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Zübeyir Huyut, Nuri Bakan, Serkan Yıldırım, Hamit Hakan Alp
No abstract text is available yet for this article.
March 13, 2018: Medical Science Monitor Basic Research
Yoichi Kadoh, Haruko Miyoshi, Takehiko Matsumura, Yoshihito Tanaka, Mitsuya Hongu, Mayumi Kimura, Kei Takedomi, Kenji Omori, Jun Kotera, Takashi Sasaki, Tamaki Kobayashi, Hiroyuki Taniguchi, Yumi Watanabe, Koki Kojima, Toshiaki Sakamoto, Toshiyuki Himiyama, Eiji Kawanishi
Phosphodiesterase (PDE) 10A is a dual hydrolase of cAMP and cGMP and highly expressed in striatal medium spiny neurons. Inhibition of PDE10A modulates the activity of medium spiny neurons (MSN) via the regulation of cAMP and cGMP. Signal control of MSN is considered associated with psychotic symptoms. Therefore PDE10A inhibitor is expected as a therapeutic method for psychosis disease such as schizophrenia. Avanafil (1) is a PDE5 inhibitor (treatment for erectile dysfunction) discovered by our company. We paid attention to the homology of PDE10A and PDE5 and took advantage of PDE5 inhibitor library to discover PDE10A inhibitors, and found a series of compounds that exhibit higher potency for PDE10A than PDE5...
2018: Chemical & Pharmaceutical Bulletin
Giovanni Corona, Mario Maggi, Emmanuele A Jannini
INTRODUCTION: Erectile dysfunction (ED) is a multidimensional disorder with an estimated prevalence of 1% to 10% in men younger than 40 years and up to 100% in men in their 70s and 80s. AIM: To evaluate the real-life characteristics and unmet needs of men with ED, its impact on well-being, and treatment rates across Europe. METHODS: Adult men in Belgium, France, Germany, Italy, Poland, Portugal, and Spain were invited to participate in the survey...
March 2018: Sexual Medicine
Luigi Di Luigi, Massimiliano Sansone, Andrea Sansone, Roberta Ceci, Guglielmo Duranti, Paolo Borrione, Clara Crescioli, Paolo Sgrò, Stefania Sabatini
Phosphodiesterase type 5 inhibitors (PDE5i) (e.g., sildenafil, tadalafil, vardenafil, and avanafil) are drugs commonly used to treat erectile dysfunction, pulmonary arterial hypertension, and benign prostatic hyperplasia. PDE5i are not prohibited by the World Anti-Doping Agency (WADA) but are alleged to be frequently misused by healthy athletes to improve sporting performance. In vitro and in vivo studies have reported various effects of PDE5i on cardiovascular, muscular, metabolic, and neuroendocrine systems and the potential, therefore, to enhance performance of healthy athletes during training and competition...
November 2017: Current Sports Medicine Reports
Faysal A Yafi, Ira D Sharlip, Edgardo F Becher
INTRODUCTION: Phosphodiesterase type 5 inhibitors (PDE5Is) have demonstrated efficacy in the treatment of erectile dysfunction (ED). Although historically found to have limited drug-related adverse events, emerging data have suggested that PDE5Is might be associated with melanoma or recurrence of prostate cancer after radical prostatectomy. AIM: To summarize the literature on the safety of PDE5Is. METHODS: A literature review was performed through PubMed from 1990 through 2016 regarding ED...
April 2018: Sexual Medicine Reviews
Richard Berges, Dieter Schremmer, Roger Limberg
OBJECTIVE AND METHOD: In the prospective, multicentric, non-interventional AVANTI study, the selection criteria for the PDE-5 inhibitor Avanafil were evaluated and it's acceptance in the treatment of patients with erectile dysfunction was investigated. Data from 1,804 probands with an average age of 58.0 years were analyzed. RESULTS: Doctors and patients most commonly referred to Avanafil as a fast-acting substance (70.6% and 78.6%, respectively). A favorable side-effect profile was more focused when the patient co-decided (62...
June 2017: MMW Fortschritte der Medizin
Hyun Jun Park, Sae Woong Kim, Je Jong Kim, Sung Won Lee, Jae Seung Paick, Tae Young Ahn, Kwangsung Park, Jong Kwan Park, Nam Cheol Park
A multi-center, randomized, double-blind, placebo-controlled study was conducted with 158 subjects who were randomized to placebo or avanafil 50, 100, and 200 mg on demand for 8 weeks to evaluate the safety, tolerability, and efficacy of avanafil in the treatment of erectile dysfunction (ED) in Korean men. The primary outcome was the erectile function (EF) domain score of the International Index of Erectile Function (IIEF) questionnaire. Secondary outcomes included changes in the scores of IIEF questions 3 and 4 (IIEF Q3, Q4) from baseline, changes in all domain scores in the IIEF from baseline, Sexual Encounter Profile questions 2-5 (SEP2-5), the Global Efficacy Assessment Question (GEAQ), and the number of subjects whose EF domain score at the 8th week visit was ≥ 26...
June 2017: Journal of Korean Medical Science
H Sperling
Due to the large number of drugs now available, the therapy of erectile dysfunction has changed profoundly in recent decades. The phosphodiesterase type 5 inhibitors (PDE5-i): sildenafil, taldalafil, vardenafil, and avanafil are EMA European Medicines Agency approved and show similar adverse events and success rates. The absolute contraindication is the simultaneous use of nitrates. Despite this wide variety of options, therapy of erectile dysfunction should be performed in an individually adapted manner. The exact patient's history, physical examination, collaboration of medical disciplines, and choice of therapy will offer every patient the possibility to achieve or regain a satisfying sexual life...
April 2017: Der Urologe. Ausg. A
Sevil Korkmaz-Icöz, Tamás Radovits, Gábor Szabó
Phosphodiesterase type 5 (PDE5) selectively hydrolyses the second messenger cGMP into 5'-GMP, thereby regulating its intracellular concentrations. Dysregulation of the cGMP-dependent pathway plays a significant role in various cardiovascular diseases. Therefore, its modulation by drugs, such as PDE5 inhibitors, may represent an effective therapeutic approach. There are currently four PDE5 inhibitors available for the treatment of erectile dysfunction: sildenafil, vardenafil, tadalafil and avanafil. Sildenafil and tadalafil have also received Food and Drug Administration approval for the treatment of pulmonary arterial hypertension...
January 2018: British Journal of Pharmacology
Carmen Lorenz, Pierre Lesimple, Raul Bukowiecki, Annika Zink, Gizem Inak, Barbara Mlody, Manvendra Singh, Marcus Semtner, Nancy Mah, Karine Auré, Megan Leong, Oleksandr Zabiegalov, Ekaterini-Maria Lyras, Vanessa Pfiffer, Beatrix Fauler, Jenny Eichhorst, Burkhard Wiesner, Norbert Huebner, Josef Priller, Thorsten Mielke, David Meierhofer, Zsuzsanna Izsvák, Jochen C Meier, Frédéric Bouillaud, James Adjaye, Markus Schuelke, Erich E Wanker, Anne Lombès, Alessandro Prigione
Mitochondrial DNA (mtDNA) mutations frequently cause neurological diseases. Modeling of these defects has been difficult because of the challenges associated with engineering mtDNA. We show here that neural progenitor cells (NPCs) derived from human induced pluripotent stem cells (iPSCs) retain the parental mtDNA profile and exhibit a metabolic switch toward oxidative phosphorylation. NPCs derived in this way from patients carrying a deleterious homoplasmic mutation in the mitochondrial gene MT-ATP6 (m.9185T>C) showed defective ATP production and abnormally high mitochondrial membrane potential (MMP), plus altered calcium homeostasis, which represents a potential cause of neural impairment...
May 4, 2017: Cell Stem Cell
Kareem AbuBakr Soliman, Howida Kamal Ibrahim, Mahmoud Mohammed Ghorab
The study investigated the effects of different combined top-down and bottom-up nanocrystallization technologies on particle size and solid state of avanafil nanoparticles. Combined antisolvent precipitation-ultrasonication (sonoprecipitation) technique was adopted to prepare 18 formulas according to 3(2).2(1) factorial design using 3 stabilizers; Tween 80, polyvinyl alcohol (PVA) and Pluronic F68 at different concentrations with different cryoprotectants. Particle size analysis of the lyophilized formulas showed that Tween 80 was an effective nanoparticles stabilizer in contrast to Pluronic F68 and PVA which failed to prevent nanoparticles flocculation when they were used at high concentration...
January 30, 2017: International Journal of Pharmaceutics
Taymour Mostafa
INTRODUCTION: Phosphodiesterase type 5 (PDE-5) hydrolyzes cyclic guanylate monophosphate (cGMP) specifically to 5' GMP, promoting successful corporeal vascular relaxation and penile erection during sexual stimulation. Oral PDE-5 inhibitors such as sildenafil, vardenafil, tadalafil, and avanafil have provided noninvasive, effective, well-tolerated treatment for erectile dysfunction (ED) patients and, at the same time, stimulated both academic and clinical interests. Lately, some oral PDE-5 inhibitors were released as low-dose preparations with the concept of potential daily administration and long-term use...
July 2016: Sexual Medicine Reviews
Kareem AbuBakr Soliman, Howida Kamal Ibrahim, Mahmoud Mohammed Ghorab
Avanafil was incorporated into solid self-nanoemulsifying systems with the aim of improving its oral bioavailability. Labrafil, Labrafac, and Miglyol 812 N were investigated as oils, Tween 80 and Cremophor EL as surfactants, and Transcutol HP as a co-surfactant. Nine formulations produced clear solutions of 13.89-38.09nm globules after aqueous dilution. Adsorption of preconcentrate onto Aeroperl 300 Pharma at a 2:1 ratio had no effect on nanoemulsion particle size. Differential scanning calorimetry, X-ray diffraction, and scanning electron microscopy indicated that avanafil was molecularly dispersed within the solid nanosystems...
October 10, 2016: European Journal of Pharmaceutical Sciences
Kareem AbuBakr Soliman, Howida Kamal Ibrahim, Mahmoud Mohammed Ghorab
In this study, we examined the effect of different polymers on the chemical, physical and pharmacokinetic properties of avanafil-β-cyclodextrin (β-CD) inclusion complex. Equimolar mixtures of drug and β-CD were used to prepare 25 ternary drug-β-CD-polymer inclusion complexes using five different polymers, polyethylene glycol (PEG 4000), polyvinyl pyrrolidone (PVP K-30), chitosan, hydroxypropylmethyl cellulose, and hydroxyethyl cellulose, each in five different concentrations, 1, 3, 5, 7, and 10% (w/w). The addition of 10% (w/w) PEG 4000 resulted in a significant decrease of drug solubility, where the infrared spectra and differential scanning thermograms revealed an interaction between PEG 4000 and avanafil which hindered drug inclusion...
October 15, 2016: International Journal of Pharmaceutics
Jonathan L Zurawin, Carrie A Stewart, James E Anaissie, Faysal A Yafi, Wayne J G Hellstrom
INTRODUCTION: Erectile dysfunction (ED) affects millions of men worldwide, and the incidence of ED will continue to increase as the aging population grows. The first generation of phosphodiesterase-5 (PDE5) inhibitors, the mainstay of oral ED therapy, has revolutionized the treatment of this condition, but not without some drawbacks. Avanafil, the only United States and European Union-approved second-generation PDE5 inhibitor, is a safe and efficacious alternative to its predecessors...
September 2016: Expert Review of Clinical Pharmacology
Vincenzo Mirone, Ferdinando Fusco, Fabio Parazzini, Alessandro Zucchi
INTRODUCTION: PDE5 inhibitors are the firstline treatment for erectile dysfunction. Although all these drugs share the same mechanism of action, each agent could have different characteristics in terms of selectivity, pharmacokinetics and tolerability profile. MATERIALS AND METHODS: This manuscript illustrates a project, undertaken by the Italian Society of Urology in order to obtain a "snapshot" of the experience of Italian urologists with the use of PDE5 inhibitors in the clinical practice...
July 4, 2016: Archivio Italiano di Urologia, Andrologia
Luca Boeri, Paolo Capogrosso, Eugenio Ventimiglia, Alessandro Serino, Giovanni La Croce, Andrea Russo, Rocco Damiano, Francesco Montorsi, Andrea Salonia
INTRODUCTION: Phosphodiesterase type 5 inhibitors (PDE5Is) represent the first-line treatment for erectile dysfunction (ED). Almost one in two patients, however, show some level of treatment dissatisfaction and up to 30% fail to respond to any of the currently available PDE5Is. Recently, the second-generation PDE5I avanafil was launched for the treatment of ED. AREAS COVERED: Pivotal studies of clinical development along with placebo-controlled randomized clinical trials (RCTs) of avanafil in patients with ED were reviewed...
September 2016: Expert Review of Clinical Pharmacology
Giovanni Ribaudo, Mario Angelo Pagano, Sergio Bova, Giuseppe Zagotto
BACKGROUND: Phosphodiesterase 5 inhibitors (PDE5-Is) sildenafil, vardenafil, tadalafil and the recently approved avanafil represent the first-line choice for both on-demand and chronic treatment of erectile dysfunction (ED). In addition to this, sildenafil and tadalafil, have also been approved for the treatment of pulmonary arterial hypertension. Due to its expression and localization in many tissues, PDE5 and its regulation has been reported to be involved in several other diseases...
2016: Current Medicinal Chemistry
(no author information available yet)
Multivariate UV-spectrophotometric methods and Quality by Design (QbD) HPLC are described for concurrent estimation of avanafil (AV) and dapoxetine (DP) in the binary mixture and in the dosage form. Chemometric methods have been developed, including classical least-squares, principal component regression, partial least-squares, and multiway partial least-squares. Analytical figures of merit, such as sensitivity, selectivity, analytical sensitivity, LOD, and LOQ were determined. QbD consists of three steps, starting with the screening approach to determine the critical process parameter and response variables...
April 7, 2016: Journal of AOAC International
Mallesh Kurakula, Osama A A Ahmed, Usama A Fahmy, Tarek A Ahmed
CONTEXT: Avanafil (AVA) is used in the treatment of erectile dysfunction, but is reported for its poor aqueous solubility. Solid lipid nanoparticles (SLNs) are lipid carriers that can greatly enhance drug solubility and bioavailability. OBJECTIVE: This work was aimed to formulate and optimize AVA SLNs with subsequent loading into hydrogel films for AVA transdermal delivery. MATERIALS AND METHODS: AVA SLNs were prepared utilizing homogenization followed by ultra-sonication technique...
December 2016: Journal of Liposome Research
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