Details
| Stereochemistry | RACEMIC |
| Molecular Formula | C11H13ClF3N3O4S3 |
| Molecular Weight | 439.882 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CN1C(CSCC(F)(F)F)NC2=CC(Cl)=C(C=C2S1(=O)=O)S(N)(=O)=O
InChI
InChIKey=CYLWJCABXYDINA-UHFFFAOYSA-N
InChI=1S/C11H13ClF3N3O4S3/c1-18-10(4-23-5-11(13,14)15)17-7-2-6(12)8(24(16,19)20)3-9(7)25(18,21)22/h2-3,10,17H,4-5H2,1H3,(H2,16,19,20)
| Molecular Formula | C11H13ClF3N3O4S3 |
| Molecular Weight | 439.882 |
| Charge | 0 |
| Count |
|
| Stereochemistry | RACEMIC |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Optical Activity | ( + / - ) |
DescriptionSources: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=abd6ecf0-dc8e-41de-89f2-1e36ed9d6535Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/5086971
Sources: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=abd6ecf0-dc8e-41de-89f2-1e36ed9d6535
Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/5086971
Polythiazide is a thiazide diuretic with actions and uses similar to those of hydrochlorothiazide. Polythiazide under brand name Rense is indicated as adjunctive therapy in edema associated with congestive heart failure, hepatic cirrhosis, and corticosteroid and estrogen therapy. Renese is indicated in the management of hypertension either as the sole therapeutic agent or to enhance the effectiveness of other antihypertensive drugs in the more severe forms of hypertension. The mechanism of action results in an interference with the renal tubular mechanism of electrolyte reabsorption. At maximal therapeutic dosage, all thiazides are approximately equal in their diuretic potency. The mechanism whereby thiazides function in the control of hypertension is unknown, but as a diuretic, polythiazide inhibits active chloride reabsorption at the early distal tubule via the thiazide-sensitive Na-Cl cotransporter (TSC), resulting in an increase in the excretion of sodium, chloride, and water. Thiazides like polythiazide also inhibit sodium ion transport across the renal tubular epithelium through binding to the thiazide sensitive sodium-chloride transporter. This results in an increase in potassium excretion via the sodium-potassium exchange mechanism. The antihypertensive mechanism of polythiazide may be mediated through its action on carbonic anhydrases in the smooth muscle or through its action on the large-conductance calcium-activated potassium (KCa) channel, also found in the smooth muscle.
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL1876 Sources: https://www.ncbi.nlm.nih.gov/pubmed/10894798 |
0.02 µM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Palliative | RENESE Approved UseRenese is indicated as adjunctive therapy in edema associated with congestive heart failure, hepatic cirrhosis, and corticosteroid and estrogen therapy. Renese has also been found useful in edema due to various forms of renal dysfunction as: Nephrotic syndrome; Acute glomerulonephritis; and Chronic renal failure. Renese is indicated in the management of hypertension either as the sole therapeutic agent or to enhance the effectiveness of other antihypertensive drugs in the more severe forms of hypertension. Launch Date1961 |
|||
| Palliative | RENESE Approved UseRenese is indicated as adjunctive therapy in edema associated with congestive heart failure, hepatic cirrhosis, and corticosteroid and estrogen therapy. Renese has also been found useful in edema due to various forms of renal dysfunction as: Nephrotic syndrome; Acute glomerulonephritis; and Chronic renal failure. Renese is indicated in the management of hypertension either as the sole therapeutic agent or to enhance the effectiveness of other antihypertensive drugs in the more severe forms of hypertension. Launch Date1961 |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
3.33 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/620486/ |
1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered: |
POLYTHIAZIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
55.7 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/620486/ |
1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered: |
POLYTHIAZIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
25.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/620486/ |
1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered: |
POLYTHIAZIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Depression after treatment with thiazide diuretics for hypertension. | 1985-09 |
|
| Prazosin and clonidine for moderately severe hypertension. | 1978-12-01 |
|
| Antihypertensive action of drug combination: polythiazide, prazosin and tolamolol. | 1977-02 |
|
| Demonstration of an additive antihypertensive effect of prazosin and polythiazide in out-patient. | 1975-05 |
|
| Propranolol and polythiazide in treatment of hypertension. | 1972-10 |
|
| [Conditions for safe and effective use of polythiazide (renese) in the treatment of obesity]. | 1967-12-20 |
Patents
Sample Use Guides
The usual dosage of tablets for diuretic therapy is 1 to 4 mg daily, and for antihypertensive therapy is 2 to 4 mg daily.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/7208592
Curator's Comment: The interaction between thiazide diuretics and contractile responses produced by 5-hydroxytryptamine, acetylcholine, noradrenaline and angiotensin II, has been examined on isolated rat uterus and guinea pig aorta. Polythiazide inhibited the contraction of isolated tissue induced by the spasmogens. These data demonstrated that the tested diuretics possess antagonistic activity on contractions induced by various spasmogens.
Unknown
| Substance Class |
Chemical
Created
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| Record UNII |
36780APV5N
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Validated (UNII)
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NDF-RT |
N0000166469
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N0000166469
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785
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WHO-ATC |
C03AA05
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WHO-VATC |
QC03AA05
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NCI_THESAURUS |
C49185
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NDF-RT |
N0000175359
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WHO-VATC |
QC03AB05
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NDF-RT |
N0000175419
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WHO-ATC |
C03AB05
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C47676
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7274
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POLYTHIAZIDE
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850
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36780APV5N
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2228
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Polythiazide
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8565
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m8975
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1187
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36780APV5N
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108161
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