Daily Administration of Phosphodiesterase Type 5 Inhibitors for Urological and Nonurological Indications

Bella, Anthony J; DeYoung, Ling; Al-Numi, Mussa; Brock, Gerald

doi:10.1016/j.eururo.2007.06.048

Cited by 54 publications

(38 citation statements)

References 143 publications

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“…Also, both treatments were well tolerated. The authors concluded that treatment with daily Tadalafil was associated with a significantly higher IIEF erectile function domain score and completion of successful intercourse compared with on-demand Tadalafil (28).…”

Section: Discussionmentioning

confidence: 99%

Evaluation of Tadalafil effect on lower urinary tract symptoms of benign prostatic hyperplasia in patients treated with standard medication

et al. 2012

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Benign Prostatic Hyperplasia (BPH) is a pathological process responsible for the majority of lower urinary tract symptoms (LUTS) in elderly men (1). In addition, erectile dysfunction (ED), which has negative effect on quality of life (QoL), is another major problem of this age group (2).The incidence of BPH increases with age. It is observed in about 50% of men over 50 year with prevalence increasing up to 90% in those older than 80 year. Moreover, 25% to 50% of men with histological confirmed BPH have LUTS (3).The α-blockers and/or 5-α reductase inhibitors are used for the treatment of BPH frequently. The phosphodiesterase inhibitors are Objectives: To evaluate safety and efficacy of tadalafil on lower urinary tract symptoms (LUTS) suggestive of benign prostatic hyperplasia (BPH) in patients treated with standard medication. Materials and Methods:In this case-controlled randomized clinical trial, from november 2008 to August 2009, 132 patients with obstructive and irritative urinary tract symptoms due to BPH, IPSS ≥ 8, no indication for surgical intervention and that reached plateau levels of response to treatment were selected. These patients were randomly allocated in two groups (each containing 66 patients). The treatment group received standard treatment of BPH and tadalafil (10 mg nightly); the placebo group received only standard treatment of BPH. IPSS, maximum urinary flow rate (Q max ) and quality of life were assessed before and after a 3-month period of study. Results: Before treatment, mean IPSS, Q max and quality of life values in the treatment and placebo groups were 13.06 ± 4.37 and 13.66 ± 4.25, 8.92 ± 2.96 mL/s and 9.09 ± 2.91 mL/s, 2.93 ± 0.86 and 2.66 ± 0.78, respectively. After treatment, mean IPSS, Q max , and quality of life values in treatment group were 7.66 ± 3.99, 9.99 ± 4.76 mL/s and 1.80 ± 0.98, respectively. These findings were compared to corresponding values of the placebo group (11.37 ± 3.64, 8.73 ± 2.22 mL/s and 2.19 ± 0.53, respectively): IPSS and quality of life were significantly different but Q max didn't show a significant change. Conclusions: Tadalafil improves quality of life and urinary symptoms in patients with LUTS suggestive of BPH, but doesn't have any significant effect on Qmax. Therefore, this drug may be effectively used in combination with standard medical therapies for BPH. Evaluation of

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Section: Discussionmentioning

confidence: 99%

Evaluation of Tadalafil effect on lower urinary tract symptoms of benign prostatic hyperplasia in patients treated with standard medication

et al. 2012

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“…Yield 50%; m.p. 129-131 C. 1 Synthesis of 1-methyl-5-methylsulfanyl-3-propyl-1H-pyrazolo [4,3-e] [1,2,4]triazine (5b). Method A: A solution of (4b) (155 mg, 0.78 mmol) and 10% hydrochloric acid (0.1 mL) in ethanol (5 mL) was refluxed for 1 h. After that time the solvent was evaporated in vacuo and the crude product was purified by column chromatography (silica gel, chloroform) to afford the final product (5b) as a yellow oil (130 mg, 0.58 mmol, 58%).…”

Section: Generalmentioning

confidence: 99%

“…The reaction was quenched with a Na 2 CO 3 saturated solution and extracted with dichloromethane. The combined organic phases were dried over MgSO 4 and concentrated in vacuo. After purification by column chromatography on silica gel, (hexane:CH 2 Cl 2 , 5:1), the desired product (6) was obtained.…”

Section: Generalmentioning

confidence: 99%

“…Phosphodiesterase 5 (PDE5) is widely distributed in vascular and visceral smooth muscle cells, platelets, kidney, lung and corpus cavernosum, and plays a key role in the regulation of the cellular level of cGMP. The main therapeutic indications for PDE5 inhibitors are the treatment of erectile dysfunction [sildenafil (Viagra), vardenafil (Levitra), and tadalafil (Cialis), udenafil (Zydena)] and idiopathic pulmonary hypertension [sildenafil (Revatio)], although several other potentials have also been identified, such as memory improvement, anticancer therapy and treatment of heart diseases 4 . PDE5 is a therapeutic target of considerable research interest as can be seen by numerous publications regarding the design, synthesis and optimization of new PDE5 inhibitors 5,6 .…”

Section: Introductionmentioning

confidence: 99%

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Relaxant effects of selected sildenafil analogues in the rat aorta

Kubacka

Mogilski

Filipek

et al. 2015

Journal of Enzyme Inhibition and Medicinal Chemistry

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A new series of sulfonamide derivatives of pyrazolo [4,3-e][1,2,4]triazine with chiral amino group has been synthesized and characterized. The compounds were tested for their relaxant effects in the rat aorta. Evaluation of prepared derivatives demonstrated that compound (8a) is probably a non-selective phosphodiesterase (PDE) inhibitor, as it induced aortic relaxation through endothelium-independent mechanism.

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“…33,34 The potential beneficial effects of PDE5 inhibitors in the pulmonary vasculature and in other systems have led to examination of alternative dosing regimens. 35 On the design of this study, patients took sildenafil citrate on-demand. The analysis of the dose regimen followed for the included patients showed that 12 of them took only one 100 mg sildenafil citrate weekly whereas the remaining 9 patients took 100 mg sildenafil citrate twice per week in different days.…”

Section: Sildenafil Citrate and Mononuclear Cells J García-cardoso Et Almentioning

confidence: 99%

Increased cyclic guanosine monophosphate production and endothelial nitric oxide synthase level in mononuclear cells from sildenafil citrate-treated patients with erectile dysfunction

et al. 2009

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Mononuclear cells express enzymes involved in the NO/cyclic guanosine monophosphate (cGMP) generating system, as well as PDE5. The objective of the study was to determine the effect of sildenafil citrate administration on the level of proteins involved in the NO/cGMP generating system in mononuclear cells from patients with ED. Twenty-one patients with ED (International Index of Erectile Function-Erectile Function Domain (IIEF-EFD) 17.9±0.8) were enrolled and 100 mg sildenafil citrate on-demand was administered during 12 weeks. All patients showed cardiovascular risk factors. After sildenafil citrate administration, IIEF-EFD score was improved (26 ± 1.2 Po0.05). In the mononuclear cells, the protein level of endothelial NO synthase (eNOS) was higher after sildenafil citrate treatment. It was accompanied by reduction in the circulating plasma levels of both high-sensitive C-reactive protein and soluble intercellular adhesive molecule-1. The protein level of soluble guanylate cyclase and PDE5 did not change in the mononuclear cells after sildenafil citrate treatment. However, in the mononuclear cells exogenous NO induced a higher cGMP production after 12-weeks sildenafil citrate administration. In conclusion, in mononuclear cells from patients with ED sildenafil citrate administration increased the level of eNOS protein and increased cGMP production in response to NO. Moreover, sildenafil citrate administration reduced the plasma circulating levels of two biomarkers associated with inflammation.

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Daily Administration of Phosphodiesterase Type 5 Inhibitors for Urological and Nonurological Indications

Cited by 54 publications

References 143 publications

Evaluation of Tadalafil effect on lower urinary tract symptoms of benign prostatic hyperplasia in patients treated with standard medication

Evaluation of Tadalafil effect on lower urinary tract symptoms of benign prostatic hyperplasia in patients treated with standard medication

Relaxant effects of selected sildenafil analogues in the rat aorta

Increased cyclic guanosine monophosphate production and endothelial nitric oxide synthase level in mononuclear cells from sildenafil citrate-treated patients with erectile dysfunction

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