Acetildenafil Explained

Acetildenafil (hongdenafil) is a synthetic drug which acts as a phosphodiesterase inhibitor.^[1] It is an analog of sildenafil (Viagra)^[2] which has been detected in numerous different brands of "herbal aphrodisiac" products sold in convenience stores that claim to boost libido and alleviate erectile dysfunction.^[3]

A range of designer analogs of licensed PDE₅ inhibitors such as sildenafil and vardenafil have been detected in recent years in over-the-counter herbal aphrodisiac products,^{[4] [5] [6] [7]} in an apparent attempt to circumvent both the legal restrictions on sale of erectile dysfunction drugs, which are prescription-only medicines in most Western countries, and the patent protection which allows sale of these drugs by competitors only with permission from the patent holders (typically, under a license from the inventors) and to introduce efficacy into otherwise ineffective herbal products. These compounds have been demonstrated to display PDE₅ inhibitory activity in vitro and presumably have similar effects when consumed, but have undergone no formal testing in either humans or animals, and as such may represent significant health risks to consumers of these products due to their unknown safety profile.^[8] Attempts to ban such ingredients have not been successful for the most part, many jurisdictions having laws restricting chemical analogs but only those of narcotics and doping agents. However, at least one court case has resulted in a product being taken off the market.^[9]

See also

• Aildenafil
• Nitrosoprodenafil
• Sulfoaildenafil

Notes and References

1. Web site: Acetildenafil . Cayman Chemical . 26 Mar 2017.
2. Blok-Tip L, Zomer B, Bakker F, Hartog KD, Hamzink M, Ten Hove J, Vredenbregt M, De Kaste D . 6 . Structure elucidation of sildenafil analogues in herbal products . Food Additives and Contaminants . 21 . 8 . 737–48 . August 2004 . 15370823 . 10.1080/02652030412331272467 . 10029/11381 . 45568769 . free .
3. Poon WT, Lam YH, Lai CK, Chan AY, Mak TW . Analogues of erectile dysfunction drugs: an under-recognised threat . Hong Kong Medical Journal = Xianggang Yi Xue Za Zhi . 13 . 5 . 359–63 . October 2007 . 17914141 .
4. Venhuis BJ, de Kaste D . Towards a decade of detecting new analogues of sildenafil, tadalafil and vardenafil in food supplements: a history, analytical aspects and health risks . Journal of Pharmaceutical and Biomedical Analysis . 69 . 196–208 . October 2012 . 22464558 . 10.1016/j.jpba.2012.02.014 .
5. Zou P, Oh SS, Hou P, Low MY, Koh HL . Simultaneous determination of synthetic phosphodiesterase-5 inhibitors found in a dietary supplement and pre-mixed bulk powders for dietary supplements using high-performance liquid chromatography with diode array detection and liquid chromatography-electrospray ionization tandem mass spectrometry . Journal of Chromatography A . 1104 . 1–2 . 113–22 . February 2006 . 16364350 . 10.1016/j.chroma.2005.11.103 .
6. Gratz SR, Gamble BM, Flurer RA . Accurate mass measurement using Fourier transform ion cyclotron resonance mass spectrometry for structure elucidation of designer drug analogs of tadalafil, vardenafil and sildenafil in herbal and pharmaceutical matrices . Rapid Communications in Mass Spectrometry . 20 . 15 . 2317–27 . 2006 . 16817245 . 10.1002/rcm.2594 . 2006RCMS...20.2317G . free .
7. Hou P, Zou P, Low MY, Chan E, Koh HL . Structural identification of a new acetildenafil analogue from pre-mixed bulk powder intended as a dietary supplement . Food Additives and Contaminants . 23 . 9 . 870–5 . September 2006 . 16901855 . 10.1080/02652030600803856 . 35240702 .
8. Oh SS, Zou P, Low MY, Koh HL . Detection of sildenafil analogues in herbal products for erectile dysfunction . Journal of Toxicology and Environmental Health. Part A . 69 . 21 . 1951–8 . November 2006 . 16982533 . 10.1080/15287390600751355 . 40831895 .
9. Venhuis BJ, Blok-Tip L, de Kaste D . Designer drugs in herbal aphrodisiacs . Forensic Science International . 177 . 2–3 . e25-7 . May 2008 . 18178354 . 10.1016/j.forsciint.2007.11.007 .