U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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
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
Demonstration of an additive antihypertensive effect of prazosin and polythiazide in out-patient.
1975 May
Antihypertensive action of drug combination: polythiazide, prazosin and tolamolol.
1977 Feb
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 Fri Dec 15 15:39:11 GMT 2023
Edited
by admin
on Fri Dec 15 15:39:11 GMT 2023
Record UNII
36780APV5N
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
POLYTHIAZIDE
HSDB   INN   JAN   MART.   MI   ORANGE BOOK   USAN   VANDF   WHO-DD  
USAN   INN  
Official Name English
POLYTHIAZIDE [HSDB]
Common Name English
POLYTHIAZIDE COMPONENT OF RENESE-R
Common Name English
POLYTHIAZIDE [ORANGE BOOK]
Common Name English
NSC-108161
Code English
POLYTHIAZIDE [JAN]
Common Name English
POLYTHIAZIDE COMPONENT OF MINIZIDE
Common Name English
POLYTHIAZIDE [VANDF]
Common Name English
6-Chloro-3,4-dihydro-2-methyl-3-[[(2,2,2-trifluoroethyl)thio]methyl]-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide
Systematic Name English
POLYTHIAZIDE [USAN]
Common Name English
P-2525
Code English
RENESE-R COMPONENT POLYTHIAZIDE
Common Name English
polythiazide [INN]
Common Name English
POLYTHIAZIDE [MART.]
Common Name English
RENESE
Brand Name English
Polythiazide [WHO-DD]
Common Name English
POLYTHIAZIDE [MI]
Common Name English
MINIZIDE COMPONENT 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
Classification Tree Code System Code
NDF-RT N0000166469
Created by admin on Fri Dec 15 15:39:11 GMT 2023 , Edited by admin on Fri Dec 15 15:39:11 GMT 2023
NDF-RT N0000166469
Created by admin on Fri Dec 15 15:39:11 GMT 2023 , Edited by admin on Fri Dec 15 15:39:11 GMT 2023
LIVERTOX 785
Created by admin on Fri Dec 15 15:39:11 GMT 2023 , Edited by admin on Fri Dec 15 15:39:11 GMT 2023
WHO-ATC C03AA05
Created by admin on Fri Dec 15 15:39:11 GMT 2023 , Edited by admin on Fri Dec 15 15:39:11 GMT 2023
WHO-VATC QC03AA05
Created by admin on Fri Dec 15 15:39:11 GMT 2023 , Edited by admin on Fri Dec 15 15:39:11 GMT 2023
NCI_THESAURUS C49185
Created by admin on Fri Dec 15 15:39:11 GMT 2023 , Edited by admin on Fri Dec 15 15:39:11 GMT 2023
NDF-RT N0000175359
Created by admin on Fri Dec 15 15:39:11 GMT 2023 , Edited by admin on Fri Dec 15 15:39:11 GMT 2023
WHO-VATC QC03AB05
Created by admin on Fri Dec 15 15:39:11 GMT 2023 , Edited by admin on Fri Dec 15 15:39:11 GMT 2023
NDF-RT N0000175419
Created by admin on Fri Dec 15 15:39:11 GMT 2023 , Edited by admin on Fri Dec 15 15:39:11 GMT 2023
WHO-ATC C03AB05
Created by admin on Fri Dec 15 15:39:11 GMT 2023 , Edited by admin on Fri Dec 15 15:39:11 GMT 2023
Code System Code Type Description
NCI_THESAURUS
C47676
Created by admin on Fri Dec 15 15:39:11 GMT 2023 , Edited by admin on Fri Dec 15 15:39:11 GMT 2023
PRIMARY
IUPHAR
7274
Created by admin on Fri Dec 15 15:39:11 GMT 2023 , Edited by admin on Fri Dec 15 15:39:11 GMT 2023
PRIMARY
WIKIPEDIA
POLYTHIAZIDE
Created by admin on Fri Dec 15 15:39:11 GMT 2023 , Edited by admin on Fri Dec 15 15:39:11 GMT 2023
PRIMARY
HSDB
850
Created by admin on Fri Dec 15 15:39:11 GMT 2023 , Edited by admin on Fri Dec 15 15:39:11 GMT 2023
PRIMARY
DAILYMED
36780APV5N
Created by admin on Fri Dec 15 15:39:11 GMT 2023 , Edited by admin on Fri Dec 15 15:39:11 GMT 2023
PRIMARY
DRUG CENTRAL
2228
Created by admin on Fri Dec 15 15:39:11 GMT 2023 , Edited by admin on Fri Dec 15 15:39:11 GMT 2023
PRIMARY
LACTMED
Polythiazide
Created by admin on Fri Dec 15 15:39:11 GMT 2023 , Edited by admin on Fri Dec 15 15:39:11 GMT 2023
PRIMARY
ECHA (EC/EINECS)
206-468-4
Created by admin on Fri Dec 15 15:39:11 GMT 2023 , Edited by admin on Fri Dec 15 15:39:11 GMT 2023
PRIMARY
MESH
D011139
Created by admin on Fri Dec 15 15:39:11 GMT 2023 , Edited by admin on Fri Dec 15 15:39:11 GMT 2023
PRIMARY
SMS_ID
100000081387
Created by admin on Fri Dec 15 15:39:11 GMT 2023 , Edited by admin on Fri Dec 15 15:39:11 GMT 2023
PRIMARY
ChEMBL
CHEMBL1587
Created by admin on Fri Dec 15 15:39:11 GMT 2023 , Edited by admin on Fri Dec 15 15:39:11 GMT 2023
PRIMARY
EPA CompTox
DTXSID6025939
Created by admin on Fri Dec 15 15:39:11 GMT 2023 , Edited by admin on Fri Dec 15 15:39:11 GMT 2023
PRIMARY
CAS
346-18-9
Created by admin on Fri Dec 15 15:39:11 GMT 2023 , Edited by admin on Fri Dec 15 15:39:11 GMT 2023
PRIMARY
PUBCHEM
4870
Created by admin on Fri Dec 15 15:39:11 GMT 2023 , Edited by admin on Fri Dec 15 15:39:11 GMT 2023
PRIMARY
RXCUI
8565
Created by admin on Fri Dec 15 15:39:11 GMT 2023 , Edited by admin on Fri Dec 15 15:39:11 GMT 2023
PRIMARY RxNorm
MERCK INDEX
m8975
Created by admin on Fri Dec 15 15:39:11 GMT 2023 , Edited by admin on Fri Dec 15 15:39:11 GMT 2023
PRIMARY Merck Index
INN
1187
Created by admin on Fri Dec 15 15:39:11 GMT 2023 , Edited by admin on Fri Dec 15 15:39:11 GMT 2023
PRIMARY
FDA UNII
36780APV5N
Created by admin on Fri Dec 15 15:39:11 GMT 2023 , Edited by admin on Fri Dec 15 15:39:11 GMT 2023
PRIMARY
EVMPD
SUB09976MIG
Created by admin on Fri Dec 15 15:39:11 GMT 2023 , Edited by admin on Fri Dec 15 15:39:11 GMT 2023
PRIMARY
DRUG BANK
DB01324
Created by admin on Fri Dec 15 15:39:11 GMT 2023 , Edited by admin on Fri Dec 15 15:39:11 GMT 2023
PRIMARY
NSC
108161
Created by admin on Fri Dec 15 15:39:11 GMT 2023 , Edited by admin on Fri Dec 15 15:39:11 GMT 2023
PRIMARY
Related Record Type Details
TARGET -> INHIBITOR
DEGRADENT -> PARENT
Related Record Type Details
ACTIVE MOIETY