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*

The clinical effect of prazosin, an alpha-1-receptor blocking agent, was studied in 31 patients with benign prostatic hypertrophy. The daily dose of 1.5-6 mg of prazosin was given for 2 weeks to 3 months. The efficacy was assessed by using uroflowmetry calculated from maximum flow rate, average flow rate and residual urine volume. The result revealed significant improvement of day time frequency, night time frequency (p<0.05) and maximum and average flow rate (p<0.05). It was suspected that prazosin was the valuable alpha-1-receptor blocker for benign prostatic hypertrophy and worth while to initiate medical treatment before undergoing any surgical intervention or when surgery is contraindicated.
Humans ; Prazosin* ; Prostatic Hyperplasia*

Prazosin, a selective alpha-1-adrenoreceptor blocker, was used in a double-blind fashion to evaluate its efficacy in 20 men with chronic nonbacterial prostatitis who have no improvement with conventional treatments for 4 weeks. When the drug was compared to placebo therapy, obstructive and irritative voiding sympment with conventional treatments for 4 weeks. When the drug was compared to placebo therapy, obstructive and irritative voiding symptoms were improved (p<0.05). No side effects were noted except one who had indigestion.
Dyspepsia ; Humans ; Male ; Prazosin* ; Prostatitis*

The therapeutic effects of prazosin hydrochloride alone and in combination with diuretic and/or beta-blocker in 41 patients with essential hypertension were evaluated. The results were as follows: 1) Of 28 patients treated with prazosin alone, 18(64.2%) achieved normalization of blood pressure and 7(25.0%) had good response of treatment. 2) Of 16 patients, with inadequate control on initial treatment, treated with prazosin in combination with diuretic and beta-blocker, 14(87.5%) achieved normalization of blood pressure. 3) After therapy with prazosin alone, the mean blood pressure reduced 25/16mmHg(p<0.05/p<0.01). 4) After addition of diuretic or beta-blocker in 6 patients receiving prazosin alone with inadequate response, the mean blood pressure reduced 31/13mmHg(p<0.01/p<0.01). 5) After addition of prazosin in 10 patients receiving diuretic alone or diuretic and beta-blocker but with inadequate control, the mean blood pressure reduced 32/14 mmHg(p<0.01/p<0.01). 6) The side effects were noted in 10 patients(25.0%). The most popular one was dizziness(17.5%), and the next was headache(10.0%).
Blood Pressure ; Humans ; Hypertension* ; Prazosin*

PURPOSE: Our experiments were done to determine the effects of alpha-1-adrenergic antagonists which have been commonly used in the treatment of BPH against the partially obstructed detrusor smooth muscle using in-vitro muscle strip study of female rat bladder. MATERIALS AND METHODS: Partial obstruction was created by means of partial ligation of the proximal urethra in 15 female Sprague-Dawley rats. After 6 weeks of obstruction, 1x0.5cm sized each bladder smooth muscle strip was stimulated by field stimulation(FS),(1-32Hz) and bethanechol administration(10(-7)-10(-4)M). After the control stimulations, each strip was pre-treated with doxazosin, tamsulosin, prazosin and atropine for 30 minutes, and then same stimulations were repeated. Seperate strip was pre-treated by propranolol for 30 minutes, and then was stimulated by norepinephrine(10(-4)M) or phenylephrine(10(-4)M). RESULTS: After the administration of doxazosin, percent decreases of maximal tension developed by FS was significantly greater in obstructed(26-50% of the control) than in normal rats(0-12% of the control)(p<0.05). Field stimulated tension were inhibited more in normal(32-40%) than in obstructed rats(p<0.05, 1-32Hz) after the administration of prazosin. Atropine inhibited field stimulated tension to a greater degree in normal(73-63%) than in obstructed(27-43%) rats(p<0.01, 1-32Hz). Complete inhibitory effects of atropine against bethanechol stimulation(10(-7)-10(-4)M) was achieved at 10(-5)M in normal rats. In obstructed rats, complete blockage was achieved at 10-4M of bethanechol. Norepinephrine decreased basal tension both in normal and obstructed rats. After pre-treatment of propranolol, phenylephrine and norepinephrine did not show any increase of basal tension. CONCLUSIONS: Our results suggest that changes of adrenoceptors may be the underlying cause of bladder instability secondary to outflow obstruction as evidenced by significant inhibition of the tension of the detrusor muscle by alpha-1-adrenoceptor blocker(doxazosin but not by tamsulosin) only in obstructed rat bladder. These results also suggest that non-cholinergic components of bladder contraction are much more in obstructed than in normal bladder. It also can be said that doxazosin may have additional effects against bladder instability caused by BPH.
Animals ; Atropine ; Bethanechol ; Doxazosin ; Female ; Humans ; Ligation ; Muscle, Smooth ; Norepinephrine ; Phenylephrine ; Prazosin ; Propranolol ; Rats* ; Rats, Sprague-Dawley ; Receptors, Adrenergic ; Urethra ; Urinary Bladder Neck Obstruction* ; Urinary Bladder*

PURPOSE: The role of spinal alpha1 adrenoceptors in normal micturition reflex of rat has not been known clearly yet. The purpose of this study is to elucidate the role of alpha1 adrenoceptor both at the spinal and peripheral level in mediating the micturition reflex which is induced by bladder distension in normal anesthetized rat and to compare the effects of different alpha1 adrenoceptor antagonists against the micturition reflex. MATERIALS AND METHODS: Wtih eighty female Sprague-Dawley rats(200-250gm) anesthetized with urethane, continuous cystometry was done by infusion of saline at a rate of 0.5ml/min. The following drugs were injected into femoral artery(intraarterial, i.a.) and subarachnoid space(intrathecal, i.t.) at the level of L6-S1 spinal cord segment; phentolamine, prazosin, doxazosin and tamsulosin. Cystometric parameters were analyzed before and after the drug injections; basal pressure(BP), micturition pressure(MP), bladder capacity(BC), micturition volume(MV), frequency and residual volume(RV). RESULTS: After i.a. injections of prazosin, doxazosin and tamsulosin, MP was significantly decreased. Doxazosin(i.a.), markedly increased MV, BC and RV. MP was more inhibited by doxazosin than prazosin or tamsulosin injection intraarterially. After i.a. injection of phentolamine, decrease in MP and frequency but increase in MV and BC were noted. Phentolamine(i.t.) raised BP and abolished MR followed by overflow incontinence. Prazosin(i.t.) induced marked increases in MV. Tamsulosin(i.t.) caused significant decreases in frequency but increases in BC. CONCLUSIONS: At spinal level, antagonism of micturition reflex evoked by bladder distension was more prominent by phentolamine. Inhibition of micturition reflex with alpha1 adrenoceptor blockers were greater peripherally. With these results, it could be suggested that micturition reflex evoked by volume-induced bladder distension could be modulated through alpha1 adrenoceptors at both the spinal and peripheral level. In some selected cases, alpha1 adrenoceptor agonist or antagonist can be useful for the management of lower urinary tract dysfunction
Animals ; Doxazosin ; Female ; Humans ; Negotiating ; Phentolamine ; Prazosin ; Rats* ; Rats, Sprague-Dawley ; Receptors, Adrenergic* ; Reflex* ; Spinal Cord ; Urethane ; Urinary Bladder ; Urinary Tract ; Urination*

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

The antihypertensive effect of Minizide(0.5mg prazosin hydrochloride and 0.25mg polythiazide per tablet)was evaluated in 30 patients with essential hypertension with a dosage of one tablet a day for four weeks. The results were as follows : 1) Of 30 patients treated with Minizide, 21 patients(70.0%) achieved normalization of blood pressure and 5 patients(16.7%) had good response. 2) Mean drop in systolic and diastolic pressure were 29.0mmHg and 15.9mmHg respectively in supine position(P<0.005). 3) Mean drop in systolic and diastolic pressure were 28.5mmHg and 16.2mmhg respectively in sitting position(P<0.005). 4) In 14 patients(46.7%) among 30 patients treated with Minizide adverse reactions developed. The most frequent one was postural dizziness(23.3%). 5) Most adverse reactions were transient and tolerable. However, in three patients(two patients with postural dizziness and one patient with dry mouth) the medication was stopped due to adverse reactions.
Blood Pressure ; Dizziness ; Humans ; Hypertension ; Polythiazide ; Prazosin

Three groups of patients with newely diagnosed hypertension, or with hypertension not optimally controlled by previous treatment, completed a comparative study on the effects of Dihydrochlorothiazide, propranolol, and prazosin on plasma lipids after three months therapy. The drugs showed equipotent antihypertensive effects(P<0.01). Dihydrochlorothiazide administration was associated with a significant elevation of total cholesterol(42%, P<0.05), and triglyceride(8.1%, P<0.01). Changes of HDL-C(5.1%), LDL-C(3.3%), and cholesterol ratio(-4.8%) were not significant. Propranolol administration was associated with significant elevation of total cholesterol(3.8%, P<0.05), triglyceride(14.5%, P<0.005), and LDL-C(5.6%, P<0.005). Reduction of HDL-C(-7.8%, P<0.05) and cholesterol ratio(-14.7%, p<0.005) was also statistically significant. Prazosin administration was associated with significant decrease in total cholesterol(-6.6%, P<0.005), triglycride(-9.6%, P<0.005), and LDL-C(-11.7%, P<0.005), and significant elevation of HDL-C(10.6%,P<0.005) and cholesterol ratio(24.2%, P<0.005) was noted.
Cholesterol ; Humans ; Hydrochlorothiazide* ; Hypertension* ; Plasma ; Prazosin* ; Propranolol*