日志
氨甲环酸 Tranexamic Acid (DB00302)
热度 1 ||
转自：http://www.drugbank.ca/drugs/DB00302
| Version | 2.5 | ||||||
| Creation Date | 2005-06-13 13:24:05 | ||||||
| Update Date | 2008-08-26 14:01:09 | ||||||
| Primary Accession Number | DB00302 | ||||||
| Secondary Accession Number |
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| Name | Tranexamic Acid | ||||||
| Drug Type |
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| Description | Antifibrinolytic hemostatic used in severe hemorrhage. [PubChem] | ||||||
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| Brand Names |
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| Brand Mixtures | Not Available | ||||||
| Chemical IUPAC Name | 4-(aminomethyl)cyclohexane-1-carboxylic acid | ||||||
| Chemical Formula | C8H15NO2 | ||||||
| Chemical Structure | |||||||
| CAS Registry Number | 1197-18-8 | ||||||
| InChI Identifier | InChI=1/C8H15NO2/c9-5-6-1-3-7(4-2-6)8(10)11/h6-7H,1-5,9H2,(H,10,11)/f/h10H | ||||||
| InChI Key | GYDJEQRTZSCIOI-KZFATGLACS | ||||||
| KEGG Drug | D01136  |
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| KEGG Compound | Not Available | ||||||
| PubChem Compound | 5526 |
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| PubChem Substance | 582925 |
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| ChEBI ID | Not Available | ||||||
| PharmGKB ID | PA451738 |
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| HET ID | AMH |
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| GenBank ID | Not Available | ||||||
| Drug ID Number [DIN] | 02064413 |
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| RxList Link | http://www.rxlist.com/cgi/generic3/cyclapron.htm |
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| PDRhealth Link | Not Available | ||||||
| Wikipedia Link | http://en.wikipedia.org/wiki/Tranexamic_acid |
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| FDA Label | Not Available | ||||||
| Material Safety Data Sheet (MSDS) | |||||||
| Synthesis Reference | Not Available | ||||||
| Average Molecular Weight | 157.2102 | ||||||
| Monoisotopic Molecular Weight | 157.1103 | ||||||
| State | Solid | ||||||
| Melting Point | >300 oC | ||||||
| Experimental Water Solubility | 1.67E+005 mg/L Source: PhysProp | ||||||
| Predicted Water Solubility | 1.82e+01 mg/mL Calculated using ALOGPS | ||||||
| Experimental LogP/Hydrophobicity | 0.3 Source: PhysProp | ||||||
| Predicted LogP | -1.42 Calculated using ALOGPS | ||||||
| Experimental LogS | Not Available | ||||||
| Predicted LogS | -0.94 Calculated using ALOGPS | ||||||
| Experimental Caco2 Permeability | Not Available | ||||||
| pKa/Isoelectric Point | Not Available | ||||||
| Mass Spectrum | Not Available | ||||||
| MOL File | Show | Download |
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| SDF File | Show | Download |
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| PDB File | Show | Download |
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| 2D Structure | |||||||
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| Experimental PDB ID | 1B2I |
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| Experimental PDB File | Show | ||||||
| Experimental PDB Structure | |||||||
| Isomeric SMILES | NC[C@H]1CC[C@H](CC1)C(O)=O | ||||||
| Canonical SMILES | NCC1CCC(CC1)C(O)=O | ||||||
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| Indication | 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. | ||||||
| Pharmacology | 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).氨甲环酸是一种人工合成药物，特异性与纤溶酶原相结合，它与纤溶酶原的强受体和弱受体均可牢固结合，因此其功能与浓度间有一定比例关系。1mg/ml的氨甲环酸不会造成血小板凝集。在遗传性出血性水肿患者中，氨甲环酸可以通过抑制纤溶酶的形成而避免因后者引发的补体蛋白（C1）激活。 |
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| Mechanism of Action | 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.氨甲环酸通过结合纤维蛋白酶原三环状结构区域，可以竞争抑制其活性，从而使其无法向纤维蛋白酶转化；后者对于降解纤维凝块、纤维蛋白及其他凝血蛋白原有重要作用。氨甲环酸还可以间接抑制纤溶酶的活性，但达到这种效果可能需要较高的浓度。 | ||||||
| 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.人体口服后大约有30%到50%的生物活性不会受到影响。 | ||||||
| Toxicity | Oral LD50 in mice is >10 gm/kg. Symptoms of overdosage may be nausea, vomiting, orthostatic symptoms and/or hypotension. | ||||||
| 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).治疗水平的氨甲环酸蛋白结合率大概在3%左右，应该大多数都是与纤溶酶原蛋白相结合的。 | ||||||
| Biotransformation | Only a small fraction of the drug is metabolized (less than 5%). | ||||||
| Half Life | Biological half-life in the joint fluid is about 3 hours. | ||||||
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| Patient Information | Not Available | ||||||
| Contraindications | Show |
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| Interactions | Show |
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| Drug Interactions | Not Available | ||||||
| Food Interactions | Not Available | ||||||
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发表评论 评论 (3 个评论)
- 回复 陆医生
- 抑肽酶看起来就复杂多了，http://www.drugbank.ca/drugs/DB06692，分子量是氨甲环酸的41.5倍左右。
- 回复 陆医生
- 氨基己酸，跟氨甲环酸类似。http://www.drugbank.ca/drugs/DB00513
