Sildenafil: Emerging Cardiovascular Indications

Raja, Shahzad G.; Nayak, Suneela H.

doi:10.1016/j.athoracsur.2004.02.125

Cited by 53 publications

(32 citation statements)

References 77 publications

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“…It did not require discontinuing the treatment in none of the patients evaluated. These AE were no different than the ones described in other studies published of sildenafil in other forms of pharmacological presentation [12] [22] [23].…”

Section: Discussioncontrasting

confidence: 35%

Efficacy and Safety Evaluation of Sildenafil Citrate in the Form of 50 mg Orodispersible Tablets Controlled by Placebo

Annunziato¹,

Teodoro²,

Vicente³

et al. 2018

CRCM

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Purpose: To evaluate the efficacy and safety of sildenafil in orodispersable tablets of 50 mg vs. placebo in men with erectile dysfunction (ED). Methods: A blind, comparative, placebo controlled, randomized study was developed in 106 patients with ED. They randomly received sildenafil orodispersable 50 mg (Group I) or placebo (Group II) 3 times per week, 1 hour before sexual activity, during 4 weeks. The efficacy was evaluated by IIEF-5 and the adverse events (AE) by poll. Results: After 4 weeks a percentage improvement of the ED was observed in Group I patients 44% of whom became without ED vs. 2% of Group II, with an additional statistical significant improvement evidenced respect to the placebo in the IIEF-5 score from 13.7 ± 4.9 to 19.9 ± 4.4 vs. 13.1 ± 4.0 to 17.8 ± 4.9 in the placebo group, Confidence Interval (CI95%): 19.90 vs. 13.98, respectively, p < 0.001. Regarding the basal value, a total increment of the IIEF-5 was observed, at the end of the 4 weeks treatment of 60% in Group I vs. 10% in Group II. In Group I was evidenced an statistical significant improvement of the IIEF-5 in each of the 5 questions at the end of the 4 weeks, specially in questions 3, 4, and 5 related to keeping the erection and satisfaction (p < 0.0001). The AE were mild, transient and could be tolerated. No patient dropped out because AE. Conclusions: Sildenafil was superior to placebo, substantially improved the IIEF-5 scores, showing a statistical significant therapeutic response in the ED treatment and it was safe and well tolerated.

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Section: Discussioncontrasting

confidence: 35%

Efficacy and Safety Evaluation of Sildenafil Citrate in the Form of 50 mg Orodispersible Tablets Controlled by Placebo

Annunziato¹,

Teodoro²,

Vicente³

et al. 2018

CRCM

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“…2 Sildenafil and other drugs in its class (tadalafil, vardenafil) enhance intracellular cGMP levels in the corpus cavernosum, making them effective treatments for erectile dysfunction. 3 Recent studies have revealed the importance of PDE5A in other organ systems, 4,5 including the pulmonary vasculature, where PDE5A inhibition appears to benefit patients with chronic pulmonary hypertension. 6,7 Editorial p 2589 cGMP also regulates cardiac function, and its synthesis in response to nitric oxide or natriuretic peptides counters adrenergic stimulation and blunts the development of cardiac hypertrophy.…”

mentioning

confidence: 99%

Sildenafil Inhibits β-Adrenergic–Stimulated Cardiac Contractility in Humans

et al. 2005

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Background-Sildenafil inhibits phosphodiesterase 5 (PDE5A) to elevate intracellular cGMP and to induce vasodilation.This effect has led to its use for treating erectile dysfunction. Although its influence on rest heart function has appeared minimal, recent animal studies suggest that sildenafil can have potent effects on hearts stimulated by ␤-adrenergic or pressure overloads. We therefore tested whether sildenafil blunts dobutamine-stimulated cardiac function in humans. Methods and Results-Thirty-five healthy volunteers underwent a randomized, double-blind, placebo-controlled study in which cardiac function was assessed in response to dobutamine before and after oral sildenafil (100 mg, nϭ19) or placebo (nϭ16). Echo Doppler and noninvasive blood pressure data yielded load-independent contractility indexes (maximal power index and end-systolic elastance), ejection fraction, and measures of diastolic function. In the initial dobutamine test, systolic and diastolic function improved similarly in both treatment groups (eg, peak power index rose 80Ϯ28% in the placebo group and 82Ϯ31% in the sildenafil group; PϭNS). However, in subjects who then received sildenafil, their second dobutamine response was significantly blunted, with peak power, ejection fraction, and end-systolic elastance changes reduced by 32Ϯ34%, 66Ϯ64%, and 56Ϯ63%, respectively (each PϽ0.001 versus the initial response). This contrasted to the placebo group, which displayed similar functional responses with both dobutamine tests. Sildenafil treatment did not significantly alter diastolic changes induced by dobutamine compared with results with placebo.

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“…The use of sildenafil is also expected to increase due to its efficacy in the management of other cardiovascular conditions [17]. For this reason, it is very important to ensure the safety of this drug in a variety of conditions, and to study the potential drug-drug interactions with a wide variety of drugs.…”

Section: Discussionmentioning

confidence: 99%

The effect of ciprofloxacin and clarithromycin on sildenafil oral bioavailability in human volunteers

Hedaya

El-Afify

Maghraby

2006

Biopharm. Drug Dispos.

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Sildenafil is the first oral therapeutic agent for the management of male erectile dysfunction. Its oral bioavailability is only 40% due to extensive presystemic elimination, mainly by CYP3A4. This study examined the effect of coadministration of ciprofloxacin or clarithromycin, which inhibit CYP3A4, on the bioavailability and pharmacokinetics of sildenafil. Twelve healthy male volunteers received sildenafil alone or after pretreatment with the inhibitors in a balanced three-way crossover design. The pharmacokinetic analysis showed that ciprofloxacin coadministration with sildenafil significantly increased the AUC from 1407 +/- 380 to 2986 +/- 917 microg h/l (90% confidence interval 119%-159%) and the Cmax from 287 +/- 67 to 623 +/- 192 microg/l (90% confidence interval 127%-152%). Similarly, clarithromycin coadministration increased sildenafil AUC from 1407 +/- 380 to 3209 +/- 762 microg h/l (90% confidence interval 127%-161%) and Cmax from 287 +/- 67 to 694 +/- 259 microg/l (90% confidence interval 132%-157%). Ciprofloxacin coadministration and clarithromycin coadministration with sildenafil did not affect the rate of sildenafil absorption significantly. These results indicate that coadministration of ciprofloxacin and clarithromycin significantly increased sildenafil bioavailability which can be attributed to the inhibitory effect of ciprofloxacin and clarithromycin on CYP3A4. Dose adjustment of sildenafil is thus necessary when administered with such drugs.

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Sildenafil: Emerging Cardiovascular Indications

Cited by 53 publications

References 77 publications

Efficacy and Safety Evaluation of Sildenafil Citrate in the Form of 50 mg Orodispersible Tablets Controlled by Placebo

Efficacy and Safety Evaluation of Sildenafil Citrate in the Form of 50 mg Orodispersible Tablets Controlled by Placebo

Sildenafil Inhibits β-Adrenergic–Stimulated Cardiac Contractility in Humans

The effect of ciprofloxacin and clarithromycin on sildenafil oral bioavailability in human volunteers

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