The Oral Efficacy of Vardenafil Hydrochloride for Inducing Penile Erection in a Conscious Rabbit Model

Bischoff, Erwin; Niewoehner, U.; Haning, Helmut; Sayed, M.E.S.; Schenke, Thomas; Schlemmer, Karl‐Heinz

doi:10.1097/00005392-200104000-00076

Cited by 9 publications

(10 citation statements)

References 12 publications

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“…The 10 mgakg dose induced a strong erection but there was no greater effect at 30 mgakg dose indicating that the maximal effect was achieved at the 10 mg dose. 17 We could con®rm also that the model was responsive to accepted agents for erectile dysfunction, eg oral sildena®l at 3, 10 and 25 mgakg induced erections as well.…”

Section: Introductionmentioning

confidence: 74%

Rabbits as models for impotence research

Bischoff¹

2001

Int J Impot Res

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Section: Introductionmentioning

confidence: 74%

Rabbits as models for impotence research

Bischoff¹

2001

Int J Impot Res

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“…In a direct comparison with sildenafil, vardenafil was proven effective at lower concentrations. 1,2,3 Also, vardenafil significantly potentiated both acetylcholine (Ach)-induced and transmural electrical stimulation-induced relaxation of trabecular smooth muscle.…”

Section: Introductionmentioning

confidence: 98%

“…Vardenafil potentiated erectile responses to intravenous sodium nitroprusside in conscious rabbits in a dose-dependent manner at doses of 0.1-3 mg/kg. 1,3 The minimum dose required for a significant erectile effect was determined to be 0.1 mg/kg. Vardenafil also demonstrated effectiveness in an anesthetized rabbit model with pelvic nerve stimulation 2 and in a rat model, displaying greater efficacy on erectile response than sildenafil at comparable doses.…”

Section: Introductionmentioning

confidence: 99%

Vardenafil preclinical trial data: potency, pharmacodynamics, pharmacokinetics, and adverse events

Bischoff

2004

Int J Impot Res

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Vardenafil potently inhibits human phosphodiesterase 5 (PDE5) with an IC 50 of 0.7 nM. Enhancement of nitric oxide (NO)-induced erections in rabbits by 0.1 mg/kg vardenafil is limited by its pharmacokinetic properties (T max ¼ 1 h; T 1/2 ¼ 1.2 h), although erectile effects have been observed after 7 h. In humans, vardenafil is rapidly absorbed (T max E40 min) and more slowly metabolized (T 1/2 E4 h), with an absolute bioavailability of 14.5% (vs 40% for sildenafil). Although the consumption of high-fat meals does not affect the drug's relative bioavailability, it retards intestinal absorption. Coadministration of CYP3A4 inhibitors such as ritonavir can affect hepatic metabolism. M1, an active metabolite of vardenafil, is a four-fold-less potent inhibitor of PDE5 than its parent compound, contributing approximately 7% to vardenafil's overall efficacy. The side effects of all selective PDE5 inhibitors commonly include vasodilation, small reductions in blood pressure, headache, and nasal congestion.

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“…8 In a rabbit model, orally administered vardenafil facilitated penile erection. [9][10][11] Additional clinical trials have demonstrated that vardenafil is an efficacious agent in improvement of erectile function. [12][13][14][15][16] In the present study, we report the results of a Phase IIb trial, which investigated safety and efficacy of vardenafil in Japanese ED patients.…”

Section: Introductionmentioning

confidence: 99%

Safety and efficacy of vardenafil in patients with erectile dysfunction: Result of a bridging study in Japan

et al. 2004

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Aim : Vardenafil is a selective and highly potent phosphodiesterase type 5 (PDE5) inhibitor for the treatment of erectile dysfunction (ED), with improved selectivity for PDE5 and demonstrated efficacy for improving sexual function in men with ED. The current study investigated the safety and efficacy of this new PDE5 inhibitor in Japanese men with ED.Methods : This was a prospective, double blind, randomized clinical trial designed to evaluate the efficacy and safety of vardenafil. Following a 4-week treatment-free observation period, 283 eligible patients were randomized to 12 weeks treatment with vardenafil 5 mg, 10 mg, 20 mg, or placebo. Primary efficacy responses were assessed using the scores of Q3 and Q4 of the international index of erectile function (IIEF).Results : All three vardenafil doses showed significantly better improvement than the placebo group in Q3 and Q4 scores of the IIEF questionnaire, either at 12 weeks or at the 'last observation carried forward' (LOCF, P < 0.0001). Q3 scores were improved to 4.06 with vardenafil 5 mg, 4.53 with vardenafil 10 mg, and 4.64 with vardenafil 20 mg, versus 3.17 with placebo. Comparable scores for Q4 were 3.47, 4.15 and 4.31 versus 2.31 for placebo. Up to 86% of patients achieved improved erections as assessed by the global assessment question (GAQ). Reported adverse event rates were 35.3%, 45.3% and 54.5% with vardenafil 5 mg, 10 mg and 20 mg, respectively, versus 21.1% in the placebo group. No serious adverse drug reactions were reported. The most common treatment-emergent adverse events were transient headache, flushing and rhinitis, which were mostly mild. Conclusion : Vardenafil is an effective and well-tolerated treatment for ED and provides improvement in key indices of erectile function among Japanese men with ED. The results of our trial show that up to nearly 90% of patients achieve improved erections with the administration of vardenafil.

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The Oral Efficacy of Vardenafil Hydrochloride for Inducing Penile Erection in a Conscious Rabbit Model

Cited by 9 publications

References 12 publications

Rabbits as models for impotence research

Rabbits as models for impotence research

Vardenafil preclinical trial data: potency, pharmacodynamics, pharmacokinetics, and adverse events

Safety and efficacy of vardenafil in patients with erectile dysfunction: Result of a bridging study in Japan

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