Sulodexide

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Sulodexide
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AHFS/Drugs.com International Drug Names
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administration
Oral, Subcutaneous, Intravenous, Intramuscular
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Identifiers
  • Glucurono-2-amino-2-deoxyglucoglucan sulfate
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Sulodexide, traded as Aterina, is a highly purified mixture of glycosaminoglycans composed of heparan sulfate (80%) and dermatan sulfate (20%).

Contents

Pharmacology

The low molecular weight of both sulodexide fractions allows for extensive oral absorption compared to unfractionated heparin. 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. [1] Due to the presence of both glycosaminoglycan fractions, sulodexide potentiates the antiprotease activities of both antithrombin III and heparin cofactor II simultaneously. [2]

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 [3] and the treatment of diabetic nephropathy. [4] [5] [6] In combination with melatonin, sulodexide has been shown to be a viable treatment option for patients suffering from central or sensorineural tinnitus. [7] [8] There have also been positive results in treating tinnitus using sulodexide as a monotherapy. [9] Sulodexide has also been effectively used in the treatment of chronic venous disease. [10]

Related Research Articles

<span class="mw-page-title-main">Anticoagulant</span> Class of drugs

Anticoagulants, commonly known as blood thinners, are chemical substances that prevent or reduce coagulation of blood, prolonging the clotting time. Some of them occur naturally in blood-eating animals such as leeches and mosquitoes, where they help keep the bite area unclotted long enough for the animal to obtain some blood. As a class of medications, anticoagulants are used in therapy for thrombotic disorders. Oral anticoagulants (OACs) are taken by many people in pill or tablet form, and various intravenous anticoagulant dosage forms are used in hospitals. Some anticoagulants are used in medical equipment, such as sample tubes, blood transfusion bags, heart–lung machines, and dialysis equipment. One of the first anticoagulants, warfarin, was initially approved as a rodenticide.

<span class="mw-page-title-main">Thrombosis</span> Medical condition caused by blood clots

Thrombosis is the formation of a blood clot inside a blood vessel, obstructing the flow of blood through the circulatory system. When a blood vessel is injured, the body uses platelets (thrombocytes) and fibrin to form a blood clot to prevent blood loss. Even when a blood vessel is not injured, blood clots may form in the body under certain conditions. A clot, or a piece of the clot, that breaks free and begins to travel around the body is known as an embolus.

<span class="mw-page-title-main">Venous thrombosis</span> Blood clot (thrombus) that forms within a vein

Venous thrombosis is the blockage of a vein caused by a thrombus. A common form of venous thrombosis is deep vein thrombosis (DVT), when a blood clot forms in the deep veins. If a thrombus breaks off (embolizes) and flows to the lungs to lodge there, it becomes a pulmonary embolism (PE), a blood clot in the lungs. The conditions of DVT only, DVT with PE, and PE only, are all captured by the term venous thromboembolism (VTE).

<span class="mw-page-title-main">Heparin</span> Anticoagulant

Heparin, also known as unfractionated heparin (UFH), is a medication and naturally occurring glycosaminoglycan. Since heparins depend on the activity of antithrombin, they are considered anticoagulants. Specifically it is also used in the treatment of heart attacks and unstable angina. It is given intravenously or by injection under the skin. Other uses for its anticoagulant properties include inside blood specimen test tubes and kidney dialysis machines.

<span class="mw-page-title-main">Microangiopathy</span> Medical condition

Microangiopathy is a disease of the microvessels, small blood vessels in the microcirculation. It can be contrasted to macroangiopathies such as atherosclerosis, where large and medium-sized arteries are primarily affected.

<span class="mw-page-title-main">Chondroitin sulfate</span> Sulfated glycosaminoglycan (GAG) compound

Chondroitin sulfate is a sulfated glycosaminoglycan (GAG) composed of a chain of alternating sugars. It is usually found attached to proteins as part of a proteoglycan. A chondroitin chain can have over 100 individual sugars, each of which can be sulfated in variable positions and quantities. Chondroitin sulfate is an important structural component of cartilage, and provides much of its resistance to compression. Along with glucosamine, chondroitin sulfate has become a widely used dietary supplement for treatment of osteoarthritis, although large clinical trials failed to demonstrate any symptomatic benefit of chondroitin.

Low-molecular-weight heparin (LMWH) is a class of anticoagulant medications. They are used in the prevention of blood clots and treatment of venous thromboembolism and in the treatment of myocardial infarction.

<span class="mw-page-title-main">Chronic kidney disease</span> Medical condition

Chronic kidney disease (CKD) is a type of kidney disease in which a gradual loss of kidney function occurs over a period of months to years. Initially generally no symptoms are seen, but later symptoms may include leg swelling, feeling tired, vomiting, loss of appetite, and confusion. Complications can relate to hormonal dysfunction of the kidneys and include high blood pressure, bone disease, and anemia. Additionally CKD patients have markedly increased cardiovascular complications with increased risks of death and hospitalization.

<span class="mw-page-title-main">Diabetic nephropathy</span> Chronic loss of kidney function

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 causes of chronic kidney disease (CKD) and end-stage renal disease (ESRD) globally. The triad of protein leaking into the urine, rising blood pressure with hypertension and then falling renal function is common to many forms of CKD. Protein loss in the urine due to damage of the glomeruli may become massive, and cause a low serum albumin with resulting generalized body swelling (edema) so called nephrotic syndrome. Likewise, the estimated glomerular filtration rate (eGFR) may progressively fall from a normal of over 90 ml/min/1.73m2 to less than 15, at which point the patient is said to have end-stage renal disease. It usually is slowly progressive over years.

Microalbuminuria is a term to describe a moderate increase in the level of urine albumin. It occurs when the kidney leaks small amounts of albumin into the urine, in other words, when an abnormally high permeability for albumin in the glomerulus of the kidney occurs. Normally, the kidneys filter albumin, so if albumin is found in the urine, then it is a marker of kidney disease. The term microalbuminuria is now discouraged by Kidney Disease Improving Global Outcomes and has been replaced by moderately increased albuminuria.

<span class="mw-page-title-main">Fondaparinux</span> Chemical compound

Fondaparinux is an anticoagulant medication chemically related to low molecular weight heparins. It is marketed by Viatris. A generic version developed by Alchemia is marketed within the US by Dr. Reddy's Laboratories.

<span class="mw-page-title-main">Dermatan sulfate</span> Glycosaminoglycan found in animals

Dermatan sulfate is a glycosaminoglycan found mostly in skin, but also in blood vessels, heart valves, tendons, and lungs.

<span class="mw-page-title-main">Heparan sulfate</span> Macromolecule

Heparan sulfate (HS) is a linear polysaccharide found in all animal tissues. It occurs as a proteoglycan in which two or three HS chains are attached in close proximity to cell surface or extracellular matrix proteins. In this form, HS binds to a variety of protein ligands, including Wnt, and regulates a wide range of biological activities, including developmental processes, angiogenesis, blood coagulation, abolishing detachment activity by GrB, and tumour metastasis. HS has also been shown to serve as cellular receptor for a number of viruses, including the respiratory syncytial virus. One study suggests that cellular heparan sulfate has a role in SARS-CoV-2 Infection, particularly when the virus attaches with ACE2.

Heparinoids are glycosaminoglycans which are chemically and pharmacologically related to heparin. They include oligosaccharides and sulfated polysaccharides of plant, animal, or synthetic origin. Multiple scientific studies have been conducted on heparinoids.

Hypercoagulability in pregnancy is the propensity of pregnant women to develop thrombosis. Pregnancy itself is a factor of hypercoagulability, as a physiologically adaptive mechanism to prevent post partum bleeding. However, when combined with an additional underlying hypercoagulable states, the risk of thrombosis or embolism may become substantial.

<span class="mw-page-title-main">Dapagliflozin</span> Diabetes medication

Dapagliflozin, sold under the brand names Farxiga (US) and Forxiga (EU) among others, is a medication used to treat type 2 diabetes. It is also used to treat adults with heart failure and chronic kidney disease.

<span class="mw-page-title-main">Calcium dobesilate</span> Chemical compound

Calcium dobesilate is a vasoprotective. It is the calcium salt of dobesilic acid. It is a synthetic molecule with the ability to reduce capillary permeability in the body. In Switzerland the drug is sold by the pharmaceutical company OM Pharma under the trade name of Doxium in capsules containing 500 mg of active ingredient.

Complications of diabetes are secondary diseases that are a result of elevated blood glucose levels that occur in diabetic patients. These complications can be divided into two types: acute and chronic. Acute complications are complications that develop rapidly and can be exemplified as diabetic ketoacidosis (DKA), hyperglycemic hyperosmolar state (HHS), lactic acidosis (LA), and hypoglycemia. Chronic complications develop over time and are generally classified in two categories: microvascular and macrovascular. Microvascular complications include neuropathy, nephropathy, and retinopathy; while cardiovascular disease, stroke, and peripheral vascular disease are included in the macrovascular complications.

Type 3c diabetes is diabetes that comes secondary to pancreatic diseases, involving the exocrine and digestive functions of the pancreas. It also occurs following surgical removal of the pancreas.

<span class="mw-page-title-main">Melatonin as a medication and supplement</span> Supplement and medication used to treat sleep disorders

Melatonin is a dietary supplement and medication as well as naturally occurring hormone. As a hormone, melatonin is released by the pineal gland and is involved in sleep–wake cycles. As a supplement, it is often used for the attempted short-term treatment of disrupted sleep patterns, such as from jet lag or shift work, and is typically taken orally. Evidence of its benefit for this use, however, is not strong. A 2017 review found that sleep onset occurred six minutes faster with use, but found no change in total time asleep.

References

  1. Lauver DA, Lucchesi BR (2006). "Sulodexide: a renewed interest in this glycosaminoglycan". Cardiovascular Drug Reviews. 24 (3–4): 214–226. doi: 10.1111/j.1527-3466.2006.00214.x . hdl: 2027.42/73024 . PMID   17214598.
  2. Harenberg J (January 1998). "Review of pharmacodynamics, pharmacokinetics, and therapeutic properties of sulodexide". Medicinal Research Reviews. 18 (1): 1–20. doi:10.1002/(SICI)1098-1128(199801)18:1<1::AID-MED1>3.0.CO;2-4. PMID   9436179. S2CID   26366651.
  3. Lauver DA, Booth EA, White AJ, Poradosu E, Lucchesi BR (February 2005). "Sulodexide attenuates myocardial ischemia/reperfusion injury and the deposition of C-reactive protein in areas of infarction without affecting hemostasis". The Journal of Pharmacology and Experimental Therapeutics. 312 (2): 794–800. doi:10.1124/jpet.104.075283. PMID   15365091. S2CID   9865911.
  4. Achour A, Kacem M, Dibej K, Skhiri H, Bouraoui S, El May M (2005). "One year course of oral sulodexide in the management of diabetic nephropathy". Journal of Nephrology. 18 (5): 568–574. PMID   16299683.
  5. Gambaro G, Venturini AP, Noonan DM, Fries W, Re G, Garbisa S, et al. (September 1994). "Treatment with a glycosaminoglycan formulation ameliorates experimental diabetic nephropathy". Kidney International. 46 (3): 797–806. doi: 10.1038/ki.1994.335 . PMID   7527876.
  6. Skrha J, Perusicová J, Pont'uch P, Oksa A (October 1997). "Glycosaminoglycan sulodexide decreases albuminuria in diabetic patients". Diabetes Research and Clinical Practice. 38 (1): 25–31. doi:10.1016/S0168-8227(97)00076-4. PMID   9347243.
  7. Neri G, Baffa C, De Stefano A, Poliandri A, Kulamarva G, Di Giovanni P, et al. (2009). "Management of tinnitus: oral treatment with melatonin and sulodexide". Journal of Biological Regulators and Homeostatic Agents. 23 (2): 103–110. PMID   19589291.
  8. Neri G. De Stefano A. Baffa C. Kulamarva G. Di Giovanni P. Petrucci G. Poliandri A. Dispenza F. Citraro L. Croce A. ,"Treatment of central and sensorineural tinnitus with orally administered Melatonin and Sulodexide: personal experience from a randomized controlled study." Acta Otorhinolaryngologica Italica. 29(2):86-91, 2009 Apr.
  9. El Beaino M, McCaskey MK, Eter E (June 2018). "Sulodexide Monotherapy in Chronic Idiopathic Subjective Tinnitus: A Randomized Controlled Trial". Otolaryngology–Head and Neck Surgery. SAGE Publications. 158 (6): 1107–1112. doi:10.1177/0194599818767618. PMID   29712507. S2CID   14058842.
  10. Andreozzi GM (April 2012). "Sulodexide in the treatment of chronic venous disease". American Journal of Cardiovascular Drugs. 12 (2): 73–81. doi:10.2165/11599360-000000000-00000. PMID   22329592. S2CID   23046029.