Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C257H383N65O77S6
Phân tử khối
5808 Daltons
Dược Lực Học :
Insulin regular is a short-acting insulin. When subcutaneously administered, the onset of action (as evidenced by a decrease in glucose level) occurs 30 minutes post-dose. Maximal effect occurs between 1.5 and 3.5 hours post-dose. The glucose-lowering effect occurs 8 hours post-dose. Compared to other rapid-acting insulin analogs, insulin regular has a slower onset of action and longer duration of action.
Cơ Chế Tác Dụng :
Insulin regular is a 51 residue peptide hormone, composed of two amino acid chains covalently linked by disulfide bonds. The structure is identical to native human insulin. Recombinant insulin is synthesized by recombinant DNA techncology. Inserting the human insulin gene into the Escherichia coli bacteria or Saccharomyces cerevisiae produces insulin for human use.
The primary activity of insulin is the regulation of glucose metabolism. Insulin promotes glucose and amino acid uptake into muscle and adipose tissues, and other tissues except brain and liver. It also has an anabolic role in stimulating glycogen, fatty acid, and protein synthesis. Insulin inhibits gluconeogenesis in the liver.
Insulin binds to the insulin receptor (IR), a heterotetrameric protein consisting of two extracellular alpha units and two transmembrane beta units. The binding of insulin to the alpha subunit of IR stimulates the tyrosine kinase activity intrinsic to the beta subunit of the receptor. The bound receptor is able to autophosphorylate and phosphorylate numerous intracellular substrates such as insulin receptor substrates (IRS) proteins, Cbl, APS, Shc and Gab 1. These activated proteins, in turn, lead to the activation of downstream signaling molecules including PI3 kinase and Akt. Akt regulates the activity of glucose transporter 4 (GLUT4) and protein kinase C (PKC) which play a critical role in metabolism and catabolism.
Dược Động Học :
▧ Absorption :
Insulin is generally well absorbed.
▧ Volume of Distribution :
0.15 L/kg
▧ Protein binding :
5% protein bound
▧ Metabolism :
Insulin is predominantly cleared by metabolic degradation via a receptor-mediated process.
Độc Tính :
Hypoglycemia is one of the most frequent adverse events experienced by insulin users.
Chỉ Định :
Indicated as an adjunct to diet and exercise to improve glycemic control in adults and children with type 1 and type 2 diabetes mellitus.
Tương Tác Thuốc :
-
Liraglutide
Coadministration may increase the risk of hypoglycemia. A lower dose of the antidiabetic agent may be needed.
Liều Lượng & Cách Dùng :
Injection - Subcutaneous - 100 units/mL; 500 units/mL
Dữ Kiện Thương Mại
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