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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...
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
Hegazy Maha, Kessiba Amira, Abdelkawy Mohamed, El Gindy Ahmed Emad
Tadalafil (TAD) and dapoxetine HCl (DAP) are recently co-formulated and both show native fluorescence. Therefore, a novel, accurate, specific and sensitive reversed-phase high performance liquid chromatographic method with fluorescence detection was developed and validated for their separation and quantitation in dosage form and human plasma using avanafil as an internal standard (IS). Separation was achieved using isocratic elution within 7.0 min on C18 column and acetonitrile-0.15% triethylamine (40:60, v/v; pH 4) as a mobile phase...
July 2015: Se Pu, Chinese Journal of Chromatography
Giovanni Corona, Giulia Rastrelli, Andrea Burri, Emmanuele A Jannini, Mario Maggi
INTRODUCTION: The discontinuation rate with phosphodiesterase type 5 inhibitors (PDE5i) remains very high. Recently, a new PDE5ì, avanafil, has become available worldwide. AREAS COVERED: All placebo-controlled randomized clinical trials (RCTs) on the effect of avanafil in patients with ED were reviewed and meta-analyzed. So far, 5 different RCTs on avanafil have been published, including 1379 and 605 patients in active and placebo groups, respectively. Avanafil was up to 3-fold superior to placebo in determining successful sexual intercourse...
2016: Expert Opinion on Drug Safety
Tariq Said Hakky, Lakshay Jain
The causes of male erectile dysfunction (ED) are quite variable and are now commonly divided into etiologies such as ischemia, smooth muscle damage, or altered blood flow. Although varying rates of ED have been reported in literature, the number of men with ED is projected to increase worldwide by 2025 to approximately 322 million. Since the introduction of phosphodiesterase 5 (PDE5) inhibitors, there has been a paradigm shift in the treatment of ED because PDE5 inhibitors address a broad spectrum of etiologies for ED...
June 2015: Turkish Journal of Urology
Jeffery D Evans, Stephen R Hill
BACKGROUND: Numerous pathways can lead to erectile dysfunction (ED) in patients, with some patients having multiple causes. Regardless of the etiology, ED has been successfully treated in many patients with the advent of oral phosphodiesterase-5 inhibitors (PDE5Is). With the release of avanafil, there are currently four PDE5I options available, and choosing between them should be based on patient-specific considerations and preferences. OBJECTIVE: To review the treatment of ED with PDE5Is, taking into account the effectiveness, safety, and patient satisfaction of these agents, as well as avanafil's place in therapy...
2015: Patient Preference and Adherence
Liang Chen, Sergej E L Staubli, Marc P Schneider, Alfons G Kessels, Sandra Ivic, Lucas M Bachmann, Thomas M Kessler
CONTEXT: Erectile dysfunction (ED) is a major health care problem worldwide and phosphodiesterase 5 inhibitors (PDE5Is) are the pharmacological treatment of choice. However, the optimal PDE5I for ED treatment is not known. OBJECTIVE: To investigate trade-offs between efficacy and adverse events for various PDE5Is in treating ED. EVIDENCE ACQUISITION: A review was performed according to the Preferred Reporting Items for Systematic Reviews and Meta-Analyses Statement...
October 2015: European Urology
Sanghapal D Sawant, G Lakshma Reddy, Mohd Ishaq Dar, M Srinivas, Gourav Gupta, Promod Kumar Sahu, Priya Mahajan, Amit Nargotra, Surjeet Singh, Subhash C Sharma, Manoj Tikoo, Gurdarshan Singh, Ram A Vishwakarma, Sajad Hussain Syed
Cyclic guanosine monophosphate (cGMP) specific phosphodiesterase type-5 (PDE5), a clinically proven target to treat erectile dysfunction and diseases associated with lower cGMP levels in humans, is present in corpus cavernosum, heart, lung, platelets, prostate, urethra, bladder, liver, brain, and stomach. Sildenafil, vardenafil, tadalafil and avanafil are FDA approved drugs in market as PDE5 inhibitors for treating erectile dysfunction. In the present study a lead molecule 4-ethoxy-N-(6-hydroxyhexyl)-3-(1-methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidin-5-yl)benzenesulfonamide, that is, compound-4a, an analog of pyrazolopyrimidinone scaffold has been identified as selective PDE5 inhibitor...
May 1, 2015: Bioorganic & Medicinal Chemistry
Y Cui, X Liu, L Shi, Z Gao
We carried out a systematic review and meta-analysis to assess the efficacy and safety of phosphodiesterase type 5 (PDE5) inhibitors for treating erectile dysfunction (ED) after bilateral nerve-sparing radical prostatectomy (BNSRP). A literature review was performed to identify all published randomised double-blind, placebo-controlled trials of PDE5 inhibitors for the treatment of ED after BNSRP. The search included the following databases: MEDLINE, EMBASE and the Cochrane Controlled Trials Register. The reference lists of the retrieved studies were also investigated...
February 2016: Andrologia
Wayne J G Hellstrom, Jed Kaminetsky, Laurence H Belkoff, Irwin Goldstein, James P Tursi, Jonathan Uy, Craig A Peterson, Charles H Bowden, Wesley W Day
PURPOSE: We examined the therapeutic effects of avanafil 15 minutes after dosing in men with mild to severe erectile dysfunction. MATERIALS AND METHODS: This randomized, double-blind, placebo controlled, 12-week study (4-week run-in and 8-week treatment) randomized 145 men to placebo, 147 to avanafil 100 mg and 148 to avanafil 200 mg on demand. The primary efficacy variable was the per subject proportion of sexual attempts during the treatment period in which subjects achieved erection sufficient for vaginal penetration within approximately 15 minutes after dosing as measured by a stopwatch...
August 2015: Journal of Urology
María Alejandra Egui-Rojo, Ignacio Moncada-Iribarren, Joaquín Carballido-Rodríguez, Juan Ignacio Martínez-Salamanca
OBJECTIVES: Avanafil is a highly selective phosfosdiesterase 5 inhibitor (PDE5 inhibitor), with rapid onset of action, approved by the Food and Drug Administration (FDA) and the European Medicines Agency for the treatment of erectile dysfunction (ED). It had been recently commercialized in Spain. This article presents a detailed review of the available literature, where the safety, tolerability and efficacy of avanafil were evaluated. METHODS: A systematic literature search using the Medline database was performed...
December 2014: Archivos Españoles de Urología
Toshiaki Sakamoto, Yuichi Koga, Masataka Hikota, Kenji Matsuki, Michino Murakami, Kohei Kikkawa, Kotomi Fujishige, Jun Kotera, Kenji Omori, Hiroshi Morimoto, Koichiro Yamada
Novel pyrimidine-5-carboxamide derivatives bearing a 3-chloro-4-methoxybenzylamino group at the 4-position were identified as potent and highly selective phosphodiesterase 5 inhibitors. Among them, we successfully found 10j (avanafil) which exhibited a potent relaxant effect on isolated rabbit cavernosum (EC30=2.1 nM) and a high isozyme selectivity.
December 1, 2014: Bioorganic & Medicinal Chemistry Letters
S Gur, S C Sikka, E A Pankey, G F Lasker, S Chandra, P J Kadowitz, W J G Hellstrom
We compared the activity of a new phosphodiesterase-5 inhibitor (PDE5i) avanafil with sildenafil and tadalafil in human and rat corpus cavernosum (CC) tissues. The effect of avanafil with several inhibitors and electrical field stimulation (EFS) was evaluated on CC after pre-contraction with phenylephrine. With the PDE5i, sildenafil and tadalafil, concentration-response curves were obtained and cyclic guanosine monophosphate (cGMP) levels were measured in tissues. Avanafil induced relaxation with maximum response of 74 ± 5% in human CC...
October 2015: Andrologia
Eric G Katz, Ronny Bw Tan, Daniel Rittenberg, Wayne J Hellstrom
The treatment modalities of erectile dysfunction range from oral pharmacotherapy to intracavernosal injections, intraurethral pellets, vacuum erectile devices, and the surgical option of penile prosthesis insertion. Oral phosphodiesterase 5 inhibitors still remain the preferred treatment for patients since they are the least invasive, not to mention that they can be prescribed by non-urologists. Due to these factors, there has been development of newer drugs with fewer side effects. This is a review of the second generation phosphodiesterase 5 inhibitor, avanafil, looking into its pharmacology as well as its clinical utility...
2014: Therapeutics and Clinical Risk Management
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