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Sildenafil

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https://www.readbyqxmd.com/read/27926905/sildenafil-in-pregnancy-a-systematic-review-of-maternal-tolerance-and-obstetric-and-perinatal-outcomes
#1
Liam Dunn, Ristan Greer, Vicki Flenady, Sailesh Kumar
INTRODUCTION: This systematic review evaluates maternal tolerance and obstetric and perinatal outcomes following sildenafil citrate (SC) use in human pregnancy. DATA SOURCES: Scopus, PubMed, Cochrane Library, Web of Science, Embase, and Google Scholar were searched. Relevant full-text studies including case series and reports in English were included. Publications were excluded if the pregnancy was terminated or if SC was used only at conception. RESULTS: Sixteen studies were included (n = 165)...
December 8, 2016: Fetal Diagnosis and Therapy
https://www.readbyqxmd.com/read/27915325/possible-role-of-sildenafil-citrate-in-the-recurrence-of-neovascularization-in-laser-regressed-aggressive-posterior-rop
#2
Chaitra Jayadev, Phanibhushan Ramasastry, Alia Gul, Anand Vinekar
BACKGROUND: Systemic diseases and their treatment influence aggressive posterior retinopathy of prematurity. CASE CHARACTERISTICS: A premature infant with aggressive posterior retinopathy of prematurity underwent laser treatment with a favourable outcome. She was started on oral sidenafil citrate for pulmonary hypertension. Ten days later she developed neovascularization within the lasered retina. INTERVENTION/OUTCOME: Considering the possible role of sildenafil in this unusual development, the drug was withdrawn resulting in regression of the neovascularization...
November 7, 2016: Indian Pediatrics
https://www.readbyqxmd.com/read/27908707/the-role-of-nmda-receptor-and-nitric-oxide-cyclic-guanosine-monophosphate-pathway-in-the-antidepressant-like-effect-of-dextromethorphan-in-mice-forced-swimming-test-and-tail-suspension-test
#3
Ehsan Sakhaee, Sattar Ostadhadi, Muhammad Imran Khan, Farbod Yousefi, Abbas Norouzi-Javidan, Reyhaneh Akbarian, Mohsen Chamanara, Samira Zolfaghari, Ahmad-Reza Dehpour
Depression is a devastating disorder which has a high impact on the wellbeing of overall society. As such, need for innovative therapeutic agents are always there. Most of the researchers focused on N-methyl-d-aspartate receptor to explore the antidepressant like activity of new therapeutic agents. Dextromethorphan is a cough suppressant agent with potential antidepressant activity reported in mouse force swimming test. Considering N-methyl-d-aspartate as a forefront in exploring antidepressant agents, here we focused to unpin the antidepressant mechanism of dextromethorphan targeting N-methyl-d-aspartate receptor induced nitric oxide-cyclic guanosine monophosphate signaling...
November 28, 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/27904030/formulation-optimization-and-in-vitro-characterization-of-orally-disintegrating-films-using-a-factorial-design-and-mathematical-modeling-for-drug-release
#4
Yeongbin Lee, Prakash Thapa, Seong Hoon Jeong, Mi Hee Woo, Du Hyung Choi
Even though experimental designs are becoming popular especially for conventional dosage forms, limited studies have been performed to optimize formulations of orally disintegrating films (ODFs). This study aimed to evaluate sildenafil citrate-loaded ODFs for a controlled release with hydroxypropyl methylcellulose as a film-forming polymer. A factorial design was utilized for optimization with three control factors: ethanol ratio, plasticizer ratio, and the type of plasticizer. Tensile strength, disintegration time, water contact angle, and thickness were chosen as responses...
November 30, 2016: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/27903966/pde5-inhibitors-enhance-the-lethality-of-pemetrexed-through-inhibition-of-multiple-chaperone-proteins-and-via-the-actions-of-cyclic-gmp-and-nitric-oxide
#5
Laurence Booth, Jane L Roberts, Andrew Poklepovic, Sarah Gordon, Paul Dent
Phosphodiesterase 5 (PDE5) inhibitors prevent the breakdown of cGMP that results in prolonged protein kinase G activation and the generation of nitric oxide. PDE5 inhibitors enhanced the anti-NSCLC cell effects of the NSCLC therapeutic pemetrexed. [Pemetrexed + sildenafil] activated an eIF2α - ATF4 - CHOP - Beclin1 pathway causing formation of toxic autophagosomes; activated a protective IRE1 - XBP-1 - chaperone induction pathway; and activated a toxic eIF2α - CHOP - DR4 / DR5 / CD95 induction pathway. [Pemetrexed + sildenafil] reduced the expression of c-FLIP-s, MCL-1 and BCL-XL that was blocked in a cell-type -dependent fashion by either over-expression of HSP90 / GRP78 / HSP70 / HSP27 or by blockade of eIF2α-CHOP signaling...
November 26, 2016: Oncotarget
https://www.readbyqxmd.com/read/27895461/sildenafil-potentiates-the-antitumor-activity-of-cisplatin-by-induction-of-apoptosis-and-inhibition-of-proliferation-and-angiogenesis
#6
Mona Mohamed El-Naa, Mohamed Othman, Sheren Younes
Sildenafil is the first phosphodiesterase-5 inhibitor used for the treatment of erectile dysfunction. However, recent studies have been suggesting an antitumor effect of sildenafil. The current study assessed the aforementioned activity of sildenafil in vivo and in vitro in solid-tumor-bearing mice and in a human cell line MCF-7, respectively. Moreover, we investigated the impact of sildenafil on cisplatin antitumor activity. The solid tumor was induced by inoculation of Ehrlich ascites carcinoma cells in female mice...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27895156/sildenafil-prevents-podocyte-injury-via-ppar-%C3%AE-mediated-trpc6-inhibition
#7
Ramon Sonneveld, Joost G Hoenderop, Andrea M Isidori, Carole Henique, Henry B Dijkman, Jo H Berden, Pierre-Louis Tharaux, Johan van der Vlag, Tom Nijenhuis
Transient receptor potential channel C6 (TRPC6) gain-of-function mutations and increased TRPC6 expression in podocytes induce glomerular injury and proteinuria. Sildenafil reduces TRPC6 expression and activity in nonrenal cell types, although the mechanism is unknown. Peroxisome proliferator-activated receptor γ (PPAR-γ) is a downstream target of sildenafil in the cyclic guanosine monophosphate (cGMP)-activated protein kinase G (PKG) axis. PPAR-γ agonists, like pioglitazone, appear antiproteinuric. We hypothesized that sildenafil inhibits TRPC6 expression in podocytes through PPAR-γ-dependent mechanisms, thereby counteracting podocyte injury and proteinuria...
November 28, 2016: Journal of the American Society of Nephrology: JASN
https://www.readbyqxmd.com/read/27887774/rationale-and-study-design-of-respite-an-open-label-phase-3b-study-of-riociguat-in-patients-with-pulmonary-arterial-hypertension-who-demonstrate-an-insufficient-response-to-treatment-with-phosphodiesterase-5-inhibitors
#8
Marius M Hoeper, James R Klinger, Raymond L Benza, Gerald Simonneau, David Langleben, Robert Naeije, Paul A Corris
Patients with pulmonary arterial hypertension (PAH) who do not have an adequate response to therapy with phosphodiesterase-5 inhibitors (PDE-5i) may have insufficient synthesis of cyclic guanosine monophosphate (cGMP). These patients may respond to a direct soluble guanylate cyclase (sGC) stimulator such as riociguat. RESPITE (NCT02007629) was an open-label, multicenter, uncontrolled, single-arm phase 3b study of riociguat in patients with PAH who demonstrated an insufficient response to treatment with PDE-5i...
November 5, 2016: Respiratory Medicine
https://www.readbyqxmd.com/read/27881492/determination-of-common-adulterants-in-herbal-medicine-and-food-samples-using-core-shell-column-coupled-to-tandem-mass-spectrometry
#9
Haider A J Al Lawati, Idris Al Busaidi, Afsal M Kadavilpparampu, FakhrEldin O Suliman
High-performance liquid chromatography coupled to tandem mass spectrometry was used to develop and validate a rapid method to qualitatively and quantitatively analyse 18 common adulterants in herbal medicine and food samples. Initially, the mobile phase composition was optimized in three different columns: core-shell, monolithic and standard 3.5-µm-particle-size columns. The results show that the core-shell column provides the best separation. Moreover, the tandem mass spectrometry was optimized. The linear range for all adulterants was 0...
November 23, 2016: Journal of Chromatographic Science
https://www.readbyqxmd.com/read/27877095/evaluation-of-the-tolerability-of-intermittent-intravenous-sildenafil-in-pediatric-patients-with-pulmonary-hypertension
#10
Robyn A Fender, Ty E Hasselman, Yanzhi Wang, Aaron A Harthan
OBJECTIVES: The primary purpose of this study was to determine the tolerability of intermittent intravenous (IV) sildenafil for the treatment of pulmonary hypertension in pediatric patients. Secondary objectives were to evaluate parameters related to efficacy. METHODS: This was a retrospective chart review from January 2013 to August 2014 of pediatric patients under age 18 years treated with intermittent doses of IV sildenafil for pulmonary hypertension. Patients were excluded if they were over age 18 years or received sildenafil for other indications...
September 2016: Journal of Pediatric Pharmacology and Therapeutics: JPPT: the Official Journal of PPAG
https://www.readbyqxmd.com/read/27873389/sildenafil-unbridled-optimism-and-heart-failure-with-preserved-ejection-fraction
#11
EDITORIAL
Yogesh N V Reddy, Barry A Borlaug
No abstract text is available yet for this article.
November 21, 2016: European Journal of Heart Failure
https://www.readbyqxmd.com/read/27873388/effects-of-sildenafil-on-cardiac-structure-and-function-cardiopulmonary-exercise-testing-and-health-related-quality-of-life-measures-in-heart-failure-patients-with-preserved-ejection-fraction-and-pulmonary-hypertension
#12
Licette C Y Liu, Yoran M Hummel, Peter van der Meer, Rolf M F Berger, Kevin Damman, Dirk J van Veldhuisen, Adriaan A Voors, Elke S Hoendermis
AIMS: We recently showed that sildenafil did not improve pulmonary pressures and exercise capacity in a cohort of patients with heart failure and preserved ejection fraction (HFpEF) and predominantly postcapillary pulmonary hypertension. Here, we present the effects of sildenafil on cardiac structure and function, cardiopulmonary exercise testing, laboratory parameters and health-related quality of life measures. METHODS AND RESULTS: Fifty-two HFpEF patients with pulmonary hypertension (mean pulmonary artery pressure >25 mmHg; pulmonary artery wedge pressure >15 mmHg) were randomized to sildenafil 60 mg three times a day or placebo and treated for 12 weeks...
November 21, 2016: European Journal of Heart Failure
https://www.readbyqxmd.com/read/27871960/useful-implications-of-low-dose-long-term-use-of-pde-5-inhibitors
#13
REVIEW
Taymour Mostafa
INTRODUCTION: Phosphodiesterase type 5 (PDE-5) hydrolyzes cyclic guanylate monophosphate (cGMP) specifically to 5' GMP, promoting successful corporeal vascular relaxation and penile erection during sexual stimulation. Oral PDE-5 inhibitors such as sildenafil, vardenafil, tadalafil, and avanafil have provided noninvasive, effective, well-tolerated treatment for erectile dysfunction (ED) patients and, at the same time, stimulated both academic and clinical interests. Lately, some oral PDE-5 inhibitors were released as low-dose preparations with the concept of potential daily administration and long-term use...
July 2016: Sexual Medicine Reviews
https://www.readbyqxmd.com/read/27867500/neurological-complications-in-chronic-kidney-disease
#14
REVIEW
Ria Arnold, Tushar Issar, Arun V Krishnan, Bruce A Pussell
Patients with chronic kidney disease (CKD) are frequently afflicted with neurological complications. These complications can potentially affect both the central and peripheral nervous systems. Common neurological complications in CKD include stroke, cognitive dysfunction, encephalopathy, peripheral and autonomic neuropathies. These conditions have significant impact not only on patient morbidity but also on mortality risk through a variety of mechanisms. Understanding the pathophysiological mechanisms of these conditions can provide insights into effective management strategies for neurological complications...
January 2016: JRSM Cardiovascular Disease
https://www.readbyqxmd.com/read/27865471/satisfaction-and-treatment-adherence-in-erectile-dysfunction-in-the-medium-and-long-term
#15
J Panach-Navarrete, A Morales-Giraldo, C Ferrandis-Cortés, F García-Morata, J C Pastor-Lence, J M Martínez-Jabaloyas
INTRODUCTION: The aim of this study was to show the satisfaction and treatment adherence in erectile dysfunction (ED) in the medium and long term. MATERIAL AND METHODS: A descriptive, comparative study was conducted in 2 centres through telephone interviews with patients who came for an initial visit between 2012 and 2014 for ED. A complete case history review was conducted on the use of and withdrawal from treatment. For current use, the Erectile Dysfunction Inventory of Treatment Satisfaction (EDITS) and the Global Assessment Questionnaire (GAQ) were filled out; for past use, only the GAQ was filled out...
November 16, 2016: Actas Urologicas Españolas
https://www.readbyqxmd.com/read/27861916/sildenafil-therapy-for-fetal-cardiovascular-dysfunction-during-hypoxic-development-studies-in-the-chick-embryo
#16
Nozomi Itani, Katie L Skeffington, Christian Beck, Dino A Giussani
There is a need for developing clinically translatable therapy for preventing fetal origins of cardiovascular disease in pregnancy complicated by chronic fetal hypoxia. Evidence shows that sildenafil protects placental perfusion and fetal growth. However, whether beneficial effects of sildenafil transcend onto the fetal heart and circulation in complicated development is unknown. We isolated the direct effects of sildenafil on the fetus using the chick embryo and hypothesised that sildenafil also protects fetal cardiovascular function in hypoxic development...
November 12, 2016: Journal of Physiology
https://www.readbyqxmd.com/read/27860185/sildenafil-attenuates-hypoxic-pulmonary-remodelling-by-inhibiting-bone-marrow-progenitor-cells
#17
Shirley Favre, Elisa Gambini, Patrizia Nigro, Alessandro Scopece, Paola Bianciardi, Anna Caretti, Giulio Pompilio, Antonio F Corno, Giuseppe Vassalli, Ludwig K von Segesser, Michele Samaja, Giuseppina Milano
The recruitment of bone marrow (BM)-derived progenitor cells to the lung is related to pulmonary remodelling and the pathogenesis of pulmonary hypertension (PH). Although sildenafil is a known target in PH treatment, the underlying molecular mechanism is still elusive. To test the hypothesis that the therapeutic effect of sildenafil is linked to the reduced recruitment of BM-derived progenitor cells, we induced pulmonary remodelling in rats by two-week exposure to chronic hypoxia (CH, 10% oxygen), a trigger of BM-derived progenitor cells...
November 18, 2016: Journal of Cellular and Molecular Medicine
https://www.readbyqxmd.com/read/27855594/when-chems-meet-sex-a-rising-phenomenon-called-chemsex
#18
Raffaele Giorgetti, Adriano Tagliabracci, Fabrizio Schifano, Simona Zaami, Enrico Marinelli, Francesco Paolo Busardò
BACKGROUND: The term "chemsex" was coined to indicate the voluntary intake of psychoactive and non psychoactive drugs in the context of recreational settings to facilitate and/or to enhance sexual intercourses mostly among men who have sex with other men (MSM). OBJECTIVE: The authors aimed to review the mechanisms of action, the toxicity and the pattern of use and abuse of substances involved in "chemsex" practice together with the sociocultural background underlying it and the health-related consequences that they may have...
November 17, 2016: Current Neuropharmacology
https://www.readbyqxmd.com/read/27853102/cardiac-safety-profile-of-sildenafil-chronotropic-inotropic-and-coronary-vasodilator-effects-in-the-canine-isolated-blood-perfused-heart-preparations
#19
Nur Jaharat Lubna, Yuji Nakamura, Xin Cao, Takeshi Wada, Hiroko Izumi-Nakaseko, Kentaro Ando, Atsushi Sugiyama
Sildenafil is a phosphodiesterase type-5 inhibitor. We evaluated the effects of sildenafil on the sinoatrial rate, developed tension of the papillary muscle and coronary blood flow by using the canine isolated, blood-perfused sinoatrial node and papillary muscle preparations. The former preparation had a regular automaticity rate of 106 ± 1 beats/min (n = 4), whereas the latter showed a developed tension of 22 ± 4 mN (n = 4) and a coronary blood flow of 3.9 ± 0.1 mL/min (n = 4). Intracoronary injection of 10, 30 and 100 µg of sildenafil, which would provide about 20 to 200 times higher plasma drug concentrations than its therapeutic level, increased the automaticity rate by 4, 12 and 22%, the developed tension by 19, 55 and 118% and the coronary blood flow by 42, 95 and 142%, respectively...
2016: Journal of Toxicological Sciences
https://www.readbyqxmd.com/read/27843323/patent-ductus-arteriosus-with-persistent-pulmonary-artery-hypertension-after-transcatheter-closure
#20
Jianqi Feng, Xiangqing Kong, Yanhui Sheng, Rong Yang
OBJECTIVES: To observe the change in pulmonary artery systolic pressure (PASP) of patients with persistent pulmonary arterial hypertension (PAH) after patent ductus arteriosus (PDA) occlusion. BACKGROUND: After occlusion of PDA in patients with PAH, some patients still tend to suffer from persistent PAH. METHODS: A chest X-ray, an electrocardiogram, and an echocardiogram were performed on nine patients at 24 hours, 1 and 6 months, and 1 year serially...
2016: Therapeutics and Clinical Risk Management
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