Liraglutide

Các tên gọi khác (10 ) :

Arg34Lys26-(N-ε-(γ-Glu(N-α-hexadecanoyl)))-GLP-1[7-37]
Liraglutida
Liraglutidum
N²⁶-(hexadecanoyl-gamma-glutamyle)-[34-arginine]GLP-1-(7-37)-peptide
N²⁶-(N-Hexadecanoyl-L-gamma-glutamyl)-[34-L-arginine]glucagon-like peptide 1-(7-37)-peptide
NN 2211
NN-2211
NN2211
NNC 90-1170
Victoza

Thuốc Gốc

Biotech

CAS: 204656-20-2

ATC: A10BX07

CTHH: C₁₇₂H₂₆₅N₄₃O₅₁

PTK: 3751.2 Da

Victoza contains liraglutide, an analog of human GLP-1 and acts as a GLP-1 receptor agonist. The peptide precursor of liraglutide, produced by a process that includes expression of recombinant DNA in Saccharomyces cerevisiae, has been engineered to be 97% homologous to native human GLP-1 by substituting arginine for lysine at position 34. Liraglutide is made by attaching a C-16 fatty acid (palmitic acid) with a glutamic acid spacer on the remaining lysine residue at position 26 of the peptide precursor.

Nhận Dạng Quốc Tế & Đặc Tính Hóa Học

Công thức hóa học

C₁₇₂H₂₆₅N₄₃O₅₁

Phân tử khối

3751.2 Da

Dược Lực Học : Liraglutide is a once-daily GLP-1 derivative for the treatment of type 2 diabetes. GLP-1, in its natural form, is short-lived in the body (the half-life after subcutaneous injection is approximately one hour), so it is not very useful as a therapeutic agent. However, liraglutide has a half-life after subcutaneous injection of 11–15 hours, making it suitable for once-daily dosing. The prolonged action of liraglutide is achieved by attaching a fatty acid molecule at one position of the GLP-1 molecule, enabling it to bind to albumin within the subcutaneous tissue and bloodstream. The active GLP-1 is then released from albumin at a slow, consistent rate. Binding with albumin also results in slower degradation and reduced elimination of liraglutide from the circulation by the kidneys compared to GLP-1.

Cơ Chế Tác Dụng : Victoza contains liraglutide, an analog of human GLP-1 and acts as a GLP-1 receptor agonist. The peptide precursor of liraglutide, produced by a process that includes expression of recombinant DNA in Saccharomyces cerevisiae, has been engineered to be 97% homologous to native human GLP-1 by substituting arginine for lysine at position 34. Liraglutide is made by attaching a C-16 fatty acid (palmitic acid) with a glutamic acid spacer on the remaining lysine residue at position 26 of the peptide precursor. Liraglutide is an acylated GLP-1 (Glucagon-Like Peptide-1) receptor agonist. Liraglutide upregulates intracellular cAMP resulting in the release of insulin given elevated blood glucose concentrations. Glucagon secretion is also decreased in a glucose-dependent fashion by liraglutide.

Dược Động Học :

▧ Absorption :
Maximum concentrations of liraglutide are achieved at 8-12 hours after dose. The mean peak and total exposures of liraglutide were 35 ng/mL and 960 ng·h/mL, respectively, for a subQ single dose of 0.6 mg. After subcutaneous single dose administrations, Cmax and AUC of liraglutide increased proportionally over the therapeutic dose range of 0.6 mg to 1.8 mg. At 1.8 mg Victoza, the average steady state concentration of liraglutide over 24 hours was approximately 128 ng/mL. AUC0-∞ was equivalent between upper arm and abdomen, and between upper arm and thigh. AUC0-∞ from thigh was 22% lower than that from abdomen. Absolute bioavailability of liraglutide following subcutaneous administration is approximately 55%.
▧ Volume of Distribution :
SubQ 0.6 mg is approximately 13L Intravenous is approximately 0.07L/kg
▧ Protein binding :
>98%
▧ Metabolism :
During the initial 24 hours following administration of a single [3H]-liraglutide dose to healthy subjects, the major component in plasma was intact liraglutide. Liraglutide is endogenously metabolized in a similar manner to large proteins without a specific organ as a major route of elimination.
▧ Route of Elimination :
Excreted in urine and feces, 6% and 5%, respectively.
▧ Half Life :
approximately 13 hours.
▧ Clearance :
The mean apparent clearance following subcutaneous administration of a single dose of liraglutide is approximately 1.2 L/h

Độc Tính : In a clinical trial, one patient with type 2 diabetes experienced a single overdose of Victoza 17.4 mg subcutaneous (10 times the maximum recommended dose). Effects of the overdose included severe nausea and vomiting requiring hospitalization. No hypoglycemia was reported. The patient recovered without complications. In the event of overdosage, appropriate supportive treatment should be initiated according to the patient’s clinical signs and symptoms. RISK OF THYROID C-CELL TUMORS

Chỉ Định : For use in/treatment of diabetes mellitus type 2.

Tương Tác Thuốc :

Acetaminophen These agents may have decreased C max and a delayed T max during coadministration.
Atorvastatin These agents may have decreased C max and a delayed T max during coadministration.
Azilsartan medoxomil Pharmacodynamic synergist- increases effects. May also increase hypoglycemic effects by improving insulin sensitivity.
Digoxin These agents may have decreased C max and a delayed T max during coadministration.
Griseofulvin Cmax may be increased.
Insulin Regular Coadministration may increase the risk of hypoglycemia. A lower dose of the antidiabetic agent may be needed.
Somatropin recombinant Somatropin may antagonize the hypoglycemic effect of liraglutide. Monitor for changes in fasting and postprandial blood sugars.

Liều Lượng & Cách Dùng : Injection - Subcutaneous - Multi-dose pen (0.6 mg, 1.2 mg, or 1.8 mg [6 mg/mL, 3 mL])

Dữ Kiện Thương Mại

Nhà Sản Xuất

Công ty : Novo Nordisk

Sản phẩm biệt dược : Victoza

Tài Liệu Tham Khảo Thêm

drugbank

http://www.drugbank.ca/drugs/DB06655

KEGG Drug

http://www.genome.jp/dbget-bin/www_bget?drug:D06404

National Drug Code Directory

http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0169-4060-13

PharmGKB

http://www.pharmgkb.org/drug/PA165958364

Wikipedia

http://en.wikipedia.org/wiki/Liraglutide

RxList

http://www.rxlist.com/victoza-drug.htm

Drugs.com

http://www.drugs.com/cdi/liraglutide.html

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