Chemical formula: C₁₀H₁₇NO₅S Molecular mass: 263.31 g/mol
Etamsylate is a synthetic antihaemorrhagic and angioprotective drug acting on the first step of haemostasis (endothelium-platelet interaction). By improving platelet adhesiveness and restoring capillary resistance, it is able to reduce bleeding time and blood losses.
Etamsylate has no vasoconstrictor action, it does not influence fibrinolysis nor modify the plasma coagulation factors.
When given p.o., etamsylate is slowly absorbed from the gastrointestinal tract. After oral administration of 500 mg etamsylate maximum plasma level, i.e. 15 µg/ml, is reached at 4 h, but bioavailability is not known. The binding rate to plasma proteins is about 95%. Plasma half-life is about 3,7 h. About 72% of the administered dose are excreted in the first 24 hurine; the molecule is excreted unchanged.
After i.v. administration of 500 mg etamsylate, the maximum plasma level, i.e. 50 μg/ml, is reached after 10 minutes; plasma half-life is about 1,9 h. About 85% of the administered dose are excreted in the first 24 h-urine. The molecule is excreted unchanged.
Etamsylate crosses the placental barrier. Maternal and cord blood contains similar concentrations of etamsylate. It is not known if etamsylate is excreted in the maternal milk.
It is not known if the pharmacokinetic properties of etamsylate are modified in patients suffering from renal and/or hepatic function disorders.
Acute and chronic toxicity studies, foetotoxicity and mutagenicity studies on etamsylate have not revealed any toxic effect.
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