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药品详细

Aminocaproic Acid(氨基己酸)

化学结构式图
中文名
氨基己酸
英文名
Aminocaproic Acid
分子式
C6H13NO2
化学名
6-aminohexanoic acid
分子量
Average: 131.1729
Monoisotopic: 131.094628665
CAS号
60-32-2
ATC分类
B02A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

An antifibrinolytic agent that acts by inhibiting plasminogen activators which have fibrinolytic properties. [PubChem]

生产厂家
  • Abraxis pharmaceutical products
  • Baxter healthcare corp anesthesia and critical care
  • Hospira inc
  • Luitpold pharmaceuticals inc
  • Mikart inc
  • Xanodyne pharmaceutics inc
封装厂家
参考
Synthesis Reference Not Available
General Reference Not Available
剂型
规格
化合物类型
Type small molecule
Classes
  • Amino Acids
  • Carboxylic Acids and Derivatives
Substructures
  • Amino Acids
  • Hydroxy Compounds
  • Acetates
  • Aliphatic and Aryl Amines
  • Carboxylic Acids and Derivatives
适应症
药理
Indication For use in the treatment of excessive postoperative bleeding.
Pharmacodynamics 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.
Mechanism of action 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).
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
Protein binding Not Available
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.

Important The metabolism module of DrugBank is currently in beta. Questions or suggestions? Please contact us.

Substrate Enzymes Product
Aminocaproic Acid
    		Adipic acid Details
    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
    Toxicity 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.
    Affected organisms
    • Humans and other mammals
    Pathways
    Pathway Name SMPDB ID
    Smp00286 Aminocaproic Acid Pathway SMP00286
    理化性质
    Properties
    State solid
    Experimental Properties
    Property Value Source
    melting point 205 °C PhysProp
    water solubility 5.05E+005 mg/L (at 25 °C) YALKOWSKY,SH & DANNENFELSER,RM (1992)
    logP -2.95 HANSCH,C ET AL. (1995)
    pKa 4.43 (at 25 °C) KORTUM,G ET AL (1961)
    Predicted Properties
    Property Value Source
    water solubility 4.52e+01 g/l ALOGPS
    logP -2.7 ALOGPS
    logP -2 ChemAxon
    logS -0.46 ALOGPS
    pKa (strongest acidic) 4.73 ChemAxon
    pKa (strongest basic) 10.21 ChemAxon
    physiological charge 0 ChemAxon
    hydrogen acceptor count 3 ChemAxon
    hydrogen donor count 2 ChemAxon
    polar surface area 63.32 ChemAxon
    rotatable bond count 5 ChemAxon
    refractivity 34.66 ChemAxon
    polarizability 14.71 ChemAxon
    药物相互作用
    食物相互作用
    • Take without regard to meals.

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