Tìm theo
Exenatide
Các tên gọi khác (10 ) :
  • AC 2993
  • AC-2993
  • AC002993
  • AC2993
  • AC2993a
  • Bydureon
  • Byetta
  • Exenatide
  • Exenatide synthetic
  • Synthetic exendin-4
Insulin và nhóm Thuốc hạ đường huyết
Thuốc Gốc
Biotech
CAS: 141758-74-9
ATC: A10BX04
ĐG : Amylin Pharmaceuticals , http://www.amylin.com
CTHH: C184H282N50O60S
PTK: 4186.6000
Exenatide, derived from a compound found in the saliva of the Gila monster, a large lizard native to the southwestern US, is a functional analog of Glucagon-Like Peptide-1 (GLP-1), a naturally occuring peptide.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C184H282N50O60S
Phân tử khối
4186.6000
Dược Lực Học : Exenatide is an incretin mimetic, which has glucoregulatory effects. While it is has blood-sugar lowering actions alone, it can also be combined with other medications such as pioglitazone, metformin, sulfonylureas, and/or insulin to improve glucose control. The approved use of exenatide is with either sulfonylureas, metformin and thiazolinediones. The medication is injected twice per day using a pre-filled pen device. Typical human responses to exenatide plus eating include improvements in the initial rapid release of endogenous insulin, suppression of glucagon release by the pancreas, regulation of gastric empyting and reduced appetite; all behaviors more typical of individuals without blood sugar control problems. Exenatide is self-regulating in that in lowers blood sugar when levels are elevated but does not continue to lower blood sugar when levels return to normal, unlike with sulfonylureas or insulins.
Cơ Chế Tác Dụng : Exenatide, derived from a compound found in the saliva of the Gila monster, a large lizard native to the southwestern US, is a functional analog of Glucagon-Like Peptide-1 (GLP-1), a naturally occuring peptide. Exenatide is a functional analog of the human incretin Glucagon-Like Peptide-1 (GLP-1). Incretins enhance glucose-dependent insulin secretion and exhibit other antihyperglycemic actions following their release into the circulation from the gut. The GLP-1 system increases insulin secretion only in the presence of elevated plasma glucose levels, avoiding inappropriately high insulin levels during fasting. The drug also moderates peak serum glucagon levels during hyperglycemic periods following meals, but does not interfere with glucagon release in response to hypoglycemia. Secondary effects of drug administration reduces the rate of gastric emptying and decreases food intake, mitigating the potential severity of hyperglycemic events after meals.
Dược Động Học :
▧ Absorption :
Following subcutaneous administration to patients with type 2 diabetes, exenatide reaches median peak plasma concentrations in 2.1 hours.
▧ Volume of Distribution :
* 28.3 L
▧ Route of Elimination :
Nonclinical studies have shown that exenatide is predominantly eliminated by glomerular filtration with subsequent proteolytic degradation.
▧ Half Life :
Mean terminal half-life is 2.4 hours.
▧ Clearance :
* Apparent cl=9.1 L/hr
Độc Tính : Effects of the overdoses included severe nausea, severe vomiting, and rapidly declining blood glucose concentrations.
Chỉ Định : Indicated as adjunctive therapy to improve glycemic control in patients with Type 2 diabetes mellitus who are taking metformin, a sulfonylurea, or a combination of both, but have not achieved adequate glycemic control.
Tương Tác Thuốc :
  • Azilsartan medoxomil Pharmacodynamic synergist- increases effects. May also increase hypoglycemic effects by improving insulin sensitivity.
  • Danazol Monitor therapy due to reduced hypoglycemic effect of exenatide.
  • Pegvisomant Monitor therapy due to enhanced hypoglycemic effect.
  • Somatropin recombinant Somatropin may antagonize the hypoglycemic effect of exenatide. Monitor for changes in fasting and postprandial blood sugars.
Liều Lượng & Cách Dùng : Solution - Subcutaneous - 250 mcg/mL
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01276
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D04121
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/66780-210-07
PharmGKB
http://www.pharmgkb.org/drug/PA164749238
Wikipedia
http://en.wikipedia.org/wiki/Exenatide
RxList
http://www.rxlist.com/cgi/generic/byetta.htm
Drugs.com
http://www.drugs.com/cdi/exenatide.html
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