Atorvastatin: A hydroxymethylglutaryl-coenzyme A reductase inhibitor

American Journal of Health-System Pharmacy

Volumn 55, Issue 21, 1998, Pages 2253-2267

  Malinowski, Jennifer M ^a,b  

^a WILKES UNIVERSITY   (United States)

^b Mercy Health Partners   (United States)

Author keywords

Antilipemic agents; Atorvastatin calcium; Clinical studies; Coronary disease; Drug comparisons; Drug interactions; Formularies; Hypercholesterolemia; Mechanism of action; Pharmacokinetics; Toxicity

Indexed keywords

ATORVASTATIN; CLARITHROMYCIN; ERYTHROMYCIN; FLUINDOSTATIN; GEMFIBROZIL; HYDROXYMETHYLGLUTARYL COENZYME A REDUCTASE INHIBITOR; INDINAVIR; ITRACONAZOLE; MEVINOLIN; NEFAZODONE; NELFINAVIR; NICOTINIC ACID; PRAVASTATIN; RITONAVIR; SAQUINAVIR; SIMVASTATIN;

ADULT; AGED; COMPETITIVE INHIBITION; CORONARY ARTERY DISEASE; DOSE RESPONSE; DRUG ABSORPTION; DRUG DISTRIBUTION; DRUG ELIMINATION; ENZYME INHIBITION; FEMALE; FIRST PASS EFFECT; HUMAN; HYPERCHOLESTEROLEMIA; LIVER TOXICITY; MAJOR CLINICAL STUDY; MALE; MYOPATHY; PRIORITY JOURNAL; REVIEW;

EID: 0032212982     PISSN: 10792082     EISSN: None     Source Type: Journal    
DOI: 10.1093/ajhp/55.21.2253     Document Type: Review

References (90)

1. National Heart, Lung, and Blood Institute. Morbidity and mortality: chartbook on cardiovascular, lung, and blood diseases. Bethesda, MD: National Institutes of Health; 1992.
2. Expert Panel on Detection, Evaluation, and Treatment of High Blood Cholesterol in Adults. Summary of the second report of the National Cholesterol Education Program (NCEP) Expert Panel on Detection, Evaluation, and Treatment of High Blood Cholesterol in Adults (Adult Treatment Panel II). JAMA. 1993; 269:3015-23.
3. Stamler J, Wentworth D, Neaton JD. Is the relationship between cholesterol and risk of premature death from CHD continuous and graded? JAMA. 1986; 256:2823-8.
4. Castelli WP, Garrison RJ, Wilson PWF et al. Incidence of coronary heart disease and lipoprotein cholesterol levels. The Framingham study. JAMA. 1986; 256:2835-8.
5. Neaton JD, Blackburn H, Jacobs D et al. Serum cholesterol level and mortality findings for men screened in the multiple risk factor intervention trial. Arch Intern Med. 1992; 152:1490-500.
6. Schucker B, Wittes JT, Santanello NC et al. Change in cholesterol awareness and action; results from national physician and public surveys. Arch Intern Med. 1991; 151:666-73.
7. Thelle DS. Epidemiology of hypercholesterolemia and European management guidelines. Cardiology. 1990; 77(S4):2-7.
8. Farmer JA, Gotto AM. Choosing the right lipid-regulating agent. Drugs. 1996; 52:649-61.
9. Lipid Research Clinics Program: the Lipid Research Clinics Coronary Primary Prevention Trial results: II. The relationship of reduction in incidence of coronary heart disease to cholesterol lowering. JAMA. 1984; 251:365-74.
10. Frick HM, Elo O, Haapo K et al. Helsinki Heart Study: primary-prevention trial with gemfibrozil in middle-aged men with dyslipidemia. N Engl J Med. 1987; 317:1237-45.
11. Shepherd J, Cobbe SM, Ford I et al. Prevention of coronary heart disease in men with hypercholesterolemia. N Engl J Med. 1995; 333:1301-7.
12. Scandinavian Simvastatin Survival Study Group. Randomised trial of cholesterol lowering in 4,444 patients with coronary heart disease; the Scandinavian Simvastatin Survival Study (4S). Lancet. 1994; 344:1383-9.
13. Sacks FM, Pfeffer M, Moye LA et al. The effect of pravastatin on coronary events after myocardial infarction in patients with average cholesterol levels; the Cholesterol and Recurrent Events trial (CARE). N Engl J Med. 1996; 335:1001-9.
14. Lipitor (atorvastatin) package insert. Morris Plains, NJ: Parke-Davis; 1997.
15. Blum C. Comparison of properties of four inhibitors of 3-hydroxy-3-methylglutaryl-coenzyme A reductase. Am J Cardiol. 1994; 73:3D-11D.
16. Jungnickel PW, Cantral KA, Maloley PA. Pravastatin: a new drug for the treatment of hypercholesterolemia. Clin Pharm. 1992; 11:677-89.
17. Levy RI, Troendle AJ, Fattu JM. A quarter century of drug treatment of dyslipoproteinemia, with a focus on the new HMG-CoA reductase inhibitor fluvastatin. Circulation. 1993; 87(suppl III):III-45-III-53.
18. Radulovic LL, Cilla DD, Posvar EL et al. Effect of food on the bioavailability of atorvastatin, an HMG-CoA reductase inhibitor. J Clin Pharmacol. 1995; 35:990-4.
19. Grundy S. HMG-CoA reductase inhibitors for the treatment of hypercholesterolemia. N Engl J Med. 1988; 319:29-32.
20. Nawrocki JW, Weiss SR, Davidson MH et al. Reduction of LDL-C cholesterol by 25% to 60% in patients with primary hypercholesterolemia by atorvastatin, a new HMG-CoA reductase inhibitor. Arterioscler Thromb Vasc Biol. 1995; 15:678-82.
21. Heinonen TM, Stein E, Weiss SR et al. The lipid lowering effects of atorvastatin, a new HMG-CoA reductase inhibitor: results of a randomized, double-masked study. Clin Ther. 1996; 18:853-63.
22. Cilla DD, Whitfield LR, Gibson DM et al. Multiple-dose pharmacokinetics, pharmacodynamics, and safety of atorvastatin, an inhibitor of HMG-CoA reductase, in healthy subjects. Clin Pharmacol Ther. 1996; 60:687-95.
23. Bakker-Arkema RG, Davidson MH, Goldstein RJ et al. Efficacy and safety of a new HMG Co-A reductase inhibitor, atorvastatin, in patients with hypertriglyceridemia. JAMA. 1996; 275: 128-33.
24. Gmerek A, Yang R, Bays H et al. Atorvastatin causes a dose-dependent reduction in LDL cholesterol and triglycerides. Paper presented at 66th Congress of the European Atherosclerosis Society. Florence, Italy; 1996 Jul 13-17.
25. Bakker-Arkema R, Best J, Fayad R et al. A brief review paper of the efficacy and safety of atorvastatin in early clinical trials. Atherosclerosis. 1997; 131:17-23.
26. Naumova RP, Marais D, Firth JC et al. Atorvastatin augments therapy of homozygous familial hypercholesterolemia by inhibiting upregulation of cholesterol synthesis after apheresis and bile acid sequestrants. Circulation. 1996; 94:I-583. Abstract.
27. Bocan TMA, Mazur MJ, Mueller SB et al. Atherosclerotic activity of inhibitors of 3-hydroxy 3-methylglutaryl-coenzyme A reductase in cholesterol-fed rabbits: a biochemical and morphological evaluation. Atherosclerosis. 1994; 111:127-42.
28. Ortega M, Bustos C, Hernandez-Presa M et al. The HMG-CoA reductase inhibitor atorvastatin reduces NF-kB activation and MCP-1 gene expression in vascular smooth muscle cells and mononuclear cells. Paper presented at 66th Congress of the European Atherosclerosis Society. Florence, Italy; 1996 Jul 13-17.
29. Soma M, Piliego T, Seregni R et al. Effect of atorvastatin on intimal carotid thickening induced by perivascular manipulation in normocholesterolemia rabbits. Paper presented at 66th Congress of the European Atherosclerosis Society. Florence, Italy; 1996 Jul 13-17.
30. Weissberg P, Clesham G, Bennett M. Is vascular smooth muscle cell proliferation beneficial? Lancet. 1996; 347:305-7.
31. Bakker-Arkema R, Fayyad R, Davidson M et al. One year study comparing the safety and efficacy of atorvastatin to that of lovastatin. Paper presented at 66th Congress of the European Atherosclerosis Society. Florence, Italy; 1996 Jul 13-17.
32. Lescol (fluvastatin) package insert. East Hanover, NJ: Sandoz Pharmaceuticals; 1995.
33. Mevacor (lovastatin) package insert. West Point, PA: Merck; 1995.
34. Pravachol (pravastatin) package insert. Princeton, NJ: Bristol-Myers Squibb; 1996.
35. Zocor (simvastatin) package insert. West Point, PA: Merck; 1997.
36. Posvar EL, Radulovic LL, Cilia DD et al. Tolerance and pharmacokinetics of single-dose atorvastatin, a potent inhibitor of HMG-CoA reductase, in healthy subjects. J Clin Pharmacol. 1996; 36:728-31.
37. Yang B, Smithers J, Stern R et al. Pharmacokinetics and dose proportionality of atorvastatin and its active metabolites. Pharm Res. 1996; 13(9, suppl):S437. Abstract.
38. Whitfield LR, Cilla DD, Posvar EL et al. Single and multiple dose pharmacokinetics of CI-981, a potent HMG-CoA reductase inhibitor. Pharm Res. 1993; 10(suppl):S340. Abstract.
39. Hsu I, Spinier S, Johnson N. Comparative evaluation of the safety and efficacy of HMG-CoA reductase inhibitor monotherapy in the treatment of primary hypercholesterolemia. Ann Pharmacother. 1995; 29:743-59.
40. McKenney JM. Lovastatin: a new cholesterol-lowering agent. Clin Pharm. 1988; 7:21-36.
41. Smith HT, Jokubaitis LA, Troendle AJ et al. Pharmacokinetics of fluvastatin and specific drug interactions. Am J Hypertens. 1993; 6:1S-8S.
42. Desylpere JP. Clinical implications of the biopharmaceutical properties of fluvastatin. Am J Cardiol. 1994; 73:12D-7D.
43. Pan H, DeVault A, Glaess S et al. Effect of food on the pharmacokinetics and pharmacodynamics of pravastatin, an HMG-CoA reductase inhibitor. Arteriosclerosis. 1988; 8:S88a. Abstract.
44. Mauro VF. Clinical pharmacokinetics and practical applications of simvastatin. Clin Pharmacol. 1993; 24:195-202.
45. Saito Y, Yoshida S, Nakaya N et al. Comparison between morning and evening doses of simvastatin in hyperlipemic subjects: a double blind comparative study. Arterioscler Thromb. 1991; 11:816-26.
46. Pan HY, DeVault AR, Brescia D et al. Comparative efficacy of once daily versus twice daily pravastatin in primary hypercholesterolemia. Clin Ther. 1991; 13:368-72.
47. Insull W, Black D, Dujovne C et al. Efficacy and safety of once daily versus twice daily dosing with fluvastatin, a synthetic reductase inhibitor, in primary hypercholesterolemia. Arch Intern Med. 1994; 154:2449-55.
48. Naumova R, Dunn S, Loubianos R et al. Prolonged inhibition of cholesterol synthesis explains the efficacy of atorvastatin. J Lipid Res. 1997; 38:1496-500.
49. Dostal LA, Schardein JL, Anderson JA. Developmental toxicity of the HMG Co-A reductase inhibitor, atorvastatin, in rats and rabbits. Teratology. 1994; 50:387-94.
50. MacDonald JS, Gerson RJ, Kornbrust DJ et al. Preclinical evaluation of lovastatin. Am J Cardiol. 1988: 62(suppl):16J-27J.
51. Cilla D, Radulovic E, Whitfield L et al. Safety, tolerance and pharmacokinetic profiles following single dose of CI-981, a potent HMG-CoA reductase inhibitor. Pharm Res. 1993; 10(suppl):S332. Abstract.
52. Gibson DM, Bron NJ, Richens A et al. Effect of age and gender on pharmacokinetics of atorvastatin in humans. J Clin Pharmacol. 1996; 36:242-6.
53. Gibson DM, Yang BB, Abel RB et al. Effects of hepatic and renal impairment on pharmacokinetics and pharmacodynamics of atorvastatin. Pharm Res. 1996; 13 (9, suppl):S428. Abstract.
54. Stern R, Yang B, Horton M et al. Renal dysfunction does not alter the pharmacokinetics or low density lipoprotein concentration reduction of atorvastatin. J Clin Pharmacol. 1997; 37(9):816-9.
55. Kellick K, Burns K, McAndrew E et al. Focus on atorvastatin: an HMG-CoA reductase inhibitor for lowering both elevated low density lipoprotein concentrations and triglycerides in hypercholesterolemic patients. Formulary. 1997; 32:352-63.
56. Bracs P, Best J, Hamilton-Craig I et al. A one year study comparing atorvastatin and simvastatin in patients with hypercholesterolemia. Paper presented at 66th Congress of the European Atherosclerosis Society. Florence, Italy; 1996 Jul 13-17.
57. Egros F, Langan J, Bertolini S et al. A one year study comparing atorvastatin and pravastatin in patients with hypercholesterolemia. Paper presented at 66th Congress of the European Atherosclerosis Society. Florence, Italy; 1996 Jul 13-17.
58. Wagner B, Huwel D, Rehorst D et al. One year treat-to-target study of atorvastatin versus pravastatin in high risk-stratified hypercholesterolemic patients. Paper presented at 66th Congress of the European Atherosclerosis Society. Florence, Italy; 1996 Jul 13-17.
59. Illingworth D, Erkelens D, Keller U et al. Defined daily doses to hypolipidaemic effects of lovastatin, pravastatin, and simvastatin. Lancet. 1994; 343:1554-5.
60. Illingworth D, Stein E, Knopp R et al. A randomized, multicenter trial comparing the effectiveness of simvastatin to fluvastatin. J Cardiovasc Pharmacol. 1996; 1(1):23-30.
61. Dart A, Jerums G, Nicholson G et al. A multicenter, double blind, one year study comparing the safety and efficacy of atorvastatin versus simvastatin in patients with hypercholesterolemia. Am J Cardiol. 1997; 80:39-44.
62. McCormick L, Black D. A 12 week study comparing atorvastatin with niacin in patients with hypertriglyceridemia with or without hypercholesterolemia. Paper presented at 66th Congress of the European Atherosclerosis Society. Florence, Italy; 1996 Jul 13-17.
63. Heinonen T, Tan M, Davignon J et al. Atorvastatin compared to fenofibrate in patients with elevated cholesterol and triglycerides. Paper presented at 66th Congress of the European Atherosclerosis Society. Florence, Italy; 1996 Jul 13-17.
64. Best J, Nicholson G, O'Neal D et al. Atorvastatin versus simvastatin reduce elevated low density lipoprotein concentrations in type II diabetes mellitus. Atherosclerosis. 1994; 109:312. Abstract.
65. Nawrocki J, Schwartz S, Fayad R et al. Atorvastatin, a new HMG-CoA reductase inhibitor is safe and effective in NIDDM with hypertriglyceridemia. Paper presented at 66th Congress of the European Atherosclerosis Society. Florence, Italy; 1996 Jul x.
66. Lovastatin Study Groups I through IV. Lovastatin 5 year safety and efficacy study. Arch Intern Med. 1993; 153:1079-87.
67. Roth T, Richardson GR, Sullivan JP et al. Comparative effects of pravastatin and lovastatin on nighttime sleep and daytime performance. Clin Cardiol. 1992; 15:426-32.
68. Vgontsas AN, Kales A, Bixler EO et al. Effects of lovastatin and pravastatin on sleep efficiency and sleep stages. Clin Pharmacol. 1991; 50:730-7.
69. Bradford RH, Shear CL, Chremos AN et al. Expanded Clinical Evaluation of Lovastatin study results (EXCEL). Efficacy of modifying plasma lipoproteins and adverse event profile in 8245 patients with moderate hypercholesterolemia. Br J Clin Pharmacol. 1993; 35:284-9.
70. Neuvonen P, Jalava K. Itraconazole drastically increases plasma concentrations of lovastatin and lovastatin acid. Clin Pharmacol Ther. 1996; 60:54-61.
71. Lees R, Lees A. Rhabdomyolysis from the coadministration of lovastatin with the antifungal agent itraconazole. N Engl J Med. 1995; 333:664-5. Letter.
72. Corpier CL, Jones PH, Suki WN et al. Rhabdomyolysis and renal injury with lovastatin use. Report of two cases in cardiac transplant patients. JAMA. 1988; 260:239-72.
73. Spach D, Bauwens J, Clark C et al. Rhabdomyolysis associated with lovastatin and erythromycin use. West J Med. 1991; 154:213-6.
74. Jacobson R, Wang P, Gluech C. Myositis and rhabdomyolysis associated with concurrent use of simvastatin and nefazodone. JAMA. 1997; 277:296.
75. Pierce LR, Wysowski DK, Gross TP. Myopathy and rhabdomyolysis associated with lovastatin-gemfibrozil combination therapy. JAMA. 1990; 264:71-5.
76. Duell P, Connor W, Illingworth D. Rhabdomyolysis after taking atorvastatin with gemfibrozil. Am J Cardiol. 1998; 81(3):368-9.
77. Desager J, Hormans Y. Clinical pharmacokinetics of 3-hydroxy-3methylglutaryl coenzyme A reductase inhibitors. Clin Pharmacokinet. 1996; 31:348-71.
78. Transon C, Leeman T, Dayer P. In vitro inhibition of major human metabolic cytochrome P450 enzymes by HMG-CoA reductase inhibitors. Eur J Pharmacol. 1996; 50:209-15.
79. Tobert J, Shear C, Chremos A et al. Clinical experience with lovastatin. Am J Cardiol. 1990; 65(5):23F-6F.
80. Yang B, Hounslow N, Sedman A et al. Effects of atorvastatin, an HMG-CoA reductase inhibitor on hepatic oxidative metabolism of antipyrine. J Clin Pharmacol. 1996; 36:356-60.
81. Yang B, Smithers J, Siedlik P et al. Atorvastatin pharmacokinetic interactions with other CYP3A4 substrates: erythromycin and ethinyl estradiol. Pharm Res. 1996; 13(9, suppl):S437. Abstract.
82. Yang B, Smithers J, Abel R et al. Effects of Maalox TC on pharmacokinetics and pharmacodynamics of atorvastatin. Pharm Res. 1996; 13(9, suppl):S437. Abstract.
83. Roberts W. Retail costs of the statin lowering drugs. Am J Cardiol. 1994; 74:1181.
84. Spearman ME, Summers K, Moore V et al. Cost-effectiveness of initial therapy with 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors to treat hypercholesterolemia in a primary care setting of a managed care organization. Clin Ther. 1997; 19:582-602.
85. McMillan K. Consideration in the formulary selection of hydroxymethylglutaryl-coenzyme A reductase inhibitors. Am J Health-Syst Pharm. 1996; 53:2206-14.
86. Rubins H, Robins S, Collins D et al. Distribution of lipids in 8500 males with coronary artery disease. Department of Veteran Administration HDL intervention trial study group. Am J Cardiol. 1995; 75:1196-201.
87. Marcellino J, Feingold K. Inadequate treatment with HMG-CoA reductase inhibitors by health care providers. Am J Med. 1996; 100:605-10.
88. Baycol (cerivastatin) package insert. West Haven, CT: Bayer; 1997.
89. Merck to file for extended release Zocor in 1998; high dose is one strategy to combat atorvastatin launch: Zocor HMG-CoA reductase inhibitor market share is 29.9%. FDC Rep. 1996; 58(Dec 23):5.
90. Gannon K. Which new drugs get the nod on hospital formularies? Hosp Pharm Rep. 1997; 107:43.