ABSTRACT
PURPOSE: To investigate the efficacy and safety of naftopidil for benign prostatic hyperplasia (BPH) patients, mainly focusing on changes in blood pressure (BP). MATERIALS AND METHODS: Of a total of 118 patients, 90 normotensive (NT) and 28 hypertensive (HT) patients were randomly assigned to be treated with naftopidil 50 mg or 75 mg for 12 weeks, once-daily. Safety and efficacy were assessed by analyzing changes from baseline in systolic/diastolic BP and total International Prostate Symptom Score (IPSS) at 4 and 12 weeks. Adverse events (AEs), obstructive/irritative subscores, quality of life (QoL) score, maximum urinary flow rate (Qmax), and benefit, satisfaction with treatment, and willingness to continue treatment (BSW) questionnaire were also analyzed. RESULTS: Naftopidil treatment decreased mean systolic BP by 18.7 mm Hg for the HT 50 mg group (p86% of all patients agreed to continue their current medications. CONCLUSION: Our results suggest that naftopidil treatment in BPH patients with hypertension allows for optimal management of BP within the normal range.
Subject(s)
Humans , Blood Pressure , Hypertension , Prospective Studies , Prostate , Prostatic Hyperplasia , Quality of Life , Reference Values , Treatment OutcomeABSTRACT
OBJECTIVE To investigate the blocking activities of a series of potential α1-adrenoceptor (α1-AR) antagonists (Compounds B1 -B9) on α1-AR.METHODS ① A series of potential α1-adrenoceptor (α1-AR) antagonists,indolylpiperidine derivative (IPD) and Compounds B1 -B9,with indolylpiperidine moiety and different substitutes were synthesized through the coupling of indolylpiperidine and piperazine derivatives.② Inotropic responses experiment was used to examine blocking effects of IPD and Compounds B1 - B9 in isolated rat atria by phenylephrine (PE) stimulation.③ Blocking effect of IPD and Compounds B1 - B9 on phosphorylation level of extracellular signal-regulated kinase (ERK) in PE treated HEK293 cells was tested by Western blotting.RESULTS ① Potential α1-adrenoceptor (α1-AR) antagonists with indolylpiperidine moiety and different substitutes were synthesized successfully.② PE caused a dose-dependent inotropic response which was inhibited by pre-incubation of phentolamine (Phen),a non-selective α1-AR antagonist,IPD and Compounds B1,B3,B4,B7,B8 and B9,respectively; IPD and Compounds B4 and B8 caused an obvious rightward shift of inotropic response-curve,the pA2 values for IPD and Compounds B4 and B8 were 6.72 ± 0.21,6.86 ± 0.29 and 6.67 ± 0.19,respectively.③ Phosphorylation level of ERK1/2 was inhibited by pre-incubation with Compounds B1,B2,B3,B5,B6,B7,B8 and B9 or IPD in PE treated α1A-AR stably expressed HEK293 cells; PE-stimulated phosphorylation level of ERK1/2 was inhibited by pre-incubation with Compounds B2,B4,B7 or B8 in α1B-AR stably expressed HEK293 cells.CONCLUSION Compound B4 has a selective blocking activity on α1B-AR,and Compounds B1,B3,B5,B6 and B9 or IPD have a selective blocking activity on the phosphorylation level of ERK1/2.
ABSTRACT
PURPOSE: The aim of this study was to assess the efficacy and safety of tamsulosin, 0.2mg/day on sexual function in Korean BPH patients. Patients and Methods: 116 patients (mean age: 60 yrs) with BPH were enrolled in this study and 0.2mg of tamsulosin was administrated every night for 3 months. Primary efficacy was evaluated with changes of IIEF and GEQ. Secondary efficacy parameters were changes of IPSS and QoL, uroflowmetry, changes of total IIEF and IIEF domain score according to the severity of IPSS, and retrograde ejaculation. RESULTS: Before treatment, patients of moderate IPSS (8-19) and severe IPSS (20-35) were 56% and 44% and QoL3 were 33.6% and 66.4%. In primary efficacy evaluation, total IIEF score was significantly increased from 37.0+/- 18.2 to 40.5+/- 18.9 (p<0.01). All domains of IIEF except orgasmic function were significantly improved. GEQ showed improvement of erection in 34.4% and intercourse ability in 30.1%. In secondary efficacy evaluation, IPSS was significantly decreased from 18.4+/- 6.9 to 12.9+/- 6.7 (p<0.01) and QoL was significantly improved from 3.8+/- 1.1 to 2.7+/- 1.4 (p<0.01). Qmax significantly increased from 14.2+/- 8.3 to 16.5+/- 11.3 ml/sec (p<0.01). Total IIEF score and EF domain score were significantly improved from 36.8+/- 18.5 to 41.8+/- 19.1 (p<0.01) and from 13.0+/- 7.1 to 14.7+/- 7.9 (p<0.01) in patients of moderate IPSS but no improvement in severe patients. Retrograde ejaculation occurred in 2 patients (2%). No serious adverse reactions were observed. CONCLUSIONS: Tamsulosin, 0.2mg/day was effective and safe dose for the improvement of LUTS and sexual function for Korean BPH/LUTS patients.
Subject(s)
Humans , Male , Ejaculation , Orgasm , Prospective Studies , SulfonamidesABSTRACT
Objective To study peripheral blood lymphocytic ?-adrenoceptor(?-AR) densities and ?_1-adrenoceptor gene(?_1-AR mRNA) expression levels in patients with heart failure,to investigate the influences of different ?-adrenoceptor antagonists in ?-AR densities and ?_1-AR mRNA expression levels.Methods 104 cases of patients with heart failure were randomly divided into non-?-adrenoceptor antagonist group(35 cases),metoprolol group(34 cases) and carvedilol group(35 cases),we repeatly determined the ?-AR densities and ?_1-AR mRNA expression levels after two-month therapy.Results The ?-AR densities and ?_1-AR mRNA expression levels in heart failure group reduced significantly compared to these in normal persons(P0.05).After two-month therapy,?-AR densities and ?_1-AR mRNA expression levels in metoprolol group were significantly higher than those in carvendilol group and non-?-adrenoceptor antagonist group(P0.05).Conclusions The peripheral blood lymphocytic ?-AR densities and ?_1-AR mRNA expression level down-regulates in heart failure,which correlate with the severity of heart failure but etiological factors.Metoprolol can up-regulate the ?-AR densities and ?_1-AR mRNA expression level,whereas carvedilol has no such effects.