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Yong-Soon Cho, Yook-Hwan Noh, Hyeong-Seok Lim, Sang-Heon Cho, Jong-Lyul Ghim, Sangmin Choe, Soon-Bae Kim, Jung-Sik Park, Sang-Koo Lee, Won-Seok Yang, Jai-Won Chang, Mi-Young Bahng, Kyun-Seop Bae
Udenafil is a phosphodiesterase-5 inhibitor used to treat erectile dysfunction. Although udenafil is not predominantly eliminated by the kidney, renal impairment can alter its secretion/transport pathways. Drug pharmacokinetics and safety must therefore be assessed in subjects with a renal impairment. We investigated the effects of impaired renal function on the pharmacokinetics and safety of a single 100-mg oral dose of udenafil in a single-dose, open-label, parallel-group study of 31 subjects. Cockcroft-Gault creatinine clearance was used to stratify these subjects into healthy controls (>80 mL·min-1 ) and individuals with mild (50 to ≤80 mL·min-1 ), moderate (30 to ≤50 mL·min-1 ), and severe (<30 mL·min-1 ) renal impairment...
March 14, 2018: Journal of Clinical Pharmacology
Bo Ram Choi, Hye Kyung Kim, Jong Kwan Park
PURPOSE: The objective of this study was to evaluate the relaxant effect of scoparone from Artemisia capillaris on rabbit penile corpus cavernosum smooth muscle (PCCSM) and to elucidate the mechanism of action of scoparone for the treatment of erectile dysfunction (ED). MATERIALS AND METHODS: PCCSM that had been precontracted with phenylephrine was treated with 3 Artemisia herbs (A. princeps, A. capillaris, and A. iwayomogi) and 3 fractions (n-hexane, ethyl acetate, and n-butanol) with different concentrations (0...
December 2017: World Journal of Men's Health
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)...
January 2018: World Journal of Men's Health
Seung T Han, Jae S Kim, Jun Y Lee, Min K Kim, Jin S Yoo, Byoung G Han, Seung O Choi, Jae W Yang
Phosphodiesterase-5 (PDE-5) inhibitors induces vasodilation in several organs by blocking cyclic GMP (guanosine monophosphate) degradation. However, the existence of alternative mechanism of action in case of an impaired nitric oxide (NO) system remains controversial. Previous studies suggested that decreased NO bioavailability may result in the downregulation of klotho expression, but the relationship between klotho and NO remains obscure. Therefore, we investigated whether a PDE-5 inhibitor could preserve epithelial-mesenchymal transition (EMT) and relationship exists between the NO and renal klotho expression...
March 2018: Clinical and Experimental Pharmacology & Physiology
Hea Min Yu, Hyo Kyun Chung, Koon Soon Kim, Jae Min Lee, Jun Hwa Hong, Kang Seo Park
Adipocytes are involved in many metabolic disorders. It was recently reported that phosphodiesterase type 5 (PDE5) is expressed in human adipose tissue. In addition, PDE5 inhibitors have been shown to improve insulin sensitivity in humans. However, the mechanism underlying the role of PDE5 inhibitors as an insulin sensitizer remains largely unknown. The present study was undertaken to investigate the role of the PDE5 inhibitor udenafil in insulin signaling in adipocytes and whether this is mediated through the regulation of mitochondrial function...
November 4, 2017: Biochemical and Biophysical Research Communications
Yusuf Özlülerden, Cihan Toktaş, Hülya Aybek, Vural Küçükatay, Nilay Şen Türk, Ali Ersin Zumrutbas
PURPOSE: The aim of this study was to investigate and compare the effects of udenafil and mannitol in an experimental renal ischemia-reperfusion (I/R) injury model. MATERIALS AND METHODS: A total of 64 female Wister Albino rats were used. Right nephrectomy was performed in all groups. In the control group; I/R injury was not performed. In the I/R group; left renal pedicle was clamped for 45 minutes and then underwent 60 minutes and 24 hours of reperfusion. In the mannitol group; 1 mL 20% mannitol was given intravenously 15 minutes before clamping...
July 2017: Investigative and Clinical Urology
Jing Li, Si Hun Roh, Jia Shaodong, Ji Yeon Hong, Dong-Kyu Lee, Byong-Kyu Shin, Jeong Hill Park, Jeongmi Lee, Sung Won Kwon
A novel analytical method for the simultaneous determination of the concentration of sildenafil and its five analogues in dietary supplements using solid-phase extraction assisted reversed-phase dispersive liquid-liquid microextraction based on solidification of floating organic droplet combined with ion-pairing liquid chromatography with an ultraviolet detector was developed. Parameters that affect extraction efficiency were systematically investigated, including the type of solid-phase extraction cartridge, pH of the extraction environment, and the type and volume of extraction and dispersive solvent...
August 2017: Journal of Separation Science
David J Goldberg, Victor Zak, Bryan H Goldstein, Shan Chen, Michelle S Hamstra, Elizabeth A Radojewski, Eileen Maunsell, Seema Mital, Shaji C Menon, Kurt R Schumacher, R Mark Payne, Mario Stylianou, Jonathan R Kaltman, Tina M deVries, James L Yeager, Stephen M Paridon
BACKGROUND: The Fontan operation results in a circulation that is dependent on low pulmonary vascular resistance to maintain an adequate cardiac output. Medical therapies that lower pulmonary vascular resistance may augment cardiac output and improve long-term outcomes. OBJECTIVES: This phase I/II clinical trial conducted by the Pediatric Heart Network was designed to evaluate short-term safety, pharmacokinetics (PK), and preliminary efficacy of udenafil in adolescents following Fontan...
June 2017: American Heart Journal
Renato De Vecchis, Arturo Cesaro, Carmelina Ariano, Anna Giasi, Carmela Cioppa
BACKGROUND: Several studies have compared the use of phosphodiesterase-5 (PDE5) inhibitors sildenafil or udenafil with the placebo in patients suffering from pulmonary hypertension (PH) due to left chronic heart failure (CHF), corresponding to group 2 (PH due to left heart disease) of the PH classification (according to 2015 ESC/ERS guidelines for the diagnosis and treatment of PH). The results of the use of PDE5 inhibitors in the PH due to left heart disease were inconsistent and heterogeneous...
June 2017: Journal of Clinical Medicine Research
Hamit H Alp, Zübeyir Huyut, Serkan Yildirim, Yıldıray Başbugan, Levent Ediz, Mehmet R Şekeroğlu
Osteoporosis is a major public health problem associated with many factors, and it affects more than 50% of women over 50 years old. In the current study, our purpose was to investigate the effects of phosphodiestarase-5 inhibitors on osteoporosis via the nitric oxide/3',5'-cyclic guanosine monophosphate/protein kinase G signalling pathway. A total of 50 female albino Wistar rats were separated into five groups. The first group was appointed as the healthy control group with no ovariectomy. All animals in the other groups underwent a bilateral ovariectomy...
May 2017: Experimental Biology and Medicine
Juhyun Park, Oh Seong Kwon, Sung Yong Cho, Jae-Seung Paick, Soo Woong Kim
The efficacy of statins is related to the 'common soil' hypothesis, which proposes oxidative stress and inflammation as main pathophysiologic processes in the disease group of diabetes and endothelial dysfunction. This study evaluated the recovery of erectile function after administration of chronic statin alone in streptozotocin (STZ)-induced diabetes mellitus (DM) rats, focusing on the anti-oxidative effects and consequentially recuperated endothelial function. A total of 45 male Sprague-Dawley rats (8 weeks old) were divided into three groups (n = 15 each): an age-matched normal control group (Control group), an uncontrolled DM group (DM group), and a statin-treated group (Statin group)...
2017: PloS One
Ki Hak Moon, Sae Woong Kim, Du Geon Moon, Je Jong Kim, Nam Cheol Park, Sung Won Lee, Jae-Seung Paick, Tai Young Ahn, Woo Sik Chung, Kwon Sik Min, Jong Kwan Park, Dae Yul Yang, Hong Seok Shin, Kwangsung Park
INTRODUCTION: Once-daily administration of phosphodiesterase type 5 inhibitors has been shown to correct erectile dysfunction (ED). AIM: To evaluate the long-term efficacy and safety after once-daily oral administration of udenafil 75 mg in men with ED. METHODS: This clinical trial was an open-label, fixed-dose, 24-week extension study (DA8159_EDDL_III) of a 24-week double-blinded efficacy and safety study of once-daily udenafil (parent study: DA8159_EDD_III)...
August 2016: Journal of Sexual Medicine
Anhye Kim, Jongtae Lee, Donghoon Shin, Yong Jin Jung, Mi Young Bahng, Joo-Youn Cho, In-Jin Jang
AIMS: The aim of this study was to develop a population pharmacokinetic (PK) model of udenafil and its active metabolite, DA-8164, in healthy subjects and patients with hepatic impairment (HI) and to estimate the optimal dosing recommendations for patients with HI. METHODS: An open label, three parallel group, age and weight matched control study was conducted in 18 volunteers, six healthy subjects (n = 6) and patients with mild (Child-Pugh class A, n = 6) and moderate HI (Child-Pugh class B, n = 6)...
August 2016: British Journal of Clinical Pharmacology
Hyang-Ki Choi, Jin Ah Jung, Jihong Shon, Mi Young Bahng, Doo-Yeoun Cho, Chang Woo Yeo, Eun-Young Kim, Jae-Gook Shin
Udenafil, a cyclic guanosine monophosphate-specific phosphodiesterase type 5 inhibitor, has been developed to treat erectile dysfunction. We evaluated the effect of age on the pharmacokinetics and tolerability of udenafil. A single-center, open-label, parallel-group phase 1 study was conducted in healthy adult subjects who took a single oral dose of udenafil (100 mg). The pharmacokinetics and tolerability of udenafil were compared between 12 healthy young men (21-27 years) and 12 healthy elderly men (65-78 years)...
November 2016: Journal of Clinical Pharmacology
T H Kim, Y-S Ha, S H Choi, E S Yoo, B W Kim, S-J Yun, W-J Kim, Y S Kwon, T G Kwon
No abstract text is available yet for this article.
March 2016: International Journal of Impotence Research
Lokman Irkilata, Hasan Riza Aydin, Ismail Ozer, Mustafa Aydin, Hüseyin Cihan Demirel, Caner Moral, Mustafa Kemal Atilla
INTRODUCTION: Erectile dysfunction (ED) is frequently observed in end-stage renal disease (ESRD) patients on hemodialysis (HD) compared to non-uremic patients. This situation causes severe psychogenic problems in patients and disrupts the quality of life. Different phosphodiesterase type 5 (PDE-5) inhibitors have been used, and efficacies revealed, for the treatment of ED in HD patients; however, there are no studies related to udenafil use or results for HD patients. This study retrospectively evaluated the efficacy and reliability of udenafil for HD patients...
2016: Renal Failure
T-H Kim, Y-S Ha, S H Choi, E S Yoo, B W Kim, S-J Yun, W-J Kim, Y S Kwon, T G Kwon
Udenafil is a selective phosphodiesterase type 5 inhibitor made available in recent years for the treatment of erectile dysfunction. Herein, we evaluated independent predictors of potency recovery in radical prostatectomy (RP) patients who underwent penile rehabilitation with udenafil 50 mg. One hundred and forty-three men who underwent RP were enrolled in a penile rehabilitation program using udenafil 50 mg every other day. The rate of regained potency in the study group was significantly higher compared with the recovery rate seen in patients who were not part of the penile rehabilitation program (41...
January 2016: International Journal of Impotence Research
B R Choi, S K Kumar, C Zhao, L T Zhang, C Y Kim, S W Lee, J-H Jeon, K K Soní, I So, S H Kim, N C Park, H K Kim, J K Park
The objective was to investigate the cellular effect and action mechanism of Artemisia capillaris extract (ACE) and its component, scopoletin, on penile corpus cavernosum smooth muscle (PCCSM). In vitro study with PCCSM, the precontracted PCCSM with phenylephrine was treated with ACE or scopoletin. Cyclic nucleotides in the perfusate were measured by radioimmunoassay and expression of protein and mRNA of endothelial nitric oxide synthase (eNOS) and neuronal nitric oxide synthase in the perfused PCCSM were measured by western blot and real-time PCR, respectively...
November 2015: International Journal of Impotence Research
Amit S Mutha, Vijay R Kulkarni, Sagar B Bhagat, Amit S Beldar, Sadiq B Patel
INTRODUCTION: Erectile dysfunction (ED) is a common occurrence and its incidence is expected to increase significantly along with the increase in various lifestyle diseases. The drug utilization for ED is very low. Also, studies describing the prescription pattern in ED are lacking. MATERIALS AND METHODS: We conducted a retrospective cross-sectional observational study, including a drug utilization analysis, of 606 prescriptions as per the standard guidelines (WHO and STROBE)...
July 2015: Journal of Clinical and Diagnostic Research: JCDR
Tae Yoon Lee, Jung Sik Choi, Hyoung-Chul Oh, Tae Jun Song, Jae Hyuk Do, Young Koog Cheon
BACKGROUND/AIMS: Acute pancreatitis is a common complication of endoscopic retrograde cholangiopancreatography (ERCP). Combination therapy w ith ora l udenafil and aceclofenac may reduce the occurrence of post-ERCP pancreatitis by targeting different pathophysiological mechanisms. We investigated whether combining udenafil and aceclofenac reduced the rates of post-ERCP pancreatitis. METHODS: A prospective, randomized, double-blind, placebo-controlled, multicenter study was conducted in four academic medical centers...
September 2015: Korean Journal of Internal Medicine
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