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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
MOL RATIO 1 MOL RATIO (average)
Stereochemistry RACEMIC
Additional Stereochemistry No
Defined Stereocenters 0 / 1
E/Z Centers 0
Optical Activity ( + / - )

Description

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 TargetPharmacologyConditionPotency
0.02 µM [IC50]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Palliative
RENESE
Palliative
RENESE

Cmax

ValueDoseCo-administeredAnalytePopulation
3.33 ng/mL
1 mg single, oral
POLYTHIAZIDE plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
55.7 ng × h/mL
1 mg single, oral
POLYTHIAZIDE plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
25.7 h
1 mg single, oral
POLYTHIAZIDE plasma
Homo sapiens

PubMed

Patents

Sample Use Guides

In Vivo Use Guide
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
Unknown
Substance Class Chemical
Record UNII
36780APV5N
Record Status Validated (UNII)
Record Version