Tìm theo
Lepirudin
Các tên gọi khác (1) :
  • Hirudin variant-1
Thuốc Gốc
Biotech
CAS: 120993-53-5
ATC: B01AE02
ĐG : Bayer Healthcare , http://www.bayerhealthcare.com
CTHH: C287H440N80O110S6
PTK: 6963.4250
Lepirudin is identical to natural hirudin except for substitution of leucine for isoleucine at the N-terminal end of the molecule and the absence of a sulfate group on the tyrosine at position 63. It is produced via yeast cells.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C287H440N80O110S6
Phân tử khối
6963.4250
Độ tan chảy
65 °C
Độ kỵ nước
-0.777
Điểm đẳng điện tích
4.04
Dược Lực Học : Lepirudin is used to break up clots and to reduce thrombocytopenia. It binds to thrombin and prevents thrombus or clot formation. It is a highly potent, selective, and essentially irreversible inhibitor of thrombin and clot-bond thrombin. Lepirudin requires no cofactor for its anticoagulant action. Lepirudin is a recombinant form of hirudin, an endogenous anticoagulant found in medicinal leeches.
Cơ Chế Tác Dụng : Lepirudin is identical to natural hirudin except for substitution of leucine for isoleucine at the N-terminal end of the molecule and the absence of a sulfate group on the tyrosine at position 63. It is produced via yeast cells. Lepirudin forms a stable non-covalent complex with alpha-thrombin, thereby abolishing its ability to cleave fibrinogen and initiate the clotting cascade. The inhibition of thrombin prevents the blood clotting cascade.
Dược Động Học :
▧ Absorption :
Bioavailability is 100% following injection.
▧ Volume of Distribution :
* 12.2 L [Healthy young subjects (n = 18, age 18-60 years)] * 18.7 L [Healthy elderly subjects (n = 10, age 65-80 years)] * 18 L [Renally impaired patients (n = 16, creatinine clearance below 80 mL/min)] * 32.1 L [HIT patients (n = 73)]
▧ Metabolism :
Lepirudin is thought to be metabolized by release of amino acids via catabolic hydrolysis of the parent drug. However, con-clusive data are not available. About 48% of the administration dose is excreted in the urine which consists of unchanged drug (35%) and other fragments of the parent drug.
▧ Route of Elimination :
Lepirudin is thought to be metabolized by release of amino acids via catabolic hydrolysis of the parent drug. About 48% of the administration dose is excreted in the urine which consists of unchanged drug (35%) and other fragments of the parent drug.
▧ Half Life :
Approximately 1.3 hours
▧ Clearance :
* 164 ml/min [Healthy 18-60 yrs] * 139 ml/min [Healthy 65-80 yrs] * 61 ml/min [renal impaired] * 114 ml/min [HIT (Heparin-induced thrombocytopenia)]
Độc Tính : In case of overdose (eg, suggested by excessively high aPTT values) the risk of bleeding is increased.
Chỉ Định : For the treatment of heparin-induced thrombocytopenia
Tương Tác Thuốc :
  • Ginkgo biloba Additive anticoagulant/antiplatelet effects may increase bleed risk. Concomitant therapy should be avoided.
  • Treprostinil The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the anticoagulant, Lepirudin. Monitor for increased bleeding during concomitant thearpy.
Liều Lượng & Cách Dùng : Powder, for solution - Intravenous
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Refludan 50 mg vial
    Giá bán buôn : USD >273.19
    Đơn vị tính : vial
Nhà Sản Xuất
  • Công ty : Berlex Labs
    Sản phẩm biệt dược : Refludan
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00001
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D06880
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/50419-150-57
PharmGKB
http://www.pharmgkb.org/drug/PA450195
Wikipedia
http://en.wikipedia.org/wiki/Lepirudin
RxList
http://www.rxlist.com/cgi/generic/lepirudin.htm
Drugs.com
http://www.drugs.com/cdi/lepirudin.html
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