AN OVERVIEW OF STATINS AS HYPOLIPIDEMIC DRUGS
Abstract
There is a wealth of evidence suggesting association between Dyslipidemia and Heart Failure. Statins are the treatment of choice for the management of Dyslipidemia because of their proven efficacy and safety profile. They also have an increasing role in managing cardiovascular risk in patients with relatively normal levels of plasma cholesterol. The article reviews the role of Statins in the treatment of Dyslipidemia. Although all statins act by act by blocking the HMG-CoA reductase enzyme, which catalyzes the rate-limiting, step in de novo cholesterol synthesis, they differ in terms of their chemical structures, pharmacokinetic profiles, and lipid-modifying efficacy. Lovastatin, Pravastatin and Simvastatin are derived from fungal metabolites and have elimination half-lives of 1–3 h. Atorvastatin, Cerivastatin (withdrawn from clinical use in 2001), Fluvastatin, Pitavastatin and Rosuvastatin are fully synthetic compounds, with elimination half-lives ranging from 1 h for Fluvastatin to 19 h for Rosuvastatin. As a class, statins are generally well tolerated and serious adverse events, including muscle toxicity leading to rhabdomyolysis, are rare. Consideration of the differences between the statins helps to provide a rational basis for their use in clinical practice.
Keywords:
Dyslipidemia, Statins, HMG-CoA reductase enzyme, adverse events.DOI
https://doi.org/10.25004/IJPSDR.2011.030303References
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2. Enas EA, Chacko V, Pazhoor SG, Chennikkara H, Devarapalli P. Dyslipidemia in South Asian Patients. Current Atherosclerosis Reports 2007; 9:367-74.
3. Indrayan A. Forecasting vascular disease cases and associated mortality in India. Reports of the National Commission on Macroeconomics and Health. Ministry of Health and Family Welfare, India 2005. Available at: http://www.whoindia.org/EN/Section102/Section201_888.htm.
4. Executive Summary of the Third Report of the National Cholesterol Education Program (NCEP) Expert Panel on Detection, Evaluation, and treatment of High Blood Cholesterol in Adults (Adult Treatment Panel III) [special communication]. JAMA 2001; 285:2486-2947.
5. Reddy KS, Prabhakaran D, Chaturvedi V, Jeemon P, Thankappan KR, Ramakrishnan L, Mohan BVM, et al. Methods for establishing a surveillance system for cardiovascular disease in Indian industrial populations. Bulletin of the World Health Organization 2006; 84:461-69.
6. Iughetti L, Volta C, Maggi E. Circulating antibodies recognizing oxidatively modified low-density lipoprotein in children. Pediatr. Res. 1999; 45: 94-99.
7. Rodenburg J, Visser MN, Wiegman A. Oxidized low-density lipoprotein in children with familial hypercholesterolemia and unaffected siblings: effect of Pravastatin. J. Am. Coll. Cardiol. 2006; 47: 1803-1810.
8. Srinivasan SR, Frontini MG, Xu J, Berenson GS. Utility of childhood non-high-density lipoprotein cholesterol levels in predicting adult dyslipidemia and other cardiovascular risks: the Bogalusa Heart Study. Pediatrics: 2006; 118(1): 201-202.
9. ALLHAT Officers and Coordinators for the ALLHAT Collaborative Research Group. Major outcomes in moderately hypercholesterolemic, hypertensive patients randomized to Pravastatin vs usual care: the Antihypertensive and Lipid- Lowering Treatment to Prevent Heart Attack Trial (ALLHATLLT). J Am Med Assoc 2002; 288:2998-3007.
10. Sever PS, Dahlof B, Poulter NR. Prevention of coronary and stroke events with Atorvastatin in hypertensive patients who have average or lower-than-average cholesterol concentrations, in the Anglo-Scandinavian Cardiac Outcomes Trial - Lipid Lowering Arm (ASCOT - LLA): a multicentre randomised controlled trial. Lancet 2003; 361:1149-58.
11. Wierzbicki AS. New lipid-lowering agents. Expert Opin. Emerg. Drugs 2003; 8: 365-376.
12. Arambepola C, Farmer AJ, Perera R, Neil HAW. Statin treatment for children and adolescents with heterozygous familial hypercholesterolaemia: a systematic review and meta-analysis. Atherosclerosis 2007; 195: 339-347.
13. Gaw A., Packard CJ. Comparative chemistry, pharmacology and mechanism of action of the statins, in: GawA., Packard CJ., Shepherd J. (Eds), Statins. The HMG CoA reductase inhibitors in perspective, Martin Dunitz, London, 2000, pp. 49-61.
14. McTavish D, Sorkin EM. Pravastatin A review of its pharmacological properties and therapeutic potential in hypercholesterolaemia. Drugs 1991; 42: 65-89.
15. McTaggart F, Buckett L, Davidson R. Preclinical and clinical pharmacology of Rosuvastatin, a new 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor. Am. J. Cardiol. 2001; 87(Suppl. B): 28-32.
16. Istvan ES, Deisenhofer J. Structural mechanism for statin inhibition of HMG-CoA reductase. Science 2001; 292: 1160-1164.
17. Corsini A, Maggi FM, Catapano AL. Pharmacology of competitive inhibitors of HMG-CoA reductase. Pharmacol. Res. 1995; 31: 9-27.
18. Corsini A, Bellosta S, Baetta R, Fumagalli R, Paoletti R, Bernini F. New insights into the pharmacodynamic and pharmacokinetic properties of statins. Pharmacol. Ther. 1999; 84: 413-428.
19. Kajinami K, Mabuchi H, Saito Y. NK-104: a novel synthetic HMG-CoA reductase inhibitor. Expert Opin. Investig. Drugs 2000; 9: 2653-2661.
20. Cilla DD Jr, Gibson DM, Whitfield LR, Sedman AJ. Pharmacodynamic effects and pharmacokinetics of Atorvastatin after administration to normocholesterolemic subjects in the morning and evening. J. Clin. Pharmacol. 1996; 36: 604–609.
21. Tse FL, Jaffe JM, Troendle A. Pharmacokinetics of Fluvastatin after single and multiple doses in normal volunteers. J. Clin. Pharmacol. 1992; 32: 630-638.
22. Pan HY, DeVault AR, Wang-Iverson D, Ivashkiv E, Swanson BN, Sugerman AA. Comparative pharmacokinetics and pharmacodynamics of Pravastatin and Lovastatin. J. Clin. Pharmacol. 1990; 30: 1128-1135.
23. Warwick MJ, Dane AL, Raza A, Schneck DW. Single and multiple-dose pharmacokinetics and safety of the new HMG-CoA reductase inhibitor ZD4522. Atherosclerosis 2000; 151: 39.
24. Martin PD, Mitchell PD, Schneck DW. Pharmacodynamic effects and pharmacokinetics of a new HMG-CoA reductase inhibitor, Rosuvastatin, after morning or evening administration in healthy volunteers. Br. J. Clin. Pharmacol. 2002; 54: 472-477.
25. Garnett WR. Interactions with hydroxymethylglutaryl-coenzyme A reductase inhibitors. Am. J. Health Syst. Pharm. 1995; 52: 1639-1645.
26. Radulovic LL, Cilla DD, Posvar EL, Sedman AJ, Whitfield LR. Effect of food on the bioavailability of Atorvastatin, an HMG-CoA reductase inhibitor. J. Clin. Pharmacol. 1995; 35: 990-994.
27. Smith HT, Jokubaitis LA, Troendle AJ, Hwang DS, Robinson WT. Pharmacokinetics of Fluvastatin and specific drug interactions. Am. J. Hypertens. 1993; 6: 375S-382S.
28. Pan HY, DeVault AR, Brescia D. Effect of food on Pravastatin pharmacokinetics and pharmacodynamics. Int. J. Clin. Pharmacol. Ther. Toxicol. 1993; 31: 291-294.
29. Davidson MH. Rosuvastatin: a highly efficacious statin for the treatment of dyslipidaemia. Expert Opin. Invest. Drugs 2002; 11: 125-141.
30. Bottorff M, Hansten P. Long-term safety of hepatic hydroxymethyl glutaryl coenzyme A reductase inhibitors: the role of metabolism – monograph for physicians. Arch. Intern. Med. 2000; 160: 2273-2280.
31. Michalets EL. Update: clinically significant cytochrome P-450 drug interactions. Pharmacotherapy 1998; 18: 84-112.
32. Jacobsen W, Kuhn B, Soldner A. Lactonization is the critical first step in the disposition of the 3-hydroxy-3-methylglutaryl-CoA reductase inhibitor atorvastatin. Drug Metab. Dispos. 2000; 28: 1369-1378.
33. Vickers S, Duncan CA, Vyas KP. In vitro and in vivo biotransformation of Simvastatin, an inhibitor of HMG CoA reductase. Drug Metab. Dispos. 1990; 18: 476-483.
34. Lennernäs H, Fager G. Pharmacodynamics and pharmacokinetics of the HMG-CoA reductase inhibitors. Clin. Pharmacokinet. 1997; 32: 403-425.
35. Fujino H, Yamada I, Kojima J, Hirano M, Matsumoto H, Yoneda M. Studies on the metabolic fate of NK-104, a new inhibitor of HMG-CoA reductase (5): in vitro metabolism and plasma protein binding in animals and human. Xeno. Metab. Disp. 1999; 14: 415-424.
36. McCormick AD, McKillop D, Butters CJ. ZD4522-an HMG-CoA reductase inhibitor free of metabolically mediated drug interactions: metabolic studies in human in vitro systems. J. Clin. Pharmacol. 2000; 40: 1055.
37. Schachter M. Statins, drug interactions and cytochrome P450. Br. J. Cardiol. 2001; 8: 311-317.
38. Sica DA, Gehr TW. Rhabdomyolysis and statin therapy: relevance to the elderly. Am. J. Geriatr. Cardiol. 2002; 11: 48-55.
39. Muscari A, Puddu GM, Puddu P. Lipid-lowering drugs: are adverse effects predictable and reversible? Cardiology 2002; 97: 115-121.
40. Knopp RH. Drug treatment of lipid disorders. N. Engl. J. Med. 1999; 341: 498-511.
41. Maron DJ, Fazio S, Linton MF. Current perspectives on statins. Circulation 2000; 101: 207-213.
42. Singhvi SM, Pan HY, Morrison RA, Willard DA. Disposition of Pravastatin sodium, a tissue-selective HMG-CoA reductase inhibitor, in healthy subjects. Br. J. Clin. Pharmacol. 1990; 29: 239-243.
43. Quion JAV, Jones PH. Clinical pharmacokinetics of Pravastatin. Clin. Pharmacokinet. 1994; 27: 94-103.
44. Martin PD, Warwick MJ, Dane AL, Brindley C, Short T. Absolute oral bioavailability of Rosuvastatin in healthy white adult male volunteers. Clin. Ther. 2003; 25: 2553-2563.
45. Martin PD, Warwick MJ, Dane AL. Metabolism, excretion, and pharmacokinetics of Rosuvastatin in healthy adult male volunteers. Clin. Ther. 2003; 25: 2822-2835.
46. Simonson SG, Martin PD, Mitchell P, Schneck DW, Lasseter KC, Warwick MJ. Pharmacokinetics and pharmacodynamics of Rosuvastatin in subjects with hepatic impairment. Eur. J. Clin. Pharmacol. 2003; 58: 669-675.
47. Olsson AG, Pears J, McKellar J, Mizan J, Raza A. Effect of Rosuvastatin on low-density lipoprotein cholesterol in patients with hypercholesterolemia. Am. J. Cardiol. 2001; 88: 504-508.
48. Jones P, Kafonek S, Laurora I, Hunninghake D. For the CURVES Investigators. Comparative dose efficacy of Atorvastatin versus Simvastatin, Pravastatin, Lovastatin, and Fluvastatin in patients with hypercholesterolaemia. Am. J. Cardiol. 1998; 81: 582-587.
49. Jones PH, Davidson MH, Stein EA. The STELLAR Study Group. Comparison of efficacy and safety of Rosuvastatin versus Atorvastatin, Simvastatin, and Pravastatin across doses (STELLAR Trial). Am. J. Cardiol. 2003; 92: 152-160.
50. Black DM. A general assessment of the safety of HMG CoA reductase inhibitors (statins).
51. Furberg CD, Pitt B. Withdrawal of Cerivastatin from the world market. Curr. Control Trials Cardiovasc. Med. 2001; 2: 205-207.
52. González-Ponte ML, González-Ruiz M, Duvós E. Atorvastatin-induced severe thrombocytopenia. Lancet 1998; 352:1284.
53. Groneberg DA, Barkhuizen A, Jeha T. Simvastatin-induced thrombocytopenia. Am J Hematol 2001; 67: 277.
54. Yamada T, Shinohara K, Katsuki K. Severe thrombocytopenia caused by Simvastatin in which thrombocyte recovery was initiated after severe bacterial infection. Clin Drug Investig 1998; 16:172-174.
55. Possamai G, Bovo P, Santonastaso M. Thrombocytopenic purpura during therapy with Simvastatin. Haematologica 1992; 77: 357-358.
56. Ames PR. Simvastatin-induced thrombocytopaenia: a further case and a brief on its clinical relevance. Ann Hematol 2008; 87: 773-774.
57. Kenney B, Stack G. Drug-induced thrombocytopenia. Arch Pathol Lab Med 2009; 133: 309-314.
58. Wolfe SM. Dangers of rosuvastatin identified before and after FDA approval. Lancet 2004; 363: 2189-2190.
59. Keller DM. Atorvastatin Beats Rosuvastatin in Protecting Kidneys in Diabetic and Nondiabetic Patients. 2010; July 2, [Medscape].
60. Buyukhatipoglu H, Sezen Y, Guntekin U, Kirhan I, Dag OF. Acute renal failure with the combined use of Rosuvastatin and Fenofibrate. Ren Fail. 2010; 32(5): 633-635.
61. Husten L. Postmarketing study finds high rate of adverse events with Rosuvastatin. 2005; May 23: [Medscape].
62. Prajapati S, Shah S, Desai C, Desai M, Dikshit RK. Atorvastatin-induced pancreatitis. Indian journal of Pharmacology 2010; 42(5): 324-325.
63. Singh S, Nautiyal A, Dolan JG. Recurrent Acute Pancreatitis Possibly Induced by Atorvastatin and Rosuvastatin. Is Statin Induced Pancreatitis a Class Effect? JOP. J Pancreas (Online) 2004; 5(6):502-504.
64. McDonald KB, Garber B, Perreault M. Pancreatitis associated with Simvastatin plus Fenofibrate. Ann Pharmacother 2002; 36:275-9.
65. Anagnostopoulos GK, Tsiakos S, Margantinis G, Kostopoulos P, Arvanitidis D. Acute pancreatitis due to pravastatin therapy. J Pancreas (Online) 2003; 4:129-32.
66. Tysk C, Al-Eryani AY, Shawabkeh AA. Acute pancreatitis induced by Fluvastatin therapy. J Clin Gastroenterol 2002; 35:406-8.
67. Miltiadous G, Anthopoulou A, Elisaf M. Acute pancreatitis possibly associated with combined salicylate and Atorvastatin therapy. J Pancreas (Online) 2003; 4:20-1.
68. Shechter M, Beigel R, Matetzky S, Freimark D, Chouraqui P. The intensive statin therapy myth. Isr Med Assoc J. 2005 Nov; 7(11):683-7.
69. Ara R, Rafia R, Ward SE, Wierzbicki AS, Reynolds TM, Rees A, Pandor A. Are Intensive Lipid-lowering Regimens an Optimal Economic Strategy in Patients with ACS? An Acute and Chronic Perspective. Expert Rev Pharmacoeconomics Outcomes Res. 2009; 9(5):423-433.
70. McKenney JM, Jones PH, Adamczyk MA, Cain VA., Bryzinski BS, Blasetto J W. Comparison of the Efficacy of Rosuvastatin versus Atorvastatin, Simvastatin, and Pravastatin in Achieving Lipid Goals: Results from the STELLAR Trial. Curr Med Res Opin. 2003; 19(8).
71. Jones PH, Davidson MH, Stein EA. Comparison of the efficacy and safety of Rosuvastatin versus Atorvastatin, Simvastatin, and Pravastatin across doses (STELLAR Trial). Am J Cardiol 2003; 92:152-60.
72. Shepherd J, Hunninghake DB, Barter P, McKenney JM, Hutchinson HG. Guidelines for lowering lipids to reduce coronary artery disease risk: a comparison of Rosuvastatin with Atorvastatin, Pravastatin, and Simvastatin for achieving lipid-lowering goals. Am J Cardiol 2003; 91(Suppl 1):11C-19C.
2. Enas EA, Chacko V, Pazhoor SG, Chennikkara H, Devarapalli P. Dyslipidemia in South Asian Patients. Current Atherosclerosis Reports 2007; 9:367-74.
3. Indrayan A. Forecasting vascular disease cases and associated mortality in India. Reports of the National Commission on Macroeconomics and Health. Ministry of Health and Family Welfare, India 2005. Available at: http://www.whoindia.org/EN/Section102/Section201_888.htm.
4. Executive Summary of the Third Report of the National Cholesterol Education Program (NCEP) Expert Panel on Detection, Evaluation, and treatment of High Blood Cholesterol in Adults (Adult Treatment Panel III) [special communication]. JAMA 2001; 285:2486-2947.
5. Reddy KS, Prabhakaran D, Chaturvedi V, Jeemon P, Thankappan KR, Ramakrishnan L, Mohan BVM, et al. Methods for establishing a surveillance system for cardiovascular disease in Indian industrial populations. Bulletin of the World Health Organization 2006; 84:461-69.
6. Iughetti L, Volta C, Maggi E. Circulating antibodies recognizing oxidatively modified low-density lipoprotein in children. Pediatr. Res. 1999; 45: 94-99.
7. Rodenburg J, Visser MN, Wiegman A. Oxidized low-density lipoprotein in children with familial hypercholesterolemia and unaffected siblings: effect of Pravastatin. J. Am. Coll. Cardiol. 2006; 47: 1803-1810.
8. Srinivasan SR, Frontini MG, Xu J, Berenson GS. Utility of childhood non-high-density lipoprotein cholesterol levels in predicting adult dyslipidemia and other cardiovascular risks: the Bogalusa Heart Study. Pediatrics: 2006; 118(1): 201-202.
9. ALLHAT Officers and Coordinators for the ALLHAT Collaborative Research Group. Major outcomes in moderately hypercholesterolemic, hypertensive patients randomized to Pravastatin vs usual care: the Antihypertensive and Lipid- Lowering Treatment to Prevent Heart Attack Trial (ALLHATLLT). J Am Med Assoc 2002; 288:2998-3007.
10. Sever PS, Dahlof B, Poulter NR. Prevention of coronary and stroke events with Atorvastatin in hypertensive patients who have average or lower-than-average cholesterol concentrations, in the Anglo-Scandinavian Cardiac Outcomes Trial - Lipid Lowering Arm (ASCOT - LLA): a multicentre randomised controlled trial. Lancet 2003; 361:1149-58.
11. Wierzbicki AS. New lipid-lowering agents. Expert Opin. Emerg. Drugs 2003; 8: 365-376.
12. Arambepola C, Farmer AJ, Perera R, Neil HAW. Statin treatment for children and adolescents with heterozygous familial hypercholesterolaemia: a systematic review and meta-analysis. Atherosclerosis 2007; 195: 339-347.
13. Gaw A., Packard CJ. Comparative chemistry, pharmacology and mechanism of action of the statins, in: GawA., Packard CJ., Shepherd J. (Eds), Statins. The HMG CoA reductase inhibitors in perspective, Martin Dunitz, London, 2000, pp. 49-61.
14. McTavish D, Sorkin EM. Pravastatin A review of its pharmacological properties and therapeutic potential in hypercholesterolaemia. Drugs 1991; 42: 65-89.
15. McTaggart F, Buckett L, Davidson R. Preclinical and clinical pharmacology of Rosuvastatin, a new 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor. Am. J. Cardiol. 2001; 87(Suppl. B): 28-32.
16. Istvan ES, Deisenhofer J. Structural mechanism for statin inhibition of HMG-CoA reductase. Science 2001; 292: 1160-1164.
17. Corsini A, Maggi FM, Catapano AL. Pharmacology of competitive inhibitors of HMG-CoA reductase. Pharmacol. Res. 1995; 31: 9-27.
18. Corsini A, Bellosta S, Baetta R, Fumagalli R, Paoletti R, Bernini F. New insights into the pharmacodynamic and pharmacokinetic properties of statins. Pharmacol. Ther. 1999; 84: 413-428.
19. Kajinami K, Mabuchi H, Saito Y. NK-104: a novel synthetic HMG-CoA reductase inhibitor. Expert Opin. Investig. Drugs 2000; 9: 2653-2661.
20. Cilla DD Jr, Gibson DM, Whitfield LR, Sedman AJ. Pharmacodynamic effects and pharmacokinetics of Atorvastatin after administration to normocholesterolemic subjects in the morning and evening. J. Clin. Pharmacol. 1996; 36: 604–609.
21. Tse FL, Jaffe JM, Troendle A. Pharmacokinetics of Fluvastatin after single and multiple doses in normal volunteers. J. Clin. Pharmacol. 1992; 32: 630-638.
22. Pan HY, DeVault AR, Wang-Iverson D, Ivashkiv E, Swanson BN, Sugerman AA. Comparative pharmacokinetics and pharmacodynamics of Pravastatin and Lovastatin. J. Clin. Pharmacol. 1990; 30: 1128-1135.
23. Warwick MJ, Dane AL, Raza A, Schneck DW. Single and multiple-dose pharmacokinetics and safety of the new HMG-CoA reductase inhibitor ZD4522. Atherosclerosis 2000; 151: 39.
24. Martin PD, Mitchell PD, Schneck DW. Pharmacodynamic effects and pharmacokinetics of a new HMG-CoA reductase inhibitor, Rosuvastatin, after morning or evening administration in healthy volunteers. Br. J. Clin. Pharmacol. 2002; 54: 472-477.
25. Garnett WR. Interactions with hydroxymethylglutaryl-coenzyme A reductase inhibitors. Am. J. Health Syst. Pharm. 1995; 52: 1639-1645.
26. Radulovic LL, Cilla DD, Posvar EL, Sedman AJ, Whitfield LR. Effect of food on the bioavailability of Atorvastatin, an HMG-CoA reductase inhibitor. J. Clin. Pharmacol. 1995; 35: 990-994.
27. Smith HT, Jokubaitis LA, Troendle AJ, Hwang DS, Robinson WT. Pharmacokinetics of Fluvastatin and specific drug interactions. Am. J. Hypertens. 1993; 6: 375S-382S.
28. Pan HY, DeVault AR, Brescia D. Effect of food on Pravastatin pharmacokinetics and pharmacodynamics. Int. J. Clin. Pharmacol. Ther. Toxicol. 1993; 31: 291-294.
29. Davidson MH. Rosuvastatin: a highly efficacious statin for the treatment of dyslipidaemia. Expert Opin. Invest. Drugs 2002; 11: 125-141.
30. Bottorff M, Hansten P. Long-term safety of hepatic hydroxymethyl glutaryl coenzyme A reductase inhibitors: the role of metabolism – monograph for physicians. Arch. Intern. Med. 2000; 160: 2273-2280.
31. Michalets EL. Update: clinically significant cytochrome P-450 drug interactions. Pharmacotherapy 1998; 18: 84-112.
32. Jacobsen W, Kuhn B, Soldner A. Lactonization is the critical first step in the disposition of the 3-hydroxy-3-methylglutaryl-CoA reductase inhibitor atorvastatin. Drug Metab. Dispos. 2000; 28: 1369-1378.
33. Vickers S, Duncan CA, Vyas KP. In vitro and in vivo biotransformation of Simvastatin, an inhibitor of HMG CoA reductase. Drug Metab. Dispos. 1990; 18: 476-483.
34. Lennernäs H, Fager G. Pharmacodynamics and pharmacokinetics of the HMG-CoA reductase inhibitors. Clin. Pharmacokinet. 1997; 32: 403-425.
35. Fujino H, Yamada I, Kojima J, Hirano M, Matsumoto H, Yoneda M. Studies on the metabolic fate of NK-104, a new inhibitor of HMG-CoA reductase (5): in vitro metabolism and plasma protein binding in animals and human. Xeno. Metab. Disp. 1999; 14: 415-424.
36. McCormick AD, McKillop D, Butters CJ. ZD4522-an HMG-CoA reductase inhibitor free of metabolically mediated drug interactions: metabolic studies in human in vitro systems. J. Clin. Pharmacol. 2000; 40: 1055.
37. Schachter M. Statins, drug interactions and cytochrome P450. Br. J. Cardiol. 2001; 8: 311-317.
38. Sica DA, Gehr TW. Rhabdomyolysis and statin therapy: relevance to the elderly. Am. J. Geriatr. Cardiol. 2002; 11: 48-55.
39. Muscari A, Puddu GM, Puddu P. Lipid-lowering drugs: are adverse effects predictable and reversible? Cardiology 2002; 97: 115-121.
40. Knopp RH. Drug treatment of lipid disorders. N. Engl. J. Med. 1999; 341: 498-511.
41. Maron DJ, Fazio S, Linton MF. Current perspectives on statins. Circulation 2000; 101: 207-213.
42. Singhvi SM, Pan HY, Morrison RA, Willard DA. Disposition of Pravastatin sodium, a tissue-selective HMG-CoA reductase inhibitor, in healthy subjects. Br. J. Clin. Pharmacol. 1990; 29: 239-243.
43. Quion JAV, Jones PH. Clinical pharmacokinetics of Pravastatin. Clin. Pharmacokinet. 1994; 27: 94-103.
44. Martin PD, Warwick MJ, Dane AL, Brindley C, Short T. Absolute oral bioavailability of Rosuvastatin in healthy white adult male volunteers. Clin. Ther. 2003; 25: 2553-2563.
45. Martin PD, Warwick MJ, Dane AL. Metabolism, excretion, and pharmacokinetics of Rosuvastatin in healthy adult male volunteers. Clin. Ther. 2003; 25: 2822-2835.
46. Simonson SG, Martin PD, Mitchell P, Schneck DW, Lasseter KC, Warwick MJ. Pharmacokinetics and pharmacodynamics of Rosuvastatin in subjects with hepatic impairment. Eur. J. Clin. Pharmacol. 2003; 58: 669-675.
47. Olsson AG, Pears J, McKellar J, Mizan J, Raza A. Effect of Rosuvastatin on low-density lipoprotein cholesterol in patients with hypercholesterolemia. Am. J. Cardiol. 2001; 88: 504-508.
48. Jones P, Kafonek S, Laurora I, Hunninghake D. For the CURVES Investigators. Comparative dose efficacy of Atorvastatin versus Simvastatin, Pravastatin, Lovastatin, and Fluvastatin in patients with hypercholesterolaemia. Am. J. Cardiol. 1998; 81: 582-587.
49. Jones PH, Davidson MH, Stein EA. The STELLAR Study Group. Comparison of efficacy and safety of Rosuvastatin versus Atorvastatin, Simvastatin, and Pravastatin across doses (STELLAR Trial). Am. J. Cardiol. 2003; 92: 152-160.
50. Black DM. A general assessment of the safety of HMG CoA reductase inhibitors (statins).
51. Furberg CD, Pitt B. Withdrawal of Cerivastatin from the world market. Curr. Control Trials Cardiovasc. Med. 2001; 2: 205-207.
52. González-Ponte ML, González-Ruiz M, Duvós E. Atorvastatin-induced severe thrombocytopenia. Lancet 1998; 352:1284.
53. Groneberg DA, Barkhuizen A, Jeha T. Simvastatin-induced thrombocytopenia. Am J Hematol 2001; 67: 277.
54. Yamada T, Shinohara K, Katsuki K. Severe thrombocytopenia caused by Simvastatin in which thrombocyte recovery was initiated after severe bacterial infection. Clin Drug Investig 1998; 16:172-174.
55. Possamai G, Bovo P, Santonastaso M. Thrombocytopenic purpura during therapy with Simvastatin. Haematologica 1992; 77: 357-358.
56. Ames PR. Simvastatin-induced thrombocytopaenia: a further case and a brief on its clinical relevance. Ann Hematol 2008; 87: 773-774.
57. Kenney B, Stack G. Drug-induced thrombocytopenia. Arch Pathol Lab Med 2009; 133: 309-314.
58. Wolfe SM. Dangers of rosuvastatin identified before and after FDA approval. Lancet 2004; 363: 2189-2190.
59. Keller DM. Atorvastatin Beats Rosuvastatin in Protecting Kidneys in Diabetic and Nondiabetic Patients. 2010; July 2, [Medscape].
60. Buyukhatipoglu H, Sezen Y, Guntekin U, Kirhan I, Dag OF. Acute renal failure with the combined use of Rosuvastatin and Fenofibrate. Ren Fail. 2010; 32(5): 633-635.
61. Husten L. Postmarketing study finds high rate of adverse events with Rosuvastatin. 2005; May 23: [Medscape].
62. Prajapati S, Shah S, Desai C, Desai M, Dikshit RK. Atorvastatin-induced pancreatitis. Indian journal of Pharmacology 2010; 42(5): 324-325.
63. Singh S, Nautiyal A, Dolan JG. Recurrent Acute Pancreatitis Possibly Induced by Atorvastatin and Rosuvastatin. Is Statin Induced Pancreatitis a Class Effect? JOP. J Pancreas (Online) 2004; 5(6):502-504.
64. McDonald KB, Garber B, Perreault M. Pancreatitis associated with Simvastatin plus Fenofibrate. Ann Pharmacother 2002; 36:275-9.
65. Anagnostopoulos GK, Tsiakos S, Margantinis G, Kostopoulos P, Arvanitidis D. Acute pancreatitis due to pravastatin therapy. J Pancreas (Online) 2003; 4:129-32.
66. Tysk C, Al-Eryani AY, Shawabkeh AA. Acute pancreatitis induced by Fluvastatin therapy. J Clin Gastroenterol 2002; 35:406-8.
67. Miltiadous G, Anthopoulou A, Elisaf M. Acute pancreatitis possibly associated with combined salicylate and Atorvastatin therapy. J Pancreas (Online) 2003; 4:20-1.
68. Shechter M, Beigel R, Matetzky S, Freimark D, Chouraqui P. The intensive statin therapy myth. Isr Med Assoc J. 2005 Nov; 7(11):683-7.
69. Ara R, Rafia R, Ward SE, Wierzbicki AS, Reynolds TM, Rees A, Pandor A. Are Intensive Lipid-lowering Regimens an Optimal Economic Strategy in Patients with ACS? An Acute and Chronic Perspective. Expert Rev Pharmacoeconomics Outcomes Res. 2009; 9(5):423-433.
70. McKenney JM, Jones PH, Adamczyk MA, Cain VA., Bryzinski BS, Blasetto J W. Comparison of the Efficacy of Rosuvastatin versus Atorvastatin, Simvastatin, and Pravastatin in Achieving Lipid Goals: Results from the STELLAR Trial. Curr Med Res Opin. 2003; 19(8).
71. Jones PH, Davidson MH, Stein EA. Comparison of the efficacy and safety of Rosuvastatin versus Atorvastatin, Simvastatin, and Pravastatin across doses (STELLAR Trial). Am J Cardiol 2003; 92:152-60.
72. Shepherd J, Hunninghake DB, Barter P, McKenney JM, Hutchinson HG. Guidelines for lowering lipids to reduce coronary artery disease risk: a comparison of Rosuvastatin with Atorvastatin, Pravastatin, and Simvastatin for achieving lipid-lowering goals. Am J Cardiol 2003; 91(Suppl 1):11C-19C.
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01-07-2011
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“AN OVERVIEW OF STATINS AS HYPOLIPIDEMIC DRUGS”. International Journal of Pharmaceutical Sciences and Drug Research, vol. 3, no. 3, July 2011, pp. 178-83, https://doi.org/10.25004/IJPSDR.2011.030303.
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Review Article
Copyright (c) 2011 K. Srinivasa Rao, T. Prasad, G. P. Mohanta, P. K. Manna
This work is licensed under a Creative Commons Attribution 4.0 International License.
How to Cite
“AN OVERVIEW OF STATINS AS HYPOLIPIDEMIC DRUGS”. International Journal of Pharmaceutical Sciences and Drug Research, vol. 3, no. 3, July 2011, pp. 178-83, https://doi.org/10.25004/IJPSDR.2011.030303.
