Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0016382 (flushing)
 6,387 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The treatment of erectile dysfunction (ED) has been revolutionised by new agents to inhibit the enzyme PDE5. The scientific basis of this treatment of ED includes relaxation of the corpus cavernosum smooth muscle tissue by inhibition of PDE5 that breaks down cGMP, the key pathway for the production of erectile function in humans. Many clinical studies, both pre- and post-marketing, have demonstrated the clinical efficacy and safety of sildenafil (Viagra, Pfizer) - the first approved selective PDE inhibitor for the treatment of ED. Sildenafil is inhibitory of PDE5 at a rate tenfold higher than for the next PDE (PDE6), which produces visual changes through the retinal rods. Its clinical effectiveness has been well documented in the majority of men with ED irrespective of aetiology. The aetiology of ED, also, does not appear to effect the function of sildenafil in relaxing corpus cavernosum smooth muscle tissue. Adverse events are usually associated with the vascular changes from PDE5 inhibition. These include headache and flushing. Each of these adverse events, however, declines with medication use. With the use of sildenafil, it has been clearly, clinically demonstrated that the selective inhibition of PDE5 is an appropriate, effective, safe method for the treatment of ED of all aetiologies and severities.
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PMID:Long-term use of sildenafil. 1261 92

The efficacy of sildenafil citrate (Viagra), an oral agent for the treatment of erectile dysfunction (ED), has been demonstrated in global studies. This 12-week randomized, double-blind, placebo-controlled, parallel-group, flexible-dose study assessed the efficacy and safety of sildenafil to treat ED in men in Egypt and South Africa. Men with ED of varied etiology were randomized to receive sildenafil 50 mg (n=128) or placebo (n=126); doses could be adjusted to 100 or 25 mg. Questions from the International Index of Erectile Function (IIEF) assessing the ability to achieve (Q3) and maintain (Q4) erections demonstrated a significant improvement with sildenafil compared with placebo (P<0.0001). Improved erections were reported by 74% of patients receiving sildenafil and 27% of those receiving placebo (P<0.0001). Headache, dyspepsia, and flushing were the most common adverse events in sildenafil-treated patients. These results are consistent with clinical trials in other countries. We conclude that sildenafil is an efficacious and well-tolerated treatment for men with ED in Egypt and South Africa.
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PMID:Efficacy and safety of sildenafil citrate (Viagra) for the treatment of erectile dysfunction in men in Egypt and South Africa. 1282 6

PT-141, a cyclic heptapeptide melanocortin analog, was evaluated following intranasal administration in healthy male subjects and in Viagra-responsive erectile dysfunction (ED) patients. Erectile response was assessed by RigiScan trade mark in healthy subjects without visual sexual stimulation (VSS) and in Viagra-responsive ED patients with VSS. In healthy subjects, mean C(max) and AUC((0-t)) increased in a dose-dependent manner. Median T(max) was 0.50 h and mean t(1/2) ranged from 1.85 to 2.09 h. In both studies, an erectile response induced by PT-141 administration was statistically significant, compared to placebo, at doses greater than 7 mg, with the onset of the first erection occurring in approximately 30 min. PT-141 was safely administered and well tolerated in both studies. A maximum-tolerated dose was not identified. Flushing and nausea were the most common adverse events reported in both studies and no clinically significant changes in vital signs, laboratory tests, ECGs, or physical exams were observed. Based upon its erectogenic potential and tolerability profile, PT-141 is a promising candidate for further evaluation as a treatment for male ED.
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PMID:Double-blind, placebo-controlled evaluation of the safety, pharmacokinetic properties and pharmacodynamic effects of intranasal PT-141, a melanocortin receptor agonist, in healthy males and patients with mild-to-moderate erectile dysfunction. 1496 71

Sildenafil (Viagra) is a selective phosphodiesterase type 5 inhibitor (PDE5-I) approved for treatment of erectile dysfunction. Although relatively well-tolerated, sildenafil is associated with undesired effects including headache, flushing, dyspepsia, nasal congestion, and visual disturbances. In the present study we explored the impact of sildenafil on nasal airway parameters in young potent men. Eleven men (age 26.0 +/- 1.8 years) with normal BMI (25.7 +/- 0.5) and without nasal respiratory disorders were enrolled in a double-blind, crossover study. All men underwent evaluation of systolic (SBP) and diastolic blood pressure (DBP), heart rate (HR), SpO2%, acoustic rhinometry, and nasal endoscopy before and after placebo or sildenafil (50 mg) plus visual sexual stimulation (VSS). Nasal examination was performed using 0 degrees rigid telescopes, 4 mm in diameter. A Student's t test was used for direct comparisons, while the Kruskal-Wallis test (K-W) was utilized for multiple comparisons. After administration of sildenafil plus VSS, the minimum cross sectional area (MCA) was significantly lower that observed with either placebo (P = 0.03) or sildenafil alone (P = 0.003). However, the post-stimulation values did not demonstrate any significant differences among the different treatment arms (P = 0.48; DF = 2; K-W test). In contrast, endonasal volume (VOL) was significantly lower after sildenafil + VSS (P = 0.01), but not after placebo + VSS (P = 0.18). None of the other parameters monitored showed any significant variations. Rhinoscopy showed a characteristic increase of the volume of the inferior turbinates, with subjective differences between placebo and sildenafil. These preliminary results suggest that sildenafil reduces nasal volume, and that sexual stimulation may decrease nasal airflow by itself.
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PMID:Nasal congestion after visual sexual stimulation with and without sildenafil (Viagra): a randomized placebo-controlled study. 1790 71

The drug sildenafil (Viagra, Pfizer) and, more recently, tadalafil (Cialis, Lilly-Icos) and vardenafil (Levitra, Bayer), has drawn public attention to aphrodisiacs. The search for such substances dates back millennia. Adverse effects associated with these drugs include hypotension, tachycardia, headache, flushing, blurred vision, dyspepsia, and musculoskeletal pain. Although sildenafil has been marketed for erection of the penis, recent attention has been paid to its application for women, including enhancement of success of in vitro fertilization but also better sexual responses (increased desire, satisfaction, and orgasm) in cases of sexual disorders. Today, there is a debate on internet forums about the potential properties of sildenafil to enhance women's sexual pleasure. This laboratory was asked to analyze a 12-cm length of light brown hair submitted by a British police force following an allegation that a young female had been subjected to sexual assaults over a two-year period. The female was 15-17 years of age at the time. The alleged perpetrator was her stepfather, and there was some suspicion that drugs may have been administered to facilitate the attacks. After decontamination and segmentation (6 x 2-cm section), the specimen was analyzed by liquid chromatography coupled with tandem mass spectrometry after alkaline (pH 9.5) extraction using dichloromethane/ isopropanol/n-heptane (25:10:65, v/v/v). The limit of quantitation was 5 pg/mg. The proximal segment tested positive for sildenafil at 38 pg/mg, and all others proved negative. This was in accord with the victim's claim. In the absence of any controlled studies, it was impossible to put any quantitative interpretation on the measured concentration.
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PMID:Hair analysis to demonstrate administration of sildenafil to a woman in a case of drug-facilitated sexual assault. 1987 68

Sildenafil (Viagra) is the most effective oral therapy currently available for erectile dysfunction. Patients should be given clear instructions regarding the use of sildenafil. The most common side effects include flushing, headaches, dyspepsia, and transient visual changes. In combination with nitrates, it can and has caused fatal hypotension. It should not be prescribed to patients on nitrates. Additionally, nitrates should not be administered to anyone who has recently ingested sildenafil. Synergetic blood pressure lowering has not been observed when sildenafil was used with other classes of antihypertensives. Sildenafil is not offered to patients with low cardiac output states, those on intensive regimens to prevent heart failure or those with acute coronary ischemia.
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PMID:Sildenafil (viagra) and the heart. 2300 45

Male erectile dysfunction is common and frustrating after the age of forty years. Erectile dysfunction is a cause of misery, relationship difficulties, and significantly reduced quality of life. Sildenafil citrate (Viagra) has shown promising results in recently published clinical trials. Sildenafil is a potent and competitive inhibitor of cGMp specific phosphodiesterase-5, predominant isoenzyme in the human corpus cavernosum. It is effective in erectile dysfunction of diverse origin, however it requires a patent vascular system to be effective. It is not effective in patients with endocrinal impotence, loss of libido, premature ejaculation or infertility. Its main adverse effects are headache, flushing, dyspepsia, diarrhoea, nasal congestion, indigestion, visual disturbances, dizziness and rash. Ventricular tachycardia and acute myocardial infraction have been reported in patients of ischaemic heart disease after consumption of sildenafil. Six deaths have been reported in patients taking nitrates. In India it is likely to be prescribed by a primary care physician without complete evaluation of patient on complaint of impotence. Hence the ethical question of who should prescribe this drug should be addressed by medical fraternity and proper guidelines formulated to avoid misuse of sildenafil. Phosphodiesterase is distributed in nerve, central nervous system, and systemic vasculature, hence long-term effects of drug on these tissues has to be ascertained. It should be made mandatory to report all adverse drug reactions to ADR monitoring centres. It is a wonder for those who require it, but has potentially dangerous adverse effects and drug interactions and hence is and not a wonder pill for all kinds of impotence.
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PMID:VIAGRA : IS IT A WONDER DRUG ? 2736 78


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