Fibrates – role and mechanisms of hypolipemic action Review article
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Published:
Dec 31, 2015
Keywords:
hypertriglyceridaemia, fibrate, PPAR, dyslipidaemia
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Abstract
Dyslipidaemias are common cardiovascular risk factor in Poland. Besides statins, fibrates are basic therapeutic agents in management of lipid disorders. Treatment with fibrates, as basal or additional drug, is indicated particularly in dyslipidaemias with elevated serum triglycerides. The mechanism of action is still unknown, but the role of nuclear receptors PPAR is suggested. In the article indications for treatment with fibrates, principles of the drug administration, mechanism of action in connection with physiological function of PPAR family are presented.
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Sobieraj , P., Lewandowski , J., Dęmbe , K., & Krasnodębski , P. (2015). Fibrates – role and mechanisms of hypolipemic action. Medycyna Faktow (J EBM), 8(4(29), 24-30. Retrieved from https://journalsmededu.pl/index.php/jebm/article/view/2279
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References
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3. Hypertriglyceridaemia and vascular risk. Report of a meeting of physicians and scientists, University College London Medical School. Lancet 1993; 342: 781-787.
4. Brunzell J.D.: Clinical practice. Hypertriglyceridemia. N. Engl. J. Med. 2007; 357: 1009-1017.
5. DeFronzo R.A., Ferrannini E.: Insulin resistance. A multifaceted syndrome responsible for NIDDM, obesity, hypertension, dyslipidemia, and atherosclerotic cardiovascular disease. Diabetes Care 1991; 14: 173-194.
6. Simpson H.C., Mann J.I., Meade T.W. et al.: Hypertriglyceridaemia and hypercoagulability. Lancet 1983; 1: 786-790.
7. Sarwar N., Danesh J., Eiriksdottir G. et al.: Triglycerides and the risk of coronary heart disease: 10,158 incident cases among 262,525 participants in 29 Western prospective studies. Circulation 2007; 115: 450-458.
8. Sprecher D.L., Pearce G.L., Cosgrove D.M. et al.: Relation of serum triglyceride levels to survival after coronary artery bypass grafting. Am. J. Cardiol. 2000; 86: 285-288.
9. Staels B., Dallongeville J., Auwerx J. et al.: Mechanism of action of fibrates on lipid and lipoprotein metabolism. Circulation 1998; 98: 2088-2093.
10. Jin F.Y., Kamanna V.S., Chuang M.Y. et al.: Gemfibrozil stimulates apolipoprotein A-I synthesis and secretion by stabilization of mRNA transcripts in human hepatoblastoma cell line (Hep G2). Arterioscler. Thromb. Vasc. Biol. 1996; 16: 1052-1062.
11. Vu-Dac N., Schoonjans K., Kosykh V. et al.: Fibrates increase human apolipoprotein A-II expression through activation of the peroxisome proliferator- activated receptor. J. Clin. Invest. 1995; 96: 741-750.
12. Rosenson R.S., Wolff D.A., Huskin A.L. et al.: Fenofibrate therapy ameliorates fasting and postprandial lipoproteinemia, oxidative stress, and the inflammatory response in subjects with hypertriglyceridemia and the metabolic syndrome. Diabetes Care 2007; 30: 1945-1951.
13. Frick M.H., Elo O., Haapa K. et al.: Helsinki Heart Study: primary-prevention trial with gemfibrozil in middle-aged men with dyslipidemia. N. Engl. J. Med. 1987; 317: 1237-1245.
14. Rubins H.B., Robins S.J., Collins D. et al.: Gemfibrozil for the secondary prevention of coronary heart disease in men with low levels of high-density lipoprotein cholesterol. Veterans Affairs High-Density Lipoprotein Cholesterol Intervention Trial Study Group. N. Engl. J. Med. 1999; 341: 410-418.
15. Keech A., Simes R.J., Barter P. et al.; The FIELD Study Investigators: Effects of long-term fenofibrate therapy on cardiovascular events in 9795 people with type 2 diabetes mellitus (the FIELD study): randomised controlled trial. Lancet 2005; 366: 1849-1861.
16. The ACCORD Study Group: Effects of combination lipid therapy in type 2 diabetes mellitus. N. Engl. J. Med. 2010; 362: 1563-1574.
17. Wanders R.J.: Metabolic functions of peroxisomes in health and disease. Biochimie 2014; 98: 36-44.
18. Varga T., Czimmerer Z., Nagy L.: PPARs are a unique set of fatty acid regulated transcription factors controlling both lipid metabolism and inflammation. Biochimica et Biophysica Acta 2011; 1812: 1007-1022.
19. Hamblin M., Chang L., Fan Y. et al.: PPARs and the cardiovascular system. Antioxid. Redox Signal. 2009; 11(6): 1415-1452.
20. Stolarczyk M., Gutman W., Derlacz R.A.: Receptory jądrowe PPAR jako miejsce działania leków w zaburzeniach metabolicznych. Postępy Biochemii 2011; 57(2): 207-214.
21. A co-operative trial in the primary prevention of ischaemic heart disease using clofibrat. Report from the Commitee of Principal Investigators: Br. Heart J. 1987; 40: 1069-1118.
22. Shephard J.: The fibrates in clinical practice: focus on micronized fenofibrate. Atherosclerosis 1994; 110: S55-63.
2. Reiner Z., Catapano A.L., Backer G.D. et al.: ESC/EAS Guidelines for the management of dyslipidaemias. Eur. Heart J. 2011; 32: 1769-1818.
3. Hypertriglyceridaemia and vascular risk. Report of a meeting of physicians and scientists, University College London Medical School. Lancet 1993; 342: 781-787.
4. Brunzell J.D.: Clinical practice. Hypertriglyceridemia. N. Engl. J. Med. 2007; 357: 1009-1017.
5. DeFronzo R.A., Ferrannini E.: Insulin resistance. A multifaceted syndrome responsible for NIDDM, obesity, hypertension, dyslipidemia, and atherosclerotic cardiovascular disease. Diabetes Care 1991; 14: 173-194.
6. Simpson H.C., Mann J.I., Meade T.W. et al.: Hypertriglyceridaemia and hypercoagulability. Lancet 1983; 1: 786-790.
7. Sarwar N., Danesh J., Eiriksdottir G. et al.: Triglycerides and the risk of coronary heart disease: 10,158 incident cases among 262,525 participants in 29 Western prospective studies. Circulation 2007; 115: 450-458.
8. Sprecher D.L., Pearce G.L., Cosgrove D.M. et al.: Relation of serum triglyceride levels to survival after coronary artery bypass grafting. Am. J. Cardiol. 2000; 86: 285-288.
9. Staels B., Dallongeville J., Auwerx J. et al.: Mechanism of action of fibrates on lipid and lipoprotein metabolism. Circulation 1998; 98: 2088-2093.
10. Jin F.Y., Kamanna V.S., Chuang M.Y. et al.: Gemfibrozil stimulates apolipoprotein A-I synthesis and secretion by stabilization of mRNA transcripts in human hepatoblastoma cell line (Hep G2). Arterioscler. Thromb. Vasc. Biol. 1996; 16: 1052-1062.
11. Vu-Dac N., Schoonjans K., Kosykh V. et al.: Fibrates increase human apolipoprotein A-II expression through activation of the peroxisome proliferator- activated receptor. J. Clin. Invest. 1995; 96: 741-750.
12. Rosenson R.S., Wolff D.A., Huskin A.L. et al.: Fenofibrate therapy ameliorates fasting and postprandial lipoproteinemia, oxidative stress, and the inflammatory response in subjects with hypertriglyceridemia and the metabolic syndrome. Diabetes Care 2007; 30: 1945-1951.
13. Frick M.H., Elo O., Haapa K. et al.: Helsinki Heart Study: primary-prevention trial with gemfibrozil in middle-aged men with dyslipidemia. N. Engl. J. Med. 1987; 317: 1237-1245.
14. Rubins H.B., Robins S.J., Collins D. et al.: Gemfibrozil for the secondary prevention of coronary heart disease in men with low levels of high-density lipoprotein cholesterol. Veterans Affairs High-Density Lipoprotein Cholesterol Intervention Trial Study Group. N. Engl. J. Med. 1999; 341: 410-418.
15. Keech A., Simes R.J., Barter P. et al.; The FIELD Study Investigators: Effects of long-term fenofibrate therapy on cardiovascular events in 9795 people with type 2 diabetes mellitus (the FIELD study): randomised controlled trial. Lancet 2005; 366: 1849-1861.
16. The ACCORD Study Group: Effects of combination lipid therapy in type 2 diabetes mellitus. N. Engl. J. Med. 2010; 362: 1563-1574.
17. Wanders R.J.: Metabolic functions of peroxisomes in health and disease. Biochimie 2014; 98: 36-44.
18. Varga T., Czimmerer Z., Nagy L.: PPARs are a unique set of fatty acid regulated transcription factors controlling both lipid metabolism and inflammation. Biochimica et Biophysica Acta 2011; 1812: 1007-1022.
19. Hamblin M., Chang L., Fan Y. et al.: PPARs and the cardiovascular system. Antioxid. Redox Signal. 2009; 11(6): 1415-1452.
20. Stolarczyk M., Gutman W., Derlacz R.A.: Receptory jądrowe PPAR jako miejsce działania leków w zaburzeniach metabolicznych. Postępy Biochemii 2011; 57(2): 207-214.
21. A co-operative trial in the primary prevention of ischaemic heart disease using clofibrat. Report from the Commitee of Principal Investigators: Br. Heart J. 1987; 40: 1069-1118.
22. Shephard J.: The fibrates in clinical practice: focus on micronized fenofibrate. Atherosclerosis 1994; 110: S55-63.