Identification
- Summary
Polythiazide is a thiazide diuretic used in the management of hypertension and treatment of edema.
- Brand Names
- Minizide, Renese, Renese-R
- Generic Name
- Polythiazide
- DrugBank Accession Number
- DB01324
- Background
A thiazide diuretic with actions and uses similar to those of hydrochlorothiazide. (From Martindale, The Extra Pharmacopoeia, 30th ed, p826)
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Polythiazide (DB01324)
- Weight
- Average: 439.882
Monoisotopic: 438.970880311 - Chemical Formula
- C11H13ClF3N3O4S3
- Synonyms
- Polythiazide
Pharmacology
- Indication
Polythiazide is a thiazide diuretic used to decrease edema and decrease blood pressure.
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- Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- 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.
Target Actions Organism ASolute carrier family 12 member 3 inhibitorHumans - 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
- Adverse Effects
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Not Available
- Pathways
Pathway Category Polythiazide Action Pathway Drug action - Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbacavir Polythiazide may increase the excretion rate of Abacavir which could result in a lower serum level and potentially a reduction in efficacy. Abaloparatide Abaloparatide may increase the hypotensive activities of Polythiazide. Abciximab The therapeutic efficacy of Abciximab can be decreased when used in combination with Polythiazide. Acarbose The therapeutic efficacy of Acarbose can be decreased when used in combination with Polythiazide. Acebutolol The therapeutic efficacy of Acebutolol can be increased when used in combination with Polythiazide. - Food Interactions
- Avoid alcohol. Alcohol may potentiate orthostatic hypotension.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Renese Tablet 1 mg/1 Oral Pfizer Labs 2005-12-14 Not applicable US 
Renese Tablet 4 mg/1 Oral Pfizer Labs 2005-12-14 Not applicable US Renese Tablet 2 mg/1 Oral Pfizer Labs 2005-12-14 Not applicable US - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Minizide Polythiazide (0.5 mg/1) + Prazosin hydrochloride (5 mg/1) Capsule Oral Pfizer Labs 2006-10-05 Not applicable US Minizide Polythiazide (0.5 mg/1) + Prazosin hydrochloride (2 mg/1) Capsule Oral Pfizer Labs 2006-10-05 Not applicable US Minizide Polythiazide (0.5 mg/1) + Prazosin hydrochloride (1 mg/1) Capsule Oral Pfizer Labs 2006-10-05 Not applicable US Renese-R Polythiazide (2 mg/1) + Reserpine (25 mg/1) Tablet Oral UNSPECIFIED 2006-02-06 Not applicable US
Categories
- ATC Codes
- C03AA05 — Polythiazide
- C03AA — Thiazides, plain
- C03A — LOW-CEILING DIURETICS, THIAZIDES
- C03 — DIURETICS
- C — CARDIOVASCULAR SYSTEM
- G01AE — Sulfonamides
- G01A — ANTIINFECTIVES AND ANTISEPTICS, EXCL. COMBINATIONS WITH CORTICOSTEROIDS
- G01 — GYNECOLOGICAL ANTIINFECTIVES AND ANTISEPTICS
- G — GENITO URINARY SYSTEM AND SEX HORMONES
- Drug Categories
- Amides
- Antihypertensive Agents
- Antihypertensive Agents Indicated for Hypertension
- Benzothiadiazines
- Cardiovascular Agents
- Diuretics
- Drugs causing inadvertant photosensitivity
- Genito Urinary System and Sex Hormones
- Gynecological Antiinfectives and Antiseptics
- Heterocyclic Compounds, Fused-Ring
- Hyperglycemia-Associated Agents
- Increased Diuresis
- Membrane Transport Modulators
- Natriuretic Agents
- OAT3/SLC22A8 Substrates
- Photosensitizing Agents
- Sodium Chloride Symporter Inhibitors
- Sulfonamides
- Sulfones
- Sulfur Compounds
- Thiazides
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as 1,2,4-benzothiadiazine-1,1-dioxides. These are aromatic heterocyclic compounds containing a 1,2,4-benzothiadiazine ring system with two S=O bonds at the 1-position.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Thiadiazines
- Sub Class
- Benzothiadiazines
- Direct Parent
- 1,2,4-benzothiadiazine-1,1-dioxides
- Alternative Parents
- Secondary alkylarylamines / Organosulfonamides / Benzenoids / Aryl chlorides / Aminosulfonyl compounds / Sulfenyl compounds / Dialkylthioethers / Azacyclic compounds / Organopnictogen compounds / Organofluorides show 4 more
- Substituents
- 1,2,4-benzothiadiazine-1,1-dioxide / Alkyl fluoride / Alkyl halide / Amine / Aminosulfonyl compound / Aromatic heteropolycyclic compound / Aryl chloride / Aryl halide / Azacycle / Benzenoid show 19 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- benzothiadiazine (CHEBI:8327)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 36780APV5N
- CAS number
- 346-18-9
- InChI Key
- 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)
- IUPAC Name
- 6-chloro-2-methyl-1,1-dioxo-3-{[(2,2,2-trifluoroethyl)sulfanyl]methyl}-3,4-dihydro-2H-1lambda6,2,4-benzothiadiazine-7-sulfonamide
- SMILES
- CN1C(CSCC(F)(F)F)NC2=CC(Cl)=C(C=C2S1(=O)=O)S(N)(=O)=O
References
- General References
- Not Available
- External Links
- Human Metabolome Database
- HMDB0015419
- KEGG Drug
- D00657
- KEGG Compound
- C07766
- PubChem Compound
- 4870
- PubChem Substance
- 46508633
- ChemSpider
- 4704
- 8565
- ChEBI
- 8327
- ChEMBL
- CHEMBL1587
- Therapeutic Targets Database
- DAP000751
- PharmGKB
- PA164748763
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Polythiazide
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Pfizer Inc.
- Dosage Forms
Form Route Strength Capsule Oral Tablet Oral 1 mg/1 Tablet Oral 2 mg/1 Tablet Oral 4 mg/1 Tablet Oral - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 214 °C PhysProp logP 1.90 SANGSTER (1994) - Predicted Properties
Property Value Source Water Solubility 0.264 mg/mL 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 Å2 Chemaxon Rotatable Bond Count 5 Chemaxon Refractivity 90.52 m3·mol-1 Chemaxon Polarizability 37.56 Å3 Chemaxon Number of Rings 2 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9884 Blood Brain Barrier - 0.5727 Caco-2 permeable - 0.6601 P-glycoprotein substrate Substrate 0.6985 P-glycoprotein inhibitor I Non-inhibitor 0.7714 P-glycoprotein inhibitor II Non-inhibitor 0.8974 Renal organic cation transporter Non-inhibitor 0.776 CYP450 2C9 substrate Non-substrate 0.6019 CYP450 2D6 substrate Non-substrate 0.8108 CYP450 3A4 substrate Non-substrate 0.5091 CYP450 1A2 substrate Non-inhibitor 0.7786 CYP450 2C9 inhibitor Non-inhibitor 0.5713 CYP450 2D6 inhibitor Non-inhibitor 0.8479 CYP450 2C19 inhibitor Non-inhibitor 0.7738 CYP450 3A4 inhibitor Inhibitor 0.6198 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.6625 Ames test Non AMES toxic 0.9133 Carcinogenicity Non-carcinogens 0.8224 Biodegradation Not ready biodegradable 1.0 Rat acute toxicity 3.3534 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.8884 hERG inhibition (predictor II) Non-inhibitor 0.8734
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS splash10-016v-6598300000-da70dfe63bf7c73c6097 Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-000i-0000900000-1f40bed1856f91ab8dd6 Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-000i-0000900000-1b28691ebe78d549eb4b Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-00kr-1005900000-f6f0171070ec8783d766 Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-0079-1100900000-af58e7b7db92191d5bef Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-0059-9031000000-1ad13c618ac499e30f6b Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-0006-1249300000-2777775b40a5c59c58cb Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 186.8673992 predictedDarkChem Lite v0.1.0 [M-H]- 195.50897 predictedDeepCCS 1.0 (2019) [M+H]+ 187.6533992 predictedDarkChem Lite v0.1.0 [M+H]+ 198.70338 predictedDeepCCS 1.0 (2019) [M+Na]+ 187.2385992 predictedDarkChem Lite v0.1.0 [M+Na]+ 207.44925 predictedDeepCCS 1.0 (2019)
Targets
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Transporter activity
- Specific Function
- Key mediator of sodium and chloride reabsorption in this nephron segment, accounting for a significant fraction of renal sodium reabsorption.
- Gene Name
- SLC12A3
- Uniprot ID
- P55017
- Uniprot Name
- Solute carrier family 12 member 3
- Molecular Weight
- 113138.04 Da
References
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- 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. [Article]
- 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. [Article]
- Gamba G: The thiazide-sensitive Na+-Cl- cotransporter: molecular biology, functional properties, and regulation by WNKs. Am J Physiol Renal Physiol. 2009 Oct;297(4):F838-48. doi: 10.1152/ajprenal.00159.2009. Epub 2009 May 27. [Article]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Binder
- General Function
- Toxic substance binding
- Specific Function
- Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
- Gene Name
- ALB
- Uniprot ID
- P02768
- Uniprot Name
- Serum albumin
- Molecular Weight
- 69365.94 Da
References
- Duarte JD, Cooper-DeHoff RM: Mechanisms for blood pressure lowering and metabolic effects of thiazide and thiazide-like diuretics. Expert Rev Cardiovasc Ther. 2010 Jun;8(6):793-802. doi: 10.1586/erc.10.27. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Involved in the renal elimination of endogenous and exogenous organic anions. Functions as organic anion exchanger when the uptake of one molecule of organic anion is coupled with an efflux of one ...
- Gene Name
- SLC22A6
- Uniprot ID
- Q4U2R8
- Uniprot Name
- Solute carrier family 22 member 6
- Molecular Weight
- 61815.78 Da
References
- Vallon V, Rieg T, Ahn SY, Wu W, Eraly SA, Nigam SK: Overlapping in vitro and in vivo specificities of the organic anion transporters OAT1 and OAT3 for loop and thiazide diuretics. Am J Physiol Renal Physiol. 2008 Apr;294(4):F867-73. doi: 10.1152/ajprenal.00528.2007. Epub 2008 Jan 23. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Plays an important role in the excretion/detoxification of endogenous and exogenous organic anions, especially from the brain and kidney. Involved in the transport basolateral of steviol, fexofenad...
- Gene Name
- SLC22A8
- Uniprot ID
- Q8TCC7
- Uniprot Name
- Solute carrier family 22 member 8
- Molecular Weight
- 59855.585 Da
References
- Vallon V, Rieg T, Ahn SY, Wu W, Eraly SA, Nigam SK: Overlapping in vitro and in vivo specificities of the organic anion transporters OAT1 and OAT3 for loop and thiazide diuretics. Am J Physiol Renal Physiol. 2008 Apr;294(4):F867-73. doi: 10.1152/ajprenal.00528.2007. Epub 2008 Jan 23. [Article]
Drug created at June 30, 2007 17:21 / Updated at February 21, 2021 18:51