Management of benign prostatic hyperplasia with silodosin

Yamanishi, Tomonori

doi:10.2147/oaju.s5004

Cited by 3 publications

(1 citation statement)

References 48 publications

(58 reference statements)

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“…RS17053 has been examined for relaxant actions at prostate smooth muscle, and relaxed prostate smooth muscle and increased urine flow in men, but did not relieve lower urinary tract symptoms (LUTS), a lack of effect ascribed to α 1A ‐adrenoceptor selectivity, and lacking actions at a putative α 1L ‐adrenoceptor [20, 21], or lacking actions at α 1D ‐adrenoceptors [22]. Our studies would suggest the latter.…”

Section: Discussionmentioning

confidence: 95%

Effects of RS17053 on α₁‐adrenoceptors in rat vas deferens and aorta

Alsufyani

Docherty

2023

Fundamemntal Clinical Pharma

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BackgroundRS17053 is classed as an α1A‐adrenoceptor selective antagonist.ObjectivesWe have examined its profile of action at all subtypes of α1‐adrenoceptor.MethodsNoradrenaline (NA) evoked contractions of rat vas deferens involve α1D‐adrenoceptors in phasic contractions and α1A‐adrenoceptors in tonic contractions. Contractions of rat aorta to NA involve α1D‐ and α1B‐adrenoceptors.ResultsRS17053 (10−5 M) shifted NA potency and virtually abolished tonic contractions to NA, with little or limited effect on phasic contractions. The α1D‐adrenoceptor antagonist BMY7378 (3 × 10−7 M) significantly inhibited the remaining phasic component of the contractions, and the α1A‐adrenoceptor antagonist RS100329 (10−7 M) inhibited further the residual tonic contraction. Hence, RS17053 shows high selectivity for α1A‐adrenoceptors over α1D‐adrenoceptors in rat vas deferens. However, RS17053 (10−5 M) produced a large shift in the potency of NA in rat aorta, with a pKB of 6.82. Large shifts of NA potency in rat aorta involve α1B‐adrenoceptor blockade.ConclusionResults in rat vas deferens demonstrate low potency of RS17053 at α1D‐adrenoceptors, but results from rat aorta can only be explained as demonstrating α1B‐adrenoceptor antagonism by RS17053. RS17053 may be a useful pharmacological tool when reclassified as a mainly α1A‐ and to a lesser extent α1B‐adrenoceptor antagonist with little effect at α1D‐adrenoceptors.

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Section: Discussionmentioning

confidence: 95%

Effects of RS17053 on α₁‐adrenoceptors in rat vas deferens and aorta

Alsufyani

Docherty

2023

Fundamemntal Clinical Pharma

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Six‐year follow up of silodosin monotherapy for the treatment of lower urinary tract symptoms suggestive of benign prostatic hyperplasia: What are the factors for continuation or withdrawal?

et al. 2015

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Objectives: To investigate the factors for continuation or withdrawal as an extension of a prospective study of silodosin monotherapy for the treatment of lower urinary tract symptoms suggestive of benign prostatic hyperplasia for more than 6 years. Methods: A total of 104 patients (age 71.5 AE 8.2 years) were enrolled in the present study. The mean prostate volume was 44.1 AE 23.9 mL. International Prostate Symptom Score, quality of life index, maximum flow rate, and postvoid residual urine volume were determined at baseline, and at 1, 3, 6 and 12-72 months after treatment. Results: Adverse events were noted in 14 patients (13.5%), and the most frequent adverse event was ejaculatory dysfunction (5.8%). Withdrawal was noted in 78 patients, and 26 patients (25.0%) were still taking silodosin at 72 months (continuing group). The reasons for withdrawals were: unknown in 27 patients (26.0%), adverse events in nine patients (8.7%), unsatisfactory effects in 30 patients (28.8%) and satisfied with the current condition for six patients (5.8%). In 30 patients who withdrew because of unsatisfactory effects, surgery was carried out in 21 patients (surgery group). The baseline total International Prostate Symptom Score did not differ between the continuing group and the surgery group. However, patients with the continuing group had significantly smaller baseline prostate volume, and lower baseline quality of life index and prostate-specific antigen, than in the surgery group. The mean total International Prostate Symptom Score, quality of life index and maximum flow rate improved significantly at 1 month, and remained stable up to 72 months. Conclusions: The withdrawal rate was higher in patients with a larger prostate. The effects of silodosin for lower urinary tract symptoms was immediate and stable up to 72 months.

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