Tìm theo
Bendroflumethiazide
Các tên gọi khác (8 ) :
  • +--3-Benzyl-3,4-dihydro-6-(trifluoromethyl)-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide
  • 6-Trifluoromethyl-3-benzyl-7-sulfamyl-3,4-dihydro-1,2,4-benzothiadiazine 1,1-dioxide
  • Bendrofluazide
  • Bendroflumethiazid
  • Bendrofluméthiazide
  • Bendroflumethiazidum
  • Bendroflumetiazida
  • Benzhydroflumethiazide
antihypertensive agents, diuretics, sodium chloride symporter inhibitors
Thuốc Gốc
Small Molecule
CAS: 73-48-3
ATC: C03AA01
ĐG : E.R. Squibb and Sons LLC
CTHH: C15H14F3N3O4S2
PTK: 421.415
A thiazide diuretic with actions and uses similar to those of hydrochlorothiazide. It has been used in the treatment of familial hyperkalemia, hypertension, edema, and urinary tract disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p810)
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C15H14F3N3O4S2
Phân tử khối
421.415
Monoisotopic mass
421.037781946
InChI
InChI=1S/C15H14F3N3O4S2/c16-15(17,18)10-7-11-13(8-12(10)26(19,22)23)27(24,25)21-14(20-11)6-9-4-2-1-3-5-9/h1-5,7-8,14,20-21H,6H2,(H2,19,22,23)
InChI Key
InChIKey=HDWIHXWEUNVBIY-UHFFFAOYSA-N
IUPAC Name
3-benzyl-1,1-dioxo-6-(trifluoromethyl)-3,4-dihydro-2H-1$l^{6},2,4-benzothiadiazine-7-sulfonamide
Traditional IUPAC Name
bendroflumethiazide
SMILES
NS(=O)(=O)C1=CC2=C(NC(CC3=CC=CC=C3)NS2(=O)=O)C=C1C(F)(F)F
Độ tan chảy
222-223 °C
Độ hòa tan
108 mg/L (at 25 °C)
logP
1.89
logS
-3.59
pKa (strongest acidic)
9.04
pKa (Strongest Basic)
-3.1
PSA
118.36 Å2
Refractivity
93.68 m3·mol-1
Polarizability
36.92 Å3
Rotatable Bond Count
4
H Bond Acceptor Count
5
H Bond Donor Count
3
Physiological Charge
0
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
pKa
8.5
Dược Lực Học : Bendroflumethiazide, a thiazide diuretic, removes excess water from the body by increasing how often you urinate (pass water) and also widens the blood vessels which helps to reduce blood pressure. 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.
Cơ Chế Tác Dụng : A thiazide diuretic with actions and uses similar to those of hydrochlorothiazide. It has been used in the treatment of familial hyperkalemia, hypertension, edema, and urinary tract disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p810) As a diuretic, bendroflumethiazide 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 bendroflumethiazide 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 bendroflumethiazide 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.
Dược Động Học :
▧ Absorption :
Absorbed relatively rapidly after oral administration
▧ Protein binding :
96%
▧ Half Life :
8.5 hours
Chỉ Định : For the treatment of high blood pressure and management of edema related to heart failure.
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 arrhythmias
  • Lithium The thiazide diuretic, bendroflumethiazide, may increase serum levels of lithium.
  • Trandolapril The thiazide diuretic, Bendroflumethiazide, may increase the hypotensive effect of Trandolapril. Bendroflumethiazide 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.
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Sản phẩm biệt dược : Aprinox
  • Công ty : LEO Pharma
    Sản phẩm biệt dược : Centyl
  • Công ty :
    Sản phẩm biệt dược : Naturetin
  • Công ty : GlaxoSmithKline
    Sản phẩm biệt dược : Neo-Naclex
  • Công ty : Pfizer
    Sản phẩm biệt dược : Salures
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00436
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=2315
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508672
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07758
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00650
ChemSpider
http://www.chemspider.com/Chemical-Structure.2225.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0003-0606-50
PharmGKB
http://www.pharmgkb.org/drug/PA448563
Wikipedia
http://en.wikipedia.org/wiki/Bendroflumethiazide
Drugs.com
http://www.drugs.com/cdi/bendroflumethiazide.html
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