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Phosphodiesterase 5 inhibitors

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https://www.readbyqxmd.com/read/28442892/bioequivalence-study-of-a-new-sildenafil-100-mg-orodispersible-film-compared-to-the-conventional-film-coated-100-mg-tablet-administered-to-healthy-male-volunteers
#1
Milko Radicioni, Chiara Castiglioni, Andrea Giori, Irma Cupone, Valeria Frangione, Stefano Rovati
A new orodispersible film formulation of the phosphodiesterase type 5 inhibitor, sildenafil, has been developed to examine the advantages of an orally disintegrating film formulation and provide an alternative to the current marketed products for the treatment of erectile dysfunction. The pharmacokinetics of the sildenafil 100 mg orodispersible film (IBSA) was compared to that of the conventional marketed 100 mg film-coated tablet (Viagra(®)) after single-dose administration to 53 healthy male volunteers (aged 18-51 years) in a randomized, open, two-way crossover bioequivalence study...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28438557/the-isozyme-selective-phosphodiesterase-4-inhibitor-abi-4-attenuates-the-effects-of-lipopolysaccharide-in-human-cells-and-rodent-models-of-peripheral-and-cns-inflammation
#2
Joseph R Hedde, Ashley N Hanks, Christopher J Schmidt, Zoë A Hughes
Inhibitors of phosphodiesterase-4 (PDE4) have been approved for the treatment of inflammatory disorders, but are associated with dose-limiting nausea and vomiting. These side effects are hypothesized to be mediated by inhibition of the PDE4D isozyme. Here we demonstrate the anti-inflammatory effects of the novel brain penetrant PDE4D-sparing PDE4 inhibitor, ABI-4. ABI-4 was a potent (EC50 ∼14 nM) inhibitor of lipopolysaccharide (LPS) induced TNF-α release from mouse microglia and human PBMCs. ABI-4 (0.32 mg/kg) blocked LPS-induced release of pro-inflammatory cytokines (TNF-α, IL-1β, IL-6) in blood and brain of mice...
April 21, 2017: Brain, Behavior, and Immunity
https://www.readbyqxmd.com/read/28436147/rapid-detection-of-six-phosphodiesterase-type-5-enzyme-inhibitors-in-health-care-products-using-thin-layer-chromatography-and-surface-enhanced-raman-spectroscopy-combined-with-bp-neural-network
#3
Xiaopeng Hu, Guozhen Fang, Ailing Han, Yunpeng Fu, Rui Tong, Shuo Wang
A novel facile method for the detection of the phosphodiesterase type 5 enzyme inhibitors added illegally into health products was established using thin-layer chromatography and surface enhanced Raman spectroscopy combined with BP neural network. When the detecting conditions were optimized in detail, a repetitive adding procedure of silver colloids with the total amount keeping constant was used to improve the enhancement effect of surface enhanced Raman spectroscopy. According to the main Raman peaks and the retention factor of analyte, the data predictive model was established...
April 24, 2017: Journal of Separation Science
https://www.readbyqxmd.com/read/28434676/meta-analysis-of-results-of-testosterone-therapy-on-sexual-function-based-on-international-index-of-erectile-function-scores
#4
Giovanni Corona, Giulia Rastrelli, Abraham Morgentaler, Alessandra Sforza, Edoardo Mannucci, Mario Maggi
CONTEXT: The interpretation of available clinical evidence related to the effect of testosterone (T) treatment (TTh) on sexual function has been inconsistent, in part due to the use of different and self-reported measures to assess outcomes. The International Index of Erectile Function (IIEF) is the most frequently used validated tool to assess male sexual function. OBJECTIVE: To perform a meta-analysis of available data evaluating the effect of TTh on male sexual function using IIEF as the primary outcome...
April 20, 2017: European Urology
https://www.readbyqxmd.com/read/28432317/psiguajadials-a-k-unusual-psidium-meroterpenoids-as-phosphodiesterase-4-inhibitors-from-the-leaves-of-psidium-guajava
#5
Gui-Hua Tang, Zhen Dong, Yan-Qiong Guo, Zhong-Bin Cheng, Chu-Jun Zhou, Sheng Yin
Bioassay-guided fractionation of the ethanolic extract of the leaves of Psidium guajava led to the isolation of 11 new Psidium meroterpenoids, psiguajadials A-K (1-11), along with 17 known ones (12-28). Their structures and absolute configurations were elucidated by spectroscopic methods and comparison of experimental and calculated ECD. Compounds 1 and 2 represent two unprecedented skeletons of 3,5-diformyl-benzyl phloroglucinol-coupled sesquiterpenoid, while 3 is the first example of Psidium meroterpenoids coupling via an oxepane ring...
April 21, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28431996/comparison-of-silodosin-monotherapy-versus-silodosin-with-tadalafil-add-on-therapy-in-patients-with-benign-prostatic-hyperplasia
#6
Takashi Yoshida, Hidefumi Kinoshita, Seiji Shimada, Makoto Taguchi, Tadashi Matsuda
OBJECTIVE: To evaluate the efficacy and safety of add-on therapy with the phosphodiesterase type 5 inhibitor tadalafil for patients with lower urinary tract symptoms secondary to benign prostatic hyperplasia (LUTS/BPH) treated with the α1-adrenoceptor blocker silodosin. METHODS: We analyzed 103 patients with LUTS/BPH with an International Prostate Symptom Score (IPSS) of >8 after ≥4 weeks of silodosin treatment from April 2016 through December 2016 at Kori Hospital...
April 18, 2017: Urology
https://www.readbyqxmd.com/read/28425346/ambrisentan-a-review-of-its-use-in-pulmonary-arterial-hypertension
#7
Belinda N Rivera-Lebron, Michael G Risbano
Pulmonary arterial hypertension (PAH) is a progressive disease defined by an elevation in pulmonary arterial pressure that can lead to right heart failure and death. Ambrisentan is a selective endothelin receptor antagonist approved for the treatment of idiopathic, heritable PAH and connective tissue disease-associated PAH. Ambrisentan has been shown to improve exercise capacity and hemodynamics with an acceptable side-effect profile. It has also proven to be safely used in combination with other PAH-specific medications, especially with phosphodiesterase-5 inhibitors...
April 1, 2017: Therapeutic Advances in Respiratory Disease
https://www.readbyqxmd.com/read/28420826/efficacy-and-safety-of-an-orally-administered-selective-prostacyclin-receptor-agonist-selexipag-in-japanese-patients-with-pulmonary-arterial-hypertension
#8
Nobuhiro Tanabe, Satoshi Ikeda, Nobuhiro Tahara, Keiichi Fukuda, Masaru Hatano, Hiroshi Ito, Tomotaka Nakayama, Toshihisa Anzai, Akiyoshi Hashimoto, Teruo Inoue, Kouji Kajinami, Yasuki Kihara, Hideyuki Kinoshita, Koichiro Kuwahara, Toyoaki Murohara, Osamu Okazaki, Satoshi Sakai, Toru Satoh, Yutaka Takeda, Yasuchika Takeishi, Mitsugu Taniguchi, Hiroshi Watanabe, Takeshi Yamamoto, Keiko Yamauchi-Takihara, Koichiro Yoshioka, Shigetake Sasayama
BACKGROUND: Selexipag is an orally available prostacyclin receptor (IP receptor) agonist with a non-prostanoid structure. In this open-label Phase II trial, the efficacy and safety of selexipag in Japanese patients with pulmonary arterial hypertension (PAH) is examined.Methods and Results:Selexipag was administered at 200 μg twice daily and titrated up to 1,600 μg by increments of 200 μg in 37 subjects to reach the individual maximum tolerated dose. At 16 weeks, in 33 patients comprising the per-protocol set, the pulmonary vascular resistance (PVR; primary endpoint) decreased from 683...
April 18, 2017: Circulation Journal: Official Journal of the Japanese Circulation Society
https://www.readbyqxmd.com/read/28419939/the-5-ht4-receptor-agonist-prucalopride-does-not-facilitate-cholinergic-neurotransmission-in-circular-and-longitudinal-smooth-muscle-preparations-of-equine-mid-jejunum
#9
Romain Adelin Lefebvre, Chana Callens, Inge Van Colen, Catherine John Ghislaine Delesalle
BACKGROUND: Postoperative ileus (POI) remains an important cause of death in horses. The recently developed selective 5-HT4 receptor agonists such as prucalopride target 5-HT4 receptors on myenteric cholinergic neurons to enhance acetylcholine release and GI motility. No clearcut in vitro evaluation whether highly selective 5-HT4 receptor agonists enhance submaximal cholinergic neurotransmission towards the muscle layer has been performed in horses. OBJECTIVES: To identify functional 5-HT4 receptors in equine jejunum...
April 8, 2017: Research in Veterinary Science
https://www.readbyqxmd.com/read/28414103/apoptosis-induction-of-poly-s-nitrosated-human-serum-albumin-in-resistant-solid-tumor-under-hypoxia-can-be-restored-by-phosphodiesterase-5-inhibition
#10
Mayumi Ikeda, Yu Ishima, Victor T G Chuang, Tsuyoshi Ikeda, Ryo Kinoshita, Hiroshi Watanabe, Tatsuhiro Ishida, Masaki Otagiri, Toru Maruyama
Poly-S-nitrosated human serum albumin (Poly-SNO-HSA) delivered and accumulated nitric oxide (NO) in tumors and induces apoptosis. Tumor hypoxia is strongly associated with malignant progression and tumor resistance to therapy. In this study, we examined the cytotoxic effect of Poly-SNO-HSA under hypoxia on the murine colon 26 adenocarcinoma (C26) cells in vitro and in vivo. Under hypoxia, at about 4 times LD50 dose of Poly-SNO-HSA in vitro, the reactive oxygen species production was hindered but apoptotic cells were induced via cGMP pathway as the effect was suppressed by a soluble guanylate cyclase inhibitor, NS2028...
April 13, 2017: Nitric Oxide: Biology and Chemistry
https://www.readbyqxmd.com/read/28408390/lidocaine-prilocaine-spray-for-premature-ejaculation
#11
(no author information available yet)
Although premature ejaculation is the most common ejaculation problem, it is poorly understood and currently has no standard definition.(1) Typically, it involves reduced time to ejaculation, inability to control or delay ejaculation and associated distress.(1-5) Treatments that have been assessed include psychosexual counselling, antidepressants (e.g. selective serotonin reuptake inhibitors), phosphodiesterase type-5 inhibitors, tramadol and topical anaesthetic agents (e.g. lidocaine/prilocaine cream). A new formulation (cutaneous spray) of lidocaine/prilocaine (Fortacin-Plethora Solutions Ltd...
April 2017: Drug and Therapeutics Bulletin
https://www.readbyqxmd.com/read/28406621/discovery-of-selective-phosphodiesterase-1-inhibitors-with-memory-enhancing-properties
#12
Brian Dyck, Bryan Branstetter, Tawfik Gharbaoui, Andrew R Hudson, J Guy Breitenbucher, Laurent Gomez, Iriny Botrous, Tami Marrone, Richard Barido, Charles K Allerston, E Peder Cedervall, Rui Xu, Vandana Sridhar, Ryan Barker, Kathleen Aertgeerts, Kara Schmelzer, David Neul, Dong Lee, Mark Eben Massari, Carsten B Andersen, Kristen Sebring, Xianbo Zhou, Robert Petroski, James Limberis, Martin Augustin, Lawrence E Chun, Thomas E Edwards, Marco Peters, Ali Tabatabaei
A series of potent thienotriazolopyrimidinone-based PDE1 inhibitors was discovered. X-ray crystal structures of example compounds from this series in complex with the catalytic domain of PDE1B and PDE10A were determined, allowing optimization of PDE1B potency and PDE selectivity. Reduction of hERG affinity led to greater than a 3000-fold selectivity for PDE1B over hERG. 6-(4-Methoxybenzyl)-9-((tetrahydro-2H-pyran-4-yl)methyl)-8,9,10,11-tetrahydropyrido[4',3':4,5]thieno[3,2-e][1,2,4]triazolo[1,5-c]pyrimidin-5(6H)-one was identified as an orally bioavailable and brain penetrating PDE1B enzyme inhibitor with potent memory-enhancing effects in a rat model of object recognition memory...
April 13, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28403587/tadalafil-once-daily-narrative-review-of-a-treatment-option-for-female-sexual-dysfunctions-fsd-in-midlife-and-older-women
#13
Chiara Borghi, Lucio Dell'Atti
Female Sexual Disorders (FSD) include a complex, multidimensional, individual experience that can change as an individual age, suggesting that these problems are caused by multiple factors including psychosocial factors, personal relationships, pathologic changes caused by diseases, and pharmacologic influences. Menopause is an important time for middle aged women and postmenopausal physiological changes could have a significant role in the development of FSD. Few is still known about their correct definition and treatment...
March 31, 2017: Archivio Italiano di Urologia, Andrologia
https://www.readbyqxmd.com/read/28398017/differential-effects-of-phosphodiesterase-5-inhibition-in-chronic-cardiac-decompensation-depending-on-the-type-whether-hfref-or-hfpef-of-heart-failure-a-meta-analysis
#14
Renato DE Vecchis, Arturo Cesaro, Carmelina Ariano
INTRODUCTION: According to 2015 ESC/ERS guidelines for the diagnosis and treatment of pulmonary hypertension(PH), no specific drug is currently indicated for PH related to left heart disease( PH-LDH), i.e., the one secondary to left chronic heart failure (CHF), which coincides with the group 2 of the PH classification endorsed by the above-mentioned guidelines. In fact, adoption of therapies that specifically apply for so-called pulmonary arterial hypertension (group 1 of the PH classification) has been regarded as substantially contraindicated in patients with PH- LHD, according to current ESC/ERS guidelines...
April 10, 2017: Minerva Cardioangiologica
https://www.readbyqxmd.com/read/28395997/discontinuation-of-dapoxetine-treatment-in-patients-with-premature-ejaculation-a-2-year-prospective-observational-study
#15
Hyun Jun Park, Nam Cheol Park, Tae Nam Kim, Seung Ryong Baek, Kyung Min Lee, Sangmin Choe
INTRODUCTION: Although dapoxetine is the only oral pharmacologic agent approved for the treatment of premature ejaculation (PE) and is very effective, the discontinuation rate is high. AIM: To assess the discontinuation rate of patients with PE and the reasons for discontinuation in real-world practice. METHODS: In total, 182 consecutive patients were enrolled. Type of PE, self-estimated intravaginal ejaculation latency time, and medical history were evaluated in all patients who also completed the erectile function domain of the International Index of Erectile Function (IIEF)...
April 5, 2017: Sexual Medicine
https://www.readbyqxmd.com/read/28394532/-phosphodiesterase-type-5-inhibitors-in-the-treatment-of-erectile-dysfunction-past-present-and-future
#16
S I Gamidov, R I Ovchinnikov, A Yu Popova, S Kh Izhbaev
This review article describes the differences in efficacy and side effects between available phosphodiesterase type 5 (PDE-5) inhibitors used for treating erectile dysfunction. The most studied PDE-5 inhibitor is sildenafil.
April 2017: Urologii︠a︡
https://www.readbyqxmd.com/read/28379598/sildenafil-associated-hepatoxicity-a-review-of-the-literature
#17
S Graziano, A Montana, S Zaami, M C Rotolo, A Minutillo, F P Busardò, E Marinelli
Sildenafil citrate (Viagra®) is a vasoactive agent available worldwide since 1998 for the treatment of male erectile dysfunction. It is a selective phosphodiesterase type 5-enzyme inhibitor able to potentiate the downstream effects of nitric oxide on smooth muscle relaxation and vasodilation through its effects on the cyclic guanosine monophosphate (c-GMP) pathway in the erectile tissue of the penis. When sildenafil is orally administered, it is rapidly absorbed with a maximum plasma concentration achieved within 1 h and has a terminal half-life of between 3 to 6 h...
March 2017: European Review for Medical and Pharmacological Sciences
https://www.readbyqxmd.com/read/28372960/the-kiel-concept-of-long-term-administration-of-daily-low-dose-sildenafil-initiated-in-the-immediate-post-prostatectomy-period-evaluation-and-comparison-with-the-international-literature-on-penile-rehabilitation
#18
REVIEW
Daniar K Osmonov, Klaus P Jünemann, Andreas Bannowsky
INTRODUCTION: Radical prostatectomy (RP) is the most common definitive invasive treatment option for localized prostate cancer. Although the different surgical procedures-open RP, laparoscopic RP, and robot-assisted laparoscopic RP-do not differ significantly for the results of postoperative erectile dysfunction (ED) and continence, the fear of losing erectile function (EF) is often an important factor for preoperatively sexually active men when deciding for or against a procedure. AIM: To review the available literature on rehabilitation of EF after RP and to evaluate the value of the "Kiel concept" against different strategies of phosphodiesterase type 5 inhibitor (PDE5i) low-dose treatments...
March 31, 2017: Sexual Medicine Reviews
https://www.readbyqxmd.com/read/28359097/a-perspective-on-middle-aged-and-older-men-with-functional-hypogonadism-focus-on-holistic-management
#19
Mathis Grossmann, Alvin M Matsumoto
Context: Middle-aged and older men (≥50 years), especially those who are obese and suffer from comorbidities, not uncommonly present with clinical features consistent with androgen deficiency and modestly reduced testosterone levels. Commonly, such men do not demonstrate anatomical hypothalamic-pituitary-testicular axis pathology but have functional hypogonadism that is potentially reversible. Evidence Acquisition: Literature review from 1970 to October 2016. Evidence Synthesis: Although definitive randomized controlled trials are lacking, evidence suggests that in such men, lifestyle measures to achieve weight loss and optimization of comorbidities, including discontinuation of offending medications, lead to clinical improvement and a modest increase in testosterone...
March 1, 2017: Journal of Clinical Endocrinology and Metabolism
https://www.readbyqxmd.com/read/28357503/small-fibre-neuropathy-in-men-with-type-1-diabetes-and-erectile-dysfunction-a-cross-sectional-study
#20
Shazli Azmi, Maryam Ferdousi, Uazman Alam, Ioannis N Petropoulos, Georgios Ponirakis, Andrew Marshall, Omar Asghar, Hassan Fadavi, Wendy Jones, Mitra Tavakoli, Andrew J M Boulton, Maria Jeziorska, Handrean Soran, Nathan Efron, Rayaz A Malik
AIMS/HYPOTHESIS: The aim of this study was to identify the contribution of small- and large-fibre neuropathy to erectile dysfunction in men with type 1 diabetes mellitus. METHODS: A total of 70 participants (29 without and 41 with erectile dysfunction) with type 1 diabetes and 34 age-matched control participants underwent a comprehensive assessment of large- and small-fibre neuropathy. RESULTS: The prevalence of erectile dysfunction in participants with type 1 diabetes was 58...
March 29, 2017: Diabetologia
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