PURPOSE: Medical therapy with an alpha-blocker is commonly used primarily in patients with benign prostatic hyperplasia (BPH). However, the efficacy of the alpha-blocker is still questionable in reference to a small prostate, with the size of 30g or less. We reviewed 117 patients who had been taken the alpha-blocker for the management of BPH, and the results were analyzed according to the prostatic size. MATERIALS AND METHODS: One hundred seventeen patients were divided into the two following groups: Group I consisted of 57 patients with a BPH of under 30g and Group II consisted of 60 patients with a BPH of over 30g. Both groups were evaluated for the international prostate symptom score, urine flow rate, and residual urine volume before and 3 months after receiving medical therapy with tamsulosin. RESULTS: The success rate after medical therapy was similar in both groups, and all components were significantly improved after 3 months. The improvement rate of the urine flow rate was more significant in group II than group I. CONCLUSIONS: According to several objective results and the preference of patients for this treatment, medical therapy with the alpha-blocker could be also available in patients with BPH of under 30g.
Adrenergic alpha-Antagonists ; Humans ; Prostate ; Prostatic Hyperplasia*

PURPOSE: The purpose of this study was to investigate the pro-erectile potential of various urethral alpha blockers using pharmacological or electrical induction of erection in anesthesized rats. MATERIALS AND METHODS: To evaluate the influence on centrally mediated erection, intravenous administeration of terazosin, doxazosin(3, 10, 30microgram/kg), and tamsulosin (0.3, 1, 3microgram/kg), followed by submaximal subcutaneous apomorphine(50microgram/kg) administration, mean arterial pressure(MAP) and intracavernosal pressure(ICP) were recorded over 30 minutes in male anesthesized rats. The time to first response, peaks within 30 minutes, maximal ICP, area under the curve, percentage of ICP/MAP were compared. To evaluate the influence on peripherally induced erections, various doses of alpha antagonists and submaximal cavernous nerve stimulation(0.5ms, 2V, 10Hz) were combined. The ICP increase and ICP/MAP percentage were also compared. RESULTS: Although various dose response relationships were shown, all three alpha blockers enhanced erectile activity triggered by apomorphine. In terms of time to first response and peaks within 30 minutes, the proerectile effects of terazosin was most prominent whereas those of tamsulosin was minimal, requiring larger doses. In combining with cavernous nerve stimulation, doxazosin and tamsulosin showed moderate proerectile activity, but the highest dose of terazosin was required to enhance ICP increase induced by cavernous nerve stimulation. Despite their pressure lowering effects, all tested alpha adrenergic blockers significantly enhanced the ICP/MAP percentage. CONCLUSIONS: The present finding clearly indicated that alpha 1 selective antagonists can enhance erectile capacity when combined with central or peripheral stimuli for erection.
Adrenergic alpha-Antagonists ; Adrenergic Antagonists ; Animals ; Apomorphine ; Doxazosin ; Humans ; Male ; Models, Animal* ; Rats*

Hypertension is a rare but well-documented manifestation of neuroblastoma. This is a case in which a hypertensive 8 month-old male with a large left adrenal mass was diagnosed as pheochromocytoma and prepared for surgery with alpha adrenergic blockers and beta adrenergic blockers. Vital signs prior to induction of anesthesia and during surgery also mimicked pheochromocytoma but pathologic examinations revealed neuroblastoma. Laboratory findings also supported pheochromocytoma taking into account the fact that hypertension is rare in neuroblastomas.
Adrenergic alpha-Antagonists ; Adrenergic beta-Antagonists ; Anesthesia ; Child* ; Humans ; Hypertension* ; Infant ; Male ; Neuroblastoma* ; Pheochromocytoma ; Vital Signs

PURPOSE: Using meta-analysis, the study's aim was to evaluate the efficacy of tamsulosin, an alpha-blocker, in the treatment of ureteral stones with or without shockwave lithotripsy (SWL) in Korean patients. MATERIALS AND METHODS: Relevant randomized controlled studies published through June 2011 were identified in a search of MEDLINE, KoreaMed, and the Korean Medical Database. No language restriction was applied. Only randomized controlled trials conducted with Korean patients were eligible for the analysis. The primary outcome assessed was the stone clearance rate. Two reviewers independently assessed the quality of the study and extracted the data. Meta-analysis was conducted by using R, version 2.13.0. RESULTS: A total of 6 articles were selected as being suitable for evaluation. Pooling of the trials demonstrated a 43% higher expulsion rate for tamsulosin treatment compared to a control group (risk ratio [RR], 1.43; 95% confidence interval [CI]: 1.24 to 1.65). Similar results were obtained in all subgroup analyses according to stone location (upper: RR, 1.31; 95% CI, 1.02 to 1.68, lower: RR, 1.50; 95% CI, 1.20 to 1.88) or concomitant SWL (yes: RR, 1.38; 95% CI, 1.14 to 1.68, no: RR, 1.48; 95% CI, 1.21 to 1.83). CONCLUSIONS: This meta-analysis of randomized controlled studies provides a high level of evidence supporting the suggestion that treatment with tamsulosin augments the stone expulsion rate for ureter stones with or without SWL in a Korean population. However, a high-quality, large-scale, multicenter, randomized controlled trial is warranted to fully support this hypothesis.
Adrenergic alpha-Antagonists ; Humans ; Lithotripsy ; Sulfonamides ; Ureter ; Ureteral Calculi

alpha1-adrenoceptor antagonists are first-line agents for the treatment of lower urinary tract symptoms suggestive of benign prostatic hyperplasia, while their adverse effects on sexual function are reported frequently in recent years, especially the induction of ejaculatory dysfunction. This review presents the distribution of alpha 1-adrenoceptors in the male genital system and the relationship of alpha1-adrenoceptors with ejaculatory function. It also highlights the interesting phenomenon of ejaculatory dysfunction related to these drugs and its possible mechanism, with the intention to provide some essential clues for further research on this problem as well as some references to safer use of these drugs in clinical settings.
Adrenergic alpha-1 Receptor Antagonists ; Adrenergic alpha-Antagonists ; adverse effects ; pharmacology ; Ejaculation ; physiology ; Erectile Dysfunction ; chemically induced ; physiopathology ; Humans ; Male ; Receptors, Adrenergic, alpha-1 ; physiology

Benign prostatic hyperplasia (BPH) is a common senile disease, and its main clinical manifestation is lower urinary tract symptom (LUTS), which has long been afflicting old male patients. Previous study showed that alpha1-receptor in the prostate was involved in the development of LUTS. At present, alpha1-receptor blocker is generally accepted as a choice drug for treating BPH and relieving LUTS. The article reviews the tissue distribution of alpha1-receptor and clinical application of alpha1-receptor blocker.
Adrenergic alpha-1 Receptor Antagonists ; Adrenergic alpha-Antagonists ; adverse effects ; pharmacokinetics ; therapeutic use ; Humans ; Male ; Prostatic Hyperplasia ; drug therapy ; Receptors, Adrenergic, alpha-1 ; analysis

PURPOSE: The medical treatment for benign prostatic hyperplasia (BPH) had recently been directed at preventing the progression of BPH, which reduces the risk of acute urinary retention (AUR) and BPH-related surgery. This study compared the long-term effectiveness of administering alpha- adrenergic blocker (alpha-blocker) and finasteride, a 5-alpha reductase inhibitor (5ARI), for treating BPH to prevent AUR and BPH-related surgery in real-life clinical practice. MATERIALS AND METHODS: This retrospective study enrolled 166 BPH patients who were treated at our hospital with the alpha-blockers doxazosin, terazosin, prazosin and alfuzosin, or tamsulosin and 5ARI as their first BPH treatment between January 1997 and December 1997, and these treatments lasted at least 12 months. Using follow-up data that was obtained at up to 7 years after treatment, we calculated the AUR and BPH-related surgery percentages in the alpha-blocker only group and in the combination group. RESULTS: During the study period, 17 of 110 patients (15.5%) in the alpha- blocker only group and 4 of 56 patients (7.1%) in the combination group experienced AUR. BPH-related surgery was performed on 10 of 110 patients (9.1%) in the alpha-blocker only group and surgery was performed on 1 of 56 patients (1.8%) in the combination group. Among them, 5 patients in the alpha-blocker only group and 1 patient in the combination group received surgery for AUR, and another 5 patients in the alpha-blocker only group showed insufficient therapeutic response. CONCLUSIONS: Real-life clinical practice showed that long-term combination treatment with alpha-blockers and 5ARI reduced the risk of the progression of BPH, such as AUR or BPH-related surgery, as compared with alpha-blocker-only treatment.
Adrenergic alpha-Antagonists ; Adrenergic Antagonists ; Doxazosin ; Finasteride ; Follow-Up Studies ; Humans ; Oxidoreductases* ; Prazosin ; Prostatic Hyperplasia* ; Retrospective Studies ; Urinary Retention*

PURPOSE: The medical treatment for benign prostatic hyperplasia (BPH) had recently been directed at preventing the progression of BPH, which reduces the risk of acute urinary retention (AUR) and BPH-related surgery. This study compared the long-term effectiveness of administering alpha- adrenergic blocker (alpha-blocker) and finasteride, a 5-alpha reductase inhibitor (5ARI), for treating BPH to prevent AUR and BPH-related surgery in real-life clinical practice. MATERIALS AND METHODS: This retrospective study enrolled 166 BPH patients who were treated at our hospital with the alpha-blockers doxazosin, terazosin, prazosin and alfuzosin, or tamsulosin and 5ARI as their first BPH treatment between January 1997 and December 1997, and these treatments lasted at least 12 months. Using follow-up data that was obtained at up to 7 years after treatment, we calculated the AUR and BPH-related surgery percentages in the alpha-blocker only group and in the combination group. RESULTS: During the study period, 17 of 110 patients (15.5%) in the alpha- blocker only group and 4 of 56 patients (7.1%) in the combination group experienced AUR. BPH-related surgery was performed on 10 of 110 patients (9.1%) in the alpha-blocker only group and surgery was performed on 1 of 56 patients (1.8%) in the combination group. Among them, 5 patients in the alpha-blocker only group and 1 patient in the combination group received surgery for AUR, and another 5 patients in the alpha-blocker only group showed insufficient therapeutic response. CONCLUSIONS: Real-life clinical practice showed that long-term combination treatment with alpha-blockers and 5ARI reduced the risk of the progression of BPH, such as AUR or BPH-related surgery, as compared with alpha-blocker-only treatment.
Adrenergic alpha-Antagonists ; Adrenergic Antagonists ; Doxazosin ; Finasteride ; Follow-Up Studies ; Humans ; Oxidoreductases* ; Prazosin ; Prostatic Hyperplasia* ; Retrospective Studies ; Urinary Retention*

PURPOSE: To evaluate the efficacy of an alpha-1 adrenergic receptor (α1-AR) blocker for the treatment of female voiding dysfunction (FVD) through a pressure-flow study. METHODS: This was a randomized, double-blind, placebo-controlled trial. Women aged ≥18 years with voiding symptoms, as defined by an American Urological Association symptom score (AUA-SS) ≥15 and a maximum flow rate (Qmax) < 15 mL/sec with a voided volume of >100 mL and/or a postvoid residual (PVR) volume >150 mL, were randomly allocated to either the alfuzosin or placebo group. After 8 weeks of treatment, changes in the AUA-SS, Bristol female lower urinary tract symptoms (BFLUTS) questionnaire, Qmax/PVR, and voiding diary were compared between groups. Patients’ satisfaction with the treatment was compared. Patients were categorized into 3 groups according to the Blaivas-Groutz bladder outlet obstruction (BOO) nomogram: none, mild, and moderate to severe. Subgroup comparisons were also made. RESULTS: Of a total of 187 women, 154 (79 alfuzosin, 75 placebo) were included in the analysis. After 8 weeks of treatment, the AUA-SS decreased by 7.0 in the alfuzosin group and by 8.0 in the placebo group. Changes in AUA-SS subscores, BFLUTS (except the I-sum), the voiding diary, and Qmax/PVR were not significantly different between groups. Approximately 54% of the alfuzosin group and 62% of the placebo group were satisfied with the treatment. No significant difference was observed between groups according to the presence or grade of BOO. CONCLUSIONS: Alfuzosin might not be more effective than placebo for treating FVD. The presence or the grade of BOO did not affect the results. A further study with sufficient power is needed to determine the efficacy of α1-AR blockers for the treatment of FVD.
Adrenergic alpha-Antagonists ; Female ; Humans ; Lower Urinary Tract Symptoms ; Nomograms ; Receptors, Adrenergic, alpha-1 ; Urinary Bladder Neck Obstruction ; Urodynamics

AIMTo establish new methods for the chiral separation and preparation of three new drugs, alfuzosin, terazosin and doxazosin.

METHODSBy optimizing factors which affect the chiral separation, modifier of solvent, chiral additive, pH of mobile phase, modifier of organic base and stationary phase, the optimum condition for chiral separation were selected. The preparation of enantiomers was carried out on semi-preparative reverse phase column (7.8 mm x 250 mm C4 5 microns). Acetonitrile-water modified by the addition of carboxymethyl-beta-cyclodextrin (2%-5%, w/v) was applied as chiral mobile phase.

RESULTSThe enantiomers of three new drugs were base-line-separated and milligram-scale samples of enantiomer were obtained.

CONCLUSIONThe newly established method can be used in research and development of the enantiomers of three new drugs.

Adrenergic alpha-1 Receptor Antagonists ; Adrenergic alpha-Antagonists ; isolation & purification ; Chromatography, High Pressure Liquid ; methods ; Doxazosin ; isolation & purification ; Molecular Structure ; Prazosin ; analogs & derivatives ; isolation & purification ; Quinazolines ; isolation & purification