用户名: 密   码:
注册 | 忘记密码?
药品详细

Quinethazone(喹乙宗)

化学结构式图
中文名
喹乙宗
英文名
Quinethazone
分子式
C10H12ClN3O3S
化学名
7-chloro-2-ethyl-4-oxo-1,2,3,4-tetrahydroquinazoline-6-sulfonamide
分子量
Average: 289.739
Monoisotopic: 289.028789662
CAS号
73-49-4
ATC分类
C03B 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Quinethazone (INN, brand name Hydromox) is a thiazide diuretic used to treat hypertension. Common side effects include dizziness, dry mouth, nausea, and low potassium levels.

生产厂家
  • Lederle laboratories div american cyanamid co
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
  • Lactams
Substructures
  • Amino Ketones
  • Sulfonyls
  • Benzene and Derivatives
  • Aryl Halides
  • Carboxylic Acids and Derivatives
  • Benzenesulfonamides
  • Halobenzenes
  • Aminals and Derivatives
  • Heterocyclic compounds
  • Aromatic compounds
  • Carboxamides and Derivatives
  • Sulfanilamides
  • Sulfonamides
  • Lactams
  • Benzoyl Derivatives
  • Benzamides
  • Anilines
适应症
药理
Indication Used to treat hypertension.
Pharmacodynamics Quinethazone is a thiazide diuretic used to treat hypertension. It inhibits Na+/Cl- reabsorption from the distal convoluted tubules in the kidneys. Thiazides also cause loss of potassium and an increase in serum uric acid. Thiazides are often used to treat hypertension, but their hypotensive effects are not necessarily due to their diuretic activity. Thiazides have been shown to prevent hypertension-related morbidity and mortality although the mechanism is not fully understood. Thiazides cause vasodilation by activating calcium-activated potassium channels (large conductance) in vascular smooth muscles and inhibiting various carbonic anhydrases in vascular tissue.
Mechanism of action As a diuretic, quinethazone inhibits active chloride reabsorption at the early distal tubule via the Na-Cl cotransporter, resulting in an increase in the excretion of sodium, chloride, and water. Thiazides like quinethazone 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 quinethazone is less well understood although it 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
Smp00091 Quinethazone Pathway SMP00091
理化性质
Properties
State solid
Experimental Properties
Property Value Source
melting point 251 °C PhysProp
water solubility 150 mg/L (at 25 °C) YALKOWSKY,SH & DANNENFELSER,RM (1992)
Predicted Properties
Property Value Source
water solubility 2.51e+00 g/l ALOGPS
logP 1.6 ALOGPS
logP 1.19 ChemAxon
logS -2.1 ALOGPS
pKa (strongest acidic) 9.56 ChemAxon
pKa (strongest basic) -0.97 ChemAxon
physiological charge 0 ChemAxon
hydrogen acceptor count 4 ChemAxon
hydrogen donor count 3 ChemAxon
polar surface area 101.29 ChemAxon
rotatable bond count 2 ChemAxon
refractivity 69.34 ChemAxon
polarizability 27.3 ChemAxon
药物相互作用
Drug Interaction
Digoxin Possible electrolyte variations and arrhythmias
Lithium The thiazide diuretic, quinethazone, may increase serum levels of lithium.
食物相互作用
  • Take with food to increase bioavailability.

返回 | 收藏