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Topic: Phosphodiesterase inhibitor


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  Phosphodiesterase type 5 inhibitor : by Ray Sahelian, M.D.
Phosphodiesterase type 5 inhibitor : by Ray Sahelian, M.D. Phosphodiesterase Inhibitors by Ray Sahelian, M.D. phosphodiesterase (PDE) is an enzyme that catalyzes the hydrolysis of phosphodiester bonds.
Phosphodiesterases are responsible for the degradation of the cyclic nucleotides cAMP and cGMP.
The early use of phosphodiesterase type 5 inhibitors in patients with hypertension, hyperlipidaemia or diabetes with concomitant ED and treating these risk factors may improve corporeal blood flow and lead to long-term preservation of cavernosal function.
www.raysahelian.com /phosphodiesterase.html   (745 words)

  
 Drugs For Mens
Brand Cialis (TADALAFIL) is a phosphodiesterase inhibitor used to treat sexual function problems such as impotence or erectile dysfunction.
Generic Cialis Soft (TADALAFIL SOFT) is a phosphodiesterase inhibitor used to treat sexual function problems such as impotence or erectile dysfunction.
Brand Levitra (VARDENAFIL) is a phosphodiesterase inhibitor used to treat sexual function problems such as impotence or erectile dysfunction.
www.drugsformens.com   (328 words)

  
 Phosphodiesterase inhibitor invention
The PDE inhibitor of the present invention is useful for treating various diseases exhibiting a relationship to PDEs, e.g., chronic obstructive pulmonary diseases, asthma, chronic artery obstruction, cardiovascular diseases, inflammatory diseases, allergic diseases, thrombosis, encephalopathy, hyperlipemia, and obesity.
This PDE inhibitor can be used as therapeutic agents for various diseases exhibiting a relationship with various PDEs, such as chronic obstructive pulmonary diseases, asthma, chronic artery obstruction, cardiovascular diseases, inflammatory diseases, allergic diseases, thrombosis, encephalopathy, hyperlipemia, and obesity.
The PDE inhibitor may be used in a desired form such as the form of solution, suspension, syrup, granule, cream, paste, or jelly, or may be shaped, if necessary.
www.freshpatents.com /Phosphodiesterase-inhibitor-dt20061221ptan20060287391.php   (1656 words)

  
 Use of inhibitors of phosphodiesterase IV - Patent 5891904   (Site not responding. Last check: )
The invention relates to the use of inhibitors of phosphodiesterase IV for the modulation of the motility and peristalsis of the hollow organs of the urogenital and gastrointestinal tract.
The invention relates to the use of inhibitors of phosphodiesterase IV (sPDE IV) for the production of pharmaceutical agents for the modulation of the motility and peristalsis of the hollow organs of the urogenital and gastrointestinal tract as well as their use as adjuvants for contrast medium studies of the urogenital and gastrointestinal tract.
Inhibitors of the PDE again reduce the degradation of cAMP and cGMP, which results in an increase of these molecules inside the cells and thus in a relaxation of the smooth muscle cells.
www.freepatentsonline.com /5891904.html   (2909 words)

  
 CIEF - Consortium for Improvement in Erectile Function
Prevalence of phosphodiesterase-5 inhibitor use in the VHA in 2004 and 2005 is twice that of a commercial health plan in 2001.
Phosphodiesterase 5 inhibitors in the treatment of premature ejaculation.
Efficacy of tadalafil in men with erectile dysfunction naive to phosphodiesterase 5 inhibitor therapy compared with prior responders to sildenafil citrate.
erectilefunction.org /Current_Literature.htm   (6975 words)

  
 International Journal of Impotence Research - Abstract of article: The role of pharmacokinetics and pharmacodynamics in ...   (Site not responding. Last check: )
The role of pharmacokinetics and pharmacodynamics in phosphodiesterase-5 inhibitor therapy
Differences in clinical pharmacology of the currently marketed phosphodiesterase (PDE)5 inhibitors sildenafil, vardenafil and tadalafil are largely determined by their pharmacokinetic (PK) properties and their PDE5 inhibitory activity profile.
It is followed by a detailed comparative discussion on the pharmacokinetics and exposure–response relationship of the currently available PDE5 inhibitors, including known drug–drug interactions and dosage adjustments in special populations.
www.nature.com /doifinder/10.1038/sj.ijir.3901522   (278 words)

  
 Phosphodiesterase inhibitor   (Site not responding. Last check: )
A phosphodiesterase inhibitor is a drug that blocks one or more of thefive subtypes of the enzyme phosphodiesterase (PDE), preventing the inactivation of the intracellular second messengers, cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP).
Sildenafil, Tadalafil and Vardenafil are selective inhibitors of type V phosphodiesterase (PDE V), whichis cGMP-specific and responsible for the degradation of cGMP in the corpus cavernosum.
These phosphodiesterase inhibitors are used as remedies for erectile dysfunction.
www.therfcc.org /phosphodiesterase-inhibitor-95853.html   (165 words)

  
 Patent 6,403,597
It is still another object of the invention to provide such a method wherein the phosphodiesterase inhibitor is a Type III inhibitor, a Type IV inhibitor, a Type V inhibitor, or a nonspecific phosphodiesterase inhibitor.
The kit includes a pharmaceutical formulation of a phosphodiesterase inhibitor, a container housing the pharmaceutical formulation during storage and prior to administration, and instructions, e.g., written instructions on a package insert or label, for carrying out drug administration in a manner effective to treat premature ejaculation.
The pharmaceutical formulation may be any formulation described herein, e.g., an oral dosage form containing a unit dosage of the phosphodiesterase inhibitor, the unit dosage being a therapeutically effective dosage for treatment of premature ejaculation.
www.pharmcast.com /Patents/Yr2002/June2002/061102/6403597_Ejaculation061102.htm   (878 words)

  
 Inhibition of phosphodiesterase in olfactory mucosa - Patent 5525329
applying a phosphodiesterase inhibitor having inhibitory activity toward phosphodiesterase present in olfactory neurons to nasal epithelium in an amount sufficient to diminish the activity of said phosphodiesterase and enhance the sense of smell.
comparing the activity of the phosphodiesterase in the presence of the test compound to activity of the phosphodiesterase in the absence of the test compound, a smell enhancer being a test compound which diminishes the activity of the phosphodiesterase.
Specificity of an inhibitor is defined as a ratio of 10-fold higher inhibitory activity of CAM-PDE (CAM-activated PDE) relative to CAM-independent PDE at a particular concentration of inhibitor.
www.freepatentsonline.com /5525329.html   (5219 words)

  
 Pharmaceutical compositions   (Site not responding. Last check: )
In the present invention where a phosphodiesterase inhibitor is used a suitable dose of active compound will in general be less than, or about, half of the dose in the absence of potentiator e.g.
In general the active compound and phosphodiesterase inhibitor are administered in a weight ratio of 1 part of active compound to from 1 to 200 parts of phosphodiesterase inhibitor.
Compressed tablets may be prepared by compressing in a suitable machine the active compound and phosphodiesterase inhibitor in a free-flowing form, such as a powder or granules, optionally mixed with a binder, lubricant, pharmaceutically inert diluent, surface active or dispersing agent.
www.sacnewsmonthly.com /invent/borate-containing_oil-in-water_microemulsion/pharmaceutical_compositions.html   (2615 words)

  
 Molecular Mechanisms and Pharmacokinetics of Phosphodiesterase-5 Antagonists   (Site not responding. Last check: )
The difference in the potencies of vardenafil and sildenafil most likely is caused by the slight differences (indicated by the arrows in Figure 1) in their molecular structures, emphasizing the potential impact of even minor changes in the molecular structure on biochemical potency.
Phosphodiesterase inhibitors are primarily degraded in the liver.
To exit the cell, the inhibitor must dissociate from PDE-5, diffuse through the cytosol to the plasma membrane without being rebound by PDE-5, traverse the plasma membrane to exit the cell, and then be transported to the liver through the bloodstream before it can be degraded.
www.current-reports.com /article.cfm?PubID=UR04-6-2-01&Type=Article&KeyWords=   (5109 words)

  
 The effect of selective phosphodiesterase inhibitors, alone and in combination, on a murine model of allergic asthma   (Site not responding. Last check: )
Sildenafil, a PDE 5 inhibitor is used for the treatment of sexual dysfunction and may potentially be used in cardiovascular disease [30], and there is the imminent release of new PDE 4 inhibitors for inflammatory lung disease [11,31].
Due to the success of these PDE inhibitors in the treatment of varied diseases, in future years there exists the potential for a patient to be taking a combination of drugs that will inhibit more than one PDE family.
Phosphodiesterase 4 (PDE4) inhibitors in asthma and chronic obstructive pulmonary disease (COPD).
www.arabmedmag.com /issue-15-03-2005/pneumology/main04.htm   (4567 words)

  
 Effects of amrinone, a phosphodiesterase inhibitor, on right ventricular/arterial coupling immediately after cardiac ...
Effects of amrinone, a phosphodiesterase inhibitor, on right ventricular/arterial coupling immediately after cardiac operations -- Ochiai et al.
Effects of amrinone, a phosphodiesterase inhibitor, on right ventricular/arterial coupling immediately after cardiac operations
Yoshie Ochiai, MD Shigeki Morita, MD Yoshihisa Tanoue, MD Yoshito Kawachi, MD Ryuji Tominaga, MD Hisataka Yasui, MD From the Department of Cardiovascular Surgery, Faculty of Medicine, Kyushu University, Fukuoka, Japan.
jtcs.ctsnetjournals.org /cgi/content/abstract/116/1/139   (312 words)

  
 [No title]
The second peak of MAP kinase activity is markedly attenuated by the protein synthesis inhibitor cycloheximide and, consequently, is paralleled by a marked de-novo synthesis of p42 and p44 MAP kinases, as measured by immunoprecipitation of [ 35S]methionine-labeled mesangial cells and by a 700% increase in total MAP kinase protein, as detected by Western-blot analysis.
A reductase inhibitor, we evaluated the effects of lovastatin on DNA replication and the proliferation of rat mesangial and aortic smooth muscle cells, both of which were mesenchymal origin cells.
Another ACE inhibitor of a different chemical class, captopril, reduced neointima formation as strongly as cilazapril (67 and 78%, respectively), but the calcium antagonist verapamil was not active as an inhibitor of neointima formation, despite similar lowering of blood pressure.
www.cs.brandeis.edu /~marc/medstract/inhibitors/inhibitor1.html   (6037 words)

  
 Patent 6,277,402
A phosphodiesterase inhibitor is administered in conjunction with the histamine H2 mimicking agent to conserve the cyclic AMP which is thus produced.
The histamine H2 mimicking agent and the phosphodiesterase inhibitor may be mixed in a gel and administered using a transdermal patch.
The composition may comprise a histamine H2 mimicking agent, a phosphodiesterase inhibitor, and a fluid medium in which the histamine H2 mimicking agent and phosphodiesterase inhibitor are mixed for simultaneous administration to a patient.
www.pharmcast.com /Patents/Yr2001/August2001/082101/6277402_MultiSclerosis082101.htm   (680 words)

  
 Gene Information
Inhibitors of phosphodiesterase 3 were used to block meiosis in ovulating oocytes in rodents (Wiersma et al., 1998).
The phosphodiesterase 3 inhibitor ORG 9935 inhibits oocyte maturation during gonadotropin-stimulated ovarian cycles in rhesus macaques Jensen JT, et al.
To determine whether phosphodiesterase (PDE) 3 inhibitors prevent the resumption of meiosis by primate oocytes in vivo, rhesus macaques were stimulated to develop multiple preovulatory follicles by administering human recombinant gonadotropins, and follicles were aspirated 34 h after an ovulatory stimulus (human chorionic gonadotropin).
ovary.stanford.edu /4_display.html?rec=29   (1491 words)

  
 Phosphodiesterase-4 Inhibitor Found Promising for COPD - CME Teaching Brief® - MedPage Today
The most common side effect that the researchers thought was likely to be related to the study drug was mild to moderate diarrhea.
Historically, phosphodiesterase-4 inhibitors have had side effects that have limited their use, including dose-limiting gastrointestinal effects and cardiac arrhythmias.
The class of phosphodiesterase-4 inhibitors "shows promise as a new therapeutic strategy," Dr. Rabe and colleagues concluded.
www.medpagetoday.com /Pulmonary/SmokingCOPD/tb/1527   (559 words)

  
 Patent 6,627,632
Inhibitors of phosphodiesterases (PDE), are agents which can block the breakdown of cAMP and cGMP in the tissue.
Phosphodiesterase inhibitors (PDE inhibitors) are agents which can block the breakdown of cAMP and cGMP in the tissue.
Preferred phosphodiesterase type IV (also referred to as PDE IV and PDE4) inhibitors are described in, for example, Bristol, et al., Annual Reports in Medicinal Chemistry, Vol.
www.pharmcast.com /Patents/Yr2003/Sept2003/093003/6627632_Anorectal093003.htm   (8484 words)

  
 Cough | Full text | Phosphodiesterase 3 inhibition and cough in elderly asthmatics
Effects of cilostazol, a PDE 3 inhibitor, on cough response to inhaled capsaicin were examined in 11 patients over 70 years with stable asthma in a randomized, placebo-controlled cross over study.
Recently, considerable attention has been focused on the potential use of selective inhibitors of cyclic nucleotide phosphodiesterases (PDEs) in the treatment of respiratory diseases as PDE isoenzymes may play an important role in the regulation of airway caliber and bronchial smooth muscle function [3].
We have demonstrated that a phosphodiesterase 3 inhibitor, cilostazol, reduces bronchial hyperresponsiveness to inhaled methacholine in elderly patients with stable asthma [10].
www.coughjournal.com /content/1/1/11   (2704 words)

  
 Cialis - Getpharma - From The Real Pharmacy!
Tadalafil is called a phosphodiesterase type 5 inhibitor, and works by preventing the action of a chemical in the body called phosphodiesterase type 5.
An erection is produced via a complex chain of events, involving signals from the nervous system and the release of chemical messengers within the tissues of the penis.
This means that the blood vessels are kept dilated for longer, improving blood flow to the penis and maintaining an erection.
www.getpharma.com /productdetail.asp?productid=100   (1406 words)

  
 Erectile dysfunction, impotence and male sexual dysfunction resourceson diagnosis and treatment options for ...
The purpose of this study will be to evaluate the clinical efficacy and safety of DA-8159, an orally administered, potent and selective inhibitor of PDE5, versus placebo for the treatment of subjects with erectile dysfunction (ED).
Chronic administration of phosphodiesterase 5 inhibitor improves erectile and endothelial function in a rat model of diabetes
Phosphodiesterase type 5 inhibitors' extended duration of response as a variable in the treatment of erectile dysfunction
www.touchendocrinedisease.com /erectile-dysfunction-c707.html   (878 words)

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