the use of tadalafil and sildenafil.
November 2017: Revue Médicale de Liège
https://www.readbyqxmd.com/read/29164680/effects-of-tadalafil-on-storage-and-voiding-function-in-patients-with-male-lower-urinary-tract-symptoms-suggestive-of-benign-prostatic-hyperplasia-a-urodynamic-based-study
#13
Yoshihisa Matsukawa, Tsuyoshi Majima, Kazuna Matsuo, Yasuhito Funahashi, Masashi Kato, Tokunori Yamamoto, Momokazu Gotoh
OBJECTIVE: To investigate the effects of tadalafil on storage and voiding function in treatment-naïve patients with lower urinary tract symptoms suggestive of benign prostatic hyperplasia, based on a urodynamic study. METHODS: This was an open-labeled, single-center, prospective study. A total of 80 untreated outpatients with lower urinary tract symptoms suggestive of benign prostatic hyperplasia received tadalafil 5 mg/day for 12 weeks. Subjective symptoms and objective findings on voiding and storage function obtained through urodynamic studies, including cystometry and pressure flow study, were evaluated before and after treatment...
November 22, 2017: International Journal of Urology: Official Journal of the Japanese Urological Association
https://www.readbyqxmd.com/read/29138357/tadalafil-a-long-acting-phosphodiesterase-inhibitor-promotes-bone-marrow-stem-cell-survival-and-their-homing-into-ischemic-myocardium-for-cardiac-repair
#14
Ibrahim Elmadbouh, Muhammad Ashraf
The aim was to evaluate the tadalafil-mediated effects at molecular level on bone marrow-derived mesenchymal stem cells (MSCs) survival and their homing into the infarcted hearts to promote cardiac repair and improve function. MSCs were pretreated in vitro with inhibitors of PKG, MAPK, FasL, nitric oxide synthase (NOS) (L-NAME), CXCR4 (AMD3100), or miR-21 inhibitors (+/-luciferase construction +/-Fas) prior to tadalafil treatment for 2 h. These MSCs were then subjected to H2O2 stress to assess their injury...
November 2017: Physiological Reports
https://www.readbyqxmd.com/read/29135645/phosphodiesterase-type-5-inhibitors-sport-and-doping
#15
Luigi Di Luigi, Massimiliano Sansone, Andrea Sansone, Roberta Ceci, Guglielmo Duranti, Paolo Borrione, Clara Crescioli, Paolo Sgrò, Stefania Sabatini
Phosphodiesterase type 5 inhibitors (PDE5i) (e.g., sildenafil, tadalafil, vardenafil, and avanafil) are drugs commonly used to treat erectile dysfunction, pulmonary arterial hypertension, and benign prostatic hyperplasia. PDE5i are not prohibited by the World Anti-Doping Agency (WADA) but are alleged to be frequently misused by healthy athletes to improve sporting performance. In vitro and in vivo studies have reported various effects of PDE5i on cardiovascular, muscular, metabolic, and neuroendocrine systems and the potential, therefore, to enhance performance of healthy athletes during training and competition...
November 2017: Current Sports Medicine Reports
https://www.readbyqxmd.com/read/29134978/testicular-and-epididymal-histology-of-rats-chronically-administered-high-doses-of-phosphodiesterase-5-inhibitors-and-tramadol
#16
Victor U Nna, Augustine L Udefa, Emmanuel O Ofutet, Eme O Osim
Testicular oxidative stress, endocrine disruption and abnormal spermatogenesis in rats exposed to high doses ofphosphodiesterase-5 inhibitors (PDE5i) and opioids, with poor reversibility following withdrawal of treatment had beenreported. In this study, we examined the histopathological effects of high doses of sildenafil, tadalafil, tramadol andsildenafil+tramadol on the testes and epididymis of rats. Seventy male rats (180 - 200 g b.w) were assigned to one of fivegroups (n = 14), namely; A: control (0.2 mL normal saline), B: sildenafil (1 mg/100g b...
June 30, 2017: Nigerian Journal of Physiological Sciences: Official Publication of the Physiological Society of Nigeria
https://www.readbyqxmd.com/read/29132113/fluorometric-detection-of-protein-ligand-engagement-the-case-of-phosphodiesterase5
#17
Giulia Di Rocco, Ilaria Martinelli, Salvatore Pacifico, Remo Guerrini, Elena Cichero, Paola Fossa, Silvia Franchini, Silvia Cardarelli, Mauro Giorgi, Marco Sola, Glauco Ponterini
Phosphodiesterases (PDEs) regulate the intracellular levels of cAMP and cGMP. The great clinical success of the PDE5 inhibitors, Sildenafil (Viagra), Vardenafil (Levitra) and Tadalafil (Cialis) has led to an increasing interest for this class of enzymes. Recent studies have shown a correlation between tumor growth and PDE5 overexpression, making PDE5-selective inhibitors promising candidates for cancer treatment. The search for such inhibitors rests today on radioactive assays. In this work, we exploit the conserved catalytic domain of the enzyme and propose a faster and safer method for detecting the binding of ligands and evaluate their affinities...
November 10, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/29094398/early-improvement-of-storage-or-voiding-symptoms-by-tadalafil-predicts-treatment-outcomes-in-patients-with-lower-urinary-tract-symptoms-from-benign-prostatic-hyperplasia
#18
Osamu Yokoyama, Akichika Ozeki, Nahoko Suzuki, Masahiro Murakami
OBJECTIVES: To determine whether early changes in International Prostate Symptom Score predict final improvement in the quality of life and treatment satisfaction of patients with lower urinary tract symptoms from benign prostatic hyperplasia receiving tadalafil. METHODS: This post-hoc analysis of three randomized-controlled trials of tadalafil for lower urinary tract symptoms from benign prostatic hyperplasia used subpopulations based on treatment status (tadalafil, placebo) and region (Japan, Asia)...
November 1, 2017: International Journal of Urology: Official Journal of the Japanese Urological Association
https://www.readbyqxmd.com/read/29094165/phosphodiesterase-inhibitors-sildenafil-and-vardenafil-reduce-zebrafish-rod-photoreceptor-outer-segment-shedding
#19
Leah J Campbell, Abbie M Jensen
Purpose: The vertebrate rod photoreceptor undergoes daily growth and shedding to renew the rod outer segment (ROS), a modified cilium that contains the phototransduction machinery. It has been demonstrated that ROS shedding is regulated by the light-dark cycle; however, we do not yet have a satisfactory understanding of the molecular mechanisms that underlie this regulation. Given that phototransduction relies on the hydrolysis of cGMP via phosphodiesterase 6 (PDE6), we examined ROS growth and shedding in zebrafish treated with cGMP-specific PDE inhibitors...
November 1, 2017: Investigative Ophthalmology & Visual Science
https://www.readbyqxmd.com/read/29089445/novel-imaging-of-the-prostate-reveals-spontaneous-gland-contraction-and-excretory-duct-quiescence-together-with-different-drug-effects
#20
Robert Kügler, Andrea Mietens, Mathias Seidensticker, Sabine Tasch, Florian M Wagenlehner, Andre Kaschtanow, Yudy Tjahjono, Claudia U Tomczyk, Daniela Beyer, Gail P Risbridger, Betty Exintaris, Stuart J Ellem, Ralf Middendorff
Prostate carcinoma and benign prostate hyperplasia (BPH) with associated lower urinary tract symptoms (LUTS) are among the most prevalent and clinically relevant diseases in men. BPH is characterized by an enlargement of prostate tissue associated with increased tone of smooth muscle cells (SMCs) which surround the single glands composing the prostate. Secretions of the glands leave the prostate through local excretory ducts during the emission phase of ejaculation. Pharmacological treatment of BPH suggests different local drug targets based on reduction of prostate smooth muscle tone as the main effect and disturbed ejaculation as a common side effect...
October 31, 2017: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
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