Complementary Therapy to Target LDL Cholesterol: The Role of the Ezetimibe/Simvastatin Combination

Figures & data

Table 1 ATPIII Guidelines 2001: CHD and CHD risk equivalents – target LDL-C < 100 mg/dL

• CHD

• Diabetes mellitus

• Noncoronary atherosclerosis

– Peripheral artery disease

– Abdominal aortic aneurysm

– Symptomatic carotid artery disease

• Multiple risk factors >20% CHD risk at 10 years

Abbreviations: CHD, coronary heart disease; LDL-C, low-density lipoprotein cholesterol.

Table 2 NCEP ATP III addendum: optional LDL-C goal <70 mg/dL for the very high-risk patient

CHD plus:

Diabetes mellitus; Severe or poorly controlled risk factors (ie, cigarette smoking, hypertension, or hyperlipidemia); Multiple risk factors associated with the metabolic syndrome; or Acute coronary syndrome.

Abbreviations: ATP III, Adult Treatment Panel III; CHD, coronary heart disease; LDL-C, low-density lipoprotein cholesterol; NCEP, National Cholesterol Education Program.

Table 3 Therapeutic options for achieving a 30%–40% reduction in LDL-C

Drug	Dose (mg/dL)	LDL-C reduction (%)
Atorvastatin	10*	39
Fluvastatin	40–80	25–35
Lovastatin	40*	31
Pravastatin	40*	34
Rosuvastatin	5–10+	39–45
Simvastatin	20–40*	35–41

Abbreviations: LDL-C, low-density lipoprotein cholesterol.

* Available at doses up to 80 mg/dL; doubling of dose will produce an additional 6% decrease in LDL-C.

+ Available at doses up to 40 mg/dL; doubling of dose will produce an additional 6% decrease in LDL-C

Grudy SM, et al. 2004. For the coordinating committee of the NCEP. Circulation, 110:227–39.

Figure 1 A schematic for sites of action of cholesterol-lowering agents, ezetimibe and simvastatin.

Abbreviations: CE, cholesterol ester; CM, chylomicron; CMr, chylomicron remnant; EZE, ezetimibe; IDL, intermediate density lipoprotein; LDL, low density lipoprotein; LDLr, low density lipoprotein receptor; VLDL, very low density lipoprotein; SIM, simvastatin; TG, triglyceride.

Figure 2 The structures for ezetimibe (a) and simvastatin (b).

Table 4 Ezetimibe plus simvastatin versus atorvastatin

Therapy	Dose	LDL reduction	Therapy	Dose	LDL reduction
Ezetimibe Study Trial Group
EZE/Sim	10/10 mg	46%	Simva	10 mg	31%
EZE/Sim	10/20 mg	51%	Simva	20 mg	35%
EZE/Sim	10/40 mg	55%	Simva	40 mg	42%
EZE/Sim	10/80 mg	61%	Simva	80 mg	46%
Ballantyne et al (2004)
EZE/Sim	10/10 mg	46%	Atorva	10 mg	37%
EZE/Sim	10/20 mg	50%	Atorva	20 mg	44%
EZE/Sim	10/40 mg	55%	Atorva	40 mg	49%
EZE/Sim	10/80 mg	59%	Atorva	80 mg	53%
Vytorin Versus Atorvastatin Study (VYVA)
EZE/Sim	10/10 mg	47%	Atorva	10 mg	36%
EZE/Sim	10/20 mg	51%	Atorva	20 mg	43%
EZE/Sim	10/40 mg	57%	Atorva	40 mg	48%
EZE/Sim	10/80 mg	59%	Atorva	80 mg	53%

Abbreviations: LDL-C, low-density lipoprotein cholesterol.

Table 5 Percent attainment of LDL-C goal <100 mg/dL with ezetimibe/simvastatin vs atorvastatin

Therapy	Dose	LDL-C goal	Therapy	Dose	LDL-C goal	p value
EZE/Sim	10/10 mg	78%	Atorva	10 mg	47%	<0.001
EZE/Sim	10/20 mg	82%	Atorva	20 mg	69%	<0.01
EZE/Sim	10/40 mg	90%	Atorva	40 mg	78%	<0.05
EZE/Sim	10/80 mg	91%	Atorva	80 mg	85%	ns
Percent attainment of LDL-C goal <70 mg/dL with ezetimibe/simvastatin vs atorvastatin

Therapy	Dose	LDL-C goal	Therapy	Dose	LDL-C goal	p value
EZE/Sim	10/10 mg	20%	Atorva	10 mg	6%	<0.01
EZE/Sim	10/20 mg	39%	Atorva	20 mg	17%	<0.001
EZE/Sim	10/40 mg	57%	Atorva	40 mg	23%	<0.001
EZE/Sim	10/80 mg	64%	Atorva	80 mg	36%	<0.001

Abbreviations: LDL-C, low-density lipoprotein cholesterol; ns, nonsignificant.

BallantyneCMBlazingMAKingTREfficacy and safety of ezetimibe co-administered with simvastatin compared with atorvastatin in adults with hypercholesterolemiaAm J Cardiol20049314879415194018

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