Aildenafil citrate: a new potent and highly selective phosphodiesterase type 5 inhibitor for the treatment of erectile dysfunction

ArticleinZhonghua nan ke xue = National journal of andrology 12(12):1080-3 · January 2007with41 Reads
Source: PubMed
To evaluate the efficacy and safety of aildenafil citrate, an oral phosphodiesterase type 5 inhibitor, in the treatment of erectile dysfunction. Integrated analyses were made of 8-week, randomized, double-blind, placebo-controlled phase 2 clinical trials involving 250 men with mild-to-severe erectile dysfunction of various etiologies who received aildenafil citrate 30 or 60 mg (n = 167) or placebo (n = 83). The statistic results of International Index of Erectile Function, Patient Sexual Encounter Profile (SEP) diaries and Global Assessment Question (GAQ) were significantly higher in the aildenafil citrate patients than in the placebo controls. The main drug-related adverse events were flushing, headache, dizziness and naupathia, which were mild and could be self-relieved. Conclusion: The aildenafil citrate therapy significantly ameliorated erectile function and was well tolerated by a wide range of patients with erectile dysfunction.
    • "Aildenafil was found to be present in two herbal supplements (VII and VIII) at levels of 49 and 46 mg per dose unit, respectively. Patent and scientific literature showed that the pharmacological effects and potency of aildenafil were similar to those of sildenafil (Liu 2005; He et al. 2006; Guo et al. 2007; Wang et al. 2007). Because the dose levels found for aildenafil with these herbal supplements exceeded the lowest commercially available sildenafil dose of a registered drug (Table 3), these supplements were considered to produce significant pharmacological effects. "
    [Show abstract] [Hide abstract] ABSTRACT: Herbal food supplements, claiming to enhance sexual potency, may contain deliberately added active pharmacological ingredients (APIs) that can be used for the treatment of erectile dysfunction (ED). The aim of this study was to determine whether herbal food supplements on the Dutch market indeed contain APIs that inhibit phosphodiesterase type 5 (PDE-5) inhibitors, such as sildenafil and analogous PDE-5 inhibitors. Herbal food supplements intended to enhance sexual potency (n = 71), and two soft drinks, were sampled from 2003 up to and including 2012. In 23 herbal supplements, nine different PDE-5 inhibitors were identified; in a few cases (n = 3), more than one inhibitor was indentified. The presence of these APIs was however not stated on the label. The concentrations of PDE-5 inhibitors per dose unit were analysed. Furthermore, the potential pharmacologically active properties of the detected PDE-5 inhibitors were estimated by using data from the scientific and patent literature regarding (1) in vitro PDE-5 activity, (2) reported effective doses of registered drugs with PDE-5 inhibitor activity and (3) similarity to other structural analogues. It was concluded that 18 of the 23 herbal food supplements, when used as recommended, would have significant pharmacological effects due to added APIs. Adequate use of existing regulation and control measures seems necessary to protect consumers against the adverse effects of these products.
    Full-text · Article · Nov 2013
  • [Show abstract] [Hide abstract] ABSTRACT: A new analogue of sildenafil was detected in a herbal aphrodisiac. The structure of the compound was established using LC-MS, UV and IR spectroscopy, MS-MS, and NMR. The compound, named thio-homosildenafil is a synthetic N-ethylpiperazine analogue of sildenafil in which also the CO moiety has been converted into a CS group. This is the first time a sildenafil analogue modified at the chromophore was identified as an adulterant of a herbal aphrodisiac. Preliminary pharmacological analysis confirmed the erectogenic potency of thio-homosildenafil.
    Article · Apr 2008
  • [Show abstract] [Hide abstract] ABSTRACT: Illicit erectile dysfunction (ED) products often contain experimental medicines. The acute health risks of using such illicit ED products, however, appear to be relatively low – at least to date. Less health damage has been reported than expected based on the presumed use of these products, although their long-term effects on human health are unknown. This report was compiled from the records of five national institutes in the Netherlands and is the third RIVM report to be published on illicit ED products. The investigated products were all confiscated outside the official distribution system. Illicit Illicit ED products are illegally produced or distributed without the necessary licences. There are three licensed ED products available on the Dutch market (Viagra®, Cialis® and Levitra®). All need to be prescribed by a physician. The use of illicit ED products has increased dramatically during the last decade, most likely due to the ease of purchasing via the Internet. Risks Risks that have been identified are overdosing, adverse combination(s) with alcohol or drugs and long-term use. Adulterated food supplements containing experimental medicines (analogues), counterfeit generics and ED products mixed with antidepressants are considered to represent the greatest health risks. Research This report describes the product characteristics and presents the chemical analysis data of 538 illicit ED products (containing PDE5 inhibitors) confiscated in the period 2007–2010. These products can be classified as counterfeit medicines (17%), illicit generics (unapproved medicines) (69%) and adulterated food supplements (13%). Most ED products contain an effective amount of the active substance, although many are fraudulently mislabelled in terms of the active drug substance and dose. The results of this study show that the composition of illicit ED products is usually unreliable. Surveillance Marketing surveillance of medicines is well organised in The Netherlands, but it does need to be improved for food supplements as current regulations and laws governing the composition of such products are too limited. According to the RIVM, improved measures aimed at safeguarding the veracity of food supplements are desirable. Although there appears to be a low incidence of health damage attributable to the use of ED products, it remains necessary to monitor these products for trends in new active drug substances and long-term health risks. It is also important to investigate user behaviour.
    Full-text · Article · Jan 2011 · Journal of Pharmaceutical and Biomedical Analysis
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