Banner
targets (1)
for drugs
Identification
Name Polythiazide
Accession Number DB01324
Type small molecule
Groups approved
Description

A thiazide diuretic with actions and uses similar to those of hydrochlorothiazide. (From Martindale, The Extra Pharmacopoeia, 30th ed, p826)
Structure Thumb
Download: MOL | SDF | SMILES | InChI
Display: 2D Structure | 3D Structure
Synonyms Not Available
Salts Not Available
Brand names Not Available
Brand mixtures Not Available
Categories
  • Antihypertensive Agents
  • Diuretics
  • Sodium Chloride Symporter Inhibitors
CAS number 346-18-9
Weight Average: 439.882
Monoisotopic: 438.970880311
Chemical Formula C11H13ClF3N3O4S3
InChI Key InChIKey=CYLWJCABXYDINA-UHFFFAOYSA-N
InChI
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)
Plain Text
IUPAC Name
6-chloro-2-methyl-1,1-dioxo-3-{[(2,2,2-trifluoroethyl)sulfanyl]methyl}-3,4-dihydro-2H-1$l^{6},2,4-benzothiadiazine-7-sulfonamide
SMILES
CN1C(CSCC(F)(F)F)NC2=CC(Cl)=C(C=C2S1(=O)=O)S(N)(=O)=O
Plain Text
Mass Spec Not Available
Taxonomy
Kingdom Organic
Classes
  • Benzenesulfonamides
  • Sulfanilamides
Substructures
  • Ethers
  • Sulfonyls
  • Benzene and Derivatives
  • Aryl Halides
  • Benzenesulfonamides
  • Halobenzenes
  • Aminals and Derivatives
  • Heterocyclic compounds
  • Aromatic compounds
  • Thiadiazines
  • Sulfanilamides
  • Sulfonamides
  • Anilines
Pharmacology
Indication Polythiazide is a thiazide diuretic used to decrease edema and decrease blood pressure.
Pharmacodynamics As a thiazide diuretic, Polythiazide inhibits the sodium-chloride symporter which decreases solute reabsorption leading to a retention of water in the urine, as water normally follows solutes. More frequent urination is due to the increased loss of water that has not been retained from the body as a result of a concomitant relationship with sodium loss from the convoluted tubule. The short-term anti-hypertensive action is based on the fact that thiazides decrease preload, decreasing blood pressure
Mechanism of action 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.
Absorption Not Available
Volume of distribution Not Available
Protein binding Not Available
Metabolism Not Available
Route of elimination Not Available
Half life Not Available
Clearance Not Available
Toxicity Not Available
Affected organisms
  • Humans and other mammals
Pathways
Pathway Name SMPDB ID
Smp00080 Polythiazide Pathway SMP00080
Pharmacoeconomics
Manufacturers
  • Pfizer inc
Packagers
Dosage forms
Form Route Strength
Tablet Oral
Prices Not Available
Patents Not Available
Properties
State solid
Experimental Properties
Property Value Source
melting point 214 °C PhysProp
logP 1.90 SANGSTER (1994)
Predicted Properties
Property Value Source
water solubility 2.64e-01 g/l ALOGPS
logP 2.13 ALOGPS
logP 1.1 ChemAxon
logS -3.2 ALOGPS
pKa (strongest acidic) 9.31 ChemAxon
pKa (strongest basic) -3.1 ChemAxon
physiological charge 0 ChemAxon
hydrogen acceptor count 5 ChemAxon
hydrogen donor count 2 ChemAxon
polar surface area 109.57 ChemAxon
rotatable bond count 5 ChemAxon
refractivity 90.52 ChemAxon
polarizability 37.56 ChemAxon
References
Synthesis Reference Not Available
General Reference Not Available
External Links
Resource Link
KEGG Drug D00657 Link_out
KEGG Compound C07766 Link_out
PubChem Compound 4870 Link_out
PubChem Substance 46508633 Link_out
ChemSpider 4704 Link_out
Therapeutic Targets Database DAP000751 Link_out
PharmGKB PA164748763 Link_out
RxList http://www.rxlist.com/cgi/generic/renese.htm Link_out
Drugs.com http://www.drugs.com/cons/polythiazide.html Link_out
ATC Codes
  • C03AA05
AHFS Codes Not Available
PDB Entries Not Available
FDA label Not Available
MSDS Not Available
Interactions
Drug Interactions
Drug Interaction
Digoxin Possible electrolyte variations and arrhythmias
Lithium The thiazide diuretic, polythiazide, may increase serum levels of lithium.
Trandolapril The thiazide diuretic, Polythiazide, may increase the hypotensive effect of Trandolapril. Polythiazide may also increase the nephrotoxicity of Trandolapril. Monitor for postural hypotension at initiation of concomitant therapy and renal dysfunction during chronic therapy.
Treprostinil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Food Interactions Not Available
Targets

1. Solute carrier family 12 member 3

Pharmacological action: yes
Actions: inhibitor

Electrically silent transporter system. Mediates sodium and chloride reabsorption

Organism class: human
UniProt ID: P55017 Link_out
Gene: SLC12A3 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
  2. Monroy A, Plata C, Hebert SC, Gamba G: Characterization of the thiazide-sensitive Na(+)-Cl(-) cotransporter: a new model for ions and diuretics interaction. Am J Physiol Renal Physiol. 2000 Jul;279(1):F161-9. Pubmed
  3. Frindt G, McNair T, Dahlmann A, Jacobs-Palmer E, Palmer LG: Epithelial Na channels and short-term renal response to salt deprivation. Am J Physiol Renal Physiol. 2002 Oct;283(4):F717-26. Pubmed
Comments
Drug created on June 30, 2007 11:21 / Updated on February 08, 2013 16:20