Tìm theo
Insulin Glulisine
antidiabetic agents
Thuốc Gốc
Biotech
CAS: 207748-29-6
ATC: A10AB06
ĐG : Sanofi-Aventis Inc. , http://www.sanofi-aventis.com
CTHH: C258H384N64O78S6
PTK: 5823 Daltons
Insulin glulisine is a biosynthetic, rapid-acting human insulin analogue produced in a non-pathogenic laboratory strain of _Escherichia coli_ (K12). This recombinant hormone differs from native human insulin in that the amino acid arginine at position B3 is replaced by lysine and the lysine at position B29 is replaced by glutamic acid. These structural modifications decrease hexamer formation, stabilize insulin glulisine monomers and increase the rate of absorption and onset of action compared to human insulin.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C258H384N64O78S6
Phân tử khối
5823 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 glulisine is a rapid-acting insulin analogue used to mimic postprandial insulin spikes in diabetic individuals. The onset of action of insulin glulisine is approximately 15 minutes. Its activity peaks 60 minutes following subcutaneous injection and its duration of action is 2-4 hours.
Cơ Chế Tác Dụng : Insulin glulisine is a biosynthetic, rapid-acting human insulin analogue produced in a non-pathogenic laboratory strain of _Escherichia coli_ (K12). This recombinant hormone differs from native human insulin in that the amino acid arginine at position B3 is replaced by lysine and the lysine at position B29 is replaced by glutamic acid. These structural modifications decrease hexamer formation, stabilize insulin glulisine monomers and increase the rate of absorption and onset of action compared to human insulin. Insulin glulisine 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 arginine at position B3 for lysine and replacement of the B29 lysine with glutamic acid decreases the propensity to form hexamers, stabilizes the hormone in monomeric form and results in a rapid rate of absorption and short duration of action.
Dược Động Học :
▧ Absorption :
Compared to regular human insulin, insulin glulisine is faster absorbed. When 0.15 units/kg was subcutaneously administered to type 1 diabetes patients, the pharmacokinetic parameters are as follows: Tmax = 60 minutes (range of 40 - 120 minutes); Cmax = 83 microUnits/mL (range of 40 - 131 microUnits/mL). Absolute bioavailability following subcutaneous administration is approximately 70%, regardless of site of injection.
▧ Volume of Distribution :
13 L
▧ Half Life :
Elimination half life= 42 minutes (following subcutaneous injection)
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 and 2 diabetes mellitus. Should be used in regimens including a long-acting or basal insulin analogue unless it is used in a continuous infusion pump. May be used with oral antidiabetic agents.
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
  • 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 glulisine. Monitor for changes in fasting and postprandial blood sugars.
Liều Lượng & Cách Dùng : Injection, solution - Subcutaneous - 100 units/ml
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Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01309
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D04540
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0088-2502-05
PharmGKB
http://www.pharmgkb.org/drug/PA164760859
Wikipedia
http://en.wikipedia.org/wiki/Insulin_glulisine
RxList
http://www.rxlist.com/apidra-drug.htm
PDRhealth
http://www.pdrhealth.com/drugs/rx/rx-mono.aspx?contentFileName=api1806.html&contentName=Apidra&contentId=70
Drugs.com
http://www.drugs.com/mtm/insulin-glulisine.html
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