Sulodexide Explained

Verifiedrevid:447908524
Iupac Name:Glucurono-2-amino-2-deoxyglucoglucan sulfate
Routes Of Administration:Oral, Subcutaneous, Intravenous, Intramuscular
Cas Number:57821-29-1
Unii:75HGV0062C
Atc Prefix:B01
Atc Suffix:AB11
Drugbank:DB06271
Kegg:D08547

Sulodexide, traded as Aterina, is a highly purified mixture of glycosaminoglycans composed of heparan sulfate (80%) and dermatan sulfate (20%).

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]

Notes and References

  1. Lauver DA, Lucchesi BR . Sulodexide: a renewed interest in this glycosaminoglycan . Cardiovascular Drug Reviews . 24 . 3–4 . 214–226 . 2006 . 17214598 . 10.1111/j.1527-3466.2006.00214.x . free . 2027.42/73024 . free .
  2. Harenberg J . Review of pharmacodynamics, pharmacokinetics, and therapeutic properties of sulodexide . Medicinal Research Reviews . 18 . 1 . 1–20 . January 1998 . 9436179 . 10.1002/(SICI)1098-1128(199801)18:1<1::AID-MED1>3.0.CO;2-4 . 26366651 .
  3. Lauver DA, Booth EA, White AJ, Poradosu E, Lucchesi BR . 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 . February 2005 . 15365091 . 10.1124/jpet.104.075283 . 9865911 .
  4. Achour A, Kacem M, Dibej K, Skhiri H, Bouraoui S, El May M . One year course of oral sulodexide in the management of diabetic nephropathy . Journal of Nephrology . 18 . 5 . 568–574 . 2005 . 16299683 .
  5. Gambaro G, Venturini AP, Noonan DM, Fries W, Re G, Garbisa S, Milanesi C, Pesarini A, Borsatti A, Marchi E . 6 . Treatment with a glycosaminoglycan formulation ameliorates experimental diabetic nephropathy . Kidney International . 46 . 3 . 797–806 . September 1994 . 7527876 . 10.1038/ki.1994.335 . free .
  6. Skrha J, Perusicová J, Pont'uch P, Oksa A . Glycosaminoglycan sulodexide decreases albuminuria in diabetic patients . Diabetes Research and Clinical Practice . 38 . 1 . 25–31 . October 1997 . 9347243 . 10.1016/S0168-8227(97)00076-4 .
  7. Neri G, Baffa C, De Stefano A, Poliandri A, Kulamarva G, Di Giovanni P, Petrucci AG, Castriotta A, Citraro L, Cerrone D, D' Orazio F, Croce A . 6 . Management of tinnitus: oral treatment with melatonin and sulodexide . Journal of Biological Regulators and Homeostatic Agents . 23 . 2 . 103–110 . 2009 . 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 . Sulodexide Monotherapy in Chronic Idiopathic Subjective Tinnitus: A Randomized Controlled Trial . Otolaryngology–Head and Neck Surgery . 158 . 6 . 1107–1112 . June 2018 . 29712507 . 10.1177/0194599818767618 . SAGE Publications . 14058842 .
  10. Andreozzi GM . Sulodexide in the treatment of chronic venous disease . American Journal of Cardiovascular Drugs . 12 . 2 . 73–81 . April 2012 . 22329592 . 10.2165/11599360-000000000-00000 . 23046029 .

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