Tìm theo
Diazoxide
Các tên gọi khác (5 ) :
  • Diazossido
  • Diazoxide
  • Diazoxido
  • Diazoxidum
  • Eudemine
sodium chloride symporter inhibitors
Thuốc Gốc
Small Molecule
CAS: 364-98-7
ATC: C02DA01, V03AH01
ĐG : Ivax Pharmaceuticals
CTHH: C8H7ClN2O2S
PTK: 230.671
A benzothiadiazine derivative that is a peripheral vasodilator used for hypertensive emergencies. It lacks diuretic effect, apparently because it lacks a sulfonamide group. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C8H7ClN2O2S
Phân tử khối
230.671
Monoisotopic mass
229.991675875
InChI
InChI=1S/C8H7ClN2O2S/c1-5-10-7-3-2-6(9)4-8(7)14(12,13)11-5/h2-4H,1H3,(H,10,11)
InChI Key
InChIKey=GDLBFKVLRPITMI-UHFFFAOYSA-N
IUPAC Name
7-chloro-3-methyl-4H-1$l^{6},2,4-benzothiadiazine-1,1-dione
Traditional IUPAC Name
diazoxide
SMILES
CC1=NS(=O)(=O)C2=C(N1)C=CC(Cl)=C2
Độ tan chảy
330
Độ hòa tan
2850 mg/L
logP
1.20
logS
-2.6
pKa (strongest acidic)
10.48
pKa (Strongest Basic)
1.33
PSA
58.53 Å2
Refractivity
54.84 m3·mol-1
Polarizability
20.98 Å3
Rotatable Bond Count
0
H Bond Acceptor Count
4
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
pKa
8.74
Dược Lực Học : Diazoxide is a potassium channel activator, which causes local relaxation in smooth muscle by increasing membrane permeability to potassium ions. This switches off voltage-gated calcium ion channels which inhibits the generation of an action potential.
Cơ Chế Tác Dụng : A benzothiadiazine derivative that is a peripheral vasodilator used for hypertensive emergencies. It lacks diuretic effect, apparently because it lacks a sulfonamide group. [PubChem] As a diuretic, diazoxide 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 diazoxide 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 diazoxide 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. As a antihypoglycemic, diazoxide inhibits insulin release from the pancreas, probably by opening potassium channels in the beta cell membrane.
Dược Động Học :
▧ Absorption :
Readily absorbed following oral administration.
▧ Protein binding :
Very high (more than 90%) to serum proteins.
▧ Metabolism :
Hepatic.
▧ Route of Elimination :
Proglycem is extensively bound (more than 90%) to serum proteins, and is excreted in the kidneys.
▧ Half Life :
28 ±8.3 hours in normal adults.
Độc Tính : Oral LD50 in rat and mouse: 980 mg/kg and 444 mg/kg, respectively.
Chỉ Định : Used parentally to treat hypertensive emergencies. Also used to treat hypoglycemia secondary to insulinoma.
Tương Tác Thuốc :
Liều Lượng & Cách Dùng : Capsule - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Mercury
    Sản phẩm biệt dược : Eudemine
  • Công ty : Schering
    Sản phẩm biệt dược : Hyperstat
  • Công ty : Gate
    Sản phẩm biệt dược : Proglycem
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01119
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3019
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508027
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C06949
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00294
ChemSpider
http://www.chemspider.com/Chemical-Structure.2911.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0575-6000-01
PharmGKB
http://www.pharmgkb.org/drug/PA449285
Wikipedia
http://en.wikipedia.org/wiki/Diazoxide
Drugs.com
http://www.drugs.com/cdi/diazoxide-suspension.html
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