Ezetimibe-Statin Combination Therapy: Efficacy and Safety as Compared With Statin Monotherapy

Nußbaumer, Barbara; Glechner, Anna; Kaminski‐Hartenthaler, Angela; Mahlknecht, Peter; Gartlehner, Gerald

doi:10.3238/arztebl.2016.0445

Cited by 16 publications

(12 citation statements)

References 33 publications

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“…The recommended ezetimibe dosage is 10 mg daily, with or without food, taken either 2 hours before or 4 hours after bile acid sequestrants (BAS) if used in combination. 11 , 12 When administered as monotherapy or coadministered with statins, timing of administration has no effect on their potency. This was confirmed by the study of Hyung Sik Yoon, who tested the therapeutic efficacy and safety of a fixed-dose combination of ezetimibe 10 mg and simvastatin 20 mg, in terms of morning versus evening administration.…”

Section: Resultsmentioning

confidence: 99%

Adding ezetimibe to statin therapy: latest evidence and clinical implications

Vavlukis¹,

Vavlukis²

2018

DIC

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BackgroundStatins are the hypolipemic treatment of choice for hyperlipidemia with confirmed atherosclerotic cardiovascular disease (ASCVD) protective effect, proven even in normolipemic patients. But in rare situations, even with a high-dose treatment regimen, or maximally tolerated statin dose treatment, treatment targets of low-density lipoprotein cholesterol (LDL-C), according to the risk profile of the patient, cannot be achieved. Combination therapy with ezetimibe is an effective treatment choice, as it is one of the few hypolipemic drugs with proven ASCVD protective effect.AimIn this review, we address the question of therapeutic efficacy and safety of ezetimibe in combination therapy with statins, as expressed through its hypolipemic and vasoprotective effects and its potential side effects.MethodsWe conducted a literature review of English articles through PubMed, PubMed Central, and Cochrane for randomized clinical trials, retrospective analyses, meta-analyses, and review articles by using key words: ezetimibe, statins, combination therapy, adverse effects. We analyzed data on ezetimibe–statin combination therapy in terms of hypolipemic efficacy, ASCVD risk reduction, and adverse effects.ResultsStatins have been proven to be very effective in reducing ASCVD risk, with no apparent threshold at which LDL-C lowering is not associated with reduced risk. Yet, a significant on-treatment residual risk of major cardiovascular (CV) events still exists according to meta-analyses of statin trials. Findings like this point to the unmet needs of the patients on statin treatment. The unmet needs in terms of LDL-C targets and ASCVD risk reduction raise the question of statin combination therapy. Ezetimibe is a cholesterol-lowering drug from the class of cholesterol absorption inhibitors, with the potency to decrease LDL-C by about 10–18% and Apo B by 11–16%, while in combination therapy with statins, an additional LDL-C lowering of 25% or total LDL-C lowering of 34–61% is observed. The effects on LDL-C and other lipoprotein (LP) fractions are translated by ASCVD risk reduction. Ezetimibe is one of the few hypolipemic medications that leads to additional ASCVD risk reduction when added to statin therapy. Present data on ezetimibe support the existence of pleotropic anti-inflammatory and antioxidative effects, in addition to its hypolipemic effect, which are responsible for this added ASCVD risk reduction on top of statin monotherapy. Ezetimibe, in combination therapy with a maximal or maximally tolerated statin therapy, is used in patients who fail to achieve target LDL-C levels with statin monotherapy. In combination with low-to-moderate statin dose treatment, or with second- or third-line statins, ezetimibe is used in situations of statin-associated muscle symptoms. The combination therapy is relatively safe.ConclusionEzetimibe add-on to statin combination therapy is an effective treatment option that leads to additional LDL-C lowering – recommended in situations where, with a maximal or maximally tolerated statin mon...

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Section: Resultsmentioning

confidence: 99%

Adding ezetimibe to statin therapy: latest evidence and clinical implications

Vavlukis¹,

Vavlukis²

2018

DIC

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“…Therefore, combination-drugs has become a promising direction to improve clinical efficacy. For instance, ezetimibe-statin combination is a more efficacy and safe therapy in clinical treating ( Nußbaumer et al, 2016 ). Unfortunately, numerous adverse effects are still a matter of concern ( Ferri and Corsini, 2020 ).…”

Section: Discussionmentioning

confidence: 99%

Linderae Radix Ethanol Extract Alleviates Diet-Induced Hyperlipidemia by Regulating Bile Acid Metabolism Through gut Microbiota

et al. 2021

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Hyperlipidemia is a common metabolic disorder and regarded as one of the main risk factors for cardiovascular disease. The gut microbiota has been identified as a potential contributor to hyperlipidemia as it can greatly regulate bile acid metabolism. Linderae radix is a natural medicine widely used in the treatment of a variety of diseases and is also a common drug for hyperlipidemia. Recently, the lipid-lowering effect of Linderae radix are receiving increasing attention but the underlying mechanism remains unknown. The study aimed to investigate the effects of Linderae radix ethanol extract (LREE) on gut microbiota in rats with hyperlipidemia syndrome. We established a hyperlipidemia rat model using a high-fat diet and used LREE as the intervention. Blood lipid levels and pathological examination were measured to assess the effects of LREE on hyperlipidemia. The gut microbiota was determined by 16s rDNA sequencing and the bile acid metabolism-related proteins were detected by western blot to discover the underlying correlations. The results show that LREE lowered TC, TG, and LDL levels effectively, and it also alleviated liver injury by reducing ALT and AST activity. Meanwhile, LREE improved gut microbiota disturbance caused by HFD via increasing intestinal microbiota diversity and changing the abundance of the Firmicutes, Bacteroidetes, and Actinobacteria. In addition, LREE can increase bile acid reabsorption and promote fecal excretion through farnesoid X receptor (FXR), apical sodium-dependent bile acid transporter (ASBT), organic solute transporter alpha (OST-α), and cytochrome P450 family 7 Subfamily A Member 1 (CYP7A1) thus restoring abnormal bile acid metabolism caused by hyperlipidemia.

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“…Interestingly, this pathway produces cholesterol and other isoprenoids, such as coenzyme Q 10 (CoQ) [22]. In addition to statins, other therapeutic strategies have been developed, for instance using inhibitors of the N-terminal Niemann-Pick C1-like protein 1 (NPC1L1) receptor, which is located on the luminal surface of enterocytes and is responsible for cholesterol uptake [23]. Recently, innovative therapies using not only chemical drugs, but also monoclonal antibodies against certain proteins, such as the proprotein convertase subtilisin/kexin type 9 (PCSK9) have been utilized with promising results.…”

Section: Atherosclerosis Treatmentmentioning

confidence: 99%

Atherosclerosis and Coenzyme Q10

Suárez-Rivero

Pastor-Maldonado

Mata

et al. 2019

IJMS

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Atherosclerosis is the most common cause of cardiac deaths worldwide. Classically, atherosclerosis has been explained as a simple arterial lipid deposition with concomitant loss of vascular elasticity. Eventually, this condition can lead to consequent blood flow reduction through the affected vessel. However, numerous studies have demonstrated that more factors than lipid accumulation are involved in arterial damage at the cellular level, such as inflammation, autophagy impairment, mitochondrial dysfunction, and/or free-radical overproduction. In order to consider the correction of all of these pathological changes, new approaches in atherosclerosis treatment are necessary. Ubiquinone or coenzyme Q10 is a multifunctional molecule that could theoretically revert most of the cellular alterations found in atherosclerosis, such as cholesterol biosynthesis dysregulation, impaired autophagy flux and mitochondrial dysfunction thanks to its redox and signaling properties. In this review, we will show the latest advances in the knowledge of the relationships between coenzyme Q10 and atherosclerosis. In addition, as atherosclerosis phenotype is closely related to aging, it is reasonable to believe that coenzyme Q10 supplementation could be beneficial for both conditions.

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Ezetimibe-Statin Combination Therapy: Efficacy and Safety as Compared With Statin Monotherapy

Cited by 16 publications

References 33 publications

Adding ezetimibe to statin therapy: latest evidence and clinical implications

Adding ezetimibe to statin therapy: latest evidence and clinical implications

Linderae Radix Ethanol Extract Alleviates Diet-Induced Hyperlipidemia by Regulating Bile Acid Metabolism Through gut Microbiota

Atherosclerosis and Coenzyme Q10

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