Tìm theo
Glucarpidase
Các tên gọi khác (4 ) :
  • Carboxypeptidase G2
  • Folate hydrolase G2
  • Glutamate carboxypeptidase
  • Pteroylmonoglutamic acid hydrolase G2
enzymes
Thuốc Gốc
Biotech
CAS: 9074-87-7
ATC: V03AF09
CTHH: C1950H3157N543O599S7
PTK: 44016.6653 g/mol
Glucarpidase is the recombinant form of the Pseudomonas sp. (strain RS-16) enzyme carboxypeptidase G2 that is produced in Escherichia coli. In patients, glucarpidase inactivates methotrexate, and other antifolates, by hydrolyzing glutamate on the carboxyl terminal of these compounds. Therefore since methotrexate is eliminated enzymatically and not by the kidneys, glucarpidase is indicated in patients on methotrexate treatment who have kidney dysfunction, and are experiencing an abnormally high plasma concentration of methotrexate (>1 micromole per liter). Glucarpidase is marketed under the brand name Voraxaze®.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C1950H3157N543O599S7
Phân tử khối
44016.6653 g/mol
Dược Lực Học : Glucarpidase acts as an antidote to toxic methotrexate levels by elminating methotrexate by a non-kidney route.
Cơ Chế Tác Dụng : Glucarpidase is the recombinant form of the Pseudomonas sp. (strain RS-16) enzyme carboxypeptidase G2 that is produced in Escherichia coli. In patients, glucarpidase inactivates methotrexate, and other antifolates, by hydrolyzing glutamate on the carboxyl terminal of these compounds. Therefore since methotrexate is eliminated enzymatically and not by the kidneys, glucarpidase is indicated in patients on methotrexate treatment who have kidney dysfunction, and are experiencing an abnormally high plasma concentration of methotrexate (>1 micromole per liter). Glucarpidase is marketed under the brand name Voraxaze®. Glucarpidase inactivates methotrexate, and other antifolates, by hydrolyzing glutamate on the carboxyl terminal of these compounds. For methotrexate specifically, it is hydrolyzed to the inactive metabolites glutamate and 4-deoxy-4-amino-N10-methylpteroic acid (DAMPA).
Dược Động Học :
▧ Absorption :
In healthy patients not taking methotrexate, the average maximum concentration for glucarpidase was 3.3 μg/mL.
▧ Volume of Distribution :
Glucarpidase is likely limited to the plasma volume since its volume of distribution is 3.6 L.
▧ Protein binding :
Plasma protein binding was not quantified.
▧ Metabolism :
Metabolism was not determined.
▧ Route of Elimination :
Route of elmination was not determined.
▧ Half Life :
In healthy patients not taking methotrexate, glucarpidase has an elimination half-life of 5.6 hours. In patients with severe renal impairment (creatinine clearance <30 mL/min), glucarpidase has an longer elimination half-life at 8.2 hours.
▧ Clearance :
In healthy patients not taking methotrexate, glucarpidase has a clearance of 7.5 mL/min.
Độc Tính : Most common adverse reactions include hypotension, flushing, nausea, vomiting, headache, and paresthesia.
Chỉ Định : Used in patients on methotrexate treatment who have kidney dysfunction, and are experiencing an abnormally high plasma concentration of methotrexate (> 1 micromole per liter).
Tương Tác Thuốc :
  • Leucovorin Do not administer leucovorin within 2 hours of glucarpidase due to the fact that leucovorin is degraded by glucarpidase.
Liều Lượng & Cách Dùng : Injection, powder, lyophilized, for solution - Intravenous - 1000 UNITS PER VIAL
Dữ Kiện Thương Mại
Nhà Sản Xuất
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB08898
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D10260
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/50633-210-11
Wikipedia
http://en.wikipedia.org/wiki/Glucarpidase
RxList
http://www.rxlist.com/voraxaze-drug.htm
Drugs.com
http://www.drugs.com/mtm/glucarpidase.html
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