Статья
Одновременное ингибирование всасывания и синтеза холестерина при сочетанном применении эзетимиба и симвастатина
Обзор посвящен фармакологической характеристике, механизму действия, гиполипидемической активности и плеотропным эффектам нового гиполипидемического средства эзетимиба, ингибирующего абсорбцию холестерина кишечником. Особое внимание уделено работам, в которых эзетимиб применялся в сочетании с другими гиполипидемическими средствами (статинами, фибратами, секвестрантами желчных кислот). Показано, что начальная доза разных статинов в сочетании с 1 таблеткой (10 мг) эзетимиба снижают уровень холестерина липопротеинов низкой плотности в такой же степени, что и максимальная доза статина.
1. Assmann G, Kannenberg F, Weng W, et al. Effects of Esetimibe, Atorvastatin, and Ezetimibe-Atorvastatin on Non-cholesterol Sterols 2004. MSD, Schering-Plough.
2. Ballantyne CM, Blazing MA, King TR, et al. Efficacy and Safety of Ezetimibe Co-Administered With Atorvastatin in Adults With Hypercholesterolaemia. Am J Cardiol 2004; 93: 1487-94.
3. Ballantyne CM, Houri J, Notarbartolo A, et al. Effect of Ezetimibe Coadministered With Atorvastatin in 628 Patients With Primary Hypercholesterolaemia. A Prospective, Randomized, Double-Blind Trial. Circulation 2003; 107: 2409-15.
4. Bauer KS, Kosoglou T, Statkevich P, et al. Ezetimibe does not affect the pharmacokinetics and pharmacodynamics of varfarin. Clin Pharmacol Ther 2001; 69: 5.
5. Bays HE, Moore PB, Drehobl MA, et al. Effectivenes and tolerability of ezetimibe in patients with primary hypercholesterolaemia: pooled analysis of two phase II studies. Clin Ther 2001; 23: 1209-30.
6. Bays HE, Ose L, Fraser N, et al. A multicenter, randomized, double-blind, placebo-controlled, factorial design study to evaluate the lipid-altering efficacy and safety profile of the ezetimibe-simvastatin tablet compared with ezetimibe and simvastatin monotherapy in patients with primary hyperccholesterolemia. Clin Ther 2004; 26(11): 1758-73.
7. Cook JR, Yin D, Alemao E, et al. Cost-effectiveness of ezetimibe coadministration in statin-treated patients not at cholesterol goal: application to Germany, Spain and Norway. Pharmacoeconomics 2004 ; 3: 49-61.
8. Davidson MH, McGarry T, Bettis R, et al. Ezetimibe coadministered with primary hypercholesterolaemia. JACC 2002; 40(12): 2125-34.
9. Davies GM, Cook JR, Erbey J, et al. Projected coronary heart disease risk benefit with ezetimibe. Atherosclerosis 2005; 179(2): 375-8.
10. Davis HR, Compton DS, Hoos L, Tetzloff G. Ezetimibe, a Potent Cholesterol Absorption Inhibitor, Inhibits the Development of Atherosclerosis in ApoE Knockout Mice. Arterioscler Thromb Vasc Biol 2001; 21: 2032-8.
11. Ezzet F, Wexler D, Statkevich P, et al. The plasma concentration and LDL-C relationship in patients receiving ezetimibe. J Clin Pharmacol 2001; 41(9): 943-9.
12. Farnier M, Freeman MW, Macdonell G, et al. Efficacy and safety of the coadministration of ezetimibe with fenofibrate in patients with mixed hyperlipidaemia. Eur Heart J 2005; 26(9): 897-905.
13. Feldman T, Koren M, Insull WJr, et al. Treatment of High Risk Patients with Ezetimibe Plus Simvastatin Coadministration Versus Simvastatin Alone to Attain National Cholesterol Education Program Adult Treatment Panel III Low-Density Lipoprotein Cholesterol Goals. Am J Cardiol 2004; 93: 1481-6.
14. Gagne C, Gaudet D, Bruckert E; Ezetimibe Study Group. Efficacy and safety of ezetimibe coadministered with atorvastatin or simvastatin in patients with homozygous familial hypercholesterolaemia. Circulation 2002; 105(21): 2469-75.
15. Gaudiani LM, Lewin A, Meneghini L, et al. Efficacy and safety of ezetimibe co-administered with simvastatin in triazolidinedione-treated type 2 diabetic patients. Diabetes Obes Metab 2005; 7(1): 88-97.
16. Geiss HC, Otto C, HundWissner E, Parhofer KG. Effects of ezetimibe on plasma lipoproteins in severely hypercholesterolemic patients treated with regular LDL-apheresis and statins. Atherosclerosis 2005; 180(1): 107-12.
17. Goettsch WG, Yin DD, Alemao E, et al. Statins are less effective in common daily practice among patients with hypercholesterolemia: the REALITY-PHARMO study. Current Medical Research and Opinion 2004; 20(7): 1025-33.
18. Harris M, Davis W, Brown WV. Ezetimibe. Drugs Today (Bare) 2003; 39(4): 229-47.
19. van Heek M, Farley C, Compton DS, et al. Ezetimibe selectively inhibits intestinal cholesterol absorption in rodents in the presence and absence of exocrine pancreatic function. Br J Pharmacol 2001; 134(2): 409-17.
20. van Heek M, Austin TM, Farley C, et al. Ezetimibe, a Potent Cholesterol Absorption Inhibitor, Normalizes Combined Dyslipidemia in Obese Hyperinsulmemic Harmsters. Diabetes 2001; 50: 1330-5, by the American Diabetes Association, Inc.
21. van Heek M, Compton DS, Davis HR. The cholesterol absorption inhibitor, ezetimibe, decreases diet-induced hypercholesterolemia in monkeys. Eur J Pharmacol 2001; 415(1): 79-84.
22. van Heek M, France CF, Compton DS, et al. In Vivo Metabolism-Based Discovery of a Potent Cholesterol Absorption Ingibitor, SCH58235, in the Rat and Rhesus Monkey through the Identification of the Active Metabolites of SCH484&bT. Pharmacology 1997; 283(1): 157-63.
23. van Heek M, Farley C, Compton D, et al. The potent cholesterol absorption inhibitor, ezetimibe, is glucuronidated in the intestine, localizes to the intestine, and circulates enterohepatically. Atherosclerosis 2000; 151-5.
24. Karpe F, Boquist S, Tang R, et al. Remnant lipoproteins are related to intima-media thickness of the carotid artery independently of LDL cholesterol and plasma triglycerides. J Lipid Res 2001; 42(1): 17-21.
25. Keung ASF, Kosoglou T, Statkevich P, et al. Ezetimibe does not affect the pharmacokinetics of oral contraceptives. Clin Pharmacol Ther 2001; 69: 5.
26. Knopp RH, Dujovne CA, Le Beaut A, et al.; Ezetimibe Study Group. Evaluation of the efficacy, safety, and tolerability of ezetimibe in primary hypercholesterolaemia: a pooled analysis from two controlledjjhase III clinical studies. Int J Clin Pract 2003; 57(5): 363-8.
27. Knopp RH, Gitter H, Truitt T, et al.; Ezetimibe Study Group. Effects of ezetimibe, a new cholesterol absorption inhibitor, on plasma lipids in patients with primary hypercholesterolaemia. Eur Heart J 2003; 24(8): 729-41.
28. Kosoglou T, Statcevich P, Meyer I, et al. Effects of ezetimibe on the pharmacodynamics and pharmacokinetics of lovastatin. Curr Med Res Opin 2004; 20(6): 955-65.
29. Kosoglou T, Statcevich P, Bauer KS, et al. Ezetimibe does not affect the pharmacokinetics and pharmacodynamics of digoxin. AAPS Pharma Sci 2001; 3: 3.
30. Kosoglou T, Statcevich P, Fruchart JC, et al. Pharmacodynamic and pharmacokinetic interaction between fenofibrate and ezetimibe. Curr Med Res Opin 2004; 8: 1197-207.
31. Kerzner B, Corbelli J, Sharp S, et al.; Ezetimibe Study Group. Efficacy and safety of ezetimibe coadministered with lovastatin in primary hypercholesterolaemia. Am J Cardiol 2003; 91(4): 418-24.
32. Kramer W, Girbig F, Corsiero D, et al. Aminopeptidase N (CD 13) is a molecular target of the cholesterol absorption inhibitor ezetimibe in the enterocyte brush border membrane. J Biol Chem 2005; 280(2): 1306-20.
33. Kugiyama K, Doi H, Takazoe K, et al. Remnant lipoprotein levels in fasting serum predict coronary events in patients with coronary artery disease. Circulation 1999; 99(22): 2858-60.
34. Lipka L, Ballantyne C, Sager P, et al. Evaluation of the LongTerm Safety and Tolerability Profile of Exetimibe Plus Atorvastatin Coadministration Therapy in Patients with Primary Hypercholesterolemia 2003. MSD, Schering-Plough.
35. Lipka L, Sager P, Capece R, et al. Effects of Ezetimibe Coadministered with Simvastatin on C-Reactive Protein in a Large Cohort of Hypercholesterolemic Patients 2003. MSD, ScheringPlough.
36. Masana L, Mata P, Gagne C, et al. Long-term safety and, tolerability profiles and lipid-modifying efficacy of ezetimibe coadministered with ongoing simvastatin treatment: a multicenter, randomized, double-blind, placebo-controlled, 48-week extension study. Cllin Ther 2005; 27(2): 174-84.
37. Mata P, Roth E, Masana L, et al. Ezetimibe Added to Ongoing Statin Therapy: Incremental Reductions in Low-Density Lipoprotein Cholestero T Are Independent of Statin Efficacy. Schering-Plough 2003.
38. Melani L, Mills R, Hassman D, et al., for the Ezetimibe Study Group. Efficacy and safety of ezetimibe coadministered with pravastatin in patients with primary hypercholesterolemia: a prospective, randomized, double-blind trial. Eur Heart J 2003; 24: 711-28.
39. Meng CQ. Ezetimibe (Schering-Plough). Curr Opin Investing Drugs 2001; 2(3): 389-92.
40. Ose L, Bays HE, Eraser N, et al. EzetimibeSimvastatin Therapy Is More Effective Than Simvastatin Alone at Reducing Remnant-Like Particle Cholesterol. MSD, Schering-Plough.
41. Patrick JE, Kosoglou T, Stauber KL, et al. Disposition of the Selective Cholesterol Absorption Inhibitor Ezetimibe in Healthy Male Subjects. Drug Metabol Dispos 2002; 30(4): 430-7.
42. Pearson TA, Denke MA, McBride PE, et al. A community-based randomized trial of ezetimibe added to statin therapy to attain NCEP ATP III goals for LDL cholesterol in hypercholesterolemic patients: the ezetimibe add-on to statin for effectiveness (EASE) trial. Mayo Clin Proc 2005; 80(5): 585-6.
43. Ridker PM, Rifai N, Pfeffer MA, et al., for the Cholesterol and Recurrent Events (CARE) Investigators. Inflammation, Pravastatin, and the risk of coronary events after myocardial infarction in patients with average cholesterol levels. Circulation 1998; 98: 839-44.
44. Sager PT, Melani L, Lipka L, et al.; Ezetimibe Study Group. Effect of coadministration of ezetimibe and simvastatin on highensitivity C-reactive protein. Am J Cardiol 2003; 92(12): 1414- 8.
45. Sager PT, Capece R, Lipka L, et al.; Ezetimibe Study Group. Effect of ezetimibe coadministration with simvastatin on C-reactive protein in a large cohort of hypercholesterolemic patients. Atherosclerosis 2005; 179(2): 361-7.
46. Salen G, von Bergmann K, Lutjohann D, et al.; Multicenter Sitosterolemia Study Group. Ezetimibe effectively reduces plasma plant sterols in patients with sitosterolemia. Circulation 2004; 109(8): 966-71.
47. Shepherd J. Combined lipid lowering drug therapy for the effective treatment of hypercholesterolaemia. Eur Heart J 2003; 24: 685-9.
48. Statkevich P, Reyderman L, Kosoglou T, et al. Ezetimibe does not affect the pharmacokinetics and pharmacodynamics of glipizide. Clin Pharmacol Ther 2001; 67-9.
49. Sudhop T, Lutjohann. Sterol-transporters: targets of natural sterols and new lipid lowering drugs. Pharmacol Ther 2005; 105(3): 333-41.
50. Turley SD, Dietschy JM. Sterol absorption by the small intestine. Curr Opin Lipidol 2003; 14(3): 233-40.
51. Wierzbicki AS, Doherty E, Lumb PJ, et al. Efficacy of ezetimibe in patients with statin-resistant and statin-intolerant familial hyperlipidaemias. Curr Med Res Opin 2005; 21(3): 333-8.
52. Xydakis AM, Guyton JR, Chiou P, et al. Effectiveness and tolerability of ezetimibe add-on therapy to a bile acid resin-based regimen for hypercholesterolemia. Am J Cardiol 2004; 94(6): 795-7.
53. Zhu Y, Statkevich P, Kosoglou T, et al. The effect of gender on the farmacokinetics of SCH58235, a holesterol absorption inhibitor. AAPS Pharm Sci 1999; 1: S-24.
54. Zilversmit DB. Atherogenesis: a postprandial phenomenon. Circulation 1979; 60(3): 473-85.
55. Zhu Y, Statkevich P, Kosoglou Т, et al. Effect of ezetimibe (SCH 58235) on the activity of drug metabolizing enzymes in vivo. Clin Pharrnacol Ter 2000; 67: 152.