open access

Vol 10, No 6 (2015)
Review Papers
Published online: 2016-01-11
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When statin treatment is not enough — statin/ezetimibe therapy for hypercholesterolaemia

Katarzyna Starzyk, Beata Wożakowska-Kapłon
DOI: 10.5603/FC.2015.0081
·
Folia Cardiologica 2015;10(6):428-437.

open access

Vol 10, No 6 (2015)
Review Papers
Published online: 2016-01-11

Abstract

Hypercholesterolaemia was the most frequent cardiovascular (CV) risk factor in Poland both in 2002 and 2011, and was diagnosed in 62% of Poles (18 million). Only 8% of patients with hypercholesterolaemia received effective treatment (consistent with current guidelines). According to Polish experts, insufficient effectiveness in achieving treatment goals is caused by using too low doses of statins, choosing the drug with low lipid-lowering activity, short treatment duration, unjustified treatment cessation, and too rare use of combination therapy. Nonpharmacological treatment related to lifestyle modifications play a key role in the management of hypercholesterolaemia. In patients who fail to achieve target low-density lipoprotein (LDL) level despite lifestyle modifications, the drugs of choice are statins. Thus, the second-line treatment of hypercholesterolaemia consists in reducing intestinal absorption of cholesterol. Ezetimibe proved to reduce cholesterol absorption by 50%, leading to increased expression (density) of receptors for LDL cholesterol on the surface of hepatocyte — mechanism of action similar to that of statins. Its metabolite, ezetimibe glucuronate, is more active that the drug itself; therefore, its halftime is 22 hours. Ezetimibe used as monotherapy reduces the level of LDL cholesterol by 18% and triglycerides — by 8%, whereas adding a statin results in additional LDL cholesterol reduction by 14–25%, and triglycerides — by 7.5–14% and high-density lipoprotein (HDL) level increase by 2–3%. Conclusions from many randomized trials suggest the use of combination therapy with a statin and ezetimibe rather than increasing the dose of stain used as monotherapy. Optimisation of lipid-lowering therapy and persistence of the treatment result in cardiovascular risk reduction which is of particular importance in high and very high risk patients.

Abstract

Hypercholesterolaemia was the most frequent cardiovascular (CV) risk factor in Poland both in 2002 and 2011, and was diagnosed in 62% of Poles (18 million). Only 8% of patients with hypercholesterolaemia received effective treatment (consistent with current guidelines). According to Polish experts, insufficient effectiveness in achieving treatment goals is caused by using too low doses of statins, choosing the drug with low lipid-lowering activity, short treatment duration, unjustified treatment cessation, and too rare use of combination therapy. Nonpharmacological treatment related to lifestyle modifications play a key role in the management of hypercholesterolaemia. In patients who fail to achieve target low-density lipoprotein (LDL) level despite lifestyle modifications, the drugs of choice are statins. Thus, the second-line treatment of hypercholesterolaemia consists in reducing intestinal absorption of cholesterol. Ezetimibe proved to reduce cholesterol absorption by 50%, leading to increased expression (density) of receptors for LDL cholesterol on the surface of hepatocyte — mechanism of action similar to that of statins. Its metabolite, ezetimibe glucuronate, is more active that the drug itself; therefore, its halftime is 22 hours. Ezetimibe used as monotherapy reduces the level of LDL cholesterol by 18% and triglycerides — by 8%, whereas adding a statin results in additional LDL cholesterol reduction by 14–25%, and triglycerides — by 7.5–14% and high-density lipoprotein (HDL) level increase by 2–3%. Conclusions from many randomized trials suggest the use of combination therapy with a statin and ezetimibe rather than increasing the dose of stain used as monotherapy. Optimisation of lipid-lowering therapy and persistence of the treatment result in cardiovascular risk reduction which is of particular importance in high and very high risk patients.

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Keywords

hypercholesterolaemia, combination therapy, ezetimibe

About this article
Title

When statin treatment is not enough — statin/ezetimibe therapy for hypercholesterolaemia

Journal

Folia Cardiologica

Issue

Vol 10, No 6 (2015)

Pages

428-437

Published online

2016-01-11

DOI

10.5603/FC.2015.0081

Bibliographic record

Folia Cardiologica 2015;10(6):428-437.

Keywords

hypercholesterolaemia
combination therapy
ezetimibe

Authors

Katarzyna Starzyk
Beata Wożakowska-Kapłon

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