Effectiveness and Safety of Ezetimibe Added to Statin Therapy in Patients with Primary Dyslipidaemia not Achieving the LDL-C Treatment Goal on Statin Monotherapy

Carlos A. González; Alberto F. Rubio-Guerra; Abel Pavía; Francisco J. Redding; José L. Cervantes; José L. Zacarías; Rubén Yza; Jaime Carranza; Pedro Fernández; Enrique Morales; Francisco J. Robles; José L. Leyva; Leticia Rodríguez


Clin Drug Invest. 2007;27(5):333-337. 

In This Article

Abstract and Introduction

Background and Objective: Elevated serum low-density lipoprotein cholesterol (LDL-C) is a major cardiovascular risk factor. This study aimed to determine the efficacy and safety of co-administration of the cholesterol absorption inhibitor ezetimibe with an HMG-CoA reductase inhibitor (statin) in the treatment of Mexican patients with dyslipidaemia who had not attained the LDL-C treatment goal with statin monotherapy.
Material and Methods: We studied 256 patients with elevated serum LDL-C (as defined by the US National Cholesterol Education Program Adult Treatment Panel III guidelines) despite statin therapy. All patients had lipid profiles performed at baseline and after 6–8 weeks of treatment with statin therapy plus ezetimibe 10 mg/day for 6–8 weeks.
Results: Addition of ezetimibe to statin treatment reduced mean serum LDL-C levels significantly (from 160 ± 42.8 to 100 ± 36 mg/dL; p < 0.001) after 6–8 weeks of treatment, with 61.7% of patients achieving LDL-C values below the goal established according to their coronary risk group. Serum LDL-C goals were achieved at the end of the study in 88.2% of the low-risk coronary group, 75.7% of the moderate-risk group and 47.8% of the high-risk group. Ezetimibe was well tolerated; no hepatic or muscle-related adverse events were observed.
Conclusion: Addition of ezetimibe to statin treatment was both efficacious and safe when used for further reduction of serum LDL-C in dyslipidaemic patients who had not reached their LDL-C treatment goal while taking statin monotherapy.

Dyslipidaemia is one of the main risk factors for the development of ischaemic heart disease. Indeed, there is a direct relationship between serum low-density cholesterol (LDL-C) levels and cardiovascular risk. This relationship is linear, such that a reduction in serum LDL-C cholesterol levels is directly related to a proportional reduction in cardiovascular risk.[1]

According to the recent National Health Survey conducted in Mexico, 43.3% of the Mexican population has elevated serum LDL-C cholesterol,[2] and most of these patients have additional cardiovascular risk factors.

Several clinical studies have demonstrated that a 25–35% reduction in serum LDL-C levels as a result of HMG-CoA reductase inhibitor (statin) treatment is associated with a decrease (23–37%) in cardiovascular mortality. Furthermore, a 1 mmol/L reduction in serum LDL-C leads to a 24% decrease in deaths in subjects with or without coronary artery disease, regardless of their LDL-C level at baseline.[3,4]

Despite the proven efficacy of statin therapy, not all patients taking statins reach the treatment goal specified for their coronary risk group by the National Cholesterol Education Program (NCEP) Adult Treatment Panel III (ATP III).[1] This translates into a need to either use higher dosages of statins, which might lead to a greater incidence of adverse effects (e.g. elevation of liver enzymes, muscle-related adverse events), or to add other lipid-lowering agents to statin therapy, which could lead to greater drug intolerance or other adverse effects.[1,5]

Ezetimibe is a drug that inhibits intestinal absorption of cholesterol at the brush border level of the enterocyte. In phase III monotherapy trials, ezetimibe has demonstrated a 17–20% reduction in serum LDL-C levels in humans.[6] Several studies have demonstrated the usefulness of ezetimibe added to statin therapy for reducing serum LDL-C levels, thereby achieving greater reductions than those obtained with use of statins alone, with no increase in incidence of adverse events.[7] The lipid-lowering effect of this combination extends to high-risk patients, in whom co-administration of ezetimibe with a statin allowed more patients to reach their serum LDL-C target of <100 mg/dL.[8,9]

The objective of the present study was to determine the therapeutic efficacy and safety of adding ezetimibe to statin treatment in a dyslipidaemic Mexican population who had not attained their NCEP ATP III serum LDL-C goals while taking statin monotherapy.


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