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药品详细

Insulin Aspart (胰岛素aspart )

化学结构式图
没有图片
中文名
胰岛素aspart
英文名
Insulin Aspart
分子式
Not Available
化学名
分子量
CAS号
116094-23-6
ATC分类
A10A 未知;A10A 未知
药物类型
biotech
阶段
商品名
NovoLog (Novo Nordisk);Novolog FlexPen (Novo Nordisk);Novolog Penfill (Novo Nordisk);NovoRapid (Novo Nordisk);NovoRapid Penfill (Novo Nordisk);
同义名
Aspart;Aspart Insulin;B28-Aspart-Insulin;INA-X14;Insulin X14;Insulin, Asp(B28);
基本介绍

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.

生产厂家
  • Novo nordisk inc
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Heller S, Kurtzhals P, Verge D, Lindholm A: Insulin aspart: promising early results borne out in clinical practice. Expert Opin Pharmacother. 2002 Feb;3(2):183-95. Pubmed
  2. Sciacca L, Cassarino MF, Genua M, Pandini G, Le Moli R, Squatrito S, Vigneri R: Insulin analogues differently activate insulin receptor isoforms and post-receptor signalling. Diabetologia. 2010 Apr 28. Pubmed
剂型
Form Route Strength
Injection, solution Subcutaneous 100 units/ml
规格
Unit description Cost Unit
Novolog 100 unit/ml cartridge 14.81 USD ml
Novolog mix 70-30 cartridge 10.45 USD ml
Novorapid 100 unit/ml Cartridge 3.89 USD cartridge
Novorapid 100 unit/ml 2.92 USD cartridge
化合物类型
Type biotech
Classes Not Available
Substructures Not Available
适应症
Diabetes 糖尿病;
药理
Indication For the treatment of Type 1 or 2 diabetes mellitus. Should normally be used in conjunction with an intermediate or long-acting insulin.
Pharmacodynamics 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.
Mechanism of action 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.
Absorption Rapidly absorbed following subcutaneous administration.
Volume of distribution Not Available
Protein binding 0-9%
Metabolism
Route of elimination Not Available
Half life 81 minutes
Clearance
  • 1.2 l/h/kg [healthy Caucasian male]
Toxicity 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.
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State liquid
Melting point Not Available
Experimental Properties Not Available
药物相互作用
Drug Interaction
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
Dexfenfluramine Fenfluramine increases the effect of insulin
Esmolol The beta-blocker, esmolol, may decrease symptoms of hypoglycemia.
Fenfluramine Fenfluramine increases the effect of insulin
Somatropin recombinant Somatropin may antagonize the hypoglycemic effect of insulin aspart. Monitor for changes in fasting and postprandial blood sugars.
食物相互作用
Not Available

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