Sulodexide

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

Sulodexide
Clinical data
AHFS/Drugs.comInternational Drug Names
Routes of
administration		Oral, Subcutaneous, Intravenous, Intramuscular
ATC code
Identifiers
  • Glucurono-2-amino-2-deoxyglucoglucan sulfate
CAS Number
DrugBank
UNII
KEGG
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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]

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. 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.


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