Silodosin

Silodosin(Rapaflo) is an α1-adrenoceptor antagonist with high uroselectivity. Silodosin causes practically no orthostatic hypotension (in contrast to other α1 blockers). Since Silodosin is a highly selective inhibitor of the α1A adrenergic receptor, it causes practically no orthostatic hypotension (in contrast to other α1 blockers).

Silodosin: a review of its use in the treatment of the signs and symptoms of benign prostatic hyperplasia.[Pubmed:25575983]

Drugs. 2015 Feb;75(2):207-17.

Silodosin is a highly selective alpha1A-adrenoceptor antagonist indicated for the treatment of the signs and symptoms of benign prostatic hyperplasia (BPH). Oral Silodosin had a rapid onset of effect in men with lower urinary tract symptoms (LUTS) associated with BPH, with improvements seen in voiding and storage symptoms, maximum urinary flow rate and health-related quality of life in well-designed, 12-week trials. Silodosin was noninferior to tamsulosin in terms of improving LUTS associated with BPH. The efficacy of Silodosin was maintained in 9-month extension studies and was also seen in a phase IV study conducted in a real-world setting. Silodosin was generally well tolerated and was associated with a low risk of orthostatic hypotension. Abnormal ejaculation was the most commonly reported adverse event, although few patients discontinued treatment with Silodosin because of this adverse event. In conclusion, Silodosin is a useful option for the treatment of LUTS associated with BPH.

Medical expulsive therapy for distal ureteric stones: tamsulosin versus silodosin.[Pubmed:25017589]

Arch Ital Urol Androl. 2014 Jun 30;86(2):103-7.

OBJECTIVES: To compare the efficacy and safety of tamsulosin and Silodosin in the context of medical expulsive therapy (MET) of distal ureteric stones. PATIENTS AND METHODS: Observational data were collected retrospectively from patients who received Silodosin (N = 50) or tamsulosin (N = 50) as MET from January 2012 to January 2013. Inclusion criteria were: patients aged >/= 18 years with a single, unilateral, symptomatic, radiopaque ureteric stone of 10 mm or smaller in the largest dimension located between the lower border of the sacroiliac joint and the vesico-ureteric junction. Stone expulsion rate, stone expulsion time, number of pain episodes, need for analgesics use, incidence of side effects were compared. RESULTS: Stone-expulsion rate in the Silodosin and in the tamsulosin groups were 88% and 82%, respectively (p not significant). Mean expulsion times were 6.7 and 6.5 days in the Silodosin and tamsulosin group, respectively (p not significant). Mean number of pain episodes were 1.6 and 1.7 in the Silodosin and tamsulosin group, respectively (p not significant). The mean number of analgesic requirement was 0.84 and 0.9 for the Silodosin and tamsulosin group, respectively (p not significant). Overall, incidence of side effects was similar in both groups. Patients taking Silodosin experienced an higher incidence of retrograde ejaculation but a lower incidence of side effects related to peripheral vasodilation when compared to patients taking tamsulosin. Subgroup analysis demonstrated significantly lower mean expulsion times and pain episodes in patients with stones Silodosin are equally effective as MET for distal ureteric stones sized 10 mm or smaller. MET with Silodosin is associatd with a lower incidence of side effects related to peripheral vasodilation but an higher incidence of retrograde ejaculation when compared to tamsulosin.

Silodosin to facilitate passage of ureteral stones: a multi-institutional, randomized, double-blinded, placebo-controlled trial.[Pubmed:25465978]

Eur Urol. 2015 May;67(5):959-64.

BACKGROUND: Using a selective alpha-blocker for medical expulsive therapy (MET) is a cost-effective treatment approach widely used for ureteral stones. OBJECTIVE: To evaluate the efficacy of Silodosin, a selective alpha-1a receptor antagonist, in this setting. DESIGN, SETTING, AND PARTICIPANTS: This was a multicenter, phase 2 study conducted in adult patients with a unilateral ureteral calculus of 4-10mm. Of 239 patients in the safety population, six discontinued due to adverse events. INTERVENTION: Patients were randomized 1:1 to receive Silodosin 8 mg or placebo for up to 4 wk. OUTCOME MEASUREMENTS AND STATISTICAL ANALYSIS: The primary outcome was spontaneous stone passage, analyzed using logistic regression. Secondary outcomes included time to stone passage, emergency room (ER) visits, hospital admissions, analgesic use, and incidence and severity of pain. RESULTS AND LIMITATIONS: No significant differences between the Silodosin and placebo groups were observed for passage rate of all stones (52% vs 44%, respectively; p=0.2). However, Silodosin achieved a significantly greater rate of distal ureter stone passage than placebo (p=0.01). Significant differences were not observed for ER visits, hospital admission, or use of analgesics. The number of patients in the intent-to-treat population was slightly below the calculated sample size (232 vs 240) and sample sizes were not calculated for subgroup analyses. CONCLUSIONS: This is among the first prospective, randomized, multi-institutional trials to examine the efficacy of a selective alpha-1a antagonist as MET in patients with ureteral calculi and did not demonstrate a benefit to the entire ureter. However, Silodosin was found to be well tolerated and beneficial in facilitating the passage of distal ureteral stones, warranting additional future studies on distal stone elimination. PATIENT SUMMARY: In this report, we looked at the efficacy of Silodosin for the treatment of ureteral stones. We found that Silodosin increased passage of distal ureteral stones.

Silodosin and its potential for treating premature ejaculation: a preliminary report.[Pubmed:22188258]

Int J Urol. 2012 Mar;19(3):268-72.

Premature ejaculation is a common sexual problem, as is erectile dysfunction. We evaluated Silodosin, a highly selective alpha1A-adrenoceptor antagonist, as a new treatment option for premature ejaculation. alpha1-Adrenoceptor antagonists are widely used for lower urinary tract symptoms, and clinical studies on Silodosin have shown excellent clinical efficacy for lower urinary tract symptoms. However, compared with other alpha1-adrenoceptor antagonists, Silodosin appeared to suppress ejaculation in a relatively higher percent of trial participants. This suppression of ejaculation by Silodosin suggested its potential for treating premature ejaculation. Consequently, we evaluated the feasibility of off-label Silodosin as a new treatment option for premature ejaculation. Eight patients suffering premature ejaculation were treated with Silodosin. Silodosin (4 mg) was given 2 h before sexual intercourse. Intravaginal ejaculatory latency time, premature ejaculation profile item, clinical global impression change in premature ejaculation and systemic adverse events were recorded. Intravaginal ejaculatory latency time was significantly prolonged (from 3.4 min to 10.1 min, P = 0.003). All patients answered better (much better) or slightly better for their own premature ejaculation problem compared with pretreatment condition in the clinical global impression change. Premature ejaculation profile also significantly improved. Two (25%), three (37.5%) and seven patients (87.5%) experienced anejaculation, reduced semen volume and discomfort during orgasm, respectively. However, these problems were not of major concern for the participants. No systemic adverse effects were reported. The current results support the possible use of Silodosin as a new treatment option for premature ejaculation, and suggest that a placebo controlled study assessing its clinical usefulness would be worthwhile.

Silodosin (KAD 3213; KMD 3213) is a potent, selective and orally active α1A-adrenergic receptor (α1A-AR) blocker. Silodosin exhibits high affinity for α1A-AR (Ki=0.036 nM), over 162-fold and 50-fold than for α1B-AR and α1D-AR with Ki values of 21 nM and 2.0 nM, respectively. Silodosin is an effective and well-tolerated agent, it can be used for the investigation of LUTS/BPH.

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