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https://www.readbyqxmd.com/read/29778625/the-mediating-role-of-phosphodiesterase-type-4-in-the-dopaminergic-modulation-of-motor-impulsivity
#1
P R A Heckman, A Blokland, N P Van Goethem, B T J Van Hagen, J Prickaerts
The current study investigated the mediating role of phosphodiesterase type 4 (PDE4) regulated cAMP in the dopaminergic modulation of premature responding (action restraint) in rats. Response inhibition, which includes action restraint, finds its neurobiological origin in cortico-striatal-thalamic circuitry and can be modulated by dopamine. Intracellularly, the effect of dopamine is largely mediated through the cAMP/PKA signaling cascade. Areas in the prefrontal cortex are very sensitive to their neurochemical environment, including catecholamine levels...
May 17, 2018: Behavioural Brain Research
https://www.readbyqxmd.com/read/29765213/health-status-in-patients-with-copd-treated-with-roflumilast-two-large-noninterventional-real-life-studies-dino-and-dacota
#2
Peter Kardos, Ingo Mokros, Rüdiger Sauer, Claus F Vogelmeier
Purpose: DINO and DACOTA were prospective, noninterventional studies assessing the health status and quality of life of patients with COPD newly treated with roflumilast 500 μg once-daily add-on therapy. Patients and methods: Patients were evaluated over 6 months. Clinical COPD questionnaire (CCQ) and COPD assessment test (CAT) scores were recorded at baseline and after 3 and 6 months. In DACOTA, post-bronchodilator FEV1 was recorded at each time point. Results: Of 5,462 and 3,645 patients recruited into DINO and DACOTA, respectively, 3,274 patients in DINO and 916 patients in DACOTA completed the 6-month visit...
2018: International Journal of Chronic Obstructive Pulmonary Disease
https://www.readbyqxmd.com/read/29763572/determinants-of-response-to-roflumilast-in-severe-copd-pooled-analysis-of-two-randomized-trials
#3
Fernando J Martinez, Klaus F Rabe, Peter M A Calverley, Leonardo M Fabbri, Sanjay Sethi, Emilio Pizzichini, Andrew McIvor, Antonio Anzueto, Vijay K T Alagappan, Shahid Siddiqui, Colin Reisner, Sofia Zetterstrand, Jonas Román, Debasree Purkayastha, Nitin Bagul, Stephen I Rennard
RATIONALE: Roflumilast reduces exacerbations in patients with severe chronic obstructive pulmonary disease associated with chronic bronchitis and a history of exacerbations. Further characterization of patients most likely to benefit is warranted. OBJECTIVES: Define characteristics that most robustly identify patients who derive greatest exacerbation risk reduction with roflumilast. METHODS: Predefined, pooled analyses of REACT (NCT01329029) and RE2 SPOND (NCT01443845) multicenter, randomized, double-blind, placebo-controlled studies...
May 15, 2018: American Journal of Respiratory and Critical Care Medicine
https://www.readbyqxmd.com/read/29716881/mini-review-chronic-obstructive-pulmonary-disease-its-new-drug-treatments-and-strategies-a-review
#4
Muhammad Hanif, Junaid Qureshi, Hira Ijaz, Muhammad Iqbal Mustafa, Akhtar Rasul, Naeem Amir, Basma Aftab, Ahad Fayyaz
COPD is a complicated disease. Current available treatments are just for symptomatic relief and they cannot reverse the damages to lungs tissues due to alveolar destruction in COPD. Research is being conducted to evaluate new treatments and strategies to find specific treatments to minimize the symptoms of COPD. A new mixture of herbal medicine i.e AKL1 has emerged and thought to cure COPD symptoms especially cough related quality of life of COPD patients. Although, the results have showed no significant difference as compared to placebo but researchers recommend further evaluation in a large population (COPD Patients) group...
May 2018: Pakistan Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29648516/the-phosphodiesterase-4-inhibitor-roflumilast-reverts-proteolysis-in-skeletal-muscle-cells-of-patients-with-copd-cachexia
#5
Esther Barreiro, Ester Puig-Vilanova, Anna Salazar-Degracia, Sergi Pascual-Guardia, Carme Casadevall, Joaquim Gea
Peripheral muscle weakness and mass loss are characteristic features in severe COPD. We hypothesized that the phosphodiesterase-4 inhibitor roflumilast-induced cAMP may ameliorate proteolysis and metabolism in skeletal muscles of COPD patients with severe muscle wasting. In myogenic precursor cells (isolated from muscle biopsies and cultured up to obtain differentiated myotubes) from 10 severe COPD patients and 10 healthy controls, which were treated with 1 microM roflumilast N-oxide (RNO) for three time-cohorts (1h, 6h, and 24h), genes of antioxidant defense and oxidative stress marker, myogenesis and muscle metabolism, proteolysis (tyrosine release assay) and ubiquitin-proteasome system markers, autophagy, and myosin isoforms were analyzed using RT-PCR and immunoblotting...
April 12, 2018: Journal of Applied Physiology
https://www.readbyqxmd.com/read/29589382/the-phosphodiesterase-4-inhibitor-roflumilast-protects-against-cigarette-smoke-extract-induced-mitophagy-dependent-cell-death-in-epithelial-cells
#6
Sun Young Kyung, Yu Jin Kim, Eun Suk Son, Sung Hwan Jeong, Jeong Woong Park
BACKGROUND: Recent studies show that mitophagy, the autophagy-dependent turnover of mitochondria, mediates pulmonary epithelial cell death in response to cigarette smoke extract (CSE) exposure and contributes to the development of emphysema in vivo during chronic cigarette smoke (CS) exposure, although the underlying mechanisms remain unclear. METHODS: In this study, we investigated the role of mitophagy in the regulation of CSE-exposed lung bronchial epithelial cell (Beas-2B) death...
April 2018: Tuberculosis and Respiratory Diseases
https://www.readbyqxmd.com/read/29573453/design-synthesis-and-molecular-modeling-of-heterocyclic-bioisostere-as-potent-pde4-inhibitors
#7
Aya M Almatary, Mohammad A Elmorsy, Walaa M El Husseiny, Khalid B Selim, Magda A-A El-Sayed
A new hybrid template was designed by combining the structural features of phosphodiesterase 4 (PDE4) inhibitors with several heterocyclic moieties which present an integral part in the skeleton of many apoptotic agents. Thirteen compounds of the synthesized hybrids displayed higher inhibitory activity against PDE4B than the reference drug, roflumilast. Further investigation indicated that compounds 13b and 20 arrested the cell cycle at the G2/M phase and the pre-G1 phase, and induced cell death by apoptosis of A549 cells in a caspase-dependent manner...
March 24, 2018: Archiv der Pharmazie
https://www.readbyqxmd.com/read/29569375/roflumilast-usage-from-2010-to-2016-a-danish-nationwide-drug-utilization-study
#8
Øyvind Nicolay Ulland Salvesen, Jesper Rømhild Davidsen, Anton Pottegård, Daniel Pilsgaard Henriksen
Roflumilast, a phosphodiesterase-4-inhibitor, is marketed as add-on treatment to inhaled bronchodilators and corticosteroids in COPD patients with frequent exacerbations. Although marketed since 2010, usage pattern of roflumilast for an entire nation has not previously been explored. This study aimed to estimate the total utilization of roflumilast in Denmark during 2010 to 2016, using the Danish nationwide health registers. We identified 1573 individuals (47% males) who used roflumilast during the study period, of whom 705 (45%) redeemed only one prescription...
March 22, 2018: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/29563781/use-of-a-4-week-up-titration-regimen-of-roflumilast-in-patients-with-severe-copd
#9
Henrik Watz, Nitin Bagul, Klaus F Rabe, Stephen Rennard, Vijay Kt Alagappan, Jonas Román, Axel Facius, Peter Ma Calverley
Background: The oral selective phosphodiesterase-4 inhibitor roflumilast (ROF) reduces exacerbations in patients with severe COPD. Adverse events (AEs) can cause early ROF discontinuation. Alternative dosing strategies may help patients continue their therapy. Methods: In this multicenter, double-blind trial, 1,321 patients with severe COPD were randomized 1:1:1 to 4 weeks' treatment with ROF 250 µg once daily (OD), 500 µg every other day (EOD), or 500 µg OD, each followed by ROF 500 µg OD for 8 weeks, plus standard therapy...
2018: International Journal of Chronic Obstructive Pulmonary Disease
https://www.readbyqxmd.com/read/29550808/phosphodiesterase-4-inhibitor-roflumilast-protects-rat-hippocampal-neurons-from-sevoflurane-induced-injury-via-modulation-of-mek-erk-signaling-pathway
#10
Sheng Peng, Hong-Zhu Yan, Pei-Rong Liu, Xiao-Wei Shi, Chun-Liang Liu, Qi Liu, Yu Zhang
BACKGROUND/AIMS: Sevoflurane, a commonly used volatile anesthetic, recently has been found has neurotoxicity in the central nervous system of neonatal rodents. This study aimed to reveal whether phosphodiesterase 4 (PDE-4) inhibitor roflumilast has protective functions in sevoflurane-induced nerve damage. METHODS: Hippocampal neurons were isolated from juvenile rats, and were exposed to sevoflurane with or without roflumilast treatment. Cell viability and apoptosis were respectively assessed by CCK-8 and flow cytometry...
2018: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/29549279/phosphodiesterase-type-4-inhibition-enhances-nitric-oxide-and-hydrogen-sulfide-mediated-bladder-neck-inhibitory-neurotransmission
#11
Ángel Agis-Torres, Paz Recio, María Elvira López-Oliva, María Pilar Martínez, María Victoria Barahona, Sara Benedito, Salvador Bustamante, Miguel Ángel Jiménez-Cidre, Albino García-Sacristán, Dolores Prieto, Vítor S Fernandes, Medardo Hernández
Nitric oxide (NO) and hydrogen sulfide (H2 S) play a pivotal role in nerve-mediated relaxation of the bladder outflow region. In the bladder neck, a marked phosphodiesterase type 4 (PDE4) expression has also been described and PDE4 inhibitors, as rolipram, produce smooth muscle relaxation. This study investigates the role of PDE4 isoenzyme in bladder neck gaseous inhibitory neurotransmission. We used Western blot and double immunohistochemical staining for the detection of NPP4 (PDE4) and PDE4A and organ baths for isometric force recording to roflumilast and tadalafil, PDE4 and PDE5, respectively, inhibitors in pig and human samples...
March 16, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29546543/maldi-imaging-facilitates-new-topical-drug-development-process-by-determining-quantitative-skin-distribution-profiles
#12
David Bonnel, Raphaël Legouffe, André H Eriksson, Rasmus W Mortensen, Fabien Pamelard, Jonathan Stauber, Kim T Nielsen
Generation of skin distribution profiles and reliable determination of drug molecule concentration in the target region are crucial during the development process of topical products for treatment of skin diseases like psoriasis and atopic dermatitis. Imaging techniques like mass spectrometric imaging (MSI) offer sufficient spatial resolution to generate meaningful distribution profiles of a drug molecule across a skin section. In this study, we use matrix-assisted laser desorption/ionization mass spectrometry imaging (MALDI-MSI) to generate quantitative skin distribution profiles based on tissue extinction coefficient (TEC) determinations of four different molecules in cross sections of human skin explants after topical administration...
April 2018: Analytical and Bioanalytical Chemistry
https://www.readbyqxmd.com/read/29502338/efficacy-and-safety-of-phosphodiesterase-4-inhibitors-in-patients-with-asthma-a-systematic-review-and-meta-analysis
#13
REVIEW
Jian Luo, Ling Yang, Jing Yang, Dan Yang, Bi-Cui Liu, Dan Liu, Bin-Miao Liang, Chun-Tao Liu
Phosphodiesterase 4 (PDE4) inhibitors are a novel medication approved for airway inflammatory diseases including chronic obstructive pulmonary disease. Their role and application in asthma are controversial and not defined. A comprehensive search was performed in major databases (1946-2016) using the keywords: 'phosphodiesterase 4 inhibitor' or 'roflumilast' and 'asthma'. Placebo-controlled trials reporting lung function, airway hyperresponsiveness by direct challenge, asthma control and exacerbations, and adverse events were included...
May 2018: Respirology: Official Journal of the Asian Pacific Society of Respirology
https://www.readbyqxmd.com/read/29477888/synthesis-and-molecular-docking-of-new-roflumilast-analogues-as-preferential-selective-potent-pde-4b-inhibitors-with-improved-pharmacokinetic-profile
#14
Bahia A Moussa, Asmaa A El-Zaher, Mohamed K El-Ashrey, Marwa A Fouad
In the present work, we designed and synthesized new roflumilast analogues with preferential-selective PDE-4B inhibition activity and improved pharmacokinetic properties. The unsubstituted benzo[d]thiazol-2-yl and -6-yl benzamide derivatives (4a and 6a) showed both good potency and preferential selectivity for PDE-4B. More remarkably, 6c revealed 6 times preferential PDE-4B/4D selectivity with a significant increase of in vitro cAMP and good % inhibition of TNF-α concentration. In addition, the in vitro pharmacokinetics of 6c showed good metabolic stability with in vitro CLint (5...
March 25, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29443750/effect-and-safety-of-roflumilast-for-chronic-obstructive-pulmonary-disease-in-chinese-patients
#15
RANDOMIZED CONTROLLED TRIAL
Dong-Yang Liu, Zhi-Guo Wang, Yuan Gao, Hui-Min Zhang, Yu-Xiang Zhang, Xiao-Jun Wang, Dan Peng
BACKGROUND: This trial aimed to evaluate the efficacy and safety of roflumilast for treating Chinese patients with chronic obstructive pulmonary disease (COPD). METHODS: A total of 120 patients with COPD were recruited and were randomly divided into 2 groups (an intervention group and a placebo group) at a 1:1 ratio. Patients received either roflumilast or placebo 500 μg once daily for a total of 12 months. The primary outcome was lung function, measured by the change from baseline of forced expiratory volume in 1 second (FEV1), FVC = forced vital capacity (FVC), and FEF25-75%...
February 2018: Medicine (Baltimore)
https://www.readbyqxmd.com/read/29441434/a-nonhuman-primate-pet-study-measurement-of-brain-pde4-occupancy-by-roflumilast-using-r-11-c-rolipram
#16
Akihiro Takano, Tolga Uz, Jesus Garcia-Segovia, Max Tsai, Gezim Lahu, Nahid Amini, Ryuji Nakao, Zhisheng Jia, Christer Halldin
PURPOSE: Phosphodiesterase 4 (PDE4) inhibition in the brain has been reported to improve cognitive function in animal models. Therefore, PDE4 inhibitors are one of key targets potential for drug development. Investigation of brain PDE4 occupancy would help to understand the effects of PDE4 inhibition to cognitive functions. Roflumilast is a selective phosphodiesterase type 4 (PDE4) inhibitor used clinically for severe chronic obstructive pulmonary disease, but the effects to the brain have not been well investigated...
February 13, 2018: Molecular Imaging and Biology: MIB: the Official Publication of the Academy of Molecular Imaging
https://www.readbyqxmd.com/read/29397527/effect-of-roflumilast-on-chronic-obstructive-pulmonary-disease-a-systematic-review-and-meta-analysis
#17
Lu-Fei Shen, Xiao-Dong Lv, Wen-Yu Chen, Qi Yang, Zhi-Xian Fang, Wei-Fen Lu
BACKGROUND: Randomized controlled trials (RCTs) of roflumilast effect on chronic obstructive pulmonary disease (COPD) have been reported in the last decade. The current meta-analysis was designed to systematically review and perform meta-analysis of the RCTs of roflumilast treatment in COPD. METHODS: Electronic databases including PubMed, EMBASE, Web of Science, and Cochrane clinical trials database were searched to identify RCTs of roflumilast treatment on COPD...
February 3, 2018: Irish Journal of Medical Science
https://www.readbyqxmd.com/read/29375047/effects-of-tadalafil-pde5-inhibitor-and-roflumilast-pde4-inhibitor-on-airway-reactivity-and-markers-of-inflammation-in-ovalbumin-induced-airway-hyperresponsiveness-in-guinea-pigs
#18
J Mokry, A Urbanova, I Medvedova, M Kertys, P Mikolka, P Kosutova, D Mokra
Selective phosphodiesterase (PDE) 4 inhibitors have recently been introduced into the therapy of chronic obstructive pulmonary disease. However, suppression of airway reactivity and eosinophilic inflammation by increased intracellular cAMP could be beneficial in bronchial asthma as well. PDE5 inhibitors are used for the therapy of erectile dysfunction, pulmonary hypertension, and other cardiovascular diseases, but an expression of PDE5 in several immune cells suggests its perspectives in inflammation, as well...
October 2017: Journal of Physiology and Pharmacology: An Official Journal of the Polish Physiological Society
https://www.readbyqxmd.com/read/29354670/effect-of-roflumilast-on-airway-blood-flow-in-copd-a-pilot-study
#19
Eliana S Mendes, Patricia Rebolledo, Lilian Cadet, Johana Arana, Andreas Scmid, Adam Wanner
No abstract text is available yet for this article.
August 28, 2017: Chronic Obstructive Pulmonary Diseases: Journal of the COPD Foundation
https://www.readbyqxmd.com/read/29348829/roflumilast-restores-camp-pka-creb-signaling-axis-for-ftmt-mediated-tumor-inhibition-of-ovarian-cancer
#20
Shipeng Gong, Yongning Chen, Fanliang Meng, Yadi Zhang, Huan Wu, Fei Wu
The abrogation of cAMP generation by overexpression of PDE isoforms promotes the inflammatory pathology, and the PDE inhibitors have showed the potential anti-inflammation effects in clinical. However, the function of PDE inhibitors in cancer treatment remains unclear. We here investigated the role of PDE4 inhibitor Roflumilast in the treatment of ovarian cancer. We found that Roflumilast could effectively inhibit the proliferation, and induce apoptosis and cell cycle arrest in two ovarian cancer cell lines OVCAR3 and SKOV3...
December 22, 2017: Oncotarget
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