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Details

Stereochemistry UNKNOWN
Molecular Formula C11H13ClF3N3O4S3
Molecular Weight 439.882
Optical Activity ( + / - )
Defined Stereocenters 0 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of POLYTHIAZIDE, (+)-

SMILES

CN1C(CSCC(F)(F)F)NC2=C(C=C(C(Cl)=C2)S(N)(=O)=O)S1(=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)

HIDE SMILES / InChI

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 ( + / - )

Description
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

Targets

Primary TargetPharmacologyConditionPotency
0.02 µM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Palliative
RENESE

Approved Use

Renese 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 Date

1961
Palliative
RENESE

Approved Use

Renese 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 Date

1961
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
3.33 ng/mL
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

AUC

ValueDoseCo-administeredAnalytePopulation
55.7 ng × h/mL
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

T1/2

ValueDoseCo-administeredAnalytePopulation
25.7 h
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

PubMed

TitleDatePubMed
[Conditions for safe and effective use of polythiazide (renese) in the treatment of obesity].
1967 Dec 20
Propranolol and polythiazide in treatment of hypertension.
1972 Oct
Demonstration of an additive antihypertensive effect of prazosin and polythiazide in out-patient.
1975 May
Patents

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
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
by admin
on Sat Dec 16 11:25:42 GMT 2023
Edited
by admin
on Sat Dec 16 11:25:42 GMT 2023
Record UNII
SWY93BD8RL
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
POLYTHIAZIDE, (+)-
Common Name English
2H-1,2,4-BENZOTHIADIAZINE-7-SULFONAMIDE, 6-CHLORO-3,4-DIHYDRO-2-METHYL-3-(((2,2,2-TRIFLUOROETHYL)THIO)METHYL)-, 1,1-DIOXIDE, (+)-
Systematic Name English
NEPHRIL, (+)-
Common Name English
Code System Code Type Description
CAS
96783-10-7
Created by admin on Sat Dec 16 11:25:42 GMT 2023 , Edited by admin on Sat Dec 16 11:25:42 GMT 2023
PRIMARY
FDA UNII
SWY93BD8RL
Created by admin on Sat Dec 16 11:25:42 GMT 2023 , Edited by admin on Sat Dec 16 11:25:42 GMT 2023
PRIMARY