Tìm theo
Furosemide
Các tên gọi khác (11 ) :
  • 2-Furfurylamino-4-chloro-5-sulfamoylbenzoic acid
  • 4-Chloro-5-sulfamoyl-N-furfuryl-anthranilic acid
  • 4-Chloro-N-(2-furylmethyl)-5-sulfamoylanthranilic acid
  • 4-Chloro-N-furfuryl-5-sulfamoylanthranilic acid
  • Frusemide
  • Furosemid
  • Furosemida
  • Furosemide
  • Furosemidu
  • Furosemidum
  • Lasix (tn)
Thuốc lợi tiểu
Thuốc Gốc
Small Molecule
CAS: 54-31-9
ĐG : Advanced Pharmaceutical Services Inc.
CTHH: C12H11ClN2O5S
PTK: 330.744
A benzoic-sulfonamide-furan. It is a diuretic with fast onset and short duration that is used for edema and chronic renal insufficiency. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C12H11ClN2O5S
Phân tử khối
330.744
Monoisotopic mass
330.007719869
InChI
InChI=1S/C12H11ClN2O5S/c13-9-5-10(15-6-7-2-1-3-20-7)8(12(16)17)4-11(9)21(14,18)19/h1-5,15H,6H2,(H,16,17)(H2,14,18,19)
InChI Key
InChIKey=ZZUFCTLCJUWOSV-UHFFFAOYSA-N
IUPAC Name
4-chloro-2-[(furan-2-ylmethyl)amino]-5-sulfamoylbenzoic acid
Traditional IUPAC Name
furosemide
SMILES
NS(=O)(=O)C1=C(Cl)C=C(NCC2=CC=CO2)C(=C1)C(O)=O
Độ tan chảy
206
Độ hòa tan
73.1 mg/L (at 30 °C)
logP
2.03
logS
-3.66
pKa (strongest acidic)
4.25
pKa (Strongest Basic)
-1.5
PSA
122.63 Å2
Refractivity
77.47 m3·mol-1
Polarizability
30.55 Å3
Rotatable Bond Count
5
H Bond Acceptor Count
5
H Bond Donor Count
3
Physiological Charge
-1
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
caco2 Permeability
-6.5
Dược Lực Học : Furosemide, a sulfonamide-type loop diuretic structurally related to bumetanide, is used to manage hypertension and edema associated with congestive heart failure, cirrhosis, and renal disease, including the nephrotic syndrome.
Cơ Chế Tác Dụng : A benzoic-sulfonamide-furan. It is a diuretic with fast onset and short duration that is used for edema and chronic renal insufficiency. [PubChem] Furosemide, a loop diuretic, inhibits water reabsorption in the nephron by blocking the sodium-potassium-chloride cotransporter (NKCC2) in the thick ascending limb of the loop of Henle. This is achieved through competitive inhibition at the chloride binding site on the cotransporter, thus preventing the transport of sodium from the lumen of the loop of Henle into the basolateral interstitium. Consequently, the lumen becomes more hypertonic while the interstitium becomes less hypertonic, which in turn diminishes the osmotic gradient for water reabsorption throughout the nephron. Because the thick ascending limb is responsible for 25% of sodium reabsorption in the nephron, furosemide is a very potent diuretic.
Dược Động Học :
▧ Absorption :
60% absorbed in patients with normal renal function
▧ Protein binding :
95% bound to plasma proteins
▧ Metabolism :
Only a small amount is hepatically metabolized to the defurfurylated derivative, 4-chloro-5-sulfamoylanthranilic acid.
▧ Route of Elimination :
Furosemide is excreted in urine. Significantly more furosemide is excreted in urine following the I.V. injection than after the tablet or oral solution.
▧ Half Life :
2 hours
Độc Tính : Profound diuresis may cause fluid and electrolyte depletion. Excessive dehydration and potassium depletion may occur. Excessive diuresis may cause rapid weight loss, orthostatic hypotension or acute hypotensive episodes. May also cause tinnitus, reversible or permanent hearing loss or reversible deafness.
Chỉ Định : For the treatment of edema associated with congestive heart failure, cirrhosis of the liver, and renal disease, including the nephrotic syndrome. Also for the treatment of hypertension alone or in combination with other antihypertensive agents.
Tương Tác Thuốc :
  • Aliskiren Monitor therapy due to potential decreased serum concentration of furosemide.
  • Amikacin Increased ototoxicity
  • Cisplatin Increased ototoxicity
  • Colesevelam Bile acid sequestrants such as colesevelam may decrease the absorption of loop diuretics such as furosemide. Monitor for decreased serum concentrations/therapeutic effects of loop diuretics if coadministered with bile acid sequestrants. Separating the administration of doses by 2 or more hours may reduce (but not eliminate) the risk of interaction. The manufacturer of colesevelam recommends that drugs should be administered at least 1 hour before or 4 hours after colesevelam.
  • Deslanoside Possible electrolyte variations and arrhythmias
  • Digitoxin Possible electrolyte variations and arrhythmias
  • Digoxin Possible electrolyte variations and arrhythmias
  • Ethotoin The hydantoin decreases the effect of furosemide
  • Fosphenytoin The hydantoin decreases the effect of furosemide
  • Gentamicin Increased ototoxicity
  • Ginseng Ginseng decreases the therapeutic effect
  • Ibuprofen The NSAID, ibuprofen, may antagonize the diuretic and antihypertensive effects of the loop diuretic, furosemide.
  • Indacaterol Concomitant therapy may increase the risk of hypokalemia via intracellular shunting. Monitor for adverse effects and especially for cardiovascular effects associated with hypokalemia.
  • Indomethacin The NSAID, indomethacin, may decrease the diuretic and antihypertensive effects of the loop diuretic, furosemide.
  • Kanamycin Increased ototoxicity
  • Mephenytoin The hydantoin decreases the effect of furosemide
  • Netilmicin Increased ototoxicity
  • Phenytoin The hydantoin decreases the effect of furosemide
  • Streptomycin Increased ototoxicity
  • Sulindac The NSAID, sulindac, may decrease the diuretic and antihypertensive effects of the loop diuretic, furosemide.
  • Tobramycin Increased ototoxicity
  • Trandolapril The loop diuretic, Furosemide, may increase the hypotensive effect of Trandolapril. Furosemide may also increase the nephrotoxicity of Trandolapril.
  • Treprostinil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Liều Lượng & Cách Dùng : Liquid - Intramuscular
Solution - Intravenous
Solution - Oral
Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Mibe Jena
    Sản phẩm biệt dược : Diurapid
  • Công ty : Mylan
    Sản phẩm biệt dược : Diurin
  • Công ty : Biomep
    Sản phẩm biệt dược : Diurmessel
  • Công ty : Sanofi
    Sản phẩm biệt dược : Eutensin
  • Công ty :
    Sản phẩm biệt dược : Frumex
  • Công ty :
    Sản phẩm biệt dược : Frusenex
  • Công ty : Rosemont
    Sản phẩm biệt dược : Frusol
  • Công ty : Actavis
    Sản phẩm biệt dược : Furo-Puren
  • Công ty : Sanofi
    Sản phẩm biệt dược : Lasix
  • Công ty : Sanofi
    Sản phẩm biệt dược : Seguril
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00695
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3440
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506779
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00331
ChemSpider
http://www.chemspider.com/Chemical-Structure.3322.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=25902
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0548-1431-00
PharmGKB
http://www.pharmgkb.org/drug/PA449719
Wikipedia
http://en.wikipedia.org/wiki/Furosemide
RxList
http://www.rxlist.com/cgi/generic/furos.htm
Drugs.com
http://www.drugs.com/furosemide.html
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