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)

Vardenafil (Levitra), recently launched in Belgium by Bayer and Glaxo-SmithKline, is a new drug that potently and selectively inhibits phosphodiesterase type 5 (PDE5) in the cavernosum tissue of the penis. Inhibition of PDE5 blocks the hydrolysis of cyclic guanosine monophosphate (GMPc) and results in increased arterial blood flow leading to enlargement of the corpus cavernosum and resulting in erection. In controlled clinical trials, vardenafil at least doubled the rate of successful erections as compared to placebo, whatever the evaluation parameter considered and the subgroup of patients studied. Vardenafil is thus indicated in the treatment of patients with erectile dysfunction. It is presented as 5, 10 and 20 mg tablets and the usual dose is 10 mg to be ingested 25 to 60 minutes before sexual activity. Vardenafil has a more potent inhibitory activity of PDE5 in vitro than sildenafil or tadalafil while its pharmacokinetics in vivo is somewhat more rapid than that of the two other compounds. The dosage of vardenafil may be reduced to 5 mg (especially in older individuals) to improve tolerance or be increased up to 20 mg (especially in the presence of organic diseases aggravating erectile dysfunction) to improve efficacy. Contra-indications (co-administration with drugs increasing nitric oxide) and side-effects (headache and flushing due to vasodilatation) of vardenafil are similar to those of other PDE5 inhibitors.
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PMID:[Medication of the month. Vardenafil (Levitra)]. 1462 53

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