Tìm theo
Chlorthalidone
Các tên gọi khác (11 ) :
  • 1-keto-3-(3'-Sulfamyl-4'-chlorophenyl)-3-hydroxyisoindoline
  • 1-oxo-3-(3-Sulfamyl-4-chlorophenyl)-3-hydroxyisoindoline
  • 2-chloro-5-(1-Hydroxy-3-oxo-1-isoindolinyl)benzenesulfonamide
  • 2-chloro-5-(2,3-dihydro-1-Hydroxy-3-oxo-1H-isoindol-1-yl)benzenesulfonamide
  • 3-(4'-chloro-3'-Sulfamoylphenyl)-3-hydroxyphthalimidine
  • 3-Hydroxy-3-(4-chloro-3-sulfamylphenyl)phthalimidine
  • Chlorphthalidolone
  • Chlortalidone
  • Chlorthalidone
  • Phthalamodine
  • Phthalamudine
antihypertensive agents, diuretics, sodium chloride symporter inhibitors
Thuốc Gốc
Small Molecule
CAS: 77-36-1
ATC: C03BA04
ĐG : Advanced Pharmaceutical Services Inc.
CTHH: C14H11ClN2O4S
PTK: 338.766
A benzenesulfonamide-phthalimidine that tautomerizes to a benzophenones form. It is considered a thiazide-like diuretic. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C14H11ClN2O4S
Phân tử khối
338.766
Monoisotopic mass
338.012805247
InChI
InChI=1S/C14H11ClN2O4S/c15-11-6-5-8(7-12(11)22(16,20)21)14(19)10-4-2-1-3-9(10)13(18)17-14/h1-7,19H,(H,17,18)(H2,16,20,21)
InChI Key
InChIKey=JIVPVXMEBJLZRO-UHFFFAOYSA-N
IUPAC Name
2-chloro-5-(1-hydroxy-3-oxo-2,3-dihydro-1H-isoindol-1-yl)benzene-1-sulfonamide
Traditional IUPAC Name
chlorthalidone
SMILES
NS(=O)(=O)C1=C(Cl)C=CC(=C1)C1(O)NC(=O)C2=CC=CC=C12
Độ tan chảy
239 °C
Độ hòa tan
120 mg/L (at 20 °C)
logP
0.85
logS
-3.8
pKa (strongest acidic)
8.58
pKa (Strongest Basic)
-2.6
PSA
109.49 Å2
Refractivity
81.3 m3·mol-1
Polarizability
31.23 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
4
H Bond Donor Count
3
Physiological Charge
0
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : 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.
Cơ Chế Tác Dụng : A benzenesulfonamide-phthalimidine that tautomerizes to a benzophenones form. It is considered a thiazide-like diuretic. [PubChem] 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.
Dược Động Học :
▧ Absorption :
Absorbed relatively rapidly after oral administration.
▧ 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
Độc Tính : Symptoms of overdose include nausea, weakness, dizziness and disturbances of electrolyte balance.
Chỉ Định : 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.
Tương Tác Thuốc :
  • 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.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Novartis
    Sản phẩm biệt dược : Hygroton
  • Công ty : Balkanpharma
    Sản phẩm biệt dược : Saluretin
  • Công ty : Monarch
    Sản phẩm biệt dược : Thalitone
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00310
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=2732
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505541
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00272
ChemSpider
http://www.chemspider.com/Chemical-Structure.2631.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=25900
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0179-0015-01
PharmGKB
http://www.pharmgkb.org/drug/PA448970
Wikipedia
http://en.wikipedia.org/wiki/Chlorthalidone
RxList
http://www.rxlist.com/cgi/generic3/chlorthalidone.htm
Drugs.com
http://www.drugs.com/cdi/chlorthalidone.html
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