Absorption, Distribution and Excretion
Absorption is relatively rapid after oral administration.
Most clopidogrels are rapidly excreted within 3–6 hours. Benzoflusidine has a longer duration of action, which is related to its slower excretion.
Thiazide drugs are absorbed via the gastrointestinal tract, and their efficacy is primarily attributed to the oral route. Absorption is relatively rapid. Most drugs show significant diuretic effects within hours of oral administration. Benzothiazines
Generally, thiazide drugs with longer durations of action have higher plasma protein binding rates and are reabsorbed by the renal tubules. The drugs readily cross the placental barrier into the fetus. All thiazide drugs may undergo active secretion in the proximal renal tubules. Thiazide Diuretics
Benzoflusidine was administered orally to 9 healthy volunteers. Peak plasma concentrations were reached at 1 ± 0.4 hours. Concentrations decreased, with a mean half-life of 3 hours. The mean apparent volume of distribution was 1.48 L/kg. Excretion is primarily via non-renal routes. The mean urinary recovery rate was 30%.
Benzoflutidine appears to be well absorbed by the gastrointestinal tract. The drug is excreted unchanged in the urine and is essentially eliminated within 24 hours.
Biological half-life
8.5 hours. The half-life is 3–3.9 hours. (Data from table)

Effects During Pregnancy and Lactation
◉ Overview of Lactation Use
There is currently no information on the content of benzfluthiazide in breast milk. The potent diuretic effect of high-dose benzfluthiazide can reduce breast milk production, especially in the neonatal period. It is recommended to prioritize low-dose, short-acting diuretics over benzfluthiazide.
◉ Effects on Breastfed Infants
As of the revision date, no relevant published information was found.
◉ Effects on Lactation and Breast Milk
Benzfluthiazide has been used to suppress lactation at a dose of 5 mg orally twice daily for 5 days; or 10 mg in the morning and 5 mg in the afternoon. The additional effects of diuretics on these effective lactation-suppressing measures have not been studied. There are currently no data on the effects of potent diuretics on breastfeeding in established, sustained lactation.

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Protein Binding 96%

:Treatment of arterial hypertensive disease with diuretics. I. Effects on blood pressure of bendroflumethiazide, potassium chloride, and spironolactone. Arch Intern Med. 1962;110:26-33.

Benzylfluorothiazide is a sulfonamide drug with the structure 7-sulfonyl-3,4-dihydro-2H-1,2,4-benzothiadiazine-1,1-dioxide, where the hydrogen at position 6 is replaced by a trifluoromethyl group and the hydrogen at position 3 is replaced by a benzyl group. It has diuretic and antihypertensive effects. It is a benzothiadiazine and sulfonamide drug. It is a thiazide diuretic, with effects and uses similar to hydrochlorothiazide. It has been used to treat familial hyperkalemia, hypertension, edema, and urinary tract diseases. (Excerpt from Martindale Pharmacopoeia, 30th edition, page 810) Benzylfluorothiazide is a thiazide diuretic. The physiological effect of benzylfluorothiazide is achieved by increasing diuresis. Benzylfluorothiazide is a long-acting drug, also known as benzylfluorothiazide, belonging to the thiazide diuretic class, and has an antihypertensive effect. It is a thiazide diuretic, with effects and uses similar to hydrochlorothiazide. It has been used to treat familial hyperkalemia, hypertension, edema, and urinary tract disorders. (Excerpt from Martindale Pharmacopoeia, 30th edition, p. 810)
See also: benzfluthiazide; nadolol (component).
Drug Indications

For the treatment of hypertension and control of heart failure-related edema.
Mechanism of Action

As a diuretic, benzfluthiazide increases the excretion of sodium, chloride, and water by inhibiting the early active reabsorption of chloride ions in the distal renal tubules via sodium-chloride cotransporters. Thiazides (such as benzfluthiazide) also inhibit the transport of sodium ions across the renal tubular epithelium by binding to thiazide-sensitive sodium-chloride transporters. This leads to increased potassium excretion via the sodium-potassium exchange mechanism. Although the antihypertensive mechanism of benzfluthiazide is not fully understood, its mechanism of action may be related to carbonic anhydrase in smooth muscle or high-conductivity calcium-activated potassium channels (KCa channels) in smooth muscle.
...Benzothiazines have a direct effect on the transport of sodium and chloride in the renal tubules...and are unrelated to carbonic anhydrase. /Thiazide Diuretics/
The nature of the chemical interaction between thiazide drugs and the specific renal receptors responsible for chloride diuresis is unclear; the key enzymatic reactions have not been identified. Thiazide Diuretics
...reduce the excretion of uric acid in the body, thereby increasing the concentration of uric acid in the plasma. The hyperuricemic effect is mainly due to the inhibition of renal tubular secretion of urate. ...Unlike most other diuretics...thiazide diuretics reduce renal calcium excretion (relative to sodium excretion).../increase/magnesium excretion...Thiazide Diuretics
Thiazide drugs inhibit the reabsorption of sodium and chloride in the distal renal tubules. ...As a class of drugs...they play an important role in potassium excretion due to the increased secretion of cations in the distal renal tubules. Thiazide drugs may reduce glomerular filtration rate, especially during experimental intravenous administration. /Thiazide Diuretics/
For more complete data on the mechanisms of action of benfluthiazides (11 in total), please visit the HSDB record page.

C15H14F3N3O4S2

421.41

421.037

73-48-3

(Rac)-Bendroflumethiazide-d5;1330183-13-5

2315

Crystals from dioxane.
WHITE TO CREAM-COLORED, FINELY DIVIDED, CRYSTALLINE POWDER

1.5±0.1 g/cm3

602.1±65.0 °C at 760 mmHg

205-207ºC

318.0±34.3 °C

0.0±1.7 mmHg at 25°C

1.584

2.07

135.12

3

10

3

27

740

0

HDWIHXWEUNVBIY-UHFFFAOYSA-N

InChI=1S/C15H14F3N3O4S2/c16-15(17,18)10-7-11-13(8-12(10)26(19,22)23)27(24,25)21-14(20-11)6-9-4-2-1-3-5-9/h1-5,7-8,14,20-21H,6H2,(H2,19,22,23)

3-Benzyl-1,1-dioxo-6-(trifluoromethyl)-3,4-dihydro-2H-1,2,4- benzothiadiazine-7-sulfonamide

Bentride Benuron FT 81Livesan NaigarilUrleaRelan Beta SaluralRauzideBenzy-RodiuranOrsile PlurylBendroflumethiazide Aprinox Be 724A Bendrofluazide Berkozide BristuronCentyl SinesalinNaturetin Neo-Rontyl NiagarilPluryle Poliuron Sodiuretic

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ~250 mg/mL (~593.25 mM)

注意: 如下所列的是一些常用的体内动物实验溶解配方，主要用于溶解难溶或不溶于水的产品（水溶度<1 mg/mL）。 建议您先取少量样品进行尝试，如该配方可行，再根据实验需求增加样品量。

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注射用配方1: DMSO : Tween 80： Saline = 10 : 5 : 85 (如： 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)
*生理盐水/Saline的制备：将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中，得到澄清溶液。
注射用配方 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)
注射用配方 3: DMSO : Corn oil = 10 : 90 (如： 100 μL DMSO → 900 μL Corn oil)
示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液，加到 900 μL Corn oil/玉米油中, 混合均匀。

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注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如：100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)]
*20% SBE-β-CD in Saline的制备（4°C，储存1周）：将2g SBE-β-CD (磺丁基-β-环糊精) 溶解于10mL生理盐水中，得到澄清溶液。
注射用配方 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (如： 500 μL 2-Hydroxypropyl-β-cyclodextrin (羟丙基环胡精)→ 500 μL Saline)
注射用配方 6: DMSO : PEG300 : Castor oil : Saline = 5 : 10 : 20 : 65 (如： 50 μL DMSO → 100 μL PEG300 → 200 μL Castor oil → 650 μL Saline)
注射用配方 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (如： 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
注射用配方 8: 溶解于Cremophor/Ethanol (50 : 50), 然后用生理盐水稀释。
注射用配方 9: EtOH : Corn oil = 10 : 90 (如： 100 μL EtOH → 900 μL Corn oil)
注射用配方 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL EtOH → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)

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口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠)
口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素)
示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中，得到0.5%CMC-Na澄清溶液；然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中，得到悬浮液。

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口服配方 3: 溶解于 PEG400 (聚乙二醇400)
口服配方 4: 悬浮于0.2% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 5: 溶解于0.25% Tween 80 and 0.5% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 6: 做成粉末与食物混合

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注意: 以上为较为常见方法，仅供参考， InvivoChem并未独立验证这些配方的准确性。具体溶剂的选择首先应参照文献已报道溶解方法、配方或剂型，对于某些尚未有文献报道溶解方法的化合物，需通过前期实验来确定（建议先取少量样品进行尝试），包括产品的溶解情况、梯度设置、动物的耐受性等。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。