Sildenafil: two decades of benefits or risks?

Leoni, Luís Antônio Baffile; Leite, Gerson S; Wichi, Rogério Brandão; Rodrigues, Bruno

doi:10.3109/13685538.2013.801952

Cited by 21 publications

(11 citation statements)

References 69 publications

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“…Sildenafil could also be taken by men with comorbidities, such as hypertension, stable coronary artery disease, congestive heart failure, diabetes mellitus, traumatic spinal cord injury, obstructive sleep apnea, multiple sclerosis, renal dysfunction, prostate cancer, Parkinson’s disease, depression, and traumatic stress disorders 6. It is usually administered in doses of 25, 50, and 100 mg, with the recommended starting dose of 50 mg to be adapted according to response and side effects 1.…”

Section: Introductionmentioning

confidence: 99%

Bioequivalence study of a new sildenafil 100 mg orodispersible film compared to the conventional film-coated 100 mg tablet administered to healthy male volunteers

Radicioni¹,

Castiglioni²,

Giori³

et al. 2017

DDDT

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A new orodispersible film formulation of the phosphodiesterase type 5 inhibitor, sildenafil, has been developed to examine the advantages of an orally disintegrating film formulation and provide an alternative to the current marketed products for the treatment of erectile dysfunction. The pharmacokinetics of the sildenafil 100 mg orodispersible film (IBSA) was compared to that of the conventional marketed 100 mg film-coated tablet (Viagra®) after single-dose administration to 53 healthy male volunteers (aged 18–51 years) in a randomized, open, two-way crossover bioequivalence study. Each subject received a single oral dose of 100 mg of sildenafil as test or reference formulation administered under fasting conditions at each of the two study periods according to a randomized crossover design. There was a washout interval of ≥7 days between the two administrations of the investigational medicinal products. Blood samples for pharmacokinetic analysis were collected up to 24 h post-dosing. The primary objective was to compare the rate (peak plasma concentration; Cmax) and extent (area under the curve [AUC] from administration to last observed concentration time; AUC0–t) of sildenafil absorption after single-dose administration of test and reference. Secondary endpoints were observed to describe the plasma pharmacokinetic profiles of sildenafil and its metabolite N-desmethyl-sildenafil relative bioavailability and safety profile after single-dose administration. The mean sildenafil and N-desmethyl-sildenafil plasma concentration–time profiles up to 24 h after single-dose administration of sildenafil 100 mg orodispersible film and film-coated tablet were nearly superimposable. The bioequivalence test was fully satisfied for sildenafil and N-desmethyl-sildenafil in terms of rate and extent of bioavailability. Adverse events occurred at similar rates for the two formulations and were of mild-to-moderate severity. The results suggest that the new orodispersible film formulation can be used interchangeably with the conventional film-coated formulation.

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Section: Introductionmentioning

confidence: 99%

Bioequivalence study of a new sildenafil 100 mg orodispersible film compared to the conventional film-coated 100 mg tablet administered to healthy male volunteers

Radicioni¹,

Castiglioni²,

Giori³

et al. 2017

DDDT

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“…Sildenafil is a selective inhibitor of phosphodiesterase-5 (PDE-5), an enzyme, which catalyzes the breakdown of cyclic guanosine monophosphate (cGMP), an essential second messenger involved in smooth muscle relaxation. The PDE-5 inhibitors cause an accumulation of Nitric Oxide (NO) driven cGMP with subsequent vasodilatation in the corpus cavernosum and in pulmonary vasculature; therefore PDE-5 inhibitors are widely used treatment for erectile dysfunction (Leoni et al, 2013) and pulmonary hypertension. Moreover, intracellular cGMP-accumulation has been shown to reduce tissue injury in conditions associated with increased free radical release and oxidative stress (Dias-Junior et al, 2005).…”

Section: Introductionmentioning

confidence: 99%

Effect of Sildenafil on Non-Alcoholic Fatty Liver

Alashry¹,

Gaballah²,

Malek³

et al. 2015

International J. of Pharmacology

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Non Alcoholic Fatty Liver Disease (NAFLD) is now the commonest liver disease worldwide and can evolve into cirrhosis in a subgroup of patients. Sildenafil citrate is a specific phosphodiesterase-5 (PDE-5) inhibitor, which has been approved for treatment of erectile dysfunction in men. To examine the effect of sildenafil citrate on NAFLD in animal model and male patients with erectile dysfunction. Sixty male mice were divided into 4 groups: The 1-received a standard diet; 2-fed with a Highfat Diet (HFD); 3-HFD + sildenafil citrate; 4-standard diet + sildenafil citrate. The experiments were conducted for 16 weeks, after that, the mice in the treatment groups received 1.4 mg kgG 1 sildenafil citrate base dissolved in distilled water daily for 8 weeks, through orogastric feeding tube. A case-control study enrolled 60 males with erectile dysfunction, who were divided into 30 patients with NAFLD and 30 patients without NAFLD (control group). They received sildenafil citrate 50 mg daily for 8 weeks. It was found that sildenafil administration improved liver enzymes, insulin resistance and lipids level compared to control group in animal model. There were insignificant changes as regard lipid profile, fasting serum insulin and liver enzymes (alkaline phosphatase, alanine 2-oxoglutarate aminotransferase) after sildenafil treatment for 8 weeks in NAFLD group in human study. There was significant decrease in aspartate 2-oxoglutarate aminotransferase (AST) level after sildenafil treatment in NAFLD. There were significant negative correlations between International Index of Erectile Function (IIEF) score and Body Mass Index (BMI), cholesterol and triglycerides levels. Sildenafil is well-tolerated and safe in NAFLD patients. However, it is less effective in NAFLD patients than in individuals without comorbidities. Further investigation is needed to test the effect of long-term sildenafil administration on insulin resistance and lipid profile.

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“…Sildenafil citrate is a potent vasodilating agent mainly used for erectile dysfunction [1]. In the recent years, its use has also become more popular among men without erectile dysfunction to enhance sexual performance [2].…”

Section: Dear Editorsmentioning

confidence: 99%