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https://www.readbyqxmd.com/read/27889014/-the-role-of-alpha-blockers-in-the-treatment-of-lower-urinary-tract-symptoms-benign-prostatic-hyperplasia-are-all-the-same-silodosin-in-real-life
#1
A Alcántara Montero
The lower urinary tract symptoms (LUTS) are very common in men, particularly in people over 65 years. Benign prostatic hyperplasia (BPH) is the pathology most associated with LUTS in males, and is a common cause of impaired quality of life. Alpha blockers monotherapy represent the treatment of choice in patients with moderate-severe LUTS secondary to BPH. Silodosin is currently the most α1A uroselective alpha blocker, uroselectivity which has been confirmed in several studies both in vitro and in vivo. In this paper the main benefits of silodosin are analyzed in both phase III clinical trials (standard approach) as in "real life" (analyzing the study SiRE [Silodosin in Real-life Evaluation], phase IV study), to validate the test data recording and confirm the positive benefit-risk profile of silodosin in a context that can reflect more closely the clinical practice...
July 2016: Semergen
https://www.readbyqxmd.com/read/27866053/lc-esi-ms-ms-evaluation-of-forced-degradation-behaviour-of-silodosin-in-vitro-anti-cancer-activity-evaluation-of-silodosin-and-major-degradation-products
#2
Chiguru Vishnuvardhan, Baikadi Saibaba, Lingesh Allakonda, Debasish Swain, S Gananadhamu, R Srinivas, N Satheeshkumar
Silodosin (SLD) a novel α1-adrenoceptor antagonist was subjected to forced degradation involving hydrolysis (acidic, alkaline and neutral), oxidative, photolysis and thermal stress, as per ICH specified conditions. The drug underwent significant degradation under hydrolytic (acidic, alkaline and neutral) and oxidative stress conditions whereas, it was found to be stable under other stress conditions. A rapid, precise, accurate and robust chromatographic method for the separation of the drug and its degradation products (DPs) was developed on a Fortis C18 analytical column (150×4...
November 10, 2016: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/27864702/selective-spectrofluorimetric-method-with-enhanced-sensitivity-for-determination-of-silodosine-in-dosage-form-and-human-plasma-application-to-stability-studies-and-content-uniformity-testing
#3
Mahmoud A Omar, Abdel-Maaboud I Mohamed, Sayed M Derayea, Mohamed A Hammad, Abobakr A Mohamed
A novel, sensitive and selective spectrofluorimetric method has been developed and validated for determination of silodosine (SLD) in its dosage form and human plasma. The method is based on nucleophilic substitution reaction of SLD with 5-(dimethylamino) naphthalene-1-sulfonyl chloride (dansyl chloride) in presence of 5.0 × 10(-4) M sodium carbonate (pH 10.50) to yield a highly fluorescent derivative that was measured at 435 nm after excitation at 347 nm. The different experimental parameters affecting the development and stability of the reaction product were carefully studied and optimized...
November 19, 2016: Journal of Fluorescence
https://www.readbyqxmd.com/read/27864032/%C3%AE-1a-adrenergic-receptor-antagonism-improves-erectile-and-cavernosal-responses-in-rats-with-cavernous-nerve-injury-and-enhances-neurogenic-responses-in-human-corpus-cavernosum-from-patients-with%C3%A2-erectile-dysfunction-secondary-to-radical-prostatectomy
#4
Juan I Martínez-Salamanca, José M La Fuente, Eduardo Martínez-Salamanca, Argentina Fernández, Augusto J Pepe-Cardoso, Nuno Louro, Joaquín Carballido, Javier Angulo
INTRODUCTION: Cavernous nerve injury (CNI) in rats and radical prostatectomy (RP) in men result in loss of nitrergic function and increased adrenergic-neurogenic contractions of cavernosal tissue. AIM: To evaluate the modulation of the α-adrenergic system as a strategy to relieve erectile dysfunction (ED) and functional cavernosal alterations induced by CNI. METHODS: A non-selective α-blocker (phentolamine 1 mg/kg daily), a selective α1A-blocker (silodosin [SILOD] 0...
November 15, 2016: Journal of Sexual Medicine
https://www.readbyqxmd.com/read/27845695/-prognostic-factors-for-the-efficacy-of-silodosin-in-the-treatment-of-symptomatic-benign-prostatic-hyperplasia-subanalysis-of-the-ural-study
#5
Jesús Salinas-Casado, Miguel Vírseda-Chamorro, Santiago Méndez-Rubio, Marcos Luján-Galán, Manuel Esteban-Fuertes, Jesús Moreno-Sierra
OBJECTIVE: To identify the prognostic factors influencing the clinical and urodynamics results on symptomatic benign prostatic hypertrophy (BHP) treatment in a series of patients with silodosin therapy from the URAL study. METHODS: A retrospective study was performed in a cohort of 318 patients with BPH which underwent silodosine treatment, during at least 12 weeks. RESULTS: Univariate analysis demonstrated that the variables in relationship with a decrease of urinary symptoms` punctuation postreatment (measured with the IPSS Questionnaire), a maximum peak flow (Q max) postreatment equal or superior to 15 ml/s, a postreatment postvoid residual lower to 100 ml, and a postreatment obstruction index ( Bladder Outlet Obstruction Index: BOOI) equal or lower to 20 cm H2O, presented such both as a clinical and urodynamic character...
November 2016: Archivos Españoles de Urología
https://www.readbyqxmd.com/read/27752927/%C3%AE-1-blockers-in-men-with-lower-urinary-tract-symptoms-suggestive-of-benign-prostatic-obstruction-is-silodosin-different
#6
REVIEW
Claus G Roehrborn, Francisco Cruz, Ferdinando Fusco
Available α1-blockers (ABs) have different profiles of receptor selectivity. Silodosin exhibits the highest selectivity for the α1A adrenergic receptor. This pharmacological feature couples with a singular urodynamic and clinical profile. The magnitude of bladder outlet obstruction improvement in patients receiving silodosin is higher if compared to other ABs. From a clinical point of view, current evidence suggests an advantage in favor of silodosin in terms of nocturia improvement and cardiovascular safety...
October 17, 2016: Advances in Therapy
https://www.readbyqxmd.com/read/27747994/in-vivo-metabolic-investigation-of-silodosin-using-uhplc-qtof-ms-ms-and-in-silico-toxicological-screening-of-its-metabolites
#7
Chiguru Vishnuvardhan, Saibaba Baikadi, Roshan M Borkar, R Srinivas, N Satheeshkumar
Silodosin (SLD) is a novel α1-adrenoceptor antagonist which has shown promising clinical efficacy and safety in patients with benign prostatic hyperplasia (BPH). However, lack of information about metabolism of SLD prompted us to investigate metabolic fate of SLD in rats. To identify in vivo metabolites of SLD, urine, feces and plasma were collected from Sprague-Dawley rats after its oral administration. The samples were prepared using an optimized sample preparation approach involving protein precipitation followed by solid-phase extraction and then subjected to LC/HR-MS/MS analysis...
October 2016: Journal of Mass Spectrometry: JMS
https://www.readbyqxmd.com/read/27747715/coma-after-quetiapine-fumarate-intentional-overdose-in-a-71-year-old-man-a-case-report
#8
S Gibiino, A Trappoli, B Balzarro, A R Atti, D De Ronchi
A 71-year-old man developed coma with severe respiratory failure, hypotension, and tachycardia induced by the intentional ingestion of quetiapine fumarate extended release (XR) 20 g. At the time, he had been treated for bipolar depression with venlafaxine 75 mg/day, lamotrigine 100 mg/day, pregabalin 75 mg/day, and quetiapine XR 400 mg/day for approximately 1 year. Comorbidities were hypertension treated with metoprolol, diabetes mellitus type 2 treated with metformin, and benign prostatic hyperplasia treated with silodosin...
December 2015: Drug Safety—Case Reports
https://www.readbyqxmd.com/read/27747713/a-suspected-case-of-silodosin-induced-erythroderma
#9
Annie Liu, Lyne Giroux
An 86-year-old man developed a suspected severe erythroderma during treatment with silodosin (dosage unknown) for benign prostatic enlargement. Two weeks after starting silodosin, he developed a total-body scaling dermatitis. A biopsy was planned but the patient improved at his subsequent visit and it was not taken. Silodosin was discontinued and the patient received UVB phototherapy, clobetasol ointment, and several bland and protective skin-care measures. One week after the initial presentation, the patient demonstrated improvement in his total-body scaling...
December 2015: Drug Safety—Case Reports
https://www.readbyqxmd.com/read/27729995/effectiveness-of-on-demand-silodosin-in-the-treatment-of-premature-ejaculation-in-patients-dissatisfied-with-dapoxetine-a-randomized-control-study
#10
Gajanan S Bhat, Anuradha Shastry
INTRODUCTION: Premature ejaculation is a common sexual disorder, which is usually underreported. Multiple treatment methodologies are in use due to the absence of an effective, universally acceptable treatment modality. The most common drug used is dapoxetine, which has adverse effects limiting its long-term use. Hence, we decided to evaluate the effectiveness of 'on demand' silidosin 4 mg in patients with premature ejaculation, who were dissatisfied with dapoxetine 30 mg. MATERIAL AND METHODS: The study included 64 patients who reported premature ejaculation who were unhappy with the treatment with 'on demand' dapoxetine 30 mg, either due to its adverse effects or because of its overall inefficacy...
2016: Central European Journal of Urology
https://www.readbyqxmd.com/read/27727093/-lower-urinary-tract-symptoms-and-pelvic-floor-dysfunction-in-renal-transplant-candidates-and-recipients
#11
R Thuret, S Hurel, F Kleinclauss, M O Timsit
OBJECTIVES: To describe lower urinary tract symptoms (LUTS) and their management in renal transplant candidates and recipients. MATERIAL AND METHODS: Relevant publications were identified through Medline (http://www.ncbi.nlm.nih.gov) and Embase (http://www.embase.com) database using the following keywords, alone or in association: "transplantation", "prostate hyperplasia", "transurethral resection of prostate", "urinary incontinence", "LUTS", "pelvic floor dysfunction"...
October 7, 2016: Progrès en Urologie
https://www.readbyqxmd.com/read/27709945/design-synthesis-and-biological-evaluation-of-novel-tetrahydroprotoberberine-derivatives-thpbs-as-selective-%C3%AE-1a-adrenoceptor-antagonists
#12
Diliang Guo, Jing Li, Henry Lin, Yu Zhou, Ying Chen, Fei Zhao, Haifeng Sun, Dan Zhang, Honglin Li, Brian K Shoichet, Lei Shan, Weidong Zhang, Xin Xie, Hualiang Jiang, Hong Liu
A novel series of tetrahydroprotoberberine derivatives (THPBs) were designed, synthesized and evaluated as selective α1A-adrenergic receptors (AR) antagonists for the treatment of benign prostatic hyperplasia. Based on the pharmacophore model of the marketed drug silodosin, THPBs were modified by introducing an indole segment into their core scaffolds. In calcium assays, 7 out of 32 compounds displayed excellent antagonistic activities against α1A-ARs, with IC50s less than 250 nM. Among them, compound (S)-27 had the most potent biological activity; its IC50 toward α1A-AR was 12...
October 6, 2016: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27687860/the-role-of-silodosin-as-a-new-medical-expulsive-therapy-for-ureteral-stones-a-meta-analysis
#13
Hui Ding, Zhongyun Ning, Yu Dai, Panfeng Shang, Li Yang
To evaluate the efficacy of Silodosin as a medical expulsive therapy of ureteral stones, we searched PubMed, EMBASE, the Cochrane Library, and CBM up to June 2015. All randomized controlled trials (RCTs) were identified in which patients were randomized to receive Silodosin versus placebo or other therapies for ureteral stones. Outcome measures assessed were overall stone expulsion rate (primary) and expulsion time, analgesics times, and the incidence of additional treatment and regarding treatment complications (secondary)...
October 2016: Renal Failure
https://www.readbyqxmd.com/read/27683251/intraprostatic-reflux-of-urine-induces-inflammation-in-a-rat
#14
Yasuhito Funahashi, Tsuyoshi Majima, Yoshihisa Matsukawa, Tokunori Yamamoto, Masaki Yoshida, Momokazu Gotoh
BACKGROUND: We examined whether urine reflux into the prostate can induce prostatic inflammation in a rat and evaluated the effect of α1-adrenoreceptor antagonist. METHODS: Experiment 1: Male Sprague-Dawley rats were injected with 500 µl of Evans Blue through the urethral orifice. Intravesical pressure was measured, and the prostate was excised to evaluate urine reflux. Experiment 2: Rats were injected with 500 µl urine or saline (control) from the urethral orifice...
September 29, 2016: Prostate
https://www.readbyqxmd.com/read/27629059/new-medical-treatments-for-lower-urinary-tract-symptoms-due-to-benign-prostatic-hyperplasia-and-future-perspectives
#15
Simone Albisinni, Ibrahim Biaou, Quentin Marcelis, Fouad Aoun, Cosimo De Nunzio, Thierry Roumeguère
BACKGROUND: Lower Urinary Tract Symptoms (LUTS) in men are a common clinical problem in urology and have been historically strictly linked to benign prostatic hyperplasia (BPH), which may lead to bladder outlet obstruction (BOO). New molecules have been approved and have entered the urologists' armamentarium, targeting new signaling pathways and tackling specific aspects of LUTS. Objective of this review is to summarize the evidence regarding the new medical therapies currently available for male non-neurogenic LUTS, including superselective α1-antagonists, PDE-5 inhibitors, anticholinergic drugs and intraprostatic onabotulinum toxin injections...
September 15, 2016: BMC Urology
https://www.readbyqxmd.com/read/27615436/comparison-of-silodosin-and-naftopidil-for-efficacy-in-the-treatment-of-benign-prostatic-enlargement-complicated-by-overactive-bladder-a-randomized-prospective-study-sniper-study
#16
Yoshihisa Matsukawa, Yasuhito Funahashi, Shun Takai, Tsuyoshi Majima, Tadashi Ogawa, Harunori Narita, Masashi Kato, Momokazu Gotoh
PURPOSE: To investigate the efficacy of two α1-blockers with different affinity for α1 adrenoceptor subtypes, silodosin and naftopidil, in the treatment of benign prostatic enlargement (BPE) complicated by overactive bladder (OAB). MATERIALS AND METHODS: This was a prospective, open-label, randomized, multicenter study involving 350 outpatients with untreated BPE associated with urinary urgency at least once per week and OAB Symptom Score (OABSS) of ≥ 3. The patients were randomly assigned to receive silodosin at 8 mg/day or naftopidil at 75 mg/day...
September 8, 2016: Journal of Urology
https://www.readbyqxmd.com/read/27605559/%C3%AE-1d-adrenoceptor-blockade-increases-voiding-efficiency-by-improving-external-urethral-sphincter-activity-in-rats-with-spinal-cord-injury
#17
Hirokazu Ishida, Hiroki Yamauchi, Hideaki Ito, Hironobu Akino, Osamu Yokoyama
PURPOSE: Ideal therapy for lower urinary tract dysfunction in patients with spinal cord injury (SCI) should decrease detrusor overactivity, thereby promoting urine storage at low intravesical pressure and promoting efficient voiding at low pressure by decreasing detrusor-sphincter dyssynergia. Here we investigated blockade of various α1-adrenoceptors to determine the subtype that was principally responsible for improving the voiding dysfunction. MATERIALS AND METHODS: The effects of the intravenous α1A/D-blocker naftopidil, the α1D-blocker BMY 7378, and the α1A-blocker silodosin were evaluated using cystometrography and external urethral sphincter-electromyography (EMG) in decerebrated, unanesthetized female Sprague-Dawley rats with chronic SCI following transection at Th8...
September 7, 2016: American Journal of Physiology. Regulatory, Integrative and Comparative Physiology
https://www.readbyqxmd.com/read/27551761/interactions-between-medications-employed-in-treating-benign-prostatic-hyperplasia-and-food-a-short-review
#18
Paweł Paśko, Tomasz Rodacki, Renata Domagała-Rodacka, Danuta Owczarek
Benign prostatic hyperplasia (BPH) is the most common disease in elderly men. BPH symptoms include frequent urination, urgent tenesmus and urination at night, a weak and interrupted urine flow and a sense of incomplete emptying of the bladder. Alpha- 1 adrenergic receptor antagonists and 5 α-reductase inhibitors form the most important groups of medications employed in BPH. Appropriately managed BPH patients shall be subject to counselling on interactions between agents belonging to these groups, and on particular components of the food they have...
October 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/27418315/effects-of-silodosin-on-bladder-activity-in-rats-with-frequent-urination-induced-by-pelvic-venous-congestion
#19
Kimio Sugaya, Saori Nishijima, Katsumi Kadekawa, Katsuhiro Ashitomi, Tomoyuki Ueda, Hideyuki Yamamoto
OBJECTIVE: To examine the effects of silodosin on bladder activity using female rats with frequent urination induced by pelvic venous congestion. METHODS: A total of 24 female rats were divided into three groups: sham, pelvic venous congestion and pelvic venous congestion/silodosin group. Rats in the pelvic venous congestion and pelvic venous congestion/silodosin groups were anesthetized with isoflurane, after which the bilateral common iliac veins and uterine veins were ligated...
July 14, 2016: International Journal of Urology: Official Journal of the Japanese Urological Association
https://www.readbyqxmd.com/read/27370818/bladder-pain-induced-by-prolonged-peripheral-alpha-1a-adrenoceptor-stimulation-involves-the-enhancement-of-transient-receptor-potential-vanilloid-1-activity-and-an-increase-of-urothelial-adenosine-triphosphate-release
#20
R Matos, J M Cordeiro, A Coelho, S Ferreira, C Silva, Y Igawa, F Cruz, A Charrua
AIM: Pathophysiological mechanisms of chronic visceral pain (CVP) are unknown. This study explores the association between the sympathetic system and bladder nociceptors activity by testing the effect of a prolonged adrenergic stimulation on transient receptor potential vanilloid 1 (TRPV1) activity and on urothelial adenosine triphosphate (ATP) release. METHODS: Female Wistar rats received saline, phenylephrine (PHE), PHE + silodosin, PHE + naftopidil or PHE + prazosin...
December 2016: Acta Physiologica
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