Our library of drug research abstracts drawn from the medical literature is updated on a regular schedule, and you can be assured that new cialis research articles will be listed here shortly after becoming available to us.
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Medical research on cialis
Transdermal Delivery of Tadalafil. I. Effect of Vehicles on Skin Permeation.
Drug Dev Ind Pharm. 2008 Sep 27; 1-8
El Maghraby GM, Alanazi FK, Alsarra IA
Transdermal delivery that avoids the presystemic disposition can provide an alternative to oral administration of tadalafil. Accordingly, the aim of this study was to select the best vehicle as the first step in optimization of tadalafil transdermal delivery. The vehicles were used neat or in selected binary combinations and were evaluated for drug solubilization and transdermal delivery. The drug solubility in pure vehicles were ranked as polyethylene glycol (PEG) 400 > propylene glycol (PG) > ethanol > ethyl oleate (EO) > isopropyl myristate (IPM) > water. The solubility in binary systems containing ethanol at 2:1 ratios with EO or IPM was greater than that obtained with pure ethanol, EO, or IPM. This effect could be due to the cosolvency effect. The transdermal drug delivery from pure vehicles was ranked as IPM > EO > ethanol > PG > PEG > water. The delivery from binary mixtures of ethanol with either IPM or EO was higher than that obtained from pure solvents with the delivery increasing with increasing ethanol concentration in the mixtures. The delivery from binary mixtures was synergistic rather than additive. The study thus demonstrated a potential of tadalafil transdermal delivery. Binary combinations of ethanol with either IPM or EO provided the first step forward toward the development of transdermal delivery system for tadalafil.
Respirology. 2008 Nov; 13(6): 916-8
Bendayan D, Shitrit D, Kramer MR
Despite the introduction of new drugs that have changed the course of pulmonary arterial hypertension (PAH), some patients are still refractory to treatment and deteriorate rapidly. Long-acting phosphodiesterase-5 inhibitors are a new class of drugs that are effective in PAH. This prospective study assessed the potential of combination therapy with prostacyclin and tadalafil for treatment of severe PAH. We report four cases of severe PAH that deteriorated despite prostacyclin therapy. Two patients had Eisenmenger syndrome, one had pulmonary hypertension associated with scleroderma and one had histiocytosis X. All were treated with tadalafil, 10-20 mg once daily, in addition to prostacyclin. After 3 months of treatment, all patients improved clinically, with an increase in mean 6MWD from 214 to 272 m. In three patients, the New York Heart Association functional class decreased from IV to III. Echocardiograms showed no significant changes in pulmonary arterial pressure. Although this study was limited by the small sample size, it suggests that tadalafil in combination with prostacyclin is an effective treatment for severe PAH. Tadalafil may be beneficial for the treatment of patients with advanced disease.
[Use of phosphodiesterase-5 inhibitors by college students.]
Rev Saude Publica. 2008 Aug 21;
Freitas VM, Menezes FG, Antonialli MM, Nascimento JW
The objective of this study was to identify the use of phosphodiesterase type 5 inhibitors among university students from the city of Sao Paulo (SP) in Brazil. Male students (n=350) replied to a questionnaire about diagnosis of erectile dysfunction, the frequency and reason for the use of phosphodiesterase type 5 inhibitors, the specific medication used, whether their use was accompanied by a medical prescription and any reported side-effects. The results shows that a total of 53 (14.7%) students had already used this kind of medication without a prescription or medical diagnosis for erectile dysfunction, of which 53% reported using sildenafil, 37% tadalafil and 10% vardenafil. The main adverse side-effects reported were headache (23%) and flushing (10%) and the main reasons for using the inhibitor were curiosity (70%) and erectile improvement (12%).
Structural elucidation of a tadalafil analogue found in a dietary supplement.
Shokuhin Eiseigaku Zasshi. 2008 Aug; 49(4): 311-5
Hasegawa T, Saijo M, Ishii T, Nagata T, Haishima Y, Kawahara N, Goda Y
A tadalafil analogue was detected in a dietary supplement marketed for tonic effect, along with hydroxyhomosildenafil and aminotadalafil. The tadalafil analogue was isolated by preparative thin layer chromatography (TLC) and its structure was elucidated using high-performance liquid chromatography (HPLC), liquid chromatography electrospray ionization-mass spectrometry (LC-ESI-MS), Fourier transform-ion cyclotron resonance-mass spectrometry (FT-ICR-MS) and nuclear magnetic resonance (NMR) spectroscopy. The compound was determined to be methyl-1-(1,3-benzodioxol-5-yl)-2-(chloroacetyl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole-3-carboxylate.
Oral Phosphodiesterase Type 5 Inhibitors: Nonerectogenic Beneficial Uses.
J Sex Med. 2008 Aug 26;
Mostafa T
Introduction. Phosphodiesterase type 5 (PDE5) hydrolyses cyclic guanylate monophosphate (cGMP) specifically to 5' GMP. PDE5 inhibitors were a breakthrough medication that addressed a previously unfulfilled medical need. They promoted vascular relaxation in the corpora cavernosa and penile erection during sexual stimulation. Sildenafil, vardenafil, and tadalafil were approved then introduced as effective treatments for male erectile dysfunction. This impact has stimulated academic, clinical, and industrial research. Aim. To highlight the nonerectogenic beneficial uses of oral PDE5 inhibitors. Method. A systematic review of published studies in this affair based on a Pubmed and medical subject heading databases search of all concerned articles. Main Outcome Measures. Demonstrated beneficial as well as applicable uses of oral PDE5 inhibitors. Results. As chemical molecules, these drugs were shown to exert potential nonerectogenic beneficial effects. They showed efficacy as a useful adjunct in the management of pulmonary hypertension. Additional uses were extended to different utilities: essential hypertension, benign prostatic hyperplasia, gastrointestinal disorders, endothelial dysfunction, female sexual dysfunction, genital blood flow, exercise capacity, Raynaud's phenomenon, sperm motility, etc. Conclusion. Exploring PDE5 inhibitors for their possible medical applications in diverse specialties seems to be beneficial in making use of these molecules for the welfare of humanity.
Prog Urol. 2008 Sep; 18(8): 536-42
Giuliano F, Vicaut E, Jeanpetit Y
INTRODUCTION: Phosphodiesterase type 5 inhibitors (PDE5I) for the treatment of erectile dysfunction (ED) have the same pharmacological target but their dissimilar chemical structures lead to different pharmacokinetic profiles and consequently possible different uses. OBJECTIVES: To study the impact of the pharmacokinetic differences of PDE5I on the time interval between drug intake and subsequent sexual intercourse. METHOD: Observational study, prospective conducted with a sample of 462 French general practitioners over one year. The physicians included patients with ED treated since at least three months by PDE5I. The patients were followed for two months. RESULTS: One thousand four hundred and two patients (mean age 57.9 years) with ED (mean duration 1.8 years) were analyzed; they were treated since 11.1 months: 939 (67%) by sildenafil, 116 (8.3%) by vardenafil and 347 (24.8%) by tadalafil. Sildenafil was taken at the recommended starting dose in 77% of cases versus 55% and 23% for vardenafil and tadalafil, respectively, that required more frequently higher doses than the recommended starting dose to be efficient. During the observational period, data from 5842 sexual intercourses (from 780 patients) were available. The median [CI: 95%] of the time interval between drug intake and sexual intercourses was 1.0h [1.0-1.0] for sildenafil, 1.0h [1.0-1.0] for vardenafil and 1.5h [1.3-1.5] for tadalafil. Questionnaires for sexual life quality and treatment satisfaction did not evidence differences between the treatments. CONCLUSION: This observational study performed in a nonspecialized medical practice indicates that despite their different pharmacokinetic profiles, the different uses of PDE5I remain fairly similar.
Pulmonary arterial hypertension: on the way to a manageable disease.
Curr Opin Investig Drugs. 2008 Sep; 9(9): 957-62
Mucke HA
Pulmonary arterial hypertension (PAH) is an orphan disease for which no specific pharmacological therapy was available until 1996. Pharmacotherapy for PAH is currently dominated by three endothelin receptor antagonists, bosentan, ambrisentan and sitaxentan (which is not yet approved in the US), and the PDE5 inhibitor sildenafil. Drug candidates undergoing phase III clinical trials for PAH include inhalable and oral treprostinil, aviptadil (an inhalable vasoactive intestinal peptide), and the PDE5 inhibitor tadalafil. Riociguat, a soluble guanylate cyclase stimulator, is scheduled to enter phase III clinical trials in 2008. By approximately 2010, the role of infusable or injectable PGs as treatment for PAH will likely diminish significantly, while inhalable nitric oxide will remain as mainstay therapy in neonatal PAH. Benefits in survival and quality-of-life will decide if any of the more experimental approaches that utilize newly discovered molecular pathways in PAH will ultimately result in marketed drugs.
J Urol. 2008 Oct; 180(4): 1228-34
Roehrborn CG, McVary KT, Elion-Mboussa A, Viktrup L
PURPOSE: Phosphodiesterase type 5 inhibitors are widely used to treat erectile dysfunction. Preliminary data have suggested phosphodiesterase type 5 inhibitor efficacy in men with lower urinary tract symptoms associated with clinical benign prostatic hyperplasia. MATERIALS AND METHODS: After a 4-week placebo run-in period 1,058 men with benign prostatic hyperplasia lower urinary tract symptoms were randomly allocated to receive 12-week, once daily treatment with placebo or tadalafil (2.5, 5, 10 or 20 mg). RESULTS: The International Prostate Symptom Score least squares mean change from baseline to end point was significantly improved for 2.5 (-3.9, p = 0.015), 5 (-4.9, p
Can Viagra really cause hearing and vision loss? If so, is this a reason to avoid using it?
Mayo Clin Health Lett. 2008 Jul; 26(7): 8
Structure -activity relationships of PDE5 inhibitors.
Curr Med Chem. 2008; 15(16): 1570-85
Eros D, Szántai-Kis C, Kiss R, Kéri G, Hegymegi-Barakonyi B, Kövesdi I, Orfi L
cGMP has a short-term effect on smooth muscle tone and a longer-term effect on responses to chronic drug treatment or proliferative signals. cGMP-Phosphodiesterase type 5 (PDE5) hydrolizes cGMP, and the result is smooth muscle contraction. PDE5 is a relatively novel therapeutic target of various diseases, such as erectile dysfunction and pulmonary hypertension. The most intensively examined and marketed PDE5 inhibitor was sildenafil (Viagra) but recently vardenafil (Levitra) and tadalafil (Cialis) were launched with beneficial ADME parameters and PDE5 selectivity. The increasing interest in PDE5 inhibition made it reasonable to collect the available inhibitory data from the scientific literature and set up a structure-activity relationship study. Chemical structures of 438 compounds and their cGMP-PDE5 inhibitory data (IC50) were collected from recently published articles. In this paper physiology, regulation and inhibition of PDE5 (and briefly other PDE-s) are discussed and inhibitors are tabulated by the core structures. Finally, a general QSAR model built from these data is presented. All data used in the QSAR study were summarized in a Supplement (for description please see the online version of the article).