Therapeutic Efficacy and Mechanism of Action of Ethamsylate, a Long-Standing Hemostatic Agent

Abstract

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.

Neonatal posthemorrhagic hydrocephalus from prematurity: pathophysiology and current treatment concepts

“…60 Etamsyl-ate (formerly ethamsylate), a synthetic hemostatic agent, improves platelet adhesion via P-selectin and restores capillary resistance. 35 A meta-analysis of etamsylate showed that, although there was no difference in neonatal mortality or neurodevelopmental outcome at 2 years, there was a decrease in IVH at 31 and 35 weeks’ EGA, without the identifcation of adverse effects. 44 Currently, antenatal cor-ticosteroid administration has shown the most effective reduction in the IVH incidence.…”

Beneficial effects of early hemostasis on spinal cord injury in the rat

“…Etamsylate, also named Ethamsylate, which acts on the first step of hemostasis by improving platelet adhesiveness and restoring capillary resistance, 12, 13 has been effectively and safely used in clinical cases such as menorrhagia, periventricular hemorrhage and postsurgical bleeding without severe side effect, except it may cause mild skin allergy. 12, 14 Blood flow changes should be considered when hemostatic treatment was used.…”

Treatment of Persistent Gross Hematuria with Tranexamic Acid in Autosomal Dominant Polycystic Kidney Disease

“…In the current study, the platelet count was increased by etamsylate treatment. Besides, etamsylate is a hemostatic agent working through improving platelet adhesiveness and restoring capillary resistance [12]. However, the less potent effect of etamsylate on persistent gross hematuria in ADPKD was probably due to the reported mild hemostatic effect of this agent and less pathogenic importance of platelets in ADPKD.…”

“…However, the evidence for efficacy of TXA treatment in ADPKD is limited since only 8 ADPKD patients were involved in a prospective uncontrolled study and two other TXA treated ADPKD patients were reported as case studies. Etamsylate is a widely-used hemostatic agent, which displays therapeutic benefits in dysfunctional uterine bleeding, periventricular hemorrhage, and surgical or postsurgical capillary bleeding through improving platelet adhesiveness and restoring capillary resistance [12]. We have used etamsylate as a hemostatic agent to stop cystic bleeding in clinical practice in our department.…”