Ethamsylate (2,5-dihydroxy-benzene-sulfonate diethylammonium salt) is a synthetic
hemostatic drug indicated in cases of capillary
bleeding. This review covers more than 40 years of intensive clinical and fundamental research with
ethamsylate. First, we summarize the large medical literature concerning its clinical efficacy. Of these, well-controlled clinical trials clearly showed the therapeutic efficacy of
ethamsylate in
dysfunctional uterine bleeding, with the magnitude of blood-loss reduction being directly proportional to the severity of the
menorrhagia. Other well-controlled clinical trials showed therapeutic efficacy of
ethamsylate in periventricular
hemorrhage in very low birth weight babies and surgical or postsurgical capillary
bleeding. Second, we review the numerous investigations performed to elucidate the mechanism of action of
ethamsylate.
Ethamsylate acts on the first step of hemostasis by improving platelet adhesiveness and restoring capillary resistance. Recent studies showed that
ethamsylate promotes
P-selectin-dependent, platelet adhesive mechanisms. Finally, we compare
ethamsylate with other recent
hemostatic agents. It is suggested that the place of
ethamsylate as a
hemostatic agent is that of a mild but well-tolerated
drug, particularly useful in
dysfunctional uterine bleeding when
contraception is not needed.