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

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)

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)