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药品详细

Polythiazide(噻)

化学结构式图
中文名
英文名
Polythiazide
分子式
C11H13ClF3N3O4S3
化学名
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
分子量
Average: 439.882
Monoisotopic: 438.970880311
CAS号
346-18-9
ATC分类
C03A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

A thiazide diuretic with actions and uses similar to those of hydrochlorothiazide. (From Martindale, The Extra Pharmacopoeia, 30th ed, p826)

生产厂家
  • Pfizer inc
封装厂家
参考
Synthesis Reference Not Available
General Reference Not Available
剂型
规格
化合物类型
Type small molecule
Classes
  • Benzenesulfonamides
  • Sulfanilamides
Substructures
  • Ethers
  • Sulfonyls
  • Benzene and Derivatives
  • Aryl Halides
  • Benzenesulfonamides
  • Halobenzenes
  • Aminals and Derivatives
  • Heterocyclic compounds
  • Aromatic compounds
  • Thiadiazines
  • Sulfanilamides
  • Sulfonamides
  • Anilines
适应症
药理
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
理化性质
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
药物相互作用
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.
食物相互作用
Not Available

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