Tìm theo
Insulin Detemir
Các tên gọi khác (7 ) :
  • Insulin detemir
  • Insulin detemir recombinant
  • Levemir
  • Levemir flexpen
  • Levemir innolet
  • Levemir penfill
  • NN-304
antidiabetic agents
Thuốc Gốc
Biotech
CAS: 169148-63-4
ĐG : Novo Nordisk Inc. , http://www.novonordisk.com
CTHH: C267H402N64O76S6
PTK: 5916.9 Daltons
Insulin detemir is a long-acting human insulin analogue used to maintain basal levels of insulin in diabetic individuals. It is produced using recombinant DNA technology in yeast cells. This insulin analogue has a 14-C fatty acid, myristic acid, bound to the lysine amino acid at position B29. The myristoyl side chain increases self-association and albumin binding. This along with slow systemic absorption from the injection site prolongs distribution of the hormone into tissues and results in a long duration of action. Novo Nordisk markets insulin detemir under the trade name Levemir.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C267H402N64O76S6
Phân tử khối
5916.9 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. Increased insulin secretion following meals is 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 detemir is a long-acting insulin analogue with a flat and predictable action profile. It is used to mimic the basal levels of insulin in diabetic individuals. The onset of action of insulin detemir is 1 to 2 hours and its duration of action is up to 24 hours. Interestingly, it has a lower affinity (30%) for the insulin receptor than human insulin.
Cơ Chế Tác Dụng : Insulin detemir is a long-acting human insulin analogue used to maintain basal levels of insulin in diabetic individuals. It is produced using recombinant DNA technology in yeast cells. This insulin analogue has a 14-C fatty acid, myristic acid, bound to the lysine amino acid at position B29. The myristoyl side chain increases self-association and albumin binding. This along with slow systemic absorption from the injection site prolongs distribution of the hormone into tissues and results in a long duration of action. Novo Nordisk markets insulin detemir under the trade name Levemir. Insulin detemir 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. Insulin detemir’s long duration of action appears to be a result of slow systemic absorption from the injection site and delayed distribution to target tissues. The myristic acid side chain on insulin detemir increases self-association and gives it a high binding affinity to serum albumin. These features slows its distribution into target tissues and prolongs its duration of action.
Dược Động Học :
▧ Absorption :
Maximum serum concentrations are reached 6 to 8 hours following subcutaneous injection. When single dose of 0.5 units/kg of insulin detemir was given to adult type 1 diabetes patients, the maximum serum concentration (Cmax) was 4,641 ± 2,299 pmol/L. Absorption is also dependent on the site of injection. When injected into the thigh, the AUC was lower than when injected into the deltoid and abdominal regions. Bioavailability is approximately 60%.
▧ Volume of Distribution :
* 0.1 L/kg
▧ Protein binding :
> 98% bound to albumin
▧ Metabolism :
As with natural insulin, all metabolites formed are inactive.
▧ Half Life :
5 - 7 hours depending on dose. The half life also differs between age groups (type 1 diabetes patients): Children (6-12 years) = 302 ± 100 minutes; Adolescents (13-17 years) = 301 ± 107 minutes; Adults (18-65 years) = 425 ± 78 minutes
▧ Clearance :
Apparent clearance (CL/F), type 1 diabetes adult patients = 3.41 ± 1.00 L/min·kg
Độc Tính : Hypoglycemia may occur with inappropriately high doses. 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. Injection site reactions may also occur. Symptoms include: redness, inflammation, bruising, swelling and itching at the injection site.
Chỉ Định : For the treatment of type 1 or 2 diabetes mellitus. May be used in combination with oral anti-diabetic agents in type 2 diabetic patients who are not in adequate metabolic control with oral anti-diabetic agents alone.
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 detemir. 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 : Levemir
  • Công ty : Novo Nordisk
    Sản phẩm biệt dược : Levemir FlexPen
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01307
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D04539
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0169-3687-12
PharmGKB
http://www.pharmgkb.org/drug/PA164746470
Wikipedia
http://en.wikipedia.org/wiki/Insulin_detemir
RxList
http://www.rxlist.com/levemir-drug.htm
PDRhealth
http://www.pdrhealth.com/drugs/rx/rx-mono.aspx?contentFileName=lev1746.html&contentName=Levemir&contentId=435
Drugs.com
http://www.drugs.com/monograph/insulin-detemir.html
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