Tìm theo
Metolazone
Các tên gọi khác (8 ) :
  • 2-Methyl-3-O-tolyl-6-sulfamyl-7-chloro-1,2,3,4-tetrahydro-4-quinazolinone
  • 7-Chloro-1,2,3,4-tetrahydro-2-methyl-3-(2-methylphenyl)-4-oxo-6-quinazolinesulfonamide
  • 7-Chloro-1,2,3,4-tetrahydro-2-methyl-4-oxo-3-O-tolyl-6-quinazolinesulfonamide
  • Metolazon
  • Metolazona
  • Métolazone
  • Metolazonum
  • Zaroxolyn
antihypertensive agents, diuretics, sodium chloride symporter inhibitors
Thuốc Gốc
Small Molecule
CAS: 17560-51-9
ATC: C03BA08
ĐG : Amerisource Health Services Corp. , http://www.amerisourcebergen.com
CTHH: C16H16ClN3O3S
PTK: 365.835
A quinazoline-sulfonamide that is considered a thiazide-like diuretic which is long-acting so useful in chronic renal failure. It also tends to lower blood pressure and increase potassium loss. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C16H16ClN3O3S
Phân tử khối
365.835
Monoisotopic mass
365.06008979
InChI
InChI=1S/C16H16ClN3O3S/c1-9-5-3-4-6-14(9)20-10(2)19-13-8-12(17)15(24(18,22)23)7-11(13)16(20)21/h3-8,10,19H,1-2H3,(H2,18,22,23)
InChI Key
InChIKey=AQCHWTWZEMGIFD-UHFFFAOYSA-N
IUPAC Name
7-chloro-2-methyl-3-(2-methylphenyl)-4-oxo-1,2,3,4-tetrahydroquinazoline-6-sulfonamide
Traditional IUPAC Name
metolazone
SMILES
CC1NC2=CC(Cl)=C(C=C2C(=O)N1C1=CC=CC=C1C)S(N)(=O)=O
Độ tan chảy
256 °C
Độ hòa tan
60.3 mg/L (at 25 °C)
logP
2.5
logS
-3.78
pKa (strongest acidic)
9.54
pKa (Strongest Basic)
-1.6
PSA
92.5 Å2
Refractivity
94.59 m3·mol-1
Polarizability
36.38 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
4
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Metolazone is a quinazoline diuretic, with properties generally similar to the thiazide diuretics. A proximal action of metolazone has been shown in humans by increased excretion of phosphate and magnesium ions and by a markedly increased fractional excretion of sodium in patients with severely compromised glomerular filtration. This action has been demonstrated in animals by micropuncture studies.
Cơ Chế Tác Dụng : A quinazoline-sulfonamide that is considered a thiazide-like diuretic which is long-acting so useful in chronic renal failure. It also tends to lower blood pressure and increase potassium loss. [PubChem] The actions of metolazone result from interference with the renal tubular mechanism of electrolyte reabsorption. Metolazone acts primarily to inhibit sodium reabsorption at the cortical diluting site and to a lesser extent in the proximal convoluted tubule. Sodium and chloride ions are excreted in approximately equivalent amounts. The increased delivery of sodium to the distal tubular exchange site results in increased potassium excretion. Metolazone does not inhibit carbonic anhydrase. The antihypertensive mechanism of action of metolazone is not fully understood but is presumed to be related to its saluretic and diuretic properties.
Dược Động Học :
▧ Absorption :
Peak blood levels are obtained within 2 to 4 hours of oral administration. The rate and extent of absorption are formulation dependent.
▧ Protein binding :
50-70% bound to erythrocytes, up to 33% bound to plasma proteins, 2-5% of the drug in circulation is unbound
▧ Metabolism :
Not substantially metabolized. 70-95% is excreted unchanged in urine via glomerular filtration and active tubular secretion. Undergoes enterohepatic recycling.
▧ Route of Elimination :
Most of the drug is excreted in the unconverted form in the urine.
▧ Half Life :
Approximately 14 hours.
Độc Tính : Symptoms of overdose include difficulty breathing, dizziness, dizziness on standing up, drowsiness, fainting, irritation of the stomach and intestines, and lethargy leading to coma.
Chỉ Định : For the treatment of hypertension, alone or in combination with other antihypertensive drugs of a different class.
Tương Tác Thuốc :
  • Deslanoside Possible electrolyte variations and arrhythmias
  • Digitoxin Possible electrolyte variations and arrhythmias
  • Digoxin Possible electrolyte variations and arrhythmias
  • Dofetilide Increased risk of cardiotoxicity and arrhythmias
  • Lithium The thiazide diuretic, metolazone, may increase serum levels of lithium.
  • Tenoxicam Tenoxicam may antagonize the blood pressure lowering effect of Metolazone. Monitor for changes in the therapeutic effect of Metolazone if Tenoxicam is initiated, discontinued or dose changed.
  • Trandolapril The thiazide diuretic, Metolazone, may increase the hypotensive effect of Trandolapril. Metolazone 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 - 10 mg
Tablet - Oral - 2.5 mg
Tablet - Oral - 5 mg
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Diulo
  • Công ty : Cipla
    Sản phẩm biệt dược : Diurem
  • Công ty : Micro Labs
    Sản phẩm biệt dược : Metadure
  • Công ty : IFET
    Sản phẩm biệt dược : Metenix
  • Công ty : Navana
    Sản phẩm biệt dược : Metolaz
  • Công ty : Sandoz
    Sản phẩm biệt dược : Metolazone
  • Công ty : Dr. Reddy's
    Sản phẩm biệt dược : Metoral
  • Công ty : Centaur
    Sản phẩm biệt dược : Metoz
  • Công ty : Ying Yuan
    Sản phẩm biệt dược : Metozone
  • Công ty : Celltech
    Sản phẩm biệt dược : Mykrox
  • Công ty : Pharma Investi
    Sản phẩm biệt dược : Pavedal
  • Công ty : sanofi-aventis
    Sản phẩm biệt dược : Zaroxolyn
  • Công ty : Zydus
    Sản phẩm biệt dược : Zytanix
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00524
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=4170
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46509058
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00431
ChemSpider
http://www.chemspider.com/Chemical-Structure.4026.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=25899
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0378-6172-01
PharmGKB
http://www.pharmgkb.org/drug/PA164781022
Wikipedia
http://en.wikipedia.org/wiki/Metolazone
RxList
http://www.rxlist.com/cgi/generic2/metolazone.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/zar1495.shtml
Drugs.com
http://www.drugs.com/cdi/metolazone.html
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