Ethamsylate
Encyclopedia
Ethamsylate is a haemostatic drug
.
It is believed to work by increasing capillary
endothelial resistance and promoting platelet
adhesion.
It also inhibits biosynthesis
and action of those prostaglandin
s which cause platelet disaggregation, vasodilation
and increased capillary permeability.
and their release from bone marrow. Haemostatic action is due to activation of thromboplastin formation on damaged sites of small blood vessels and decrease of PgI2 (Prostacyclin
I2) synthesis; it also facilitates platelet aggregation and adhesion
, that at last induce decrease and stop of hemorrhage.
The precise mechanism of action of etamsylate is unknown. It has been shown to reduce bleeding time and blood loss from wounds. This appears to relate to increased platelet aggregation mediated by a thromboxane A2 or prostaglandin F2a dependent mechanism. It has also been associated with decreased concentrations of 6-oxoprostaglandin F1a, a stable metabolite of prostacyclin. Prostacyclin is a potent vasodilator, and may be implicated in reperfusion; it is also a disaggregator of platelets. Whereas prostaglandins themselves may have a role in regulating cerebral blood flow, etamsylate appears to have no effect on cerebral blood flow. Etamsylate was also thought to stabilise capillaries, reinforcing capillary membranes by polymerising hyaluronic acid.
Etamsylate limits capillary bleeding through its action on hyaluronic acid and initial studies showed a reduction in intraventricular haemorrhage.
Etamsylate may also have an effect on the microcirculation, encouraging platelet aggregation and vasoconstriction and therefore haemostasis. It also inhibits the effects of the prostaglandin mediated vasodilatation and increased capillary permeability, thereby reducing oedema secondary to capillary leakage. It is also possible that etamsylate would reduce reperfusion haemorrhage in ischaemic areas of the brain, preventing secondary damage.
By inhibiting the effects of prostaglandins, etamsylate may exert an effect by closing the patent ductus
and thereby increasing cerebral blood flow.
Drug
A drug, broadly speaking, is any substance that, when absorbed into the body of a living organism, alters normal bodily function. There is no single, precise definition, as there are different meanings in drug control law, government regulations, medicine, and colloquial usage.In pharmacology, a...
.
It is believed to work by increasing capillary
Capillary
Capillaries are the smallest of a body's blood vessels and are parts of the microcirculation. They are only 1 cell thick. These microvessels, measuring 5-10 μm in diameter, connect arterioles and venules, and enable the exchange of water, oxygen, carbon dioxide, and many other nutrient and waste...
endothelial resistance and promoting platelet
Platelet
Platelets, or thrombocytes , are small,irregularly shaped clear cell fragments , 2–3 µm in diameter, which are derived from fragmentation of precursor megakaryocytes. The average lifespan of a platelet is normally just 5 to 9 days...
adhesion.
It also inhibits biosynthesis
Biosynthesis
Biosynthesis is an enzyme-catalyzed process in cells of living organisms by which substrates are converted to more complex products. The biosynthesis process often consists of several enzymatic steps in which the product of one step is used as substrate in the following step...
and action of those prostaglandin
Prostaglandin
A prostaglandin is any member of a group of lipid compounds that are derived enzymatically from fatty acids and have important functions in the animal body. Every prostaglandin contains 20 carbon atoms, including a 5-carbon ring....
s which cause platelet disaggregation, vasodilation
Vasodilation
Vasodilation refers to the widening of blood vessels resulting from relaxation of smooth muscle cells within the vessel walls, particularly in the large arteries, smaller arterioles and large veins. The process is essentially the opposite of vasoconstriction, or the narrowing of blood vessels. When...
and increased capillary permeability.
Indications
Prophylaxis and control of haemorrhages from small blood vessels, neonatal intraventricular haemorrhage , capillary bleeding of different etiology, including: menorrhagia and metrorrhagia without organic pathology, after trans-urethral resection of the prostate, hematemesis, melena, hematuria, epistaxis; secondary bleeding due to thrombocytopenia or thrombocytopathia, hypocoagulation, prevention of periventricular hemorrhages in prematurely born children.Mechanism of action
Ethamsylate is a haemostatic agent; also promotes angioprotective and proaggregant action. It stimulates thrombopoiesisThrombopoiesis
Thrombopoiesis refers to the process of thrombocyte generation.Thromobocytes are ligations of the cytoplasm from megakaryocytes. A single megakaryocyte can give rise to thousands of thrombocytes....
and their release from bone marrow. Haemostatic action is due to activation of thromboplastin formation on damaged sites of small blood vessels and decrease of PgI2 (Prostacyclin
Prostacyclin
Prostacyclin is a member of the family of lipid molecules known as eicosanoids.As a drug, it is also known as "epoprostenol". The terms are sometimes used interchangeably.-History:...
I2) synthesis; it also facilitates platelet aggregation and adhesion
Adhesion
Adhesion is any attraction process between dissimilar molecular species that can potentially bring them in close contact. By contrast, cohesion takes place between similar molecules....
, that at last induce decrease and stop of hemorrhage.
The precise mechanism of action of etamsylate is unknown. It has been shown to reduce bleeding time and blood loss from wounds. This appears to relate to increased platelet aggregation mediated by a thromboxane A2 or prostaglandin F2a dependent mechanism. It has also been associated with decreased concentrations of 6-oxoprostaglandin F1a, a stable metabolite of prostacyclin. Prostacyclin is a potent vasodilator, and may be implicated in reperfusion; it is also a disaggregator of platelets. Whereas prostaglandins themselves may have a role in regulating cerebral blood flow, etamsylate appears to have no effect on cerebral blood flow. Etamsylate was also thought to stabilise capillaries, reinforcing capillary membranes by polymerising hyaluronic acid.
Etamsylate limits capillary bleeding through its action on hyaluronic acid and initial studies showed a reduction in intraventricular haemorrhage.
Etamsylate may also have an effect on the microcirculation, encouraging platelet aggregation and vasoconstriction and therefore haemostasis. It also inhibits the effects of the prostaglandin mediated vasodilatation and increased capillary permeability, thereby reducing oedema secondary to capillary leakage. It is also possible that etamsylate would reduce reperfusion haemorrhage in ischaemic areas of the brain, preventing secondary damage.
By inhibiting the effects of prostaglandins, etamsylate may exert an effect by closing the patent ductus
and thereby increasing cerebral blood flow.