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The Journal of Pharmacy Technology :... Apr 2018To review the literature for α-blocker treatment of kidney stones. PubMed search performed November 15, 2017, using the following search terms: alpha-blocker,... (Review)
Review
To review the literature for α-blocker treatment of kidney stones. PubMed search performed November 15, 2017, using the following search terms: alpha-blocker, alfuzosin, silodosin, or tamsulosin AND kidney or ureteral stones. Additional studies found through references of primary and tertiary literature. Inclusion criteria included English language, randomized controlled trials (not included in meta-analyses), and meta-analyses evaluating US available alpha-blockers as medical expulsive therapy with or without lithotripsy in adults with renal or ureteral stones, and no date limits. Seven randomized controlled trials (RCTs), 1 case-control trial, and 6 meta-analyses were found and included in this review. Two RCTs and 4 meta-analyses evaluated alpha-blockers without lithotripsy. Five RCTs, 1 case-control trial, and 2 meta-analyses evaluated their use post-lithotripsy. The primary endpoint was stone clearance rate in most studies. For ureteral stones ≤10 mm treated without lithotripsy, alpha-blockers increased clearance in all meta-analyses and one RCT versus control. For ureteral or renal stones treated with lithotripsy, 4 RCTs and all meta-analyses found benefit with alpha-blockers compared with control. When results were stratified by stone size, alpha-blockers performed better for stones 10 to 20 mm, while there was no difference for stones <10 mm. Alpha-blockers are beneficial without lithotripsy for ureteral stones 5 to 10 mm. They are beneficial post-lithotripsy for renal or ureteral stones >10 mm. They can be considered post-lithotripsy for stones 5 to 10 mm, but little benefit may be seen. Although all uroselective alpha-blockers have been found to be effective, most data are with tamsulosin 0.4 mg daily.
PubMed: 34860948
DOI: 10.1177/8755122517750398 -
Journal of Clinical and Diagnostic... Jun 2015To evaluate the efficacy/safety of 'tamsulosin and darifenacin' (TD) vs. 'tamsulosin and placebo' (TP) for patients with symptomatic benign prostrate hyperplasia (BPH)...
PURPOSE
To evaluate the efficacy/safety of 'tamsulosin and darifenacin' (TD) vs. 'tamsulosin and placebo' (TP) for patients with symptomatic benign prostrate hyperplasia (BPH) with accompanying overactive bladder (OAB) symptoms.
MATERIALS AND METHODS
This study included symptomatic patients of BPH with one or more of the following OAB symptoms; micturition frequency >8, nocturnal frequency > 2, urgency > 1 per 24 hour between November 2012 and February 2014. After protocol approval by ethics committee and obtaining informed consent, patients were randomly assigned to receive tamsulosin 0.4mg plus placebo (TP) (n=30) or tamsulosin 0.4 mg plus darifenacin 7.5 mg (TD) (n=30) for 8 weeks. The mean change from baseline in urinary frequency and incontinence episodes/24 hour (primary end points), and nocturnal frequency; mean change in PVR and changes in IPSS (secondary end points) were compared between groups at 0/eight week using voiding diary and ultrasonography.
RESULTS
The mean change in frequency, incontinence, nocturnal frequency/24 hour and IPSS (International prostrate symptom score) were (-4.83 vs. -3.93, p=0.023), (-1.50 vs. 1.08, p=0.001), (-2.20 vs. -1.87, p<0.001) and (-7.90 vs. -6.27, p<0.001) in the TD/TP group respectively (significant). Apart from some minor side effects (12 vs. 9) all interventions appeared to be safe and well tolerated. The mean change in the PVR (Postvoid residual) was marginal (+10.84ml and -16.93) and the incidence of urinary retention was 13% and 3% in the TD and TP groups respectively (p=0.35).
CONCLUSION
Treatment with tamsulosin and darifenacin for 8 weeks is an effective and safe treatment modality in select patients of BPH with accompanying OAB symptoms.
PubMed: 26266159
DOI: 10.7860/JCDR/2015/12526.6019 -
American Journal of Men's Health 2020Studies reported that was effective in relieving lower urinary tract symptoms (LUTS). This article carried out a systematic review and meta-analysis to compare with... (Meta-Analysis)
Meta-Analysis
Studies reported that was effective in relieving lower urinary tract symptoms (LUTS). This article carried out a systematic review and meta-analysis to compare with tamsulosin in the treatment of benign prostatic hyperplasia (BPH) after at least 6-month treatment cycle. Four studies involving 1,080 patients (543 in the group and 537 in the tamsulosin group) were included in the meta-analysis. The results were as follows: compared with tamsulosin, had a same effect in treating BPH in terms of International Prostate Symptom Score (IPSS) (mean difference [MD] 0.63, 95% confidence interval [CI] [-0.33, 1.59], = 0.20), quality of life (QoL) (MD 1.51, 95% CI [-1.51, 4.52], = 0.33), maximum flow rate (Qmax) (MD 0.27, 95% CI [-0.15, 0.68], = 0.21), postvoid residual volume (PVR) (MD -4.23, 95% CI [-22.97, 14.44], = 0.65), prostate-specific antigen (PSA) (MD 0.46, 95% CI [-0.06, 0.97], = 0.08) with the exception of prostate volume (PV) (MD -0.29, 95% CI [-0.41, -0.17], < 0.00001). For side effects, was well tolerated compared with tamsulosin especially in ejaculation disorders (odds ratio [OR] = 12.56, 95% CI [3.83, 41.18], < 0.0001) and decreased libido (OR = 5.40; 95% CI [1.17, 24.87]; = 0.03). This study indicated that had the same effect in treating BPH compared with tamsulosin in terms of IPSS, QoL, and PVR after at least 6-month treatment cycle, however, the latter had a greater improvement in PV compared with the former. And did not increase the risk of adverse events especially with respect to ejaculation disorders and libido decrease.
Topics: Aged; Aged, 80 and over; Humans; Male; Middle Aged; Outcome Assessment, Health Care; Plant Extracts; Prostatic Hyperplasia; Serenoa; Tamsulosin; Urological Agents
PubMed: 32274957
DOI: 10.1177/1557988320905407 -
Journal of Endourology Case Reports 2020Tamsulosin in a widely used drug in urology practice in treating lower urinary tract symptoms of benign prostatic hyperplasia, distal ureteral stones, and ureteral...
Tamsulosin in a widely used drug in urology practice in treating lower urinary tract symptoms of benign prostatic hyperplasia, distal ureteral stones, and ureteral stent-related symptoms. Ischemic priapism is a rare but serious adverse effect of tamsulosin. We report two cases of tamsulosin-induced priapism and reviewed available literature citing priapism as a complication of tamsulosin. We also reviewed the U.S. Food and Drug Administration Adverse Event Reporting System (FAERS) database to identify reported cases of tamsulosin-induced priapism. First patient was a 61-year-old African American male with paraplegia of 30-year duration. He developed priapism after taking first dose of tamsulosin for lower urinary tract symptoms. He presented with 18 hours of painful erection and was treated with aspiration and irrigation, followed by phenylephrine injection. The patient maintained potency after treatment. The second patient was a 24-year-old male who received tamsulosin in the emergency department as medical expulsive therapy for 11 mm distal ureteral stone. Since he had intractable pain, he underwent emergency primary ureteroscopy with laser lithotripsy as definitive treatment of his ureteral calculus. He developed intraoperative priapism that subsided postoperatively. However, he was discharged with tamsulosin to reduce stent-related urinary symptoms. He returned back to the emergency department after 3 days with persistent priapism for 3 days and needed penoscrotal corporeal decompression to treat his priapism. At 6 weeks follow-up visit, the patient has lost his potency. Although there were only 4 case reports on review of the literature, we were able to identify 46 cases reported in the U.S. FAERS database. Priapism can be an adverse reaction to tamsulosin. Providers and patients should be aware about this complication to ensure early seeking of management to avoid devastating outcomes, particularly in young patients when tamsulosin is given as medical expulsive therapy for ureteral stone and stent-related symptoms.
PubMed: 33102720
DOI: 10.1089/cren.2019.0157 -
Therapeutic Advances in Urology Feb 2016Despite their multifactorial etiology, male lower urinary tract symptoms (LUTS) have been traditionally associated with benign prostatic enlargement (BPE) because of... (Review)
Review
Despite their multifactorial etiology, male lower urinary tract symptoms (LUTS) have been traditionally associated with benign prostatic enlargement (BPE) because of benign prostatic hyperplasia (BPH). Several pharmaceutical therapies have been used to manage LUTS, with α1-adrenergic receptor antagonists (α1-blockers) and inhibitors of 5α-reductase (5α-RIs) representing the most commonly prescribed agents currently in use for LUTS treatment. Due to their different modes of action, combined use of α1-blockers and 5α-RIs has been proven to offer more optimal control of symptoms and better associated quality of life, even though higher rates of adverse events have been shown. Following previous studies on the separate administration of dutasteride and tamsulosin, a fixed-dose combination capsule of tamsulosin 0.4 mg and dutasteride 0.5 mg has been approved and released for clinical use in men with BPH. The present review aims to discuss the rationale behind the combined use of tamsulosin and dutasteride for treating male LUTS, and to present the available data on the role of combination therapy in the management of BPH-related symptoms in terms of efficacy and safety. Special attention is given to the impact of combination treatment on the prevention of clinical progression of BPH. Cost-effectiveness of fixed-dose combination and patients' adherence to treatment are also discussed.
PubMed: 26834837
DOI: 10.1177/1756287215607419 -
Surgery Nov 2018Tamsulosin, an α-adrenergic receptor inhibitor, is prescribed to treat benign prostatic hyperplasia in men >60 years of age, the same demographic most susceptible to...
BACKGROUND
Tamsulosin, an α-adrenergic receptor inhibitor, is prescribed to treat benign prostatic hyperplasia in men >60 years of age, the same demographic most susceptible to abdominal aortic aneurysm. The goal of this study was to investigate the effect of tamsulosin on abdominal aortic aneurysm pathogenesis.
METHODS
Abdominal aortic aneurysms were induced in WT C57BL/6 male mice (n = 9-18/group), using an established topical elastase abdominal aortic aneurysm model. Osmotic pumps were implanted in mice 5 days before operation to create the model, administering either low dose (0.125 µg/day tamsulosin), high dose (0.250µg/day tamsulosin), or vehicle treatments with and without topical application of elastase. Blood pressures were measured preoperatively and on postoperative days 0, 3, 7, and 14. On postoperative day 14, aortic diameter was measured before harvest. Sample aortas were prepared for histology and cytokine analysis.
RESULTS
Measurements of systolic blood pressure did not differ between groups. Mice treated with the low dose of tamsulosin and with the high dose of tamsulosin showed decreased aortic diameter compared with vehicle-treated control (93% ± 24 versus 94% ± 30 versus 132% ± 24, respectively; P = .0003, P = .0003). Cytokine analysis demonstrated downregulation of pro-inflammatory cytokines in both treatment groups compared with the control (P < .05). Histology exhibited preservation of elastin in both low- and high-dose tamsulosin-treated groups (P = .0041 and P = .0018, respectively).
CONCLUSION
Tamsulosin attenuates abdominal aortic aneurysm formation with increased preservation of elastin and decreased production of pro-inflammatory cytokines. Further studies are necessary to elucidate the mechanism by which tamsulosin attenuates abdominal aortic aneurysm pathogenesis.
Topics: Adrenergic alpha-1 Receptor Antagonists; Animals; Aorta, Abdominal; Aortic Aneurysm, Abdominal; Blood Pressure; Cytokines; Disease Models, Animal; Down-Regulation; Drug Evaluation, Preclinical; Elastin; Humans; Male; Mice; Mice, Inbred C57BL; Pancreatic Elastase; Tamsulosin; Treatment Outcome
PubMed: 30174141
DOI: 10.1016/j.surg.2018.06.036 -
Medical Archives (Sarajevo, Bosnia and... Feb 2023Following the c In the management of BPH, Tamsulosin is an example of a-adrenergic receptor blocker drug that is usually used. In addition, dutasteride is also a BPH...
The Effect of Tamsulosin, Dutasteride Monotherapy and Tamsulosin-Dutasteride Combination on Prostate Smooth Muscle Contractility in BPH Model Wistar Strain Rattus Novergicus.
BACKGROUND
Following the c In the management of BPH, Tamsulosin is an example of a-adrenergic receptor blocker drug that is usually used. In addition, dutasteride is also a BPH drug that works as a group of 5 a reductase inhibitor. However, the weakness of long-term administration of a1-adrenergic receptor antagonists can result in upregulation of prostate smooth muscle cell contractility and expression of a-adrenergic mRNA receptors, resulting in hyperactivity and supersensitivity to a-agonists.
OBJECTIVE
Our study aimed to determine the effect of long-term administration of tamsulosin, dutasteride and tamsulosin-dutasteride combination on the contractility of prostate smooth muscle cells in BPH model rats.
METHODS
This study was designed using an experimental post test only method, control group design. It measured the contractility of prostate smooth muscle cells from samples obtained from the prostatic stroma of experimental animals adult male Rattus norvegicus Wistar strain induced BPH and administered tamsulosin 1 mg/kg/day, dutasteride 0.5 mg/kg/day, and a combination of continuous administration for 1, 6 and 12 consecutive days. Data were analyzed using one way ANOVA if the data distribution was normal or Kruskall Walis if the data distribution was abnormal.
RESULT
The effect of tamsulosin, dutasteride and the combination of tamsulosin with dutasteride on prostate smooth muscle cell contractility in experimental animals Rattus norvegicus Wistar strain showed that tamsulosin administration for six days, twelve days, and the combination of tamsulosin dutasteride for one day got statistically significant different result (p=0.016; p=0.006; p=0.029) compared to the negative control group. In addition, there was a difference between the tamsulosin and dutasteride combination group for 12 days compared to tamsulosin monotherapy for 6 days and 12 days (p=0.160; p=0.010).
CONCLUSION
Continuous administration of monotherapy tamsulosin has an upregulation effect on the sixth to twelfth day. Decreased contractility of prostate smooth muscle cells occurs on the first day but will increase on the sixth to twelfth day. On the other hand, the results of our study also showed that the combination of tamsulosin and dutasteride gave the effect of reducing contractility and was most effective on day 12.
Topics: Humans; Male; Animals; Rats; Dutasteride; Tamsulosin; Prostatic Hyperplasia; Prostate; 5-alpha Reductase Inhibitors; Azasteroids; Sulfonamides; Drug Therapy, Combination; Rats, Wistar; Muscle, Smooth
PubMed: 36919125
DOI: 10.5455/medarh.2023.77.13-17 -
Urologia Internationalis 2023Urolithiasis is one of the most common diseases in the world, and at present, ureteroscopy (URS) is the first choice for its treatment. Although the effect is good,... (Meta-Analysis)
Meta-Analysis
INTRODUCTION
Urolithiasis is one of the most common diseases in the world, and at present, ureteroscopy (URS) is the first choice for its treatment. Although the effect is good, there is a risk of insertion failure of ureteroscope. Tamsulosin, as an α-receptor blocker, has the function of relaxing ureteral muscles, and can help stones to be discharged from ureteral orifice. In this study, we aimed to determine the effect of preoperative tamsulosin on ureteral navigation, operation, and safety.
METHODS
This study was conducted and reported according to the meta-analysis extension of the Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA). The PubMed and Embase databases were searched for studies. Data were extracted according to the PRISMA principles. We collected and combined randomized controlled trial and researches in reviews of preoperative tamsulosin to explore the effect of preoperative tamsulosin on ureteral navigation, operation, and safety. A data synthesis was performed using RevMan 5.4.1 software (Cochrane). Heterogeneity was mainly evaluated with I2 tests. Key metrics include: success rate of ureteral navigation, time of URS, stone-free rate, and postoperative symptoms.
RESULT
We summarized and analyzed 6 studies. We noted a statistically significant improvement in the success rate of ureteral navigation (Mantel-Haenszel [M-H], odds ratio [OR]: 3.78, 95% confidence interval [CI]: [2.34, 6.12], p < 0.01) and stone-free rate (M-H, OR: 2.25, 95% CI: [1.16, 4.36], p = 0.02) with tamsulosin preoperatively. At the same time, we also observed that postoperative fever (M-H, OR: 0.37, 95% CI: [0.16, 0.89], p = 0.03) and postoperative analgesia (M-H, OR: 0.21, 95% CI: [0.05, 0.92], p = 0.04) were also reduced because of preoperative tamsulosin.
CONCLUSION
Preoperative tamsulosin can not only increase the one-time success rate of ureteral navigation and the stone-free rate of URS but also reduce the incidence of postoperative adverse symptoms such as postoperative fever and postoperative pain.
Topics: Humans; Tamsulosin; Ureteral Calculi; Sulfonamides; Treatment Outcome; Ureter; Adrenergic alpha-Antagonists
PubMed: 36812907
DOI: 10.1159/000528889 -
Nature Communications Jun 2023The αadrenergic receptor (αAR) belongs to the family of G protein-coupled receptors that respond to adrenaline and noradrenaline. αAR is involved in smooth muscle...
The αadrenergic receptor (αAR) belongs to the family of G protein-coupled receptors that respond to adrenaline and noradrenaline. αAR is involved in smooth muscle contraction and cognitive function. Here, we present three cryo-electron microscopy structures of human αAR bound to the endogenous agonist noradrenaline, its selective agonist oxymetazoline, and the antagonist tamsulosin, with resolutions range from 2.9 Å to 3.5 Å. Our active and inactive αAR structures reveal the activation mechanism and distinct ligand binding modes for noradrenaline compared with other adrenergic receptor subtypes. In addition, we identified a nanobody that preferentially binds to the extracellular vestibule of αAR when bound to the selective agonist oxymetazoline. These results should facilitate the design of more selective therapeutic drugs targeting both orthosteric and allosteric sites in this receptor family.
Topics: Humans; Oxymetazoline; Cryoelectron Microscopy; Receptors, Adrenergic, alpha-1; Norepinephrine; Tamsulosin
PubMed: 37339967
DOI: 10.1038/s41467-023-39310-x -
Medical Archives (Sarajevo, Bosnia and... 2023The α-adrenergic receptor antagonist is the most effective medical therapy to reduce the dynamic component in patients with BPH. However, long-term administration of...
BACKGROUND
The α-adrenergic receptor antagonist is the most effective medical therapy to reduce the dynamic component in patients with BPH. However, long-term administration of receptor antagonists can cause upregulation of mRNA receptor expression, resulting in tolerance of drug effectiveness. PKC-α is involved in the process of prostate smooth muscle contraction through activation of the voltage-gated Ca2+ conducted canal, influenced by androgen hormones, especially testosterone, and has an isoform with Twist1, a transcription factor that plays a role in up-regulation of androgen receptors.
OBJECTIVE
The aim of the study was to compare the effect of long-term tamsulosin monotherapy and tamsulosin - dutasteride combination therapy in PKC-α enzyme expression in prostate stromal tissue of Rattus norvegicus rats of Wistar strain.
METHODS
Out of 80 samples of Rattus norvegicus rats were divided into 8 groups with different interventions: negative control group, positive control group, tamsulosin monotherapy administration for 1 day, 3 day, and 6 day groups, and tamsulosin - dutasteride combination therapy for 1 day, 3 day, and 6 day groups. BPH was induced with 3 mg/kg of testosterone proprionate for 3 weeks, continued with drugs administration according to intervention grouping. Prostate stromal tissue was taken and prepared for PKC-α enzyme measurement with ELISA method.
RESULTS
There was a significant difference (p<0.05) in the effect of tamsulosin monotherapy and tamsulosin-dutasteride combination therapy on the PKC-α expression. There was a strong positive relationship between the duration of tamsulosin-dutasteride combination therapy on the PKC-α expression, which means the longer the duration of the combination of tamsulosin-dutasteride combination the higher the PKC-α expression.
CONCLUSION
Administration of long-term tamsulosin - dutasteride combination therapy causes upregulation PKC-α expression more than tamsulosin only.
Topics: Animals; Male; Rats; 5-alpha Reductase Inhibitors; Azasteroids; Drug Therapy, Combination; Dutasteride; Prostate; Prostatic Hyperplasia; Rats, Wistar; Sulfonamides; Tamsulosin; Testosterone
PubMed: 38313112
DOI: 10.5455/medarh.2023.77.446-450