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https://www.readbyqxmd.com/read/28938916/use-of-the-kladh3-promoter-for-the-quantitative-production-of-the-murine-pde5a-isoforms-in-the-yeast-kluyveromyces-lactis
#1
Silvia Cardarelli, Mauro Giorgi, Fabio Naro, Francesco Malatesta, Stefano Biagioni, Michele Saliola
BACKGROUND: Phosphodiesterases (PDE) are a superfamily of enzymes that hydrolyse cyclic nucleotides (cAMP/cGMP), signal molecules in transduction pathways regulating crucial aspects of cell life. PDEs regulate the intensity and duration of the cyclic nucleotides signal modulating the downstream biological effect. Due to this critical role associated with the extensive distribution and multiplicity of isozymes, the 11 mammalian families (PDE1 to PDE11) constitute key therapeutic targets...
September 22, 2017: Microbial Cell Factories
https://www.readbyqxmd.com/read/28934694/development-and-implementation-of-a-pass-fail-field-friendly-method-for-detecting-sildenafil-in-suspect-pharmaceutical-tablets-using-a-handheld-raman-spectrometer-and-silver-colloids
#2
Adam Lanzarotta, Lisa Lorenz, JaCinta S Batson, Cheryl Flurer
A simple, fast, sensitive and effective pass/fail field-friendly method has been developed for detecting sildenafil in suspect Viagra and unapproved tablets using handheld Raman spectrometers and silver colloids. The method involves dissolving a portion of a tablet in water followed by filtration and addition of silver colloids, resulting in a solution that can be measured directly through a glass vial. Over one hundred counterfeit Viagra and unapproved tablets were examined on three different devices during the method development phase of the study...
September 8, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28932631/tadalafil-has-biologic-activity-in-human-melanoma-results-of-a-pilot-trial-with-tadalafil-in-patients-with-metastatic-melanoma-tame
#3
Jessica C Hassel, Huanhuan Jiang, Carolin Bender, Julia Winkler, Alexandra Sevko, Ivan Shevchenko, Niels Halama, Antonia Dimitrakopoulou-Strauss, Walter E Haefeli, Dirk Jäger, Alexander Enk, Jochen Utikal, Viktor Umansky
Myeloid-derived suppressor cells (MDSCs) are known to play a critical role in the suppression of T cell antitumor responses. Our preclinical data showed that the phosphodiesterase (PDE)-5 inhibitor sildenafil impaired MDSC functions, enhanced intratumoral T cell activity and prolonged survival of melanoma-bearing mice. In this study, we evaluated biologic effects, safety and efficacy of palliative treatment with the PDE-5 inhibitor tadalafil in metastatic melanoma patients. We conducted an open-label, dose de-escalation trial with tadalafil in pretreated metastatic melanoma patients...
2017: Oncoimmunology
https://www.readbyqxmd.com/read/28926088/treatments-for-priapism-in-boys-and-men-with-sickle-cell-disease
#4
REVIEW
Francis I Chinegwundoh, Sherie Smith, Kofi A Anie
BACKGROUND: Sickle cell disease comprises a group of genetic haemoglobin disorders. The predominant symptom associated with sickle cell disease is pain resulting from the occlusion of small blood vessels by abnormally 'sickle-shaped' red blood cells. There are other complications, including chronic organ damage and prolonged painful erection of the penis, known as priapism. Severity of sickle cell disease is variable, and treatment is usually symptomatic. Priapism affects up to half of all men with sickle cell disease, however, there is no consistency in treatment...
September 19, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/28923561/update-on-the-safety-of-phosphodiesterase-type-5-inhibitors-for-the-treatment-of-erectile-dysfunction
#5
REVIEW
Faysal A Yafi, Ira D Sharlip, Edgardo F Becher
INTRODUCTION: Phosphodiesterase type 5 inhibitors (PDE5Is) have demonstrated efficacy in the treatment of erectile dysfunction (ED). Although historically found to have limited drug-related adverse events, emerging data have suggested that PDE5Is might be associated with melanoma or recurrence of prostate cancer after radical prostatectomy. AIM: To summarize the literature on the safety of PDE5Is. METHODS: A literature review was performed through PubMed from 1990 through 2016 regarding ED...
September 8, 2017: Sexual Medicine Reviews
https://www.readbyqxmd.com/read/28918687/comments-on-utero-placental-perfusion-doppler-indices-in-growth-restricted-fetuses-effect-of-sildenafil-citrate
#6
Ahmed M Abbas
No abstract text is available yet for this article.
September 17, 2017: Journal of Maternal-fetal & Neonatal Medicine
https://www.readbyqxmd.com/read/28906529/the-effect-of-iloprost-and-sildenafil-alone-and-in-combination-on-myocardial-ischaemia-and-nitric-oxide-and-irisin-levels
#7
Suna Aydin, Tuncay Kuloglu, Suleyman Aydin, Meltem Yardim, Davut Azboy, Zeki Temizturk, Ali Kemal Kalkan, Mehmet Nesimi Eren
AIM: Insufficient oxygen supply to organs and tissues due to reduced arterial or venous blood flow results in ischaemia, during which, although ATP production stops, AMP and adenosine continue to be produced from ATP. The fate of irisin, which causes the production of heat instead of ATP during ischaemia, is unknown. Iloprost and sildenafil are two pharmaceutical agents that mediate the resumption of reperfusion (blood supply) via vasodilatation during ischaemic conditions. Our study aimed to explore the effects of iloprost and sildenafil on irisin levels in the heart, liver and kidney tissues and whether these pharmaceutical agents had any impact on serum irisin and nitric oxide levels in rats with induced experimental myocardial ischaemia...
August 31, 2017: Cardiovascular Journal of Africa
https://www.readbyqxmd.com/read/28903860/a-review-of-synthetic-phosphodiesterase-type-5-inhibitors-pde-5i-found-as-adulterants-in-dietary-supplements
#8
REVIEW
Chee-Leong Kee, Xiaowei Ge, Véronique Gilard, Myriam Malet-Martino, Min-Yong Low
To date, there are 80 synthetic PDE-5i found as adulterants in dietary supplements. Analogues of sildenafil remain as the top list with 50 (62%) and are followed by analogues of tadalafil, 21 (26%), analogues of vardenafil, 7 (9%) and others, 2 (3%). The sildenafil group can be sub-categorized into sulphonamide-bonded (24, 48%), acetyl-bonded (11, 22%), carbonyl or thiocarbonyl-bonded (8, 16%) and other types (7, 14%) based on the functional group linked to pyrazolopyrimidine-one moieties. Meanwhile, analogues of tadalafil have become popularly found as adulterants in dietary supplements like beverages and herbal extracts from 2015 to 2016...
August 9, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28893896/sildenafil-during-pregnancy-a-preclinical-meta-analysis-on-fetal-growth-and-maternal-blood-pressure
#9
Nina D Paauw, Fieke Terstappen, Wessel Ganzevoort, Jaap A Joles, Hendrik Gremmels, A Titia Lely
Sildenafil is a new approach to treat fetal growth restriction (FGR) and preeclampsia. We performed a systematic meta-analysis to evaluate effects of sildenafil. Our search identified 22 animal studies (mouse, rat, rabbit, sheep, and guinea pigs) and 2 human randomized controlled trials. Data were pooled using ratio of means and mean differences with 95% confidence intervals for fetal growth and maternal blood pressure, respectively. Meta-regression analyses were performed for study-related factors that might affect efficacy of sildenafil, including the model used (healthy pregnancy versus FGR/preeclampsia) and route of administration...
September 11, 2017: Hypertension
https://www.readbyqxmd.com/read/28892218/quality-of-erections-by-age-group-in-men-with-erectile-dysfunction
#10
Jed C Kaminetsky, Vera Stecher, Li-Jung Tseng
AIMS: The aim of this study was to assess erection quality with sildenafil vs placebo and adverse events (AEs) according to age (≤45, 46-55 and ≥56 years) in 997 men with erectile dysfunction (ED) using pooled data from four randomized, double-blind, placebo-controlled, flexible-dose trials. METHODS: The trials included 6- to 10-week treatment periods. The starting sildenafil dose was 50 mg, taken ~1 hour before sexual activity but not more than once daily, with subsequent adjustment to 100 or 25 mg based on efficacy and safety...
September 11, 2017: International Journal of Clinical Practice
https://www.readbyqxmd.com/read/28891448/a-special-focus-on-selexipag-treatment-of-pulmonary-arterial-hypertension
#11
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/28885747/palladium-catalyzed-2-2-2-trifluoroethoxylation-of-aromatic-and-heteroaromatic-chlorides-utilizing-borate-salt-and-the-synthesis-of-trifluoro-analog-of-sildenafil
#12
Bálint Pethő, Márton Zwillinger, János Csenki, Anna Káncz, Balázs Krámos, Judit Müller, György Tibor Balogh, Zoltán Novák
A simple and convenient method was developed for the introduction of 2,2,2-trifluoroethoxy group to various aromatic and heteroaromatic systems. The novel process utilizes aromatic chlorides as substrates, and tetrakis(2,2,2-trifluoroethoxy) borate salt as an inexpensive and readily available fluoroalkoxy source in a palladium-catalyzed cross coupling reaction. The power of the developed methodology was demonstrated in the synthesis of fluorous derivative of Sildenafil.
September 8, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28884903/long-term-follow-up-of-lymphatic-malformations-in-children-treated-with-sildenafil
#13
Joanna H Tu, Elidia Tafoya, Michael Jeng, Joyce M Teng
BACKGROUND/OBJECTIVES: Lymphatic malformations (LMs) are challenging to treat. Reports on the benefits of sildenafil for LM management have been mixed. This study evaluated long-term clinical outcomes of pediatric LM patients after sildenafil treatment. METHODS: A retrospective chart review was performed on pediatric LM patients treated with sildenafil in the past 5 years. Patients were also contacted to complete a survey of comprehensive questions about their LM after sildenafil and subsequent interventions...
September 2017: Pediatric Dermatology
https://www.readbyqxmd.com/read/28884212/routine-sildenafil-does-not-improve-clinical-outcomes-after-fontan-operation
#14
J Leslie Gaddis Collins, Mark A Law, Santiago Borasino, W Clinton Erwin, David C Cleveland, Jeffrey A Alten
Fontan operation can be complicated by persistent chest tube output (CTO) leading to prolonged hospital length of stay (LOS). Postoperative sildenafil administration has been shown to improve clinical outcomes in selected patients after Fontan. We initiated a practice change utilizing intravenous (IV) sildenafil in early postoperative period in all patients undergoing Fontan operation with aim to decrease LOS and CTO. Nineteen patients (February 2014-May 2016) received 0.35 mg/kg sildenafil IV (three doses) followed by enteral, 1 mg/kg every eight hours until hospital discharge...
September 7, 2017: Pediatric Cardiology
https://www.readbyqxmd.com/read/28883919/a-case-of-klinefelter-syndrome-with-hypersexual-desire
#15
Kingsley Okolie, Sumathy Perampalam, Anthony Barker, Christopher J Nolan
Klinefelter syndrome (KS) is a chromosomal disorder affecting males, with the typical karyotype of 47,XXY due to a supernumerary X chromosome, which causes progressive testicular failure resulting in androgen deficiency and infertility. Despite it being the most common sex chromosomal disorder, its diagnosis is easily missed. In addition to its classical clinical features of tall stature, gynaecomastia, small testes, and symptoms and signs of hypogonadism including infertility, KS is also often associated with neurocognitive, behavioural and psychiatric disorders...
2017: Endocrinology, Diabetes & Metabolism Case Reports
https://www.readbyqxmd.com/read/28874133/sildenafil-dosed-concomitantly-with-bosentan-for-adult-pulmonary-arterial-hypertension-in-a-randomized-controlled-trial
#16
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/28871716/the-influence-of-eruca-sativa-arugula-on-pharmacokinetics-of-sildenafil-in-rats
#17
Eyad Mallah, Soadad Saleh, Walid Abu Rayyan, Wael Abu Dayyih, Feras Darwish Elhajji, Mohammed Mima, Riad Awad, Tawfiq Arafat
OBJECTIVES: A drug like Sildenafil is commonly used for the treatment of erectile dysfunction. Eruca sativa is known as a garden plant used in folk medicine to enhance the sexual desire in males. Nevertheless, the interaction of Sildenafil and Eruca sativa was not studied. In the current study, we aimed to examine the influence of Eruca sativa on Sildenafil pharmacokinetics in rats. STUDY DESIGN: A crossover experiment with washout period of two weeks was conducted...
August 5, 2017: Neuro Endocrinology Letters
https://www.readbyqxmd.com/read/28868518/associations-of-%C3%AE-thalassemia-and-bcl11a-with-stroke-in-nigerian-united-states-and-united-kingdom-sickle-cell-anemia-cohorts
#18
Santosh L Saraf, Titilola S Akingbola, Binal N Shah, Chinedu A Ezekekwu, Omowunmi Sonubi, Xu Zhang, Lewis L Hsu, Mark T Gladwin, Roberto F Machado, Richard S Cooper, Victor R Gordeuk, Bamidele O Tayo
Alpha-thalassemia and the BCL11A rs1427407 T allele are commonly observed in sickle cell anemia (SCA) patients and are associated with reduced hemolysis and higher hemoglobin F levels, respectively. We investigated whether a high-risk genetic profile, defined as SCA patients who did not inherit either α-thalassemia or the BCL11A rs1427407 T allele, had stronger associations with clinical and laboratory variables than the individual genetic components in the University of Ibadan cohort (n=249). We then replicated our findings in SCA cohorts from the University of Illinois at Chicago (UIC)(n=260) and Walk-Treatment of Pulmonary Hypertension and Sickle cell disease with Sildenafil Therapy (Walk-PHaSST)(n=387)...
April 25, 2017: Blood Advances
https://www.readbyqxmd.com/read/28860509/age-related-differences-in-responsiveness-to-sildenafil-and-tamsulosin-are-due-to-myogenic-smooth-muscle-tone-in-the-human-prostate
#19
Sophie N Lee, Basu Chakrabarty, Brad Wittmer, Melissa Papargiris, Andrew Ryan, Mark Frydenberg, Nathan Lawrentschuk, Ralf Middendorff, Gail P Risbridger, Stuart J Ellem, Betty Exintaris
Lower urinary tract symptoms (LUTS) due to Benign Prostatic Hyperplasia (BPH) are highly prevalent in older men, having a profound impact on patient quality of life. Current therapeutics for BPH/LUTS target neurogenic smooth muscle tone, but response is unpredictable and many patients fail to respond. Spontaneous myogenic tone is another component of smooth muscle contractility that is uncharacterized in human prostate. To better understand and improve the predictability of patient response, we defined myogenic contractility using human prostate specimens and examined the effect of existing therapeutics...
August 31, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28845950/-pde-5-inhibitors-patients-preferences
#20
E A Efremov, E V Kasatonova, Ya I Melnik, A A Nikushina
To date, multidisciplinary approach is commonly used to treat erectile dysfunction (ED), and the first line of ED pharmacotherapy, despite its multiple causes, is phosphodiesterase inhibitors of type 5 (PDE-5). They are considered an effective and well tolerated treatment option [1-4]. Concurrently, sildenafil has the largest evidence base for efficacy and safety [5]. The satisfaction of patients with ED therapy is a complex and personal matter, and there are no clearly established and reliable criteria for showing preferences when choosing a PDE-5...
July 2017: Urologii︠a︡
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