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药品详细

Chlorthalidone(氯噻酮)

化学结构式图
中文名
氯噻酮
英文名
Chlorthalidone
分子式
C14H11ClN2O4S
化学名
2-chloro-5-(1-hydroxy-3-oxo-2,3-dihydro-1H-isoindol-1-yl)benzene-1-sulfonamide
分子量
Average: 338.766
Monoisotopic: 338.012805247
CAS号
77-36-1
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

A benzenesulfonamide-phthalimidine that tautomerizes to a benzophenones form. It is considered a thiazide-like diuretic. [PubChem]

生产厂家
  • Abbott laboratories pharmaceutical products div
  • Ascot hosp pharmaceuticals inc div travenol laboratories inc
  • Clonmel healthcare ltd
  • Ivax pharmaceuticals inc
  • Kv pharmaceutical co
  • Monarch pharmaceuticals inc
  • Mutual pharmaceutical co inc
  • Mylan pharmaceuticals inc
  • Pioneer pharmaceuticals inc
  • Pliva inc
  • Purepac pharmaceutical co
  • Sandoz inc
  • Sanofi aventis us llc
  • Superpharm corp
  • Teva pharmaceuticals usa inc
  • Usl pharma inc
  • Vangard laboratories inc div midway medical co
  • Warner chilcott div warner lambert co
  • Watson laboratories 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
  • Indoles and Indole Derivatives
  • Lactams
  • Benzamides
Substructures
  • Hydroxy Compounds
  • Benzyl Alcohols and Derivatives
  • Amino Ketones
  • Sulfonyls
  • Benzene and Derivatives
  • Aminals and Derivatives
  • Aryl Halides
  • Carboxylic Acids and Derivatives
  • Benzenesulfonamides
  • Halobenzenes
  • Indoles and Indole Derivatives
  • Heterocyclic compounds
  • Aromatic compounds
  • Carboxamides and Derivatives
  • Sulfonamides
  • Lactams
  • Benzoyl Derivatives
  • Benzamides
  • Pyrrolines
适应症
药理
Indication For management of hypertension either as the sole therapeutic agent or to enhance the effect of other antihypertensive drugs in the more severe forms of hypertension.
Pharmacodynamics Chlorthalidone, a monosulfonamyl diuretic, differs form other thiazide diuretics in that a double ring system is incorporated into its structure. Chlorthalidone is used alone or with atenolol in the management of hypertension and edema.
Mechanism of action Chlorthalidone inhibits sodium ion transport across the renal tubular epithelium in the cortical diluting segment of the ascending limb of the loop of Henle. By increasing the delivery of sodium to the distal renal tubule, Chlorthalidone indirectly increases potassium excretion via the sodium-potassium exchange mechanism.
Absorption Absorbed relatively rapidly after oral administration.
Volume of distribution Not Available
Protein binding High (75% [58% to albumin])
Metabolism
Liver
Route of elimination The major portion of the drug is excreted unchanged by the kidneys.
Half life 40 hours
Clearance Not Available
Toxicity Symptoms of overdose include nausea, weakness, dizziness and disturbances of electrolyte balance.
Affected organisms
  • Humans and other mammals
Pathways
Pathway Name SMPDB ID
Smp00122 Chlorthalidone Pathway SMP00122
理化性质
Properties
State solid
Experimental Properties
Property Value Source
melting point 239 °C PhysProp
water solubility 120 mg/L (at 20 °C) MERCK INDEX (1996)
logP 0.85 BERTHOD,A ET AL. (1999)
Predicted Properties
Property Value Source
water solubility 5.28e-02 g/l ALOGPS
logP 1.27 ALOGPS
logP 1.6 ChemAxon
logS -3.8 ALOGPS
pKa (strongest acidic) 8.58 ChemAxon
pKa (strongest basic) -2.6 ChemAxon
physiological charge 0 ChemAxon
hydrogen acceptor count 4 ChemAxon
hydrogen donor count 3 ChemAxon
polar surface area 109.49 ChemAxon
rotatable bond count 2 ChemAxon
refractivity 81.3 ChemAxon
polarizability 31.23 ChemAxon
药物相互作用
Drug Interaction
Deslanoside Possible electrolyte variations and arrhythmias
Diazoxide Significant hyperglycemic effect
Digitoxin Possible electrolyte variations and arrhythmias
Digoxin Possible electrolyte variations and arrhythmias
Dofetilide Increased risk of cardiotoxicity and arrythmias
Indacaterol Concomitant therapy may increase the risk of hypokalemia via intracellular shunting. Monitor for adverse effects and especially for cardiovascular effects associated with hypokalemia.
Lithium The thiazide diuretic, chlorthalidone, may increase serum levels of lithium.
Tenoxicam Tenoxicam may antagonize the blood pressure lowering effect of Chlorthalidone. Monitor for changes in the therapeutic effect of Chlorthalidone if Tenoxicam is initiated, discontinued or dose changed.
Trandolapril The thiazide diuretic, Chlorthalidone, may increase the hypotensive effect of Trandolapril. Chlorthalidone 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
  • Take with food (increases availability).

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