Recreational Use of Oral PDE5 Inhibitors: The Other Side of Midnight

Mostafa, Taymour; Alghobary, Moheiddin

doi:10.1016/j.sxmr.2021.10.004

Cited by 7 publications

(3 citation statements)

References 77 publications

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“…Sildenafil is a synthetic phosphodiesterase type 5 enzyme (PDE‐5) inhibitor, and the representative drugs also include tadalafil, vardenafil and avanafil (Madeira et al, 2021; Mostafa et al, 2023; Pyrgidis et al, 2021). To pursue drug effects unilaterally and obtain huge profits, some sexual enhancement dietary supplements, mainly available in online markets, have been adulterated with these PDE‐5 inhibitors by aphrodisiac dealers (Değer & Madendere, 2021; Langarizadeh et al, 2023; Madeira et al, 2021; Mostafa & Alghobary, 2022). As reported by the US Food and Drug Administration Center for Drug Evaluation and Research, 556 of 1935 dietary supplement products were deemed to be tainted were sexual enhancement products that contained one or more PDE‐5 inhibitors from 2007 to 2023 (US Food and Drug Administration, Tainted products marketed as dietary supplements_CDER, 2023, https://www.fda.gov/consumers/health-fraud-scams/health-fraud-product-database), while furthermore, more than 50% were adulterated by sildenafil.…”

Section: Introductionmentioning

confidence: 99%

A novel standard‐free detection of adulteration method for sildenafil derivatives in dietary supplements

Lv,

Wang,

et al. 2024

Biomedical Chromatography

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The rapid and accurate detection of illegal adulteration of chemical drugs into dietary supplements is a big challenge in the food chemistry field. Detection of compounds without a standard reference is even more difficult; however, this is a common situation. Here in this study, a novel “standard‐free detection of adulteration” (SFDA) method was proposed and phosphodiesterase‐5 inhibitor derivatives were used as an example to figure out the possibility and reliability of this SFDA method. After analysis by quadrupole coupled time of flight–tandem mass spectrometry detection and multivariable statistics, six common fragment ions were chosen to indicate whether adulteration was present or not, while 20 characteristic fragment ions indicated whether adulteration was by nitrogen‐containing heterocycles or by anilines. Furthermore, the quantitative methods were conducted by high‐performance liquid chromatography–tandem mass spectrometry. In a word, this strategy allows for a quick determination of dietary supplement adulteration without any need for standard materials, improving the efficacy of food safety testing.

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Section: Introductionmentioning

confidence: 99%

A novel standard‐free detection of adulteration method for sildenafil derivatives in dietary supplements

Lv,

Wang,

et al. 2024

Biomedical Chromatography

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“…The multifaceted potential of PDE5 inhibition extends beyond erectile dysfunction to encompass a spectrum of vasodysfunctional disorders [12] . This is underscored by the clinical application of PDE5 inhibitors, such as tadalafil, vardenafil, and avanafil, in diverse contexts [13] . The concept of drug repurposing, wherein existing drugs are explored for new therapeutic indications, provides a promising avenue for expediting the development of treatments for various conditions [14] .…”

Section: Introductionmentioning

confidence: 99%

“… [12] This is underscored by the clinical application of PDE5 inhibitors, such as tadalafil, vardenafil, and avanafil, in diverse contexts. [13] The concept of drug repurposing, wherein existing drugs are explored for new therapeutic indications, provides a promising avenue for expediting the development of treatments for various conditions. [14] This approach capitalizes on existing safety and efficacy data, potentially shortening the drug development timeline and reducing costs.…”

Section: Introductionmentioning

confidence: 99%

Identifying Phosphodiesterase‐5 Inhibitors with Drug Repurposing Approach: Implications in Vasodysfunctional Disorders

Khan,

Mohammad,

Shahwan

et al. 2023

ChemistryOpen

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Phosphodiesterase type 5 (PDE5) is a multidomain protein that plays a crucial role in regulating cellular cyclic guanosine monophosphate (cGMP), a key signaling molecule involved in various physiological processes. Dysregulation of PDE5 and cGMP signaling is associated with a range of vasodysfunctional disorders, necessitating the development of effective therapeutic interventions. This study adopts comprehensive approach, combining virtual screening and molecular dynamics (MD) simulations, to repurpose FDA‐approved drugs as potential PDE5 inhibitors. The initial focus involves selecting compounds based on their binding affinity. Shortlisted compounds undergo a meticulous analysis for their drug profiling and biological significance, followed by the activity evaluation and interaction analysis. Notably, based on binding potential and drug profiling, two molecules, Dutasteride and Spironolactone, demonstrate strong potential as PDE5 inhibitors. Furthermore, all atom MD simulations were employed (500 ns) to explore dynamic behavior of Dutasteride and Spironolactone in complexes with PDE5. Principal components analysis (PCA) and free energy landscape (FEL) analyses are further leveraged to decipher that the binding of Dutasteride and Spironolactone stabilizes the structure of PDE5 with minimal conformational changes. In summary, Dutasteride and Spironolactone exhibit remarkable affinity for PDE5 and possess characteristics that suggest their potential as therapeutic agents for conditions associated with PDE5 dysfunction.

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Pelvic Floor Disorders Due to Anal Sexual Activity in Men and Women: A Narrative Review

Chen,

Kalichman

2024

Arch Sex Behav

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Recent evidence shows that consensual anal penetrative intercourse has become more prevalent, not only limited to gay, bisexual, and other men who have sex with men but also for women who are in a sexual relationship with men. The aim of this review was to study the influence of consensual anal intercourse on pelvic floor function and the role of pelvic floor physical therapy treatment in preventing or treating consensual anal intercourse-induced anodyspareunia and/or fecal incontinence. We reviewed 68 references that showed that anal penetrative intercourse is a risk factor for anodyspareunia and fecal incontinence in both men and women. This risk of anal intercourse may increase with emotional discomfort, an overactive pelvic floor, lack of lubrication, frequency of anal penetrative intercourse, and hard practice (BDSM: bondage and discipline, dominance and submission, sadism, and masochism). It seems that pelvic floor physical therapists play an essential role in preventing and treating pelvic floor dysfunctions due to anal intercourse, which can lead to anodyspareunia and fecal incontinence; the treatment includes education, pelvic floor training with and without biofeedback, electric stimulation, manual therapy, and dilatators. Further studies are warranted to enhance our understanding of the causes and treatment efficacy of pelvic floor dysfunctions due to anal penetrative intercourse.

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Recreational Use of Oral PDE5 Inhibitors: The Other Side of Midnight

Cited by 7 publications

References 77 publications

A novel standard‐free detection of adulteration method for sildenafil derivatives in dietary supplements

A novel standard‐free detection of adulteration method for sildenafil derivatives in dietary supplements

Identifying Phosphodiesterase‐5 Inhibitors with Drug Repurposing Approach: Implications in Vasodysfunctional Disorders

Pelvic Floor Disorders Due to Anal Sexual Activity in Men and Women: A Narrative Review

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