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https://www.readbyqxmd.com/read/28922692/phosphodiesterase-4-inhibitors-for-chronic-obstructive-pulmonary-disease
#1
REVIEW
Jimmy Chong, Bonnie Leung, Phillippa Poole
BACKGROUND: Chronic obstructive pulmonary disease (COPD) is associated with cough, sputum production or dyspnoea and a reduction in lung function, quality of life and life expectancy. Apart from smoking cessation, there are no other treatments that slow lung function decline. Roflumilast and cilomilast are oral phosphodiesterase 4 (PDE4) inhibitors proposed to reduce the airway inflammation and bronchoconstriction seen in COPD. This is an update of a Cochrane review first published in 2011 and updated in 2013...
September 19, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/28889106/prevention-of-copd-exacerbations-a-european-respiratory-society-american-thoracic-society-guideline
#2
Jadwiga A Wedzicha, Peter M A Calverley, Richard K Albert, Antonio Anzueto, Gerard J Criner, John R Hurst, Marc Miravitlles, Alberto Papi, Klaus F Rabe, David Rigau, Pawel Sliwinski, Thomy Tonia, Jørgen Vestbo, Kevin C Wilson, Jerry A Krishnan
This document provides clinical recommendations for the prevention of chronic obstructive pulmonary disease (COPD) exacerbations. It represents a collaborative effort between the European Respiratory Society and the American Thoracic Society.Comprehensive evidence syntheses were performed to summarise all available evidence relevant to the Task Force's questions. The evidence was appraised using the Grading of Recommendations, Assessment, Development and Evaluation approach and the results were summarised in evidence profiles...
September 2017: European Respiratory Journal: Official Journal of the European Society for Clinical Respiratory Physiology
https://www.readbyqxmd.com/read/28799255/synergy-between-5-ht4-receptor-stimulation-and-phosphodiesterase-4-inhibition-in-facilitating-acetylcholine-release-in-human-large-intestinal-circular-muscle
#3
V Pauwelyn, W Ceelen, R A Lefebvre
BACKGROUND: Gastroprokinetic properties of 5-HT4 receptor agonists, such as prucalopride, are attributed to activation of 5-HT4 receptors on cholinergic nerves innervating smooth muscle in the gastrointestinal smooth muscle layer, increasing acetylcholine release and muscle contraction. In porcine stomach and colon, phosphodiesterase (PDE) 4 has been shown to control the signaling pathway of these 5-HT4 receptors. The aim of this study was to investigate the PDE-mediated control of these 5-HT4 receptors in human large intestine...
August 10, 2017: Neurogastroenterology and Motility: the Official Journal of the European Gastrointestinal Motility Society
https://www.readbyqxmd.com/read/28772081/investigational-phosphodiesterase-inhibitors-in-phase-i-and-phase-ii-clinical-trials-for-alzheimer-s-disease
#4
REVIEW
Jos Prickaerts, Pim R A Heckman, Arjan Blokland
Phosphodiesterase (PDE) inhibitors improve signaling pathways in brain circuits by increasing intracellular cyclic adenosine monophosphate (cAMP) and/or cyclic guanosine monophosphate (cGMP). In the last decade, the first clinical studies investigating selective PDE inhibitors in Alzheimer's disease (AD) have been initiated, based on their positive effects on cognitive processes and neuroprotection in numerous animal studies. Areas covered: This article reviews the clinical studies investigating the pro-cognitive/neuroprotective effects of PDE inhibitors in patients with AD, as well as in age-associated memory impaired elderly and patients with mild cognitive impairment (MCI), the prodromal stage of AD...
September 2017: Expert Opinion on Investigational Drugs
https://www.readbyqxmd.com/read/28756610/treatment-of-obesity-associated-overactive-bladder-by-the-phosphodiesterase-type-4-inhibitor-roflumilast
#5
Honglin Ding, Ning Li, Xiaoning He, Bing Liu, Liming Dong, Yili Liu
PURPOSE: To prove that phosphodiesterase type-4 inhibitors could potentially treat obesity-associated overactive bladder through modulation of the systemic inflammatory response. METHODS: In this 12-week study, 90 female Sprague-Dawley rats were divided into three groups: (1) vehicle-treated normal diet (ND)-fed rats; (2) vehicle-treated high-fat diet (HFD)-fed rats; and (3) roflumilast-treated HFD-fed rats. Oral roflumilast (5 mg/kg/day) was administered during the last 4 weeks of HFD feeding in the test group...
July 29, 2017: International Urology and Nephrology
https://www.readbyqxmd.com/read/28684234/roflumilast-treatment-inhibits-lung-carcinogenesis-in-benzo-a-pyrene-induced-murine-lung-cancer-model
#6
Chang Dong Yeo, Young Ae Kim, Hwa Young Lee, Jin Woo Kim, Seung Joon Kim, Sang Haak Lee, Young Kyoon Kim
Roflumilast, a potent and selective inhibitor of phosphodiesterase-4 (PDE4), has been used in treatment of COPD. PDE4 inhibitor is associated with inhibition of chronic airway inflammation, oxidative stress, and mesenchymal markers in B(a)P-induced lung tumors. The aim of this study was to assess whether roflumilast alone or added to inhaled budesonide might have dose-dependent inhibition on lung carcinogenesis induced by carcinogen B(a)P in mice. Female A/J mice were given a single dose of benzo(a)pyrene. Administration of roflumilast (1mg/kg or 5mg/kg) via oral gavage and aerosolized budesonide (2...
July 4, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28650427/roflumilast-reverses-polymicrobial-sepsis-induced-liver-damage-by-inhibiting-inflammation-in-mice
#7
Hongfang Feng, Jiajia Chen, Haitao Wang, Yufang Cheng, Zhengqiang Zou, Qiuping Zhong, Jiangping Xu
Sepsis is a life-threatening syndrome accompanied by an overwhelming inflammatory response and organ dysfunction. Selective targeting of phosphodiesterase 4 (PDE4) is currently being investigated as an effective therapeutic approach for inflammation-associated diseases. Roflumilast is a selective PDE4 inhibitor, used for the treatment of severe chronic obstructive pulmonary disease in clinic. However, its role in the treatment of sepsis-induced liver damage remains unclear. In the present study, we evaluated the effects of roflumilast in mice with cecal ligation and puncture-induced sepsis, and investigated the underlying mechanism...
September 2017: Laboratory Investigation; a Journal of Technical Methods and Pathology
https://www.readbyqxmd.com/read/28637505/human-lung-and-monocyte-derived-macrophages-differ-with-regard-to-the-effects-of-%C3%AE-2-adrenoceptor-agonists-on-cytokine-release
#8
Tatiana Victoni, Hélène Salvator, Charlotte Abrial, Marion Brollo, Luis Cristovão Sobrino Porto, Vincent Lagente, Emmanuel Naline, Stanislas Grassin-Delyle, Philippe Devillier
BACKGROUND: β2-adrenoceptor agonists have been shown to reduce the lipopolysaccharide (LPS)-induced cytokine release by human monocyte-derived macrophages (MDMs). We compare the expression of β2-adrenoceptors and the inhibitory effect of formoterol and salmeterol on the LPS-induced release of tumor necrosis factor (TNF)-α, interleukin (IL)-1β, IL-6 and a range of chemokines (CCL2, 3, 4, and IL-8) by human lung macrophages (LMs) and MDMs. METHODS: LMs were isolated from patients undergoing resection and MDMs were obtained from blood monocytes in the presence of GM-CSF...
June 21, 2017: Respiratory Research
https://www.readbyqxmd.com/read/28596292/the-pde4-inhibitor-chf-6001-and-lamas-inhibit-bronchoconstriction-induced-remodeling-in-lung-slices
#9
Loes E M Kistemaker, Tjitske A Oenema, Hoeke A Baarsma, I Sophie T Bos, Martina Schmidt, Fabrizio Facchinetti, Maurizio Civelli, Gino Villetti, Reinoud Gosens
Combination therapy of PDE4 inhibitors and anticholinergics induces bronchoprotection in COPD. Mechanical forces that arise during bronchoconstriction may contribute to airway remodeling. Therefore, we investigated the impact of PDE4 inhibitors and anticholinergics on bronchoconstriction-induced remodeling. Because of the different mechanism of action of PDE4 inhibitors and anticholinergics, we hypothesized functional interactions of these two drug classes. Guinea pig precision-cut lung slices were preincubated with the PDE4 inhibitors CHF-6001 or roflumilast and/or the anticholinergics tiotropium or glycopyorrolate, followed by stimulation with methacholine (10 μM) or TGF-β1 (2 ng/ml) for 48 h...
September 1, 2017: American Journal of Physiology. Lung Cellular and Molecular Physiology
https://www.readbyqxmd.com/read/28558784/hesperetin-5-7-3-o-triacetate-suppresses-airway-hyperresponsiveness-in-ovalbumin-sensitized-and-challenged-mice-without-reversing-xylazine-ketamine-induced-anesthesia-in-normal-mice
#10
You-Lan Yang, Chi-Li Chen, Chi-Ming Chen, Wun-Chang Ko
BACKGROUND: We recently reported that hesperetin-5,7,3'-O-triacetate (HTA) dually inhibited phosphodiesterase (PDE)3/4 with a therapeutic ratio of 20.8. The application and development of PDE4 inhibitors for treating asthma or COPD are limited by their side effects, such as nausea, vomiting and gastric hypersecretion. PDE4 inhibitors were reported to reverse xylazine/ketamine-induced anesthesia in rats and triggered vomiting in ferrets. Thus the reversing effect of HTA on xylazine/ketamine-induced anesthesia in mice was studied to assess emetic effect of HTA...
May 30, 2017: BMC Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28554321/phosphodiesterase-4-inhibitors-in-immune-mediated-diseases-mode-of-action-clinical-applications-current-and-future-perspectives
#11
Lazaros I Sakkas, Athanasios Mavropoulos, Dimitrios P Bogdanos
Phosphodiesterase (PDE) 4 is a superfamily of enzymes that catalyze the hydrolysis of cyclic adenosine 3',5'-monophosphate (cAMP), an intracellular second messenger and regulator of a wide array of genes and proteins. Increased levels of intracellular cAMP lead to activation of genes but also to inhibition of nuclear factor-kappa B, involved in pro-inflammatory responses. By increasing cAMP levels, PDE4 inhibitors, such as apremilast, reduced production of pro-inflammatory TNFα, IFNγ, and IL-17 and increased production of anti-inflammatory IL-10 in lipopolysaccharide-stimulated peripheral blood mononuclear cells, and in patients with psoriatic arthritis (PsA)...
May 29, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28523172/roles-of-roflumilast-a-selective-phosphodiesterase-4-inhibitor-in-airway-diseases
#12
REVIEW
Theerasuk Kawamatawong
Asthma and chronic obstructive pulmonary disease (COPD) are common chronic respiratory diseases. Both diseases have incompletely distinct pathophysiology, clinical manifestation, and treatment responsiveness. Pulmonary and systemic inflammations are the hallmarks of COPD. Most asthma responds to inhaled corticosteroid (ICS) treatment. In contrast, COPD is a corticosteroid-resistant disease. Bronchodilators are a preferred treatment method of COPD, with the aim of improving symptoms and preventing exacerbation...
April 2017: Journal of Thoracic Disease
https://www.readbyqxmd.com/read/28506848/inflammatory-marker-analysis-in-psoriatic-skin-under-topical-phospodiesterase-4-inhibitor-treatment
#13
Lennart M Roesner, Petra Kienlin, Gabriele Begemann, Oliver Dittrich-Breiholz, Thomas Werfel
Topical formulations of the two PDE4i roflumilast and TAK-084 lead to a reduction of inflammatory markers and infiltrating cells in psoriatic lesional skin.
May 12, 2017: Journal of Allergy and Clinical Immunology
https://www.readbyqxmd.com/read/28504599/is-concomitant-use-of-theophylline-and-roflumilast-really-contraindicated
#14
Alok Nath, Ajmal Khan, Zia Hashim
No abstract text is available yet for this article.
May 15, 2017: American Journal of Respiratory and Critical Care Medicine
https://www.readbyqxmd.com/read/28477089/the-phosphodiesterase-4-inhibitor-roflumilast-decreases-ethanol-consumption-in-c57bl-6j-mice
#15
Xin Liu, Pi-Da Hao, Ming-Feng Yang, Jing-Yi Sun, Lei-Lei Mao, Cun-Dong Fan, Zong-Yong Zhang, Da-Wei Li, Xiao-Yi Yang, Bao-Liang Sun, Han-Ting Zhang
RATIONALE: Alcohol use disorders have become one of the most damaging psychiatric disorders in the world; however, there are no ideal treatments in clinic. Phosphodiesterase-4 (PDE4), an enzyme that specifically hydrolyzes intracellular cyclic AMP (cAMP), has been involved in alcohol use disorders. Roflumilast is the first PDE4 inhibitor approved for treatment of chronic obstructive pulmonary diseases in clinic. It was of particular interest to researchers to determine whether roflumilast altered ethanol consumption...
August 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28451841/roflumilast-reduces-cerebral-inflammation-in-a-rat-model-of-experimental-subarachnoid-hemorrhage
#16
Qingjian Wu, Lifeng Qi, Hanxia Li, Leilei Mao, Mingfeng Yang, Rongxia Xie, Xiaoyi Yang, Jian Wang, Zongyong Zhang, Jiming Kong, Baoliang Sun
Roflumilast, a selective inhibitor for PDE4, is approved by FDA as an anti-inflammation drug for treatment of chronic obstructive pulmonary disease (COPD). This study investigates the effects of roflumilast on cerebral inflammation in the rat SAH model. Here, we show that subcutaneous administration of roflumilast (3 mg/kg) significantly improved the neurological deficits. Measurement of evans blue extravasation and brain water content revealed a significant reduction of blood-brain barrier permeability and brain edema...
August 2017: Inflammation
https://www.readbyqxmd.com/read/28419462/modeling-and-simulation-of-pivotal-clinical-trials-using-linked-models-for-multiple-endpoints-in-chronic-obstructive-pulmonary-disease-with-roflumilast
#17
Axel Facius, Andreas Krause, Laurent Claret, Rene Bruno, Gezim Lahu
Roflumilast is a selective phosphodiesterase 4 inhibitor (PDE4i) for the treatment of severe chronic obstructive pulmonary disease (COPD). In 2 large phase 3 trials in a broader population of COPD patients (BY217/M2-111, ClinicalTrials.gov: NCT00076089 and BY217/M2-112, ClinicalTrials.gov: NCT00430729), treatment with roflumilast reduced the rate of exacerbations; however, the reduction did not reach statistical significance. Two linked dose-response models for the primary (annualized COPD exacerbation counts) and secondary (change from baseline in forced expiratory volume in 1 second [FEV1 ]) end points were therefore developed to characterize and quantify effect sizes and the patient characteristics influencing them...
August 2017: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28366471/phosphodiesterase-4-inhibition-restored-hippocampal-long-term-potentiation-after-primary-blast
#18
Edward W Vogel, Fatima N Morales, David F Meaney, Cameron R Bass, Barclay Morrison
Due to recent military conflicts and terrorist attacks, blast-induced traumatic brain injury (bTBI) presents a health concern for military and civilian personnel alike. Although secondary blast (penetrating injury) and tertiary blast (inertia-driven brain deformation) are known to be injurious, the effects of primary blast caused by the supersonic shock wave interacting with the skull and brain remain debated. Our group previously reported that in vitro primary blast exposure reduced long-term potentiation (LTP), the electrophysiological correlate of learning and memory, in rat organotypic hippocampal slice cultures (OHSCs) and that primary blast affects key proteins governing LTP...
July 2017: Experimental Neurology
https://www.readbyqxmd.com/read/28326174/copd-stage-and-treatment-in-a-large-outpatient-clinic
#19
Claire Præst Holm, Jakob Holm, Annette Nørgaard, Nina Godtfredsen
Some COPD patients suffer from frequent exacerbations despite triple inhalation treatment. These frequent exacerbators should be identified, as exacerbations often lead to decreasing lung function and increasing mortality. Roflumilast reduces exacerbations in patients with a previous history of exacerbations. Our aim was to describe COPD patient characteristics and compare roflumilast treatment eligible to non-eligible patients. An observational cross-section study was conducted. Patients were included from a large COPD outpatient clinic...
2017: European Clinical Respiratory Journal
https://www.readbyqxmd.com/read/28201975/selective-inhibition-of-phosphodiesterases-4a-b-c-and-d-isoforms-in-chronic-respiratory-diseases-current-and-future-evidences
#20
Sonia Contreras, Javier Milara, Esteban Morcillo, Julio Cortijo
Chronic respiratory diseases affect millions of people every day. According to the World Health Organization estimates, ~235 million people suffer from asthma, ~64 million suffer from chronic obstructive pulmonary disease (COPD), and millions more suffer from allergic rhinitis around the world. In recent last years, the first phosphodiesterase 4 (PDE4) inhibitor, roflumilast, was approved as a treatment to reduce the risk of exacerbations in stable and severe COPD associated with chronic bronchitis and a history of exacerbations...
2017: Current Pharmaceutical Design
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