Tìm theo
Hydroflumethiazide
Các tên gọi khác (9 ) :
  • Dihydroflumethazide
  • Hidroflumetiazid
  • Hidroflumetiazida
  • Hydrofluméthiazide
  • Hydroflumethiazide
  • Hydroflumethiazidum
  • Idroflumetiazide
  • Metforylthiadiazin
  • Saluron
antihypertensive agents, diuretics, sodium chloride symporter inhibitors
Thuốc Gốc
Small Molecule
CAS: 135-09-1
ATC: C03AA02
ĐG : Shire Inc. , http://www.shire.com
CTHH: C8H8F3N3O4S2
PTK: 331.292
A thiazide diuretic with actions and uses similar to those of hydrochlorothiazide. (From Martindale, The Extra Pharmacopoeia, 30th ed, p822)
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C8H8F3N3O4S2
Phân tử khối
331.292
Monoisotopic mass
330.990831754
InChI
InChI=1S/C8H8F3N3O4S2/c9-8(10,11)4-1-5-7(2-6(4)19(12,15)16)20(17,18)14-3-13-5/h1-2,13-14H,3H2,(H2,12,15,16)
InChI Key
InChIKey=DMDGGSIALPNSEE-UHFFFAOYSA-N
IUPAC Name
1,1-dioxo-6-(trifluoromethyl)-3,4-dihydro-2H-1$l^{6},2,4-benzothiadiazine-7-sulfonamide
Traditional IUPAC Name
hydroflumethiazide
SMILES
NS(=O)(=O)C1=CC2=C(NCNS2(=O)=O)C=C1C(F)(F)F
Độ tan chảy
272-273
Độ hòa tan
300 mg/L (at 25 °C)
logP
0.36
logS
-2.6
pKa (strongest acidic)
9.07
pKa (Strongest Basic)
-2.7
PSA
118.36 Å2
Refractivity
64.28 m3·mol-1
Polarizability
25.68 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
5
H Bond Donor Count
3
Physiological Charge
0
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
pKa
8.9
Dược Lực Học : Hydroflumethiazide is an oral thiazide used to treat hypertension and edema. High blood pressure adds to the workload of the heart and arteries. If it continues for a long time, the heart and arteries may not function properly. This can damage the blood vessels of the brain, heart, and kidneys, resulting in a stroke, heart failure, or kidney failure. High blood pressure may also increase the risk of heart attacks. Like other thiazides, Hydroflumethiazide promotes water loss from the body (diuretics). Thiazides inhibit 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. (From Martindale, The Extra Pharmacopoeia, 30th ed, p822) Hydroflumethiazide is a thiazide diuretic that inhibits water reabsorption in the nephron by inhibiting the sodium-chloride symporter (SLC12A3) in the distal convoluted tubule, which is responsible for 5% of total sodium reabsorption. Normally, the sodium-chloride symporter transports sodium and chloride from the lumen into the epithelial cell lining the distal convoluted tubule. The energy for this is provided by a sodium gradient established by sodium-potassium ATPases on the basolateral membrane. Once sodium has entered the cell, it is transported out into the basolateral interstitium via the sodium-potassium ATPase, causing an increase in the osmolarity of the interstitium, thereby establishing an osmotic gradient for water reabsorption. By blocking the sodium-chloride symporter, Hydroflumethiazide effectively reduces the osmotic gradient and water reabsorption throughout the nephron.
Dược Động Học :
▧ Absorption :
Hydroflumethiazide is incompletely but fairly rapidly absorbed from the gastrointestinal tract
▧ Protein binding :
74%
▧ Metabolism :
Essentially unchanged
▧ Half Life :
It appears to have a biphasic biological half-life with an estimated alpha-phase of about 2 hours and an estimated beta-phase of about 17 hours
Độc Tính : Overdoses lead to diuresis, lethargy progressing to coma, with minimal cardiorespiratory depression and with or without significant serum electrolyte changes or dehydration.
Chỉ Định : Used as adjunctive therapy in edema associated with congestive heart failure, hepatic cirrhosis, and corticosteroid and estrogen therapy. Also used in the 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 :
  • Digoxin Possible electrolyte variations and arrhythmias
  • Lithium The thiazide diuretic, hydroflumethiazide, may increase serum levels of lithium.
  • Trandolapril The thiazide diuretic, Hydroflumethiazide, may increase the hypotensive effect of Trandolapril. Hydroflumethiazide 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
Nhà Sản Xuất
  • Công ty : Leo
    Sản phẩm biệt dược : Leodrine
  • Công ty : Shire
    Sản phẩm biệt dược : Saluron
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00774
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3647
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505220
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07763
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00654
ChemSpider
http://www.chemspider.com/Chemical-Structure.3521.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=25897
PharmGKB
http://www.pharmgkb.org/drug/PA164752557
RxList
http://www.rxlist.com/cgi/generic2/hydroflumethiazide.htm
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