Tìm theo
Tolazamide
Các tên gọi khác (17 ) :
  • 1-(hexahydro-1-Azepinyl)-3-P-tolylsulfonylurea
  • 1-(hexahydro-1H-Azepin-1-yl)-3-(P-tolylsulfonyl)urea
  • 4-(P-Tolylsulfonyl)-1,1-hexamethylenesemicarbazide
  • BRN 1323565
  • CCRIS 591
  • Diabewas
  • EINECS 214-588-3
  • N-(P-Toluenesulfonyl)-n'-hexamethyleniminourea
  • N-{[(hexahydro-1H-azepin-1-yl)-amino]carbonyl}-4-methylbenzenesulfonamide
  • Norglycin
  • Tolazamid
  • Tolazamida
  • Tolazamide
  • Tolazamidum
  • Tolinase
  • U 17835
  • U-17835
Thuốc Gốc
Small Molecule
CAS: 1156-19-0
ATC: A10BB05
ĐG : Apotheca Inc.
CTHH: C14H21N3O3S
PTK: 311.4
A sulphonylurea hypoglycemic agent with actions and uses similar to those of chlorpropamide. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C14H21N3O3S
Phân tử khối
311.4
Monoisotopic mass
311.130362243
InChI
InChI=1S/C14H21N3O3S/c1-12-6-8-13(9-7-12)21(19,20)16-14(18)15-17-10-4-2-3-5-11-17/h6-9H,2-5,10-11H2,1H3,(H2,15,16,18)
InChI Key
InChIKey=OUDSBRTVNLOZBN-UHFFFAOYSA-N
IUPAC Name
1-(azepan-1-yl)-3-[(4-methylbenzene)sulfonyl]urea
Traditional IUPAC Name
1-(azepan-1-yl)-3-(4-methylbenzenesulfonyl)urea
SMILES
CC1=CC=C(C=C1)S(=O)(=O)NC(=O)NN1CCCCCC1
Độ tan chảy
170-173 °C
Độ hòa tan
65.4 mg/L (at 30 °C)
logP
2.69
logS
-3.68
pKa (strongest acidic)
4.07
pKa (Strongest Basic)
1.61
PSA
78.51 Å2
Refractivity
81.34 m3·mol-1
Polarizability
32.82 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
4
H Bond Donor Count
2
Physiological Charge
-1
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Tolazamide is an oral blood glucose lowering drug of the sulfonylurea class. Tolazamide appears to lower the blood glucose acutely by stimulating the release of insulin from the pancreas, an effect dependent upon functioning beta cells in the pancreatic islets. The mechanism by which tolazamide lowers blood glucose during long-term administration has not been clearly established. With chronic administration in Type II diabetic patients, the blood glucose lowering effect persists despite a gradual decline in the insulin secretory response to the drug. Extrapancreatic effects may be involved in the mechanism of action of oral sulfonylurea hypoglycemic drugs. Some patients who are initially responsive to oral hypoglycemic drugs, including tolazamide, may become unresponsive or poorly responsive over time. Alternatively, tolazamide may be effective in some patients who have become unresponsive to one or more other sulfonylurea drugs. In addition to its blood glucose lowering actions, tolazamide produces a mild diuresis by enhancement of renal free water clearance.
Cơ Chế Tác Dụng : A sulphonylurea hypoglycemic agent with actions and uses similar to those of chlorpropamide. [PubChem] Sulfonylureas likely bind to ATP-sensitive potassium-channel receptors on the pancreatic cell surface, reducing potassium conductance and causing depolarization of the membrane. Depolarization stimulates calcium ion influx through voltage-sensitive calcium channels, raising intracellular concentrations of calcium ions, which induces the secretion, or exocytosis, of insulin.
Dược Động Học :
▧ Absorption :
Rapidly and well absorbed from the gastrointestinal tract.
▧ Metabolism :
Tolazamide is metabolized to five major metabolites ranging in hypoglycemic activity from 0 to 70%.
▧ Route of Elimination :
Tolazamide is metabolized to five major metabolites ranging in hypoglycemic activity from 0% to 70%. They are excreted principally in the urine.
▧ Half Life :
The average biological half-life of the drug is 7 hours.
Độc Tính : Overdosage of sulfonylureas can produce hypoglycemia. Severe hypoglycemic reactions with coma, seizure, or other neurological impairment occur infrequently, but constitute medical emergencies requiring immediate hospitalization.
Chỉ Định : For use as an adjunct to diet to lower the blood glucose in patients with non-insulin dependent diabetes mellitus (Type II) whose hyperglycemia cannot be satisfactorily controlled by diet alone.
Tương Tác Thuốc :
  • Acebutolol Acebutolol may decrease symptoms of hypoglycemia and increase the time required for the body to compensate for hypoglycemia.
  • Acetylsalicylic acid Acetylsalicylic acid increases the effect of the sulfonylurea, tolazamide.
  • Amifostine Additive hypotensive effects may occur. At chemotherapeutic doses of Amifostine, Tolazamide should be withheld for 24 hours prior to Amifostine administration. Use caution at lower doses of Amifostine.
  • Atenolol The beta-blocker, atenolol, may decrease symptoms of hypoglycemia.
  • Bisoprolol The beta-blocker, bisoprolol, may decrease symptoms of hypoglycemia.
  • Carvedilol The beta-blocker, carvedilol, may decrease symptoms of hypoglycemia.
  • Chloramphenicol Chloramphenicol may increase the effect of sulfonylurea, tolazamide.
  • Clofibrate Clofibrate may increase the effect of sulfonylurea, tolazamide.
  • Esmolol The beta-blocker, esmolol, may decrease symptoms of hypoglycemia.
  • Labetalol The beta-blocker, labetalol, may decrease symptoms of hypoglycemia.
  • Metoprolol The beta-blocker, metoprolol, may decrease symptoms of hypoglycemia.
  • Nadolol The beta-blocker, nadolol, may decrease symptoms of hypoglycemia.
  • Oxprenolol The beta-blocker, oxprenolol, may decrease symptoms of hypoglycemia.
  • Phenylbutazone Phenylbutazone increases the effect of the hypoglycemic agent
  • Pindolol The beta-blocker, pindolol, may decrease symptoms of hypoglycemia.
  • Propranolol The beta-blocker, propranolol, may decrease symptoms of hypoglycemia.
  • Rifampicin Rifampin may decrease the effect of sulfonylurea, tolazamide.
  • Rituximab Additive hypotensive effects may occur. Consider withholding Tolazamide for 12 hours prior to administration of Rituximab.
  • Somatropin recombinant Somatropin may antagonize the hypoglycemic effect of Tolazamide. Dose adjustments of Tolazamide may be required.
  • Timolol The beta-blocker, timolol, may decrease symptoms of hypoglycemia.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Hua Shin
    Sản phẩm biệt dược : Desumide
  • Công ty : Chung Mei
    Sản phẩm biệt dược : Esulin
  • Công ty : Pfizer
    Sản phẩm biệt dược : Norglycin
  • Công ty : Upjohn
    Sản phẩm biệt dược : Tolanase
  • Công ty : Sandoz
    Sản phẩm biệt dược : Tolazamide
  • Công ty :
    Sản phẩm biệt dược : Tolinase
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00839
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5503
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505642
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00379
ChemSpider
http://www.chemspider.com/Chemical-Structure.5302.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0378-0217-01
PharmGKB
http://www.pharmgkb.org/drug/PA164774902
Wikipedia
http://en.wikipedia.org/wiki/Tolazamide
RxList
http://www.rxlist.com/cgi/generic/tolinase.htm
Drugs.com
http://www.drugs.com/cdi/tolazamide.html
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