e141
etamsylate
CAS: 2624-44-4
Molecular Formula: C10H17NO5S
e141 - Names and Identifiers
| Name | etamsylate |
| Synonyms | e141 md141 eselin altodor etamsylate Ethamsylate diethylammonium 2,5-dihydroxybenzenesulphonate 2,5-dihydroxy-benzenesulfonicacicompd.withdiethylamine 2,5-DihydroxybenzenesulfonicacidcompdwithN-ethylethanamine 2,5-dihydroxybenzenesulfonicacidcompd.withn-ethylethanamine |
| CAS | 2624-44-4 |
| EINECS | 220-090-7 |
| InChI | InChI=1/C6H6O5S.C4H11N/c7-4-1-2-5(8)6(3-4)12(9,10)11;1-3-5-4-2/h1-3,7-8H,(H,9,10,11);5H,3-4H2,1-2H3 |
| InChIKey | HBGOLJKPSFNJSD-UHFFFAOYSA-N |
e141 - Physico-chemical Properties
| Molecular Formula | C10H17NO5S |
| Molar Mass | 263.31 |
| Density | 1.3441 (rough estimate) |
| Melting Point | 125° |
| Boling Point | 496.4°C at 760 mmHg |
| Flash Point | 254°C |
| Solubility | DMSO 53 mg/mL Water 53 mg/mL Ethanol <1 mg/mL |
| Vapor Presure | 1.13E-10mmHg at 25°C |
| Appearance | Crystalline powder |
| Color | White to Pale Red |
| Merck | 14,3722 |
| Storage Condition | Keep in dark place,Inert atmosphere,Room temperature |
| Stability | Hygroscopic |
| Refractive Index | 1.5060 (estimate) |
| Physical and Chemical Properties | White crystalline powder. Melting point 125 °c (127-131 °c). Soluble in water, soluble in ethanol, acetone-soluble, insoluble in chloroform, ether. There is hygroscopicity, easy to deteriorate in light. Odorless and bitter. |
| Use | For the prevention and treatment of bleeding before surgery, but also for intestinal bleeding, cerebral hemorrhage and urinary tract bleeding |
e141 - Risk and Safety
| RTECS | DB6145000 |
| Hazard Class | IRRITANT |
| Toxicity | LD50 i.v. in mice, rats: 800, 1350 mg/kg (Esteve) |
e141 - Reference
| Reference Show more | 1. Chen Ya-hong, Tian Hao, Fan Xiao-rui. Enzyme-catalyzed fluorimetric determination of etamsylate [J]. Pharmaceutical Analysis, 2011, 26 (05):973-976. |
e141 - Reference Information
| EPA chemical information | Information provided by: ofmpub.epa.gov (external link) |
| introduction | ethamsylate is also known as hemostatic sensitivity, and its chemical name is 2, 5-dihydroxybenzenesulfonate diethylamine salt. ethamsylate plays a role by promoting the coagulation process. It can increase the number of platelets in the blood, enhance their aggregation and adhesion, and promote the release of coagulation substances to accelerate coagulation. It is clinically used to prevent and treat hemorrhage caused by surgical excessive bleeding, thrombocytopenic purpura or allergic purpura and other reasons. [classification] proclotting factor active drugs [structural characteristics] drugs that are easily affected by light and deteriorate |
| traits | this product is a white or white-like loose lump. |
| pharmacological action | ethamsylate can increase the number of platelets, enhance their aggregation and adhesion, promote platelets to release coagulants, shorten coagulation time and accelerate blood clot contraction. In addition, it has the effects of enhancing capillary resistance, reducing its permeability, and reducing blood exudation. The hemostatic effect of this product is rapid, and the effect reaches a peak 1 hour after intravenous injection, and the efficacy can be maintained for 4-6 hours. |
| indications | ethamsylate is suitable for the prevention and treatment of surgical bleeding, thrombocytopenic purpura or allergic purpura and bleeding caused by other reasons, such as cerebral hemorrhage, gastrointestinal bleeding, urinary tract bleeding, fundus bleeding, gingival bleeding, epistaxis, etc. It can be used together with other hemostatic drugs such as aminomethylbenzoic acid and vitamin K. |
| pharmacokinetics | oral absorption is easy, intravenous injection reaches a peak for 1 hour, and the effect is maintained for 4-6 hours. It is mainly excreted from the kidney in its original form, and a small amount of bile is excreted with feces. |
| usage and dosage | 1. prevention of surgical hemorrhage: intramuscular injection or intravenous injection of 0.25~0.5g 15~30 minutes before operation, and repeat once after 2 hours if necessary. 2. treatment: adult dosage: oral administration: 0.5~1g each time, 3 times a day; Intramuscular injection or intravenous injection: 0.25~0.5g each time, 2~3 times a day; Intravenous drip: 2.5~5g each time, diluted with 500ml of 5% glucose solution and then instilled, no more than 5mg per minute. Dosage for children: oral: 10mg/kg, 3 times a day. |
| adverse reactions | adverse reactions are mild, occasionally nausea, headache and rash. Under general anesthesia, blood pressure may drop when intravenous injection is too fast. |
| precautions | 1. those with a history of thrombosis should use it with caution. 2. High molecular weight plasma expanders (such as dextran) can be used after this product is used and not before it is used. 3. This product should not be mixed with other drugs, especially mixed with alkaline drugs, which can make this product change color and fail. |
| production method | the production method of ethamsylate on the market now includes benzoquinone method, in which benzoquinone method is to pass sulfur dioxide into a solution of diethylamine, ethanol and water to first prepare diethylamine sulfite, then add p-benzoquinone to diethylamine sulfite solution at low temperature, distill ethanol under reduced pressure after reaction, and precipitate crude products after cooling, add sodium bisulfite and activated carbon to water or dilute ethanol to decolorize and refine the product. The disadvantage of this process is: due to the incomplete reaction of p-benzoquinone, and the solubility of ethamsylate in water and ethanol is relatively large, So that the product yield is low, generally not more than 40%, and the price of p-benzoquinone is high, and the use of sulfur dioxide has problems such as exhaust gas absorption. In addition, chlorosulfonic acid is used as a sulfonating agent on the market. Before sulfonation, hydroquinone and organic solvent are azeotropic and dehydrated to anhydrous, but this method uses organic solvents to pollute the environment. The hydrogen chloride gas produced during the sulfonation reaction pollutes the environment. It is obtained by adding diethylamine with sulfur dioxide to salt and p-benzodiquinone. Diethylamine, ethanol and water are added to the reaction pot, cooled to 0 ℃, sulfur dioxide is introduced until the pH of the reaction solution is 3.5-4, and the reaction temperature is controlled below 10 ℃ to obtain diethylamine sulfite solution. Then, p-benzodiquinone was slowly added at 0-10 ℃. After addition, ethanol is recovered under reduced pressure, crystallization is cooled and filtered. Crystallization is heated and dissolved in distilled water, and decolorized and refined with activated carbon to obtain ethamsylate finished product. |
| drug interaction | intravenous injection of polymer plasma extender should be after using this product instead of before use, because dextran and the like inhibit platelet aggregation, prolong bleeding and clotting time, which is theoretically antagonistic to this product. Do not mix with aminocaproic acid injection to avoid poisoning; should not be compatible with alkaline drugs. |
| mechanism of action | can enhance platelet function, reduce capillary permeability, reduce blood exudation, show hemostatic effect, increase the number of platelets in blood, enhance its aggregation and adhesion, promote the release of coagulants, shorten coagulation time, and accelerate blood clot contraction. |
| use | this product can increase the number, aggregation and adhesion of platelets and promote the release of coagulants from platelets. It can also accelerate the contraction of blood clots, shorten the clotting time, and can also enhance capillary resistance and reduce capillary permeability. It is used to prevent and treat bleeding before surgery. It is also used for bleeding caused by platelet insufficiency or other causes of bleeding, such as gastrointestinal bleeding, cerebral hemorrhage and urinary bleeding. Intravenous LD50 in rats was 800-1350 mg/kg. It is used to prevent and treat bleeding before surgery, and it is also used for intestinal bleeding, cerebral hemorrhage and urinary tract bleeding. |
Last Update：2024-04-09 21:01:54
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