Absorption, Distribution and Excretion
Thiazide drugs are rapidly absorbed through the gastrointestinal tract…Most thiazide drugs exhibit a significant diuretic effect within hours of oral administration. …Thiazide drugs with a relatively long duration of action…can bind to plasma proteins and be reabsorbed by the renal tubules. /Thiazide Drugs/
…Thiazide drugs may be actively secreted in the proximal tubules. Renal clearance is high, potentially higher or lower than the glomerular filtration rate. Most compound thiazide drugs are rapidly excreted within 3 to 6 hours. /Thiazide Drugs/

Interactions
...Diuretics can antagonize the effects of oral anticoagulants by increasing clotting factor concentrations through reduced plasma volume and by increasing clotting factor synthesis through reduced hepatic congestion. /Thiazide Diuretics/
Concomitant use of thiazide diuretics and monoamine oxidase inhibitors may worsen hypotension. /Thiazide Diuretics/
...Hypokalemia may enhance the effects of neuromuscular blocking agents. ...Kopaqueous-depleting diuretics are known to cause hypokalemia and may enhance this effect. /Diuretics/
Thiazide drugs can enhance the antihypertensive effect of guanethidine, thereby reducing the dose of guanethidine and decreasing the incidence of adverse reactions... /Thiazide Drugs/
For more complete data on interactions of cyclothiazides (23 in total), please visit the HSDB record page.

Proc Natl Acad Sci U S A. 2006 Feb 21; 103(8): 2943–2947.

Therapeutic Uses
Antihypertensive drugs; Thiazide diuretics. Less common uses include treating diabetes insipidus and hypercalciuria in patients with recurrent urinary tract stones (calcification). /Thiazides/ Thiazide diuretics can be used as adjunctive therapy for edema caused by congestive heart failure, cirrhosis, corticosteroid and estrogen therapy, and various types of renal insufficiency… and severe edema caused by pregnancy. Thiazide drugs. Cyclothiazides are orally effective diuretics and antihypertensives. Diuretic effects occur within 2 hours and last for 18 to 24 hours. …It can be used as adjunctive therapy for other antihypertensive drugs, such as diuretics and ganglion blockers. For more complete data on the therapeutic uses of cyclothiazides (10 in total), please visit the HSDB record page.

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Drug Warnings Patients taking thiazide diuretics long-term should have their plasma potassium levels monitored regularly. Benzothiazide Diuretics
Thiazide diuretics are contraindicated in patients with anuria, patients allergic to this product or other sulfonamides, and healthy pregnant women with or without mild edema. …Use with caution in patients with kidney disease, as they may develop azotemia. Thiazides
All patients should have their serum electrolytes measured regularly to detect electrolyte imbalances such as hyponatremia, hypochloremic alkalosis, and hypokalemia. Thiazides
The primary action of thiazides is to increase the renal excretion of sodium, chloride, and their associated anions (chloride). …Thiazides inhibit the reabsorption of sodium and its associated anions (chloride) in the distal renal tubules.
For more complete data on drug warnings for cyclothiazides (10 in total), please visit the HSDB record page.
Pharmacodynamics
As with other thiazides, cyclothiazides promote water loss (diuresis). It inhibits the reabsorption of sodium/chloride ions in the distal renal tubules. Thiazide drugs can also lead to potassium loss and elevated serum uric acid. Thiazide drugs are commonly used to treat hypertension, but their antihypertensive effect is not entirely attributable to their diuretic activity. Thiazide drugs have been shown to prevent hypertension-related morbidity and mortality, although the mechanism is not fully understood. Thiazide drugs induce vasodilation by activating calcium-activated potassium channels (high conductance) in vascular smooth muscle and inhibiting various carbonic anhydrases in vascular tissue. Cyclothiazides affect the reabsorption of electrolytes in the distal renal tubules. At maximum therapeutic doses, the diuretic effect of all thiazide drugs is roughly the same. Cyclothiazides increase sodium and chloride excretion, and the increases are roughly equal. Increased sodium excretion may be accompanied by small amounts of potassium and bicarbonate loss.

C14H16N3O4S2CL

389.87754

389.027

2259-96-3

191744-13-5 (CX614); 22503-72-6 (IDRA-21); 742-20-1 (Cyclopenthiazide)

2910

White to off-white solid powder

1.6±0.1 g/cm3

627.3±65.0 °C at 760 mmHg

234ºC

333.2±34.3 °C

0.0±1.8 mmHg at 25°C

1.654

1.15

3

7

2

24

758

0

BOCUKUHCLICSIY-UHFFFAOYSA-N

InChI=1S/C14H16ClN3O4S2/c15-10-5-11-13(6-12(10)23(16,19)20)24(21,22)18-14(17-11)9-4-7-1-2-8(9)3-7/h1-2,5-9,14,17-18H,3-4H2,(H2,16,19,20)

3-(bicyclo[2.2.1]hept-5-en-2-yl)-6-chloro-3,4-dihydro-2H-benzo[e][1,2,4]thiadiazine-7-sulfonamide 1,1-dioxide

CTZ, Cyclothiazide; Fluidil; Anhydron; Anhydron; Renazide; Valmiran; Doburil; Acquirel; Renazide; Tensodiural

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 : ~125 mg/mL (~320.61 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.)