Tìm theo
Insulin Aspart
Các tên gọi khác (6 ) :
  • Aspart
  • Aspart Insulin
  • B28-Aspart-Insulin
  • INA-X14
  • Insulin X14
  • Insulin, Asp(B28)
Insulin và nhóm Thuốc hạ đường huyết
Thuốc Gốc
Biotech
CAS: 116094-23-6
ĐG : Novo Nordisk Inc. , http://www.novonordisk.com
CTHH: C256H381N65O79S6
PTK: 5825.8 Daltons
Insulin aspart is a recombinant, biosynthetic, fast-acting insulin analogue. It has a single amino acid substitution at position B28 where proline is replaced with aspartic acid. This substitution decreases its propensity to form hexamers and gives it a higher rate of absorption following subcutaneous administration compared to native insulin. Insulin aspart is produced in a genetically modified strain of _Saccharomyces cerevisiae_ and harvested from a bioreactor.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C256H381N65O79S6
Phân tử khối
5825.8 Daltons
Dược Lực Học : Insulin is a natural hormone produced by beta cells of the pancreas. In non-diabetic individuals, a basal level of insulin is supplemented with insulin spikes following meals. Postprandial insulin spikes are responsible for the metabolic changes that occur as the body transitions from a postabsorptive to absorptive state. Insulin promotes cellular uptake of glucose, particularly in muscle and adipose tissues, promotes energy storage via glycogenesis, opposes catabolism of energy stores, increases DNA replication and protein synthesis by stimulating amino acid uptake by liver, muscle and adipose tissue, and modifies the activity of numerous enzymes involved in glycogen synthesis and glycolysis. Insulin also promotes growth and is required for the actions of growth hormone (e.g. protein synthesis, cell division, DNA synthesis). Insulin aspart is a rapid-acting insulin analogue used to mimic postprandial insulin spikes in diabetic individuals. The onset of action of insulin aspart is 10-15 minutes. Its activity peaks 60-90 minutes following subcutaneous injection and its duration of action is 4-5 hours.
Cơ Chế Tác Dụng : Insulin aspart is a recombinant, biosynthetic, fast-acting insulin analogue. It has a single amino acid substitution at position B28 where proline is replaced with aspartic acid. This substitution decreases its propensity to form hexamers and gives it a higher rate of absorption following subcutaneous administration compared to native insulin. Insulin aspart is produced in a genetically modified strain of _Saccharomyces cerevisiae_ and harvested from a bioreactor. Insulin aspart 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 autophosphorylates and phosphorylates numerous intracellular substrates such as insulin receptor substrates (IRS) proteins, Cbl, APS, Shc and Gab 1. Activation of these proteins leads 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), both of which play critical roles in metabolism and catabolism. In humans, insulin is stored in the form of hexamers; however, only insulin monomers are able to interact with IR. Substitution of the proline residue at B28 with aspartic acid reduces the tendency to form hexamers and results in a faster rate of absorption and onset of action and shorter duration of action.
Dược Động Học :
▧ Absorption :
Rapidly absorbed following subcutaneous administration (more so than regular human insulin). Furthermore, insulin aspart has a faster absorption, a faster onset of action, and a shorter duration of action than regular human insulin after subcutaneous injection. It takes 40 - 50 minutes to reach maximum concentration. When a dose of 0.15 U/kg body weight was injected in type 1 diabetes patients, the mean maximum concentration (Cmax) was 82 mU/L. The site of injection has no impact on extent or speed of absorption.
▧ Protein binding :
<10% bound to plasma proteins.
▧ Half Life :
81 minutes (following subcutaneous administration in healthy subjects).
▧ Clearance :
* 1.2 L/h/kg [healthy Caucasian male], excreted in the urine
Độc Tính : Inappropriately high dosages relative to food intake and/or energy expenditure may result in severe and sometimes prolonged and life-threatening hypoglycemia. Neurogenic (autonomic) signs and symptoms of hypoglycemia include trembling, palpitations, sweating, anxiety, hunger, nausea and tingling. Neuroglycopenic signs and symptoms of hypoglycemia include difficulty concentrating, lethargy/weakness, confusion, drowsiness, vision changes, difficulty speaking, headache, and dizziness. Mild hypoglycemia is characterized by the presence of autonomic symptoms. Moderate hypoglycemia is characterized by the presence of autonomic and neuroglycopenic symptoms. Individuals may become unconscious in severe cases of hypoglycemia.
Chỉ Định : For the treatment of Type 1 or 2 diabetes mellitus. Should normally be used in conjunction with an intermediate or long-acting insulin.
Tương Tác Thuốc :
  • Acebutolol The beta-blocker, acebutolol, may decrease symptoms of hypoglycemia.
  • 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.
  • Clofibrate Increases the effect of insulin
  • Danazol Monitor therapy due to decreased hypoglycemic effect of insulin aspart.
  • Dexfenfluramine Fenfluramine increases the effect of insulin
  • Edetic Acid Monitor therapy due to enhanced hypoglycemic effect.
  • Esmolol The beta-blocker, esmolol, may decrease symptoms of hypoglycemia.
  • Fenfluramine Fenfluramine increases the effect of insulin
  • Pegvisomant Monitor therapy due to enhanced hypoglycemic effect.
  • Somatropin recombinant Somatropin may antagonize the hypoglycemic effect of insulin aspart. Monitor for changes in fasting and postprandial blood sugars.
Liều Lượng & Cách Dùng : Injection, solution - Subcutaneous - 100 units/ml
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Novo Nordisk
    Sản phẩm biệt dược : NovoLog
  • Công ty : Novo Nordisk
    Sản phẩm biệt dược : Novolog FlexPen
  • Công ty : Novo Nordisk
    Sản phẩm biệt dược : Novolog Penfill
  • Công ty : Novo Nordisk
    Sản phẩm biệt dược : NovoRapid
  • Công ty : Novo Nordisk
    Sản phẩm biệt dược : NovoRapid Penfill
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01306
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D04475
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0169-7501-11
PharmGKB
http://www.pharmgkb.org/drug/PA164784029
Wikipedia
http://en.wikipedia.org/wiki/Insulin_aspart
RxList
http://www.rxlist.com/novolog-drug.htm
Drugs.com
http://www.drugs.com/mtm/insulin-aspart.html
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