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Phosphodiesterase 5 inhibitors

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https://www.readbyqxmd.com/read/29220595/dose-dependent-effects-of-tadalafil-and-roflumilast-on-ovalbumin-induced-airway-hyperresponsiveness-in-guinea-pigs
#1
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/29220542/safety-and-efficacy-of-apremilast-through-104-weeks-in-patients-with-moderate-to-severe-psoriasis-who-continued-on-apremilast-or-switched-from-etanercept-treatment-findings-from-the-liberate-study
#2
K Reich, M Gooderham, A Bewley, L Green, J Soung, R Petric, J Marcsisin, J Cirulli, R Chen, V Piguet
BACKGROUND: Apremilast, an oral phosphodiesterase 4 inhibitor, has demonstrated efficacy in patients with moderate to severe psoriasis. OBJECTIVE: To evaluate long-term efficacy and safety of apremilast in biologic-naive patients with moderate to severe plaque psoriasis and safety of switching from etanercept to apremilast in the phase 3b LIBERATE trial. METHODS: Two hundred fifty patients were randomized to placebo, apremilast 30 mg BID, or etanercept 50 mg QW through Week 16; thereafter, all patients continued or switched to apremilast through Week 104 (extension phase)...
December 8, 2017: Journal of the European Academy of Dermatology and Venereology: JEADV
https://www.readbyqxmd.com/read/29216624/sildenafil-viagra%C3%A2-prevents-cox-1-txa2-pathway-mediated-vascular-hypercontractility-in-apoe-mice
#3
Marcos A S Leal, Ananda T Dias, Marcella L Porto, Bruna F Brun, Agata L Gava, Silvana S Meyrelles, José Gil-Longo, Manuel Campos-Toimil, Thiago M C Pereira, Elisardo C Vasquez
BACKGROUND/AIMS: The atherosclerotic apolipoprotein E-deficient (apoE-/-) mouse exhibits impaired vasodilation and enhanced vasoconstriction responsiveness. The objectives of this study were: a) to determine the relative contribution of cyclooxygenases (Cox-1 and Cox-2), thromboxane A2 (TXA2) and endothelin-1 (ET-1) to enhancing vascular hyperresponsiveness in this model of atherosclerosis and b) to investigate the beneficial effects of the phosphodiesterase 5 inhibitor sildenafil on this endothelial dysfunction...
December 7, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/29205161/-low-dose-rate-brachytherapy-in-low-and-middle-risk-prostate-cancer-results-and-impact-on-quality-of-life-with-5-year-follow-up
#4
Felipe Balbontín, Pablo Pizzi, Andrea Canals, Isabel Alliende
Low dose rate brachytherapy (LDR-Br) with radioactive isotopes is a curative treatment and has shown to be comparable for the management of localized prostate cancer (PCa) to more conventional treatments such as radical prostatectomy or external beam radiotherapy, but with fewer side effects. The aim of this study is to show the global, specific and biochemical recurrence-free survival in 193 patients undergoing low dose rate Brachytherapy with permanent implants with iodine 125 and analyze the quality of life impact...
December 2017: Archivos Españoles de Urología
https://www.readbyqxmd.com/read/29202488/acute-tadalafil-administration-increases-plasma-fatty-acids-without-changes-in-the-inflammatory-response-in-healthy-men
#5
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/29201504/effect-of-sildenafil-citrate-in-testosterone-induced-benign-prostate-hyperplasia-rat-model
#6
Selahattin Çalışkan, Muzaffer Oğuz Keleş, Metin İshak Öztürk, Musab Ali Kutluhan, Olgu Enis Tok, Feriha Ercan, Muhammet İhsan Karaman
Objective: Efficacy of treatments for benign prostate hyperplasia (BPH) is limited because the disease has complex etiopathogenesis. Recent studies have demonstrated the presence of phosphodiesterase-5 (PDE-5) receptors in prostate tissue. We investigated efficacy of sildenafil citrate in testosteron - induced BPH in rats. Material and methods: The rats were divided into three groups. Each groups had 7 rats. Group 1 was control group. Testosteron propionate 3 mg/kg/day was injected subcutaneously for two weeks in Group 2...
December 2017: Turkish Journal of Urology
https://www.readbyqxmd.com/read/29201436/therapeutic-benefits-of-phosphodiesterase-5-inhibition-in-chronic-heart-failure-a-meta-analysis
#7
Renato De Vecchis, Arturo Cesaro, Carmelina Ariano
Background: Phosphodiesterase-5 inhibitors (PDE5i) have been shown to be beneficial for patients with pulmonary arterial hypertension. However, several studies would have documented a useful effect of PDE5i even for pulmonary hypertension secondary to left-sided chronic heart failure (CHF). Methods: We performed a meta-analysis including randomized controlled trials (RCTs) which had compared PDE5i (mostly sildenafil) and placebo in CHF patients. Results: Fourteen studies enrolling a total of 928 patients were incorporated in the meta-analysis...
September 2017: Interventional Medicine & Applied Science
https://www.readbyqxmd.com/read/29198514/erectile-dysfunction-medications-and-treatment-for-cardiometabolic-risk-factors-a-pharmacoepidemiologic-study
#8
Sean C Skeldon, Lucy Cheng, Steven G Morgan, Allan S Detsky, S Larry Goldenberg, Michael R Law
BACKGROUND: Erectile dysfunction (ED) can be a sentinel marker for future cardiovascular disease and has been described as providing a "window of curability" for men to receive targeted cardiovascular risk assessment. AIM: To determine whether the prescription of phosphodiesterase type 5 inhibitors (PDE5is) for ED leads to the detection and treatment of previously undiagnosed cardiometabolic risk factors. METHODS: We performed a retrospective population-based cohort study of residents of British Columbia, Canada using linked health care databases from 2004 to 2011...
December 2017: Journal of Sexual Medicine
https://www.readbyqxmd.com/read/29198447/fabrication-and-evaluation-of-magnetic-phosphodiesterase-5-linked-nanoparticles-as-adsorbent-for-magnetic-dispersive-solid-phase-extraction-of-inhibitors-from-chinese-herbal-medicine-prior-to-ultra-high-performance-liquid-chromatography-quadrupole-time-of-flight
#9
Yi Tao, Xianghui Gu, Weidong Li, Baochang Cai
In the present study, the preparation of the magnetic phosphodiesterase-5 linked Fe3O4@ SiO2 nanoparticles was successfully achieved by amide reaction and the magnetic phosphodiesterase-5 linked Fe3O4@SiO2 nanoparticles were evaluated as a new adsorbent for magnetic dispersive solid-phase extraction of ligands from medicinal plant samples before the analysis by UHPLC-Q-TOF/MS. The prepared phosphodiesterase-5 linked Fe3O4@SiO2 nanoparticles were characterized by X-ray diffraction, Fourier transform infrared spectroscopy, transmission electron microscopy, vibration sample magnetometer and potential laser particle size analyzer...
November 27, 2017: Journal of Chromatography. A
https://www.readbyqxmd.com/read/29194814/how-sildenafil-viagra%C3%A2-may-cause-melanoma-a-histopathologic-study-providing-a-potential-physiological-etiopathological-mechanism
#10
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/29184786/phosphodiesterase-type-5-inhibitors-usage-and-prostate-cancer-a-match-paired-analysis
#11
G Luke Machen, M Hasan Rajab, Jessica Pruszynski, K Scott Coffield
Background: To treat erectile dysfunction (ED), phosphodiesterase type 5 inhibitors (PDE5i) are commonly used. However, to date, only a few studies exist evaluate a possible effect on the incidence of prostate cancer. One such study completed by the authors' institution suggested men who use PDE5i for ED may have a lower incidence of prostate cancer. This study was meant to address some of the shortcomings of the former study and further characterize the link between prostate cancer and PDE5i use...
October 2017: Translational Andrology and Urology
https://www.readbyqxmd.com/read/29175000/cyclic-nucleotide-signaling-changes-associated-with-normal-aging-and-age-related-diseases-of-the-brain
#12
REVIEW
Michy P Kelly
Deficits in brain function that are associated with aging and age-related diseases benefit very little from currently available therapies, suggesting a better understanding of the underlying molecular mechanisms is needed to develop improved drugs. Here, we review the literature to test the hypothesis that a break down in cyclic nucleotide signaling at the level of synthesis, execution, and/or degradation may contribute to these deficits. A number of findings have been reported in both the human and animal model literature that point to brain region-specific changes in Galphas (a...
November 23, 2017: Cellular Signalling
https://www.readbyqxmd.com/read/29171944/-central-serous-chorioretinopathy-following-the-use-of-phosphodiesterase-5-inhibitors
#13
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/29171080/testosterone-therapy-for-sexual-dysfunction-in-men-with-type-2-diabetes-a-systematic-review-and-meta-analysis-of-randomized-controlled-trials
#14
M Algeffari, C N Jayasena, P MacKeith, A Thapar, W S Dhillo, N Oliver
AIM: To evaluate the effectiveness of testosterone therapy on a range of sexual function domains in men with Type 2 diabetes. METHOD: Electronic databases were searched for studies investigating the effect of testosterone therapy on sexual function in men with Type 2 diabetes. All randomized controlled trials were considered for inclusion if they compared the efficacy of testosterone therapy with that of placebo and reported sexual function outcomes. Statistical analysis was performed using a random-effects model, and heterogeneity was expressed using the I(2) statistic...
November 24, 2017: Diabetic Medicine: a Journal of the British Diabetic Association
https://www.readbyqxmd.com/read/29164831/udenafil-a-phosphodiesterase-5-inhibitor-reduces-body-weight-in-high-fat-fed-mice
#15
Seong Yul Ryu, Yoon Jung Choi, So Young Park, Jong Yeon Kim, Yong Dae Kim, Yong Woon Kim
PURPOSE: High-fat (HF) feeding induces hypothalamic leptin resistance via the activation of toll-like receptor 4 (TLR4). TLR4 deficiency confers resistance to diet-induced obesity. Udenafil, an anti-impotence drug, inhibits TLR4 in airway epithelial cells in vitro. In this study, we evaluated whether udenafil suppressed the hypothalamic expression of TLR4 and reduced body weight. MATERIALS AND METHODS: The hypothalamic expression of TLR4, phosphodiesterase 5 (PDE5), nuclear factor-κB (NF-κB), and myeloid differentiation primary response gene 88 (Myd88) was analyzed by real-time polymerase chain reaction after treating mice for 2 days with udenafil (0, 12, 120, or 600 μg/d)...
November 16, 2017: World Journal of Men's Health
https://www.readbyqxmd.com/read/29158679/treatment-of-pulmonary-hypertension-with-left-heart-disease-a-concise-review
#16
REVIEW
Anish Desai, Shilpa A Desouza
Pulmonary hypertension (PH) is defined by a mean pulmonary artery pressure ≥ 25 mmHg, as determined by right heart catheterization. Pulmonary arterial hypertension (PAH) can no longer be considered an orphan disease given the increase in awareness and availability of new drugs. PH carries with it a dismal prognosis and leads to significant morbidity and mortality. Symptoms can range from dyspnea, fatigue and chest pain to right ventricular failure and death. PH is divided into five groups by the World Health Organization (WHO), based on etiology...
2017: Vascular Health and Risk Management
https://www.readbyqxmd.com/read/29151951/potential-synergistic-effect-of-phosphodiesterase-inhibitors-with-chemotherapy-in-lung-cancer
#17
Kalliopi Domvri, Konstantinos Zarogoulidis, Nikolaos Zogas, Paul Zarogoulidis, Savvas Petanidis, Konstantinos Porpodis, Efrosini Kioseoglou, Wolfgang Hohenforst-Schmidt
Purpose: Lung cancer remains the leading cause of cancer-related deaths worldwide and novel therapeutic approaches targeting crucial pathways are urgently needed to improve its treatment. Differentiation-based therapeutics (Methylxanthines) and phosphodiesterase inhibitors (type 4 and 5), have been implicated in cancer treatment. Our objectives were to capture any potential anti-tumor effect of these drug combinations with chemotherapeutic agents in vitro. Methods: Theophylline as Methylxanthines, Roflumilast as phosphodiesterase type 4 (PDE4) inhibitor and Sildenafil as phosphodiesterase type 5 (PDE5) inhibitor are the drugs that we combined with the chemotherapeutic agents (Docetaxel, Cisplatin and Carboplatin) in vitro...
2017: Journal of Cancer
https://www.readbyqxmd.com/read/29150274/neuroprotective-potential-of-high-dose-biotin
#18
Mark F McCarty, James J DiNicolantonio
A recent controlled trial has established that high-dose biotin supplementation - 100 mg, three times daily - has a stabilizing effect on progression of multiple sclerosis (MS). Although this effect has been attributed to an optimization of biotin's essential cofactor role in the brain, a case can be made that direct stimulation of soluble guanylate cyclase (sGC) by pharmacological concentrations of biotin plays a key role in this regard. The utility of high-dose biotin in MS might reflect an anti-inflammatory effect of cGMP on the cerebral microvasculature, as well on oligodendrocyte differentiation and on Schwann cell production of neurotrophic factors thought to have potential for managing MS...
November 2017: Medical Hypotheses
https://www.readbyqxmd.com/read/29141888/lung-cancer-associated-pulmonary-hypertension-role-of-microenvironmental-inflammation-based-on-tumor-cell-immune-cell-cross-talk
#19
Soni Savai Pullamsetti, Baktybek Kojonazarov, Samantha Storn, Henning Gall, Ylia Salazar, Janine Wolf, Andreas Weigert, Nefertiti El-Nikhely, Hossein Ardeschir Ghofrani, Gabriele A Krombach, Ludger Fink, Stefan Gattenlöhner, Ulf R Rapp, Ralph Theo Schermuly, Friedrich Grimminger, Werner Seeger, Rajkumar Savai
Dyspnea is a frequent, devastating, and poorly understood symptom of advanced lung cancer. In our cohort, among 519 patients who underwent a computed tomography scan for the diagnosis of lung cancer, 250 had a mean pulmonary artery diameter of >28 mm, indicating pulmonary hypertension (PH). In human lung cancer tissue, we consistently observed increased vascular remodeling and perivascular inflammatory cell accumulation (macrophages/lymphocytes). Vascular remodeling, PH, and perivascular inflammatory cell accumulation were mimicked in three mouse models of lung cancer (LLC1, KRasLA2 , and cRaf-BxB)...
November 15, 2017: Science Translational Medicine
https://www.readbyqxmd.com/read/29138698/soluble-epoxide-hydrolase-inhibitor-and-14-15-epoxyeicosatrienoic-acid-facilitated-long-term-potentiation-through-camp-and-camkii-in-the-hippocampus
#20
Han-Fang Wu, Yi-Ju Chen, Su-Zhen Wu, Chi-Wei Lee, I-Tuan Chen, Yi-Chao Lee, Chi-Chen Huang, Chung-Hsi Hsing, Chih-Wei Tang, Hui-Ching Lin
Epoxyeicosatrienoic acids (EETs) are derived from arachidonic acid and metabolized by soluble epoxide hydrolase (sEH). The role of EETs in synaptic function in the central nervous system is still largely unknown. We found that pharmacological inhibition of sEH to stabilize endogenous EETs and exogenous 14,15-EET significantly increased the field excitatory postsynaptic potential (fEPSP) response in the CA1 area of the hippocampus, while additionally enhancing high-frequency stimulation- (HFS-) induced long-term potentiation (LTP) and forskolin- (FSK-) induced LTP...
2017: Neural Plasticity
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