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https://www.readbyqxmd.com/read/28090294/the-effects-of-pulmonary-vasodilating-agents-on-right-ventricular-parameters-in-severe-group-3-pulmonary-hypertension-a-pilot-study
#1
Takahiro Sato, Ichizo Tsujino, Ayako Sugimoto, Toshitaka Nakaya, Taku Watanabe, Hiroshi Ohira, Masaru Suzuki, Satoshi Konno, Noriko Oyama-Manabe, Masaharu Nishimura
Pulmonary arterial hypertension (PAH)-approved vasodilators improve right ventricular (RV) function in patients with PAH. However, whether PAH-approved drugs ameliorate RV morphology and function in lung disease-associated pulmonary hypertension (lung-PH) remains unclear. We aimed to prospectively evaluate the changes in RV volume and ejection fraction (RVEF) in 14 consecutive severe lung-PH patients treated with PAH-approved vasodilators. Severe lung-PH was defined as a mean pulmonary arterial pressure (MPAP) of ≥35 mmHg or an MPAP of ≥25 mmHg with a cardiac index (L/min/m(2)) of <2...
December 2016: Pulmonary Circulation
https://www.readbyqxmd.com/read/28088782/pde5-inhibitors-enhance-the-lethality-of-pemetrexed-sorafenib
#2
Laurence Booth, Jane L Roberts, Andrew Poklepovic, Paul Dent
The combination of pemetrexed and sorafenib has significant clinical activity against a wide variety of tumor types in patients and the present studies were performed to determine whether sildenafil enhances the killing potential of [pemetrexed + sorafenib]. In multiple genetically diverse lung cancer cell lines, sildenafil enhanced the lethality of [pemetrexed + sorafenib]. The three-drug combination reduced the activities of AKT, mTOR and STAT transcription factors; increased the activities of eIF2α and ULK-1; lowered the expression of MCL-1, BCL-XL, thioredoxin and SOD2; and increased the expression of Beclin1...
January 9, 2017: Oncotarget
https://www.readbyqxmd.com/read/28067999/evaluation-of-pharmacokinetic-interactions-between-lesinurad-a-new-selective-urate-reabsorption-inhibitor-and-cyp-enzyme-substrates-sildenafil-amlodipine-tolbutamide-and-repaglinide
#3
Michael Gillen, Chun Yang, David Wilson, Shakti Valdez, Caroline Lee, Bradley Kerr, Zancong Shen
Lesinurad is a selective uric acid reabsorption inhibitor approved for the treatment of hyperuricemia associated with gout in combination with xanthine oxidase inhibitors. In vitro assays indicate that lesinurad is an inducer of CYPs in the order CYP3A > CYP2C8 > CYP2C9 > CYP2C19 > CYP2B6 and an inhibitor of CYP2C8 and CYP2C9. To investigate the drug interaction potential of lesinurad, clinical drug interaction studies were conducted. Open-label studies in volunteers investigated the effects of single-/multiple-dose lesinurad on the pharmacokinetics of sildenafil and amlodipine (CYP3A4 induction), tolbutamide (CYP2C9 inhibition/induction), and repaglinide (CYP2C8 inhibition/induction)...
January 9, 2017: Clinical Pharmacology in Drug Development
https://www.readbyqxmd.com/read/28060942/white-cgmp-interaction-promotes-fast-locomotor-recovery-from-anoxia-in-adult-drosophila
#4
Chengfeng Xiao, R Meldrum Robertson
Increasing evidence indicates that the white (w) gene in Drosophila possesses extra-retinal functions in addition to its classical role in eye pigmentation. We have previously shown that w+ promotes fast and consistent locomotor recovery from anoxia, but how w+ modulates locomotor recovery is largely unknown. Here we show that in the absence of w+, several PDE mutants, especially cyclic guanosine monophosphate (cGMP)-specific PDE mutants, display wildtype-like fast locomotor recovery from anoxia, and that during the night time, locomotor recovery was light-sensitive in white-eyed mutant w1118, and light-insensitive in PDE mutants under w1118 background...
2017: PloS One
https://www.readbyqxmd.com/read/28057946/ismp-adverse-drug-reactions-sildenafil-induced-erythema-multiforme-acute-liver-injury-due-to-febuxostat-intravenous-acetaminophen-induced-acute-hepatotoxicity-acute-transient-myopia-induced-by-zanamivir-lidocaine-induced-hoigne-syndrome
#5
Michael A Mancano
The purpose of this feature is to heighten awareness of specific adverse drug reactions (ADRs), discuss methods of prevention, and promote reporting of ADRs to the US Food and Drug Administration's (FDA's) MedWatch program (800-FDA-1088). If you have reported an interesting, preventable ADR to MedWatch, please consider sharing the account with our readers. Write to Dr. Mancano at ISMP, 200 Lakeside Drive, Suite 200, Horsham, PA 19044 (phone: 215-707-4936; e-mail: mmancano@temple.edu). Your report will be published anonymously unless otherwise requested...
December 2016: Hospital Pharmacy
https://www.readbyqxmd.com/read/28053559/systemic-lupus-erythematosus-and-pulmonary-arterial-hypertension-links-risks-and-management-strategies
#6
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/28052870/phosphodiesterase-5-inhibition-ameliorates-angiotensin-ii-dependent-hypertension-and-renal-vascular-dysfunction
#7
Manuel Thieme, Sema Hayriye Sivritas, Evanthia Mergia, Sebastian Alexander Potthoff, Guang Yang, Lydia Hering, Katharina Grave, Henning Hoch, Lars Christian Rump, Johannes Stegbauer
Changes in renal hemodynamics have a major impact on blood pressure (BP). Angiotensin (Ang) II has been shown to induce vascular dysfunction by interacting with phosphodiesterases (PDE)1 and PDE5. The predominant PDE isoform responsible for renal vascular dysfunction in hypertension is unknown. Here, we measured effects of PDE5-(sildenafil) or PDE1-(vinpocetine) inhibition on renal blood flow (RBF), BP and renal vascular function in normotensive and hypertensive mice. During acute short-term Ang II infusion, sildenafil decreased BP and increased RBF in C57BL/6 (WT) mice...
January 4, 2017: American Journal of Physiology. Renal Physiology
https://www.readbyqxmd.com/read/28042638/black-lung-persistent-pulmonary-hypertension-of-the-newborn-saudi-experience-with-sildenafil-and-nitric-oxide
#8
AbdulRahman M Alnemri
To determine the clinical presentation, risk factors, diagnosis, and treatment outcome of Saudi infants with black lung persistent pulmonary hypertension of the newborn (PPHN). Methods: This is a retrospective review of all neonates with PPHN presented to the Armed Force Hospital Southern Region, Kingdom of Saudi Arabia from January 2012 to December 2014. Results: Ten term and near term infants presented with PPHN were included. Maternal diabetes and Down syndrome were the most common identified risk factors for PPHN in the study group...
January 2017: Saudi Medical Journal
https://www.readbyqxmd.com/read/28033452/electrophysiologic-effects-of-very-high-dose-sildenafil
#9
Hoon Dong Kim, Jee Ho Chang, Yoon Kyung Kim, Young-Hoon Ohn
No abstract text is available yet for this article.
December 29, 2016: JAMA Ophthalmology
https://www.readbyqxmd.com/read/28025967/a-single-dose-randomized-open-label-cross-over-bioequivalence-study-of-sildenafil-citrate-tablets-in-healthy-chinese-volunteers%C3%A2
#10
Dai Li, Yu-Lu Wang, Su-Mei Xu, Dan Li, Xiao-Min Li, Jing Pan, Ping-Sheng Xu
OBJECTIVE: The present study was designed to evaluate the bioequivalence of a newly developed sildenafil citrate tablet 50 mg (Jinge®, Test) and a marketed counterpart (Viagra®, 100 mg, Reference) in healthy adult male Chinese volunteers. METHODS: This single-dose, randomized, open-label, four-period, and two-treatment self-crossover study included two parts: fasting and postprandial studies. In each part of the study, the subjects were randomly assigned to receive test or reference products (100 mg sildenafil) in a 1 : 1 ratio, and then received the alternative products, following a 1-week washout period...
December 27, 2016: International Journal of Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28018821/pimobendan-in-chronic-right-heart-failure-in-a-left-ventricular-assist-device-patient
#11
Maximilian Kreibich, Michael Berchtold-Herz, Friedhelm Beyersdorf, Georg Trummer
We report the case of a 76-year-old patient who developed chronic right heart failure 1 year after left ventricular assist device implantation due to ischemic cardiomyopathy. Initial recompensation was achieved through dobutamin, sildenafil, and levosimendan treatment. Yet, discharge was successful only after the off-label use of the oral calcium sensitizer pimobendan. Ten months after discharge, the patient presents with no clinical signs of right heart failure and significantly improved right heart function without any impairment in quality of life...
December 2016: Thoracic and Cardiovascular Surgeon Reports
https://www.readbyqxmd.com/read/28017777/the-cardioprotective-effect-of-sildenafil-is-mediated-by-the-activation-of-malate-dehydrogenase-and-an-increase-in-the-malate-aspartate-shuttle-in-cardiomyocytes
#12
Gevi Federica, Campolo Federica, Naro Fabio, Zolla Lello
Recent evidence has shown showed the cardioprotective effect of PDE5 inhibition in myocardial ischemia/reperfusion injury, heart failure and cardiac hypertrophy. To investigate the biochemical changes that occur during PDE5 inhibition in cardiac cells, this study assessed the metabolic profile of the HL1 cell line, a murine atrial cell line with adult cardiomyocyte properties. After one hour of treatment with sildenafil, glycolysis was moderately but selectively stimulated, unlike the pentose phosphate pathway and the Krebs cycle...
December 22, 2016: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28013386/potentiation-of-the-no-cgmp-pathway-and-blood-flow-responses-during-dynamic-exercise-in-healthy-humans
#13
Jacqueline K Limberg, Katherine R Malterer, J Mikhail Kellawan, William G Schrage, Brad W Wilkins, Wayne T Nicholson, John H Eisenach, Michael J Joyner, Timothy B Curry
PURPOSE: Previous work has shown nitric oxide (NO) contributes to ~15% of the hyperemic response to dynamic exercise in healthy humans. This NO-mediated vasodilation occurs, in part, via increases in intracellular cyclic guanosine monophosphate (cGMP), which is catabolized by phosphodiesterase. We sought to examine the effect of phosphodiesterase-5 (PDE-5) inhibition on forearm blood flow (FBF) responses to dynamic handgrip exercise in healthy humans and the role of NO. We hypothesized exercise hyperemia would be augmented by sildenafil citrate (SDF, PDE-5 inhibitor)...
December 24, 2016: European Journal of Applied Physiology
https://www.readbyqxmd.com/read/28013355/effect-of-sildenafil-on-the-activity-of-some-antidepressant-drugs-and-electroconvulsive-shock-treatment-in-the-forced-swim-test-in-mice
#14
Katarzyna Socała, Dorota Nieoczym, Elżbieta Wyska, Piotr Wlaź
Sildenafil, a potent and selective inhibitor of phosphodiesterase type 5, is used clinically to treat erectile dysfunction and pulmonary arterial hypertension. It is often taken by patients suffering from depression and receiving antidepressant drug treatment. However, its influence on the efficacy of antidepressant treatment was not sufficiently studied. Therefore, the aim of the present study was to investigate the influence of sildenafil on the anti-immobility action of several antidepressant drugs (i.e...
December 24, 2016: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28011207/quantifying-barriers-to-improvement-of-treatment-satisfaction-in-men-with-erectile-dysfunction-use-of-person-item-maps
#15
Andrew G Bushmakin, Joseph C Cappelleri, Vera Stecher, Tom F Lue
INTRODUCTION: Patient-reported outcomes are a valuable tool used to gauge treatment satisfaction in different conditions, including erectile dysfunction (ED). AIM: To use person-item maps to quantify barriers to improvement of treatment satisfaction in men with ED. METHODS: Men 18 to 65 years old with documented ED received sildenafil 50 mg, sildenafil 100 mg, or placebo for 8 weeks in a double-blinded manner. Post hoc analyses were conducted on Erectile Dysfunction Inventory of Treatment Satisfaction (EDITS) data (11 items rating treatment satisfaction; each item score range = 0-4)...
January 2017: Journal of Sexual Medicine
https://www.readbyqxmd.com/read/28008796/isolation-and-identification-of-a-novel-sildenafil-analogue-adulterant-in-herbal-products
#16
Ya-Tze Lin, Yen-Chun Huang, Hui-Chun Lee, Chen-Hsiang Liao, Yun-Lian Lin, Chia-Fen Tsai, Hwei-Fang Cheng
A novel sildenafil analogue found in herbal products by a routine drug-adulteration screening programme was isolated by column chromatography. On the basis of extensive 1D- and 2D-nuclear magnetic resonance (NMR) spectroscopy and mass spectral analysis, the structure of a new compound YJ-07 was established as 1-[4-ethoxy-3-(6,7-dihydro-1-methyl-7-oxo-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-5-yl) benzenesulfonamide. It common name is aminosildenafil.
December 23, 2016: Food Additives & Contaminants. Part A, Chemistry, Analysis, Control, Exposure & Risk Assessment
https://www.readbyqxmd.com/read/28007723/stability-of-sildenafil-in-combination-with-heparin-and-dopamine
#17
Yao Luu, Jim Thigpen, Stacy D Brown
PURPOSE: The stability of sildenafil in combination with heparin and dopamine was evaluated. METHODS: A stability-indicating high-performance liquid chromatography method with ultraviolet detection was developed for sildenafil citrate and validated. The method was applied to the investigation of sildenafil alone, sildenafil with heparin, sildenafil with dopamine, and sildenafil with heparin and with dopamine, all in 5% dextrose injection at room temperature and under refrigeration for 30 days...
January 1, 2017: American Journal of Health-system Pharmacy: AJHP
https://www.readbyqxmd.com/read/27999095/a-case-report-of-fatal-desmethyl-carbodenafil-toxicity
#18
Erica L Bakota, Anna T Kelly, Jeffrey P Walterscheid, Darshan R Phatak
We present the case report of a 34-year-old Hispanic male who was found unresponsive in the carport of his residence. Surveillance video footage from a security camera showed that he collapsed as he was walking to his vehicle. The decedent had no medical history and no history of illicit drug use. Initial toxicology testing revealed no alcohol or illicit drugs. Autopsy findings indicated a need for additional toxicological analysis due to a lack of trauma and the paucity of pathophysiologically significant natural disease...
December 19, 2016: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/27995418/the-effects-of-sildenafil-citrate-on-urinary-podocin-and-nephrin-mrna-expression-in-an-l-name-model-of-pre-eclampsia
#19
Sooraj Baijnath, Saravanakumar Murugesan, Irene Mackraj, Prem Gathiram, Jagidesa Moodley
We investigated the effects of sildenafil citrate (SC) on podocyturia in N (ω)-nitro-L-arginine methyl ester hydrochloride (L-NAME) model of pre-eclampsia (PE). One hundred and twenty Sprague-Dawley rats (SDR) were divided into five groups like pregnant control (PC), early-onset PE (EOPE), late-onset PE(LOPE), early and late-onset PE with SC-treated groups [EOPE (SC); LOPE (SC)]. PE was induced in SDR by oral administration of L-NAME in drinking water for 4-8 days for EOPE and 8-14 day for LOPE. The blood pressure, urine volume and total urine protein were increased in EOPE and LOPE groups when compared to PC, and all the above parameters decreased in EOPE (SC) and LOPE (SC) groups when compared to EOPE and LOPE groups, respectively...
December 19, 2016: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/27989487/effect-of-bkca-channel-opener-ldd175-on-erectile-function-in-an-in%C3%A2-vivo-diabetic-rat-model
#20
Hyun Hwan Sung, Su Jeong Kang, Mee Ree Chae, Hye Kyung Kim, Jong Kwan Park, Chul Young Kim, Sung Won Lee
INTRODUCTION: The development of novel therapeutic options is imperative in patients with erectile dysfunction, especially those non-responsive to phosphodiesterase type 5 inhibitors. LDD175, a potent BKCa channel opener, has a relaxation effect on the in vitro cavernosal smooth muscle strip. AIM: To investigate the effect of LDD175 on erectile function using in vivo animal disease model. METHODS: Male Sprague-Dawley rats were assigned to a normal control group and seven diabetic groups: diabetic control, sildenafil (1 and 5 mg/kg), LDD175 (5 and 10 mg/kg), LDD175 5 mg/kg plus sildenafil 1 mg/kg, and LDD175 10 mg/kg plus tetraethylammonium...
December 15, 2016: Journal of Sexual Medicine
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