Hemostatic;prostaglandin synthesis inhibitor
Haemostatic / Anti Coagulant
ChEBI: Etamsylate is a sulfonic acid derivative and an organosulfur compound.
Etamsylate is a haemostatic agent th at is used for the management of blood loss. Apparently etamsylate increases capillary wall resistance and platelet adhesives by inhibition of the biosynthesis of prostaglandins causing platelet disaggregation in a presence of vascular wound. Recent studies suggest th at etamsylate antagonizes anti-coagulant activity of heparin.
Etamsylate is an antihaemorrhagic and vasoprotective agent. It increases platelet adhesiveness and capillary vascular wall resistance, thereby reducing capillary exudation and blood loss.
Short-term treatment of blood loss in menorrhagiaProphylaxis of surgical bleeding (unlicensed)
Significant: Hypotension (parenteral). Rarely, severe hypersensitivity reaction, including anaphylaxis.
Blood and lymphatic system disorders: Parenteral: Rarely, neutropenia, agranulocytosis, thrombocytopenia.
Gastrointestinal disorders: Nausea, vomiting, diarrhoea, abdominal pain or discomfort.
General disorders and administration site conditions: Asthenia (parenteral). Rarely, fever.
Musculoskeletal and connective tissue disorders: Rarely, arthralgia.
Nervous system disorders: Headache.
Skin and subcutaneous tissue disorders: Rash.
Vascular disorders: Rarely, thromboembolism (parenteral).
Nowadays, the production methods of etamsylate in the market are benzoquinone method, in which benzoquinone method is to pass sulfur dioxide in the solution of diethylamine, ethanol and water, and then make diethylamine sulfite salt, then add p-benzoquinone into diethylamine sulfite salt solution under low temperature, and then distill and recycle the ethanol under reduced pressure after the reaction is finished and precipitate out the crude product after cooling, and then add sodium bisulfite and activated carbon to decolorize it in the water or diluted ethanol and then refine it to obtain the product, the The disadvantages of the process are: due to the incomplete reaction of p-benzoquinone, coupled with the solubility of phenolsulfonyl ethylamine in water and ethanol, so that the product yield is low, generally not more than 40%, and p-benzoquinone is more expensive, the use of sulfur dioxide, there are problems such as absorption of the tail gas.
Also on the market is the use of chlorosulfonic acid as a sulfonation agent, before sulfonation so that p-benzoquinone and organic solvents azeotropic dehydration to anhydrous, but this method uses organic solvents, pollution of the environment, which in the process of sulfonation reaction of hydrogen chloride gas, pollution of the environment.
Etamsylate is excreted unchanged, mainly in the urine.
