Etamsylate 500mg/5ml oral solution

The diagnosis of hereditary hemorrhagic telangiectasia (HHT) is based on the Curaçao criteria: epistaxis, telangiectases, arteriovenous malformations in internal organs, and family history. Genetically speaking, more than 90% of HHT patients show mutations in ENG or ACVRL1/ALK1 genes, both belonging to the TGF-β/BMP9 signaling pathway. Despite clear knowledge of the symptoms and genes of the disease, we still lack a definite cure for HHT, having just palliative measures and pharmacological trials. Among the former, two strategies are: intervention at "ground zero" to minimize by iron and blood transfusions in order to counteract anemia. Among the later, along the last 15 years, three different strategies have been tested: (1) To favor coagulation with antifibrinolytic agents (tranexamic acid); (2) to increase transcription of ENG and ALK1 with specific estrogen-receptor modulators (bazedoxifene or raloxifene), antioxidants (N-acetylcysteine, resveratrol), or immunosuppressants (tacrolimus); and (3) to impair the abnormal angiogenic process with antibodies (bevacizumab) or blocking drugs like etamsylate, and propranolol. This manuscript reviews the main strategies and sums up the clinical trials developed with drugs alleviating HHT.

Abstract licence: CC BY

Abstract The objective of this study was to investigate the effect of etamsylate on canine blood and heparinised canine blood from healthy dogs using thromboelastography (TEG). Citrated blood was obtained from twenty healthy client-owned dogs, and 3 experiments were performed. Experiment 1 compared TEG in blood versus blood with etamsylate (250 mM). Experiment 2 evaluated TEG in heparinised blood (1 U/mL) with and without the addition of etamsylate (250 mM). Experiment 3 evaluated dose escalation of etamsylate (control, 250 μM, 500 μM and 1000 μM) in heparinised blood (1 U/mL). The addition of etamsylate to canine blood in experiment 1 increased the percentage of clot lysis at 30 min (z = −2.103, p = .035) and 60 min (z = −1.988, p = .047), suggesting that etamsylate could have a fibrinolytic effect. When etamsylate was added to heparinised canine blood (1 U/mL), etamsylate produced a dose-dependent inhibition of the effect of heparin when higher concentrations of etamsylate were used (500 μM and 1000 μM). The linear mixed effects model showed significant increases in α angle and maximal amplitude when high dose etamsylate was added compared to the control. In conclusion, etamsylate could be used at higher doses to inhibit the effect of heparin in dogs when protamine might not be available. However, etamsylate might have a fibrinolytic effect when used in healthy dogs.

Abstract licence: CC BY 4.0