Tìm theo
Tranexamic Acid
Các tên gọi khác (12 ) :
  • Acide tranexamique
  • Acido tranexamico
  • Acidum tranexamicum
  • Cyklokapron
  • Tranexamsaeure
  • Tranexmic acid
  • Tranhexamic acid
  • Trans AMCHA
  • trans-4-(Aminomethyl)cyclohexanecarboxylic acid
  • trans-4-aminomethylcyclohexane-1-carboxylic acid
  • trans-Amcha
  • trans-Tranexamic acid
Thuốc tác dụng đối với máu
Thuốc Gốc
Small Molecule
CAS: 1197-18-8
ATC: B02AA02
ĐG : Gallipot , http://www.gallipot.com
CTHH: C8H15NO2
PTK: 157.2102
Antifibrinolytic hemostatic used in severe hemorrhage. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C8H15NO2
Phân tử khối
157.2102
Monoisotopic mass
157.110278729
InChI
InChI=1S/C8H15NO2/c9-5-6-1-3-7(4-2-6)8(10)11/h6-7H,1-5,9H2,(H,10,11)/t6-,7-
InChI Key
InChIKey=GYDJEQRTZSCIOI-LJGSYFOKSA-N
IUPAC Name
(1r,4r)-4-(aminomethyl)cyclohexane-1-carboxylic acid
Traditional IUPAC Name
cyklokapron
SMILES
NC[C@H]1CC[C@@H](CC1)C(O)=O
Độ tan chảy
>300 °C
Độ hòa tan
1.67E+005 mg/L
logP
0.3
logS
-0.94
pKa (strongest acidic)
4.56
pKa (Strongest Basic)
10.22
PSA
63.32 Å2
Refractivity
41.9 m3·mol-1
Polarizability
17.28 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
3
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
1
Bioavailability
1
Rule of Five
true
Dược Lực Học : Tranexamic acid is an antifibrinolytic that competitively inhibits the activation of plasminogen to plasmin. Tranexamic acid is a competitive inhibitor of plasminogen activation, and at much higher concentrations, a noncompetitive inhibitor of plasmin, i.e., actions similar to aminocaproic acid. Tranexamic acid is about 10 times more potent in vitro than aminocaproic acid. Tranexamic acid binds more strongly than aminocaproic acid to both the strong and weak receptor sites of the plasminogen molecule in a ratio corresponding to the difference in potency between the compounds. Tranexamic acid in a concentration of 1 mg per mL does not aggregate platelets in vitro. In patients with hereditary angioedema, inhibition of the formation and activity of plasmin by tranexamic acid may prevent attacks of angioedema by decreasing plasmin-induced activation of the first complement protein (C1).
Cơ Chế Tác Dụng : Antifibrinolytic hemostatic used in severe hemorrhage. [PubChem] Tranexamic acid competitively inhibits activation of plasminogen (via binding to the kringle domain), thereby reducing conversion of plasminogen to plasmin (fibrinolysin), an enzyme that degrades fibrin clots, fibrinogen, and other plasma proteins, including the procoagulant factors V and VIII. Tranexamic acid also directly inhibits plasmin activity, but higher doses are required than are needed to reduce plasmin formation.
Dược Động Học :
▧ Absorption :
Absorption of tranexamic acid after oral administration in humans represents approximately 30 to 50% of the ingested dose and bioavailability is not affected by food intake.
▧ Volume of Distribution :
* 9 to 12 L
▧ Protein binding :
The plasma protein binding of tranexamic acid is about 3% at therapeutic plasma levels and seems to be fully accounted for by its binding to plasminogen (does not bind serum albumin).
▧ Metabolism :
Only a small fraction of the drug is metabolized (less than 5%).
▧ Route of Elimination :
Urinary excretion is the main route of elimination via glomerular filtration.
▧ Half Life :
Biological half-life in the joint fluid is about 3 hours.
▧ Clearance :
* 110 - 116 mL/min
Độc Tính : Oral LD50 in mice is >10 gm/kg. Symptoms of overdosage may be nausea, vomiting, orthostatic symptoms and/or hypotension.
Chỉ Định : For use in patients with hemophilia for short term use (two to eight days) to reduce or prevent hemorrhage and reduce the need for replacement therapy during and following tooth extraction. It can also be used for excessive bleeding in menstruation, surgery, or trauma cases.
Liều Lượng & Cách Dùng : Solution - Intravenous
Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Cyclo-F
  • Công ty :
    Sản phẩm biệt dược : Cyklokapron
  • Công ty :
    Sản phẩm biệt dược : Espercil
  • Công ty :
    Sản phẩm biệt dược : Femstrual
  • Công ty :
    Sản phẩm biệt dược : Lysteda
  • Công ty :
    Sản phẩm biệt dược : Rikavarin
  • Công ty :
    Sản phẩm biệt dược : Transamin
  • Công ty :
    Sản phẩm biệt dược : Transcam
  • Công ty :
    Sản phẩm biệt dược : Traxyl
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00302
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D01136
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0013-1114-10
PharmGKB
http://www.pharmgkb.org/drug/PA164750514
Wikipedia
http://en.wikipedia.org/wiki/Tranexamic_acid
RxList
http://www.rxlist.com/cgi/generic3/cyclapron.htm
Drugs.com
http://www.drugs.com/cdi/tranexamic-acid.html
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