Tamsulosin
(Synonyms: 坦索罗辛; (R)-(-)-YM12617 free base; LY253351 free base) 目录号 : GC39449
A potent α1-AR antagonist
Cas No.:106133-20-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Tamsulosin is a potent antagonist of α1-adrenergic receptors (α1-ARs; Ki = 0.229 nM in a radioligand binding assay).1 It is 3,800-fold selective for α1-ARs over α2-ARs (Ki = 871 nM). Tamsulosin antagonizes norepinephrine-induced contraction of isolated rabbit aorta (pA2 = 10.11) but has no effect on contraction stimulated by histamine, serotonin , angiotensin II , or prostaglandin F2α . In vivo, tamsulosin reverses the pressor effect of phenylephrine in pithed rats. It reversibly reduces fertility in male rats when administered at a dose of 0.15 mg/kg.2 Tamsulosin (1-100 μg/kg) also reduces prostatic pressure in a dose-dependent manner with minimal hypotensive effects in anesthetized dogs.3 Formulations containing tamsulosin have been used for the treatment of benign prostatic hyperplasia.
1.Honda, K., Takenaka, T., Miyata-Osawa, A., et al.Studies on YM-12617: A selective and potent antagonist of postsynaptic α1-adrenoceptorsNaunyn Schmiedebergs Arch. Pharmacol.328(3)264-272(1985) 2.Ratnasooriya, W.D., and Wadsworth, R.M.Tamsulosin, a selective alpha 1-adrenoceptor antagonist, inhibits fertility of male ratsAndrologia26(2)107-110(1994) 3.Sudoh, K., Tanaka, H., Inagaki, O., et al.Effect of tamsulosin, a novel alpha 1-adrenoceptor antagonist, on urethral pressure profile in anaesthetized dogsJ. Auton. Pharmacol.16(3)147-154(1996)
| Cas No. | 106133-20-4 | SDF | |
| 别名 | 坦索罗辛; (R)-(-)-YM12617 free base; LY253351 free base | ||
| Canonical SMILES | O=S(C1=CC(C[C@H](NCCOC2=CC=CC=C2OCC)C)=CC=C1OC)(N)=O | ||
| 分子式 | C20H28N2O5S | 分子量 | 408.51 |
| 溶解度 | DMSO: 100 mg/mL (244.79 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4479 mL | 12.2396 mL | 24.4792 mL |
| 5 mM | 0.4896 mL | 2.4479 mL | 4.8958 mL |
| 10 mM | 0.2448 mL | 1.224 mL | 2.4479 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Tadalafil Alone or in Combination with Tamsulosin for the Management for LUTS/BPH and ED
Curr Urol Rep 2020 Oct 27;21(12):56.PMID:33108544DOI:10.1007/s11934-020-01009-7.
Purpose of review: Aim of our systematic review is to evaluate and summarize the efficacy and safety of tadalafil alone or in combination with Tamsulosin for the management of lower urinary tract symptoms (LUTS)/benign prostatic hyperplasia (BPH) and erectile dysfunction (ED). Recent findings: Daily tadalafil, in particular 5 mg, according to retrieved studies, appears to be both safe and effective in treating LUTS/BPH and ED, compared with placebo or Tamsulosin. The combination of daily tadalafil 5 mg and Tamsulosin 0.4 mg allows a better improvement of LUTS compared with both the monotherapies, even if with an increased, but acceptable and tolerated, adverse events rate. After discontinuation of Tamsulosin or tadalafil in patients previously treated with their combination, the improvement of LUTS retains significance compared with baseline. Tadalafil 5 mg should be considered a primary treatment option for patients with LUTS/BPH and ED. Evidence highlight an excellent tolerability, safety, and effectiveness profile, both alone or in combination with Tamsulosin 0.4 mg. A better efficacy on LUTS relief has been observed for combination therapy, preserving also sexual function. The further switch to monotherapy allows to preserve LUTS relief, but tadalafil only is able to retain ED improvement. Our results support the evidence for a more and more tailored and modular LUTS treatment.
Effect of Tamsulosin on Passage of Symptomatic Ureteral Stones: A Randomized Clinical Trial
JAMA Intern Med 2018 Aug 1;178(8):1051-1057.PMID:29913020DOI:10.1001/jamainternmed.2018.2259.
Importance: Urinary stone disease is a common presentation in the emergency department, and α-adrenergic receptor blockers, such as Tamsulosin, are commonly used to facilitate stone passage. Objective: To determine if Tamsulosin promotes the passage of urinary stones within 28 days among emergency department patients. Design, setting, and participants: We conducted a double-blind, placebo-controlled clinical trial from 2008 to 2009 (first phase) and then from 2012 to 2016 (second phase). Participants were followed for 90 days. The first phase was conducted at a single US emergency department; the second phase was conducted at 6 US emergency departments. Adult patients were eligible to participate if they presented with a symptomatic urinary stone in the ureter less than 9 mm in diameter, as demonstrated on computed tomography. Interventions: Participants were randomized to treatment with either Tamsulosin, 0.4 mg, or matching placebo daily for 28 days. Main outcomes and measures: The primary outcome was stone passage based on visualization or capture by the study participant by day 28. Secondary outcomes included crossover to open-label Tamsulosin, time to stone passage, return to work, use of analgesic medication, hospitalization, surgical intervention, and repeated emergency department visit for urinary stones. Results: The mean age of 512 participants randomized to Tamsulosin or placebo was 40.6 years (range, 18-74 years), 139 (27.1%) were female, and 110 (22.8%) were nonwhite. The mean (SD) diameter of the urinary stones was 3.8 (1.4) mm. Four hundred ninety-seven patients were evaluated for the primary outcome. Stone passage rates were 50% in the Tamsulosin group and 47% in the placebo group (relative risk, 1.05; 95.8% CI, 0.87-1.27; P = .60), a nonsignificant difference. None of the secondary outcomes were significantly different. All analyses were performed according to the intention-to-treat principle, although patients lost to follow-up before stone passage were excluded from the analysis of final outcome. Conclusions and relevance: Tamsulosin did not significantly increase the stone passage rate compared with placebo. Our findings do not support the use of Tamsulosin for symptomatic urinary stones smaller than 9 mm. Guidelines for medical expulsive therapy for urinary stones may need to be revised. Trial registration: ClinicalTrials.gov Identifier: NCT00382265.
Tamsulosin for treatment of lower urinary tract symptoms in women: a systematic review and meta-analysis
Int J Impot Res 2017 Jul;29(4):148-156.PMID:28424499DOI:10.1038/ijir.2017.12.
Tamsulosin has been used for the off-label treatment of lower urinary tract symptoms (LUTS) in women. Over the past few years, several randomized controlled trials (RCTs) have reported the clinical effectiveness and safety of Tamsulosin for LUTS in women. Therefore, the aim of the present study was to perform a meta-analysis to evaluate the safety and efficacy of Tamsulosin in treating LUTS in women, which may resolve some of the current controversies over use of the drug and provide more reliable evidence for the use of Tamsulosin. A literature review was performed to identify all published RCTs of Tamsulosin for the treatment of LUTS in women. The search included the following databases: PUBMED, EMBASE, the Cochrane Controlled Trail Register of Controlled Trials, Chinese Biomedical Literature Database, China National Knowledge Infrastructure, Chinese Science and Technique Journals Database (VIP) and Wanfang Database. A systematic review and meta-analysis were conducted. Six RCTs studies involving 764 female participants were included in the analysis. Four out of the six RCTs compared Tamsulosin with placebo, one RCT compared Tamsulosin with prazosin and the other study compared Tamsulosin with Tamsulosin combined with tolterodine. Two RCTs evaluated total International Prostate Symptom Score (IPSS) and improved total IPSS compared with the placebo (standardized mean difference=-4.08, 95% confidence interval=-5.93 to -2.23, P<0.00001). IPSS (storage symptom score), IPSS (voiding symptom score) and quality-of-life score also showed the similar effects. In addition, Tamsulosin improved the Overactive Bladder Questionnaire score when compared with placebo in only one RCT. For urodynamic parameters, Tamsulosin improved the average flow rate and the post-void residual volume when compared with prazosin and tolterodine combined with Tamsulosin, respectively. Beyond that, the other parameters showed no significant difference between the treatment and control groups. On the basis of the present evidence, Tamsulosin is an effective treatment for the relief of LUTS in women when compared with placebo. However, the safety of the Tamsulosin remains unknown. Further, well-conducted trials that examine long-term outcomes are required.
Preoperative Tamsulosin to Prevent Postoperative Urinary Retention: A Randomized Controlled Trial
J Surg Res 2021 Jun;262:130-139.PMID:33561724DOI:10.1016/j.jss.2020.12.055.
Background: The purpose of this study was to evaluate the efficacy of Tamsulosin, administered preoperatively, for the prevention of postoperative urinary retention (POUR). POUR is a common complication of abdominal surgery, leading to the use of urinary catheters, which are a risk factor for urinary tract infection. Tamsulosin is a uroselective alpha-1a blocker used for the treatment of lower urinary tract symptoms. Materials and methods: A randomized, double-blind, placebo-controlled trial was undertaken from August 2015 to May 2018. Adults undergoing elective inpatient abdominal surgery were randomized to receive either Tamsulosin 0.4 mg or placebo daily for 7 d before surgery and continuing for up to 7 d postoperatively. The primary outcome was need for at least a single intermittent catheterization postoperatively. Secondary outcomes included first postvoid residual volume, number of catheterizations, need for replacement of an indwelling catheter, hospital length of stay, and urinary tract infection within 30 d of surgery. Results: A total of 158 participants were enrolled, with a final analytic cohort of 141 participants. The two groups had similar baseline characteristics, operative characteristics, and timing of catheter removal. There was no difference in the incidence of POUR between the two groups (26% in Tamsulosin versus 31% in placebo, P = 0.49). There was also no difference in any of the secondary outcomes between the two groups. Epidural usage, open surgery, and age <50 were identified as risk factors for POUR. Conclusions: Perioperative prophylaxis with Tamsulosin is not effective in reducing the incidence of POUR in patients undergoing elective abdominal surgery.
A randomized, comparative, open-label study of efficacy and tolerability of alfuzosin, Tamsulosin and silodosin in benign prostatic hyperplasia
Indian J Pharmacol 2016 Mar-Apr;48(2):134-40.PMID:27127315DOI:10.4103/0253-7613.178825.
Objectives: Benign prostatic hyperplasia (BPH) is a common and progressive disease affecting elderly males, often associated with lower urinary tract symptoms (LUTS). α1-blockers are the mainstay in symptomatic therapy of BPH. Because of their greater uroselectivity and minimal hemodynamic effects, alfuzosin, Tamsulosin, and silodosin are generally preferred. The aim of this study was to compare the efficacy and tolerability of alfuzosin, Tamsulosin, and silodosin in patients with BPH and LUTS. Methods: Ninety subjects with BPH and LUTS were randomized into three groups of thirty in each, to receive alfuzosin sustained release (SR) 10 mg, Tamsulosin 0.4 mg, or silodosin 8 mg for 12 weeks. The primary outcome measure was a change in the International Prostate Symptom Score (IPSS), and the secondary outcome measures were changes in individual subjective symptom scores, quality of life score (QLS), and peak flow rate (Qmax) from baseline. The treatment response was monitored at 2, 4, 8, and 12 weeks. Results: IPSS improved by 88.18%, 72.12%, and 82.23% in alfuzosin SR, Tamsulosin and silodosin groups (P < 0.001) at 12 weeks. Improvement in QLS was >75% in all the three groups (P < 0.001). A significant improvement in Qmax was seen with alfuzosin and Tamsulosin (P = 0.025 and P < 0.001) but not with silodosin (P = 0.153). However, the intergroup differences in IPSS, QLS, and Qmax were not significant. Ejaculatory dysfunction was more common with silodosin and corrected QT (QTc) prolongation occurred only with alfuzosin (two subjects) and Tamsulosin (three subjects). Conclusion: Alfuzosin, Tamsulosin, and silodosin showed similar efficacy in improvement of LUTS secondary to BPH, with good tolerability, acceptability, and minimum hemodynamic adverse effects. Alfuzosin, Tamsulosin, and silodosin are comparable in efficacy in symptomatic management of BPH. The occurrence of QTc prolongation in three subjects with Tamsulosin in the present study is an unexpected adverse event as there are no reports of QTc prolongation with Tamsulosin in any of the previous studies.