Tìm theo
Gliclazide
Các tên gọi khác (5 ) :
  • 1-(3-Azabicyclo(3.3.0)oct-3-yl)-3-(p-tolylsulfonyl)urea
  • 1-(Hexahydrocyclopenta(c)pyrrol-2(1H)-yl)-3-(p-tolylsulfonyl)urea
  • Gliclazida
  • Gliclazidum
  • N-(4-Methylbenzenesulfonyl)-N'-(3-azabicyclo(3.3.0)oct-3-yl)urea
Hormon, Nội tiết tố
Thuốc Gốc
Small Molecule
CAS: 21187-98-4
ATC: A10BB09
CTHH: C15H21N3O3S
PTK: 323.411
Gliclazide is an oral antihyperglycemic agent used for the treatment of non-insulin-dependent diabetes mellitus (NIDDM). It belongs to the sulfonylurea class of insulin secretagogues, which act by stimulating β cells of the pancreas to release insulin. Sulfonylureas increase both basal insulin secretion and meal-stimulated insulin release. Medications in this class differ in their dose, rate of absorption, duration of action, route of elimination and binding site on their target pancreatic β cell receptor. Sulfonylureas also increase peripheral glucose utilization, decrease hepatic gluconeogenesis and may increase the number and sensitivity of insulin receptors. Sulfonylureas are associated with weight gain, though less so than insulin. Due to their mechanism of action, sulfonylureas may cause hypoglycemia and require consistent food intake to decrease this risk. The risk of hypoglycemia is increased in elderly, debilitated and malnourished individuals. Gliclazide has been shown to decrease fasting plasma glucose, postprandial blood glucose and glycosolated hemoglobin (HbA1c) levels (reflective of the last 8-10 weeks of glucose control). Gliclazide is extensively metabolized by the liver; its metabolites are excreted in both urine (60-70%) and feces (10-20%).
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C15H21N3O3S
Phân tử khối
323.411
Monoisotopic mass
323.130362243
InChI
InChI=1/C15H21N3O3S/c1-11-5-7-14(8-6-11)22(20,21)17-15(19)16-18-9-12-3-2-4-13(12)10-18/h5-8,12-13H,2-4,9-10H2,1H3,(H2,16,17,19)/t12-,13+
InChI Key
InChIKey=BOVGTQGAOIONJV-BETUJISGNA-N
IUPAC Name
3-[(3aR,6aS)-octahydrocyclopenta[c]pyrrol-2-yl]-1-(4-methylbenzenesulfonyl)urea
Traditional IUPAC Name
gliclazidum
SMILES
[H][C@@]12CCC[C@]1([H])CN(C2)NC(=O)NS(=O)(=O)C1=CC=C(C)C=C1
Độ tan chảy
180-182
Độ hòa tan
1.90e-01 g/l
logP
2.6
logS
-3.2
pKa (strongest acidic)
4.07
pKa (Strongest Basic)
1.38
PSA
78.51 Å2
Refractivity
83.88 m3·mol-1
Polarizability
34.17 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
4
H Bond Donor Count
2
Physiological Charge
-1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Gliclazide is a second generation sulphonylurea which acts as a hypoglycemic agent. It stimulates β cells of the islet of Langerhans in the pancreas to release insulin. It also enhances peripheral insulin sensitivity. Overall, it potentiates insulin release and improves insulin dynamics.
Cơ Chế Tác Dụng : Gliclazide is an oral antihyperglycemic agent used for the treatment of non-insulin-dependent diabetes mellitus (NIDDM). It belongs to the sulfonylurea class of insulin secretagogues, which act by stimulating β cells of the pancreas to release insulin. Sulfonylureas increase both basal insulin secretion and meal-stimulated insulin release. Medications in this class differ in their dose, rate of absorption, duration of action, route of elimination and binding site on their target pancreatic β cell receptor. Sulfonylureas also increase peripheral glucose utilization, decrease hepatic gluconeogenesis and may increase the number and sensitivity of insulin receptors. Sulfonylureas are associated with weight gain, though less so than insulin. Due to their mechanism of action, sulfonylureas may cause hypoglycemia and require consistent food intake to decrease this risk. The risk of hypoglycemia is increased in elderly, debilitated and malnourished individuals. Gliclazide has been shown to decrease fasting plasma glucose, postprandial blood glucose and glycosolated hemoglobin (HbA1c) levels (reflective of the last 8-10 weeks of glucose control). Gliclazide is extensively metabolized by the liver; its metabolites are excreted in both urine (60-70%) and feces (10-20%). Gliclazide binds to the β cell sulfonyl urea receptor (SUR1). This binding subsequently blocks the ATP sensitive potassium channels. The binding results in closure of the channels and leads to a resulting decrease in potassium efflux leads to depolarization of the β cells. This opens voltage-dependent calcium channels in the β cell resulting in calmodulin activation, which in turn leads to exocytosis of insulin containing secretorty granules.
Dược Động Học :
▧ Absorption :
Rapidly and well absorbed but may have wide inter- and intra-individual variability. Peak plasma concentrations occur within 4-6 hours of oral administration.
▧ Protein binding :
94%, highly bound to plasma proteins
▧ Metabolism :
Extensively metabolized in the liver. Less than 1% of the orally administered dose appears unchanged in the urine. Metabolites include oxidized and hydroxylated derivates, as well as glucuronic acid conjugates.
▧ Route of Elimination :
Metabolites and conjugates are eliminated primarily by the kidneys (60-70%) and also in the feces (10-20%).
▧ Half Life :
10.4 hours. Duration of action is 10-24 hours.
Độc Tính : LD50=3000 mg/kg (orally in mice). Gliclazide and its metabolites may accumulate in those with severe hepatic and/or renal dysfunction. Symptoms of hypoglycemia include: dizziness, lack of energy, drowsiness, headache and sweating.
Chỉ Định : For the treatment of NIDDM in conjunction with diet and exercise.
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, gliclazide.
  • Atenolol The beta-blocker, atenolol, may decrease symptoms of hypoglycemia.
  • Betaxolol The beta-blocker, betaxolol, may decrease symptoms of hypoglycemia.
  • Bevantolol The beta-blocker, bevantolol, may decrease symptoms of hypoglycemia.
  • Bismuth Subsalicylate The salicylate, bismuth subsalicylate, increases the effect of the sulfonylurea, gliclazide.
  • Bisoprolol The beta-blocker, bisoprolol, may decrease symptoms of hypoglycemia.
  • Carteolol The beta-blocker, carteolol, may decrease symptoms of hypoglycemia.
  • Carvedilol The beta-blocker, carvedilol, may decrease symptoms of hypoglycemia.
  • Chloramphenicol Chloramphenicol may increase the effect of sulfonylurea, gliclazide.
  • Clofibrate Clofibrate may increase the effect of sulfonylurea, gliclazide.
  • Dicoumarol Dicumarol may increase the effect of sulfonylurea, gliclazide.
  • Esmolol The beta-blocker, esmolol, may decrease symptoms of hypoglycemia.
  • Glucosamine Possible hyperglycemia
  • Labetalol The beta-blocker, labetalol, may decrease symptoms of hypoglycemia.
  • Magnesium salicylate The salicylate, magnesium salicylate, increases the effect of the sulfonylurea, gliclazide.
  • 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.
  • Penbutolol The beta-blocker, penbutolol, may decrease symptoms of hypoglycemia.
  • Phenylbutazone Phenylbutazone increases the effect of the hypoglycemic agent
  • Pindolol The beta-blocker, pindolol, may decrease symptoms of hypoglycemia.
  • Practolol The beta-blocker, practolol, may decrease symptoms of hypoglycemia.
  • Propranolol The beta-blocker, propranolol, may decrease symptoms of hypoglycemia.
  • Rifampicin Rifampin may decrease the effect of sulfonylurea, gliclazide.
  • Salicylate-sodium The salicylate, salicylate-sodium, increases the effect of the sulfonylurea, gliclazide.
  • Salsalate The salicylate, salsalate, increases the effect of the sulfonylurea, gliclazide.
  • Somatropin recombinant Somatropin may antagonize the hypoglycemic effect of gliclazide. Monitor for changes in fasting and postprandial blood sugars.
  • Sotalol The beta-blocker, sotalol, may decrease symptoms of hypoglycemia.
  • Timolol The beta-blocker, timolol, may decrease symptoms of hypoglycemia.
  • Trisalicylate-choline The salicylate, trisalicylate-choline, increases the effect of the sulfonylurea, gliclazide.
Liều Lượng & Cách Dùng : Tablet - Oral - 80 mg
Tablet, extended release - Oral - 30 mg
Tablet, extended release - Oral - 60 mg
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Servier
    Sản phẩm biệt dược : Diamicron
  • Công ty : Servier
    Sản phẩm biệt dược : Diamicron MR
  • Công ty :
    Sản phẩm biệt dược : Glimicron
  • Công ty : Mylan
    Sản phẩm biệt dược : Mylan-Gliclazide
  • Công ty :
    Sản phẩm biệt dược : Nordialex
  • Công ty : Pharmascience
    Sản phẩm biệt dược : PMS-Gliclazide
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01120
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D01599
PharmGKB
http://www.pharmgkb.org/drug/PA10892
Wikipedia
http://en.wikipedia.org/wiki/Gliclazide
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