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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
#1
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/29526379/an-immunohistochemical-and-ultrastructural-analysis-of-the-retina-in-tadalafil-cialis-treated-rats
#2
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...
March 8, 2018: Acta Histochemica
https://www.readbyqxmd.com/read/29402684/implications-of-survey-labels-and-categorisations-for-understanding-drug-use-in-the-context-of-sex-among-gay-and-bisexual-men-in-melbourne-australia
#3
Kathleen E Ryan, Anna L Wilkinson, Alisa Pedrana, Brendan Quinn, Paul Dietze, Margaret Hellard, Mark Stoové
BACKGROUND: Reliably measuring drug use by gay, bisexual and other men who have sex with men (GBM) in the context of sex can inform sexual health service responses. We report changing drug use patterns among GBM testing for HIV at a community-based service in Melbourne in response to behavioural survey modifications. METHODS: Surveys were completed by GBM prior to all HIV tests. Survey one asked about use of "party drugs for the purpose of sex" and survey two asked about specific drug use (alcohol, amyl nitrate, methamphetamine, cocaine, ecstasy, GHB, Viagra®/Cialis®) before or during sex...
February 2, 2018: International Journal on Drug Policy
https://www.readbyqxmd.com/read/29313080/evolution-of-potent-odorants-within-the-volatile-metabolome-of-high-quality-hazelnuts-corylus-avellana-l-evaluation-by-comprehensive-two-dimensional-gas-chromatography-coupled-with-mass-spectrometry
#4
Marta Cialiè Rosso, Erica Liberto, Nicola Spigolon, Mauro Fontana, Marco Somenzi, Carlo Bicchi, Chiara Cordero
Within the pattern of volatiles released by food products (volatilome), potent odorants are bio-active compounds that trigger aroma perception by activating a complex array of odor receptors (ORs) in the regio olfactoria. Their informative role is fundamental to select optimal post-harvest and storage conditions and preserve food sensory quality. This study addresses the volatile metabolome from high-quality hazelnuts (Corylus avellana L.) from the Ordu region (Turkey) and Tonda Romana from Italy, and investigates its evolution throughout the production chain (post-harvest, industrial storage, roasting) to find functional correlations between technological strategies and product quality...
January 9, 2018: Analytical and Bioanalytical Chemistry
https://www.readbyqxmd.com/read/29194814/how-sildenafil-viagra-%C3%A2-may-cause-melanoma-a-histopathologic-study-providing-a-potential-physiological-etiopathological-mechanism
#5
LETTER
W C Lambert, M W Lambert, C M Ring, C E Gagna, J D Espinal-Mariotte, R A Schwartz
No abstract text is available yet for this article.
December 1, 2017: Journal of the European Academy of Dermatology and Venereology: JEADV
https://www.readbyqxmd.com/read/29132113/fluorometric-detection-of-protein-ligand-engagement-the-case-of-phosphodiesterase5
#6
Giulia Di Rocco, Ilaria Martinelli, Salvatore Pacifico, Remo Guerrini, Elena Cichero, Paola Fossa, Silvia Franchini, Silvia Cardarelli, Mauro Giorgi, Marco Sola, Glauco Ponterini
Phosphodiesterases (PDEs) regulate the intracellular levels of cAMP and cGMP. The great clinical success of the PDE5 inhibitors, Sildenafil (Viagra), Vardenafil (Levitra) and Tadalafil (Cialis) has led to an increasing interest for this class of enzymes. Recent studies have shown a correlation between tumor growth and PDE5 overexpression, making PDE5-selective inhibitors promising candidates for cancer treatment. The search for such inhibitors rests today on radioactive assays. In this work, we exploit the conserved catalytic domain of the enzyme and propose a faster and safer method for detecting the binding of ligands and evaluate their affinities...
February 5, 2018: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28719717/audiometry-results-and-teoae-and-dpoae-amplitudes-in-men-taking-a-phosphodiesterase-type-5-inhibitor-for-erectile-dysfunction
#7
Sertan Öntepeli, Nuray Bayar Muluk, Devrim Tuğlu, Timuçin Şipal
We conducted a prospective study of transient evoked otoacoustic emissions (TEOAEs) and distortion-product otoacoustic emissions (DPOAEs) in men who were taking an oral phosphodiesterase type 5 (PDE5) inhibitor for erectile dysfunction. Our study group was made up of 30 men (60 ears), aged 34 to 60 years (mean: 50.9). They were randomly divided into three groups; 10 men were given sildenafil (Viagra) at 50 mg twice a week, 10 were given tadalafil (Cialis) at 20 mg twice a week, and 10 were given vardenafil (Levitra) at 20 mg twice a week...
July 2017: Ear, Nose, & Throat Journal
https://www.readbyqxmd.com/read/28606335/atr-ftir-characterization-of-generic-brand-named-and-counterfeit-sildenafil-and-tadalafil-based-tablets-found-on-the-brazilian-market
#8
José Coelho Neto, Fernanda L C Lisboa
Viagra and Cialis are among the most counterfeited medicines in many parts of the world, including Brazil. Despite the many studies that have been made regarding discrimination between genuine and counterfeit samples, most published works do not contemplate generic and similar versions of these medicines and also do not explore excipients/adjuvants contributions when characterizing genuine and suspected samples. In this study, we present our findings in exploring ATR-FTIR spectral profiles for characterizing both genuine and questioned samples of several generic and brand-name sildenafil- and tadalafil-based tablets available on the Brazilian market, including Viagra and Cialis...
July 2017: Science & Justice: Journal of the Forensic Science Society
https://www.readbyqxmd.com/read/28579005/tadalafil-solid-dispersion-formulations-based-on-pvp-va-s-630-improving-oral-bioavailability-in-rats
#9
Jin-Seok Choi, Sang-Eun Lee, Woo Suk Jang, Jong Chan Byeon, Jeong-Sook Park
Here, solid dispersion (SD) techniques were utilized to improve the oral bioavailability of tadalafil (TDF). Poly(vinyl pyrrolidone-covinyl acetate) (PVP/VA S-630; 60% VP and 40% VA; MW 50,000) SD formulations were previously found to improve the solubility and dissolution (%) of TDF. The effect of various weak acids and bases on SD formulations was also investigated herein. PVP/VA S-630 SD formulations in combination with weak acids and bases increased the apparent solubility of TDF. After 1h, the apparent solubility of PVP/VA S-630 SD formulations with MgO, meglumine, and tartaric acid were significantly higher by 387...
August 30, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28450170/use-of-acidifier-and-solubilizer-in-tadalafil-solid-dispersion-to-enhance-the-in-vitro-dissolution-and-oral-bioavailability-in-rats
#10
Jin-Seok Choi, Soon-Hyung Kwon, Sang-Eun Lee, Woo Suk Jang, Jong Chan Byeon, Hyeong Mo Jeong, Jeong-Sook Park
The purpose of this study is to improve the solubility, in vitro dissolution, and oral bioavailability in rats of tadalafil (TDF) by using SD technique with a weak acid and a copolymer. TDF-SD was prepared via solvent evaporation, coupled with the incorporation of an acidifier and solubilizer. Tartaric acid enhanced the solubility of TDF over 5-fold in DW, and Soluplus® enhanced the solubility of TDF over 8.7-fold and 19.2-fold compared to that of TDF (pure) in DW and pH 1.2 for 1h, respectively. The optimal formulation of TDF-SD3 was composed of TDF vs Tartaric acid vs Soluplus® vs Aerosil=1:1:3:3...
June 30, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27919702/design-of-pvp-va-s-630-based-tadalafil-solid-dispersion-to-enhance-the-dissolution-rate
#11
Jin-Seok Choi, Jeong-Sook Park
Tadalafil (TDF) is a Biopharmaceutics Classification System (BCS) class II drug; the efficacy thereof is critically limited by inherent poor water solubility. Solid dispersion (SD) techniques are widely used to improve the bioavailability of drugs that are poorly water-soluble. Herein, we used an SD technique to improve the solubility and in vitro dissolution rate of TDF; a solvent evaporation method was applied involving the use of hydrophilic carriers (PVP/VA S-630) and assistants (malic acid or meglumine)...
January 15, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27860446/a-genetic-algorithm-based-framework-for-wavelength-selection-on-sample-categorization
#12
Michel J Anzanello, Gabrielli Yamashita, Marcelo Marcelo, Flávio S Fogliatto, Rafael S Ortiz, Kristiane Mariotti, Marco F Ferrão
In forensic and pharmaceutical scenarios, the application of chemometrics and optimization techniques has unveiled common and peculiar features of seized medicine and drug samples, helping investigative forces to track illegal operations. This paper proposes a novel framework aimed at identifying relevant subsets of attenuated total reflectance Fourier transform infrared (ATR-FTIR) wavelengths for classifying samples into two classes, for example authentic or forged categories in case of medicines, or salt or base form in cocaine analysis...
August 2017: Drug Testing and Analysis
https://www.readbyqxmd.com/read/27800121/erectile-dysfunction-drugs-changed-the-protein-expressions-and-activities-of-drug-metabolising-enzymes-in-the-liver-of-male-rats
#13
Salah A Sheweita, Mona Wally, Mostafa Hassan
Erectile dysfunction (ED) is a major health problem and is mainly associated with the persistent inability of men to maintain sufficient erection for satisfactory sexual performance. Millions of men are using sildenafil, vardenafil, and/or tadalafil for ED treatment. Cytochrome P450s (CYPs) play a central role in the metabolism of a wide range of xenobiotics as well as endogenous compounds. Susceptibility of individuals to the adverse effects of different drugs is mainly dependent on the expression of CYPs proteins...
2016: Oxidative Medicine and Cellular Longevity
https://www.readbyqxmd.com/read/27650039/propping-up-pharma-s-natural-neoliberal-phallic-man-pharmaceutical-representations-of-the-ideal-sexuopharmaceutical-user
#14
Maria Gurevich, Usra Leedham, Amy Brown-Bowers, Nicole Cormier, Zara Mercer
Contemporary social theorists emphasise the cultural quest for authenticity under conditions of increasing artificiality. Within this context, the body is commonly treated as an 'unfinished' surface requiring ongoing transformation to fulfil identity obligations. In this paper, we examine one such identity authentication project in the form of marketing of men's sexuopharmaceuticals. We use online pharmaceutical advertising for four approved sexuopharmaceuticals (Viagra, Cialis, STAXYN and Stendra) to describe the ideal neoliberal consumer...
April 2017: Culture, Health & Sexuality
https://www.readbyqxmd.com/read/27152308/flibanserin-for-treating-hypoactive-sexual-desire-disorder
#15
REVIEW
Jae Hong Sang, Tae-Hee Kim, Soo Ah Kim
There have been several products developed for male sexual dysfunction. However, developing agents for female sexual dysfunction is lagging behind for various reasons. Sildenafil citrate (Viagra) and Tadalafil (Cialis), which have been prescribed for male sexual function disorders, are known to act on vessels.[1] On the other hand, flibanserin is thought to act on brain. Flibanserin has been approved by U. S. Food and Drug Administration (FDA) for treatment of hypoactive sexual desire disorder (HSDD) of premenopausal women in 2015, and is expected to be released in South Korea soon...
April 2016: Journal of Menopausal Medicine
https://www.readbyqxmd.com/read/26637485/study-on-health-hazards-through-medicines-purchased-on-the-internet-a-cross-sectional-investigation-of-the-quality-of-anti-obesity-medicines-containing-crude-drugs-as-active-ingredients
#16
Naoko Yoshida, Midori Numano, Yoko Nagasaka, Kaori Ueda, Hirohito Tsuboi, Tsuyoshi Tanimoto, Kazuko Kimura
BACKGROUND: Weight-loss medicines, including crude drugs and herbal supplements disguised as diet-aid products, are readily obtainable and distributed widely, especially in Southeast Asia. Even if such products are unapproved or prescription-only medicines, consumers can purchase them through an agency or directly on the Internet. We evaluated the quality and safety of herbal products purchased on the Internet to reveal their influence on public health. METHODS: Diet-aid products containing Bukuryo (Poria sclerotium), Bakumondo (Ophiopogonis tuber), or Daio (rhubarb rhizome) were purchased through websites that did not provide physical addresses or which advertised misleading medicines (e...
2015: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/26551887/the-cyclic-gmp-protein-kinase-g-pathway-as-a-therapeutic-target-in-head-and-neck-squamous-cell-carcinoma
#17
Traci R Tuttle, Michelle L Mierzwa, Susanne I Wells, Sejal R Fox, Nira Ben-Jonathan
Head and neck squamous cell carcinoma (HNSCC) is an aggressive disease with high mortality. Treatments, which can result in significant morbidity, have not substantially changed in three decades. The second messenger cyclic GMP (cGMP), which targets protein kinase G (PKG), is generated by guanylate cyclases (GCs), and is rapidly hydrolyzed by phosphodiesterases (PDEs). Activation of the cGMP/PKG pathway is antineoplastic in several cancer types, but its impact on HNSCC has not been fully exploited. We found differential expression of critical components of this pathway in four HNSCC cell lines...
January 28, 2016: Cancer Letters
https://www.readbyqxmd.com/read/26033891/physical-profiling-and-ir-spectroscopy-simple-and-effective-methods-to-discriminate-between-genuine-and-counterfeit-samples-of-viagra%C3%A2-and-cialis%C3%A2
#18
Deborah Custers, Suzanne Vandemoortele, Jean-Luc Bothy, Jacques O De Beer, Patricia Courselle, Sandra Apers, Eric Deconinck
Counterfeit medicines are a global threat to public health. High amounts enter the European market, enforcing the need for simple techniques to help customs detect these pharmaceuticals. This study focused on physical profiling and IR spectroscopy to obtain a prime discrimination between genuine and illegal Viagra® and Cialis® medicines. Five post-tableting characteristics were explored: colour, mass, long length, short length, and thickness. Hypothesis testing showed that most illegal samples (between 60 and 100%) significantly differ from the genuine medicines, in particular for mass and long length...
March 2016: Drug Testing and Analysis
https://www.readbyqxmd.com/read/25843350/a-synthetic-cgmp-sensitive-gene-switch-providing-viagra-%C3%A2-controlled-gene-expression-in-mammalian-cells-and-mice
#19
Taeuk Kim, Marc Folcher, Ghislaine Charpin-El Hamri, Martin Fussenegger
Cyclic guanosine monophosphate (cGMP) is a universal second messenger that is synthesized from guanosine triphosphate (GTP) by guanylyl cyclases (GCs) and hydrolyzed into guanosine monophosphate (GMP) by phosphodiesterases (PDEs). Small-molecule drugs that induce high cGMP levels in specialized tissues by boosting GC activity or inhibiting PDE activity have become the predominant treatment strategy for a wide range of medical conditions, including congestive heart failure, pulmonary hypertension, atherosclerosis-based claudication and erectile dysfunction...
May 2015: Metabolic Engineering
https://www.readbyqxmd.com/read/25768099/interventions-to-treat-premature-ejaculation-a-systematic-review-short-report
#20
REVIEW
Katy Cooper, Marrissa Martyn-St James, Eva Kaltenthaler, Kath Dickinson, Anna Cantrell
BACKGROUND: Premature ejaculation (PE) is commonly defined as ejaculation with minimal sexual stimulation before, on or shortly after penetration and before the person wishes it. PE can be either lifelong and present since first sexual experiences (primary), or acquired (secondary), beginning later (Godpodinoff ML. Premature ejaculation: clinical subgroups and etiology. J Sex Marital Ther 1989;15:130-4). Treatments include behavioural and pharmacological interventions. OBJECTIVE: To systematically review evidence for clinical effectiveness of behavioural, topical and systemic treatments for PE...
March 2015: Health Technology Assessment: HTA
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