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A 19-question qualitative survey, sponsored by the American Foundation of Urologic Disease, was mailed April 2004 to 7500 UROs and 17,500 PCPs, with responses collected until May 2004.
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To compare the efficacy of silodosin (8 mg) vs tamsulosin (0.4 mg), as a medical expulsive therapy, in the management of distal ureteric stones (DUS) in terms of stone clearance rate and stone expulsion time.
Tamsulosin helps in clearance of upper ureteral stones after 1 month of SWL, particularly stones with size of 11 to 15 mm with less requirement of SWL sessions and analgesics.
A total of 516 patients were enrolled from 2 European open label studies that were extensions of 3 double-blind controlled studies.
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1. In this study, we examined the interaction between noradrenaline (NA) and phenylephrine (PE) with seven antagonists (prazosin, tamsulosin, phentolamine, WB-4101, 5-methylurapidil, spiperone and HV 723) in an attempt to characterize the alpha 1-adrenoceptor population of the rat isolated small mesenteric artery (SMA) preparation. 2. Six of the seven antagonists investigated produced concentration-dependent, parallel, rightward shift of the NA concentration-effect (E/[A]) curves. The exception was tamsulosin, which produced significant decrease of the upper asymptote. In the case of 5-methylurapidil and HV723, the Schild plot slope parameters were not significantly different from unity over the range of concentrations used. However, the Schild plot slopes obtained for the other antagonists were all significantly greater than unity, inconsistent with expectations for simple competitive antagonism. 3. HV723, prazosin and tamsulosin were also tested using PE as an agonist. All three antagonists produced concentration-dependent, parallel, rightward shifts of the PE curves and Schild analysis yielded slope parameters not significantly different from unity. The pKB estimates obtained for tamsulosin and prazosin were not significantly different from the pA2 values obtained when NA was used as agonist. In the case of HV723, the 95% confidence intervals for the pKB values yielded with NA and PE did not overlap (pKB = 8.80-9.13 and 8.15-8.77 for NA and PE, respectively). 4. In the absence of evidence to indicate that the steep Schild plots were due to failure to satisfy the basic criteria for quantitative analysis in a one-receptor system, we considered the possibility that the complexity was caused by an action of NA at inhibitory D1 receptors. The selective D1 receptor antagonists, SCH-23390 (10 nM), had no significant effect on the NA E/[A] control curve, but the apparent potency of 100 nM prazosin was reduced by approximately 3.5 fold. 5. This study indicates that the steep Schild plots obtained from the interaction between NA and alpha 1-adrenoceptor antagonists were due to the simultaneous activation of inhibitory D1 receptors by NA. Notwithstanding this complexity, our explanatory model of the system (see Appendix) suggests that the antagonist affinity values estimated in the absence of D1 receptor block were not significantly affected by this other action of NA. The low affinity estimate obtained for prazosin suggests that the pharmacologically-defined alpha IL-subtype operates in the SMA.
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From February to August 2012, 100 patients who were between the age group of 18-50 years, who had unilateral, uncomplicated middle or lower ureteral stones = 1cm were enrolled and they were divided into two groups. Group 1 received tamsulosin (0.4mg) daily, whereas Group 2 received silodosin (8mg) daily for a maximum period of 4 weeks. The patients were followed up weekly or biweekly with imaging studies. The primary endpoint was the stone expulsion rate and the secondary endpoints were the stone expulsion time, the rate of the interventions and the side effects.
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Of the 211 patients from six urology outpatient centres who participated in this investigation, 146 patients were evaluable. Tamsulosin 0.2 mg/day was administered orally in a nonblind design for a 1-year period. The primary efficacy parameters were improvement in the total, obstructive and irritative International Prostate Symptom Score (IPSS), measured at baseline and at weeks 12, 24, 36 and 52, and in the maximal urinary flow rate (Qmax) measured at baseline and at weeks 24 and 52. The secondary efficacy parameters were a decrease of >/=30% in IPSS, and an increase in Qmax of >/=30% from baseline. Changes in parameters between baseline and 52 weeks were assessed using Student's paired t-test.
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Thirty-seven (68.5%) and 17 (31.5%) patients were in Groups 1 and 2, respectively. The mean s/T ratios in Groups 1 and 2 increased to 0.38 ± 0.19 from 0.33 ± 0.08 (P = 0.03) and decreased to 0.54 ± 0.18 from 0.59 ± 0.1 (P = 0.17) during the 3rd month of follow-up, respectively. The treatment success rates of Groups 1 and 2 were 88.4% and 75.7%, respectively. Nine unsuccessful cases were treated with combination therapy and the treatment success was 86.6% at follow-up.
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The management of ureteral calculi has evolved over the past decades with the advent of new surgical and medical treatments. The current guidelines support conservative management as a possible approach for ureteral stones sized = 10 mm.
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Tamsulosin may have a different effect on the bladder and/or the neuronal pathways that is unrelated to ATP, so the combination of tamsulosin and solifenacin may synergistically inhibit urinary frequency after bladder stimulation.
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To investigate the effect of combination therapy with dutasteride plus tamsulosin compared with each monotherapy on patient-reported health outcomes over 4 years in men with moderate-to-severe lower urinary tract symptoms (LUTS) because of benign prostatic hyperplasia (BPH).
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To develop and validate a liquid chromatography-tandem mass spectrometric (LC-MS/MS) method for the determination of tamsulosin in dog plasma after oral administration of controlled-release tablet of tamsulosin hydrochloride, the samples and the internal standard, diphenhydramine, were extracted from dog plasma by n-hexane-dichloromethane (2 : 1), and separated on a Bonchrom XBP-C18 column using a mobile phase consisted of methanol-acetonitrile-ammonium formate (10 mmol x L(-1)) (30 : 40 : 30, v/v/v), at a flow rate of 0.4 mL x min(-1). Mass spectrometric detection was operated on a triple quadrupole tandem mass spectrometer equipped with atmospheric pressure chemical ionization (APCI) source in positive mode. Quantification was performed using selected reaction monitoring (SRM) of the transitions m/z 409 --> 228 for tamsulosin and m/z 256 --> 167 for the internal standard, respectively. The linear concentration ranges of the calibration curves for tamsulosin were 0.02 - 50 ng x mL(-1). The lower limit of quantification was 0.02 ng x mL(-1). The accuracy ranged from -2.61% to 8.82% in terms of relative error (RE). The intra- and inter-day relative standard deviation (RSD) across three-run validations were lower than 9.72%. The method was proved to be highly sensitive, selective, and had been successfully applied to the pharmacokinetic study after an oral administration of 0.4 mg tamsulosin hydrochloride controlled release preparations to dogs.
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We have investigated the affinity and selectivity of tamsulosin and its metabolites, M1, M2, M3, M4 and AM1, at the tissue and the cloned alpha-1 adrenoceptor subtypes in the radioligand binding and the functional studies. In the radioligand binding studies, the compounds competed for [3H]prazosin binding to the rat liver and kidney alpha-1 adrenoceptors, with the rank order of potency tamsulosin approximately M4 > M1 > M2 approximately M3 > > AM1 with the latter having a negligible affinity. All compounds differentiated cloned alpha-1 adrenoceptor subtypes with the rank order of potency of alpha-1A > or = alpha-1D > alpha-1B, except for M4 which had the highest affinity for the alpha-1D adrenoceptor. The compounds also concentration-dependently antagonized phenylephrine-induced contractions in the rabbit aorta and prostate. The resulting apparent pA2 values were very similar to those at the cloned rat alpha-1A adrenoceptor. We conclude that most tamsulosin metabolites are high potency antagonists at the alpha-1 adrenoceptors and retain the alpha-1A over the alpha-1B adrenoceptor selectivity of tamsulosin.
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The study clarified that 5 characteristic symptom patterns exist by cluster analysis of IPSS in male patients with LUTS. Tamsulosin improved various symptoms and QOL in each symptom group. The study reports many male patients with LUTS being satisfied with monotherapy using tamsulosin and suggests the usefulness of α1-blockers as a drug of first choice.
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We wanted to test whether phytotherapeutic agents used in the treatment of lower urinary tract symptoms have alpha1-adrenoceptor antagonistic properties in vitro.
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Male LUTS/OAB (≥50 years) patients who had a total International Prostate Symptom Score (I-PSS) of ≥12, I-PSS urgency-related question of ≥2, and quality of life (QoL) of ≥3 points were enrolled. Patients who complained of storage symptoms as the most bothersome were included in the 'storage' group. Patients who complained of voiding symptoms as the most bothersome were included in the 'voiding' group. The change in the I-PSS was compared between the two groups 4 weeks after commencing treatment.
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After 3 months of treatment tamsulosin significantly improved the mean total I-PSS compared to baseline. After 6 months, the mean total I-PSS was reduced by 11.0 points from a baseline score of 20.3 (> 50% reduction). Tamsulosin also significantly improved the mean total BSIA score and the mean Total Mental Health Rate. These observations were confirmed by the urologists' assessment of the patient's condition: an increase of more than 50% of patients with no or mild voiding and filling LUTS and an increase of 45% of patients with no or only a small interference of their LUTS with daily life activities. The withdrawal rate due to adverse reactions was 2.4%.
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Benign prostate hyperplasia (BPH) occurs in up to 50% of men by age 50, and the incidence increases with age. This common clinical problem is diagnosed by history, including the International Prostate Symptom Score (IPSS) questionnaire, and physical examination by digital rectal examination (DRE). Initial management for BPH includes lifestyle modification, and smooth muscle relaxant alpha blocker therapy. Alpha blockers usually take effect quickly within 3-5 days, and have minimal side effects. Current commonly used alpha blockers include the selective alpha blockers tamsulosin (Flomax), alfusosin (Xatral), and silodosin (Rapaflo). For patients with larger prostates, the 5-alpha reductase inhibitor class (finasteride (Proscar) and dutasteride (Avodart)) work effectively to shrink prostate stroma resulting in improved voiding. The 5-ARI class of drugs, in addition to reducing prostate size, also reduce the need for future BPH-related surgery, and reduce the risk of future urinary retention. Drugs from the phosphodiesterase-5 (PDE-5) inhibitor class may now be considered for treating BPH. Once daily 5 mg tadalafil has been shown to improve BPH-related symptoms and is currently approved to treat patients with BPH. Referral to a urologist can be considered for patients with a rising prostate-specific antigen (PSA), especially while on 5-ARI, failure of urinary symptom control despite maximal medical therapy, suspicion of prostate cancer, hematuria, recurrent urinary infections, urinary retention, or renal failure. Currently the primary care physician is armed with multiple treatment options to effectively treat men with symptomatic BPH.
To investigate the effects of dutasteride on serum testosterone level and body mass index (BMI) in men who received medical therapy for benign prostatic hyperplasia (BPH).
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Computer simulations of the human alpha(1d)-adrenergic receptor (alpha(1d)-AR) based on the crystal structure of rhodopsin have been combined with experimental site-directed mutagenesis to investigate the role of residues in the transmembrane domains in antagonist binding. Our results indicate that the amino acids Asp176 in the third transmembrane domain (TMD), Glu237 in TMD IV, and Ser258 in TMD V of alpha(1d)-AR were directly involved in prazosin and tamsulosin binding. The Asp176Ala mutant did not exhibit any affinity for [(3)H]prazosin and neither did it show agonist-stimulated inositol phosphates (IP) formation. On the other hand, the Glu237Ala and Ser258Ala mutant alpha(1d)-AR showed increased binding affinity for [(3)H]prazosin. Competition binding experiments showed that prazosin affinity had increased to 5-fold and 3-fold in the Glu237Ala and Ser258Ala mutants, respectively, versus wild-type; and tamsulosin affinity only increased in the Ser258Ala mutant (2-fold vs wild-type). It seems that these two residues constrain the receptor by interaction with other residues and this disruption of the interaction increased the receptor's binding affinity towards antagonists. However, the Glu237Ala and Ser258Ala mutant receptors retained the ability to stimulate the formation of myo-[(3)H]inositol but had activities lower than that of the wild-type receptor. The present results provide direct evidence that these amino acid residues are responsible for the interactions between alpha(1d)-AR and the radioligand [(3)H]prazosin as well as tamsulosin.
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This randomized, double-blind, parallel-design trial compared the efficacy and safety of tamsulosin and alfuzosin in 76 men with symptomatic benign prostatic hyperplasia. Patients were randomized to receive 0.2 mg tamsulosin once daily orally (n = 40) or 10 mg alfuzosin once daily orally (n = 36), and changes in the International Prostate Symptom Score (IPSS), maximal urinary flow rate (Qmax) and the Danish prostatic symptom sexual function score and morbidity rates were compared after 8 weeks of treatment. There was a mean overall decrease in the IPSS, with no significant difference between the treatment groups. There was an overall increase in the Qmax, which again was similar in the two groups. There was no significant change in the sexual function scores in either group. The incidence of adverse events was similar for tamsulosin (25%) and alfuzosin (19.4%) therapy. In conclusion, both treatment regimens similarly improved the IPSS and Qmax, did not alter sexual function and were well tolerated.
SJC can effectively relieve anxiety, depression and other psychological problems in type III B prostatitis patients with sexual dysfunction and improve their clinical symptoms as well.
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Long-term tamsulosin therapy is safe, well tolerated and improvements in urinary flow and symptoms are maintained for at least 60 weeks of treatment.
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Men with smaller prostates and moderate-to-severe LUTS including OAB symptoms benefited from tolterodine ER. Therapy with tolterodine ER+tamsulosin was effective regardless of prostate size. Tolterodine ER, with or without tamsulosin, was well tolerated and not associated with increased incidence of AUR.
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The study enrolled 271 patients and eventually only 249 (123 in TG and 126 in CG) completed the study. The overall stone free rate was 73.5%: 78.0% in TG and 69.0% in CG (p = 0.108). In TG, 8.1% of patients experienced at least one episode of acute renal/ureteral colic compared with 19.8% of controls (p = 0.008). The mean cumulative analgesia dosage per subject was 313 mg in TG and 346 mg in CG (p < 0.001). Overall, 14 patients developed steinstrasse and 6 of them (all in CG) needed urgent intervention (p = 0.031).