Tìm theo
Miglitol
Các tên gọi khác (3) :
  • Glyset
  • Miglitol
  • Miglitolum
Thuốc Gốc
Small Molecule
CAS: 72432-03-2
ATC: A10BF02
ĐG : Bayer Healthcare , http://www.bayerhealthcare.com
CTHH: C8H17NO5
PTK: 207.2243
Miglitol is an oral anti-diabetic drug that acts by inhibiting the ability of the patient to breakdown complex carbohydrates into glucose. It is primarily used in diabetes mellitus type 2 for establishing greater glycemic control by preventing the digestion of carbohydrates (such as disaccharides, oligosaccharides, and polysaccharides) into monosaccharides which can be absorbed by the body. Miglitol inhibits glycoside hydrolase enzymes called alpha-glucosidases. Since miglitol works by preventing digestion of carbohydrates, it lowers the degree of postprandial hyperglycemia. It must be taken at the start of main meals to have maximal effect. Its effect will depend on the amount of non-monosaccharide carbohydrates in a person's diet. In contrast to acarbose (another alpha-glucosidase inhibitor), miglitol is systemically absorbed; however, it is not metabolized and is excreted by the kidneys.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C8H17NO5
Phân tử khối
207.2243
Monoisotopic mass
207.110672659
InChI
InChI=1S/C8H17NO5/c10-2-1-9-3-6(12)8(14)7(13)5(9)4-11/h5-8,10-14H,1-4H2/t5-,6+,7-,8-/m1/s1
InChI Key
InChIKey=IBAQFPQHRJAVAV-ULAWRXDQSA-N
IUPAC Name
(2R,3R,4R,5S)-1-(2-hydroxyethyl)-2-(hydroxymethyl)piperidine-3,4,5-triol
Traditional IUPAC Name
miglitol
SMILES
OCCN1C[C@H](O)[C@@H](O)[C@H](O)[C@H]1CO
Độ tan chảy
114 °C
Độ hòa tan
Soluble
logP
-2.7
logS
0.47
pKa (strongest acidic)
12.9
pKa (Strongest Basic)
7.6
PSA
104.39 Å2
Refractivity
48.16 m3·mol-1
Polarizability
20.81 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
6
H Bond Donor Count
5
Physiological Charge
1
Number of Rings
1
Bioavailability
1
Rule of Five
true
pKa
5.9
Dược Lực Học : Miglitol, an oral alpha-glucosidase inhibitor, is a desoxynojirimycin derivative that delays the digestion of ingested carbohydrates, thereby resulting in a smaller rise in blood glucose concentration following meals. As a consequence of plasma glucose reduction, miglitol reduce levels of glycosylated hemoglobin in patients with Type II (non-insulin-dependent) diabetes mellitus. Systemic nonenzymatic protein glycosylation, as reflected by levels of glycosylated hemoglobin, is a function of average blood glucose concentration over time. Because its mechanism of action is different, the effect of miglitol to enhance glycemic control is additive to that of sulfonylureas when used in combination. In addition, miglitol diminishes the insulinotropic and weight-increasing effects of sulfonylureas. Miglitol has minor inhibitory activity against lactase and consequently, at the recommended doses, would not be expected to induce lactose intolerance.
Cơ Chế Tác Dụng : Miglitol is an oral anti-diabetic drug that acts by inhibiting the ability of the patient to breakdown complex carbohydrates into glucose. It is primarily used in diabetes mellitus type 2 for establishing greater glycemic control by preventing the digestion of carbohydrates (such as disaccharides, oligosaccharides, and polysaccharides) into monosaccharides which can be absorbed by the body. Miglitol inhibits glycoside hydrolase enzymes called alpha-glucosidases. Since miglitol works by preventing digestion of carbohydrates, it lowers the degree of postprandial hyperglycemia. It must be taken at the start of main meals to have maximal effect. Its effect will depend on the amount of non-monosaccharide carbohydrates in a person's diet. In contrast to acarbose (another alpha-glucosidase inhibitor), miglitol is systemically absorbed; however, it is not metabolized and is excreted by the kidneys. In contrast to sulfonylureas, miglitol does not enhance insulin secretion. The antihyperglycemic action of miglitol results from a reversible inhibition of membrane-bound intestinal a-glucoside hydrolase enzymes. Membrane-bound intestinal a-glucosidases hydrolyze oligosaccharides and disaccharides to glucose and other monosaccharides in the brush border of the small intestine. In diabetic patients, this enzyme inhibition results in delayed glucose absorption and lowering of postprandial hyperglycemia.
Dược Động Học :
▧ Absorption :
Absorption of miglitol is saturable at high doses with 25 mg being completely absorbed while a 100-mg dose is only 50-70% absorbed. No evidence exists to show that systemic absorption of miglitol adds to its therapeutic effect.
▧ Volume of Distribution :
* 0.18 L/kg
▧ Protein binding :
The protein binding of miglitol is negligible (<4.0%).
▧ Metabolism :
Miglitol is not metabolized in man or in any animal species studied.
▧ Route of Elimination :
Miglitol is not metabolized in man or in any animal species studied. It is eliminated by renal excretion as an unchanged drug.
▧ Half Life :
The elimination half-life of miglitol from plasma is approximately 2 hours.
Độc Tính : Unlike sulfonylureas or insulin, an overdose will not result in hypoglycemia. An overdose may result in transient increases in flatulence, diarrhea, and abdomi-nal discomfort. Because of the lack of extra-intestinal effects seen with miglitol, no serious systemic reactions are expected in the event of an overdose.
Chỉ Định : For use as an adjunct to diet to improve glycemic control in patients with non-insulin-dependent diabetes mellitus (NIDDM) whose hyperglycemia cannot be managed with diet alone.
Tương Tác Thuốc :
  • Glucosamine Possible hyperglycemia
  • Somatropin recombinant Somatropin may antagonize the hypoglycemic effect of miglitol. Monitor for changes in fasting and postprandial blood sugars.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Glyset 25 mg tablet
    Giá bán buôn : USD >1.11
    Đơn vị tính : tablet
  • Biệt dược thương mại : Glyset 50 mg tablet
    Giá bán buôn : USD >1.24
    Đơn vị tính : tablet
  • Biệt dược thương mại : Glyset 100 mg tablet
    Giá bán buôn : USD >1.46
    Đơn vị tính : tablet
Nhà Sản Xuất
  • Công ty : Chen Ho
    Sản phẩm biệt dược : Diaban
  • Công ty : Micro DTF
    Sản phẩm biệt dược : Diamig
  • Công ty : ACI
    Sản phẩm biệt dược : Diaset
  • Công ty : Sanofi-Aventis
    Sản phẩm biệt dược : Diastabol
  • Công ty : Ranbaxy
    Sản phẩm biệt dược : Elitox
  • Công ty : Abbott
    Sản phẩm biệt dược : Euglitol
  • Công ty : Pfizer
    Sản phẩm biệt dược : Glycet
  • Công ty :
    Sản phẩm biệt dược : Glyset
  • Sản phẩm biệt dược : Laiping
  • Công ty : Standard
    Sản phẩm biệt dược : Migbose
  • Công ty : Biocon
    Sản phẩm biệt dược : Miglit
  • Công ty : Glenmark
    Sản phẩm biệt dược : Mignar
  • Công ty : Torrent
    Sản phẩm biệt dược : Migtor
  • Công ty : Lupin
    Sản phẩm biệt dược : Misobit
  • Công ty : Lacer
    Sản phẩm biệt dược : Plumarol
  • Công ty : Sanwa Kagaku
    Sản phẩm biệt dược : Seibule
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00491
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=441314
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46504492
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07708
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00625
ChemSpider
http://www.chemspider.com/Chemical-Structure.390074.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0009-5012-01
PharmGKB
http://www.pharmgkb.org/drug/PA164776726
Wikipedia
http://en.wikipedia.org/wiki/Miglitol
RxList
http://www.rxlist.com/cgi/generic2/miglitol.htm
Drugs.com
http://www.drugs.com/cdi/miglitol.html
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