Bendroflumethiazide
(Synonyms: 苄氟噻嗪,Bendrofluazide) 目录号 : GC42914
An Analytical Reference Standard
Cas No.:73-48-3
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
Bendroflumethiazide is an analytical reference standard categorized as a diuretic. Diuretics, including bendroflumethiazide, have been abused as performance-enhancing drugs and masking agents in sports doping. This product is intended for research and forensic applications.
| Cas No. | 73-48-3 | SDF | |
| 别名 | 苄氟噻嗪,Bendrofluazide | ||
| Canonical SMILES | O=S1(C2=C(C=C(C(F)(F)F)C(S(N)(=O)=O)=C2)NC(CC3=CC=CC=C3)N1)=O | ||
| 分子式 | C15H14F3N3O4S2 | 分子量 | 421.4 |
| 溶解度 | DMF: 10 mg/ml,DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml,DMSO: 10 mg/ml,Ethanol: 2 mg/ml | 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 | 2.373 mL | 11.8652 mL | 23.7304 mL |
| 5 mM | 0.4746 mL | 2.373 mL | 4.7461 mL |
| 10 mM | 0.2373 mL | 1.1865 mL | 2.373 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。
Pharmacokinetics of Bendroflumethiazide
Clin Pharmacol Ther 1977 Oct;22(4):385-8.PMID:902450DOI:10.1002/cpt1977224385.
Bendroflumethiazide (bft), 10 mg, was administered orally to 9 healthy volunteers. The concentrations of the diuretic in plasma and urine were determined by gas-liquid chromatography (GLC). Peak plasma levels (86 +/- 18 ng/ml) of bft were reached at 2 +/- 0.4 hr. The concentration declined with a mean t1/2 of 3.0 hr. The apparent volume of distribution averaged 1.48 L/kg. The major part of the drug was eliminated via nonrenal mechanisms, the nonrenal clearance being estimated to 269 +/- 77 ml/min and renal clearance to 105 +/- 24 ml/min. Urinary recovery of the thiazide averaged 30%.
The effect of indapamide vs. Bendroflumethiazide for primary hypertension: a systematic review
Br J Clin Pharmacol 2019 Feb;85(2):285-303.PMID:30312512DOI:10.1111/bcp.13787.
The aims of the current review were to compare the efficacy of monotherapy with Bendroflumethiazide vs. indapamide on mortality, cardiovascular outcomes, blood pressure, need for intensification of treatment and treatment withdrawal. Two authors independently screened the results of a literature search, assessed the risk of bias and extracted relevant data. Randomized clinical trials of hypertensive patients of at least a 1-year duration were included. When there was disagreement, a third reviewer was consulted. Risk ratio (RR) and mean differences were used as measures of effect. Two trials comparing Bendroflumethiazide against placebo, one comparing indapamide with placebo and three of short duration directly comparing indapamide and Bendroflumethiazide, were included. No statistically significant difference was found between indapamide and Bendroflumethiazide for all deaths [RR 0.82; 95% confidence interval (CI) 0.57, 1.18], cardiovascular deaths (RR 0.82; 95% CI 0.55, 1.20), noncardiovascular deaths (0.81; 95% CI 0.54, 1.22), coronary events (RR 0.73; 95% CI 0.30, 1.79) or all cardiovascular events (RR 0.89; 95% CI 0.67, 1.18). Indapamide performed worse for stroke (RR 2.21; 95% CI 1.19, 4.11), even though a reduction in RR compared with placebo was observed in both groups. There was no statistically or clinically significant difference between indapamide and Bendroflumethiazide in blood pressure reduction (mean absolute difference <1 mmHg). The present review highlights a lack of studies to answer the review question but also a lack of evidence of superiority of one drug over the other. Therefore, there is a clear need for new studies directly comparing the effect of these drugs on the outcomes of interest.
Metolazone and Bendroflumethiazide in hypertension: physiologic and metabolic observations
Clin Pharmacol Ther 1980 Nov;28(5):611-8.PMID:7438679DOI:10.1038/clpt.1980.211.
A double-blind crossover comparison was made in 18 nonedematous hypertensive subjects with glomerular filtration rates exceeding 70 ml/min/1.73 m2 of the effects of 5 mg metolazone and 5 mg Bendroflumethiazide on blood pressure and metabolic parameters. After a 4-wk run-in placebo period, patients received either metolazone or Bendroflumethiazide for 6 wk in a crossover fashion with an intervening washout period of 4 wk. Metolazone induced a more sustained and greater blood pressure response than Bendroflumethiazide. Changes in plasma potassium, urate, bicarbonate, renin, and angiotensin II occurred during treatment with both metolazone and Bendroflumethiazide; the only significant difference, however, was in changes in plasma bicarbonate. Total body potassium (TBK), measured by whole-body monitor, did not fall outside the normal range with either metolazone or Bendroflumethiazide, although metolazone induced a greater reduction in TBK (6.2 gm, 5.5% of TBK) than Bendroflumethiazide (1.2 gm, 1.1% of TBK, p < 0.05). Our results suggest that metolazone is a more effective antihypertensive and induces similar but greater metabolic changes than Bendroflumethiazide. The results of our comparison suggest that although changes in plasma potassium and TBK are minor, they are greater with metolazone, and potassium supplements may not be necessary in nonedematous hypertensive patients with normal renal function.
Pharmacokinetics of Bendroflumethiazide alone and in combination with propranolol and hydralazine
Eur J Clin Pharmacol 1982;21(4):315-23.PMID:7056277DOI:10.1007/BF00637620.
Bendroflumethiazide (Bft) was administered to 6 healthy subjects at 3 different dose levels (2.5, 5 and 10mg) in a cross-over design, either as capsules (2.5mg) or as tablets (5mg). Its pharmacokinetics were evaluated then and following administration of a fixed combination of Bft and propranolol and hydralazine to a further 7 volunteers. Plasma and urinary concentrations of Bft were determined by a new fluorimetric - thin-layer chromatography procedure. Peak plasma levels occurred after 2-3h and averaged 15, 27 and 45 microgram/l in the three dose groups. Areas under the plasma concentration - time curves (AUC0 leads to 12), which were 75, 147 and 250 microgram 1(-1)h respectively, and cumulative urinary recovery (20%) were independent of the dose administered and the type of formulation. Thus Bft kinetics proved to be linear within the dose range evaluated. The plasma clearance was calculated to be 505 ml/min, renal clearance 108 ml/min and nonrenal clearance 396 ml/min. Bioavailability of Bft was not altered following administration of the fixed combination. The amount of propranolol found in the circulation did not change, whereas that of hydralazine (determined as apparent hydralazine) increased by 59% when the fixed combination was administered.
Efficacy and safety of 24 weeks of therapy with Bendroflumethiazide 1.25 mg/day or 2.5 mg/day and potassium chloride compared with enalapril 10 mg/day and amlodipine 5 mg/day in patients with mild to moderate primary hypertension : a multicentre, randomised, open study
Clin Drug Investig 2006;26(2):91-101.PMID:17163239DOI:10.2165/00044011-200626020-00004.
Background: The efficacy and safety of therapy with low-dose Bendroflumethiazide 1.25 mg/day or 2.5 mg/day and potassium chloride was compared with that of enalapril 10 mg/day and amlodipine 5 mg/day in patients with mild to moderate primary hypertension. Study design: This was a multicentre study in general practice with patients randomised in a double-blind fashion and on open-label treatment. After a washout phase that lasted 4-6 weeks, 312 patients with a diastolic blood pressure of between 100 and 115 mm Hg were randomised in a double-blind fashion to treatment with either Bendroflumethiazide 1.25 mg/day and potassium chloride (n = 117), Bendroflumethiazide 2.5 mg/day and potassium chloride (n = 60), amlodipine 5 mg/day (n = 61) or enalapril 10 mg/day (n = 60), all given once daily (numbers in parentheses indicate the intention-to-treat population, with a total of 298 patients). The primary efficacy parameter was the reduction in diastolic blood pressure. Effects on systolic blood pressure, heart rate, biochemical variables, adverse events and quality of life were studied as secondary efficacy parameters. Results: All treatments reduced diastolic blood pressure significantly; reductions were as follows: 6.8 mm Hg with Bendroflumethiazide 1.25 mg/day, 9.1 mm Hg with Bendroflumethiazide 2.5 mg/day, 10.8 mm Hg with amlodipine 5 mg/day and 6.8 mm Hg with enalapril 10 mg/day. The reduction in diastolic blood pressure on amlodipine was significantly greater than on Bendroflumethiazide 1.25 mg/day and enalapril 10 mg/day (p = 0.013). The percentage of patients achieving a diastolic blood pressure of < 95 mm Hg was 34% (SD 4.4) with Bendroflumethiazide 1.25 mg/day, 48% (SD 6.5) with Bendroflumethiazide 2.5 mg/day (p = 0.075 vs Bendroflumethiazide 1.25 mg/day), 57% (SD 6.3) with amlodipine 5 mg/day (p = 0.004 vs Bendroflumethiazide 1.25 mg/day) and 41% (SD 6.4) with enalapril 10 mg/day (p = 0.41 vs Bendroflumethiazide 1.25 mg/day) [mean reductions]. The effect on systolic blood pressure was similar with all treatments. No clinically significant changes occurred in heart rate, serum potassium, blood glucose, serum urate or serum cholesterol levels. The incidences of adverse events were similar in the low-dose Bendroflumethiazide groups, with significantly higher incidences in the enalapril and amlodipine groups. Quality of life was similar in the different treatment groups, but the study had limited power to detect any difference in this parameter. Conclusion: The present study has confirmed, in a general practice population, that low-dose Bendroflumethiazide (Bendroflumethiazide 1.25-2.5 mg/day) in combination with potassium chloride is a well tolerated and efficacious first-line treatment for patients with mild to moderate essential hypertension.