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Aminocaproic Acid
Các tên gọi khác (21 ) :
  • 6-Aminocaproic acid
  • 6-aminohexanoic acid
  • Acide aminocaproïque
  • Acide aminocaproque
  • Ácido aminocapróico
  • Acidum Aminocaproicum
  • Ahx
  • AMICAR
  • AMINOCAPROIC
  • Aminocaproic acid
  • Aminocapronsäure
  • Aminohexanoic acid
  • Caproamin
  • Eaca
  • EACA
  • Epsicaprom
  • Epsilcapramine
  • epsilon-Ahx
  • Epsilon-Aminocaproic Acid
  • epsilon-Aminohexanoic acid
  • Z
Thuốc Gốc
Small Molecule
CAS: 60-32-2
ATC: B02AA01
ĐG : American Regent , http://www.americanregent.com
CTHH: C6H13NO2
PTK: 131.1729
An antifibrinolytic agent that acts by inhibiting plasminogen activators which have fibrinolytic properties. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
Phân tử khối
131.1729
Monoisotopic mass
131.094628665
InChI
InChI=1S/C6H13NO2/c7-5-3-1-2-4-6(8)9/h1-5,7H2,(H,8,9)
InChI Key
InChIKey=SLXKOJJOQWFEFD-UHFFFAOYSA-N
IUPAC Name
6-aminohexanoic acid
Traditional IUPAC Name
aminocaproic acid
SMILES
NCCCCCC(O)=O
Độ tan chảy
205 °C
Độ hòa tan
5.05E+005 mg/L (at 25 °C)
logP
-2.95
logS
-0.46
pKa (strongest acidic)
4.73
pKa (Strongest Basic)
10.21
PSA
63.32 Å2
Refractivity
34.66 m3·mol-1
Polarizability
14.71 Å3
Rotatable Bond Count
5
H Bond Acceptor Count
3
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
0
Bioavailability
1
Rule of Five
true
pKa
4.43 (at 25 °C)
Dược Lực Học : Aminocaproic acid works as an antifibrinolytic. It is a derivative of the amino acid lysine. The fibrinolysis-inhibitory effects of aminocaproic acid appear to be exerted principally via inhibition of plasminogen activators and to a lesser degree through antiplasmin activity. Aminocaproic acid may be a possible prophylactic for vascular disease, as it may prevent formation of lipoprotein (a), a risk factor for vascular disease.
Cơ Chế Tác Dụng : An antifibrinolytic agent that acts by inhibiting plasminogen activators which have fibrinolytic properties. [PubChem] Aminocaproic acid binds reversibly to the kringle domain of plasminogen and blocks the binding of plasminogen to fibrin and its activation to plasmin. With NO activation of plasmin, there is a reduction in fibrinolysis. This consequently will reduce the amount of bleeding post surgery. Elevated plasma levels of lipoprotein(a) have been shown to increase the risk of vascular disease. Lipoprotein 9a)a has two components, apolipoprotein B-100, linked to apolipoprotein (a). Aminocaproic acid may change the conformation of apoliprotein (a), changing its binding properties and potentially preventing the formation of lipoprotein (a).
Dược Động Học :
▧ Absorption :
Absorbed rapidly following oral administration. In adults, oral absorption appears to be a zero-order process with an absorption rate of 5.2 g/hr. The mean lag time in absorption is 10 minutes. After a single oral dose of 5 g, absorption was complete (F=1).
▧ Volume of Distribution :
* 23.1 ± 6.6 L
▧ Metabolism :
Sixty-five percent of the dose is recovered in the urine as unchanged drug and 11% of the dose appears as the metabolite adipic acid.
▧ Route of Elimination :
Renal excretion is the primary route of elimination, whether aminocaproic acid is administered orally or intravenously.
▧ Half Life :
The terminal elimination half-life is approximately 2 hours.
▧ Clearance :
* 169 mL/min
Độc Tính : A few cases of acute overdosage with intravenous administration have been reported. The effects have ranged from no reaction to transient hypotension to severe acute renal failure leading to death. The intravenous and oral LD50 were 3.0 and 12.0 g/kg respectively in the mouse and 3.2 and 16.4 g/kg respectively in the rat. An intravenous infusion dose of 2.3 g/kg was lethal in the dog.
Chỉ Định : For use in the treatment of excessive postoperative bleeding.
Liều Lượng & Cách Dùng : Injection, solution - Intravenous
Syrup - Oral
Tablet - Oral
Dữ Kiện Thương Mại
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