Fixed dose combination of rosuvastatin and ezetimibe – drug profile
Authors:
O. Kyselák 1; V. Soška 1,2
Authors‘ workplace:
Oddělení klinické biochemie, FN u sv. Anny v Brně 2 II. interní klinika LF MU, Brno
1
Published in:
Kardiol Rev Int Med 2018, 20(2): 142-146
Overview
Hypercholesterolemia is the major risk factor for atherosclerotic cardiovascular diseases (ASCVD), particularly myocardial infarction. Statins are essential drugs for treatment of patients with hypercholesterolemia, but in monotherapy they are usually not effective enough to achieve the target values of LDL cholesterol. Therefore it is recommended to combine statins with ezetimibe. This combination has proven good safety and efficiency. In addition, a fixed dose combination increases patient adherence to long-term treatment.
Key words:
rosuvastatin – ezetimibe – LDL-cholesterol – cardiovascular diseases
Sources
1. Baigent C, Blackwell L, Emberson J et al. Efficacy and safety of more intensive lowering of LDL cholesterol: a meta-analysis of data from 170 000 participants in 26 randomised trials. Lancet 2010; 376(9753): 1670– 1681. doi: 10.1016/ S0140-6736(10)61350-5.
2. Mihaylova B, Emberson J, Blackwell L et al. The effects of lowering LDL cholesterol with statin therapy in people at low risk of vascular disease: meta-analysis of individual data from 27 randomised trials. Lancet 2012; 380(9841): 581– 590. doi: 10.1016/ S0140-6736(12)60367-5.
3. Catapano AL, Graham I, De Backer G et al. 2016 ESC/ EAS Guidelines for the management of dyslipidaemias. the task force for the management of dyslipidaemias of the European Society of Cardiology (ESC) and European Atherosclerosis Society (EAS). Atherosclerosis 2016; 253: 281– 344. doi: 10.1016/ j.atherosclerosis.2016.08.018
4. Wiegman A, Gidding SS, Watts, GF et al. Familial hypercholesterolaemia in children and adolescents: gaining decades of life by optimizing detection and treatment. Eur Heart J 2015; 36(36): 2425– 2437. doi: 10.1093/ eurheartj/ ehv157.
5. Rosuvastatin. Pubchem diabase. Available at: https:/ / pubchem.ncbi.nlm.nih.gov/ compound/ Ro-suvastatin#section=Top.
6. Duriez P. Mechanisms of actions of statins and fibrates. Therapie 2003; 58(1): 5– 14.
7. Current Medication Information for Crestor. Rosuvastatin Calcium Tablet, Film-Coated. NIH, U.S. National Library of Medicine. DailyMed. Updated: May 2016. Available at: https:/ / dailymed.nlm.nih.gov/ dailymed/ drugInfo.cfm?setid=bb0f3b5e-4bc6-41c9-66b9-6257e2513512.
8. Rosuvastatin (SPC). Souhrn informací o přípravku. Dostupný na: www.sukl.cz.
9. Drug Information 2016. Bethesda: American Society of Health-System Pharmacists 2016: 1865– 1866.
10. Jones PH, Davidson MH, Stein EA et al. Comparison of the efficacy and safety of rosuvastatin versus atorvastatin, simvastatin, and pravastatin across doses (STELLAR* Trial). Am J Cardiol 2003; 92(2): 152– 160.
11. Lund TM, Torsvik H, Falch D et al. Effect of morning versus evening intake of simvastatin on the serum cholesterol level in patients with coronary artery disease. Am J Cardiol 2002; 90(7): 784– 786.
12. Athyros VG, Alexandrides TK, Bilianou H et al. The use of statins alone, or in combination with pioglitazone and other drugs, for the treatment of non-alcoholic fatty liver disease/ non-alcoholic steatohepatitis and related cardiovascular risk. An Expert Panel Statement. Metabolism 2017; 71: 17– 32. doi: 10.1016/ j.metabol.2017.02.014.
13. Stroes ES, Thompson PD, Corsini A et al. Statin--associated muscle symptoms: impact on statin therapy-European Atherosclerosis Society Consensus Panel Statement on Assessment, Aetiology and Management. Eur Heart J 2015; 36(17): 1012– 1022. doi: 10.1093/ eurheartj/ ehv043.
14. Gupta A, Thompson D, Whitehouse A et al. ASCOT Investigators. Adverse events associated with unblinded, but not with blinded, statin therapy in the Anglo-Scandinavian Cardiac Outcomes Trial-Lipid-Lowering Arm (ASCOT-LLA): a randomised double-blind placebo-controlled trial and its non-randomised non-blind extension phase. Lancet 2017; 389(10088): 2473– 2481. doi: 10.1016/ S0140-6736(17)31075-9.
15. Law M, Rudnicka AR. Statin safety: a systematic review. Am J Cardiol 2006; 97(8A): 52C– 60C.
16. Piepoli MF, Hoes AW, Agewall S et al. 2016 European Guidelines on cardiovascular disease prevention in clinical practice The Sixth Joint Task Force of the European Society of Cardiology and Other Societies on Cardiovascular Disease Prevention in Clinical Practice (constituted by representatives of 10 societies and by invited experts). Euro Heart J 2016; 37(29): 2315– 2381. doi: 10.1093/ eurheartj/ ehw106.
17. Sattar N, Preiss D, Murray HM et al. Statins and risk of incident diabetes: a collaborative meta-analysis of randomised statin trials. Lancet 2010; 375(9716): 735– 742. doi: 10.1016/ S0140-6736(09)61965-6.
18. Ridker PM, Pradhan A, MacFadyen JG et al. Cardiovascular benefits and diabetes risks of statin therapy in primary prevention: an analysis from the JUPITER trial. Lancet 2012; 380(9841): 565– 571. doi: 10.1016/ S0140-6736(12)61190-8.
19. Knopp RH, Gitter H, Truitt T et al. Ezetimibe reduces low-density lipoprotein cholesterol: results of a Phase III, randomized, double-blind, placebo--controlled trial (abstr). Atherosclerosis 2001; 2(2): 38. doi: 10.1016/ S1567-5688(01)80027-1.
20. Gagné C, Bays HE, Weiss SR et al. Ezetimibe Study Group. Efficacy and safety of ezetimibe added to ongoing statin therapy for treatment of patients with primary hypercholesterolemia. Am J Cardiol 2002; 90(10): 1084– 1091.
21. Ge L, Wang J, Qi W et al. The cholesterol absorption inhibitor ezetimibe acts by blocking the sterol-induced internalization of NPC1L1. Cell Metab 2008; 7(6): 508– 519. doi: 10.1016/ j.cmet.2008.04.001.
22. Kishimoto M, Sugiyama T, Osame K et al. Efficacy of ezetimibe as monotherapy or combination therapy in hypercholesterolemic patients with and without diabetes. J Med Invest 2011; 58(1– 2): 86– 94.
23. Ezetímib. Pubchem diabase. Available at: https:/ / pubchem.ncbi.nlm.nih.gov/ compound/ Ezetimibe#section=Top.
24. Ezetimib (SPC). Souhrn informací o přípravku. Dostupný na: www.sukl.cz .
25. Cannon CP, Blazing MA, Giugliano RP et al. Ezetimibe added to statin therapy after acute coronary syndromes. N Engl J Med 2015; 372(25): 2387– 2397. doi: 10.1056/ NEJMoa1410489.
26. Baigent C, Landray MJ, Reith C et tal. The effects of lowering LDL cholesterol with simvastatin plus ezetimibe in patients with chronic kidney disease (Study of Heart and Renal Protection): a randomised placebo-controlled trial. Lancet 2011; 377(9784): 2181– 2192. doi: 10.1016/ S0140-6736(11)60739-3.
27. Giugliano RP, Cannon CP, Blazing MA et al. Benefit of adding ezetimibe to statin therapy on cardiovascular outcomes and safety in patients with versus without diabetes mellitus: results from IMPROVE-IT (Improved Reduction of Outcomes: Vytorin Efficacy International Trial). Circulation 2018; 137(15): 1571– 1582. doi: 10.1161/ CIRCU-LATIONAHA.117.030950.
28. Kosoglou T, Statkevich P, Yang B et al. Pharmacodynamic interaction between ezetimibe and rosuvastatin. Curr Med Res Opin 2004; 20(8): 1185– 1195. doi: 10.1185/ 030079904125004213.
29. Hong SJ, Jeong HS, Ahn, JC et al. A phase III, multicenter, randomized, double-blind, active comparator clinical trial to compare the efficacy and safety of combination therapy with ezetimibe and rosuvastatin versus rosuvastatin monotherapy in patients with hypercholesterolemia: I-ROSETTE (Ildong Rosuvastatin & Ezetimibe for Hypercholesterolemia) randomized controlled trial. Clin Ther 2018; 40(2): 226– 241. doi: 10.1016/ j.clinthera.2017.12.018.
30. Kim KJ, Kim SH, Yoon YW et al. Effect of fixed-dose combinations of ezetimibe plus rosuvastatin in patients with primary hypercholesterolemia: MRS-ROZE (Multicenter Randomized Study of ROsuvastatin and eZEtimibe). Cardiovasc Ther 2016; 34(5): 371– 382. doi: 10.1111/ 1755-5922.12213.
31. Masuda J, Tanigawa T, Yamada T et al. Effect of combination therapy of ezetimibe and rosuvastatin on regression of coronary atherosclerosis in patients with coronary artery disease. Int Heart J 2015; 56(3): 278– 285. doi: 10.1536/ ihj.14-311.
32. Kang WY, Seong SJ, Ohk B et al. Pharmacokinetics and bioequivalence of a rosuvastatin/ ezetimibe fixed-dose combination tablet versus single agents in healthy male subjects. Int J Clin Pharmacol Ther 2018; 56(1): 43– 52. doi: 10.5414/ CP203026.
33. Guglielmi V, Bellia A, Pecchioli S et al. Effectiveness of adherence to lipid lowering therapy on LDL-cholesterol in patients with very high cardiovascular risk: A real-world evidence study in primary care. Atherosclerosis 2017; 263: 36– 41. doi: 10.1016/ j.atherosclerosis.2017.05.018.
34. Selak V, Elley CR, Bullen C et al. Effect of fixed dose combination treatment on adherence and risk factor control among patients at high risk of cardiovascular disease: randomised controlled trial in primary care. BMJ 2014; 348: g3318. doi: 10.1136/ bmj.g3318.
35. Thom S, Poulter N, Field J et al. Effects of a fixed--dose combination strategy on adherence and risk factors in patients with or at high risk of CVD. The UMPIRE Randomized Clinical Trial. JAMA 2013; 310(9): 918– 929. doi: 10.1001/ jama.2013.277064.
36. Planès S, Villier C, Mallaret M. The nocebo effect of drugs. Pharmacol Res Perspect 2016; 4(2): e00208. doi: 10.1002/ prp2.208.
Labels
Paediatric cardiology Internal medicine Cardiac surgery CardiologyArticle was published in
Cardiology Review
2018 Issue 2
Most read in this issue
- Arrhythmias in young adults
- Juvenile hypertension
- Fixed dose combination of rosuvastatin and ezetimibe – drug profile
- Chronic venous insufficiency and varicose veins in young people