Sulodexide, traded as Aterina, is a highly purified mixture of
glycosaminoglycans
Glycosaminoglycans (GAGs) or mucopolysaccharides are long, linear polysaccharides consisting of repeating disaccharide units (i.e. two-sugar units). The repeating two-sugar unit consists of a uronic acid, uronic sugar and an amino sugar, except i ...
composed of
heparan sulfate
Heparan sulfate (HS) is a linear polysaccharide found in all animal tissues. It occurs in a proteoglycan (HSPG, i.e. Heparan Sulfate ProteoGlycan) in which two or three HS chains are attached in close proximity to cell surface or extracellular ma ...
(80%) and
dermatan sulfate
Dermatan sulfate is a glycosaminoglycan (formerly called a mucopolysaccharide) found mostly in skin, but also in blood vessels, heart valves, tendons, and lungs.
It is also referred to as chondroitin sulfate B, although it is no longer classifi ...
(20%).
Pharmacology
The low molecular weight of both sulodexide fractions allows for extensive oral absorption compared to unfractionated
heparin
Heparin, also known as unfractionated heparin (UFH), is a medication and naturally occurring glycosaminoglycan. Heparin is a blood anticoagulant that increases the activity of antithrombin. It is used in the treatment of myocardial infarction, ...
. The pharmacological effects of sulodexide differ substantially from other glycosaminoglycans and are mainly characterized by a prolonged half-life and reduced effect on global coagulation and bleeding parameters. Due to the presence of both glycosaminoglycan fractions, sulodexide potentiates the antiprotease activities of both
antithrombin III
Antithrombin (AT) is a small glycoprotein that inactivates several enzymes of the coagulation system. It is a 464-amino-acid protein produced by the liver. It contains three disulfide bonds and a total of four possible glycosylation sites. α-An ...
and
heparin cofactor II simultaneously.
Uses
Clinically, sulodexide is used for the prophylaxis and treatment of thromboembolic diseases. Research has also demonstrated the beneficial effects of sulodexide in animal models of
reperfusion injury
Reperfusion injury, sometimes called ischemia-reperfusion injury (IRI) or reoxygenation injury, is the tissue damage caused when blood supply returns to tissue ('' re-'' + ''perfusion'') after a period of ischemia or lack of oxygen (anoxia or hy ...
and the treatment of
diabetic nephropathy
Diabetic nephropathy, also known as diabetic kidney disease, is the chronic loss of kidney function occurring in those with diabetes mellitus. Diabetic nephropathy is the leading cause of chronic kidney disease (CKD) and end-stage renal disease ...
.
In combination with
melatonin
Melatonin, an indoleamine, is a natural compound produced by various organisms, including bacteria and eukaryotes. Its discovery in 1958 by Aaron B. Lerner and colleagues stemmed from the isolation of a substance from the pineal gland of cow ...
, sulodexide has been shown to be a viable treatment option for patients suffering from central or sensorineural
tinnitus
Tinnitus is a condition when a person hears a ringing sound or a different variety of sound when no corresponding external sound is present and other people cannot hear it. Nearly everyone experiences faint "normal tinnitus" in a completely ...
.
There have also been positive results in treating tinnitus using sulodexide as a monotherapy.
Sulodexide has also been effectively used in the treatment of
chronic venous disease
Chronic venous insufficiency (CVI) is a medical condition characterized by blood pooling in the veins, leading to increased pressure and strain on the vein walls. The most common cause of CVI is superficial venous reflux, which often results in ...
.
References
External links
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Glycosaminoglycans
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