Tìm theo
Glipizide
Các tên gọi khác (32 ) :
  • 1-Cyclohexyl-3-({p-[2-(5-methylpyrazinecarboxamido)ethyl]phenyl}sulfonyl)urea
  • Aldiab
  • CP 28,720
  • CP 28720
  • CP-28,720
  • Digrin
  • Dipazide
  • Glibenese
  • Glibetin
  • Glican
  • Glidiab
  • Glipid
  • Glipizida
  • Glipizidum
  • Gluco-rite
  • Glucolip
  • Glucotrol
  • Glucozide
  • Glupitel
  • Glupizide
  • Glyde
  • Glydiazinamide
  • K 4024
  • Melizide
  • Mindiab
  • Minidab
  • Minidiab
  • Minodiab
  • N-{4-[beta-(5-methylpyrazine-2-carboxamido)ethyl]benzenesulphonyl}-n'-cyclohexylurea
  • Napizide
  • Ozidia
  • Sucrazide
Hormon, Nội tiết tố
Thuốc Gốc
Small Molecule
CAS: 29094-61-9
ATC: A10BB07
ĐG : Actavis Group , http://www.actavis.com
CTHH: C21H27N5O4S
PTK: 445.535
An oral hypoglycemic agent which is rapidly absorbed and completely metabolized. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C21H27N5O4S
Phân tử khối
445.535
Monoisotopic mass
445.178375067
InChI
InChI=1S/C21H27N5O4S/c1-15-13-24-19(14-23-15)20(27)22-12-11-16-7-9-18(10-8-16)31(29,30)26-21(28)25-17-5-3-2-4-6-17/h7-10,13-14,17H,2-6,11-12H2,1H3,(H,22,27)(H2,25,26,28)
InChI Key
InChIKey=ZJJXGWJIGJFDTL-UHFFFAOYSA-N
IUPAC Name
N-[2-(4-{[(cyclohexylcarbamoyl)amino]sulfonyl}phenyl)ethyl]-5-methylpyrazine-2-carboxamide
Traditional IUPAC Name
N-(2-{4-[(cyclohexylcarbamoyl)aminosulfonyl]phenyl}ethyl)-5-methylpyrazine-2-carboxamide
SMILES
CC1=CN=C(C=N1)C(=O)NCCC1=CC=C(C=C1)S(=O)(=O)NC(=O)NC1CCCCC1
Độ tan chảy
200-203
Độ hòa tan
37.2 mg/L
logP
1.91
logS
-4.4
pKa (strongest acidic)
4.32
pKa (Strongest Basic)
0.059
PSA
130.15 Å2
Refractivity
115.62 m3·mol-1
Polarizability
47.64 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
6
H Bond Donor Count
3
Physiological Charge
-1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
MDDR-Like Rule
true
pKa
5.9
Dược Lực Học : Glipizide, a second-generation sulfonylurea, is used with diet to lower blood glucose in patients with diabetes mellitus type II. The primary mode of action of glipizide in experimental animals appears to be the stimulation of insulin secretion from the beta cells of pancreatic islet tissue and is thus dependent on functioning beta cells in the pancreatic islets. In humans glipizide 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. In man, stimulation of insulin secretion by glipizide in response to a meal is undoubtedly of major importance. Fasting insulin levels are not elevated even on long-term glipizide administration, but the postprandial insulin response continues to be enhanced after at least 6 months of treatment. Some patients fail to respond initially, or gradually lose their responsiveness to sulfonylurea drugs, including glipizide.
Cơ Chế Tác Dụng : An oral hypoglycemic agent which is rapidly absorbed and completely metabolized. [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 :
Gastrointestinal absorption is uniform, rapid, and essentially complete.
▧ Volume of Distribution :
* 11 L
▧ Protein binding :
98-99%, primarily to albumin.
▧ Metabolism :
Hepatic. The major metabolites of glipizide are products of aromatic hydroxylation and have no hypoglycemic activity. A minor metabolite which accounts for less than 2% of a dose, an acetylaminoethyl benzine derivatives, is reported to have 1/10 to 1/3 as much hypoglycemic activity as the parent compound.
▧ Route of Elimination :
The primary metabolites are inactive hydroxylation products and polar conjugates and are excreted mainly in the urine.
▧ Half Life :
2-5 hours
Độc Tính : The acute oral toxicity was extremely low in all species tested (LD50 greater than 4 g/kg). Overdosage of sulfonylureas including glipizide can produce hypoglycemia.
Chỉ Định : For use as an adjunct to diet for the control of hyperglycemia and its associated symptomatology in patients with non-insulin-dependent diabetes mellitus (NIDDM; type II), formerly known as maturity-onset diabetes, after an adequate trial of dietary therapy has proved unsatisfactory.
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, glipizide.
  • 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, glipizide.
  • Clofibrate Clofibrate may increase the effect of sulfonylurea, glipizide.
  • Cyclosporine The sulfonylurea, glipizide, may increase the effect of cyclosporine.
  • 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, glipizide.
  • Somatropin recombinant Somatropin may antagonize the hypoglycemic effect of glipizide. Monitor for changes in fasting and postprandial blood sugars.
  • Timolol The beta-blocker, timolol, may decrease symptoms of hypoglycemia.
  • Tolbutamide Tolbutamide, a strong CYP2C9 inhibitor, may decrease the metabolism and clearance of Glipizide. Consider alternate therapy or monitor for changes in Glipizide therapeutic and adverse effects if Tolbutamide is initiated, discontinued or dose changed.
Liều Lượng & Cách Dùng : Tablet - Oral
Tablet, extended release - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Pfizer
    Sản phẩm biệt dược : Glibenese
  • Công ty : Dexo
    Sản phẩm biệt dược : Glibénèse
  • Công ty : Johnson
    Sản phẩm biệt dược : Glibetin
  • Công ty : Swiss Pharm
    Sản phẩm biệt dược : Glipin
  • Công ty :
    Sản phẩm biệt dược : GlipizideER
  • Công ty : YSP
    Sản phẩm biệt dược : Glix
  • Công ty : Pfizer
    Sản phẩm biệt dược : Glucotrol
  • Công ty : Pfizer
    Sản phẩm biệt dược : Glucotrol XL
  • Công ty : Pfizer
    Sản phẩm biệt dược : Mindiab
  • Công ty : Pfizer
    Sản phẩm biệt dược : Minidiab
  • Công ty : Square
    Sản phẩm biệt dược : Zitrol XR
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01067
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3478
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505865
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00335
ChemSpider
http://www.chemspider.com/Chemical-Structure.3359.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50012956
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0378-1105-01
PharmGKB
http://www.pharmgkb.org/drug/PA449762
Wikipedia
http://en.wikipedia.org/wiki/Glipizide
RxList
http://www.rxlist.com/cgi/generic/glip.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/cx1655.shtml
Drugs.com
http://www.drugs.com/glipizide.html
... loading
... loading