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https://www.readbyqxmd.com/read/29777732/antinociceptive-effect-of-tadalafil-in-various-pain-models-involvement-of-opioid-receptors-and-nitric-oxide-cyclic-gmp-pathways
#1
Mohammad M Mehanna, Souraya Domiati, Hania Nakkash Chmaisse, Ahmed El Mallah
Nitric oxide has been proven to play an important role in nociception, accordingly, its promoters, phosphodiesterase inhibitors have been investigated as pain response modulators. Aiming to evaluate the central effect of tadalafil, a phosphodiesterase 5 inhibitor, and to determine its EC50, tail flick and hot plate tests were utilized. On the other hand, its nociceptive peripheral analgesic effect was assessed through acetic-acid induced writhing model. Formalin test was used to appraise both non-inflammatory and inflammatory pain responses...
May 16, 2018: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/29743944/repurposing-drugs-in-oncology-redo-selective-pde5-inhibitors-as-anti-cancer-agents
#2
Pan Pantziarka, Vidula Sukhatme, Sergio Crispino, Gauthier Bouche, Lydie Meheus, Vikas P Sukhatme
Selective phosphodiesterase 5 inhibitors, including sildenafil, tadalafil and vardenafil, are widely-used in the treatment of erectile dysfunction and pulmonary arterial hypertension. They are also well-known as examples of successful drug repurposing in that they were initially developed for angina and only later developed for erectile dysfunction. However, these drugs may also be effective cancer treatments. A range of evidentiary sources are assessed in this paper and the case made that there is pre-clinical and clinical evidence that these drugs may offer clinical benefit in a range of cancers...
2018: Ecancermedicalscience
https://www.readbyqxmd.com/read/29735634/evaluation-of-sildenafil-and-tadalafil-for-reversing-constriction-of-fetal-arteries-in-a-human-placenta-perfusion-model
#3
Robert B Walton, Luckey C Reed, Sarah M Estrada, Stacey S Schmiedecke, Diana L Villazana-Kretzer, Peter G Napolitano, Nicholas Ieronimakis
Fetal growth restriction resulting from reduced placental blood perfusion is a major cause of neonatal morbidity and mortality. Aside from intense surveillance and early delivery, there is no treatment for fetal growth restriction. A potential treatment associated with placental vasoconstriction is the class of PDE5 (phosphodiesterase type 5) inhibitors such as sildenafil, which is known to cross the placenta. In contrast, tadalafil, a more potent and selective PDE5 inhibitor has not been studied in pregnancy or experimental models of fetal growth restriction...
May 7, 2018: Hypertension
https://www.readbyqxmd.com/read/29733797/comparison-of-safety-and-efficacy-of-silodosin-solifenacin-tadalafil-and-their-combinations-in-the-treatment-of-double-j-stent-related-lower-urinary-system-symptoms-a-prospective-randomized-trial
#4
Rohit Bhattar, Vinay Tomar, Sher Singh Yadav, Devendra Singh Dhakad
OBJECTIVE: To evaluate the efficacy and safety of silodosin, solifenacin, tadalafil and their combinations in reducing double J (DJ) stent-related symptoms (SRS). MATERIAL AND METHODS: A total of 335 patients who underwent DJ stenting and develop SRS at 1st week were randomized into eight groups. Ureteral stent symptom questionnaire (USSQ) and Quality of life (QOL) scores were noted in each group: Group A-Silodosin (8 mg OD)+ Solifenacin (10 mg OD)+ Tadalafil (5 mg OD), B - Silodosin 8 mg OD, C - Solifenacin 10 mg OD, D- Tadalafil 5 mg OD, E- Silodosin (8 mg OD) + Solifenacin (10 mg OD), F- Silodosin (8 mg 0D)+ Tadalafil (5 mg OD), G- Solifenacin (10 mg OD)+ Tadalafil (5 mg OD) and H-placebo...
May 2018: Turkish Journal of Urology
https://www.readbyqxmd.com/read/29724204/efficacy-and-safety-of-pde5-is-and-%C3%AE-1-blockers-for-treating-lower-ureteric-stones-or-luts-a-meta-analysis-of-rcts
#5
Xifeng Sun, Wei Guan, Haoran Liu, Kun Tang, Libin Yan, Yangjun Zhang, Jin Zeng, Zhiqiang Chen, Hua Xu, Zhangqun Ye
BACKGROUND: Lower ureteric stones and lower urinary tract symptoms are common in urology.Drug treatment is one of standard therapy,but the efficacy was controversial.Thus we aimed to investigate the efficacy and safety of monotherapy or combination therapy of adrenoceptor1 blockers and phosphodiesterase5 inhibitors for treatment. METHODS: Randomized controlled trials up to November 2016 were retrieved from PubMed, the Cochrane Library, Web of Science and Embase...
May 3, 2018: BMC Urology
https://www.readbyqxmd.com/read/29722944/-effects-of-different-medications-with-tadalafil-on-erectile-dysfunction-in-males-with-primary-sexual-failure
#6
Wen-Ji Li, Ming-Xi Xu, Jian-Hua Guo, Zhi-Kang Cai, Yue-Qing Jiang, Zhong Wang
Objective: To evaluate the effects of three different medications with tadalafil on erectile dysfunction (ED) in young men with primary sexual failure. METHODS: This study included 76 male ED patients aged 21-35 years who had primary sexual failure but normal nocturnal penile tumescence and rigidity and failed to respond to psychotherapy. We randomly assigned them to receive oral tadalafil once daily, on demand, or once-daily + on-demand. After 2-3 months of treatment, we evaluated the effects based on the scores of the patients in the five domains of the International Index of Erectile Function (IIEF-5)...
June 2017: Zhonghua Nan Ke Xue, National Journal of Andrology
https://www.readbyqxmd.com/read/29719379/comparison-of-tadalafil-pharmacokinetics-after-administration-of-a-new-orodispersible-film-versus-a-film-coated-tablet
#7
Sang-In Park, Su-Hak Heo, Gihwan Kim, Seokhoon Chang, Keon-Hyoung Song, Min-Gul Kim, Eun-Heui Jin, JaeWoo Kim, SeungHwan Lee, Jang Hee Hong
Background: An orodispersible film (ODF) of tadalafil may provide increased convenience for erectile dysfunction (ED) patients as compared to conventional tablet formulations. In this study, we aimed to compare the pharmacokinetic, safety, and tolerability profiles of a newly developed ODF formulation of tadalafil to those of a film-coated tablet (FCT) of tadalafil. Materials and methods: This study was conducted in healthy male subjects using an open-label, randomized sequence, two-period, two-formulation, single-dose, crossover design...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29669541/three-dimensional-models-of-mycobacterium-tuberculosis-proteins-rv1555-rv1554-and-their-docking-analyses-with-sildenafil-tadalafil-vardenafil-drugs-suggest-interference-with-quinol-binding-likely-to-affect-protein-s-function
#8
Pallabini Dash, M Bala Divya, Lalitha Guruprasad, Kunchur Guruprasad
BACKGROUND: Earlier based on bioinformatics analyses, we had predicted the Mycobacterium tuberculosis (M.tb) proteins; Rv1555 and Rv1554, among the potential new tuberculosis drug targets. According to the 'TB-drugome' the Rv1555 protein is 'druggable' with sildenafil (Viagra), tadalafil (Cialis) and vardenafil (Levitra) drugs. In the present work, we intended to understand via computer modeling studies, how the above drugs are likely to inhibit the M.tb protein's function. RESULTS: The three-dimensional computer models for M...
April 18, 2018: BMC Structural Biology
https://www.readbyqxmd.com/read/29621715/comparison-of-phosphodiesterase-type-v-inhibitors-use-in-eight-european-cities-through-analysis-of-urban-wastewater
#9
Ana Causanilles, Daniela Rojas Cantillano, Erik Emke, Richard Bade, Jose Antonio Baz-Lomba, Sara Castiglioni, Erika Castrignanò, Emma Gracia-Lor, Félix Hernández, Barbara Kasprzyk-Hordern, Juliet Kinyua, Ann-Kathrin McCall, Alexander L N van Nuijs, Benedek G Plósz, Pedram Ramin, Nikolaos I Rousis, Yeonsuk Ryu, Kevin V Thomas, Pim de Voogt
In this work a step forward in investigating the use of prescription drugs, namely erectile dysfunction products, at European level was taken by applying the wastewater-based epidemiology approach. 24-h composite samples of untreated wastewater were collected at the entrance of eight wastewater treatment plants serving the catchment within the cities of Bristol, Brussels, Castellón, Copenhagen, Milan, Oslo, Utrecht and Zurich. A validated analytical procedure with direct injection of filtered aliquots by liquid chromatography-tandem mass spectrometry was applied...
April 2, 2018: Environment International
https://www.readbyqxmd.com/read/29616790/novel-tadalafil-derivatives-ameliorates-scopolamine-induced-cognitive-impairment-in-mice-via-inhibition-of-acetylcholinesterase-ache-and-phosphodiesterase-5-pde5
#10
Wei Ni, Huan Wang, Xiaokang Li, Xinyu Zheng, Manjiong Wang, Jian Zhang, Qi Gong, Dazheng Ling, Fei Mao, Haiyan Zhang, Jian Li
On the basis of the drug-repositioning and redeveloping strategy, first-generation dual-target inhibitors of acetylcholinesterase (AChE) and phosphodiesterase 5 (PDE5) have been recently reported as a potentially novel therapeutic method for the treatment of Alzheimer's disease (AD), and the lead compound 2 has proven this method was feasible in AD mouse models. In this study, our work focused on exploring alternative novel tadalafil derivatives (3a-s). Among the 19 analogues, compound 3c exhibited good selective dual-target AChE/PDE5 inhibition and good blood-brain barrier (BBB) permeability...
April 17, 2018: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29602721/efficacy-and-safety-of-tadalafil-5-mg-once-daily-for-the-treatment-of-erectile-dysfunction-after-robot-assisted-laparoscopic-radical-prostatectomy-a-2-year-follow-up
#11
Soodong Kim, Gyung Tak Sung
BACKGROUND: Although nerve-sparing robot-assisted radical prostatectomy (NS-RALP) is performed, a large number of patients still experience erectile dysfunction (ED) after surgery. AIM: To evaluate the efficacy and safety of tadalafil 5 mg once daily (OaD) in ED treatment over 2 years and investigate the cause of vascular ED after NS-RARP. METHODS: We retrospectively evaluated 95 men who underwent NS-RARP and had a penile rehabilitation treatment with tadalafil 5 mg OaD...
March 27, 2018: Sexual Medicine
https://www.readbyqxmd.com/read/29601254/identification-of-a-new-type-tadalafil-analogue-in-a-supplement-product
#12
Yen-Chun Huang, Hui-Chun Lee, Yun-Lian Lin, Chia-Fen Tsai, Hwei-Fang Cheng
A novel compound structurally similar to tadalafil was found in a dietary supplement by adulterants screening and isolated by column chromatography. After analysis by accurate mass, nuclear magnetic resonance (NMR) and X-ray, the structure of this novel tadalafil analogue was determined as (5R, 16R)-5-(1,3-benzodioxol-5-yl)-2- (3-ethypentan-3-yl)-15,16-dihydro(1H-imidazo[1,5-a]pyrido)[3,4-b]indol-1,3-dione.
March 30, 2018: Food Additives & Contaminants. Part A, Chemistry, Analysis, Control, Exposure & Risk Assessment
https://www.readbyqxmd.com/read/29580120/placental-growth-factor-as-a-predictor-of-the-efficacy-of-tadalafil-treatment-for-fetal-growth-restriction
#13
Michiko Kubo-Kaneda, Hiroaki Tanaka, Shintaro Maki, Masafumi Nii, Takashi Umekawa, Kazuhiro Osato, Yuki Kamimoto, Eiji Kondo, Tomoaki Ikeda
PURPOSE: We recently demonstrated the efficacy of tadalafil treatment for fetal growth restriction (FGR). This study aimed to evaluate the utility of serum placental growth factor (PlGF) level for predicting the efficacy of tadalafil for the treatment of FGR. MATERIALS AND METHODS: The correlations between serum level of PlGF and fetal growth velocity were retrospectively assessed in nine pregnant women receiving tadalafil for FGR before 30 weeks' gestation. RESULTS: Median gestational age was 26 weeks (range 26-28 weeks), and median deviation of estimated fetal weight from standard weight was -2...
March 26, 2018: Journal of Maternal-fetal & Neonatal Medicine
https://www.readbyqxmd.com/read/29577372/effect-of-tadalafil-on-chronic-pelvic-pain-and-prostatic-inflammation-in-a-rat-model-of-experimental-autoimmune-prostatitis
#14
Ken Okamoto, Maki Kurita, Hiroshi Yamaguchi, Yuki Numakura, Michiko Oka
BACKGROUND: Experimental autoimmune prostatitis (EAP) shares important clinical features with clinical chronic prostatitis/chronic pelvic pain. We investigated the effect of tadalafil on pelvic pain and prostatic inflammation in a rat EAP model. METHODS: EAP was induced in rats by intradermal injection of rat prostate antigen and complete Freund's adjuvant on days 0 and 28. Rats were treated with tadalafil (2 mg/kg, p.o.; EAP-tadalafil) or vehicle (EAP-vehicle) once daily from day 0, while sham-operated animals were treated with vehicle only (Sham)...
March 26, 2018: Prostate
https://www.readbyqxmd.com/read/29572341/in-vitro-assessment-of-pharmacokinetic-drug-drug-interactions-of-direct-oral-anticoagulants-type-5-phosphodiesterase-inhibitors-are-inhibitors-of-rivaroxaban-and-apixaban-efflux-by-p-glycoprotein
#15
Victor Margelidon-Cozzolino, Sophie Hodin, Elodie Jacqueroux, Olivier Delezay, Laurent Bertoletti, Xavier Delavenne
Direct oral anticoagulants (DOACs) could represent an interesting alternative to conventional anticoagulant treatment with vitamin K antagonists in pulmonary arterial hypertension (PAH) patients because of lower bleeding risk and their simplicity of use. P-glycoprotein (P-gp) plays a key role in DOACs pharmacokinetics. Type 5-phosphodiesterase inhibitors (PDE5i), a drug class commonly used in the treatment of PAH, have been shown to strongly inhibit P-gp. This work aimed to assess potential P-gp mediated-drug-drug interactions between PDE5i and DOACs using in vitro methods...
March 23, 2018: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/29569389/serenoa-repens-selenium-lycopene-vs-tadalafil-5-mg-for-the-treatment-of-luts-secondary-to-benign-prostatic-obstruction-a-phase-iv-non-inferiority-open-label-clinical-study-sprite-study
#16
Giuseppe Morgia, Giuseppe Vespasiani, Rosaria Maria Pareo, Salvatore Voce, Massimo Madonia, Marco Carini, Antonio Ingrassia, Carlo Terrone, Marcello Gentile, Maurizio Carrino, Antonella Giannantoni, Franco Blefari, Salvatore Arnone, Giorgio Santelli, Giorgio Ivan Russo
INTRODUCTION: In this randomized, open label, not-inferior clinical study, we aimed to compare the efficacy and tolerability of Serenoa Repens (SeR) + Lycopene (Ly) + Selenium (Se) therapy versus Tadalafil 5 mg in patients affected by lower urinary tract symptoms (LUTS). METHODS: From May 2015 to January 2017, 427 patients were enrolled in 21 different centres (ISRCTN73316039). Inclusion criteria were: age between 50 and 80 years old, international prostate symptom score (IPSS) ≥ 12, peak flow ≤15 ml/s, post-void residual (PVR) <100 ml...
March 22, 2018: BJU International
https://www.readbyqxmd.com/read/29566267/tadalafil-attenuates-hypotonicity-induced-ca-2-influx-via-trpv2-and-trpv4-in-primary-rat-bladder-urothelial-cell-cultures
#17
Xiao Dong, Hiroshi Nakagomi, Tatsuya Miyamoto, Tatsuya Ihara, Satoru Kira, Norifumi Sawada, Takahiko Mitsui, Masayuki Takeda
AIMS: To investigate the localization of phosphodiesterase 5 (PDE5) and the molecular mechanism underlying the effect of the PDE5 inhibitor tadalafil in signal transduction in the bladder urothelium. METHODS: PDE5 expression in rat bladder tissues and cultured primary rat bladder urothelial cells was evaluated using immunochemistry and western blot assays. Ca2+ influx in cells exposed to isotonic solution, hypotonic solution, a selective transient receptor potential vanilloid 2 (TRPV2) channel agonist (cannabidiol), a selective TRPV4 channel agonist (GSK1016790A), a TRP cation channel melastatin 7 (TRPM7) channel agonist (PIP2), or a purinergic receptor agonist (ATP) in the presence or absence of 10 µM tadalafil was evaluated using calcium imaging techniques...
March 22, 2018: Neurourology and Urodynamics
https://www.readbyqxmd.com/read/29549279/phosphodiesterase-type-4-inhibition-enhances-nitric-oxide-and-hydrogen-sulfide-mediated-bladder-neck-inhibitory-neurotransmission
#18
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/29527702/efficacy-and-safety-of-daily-use-of-tadalafil-in-treatment-of-patients-with-premature-ejaculation-a-randomised-placebo-controlled-clinical-trial
#19
M Abu El-Hamd
The study aimed to evaluate the efficacy and safety of the once-daily use of 5 mg tadalafil in the treatment of patients with premature ejaculation (PE). In a single-blind placebo-controlled clinical study, it was carried out on 100 patients with PE. All patients were randomised equally divided into two groups (50 patients each). Group 1 was given placebo in the form of oral multivitamin tablet once a day for 6 weeks. Group 2 was given 5 mg tadalafil once a day for 6 weeks. All patients were asked to complete Arabic Index of Premature Ejaculation (AIPE) before and after the treatment...
March 12, 2018: Andrologia
https://www.readbyqxmd.com/read/29526379/an-immunohistochemical-and-ultrastructural-analysis-of-the-retina-in-tadalafil-cialis-treated-rats
#20
Nahla Reda Sarhan, Nesreen Moustafa Omar
Tadalafil (Cialis) is one of the most commonly used phosphodiesterase type5 (PDE5) inhibitors. This work aimed to analyze the histological and ultrastructural changes provoked by chronic tadalafil administration in the rat retina, correlate between such changes and PDE5 immunoexpression and to evaluate the possible reversibility of these changes. Thirty Sprague Dawley male rats were randomly distributed into 3 groups. Control group; given 1 ml distilled water daily for 6 weeks. Tadalafil group; given tadalafil in a daily dose of 2...
May 2018: Acta Histochemica
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