Effects of ezetimibe, a new cholesterol absorption inhibitor, on plasma lipids in patients with primary hypercholesterolemia

Knopp, Robert H.; Gitter, H.; Truitt, Tyler; Bays, Harold; Manion, Carl V.; Lipka, Leslie J.; LeBeaut, Alexandre; Suresh, Ramachandran; Yang, Bo; Veltri, Enrico P.

doi:10.1016/s0195-668x(02)00807-2

Cited by 360 publications

(67 citation statements)

References 12 publications

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“…The very significant decrease of triglycerides observed in our patients was due to fibrate action; it should however be noted that some studies on non-HIV patients found a limited, but statistically significant decrease of triglycerides during ezetimibe monotherapy [19,20]. We also observed a significant increase in HDL cholesterol, which has already been described during ezetimibe monotherapy in studies on non-HIV patients; this HDL increase has been connected to the greater increase in concentration of apolipoprotein A-I with ezetimibe compared to placebo [19–22]. …”

Section: Resultssupporting

confidence: 68%

“…Both efficacy and safety of ezetimibe monotherapy as well as of ezetimibe+statin coadministration have been widely demonstrated in dyslipidemic non-HIV patients [16–22]: ezetimibe monotherapy reduced LDL cholesterol by 17–20% compared with placebo, triglycerides levels also decreased significantly by 5% and HDL cholesterol increased by 2–3%. Furthermore, studies on HIV+ patients showed that ezetimibe is as effective as statin monotherapy in decreasing cholesterol, is well tolerated and does not interact with HAART [23–25].…”

Section: Introductionmentioning

confidence: 99%

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Dyslipidemia in HIV‐positive patients: a randomized, controlled, prospective study on ezetimibe+fenofibrate versus pravastatin monotherapy

Grandi

Nicolini

Rizzi

et al. 2014

Journal of the International AIDS Society

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IntroductionWe designed a randomized, controlled prospective study aimed at comparing efficacy and tolerability of ezetimibe+fenofibrate treatment versus pravastatin monotherapy in dyslipidemic HIV-positive (HIV+) patients treated with protease inhibitors (PIs).MethodsWe consecutively enrolled 42 HIV+ dyslipidemic patients on stable PIs therapy (LDL cholesterol >130 mg/dl or triglycerides 200–500 mg/dl with non-HDL cholesterol >160 mg/dl). After basal evaluation, patients were randomized to a six-month treatment with ezetimibe 10 mg/day+fenofibrate 200 mg/day or with pravastatin 40 mg/day. Both at the basal evaluation and after the six-month treatment, the patients underwent blood tests for lipid parameters, and muscle and liver enzymes.ResultsAt baseline, the two groups (21 patients each) were similar with regards to gender, age, BMI, blood pressure and virologic and metabolic parameters. After the six-month therapy, total cholesterol, LDL cholesterol and non-HDL cholesterol decreased significantly (p<0.01) in both groups. high-density lipoprotein (HDL) cholesterol increased (44±10 to 53±12 mg/dl, p<0.005) and triglycerides decreased (from 265±118 mg/dl to 149±37 mg/dl, p<0.001) in the ezetimibe+fenofibrate group, whereas both parameters remained unchanged in the pravastatin group. Mean values of creatine kinase (CK), alanine aminotransferase and aspartate aminotransferase were unchanged in both groups; only one patient in the pravastatin group stopped the treatment after two months, due to increased CK.ConclusionsIn dyslipidemic HIV+ patients on PI therapy, the association of ezetimibe+fenofibrate is more effective than pravastatin monotherapy in improving lipid profile and is also well tolerated.

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Section: Resultssupporting

confidence: 68%

Section: Introductionmentioning

confidence: 99%

Dyslipidemia in HIV‐positive patients: a randomized, controlled, prospective study on ezetimibe+fenofibrate versus pravastatin monotherapy

Grandi

Nicolini

Rizzi

et al. 2014

Journal of the International AIDS Society

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“…Ezetimibe (Zetia) is an FDA approved hypocholesterolemic drug that blocks cholesterol absorption from the intestine by interfering with the bona fide gut cholesterol transporter NPC1L1 107-109 . Inhibition of cholesterol absorption by ezetimibe also causes LDL receptor levels to increase, thereby facilitating removal of cholesterol from the circulation.…”

Section: Cholesterol Targeting and Prostate Healthmentioning

confidence: 99%

Cholesterol and benign prostate disease

Freeman

Solomon

2011

Differentiation

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The origins of benign prostatic diseases, such as benign prostatic hyperplasia (BPH) and chronic prostatitis/chronic pelvic pain syndrome (CP/CPPS), are poorly understood. Patients suffering from benign prostatic symptoms report a substantially reduced quality of life, and the relationship between benign prostate conditions and prostate cancer is uncertain. Epidemiologic data for BPH and CP/CPPS are limited, however an apparent association bet ween BPH symptoms and cardiovascular disease (CVD) has been consistently reported. The prostate synthesizes and stores large amounts of cholesterol and prostate tissues may be particularly sensitive to perturbations in cholesterol metabolism. Hypercholesterolemi, a major risk factor for CVD, is also a risk factor for BPH. Animal model and clinical trial findings suggest that agents that inhibit cholesterol absorption from the intestine, such as the class of compounds known as polyene macrolides, can reduce prostate gland size and improve lower urinary tract symptoms (LUTS). Observational studies indicate that cholesterol-lowering drugs reduce the risk of aggressive prostate cancer, while prostate cancer cell growth and survival pathways depend in part on cholesterol-sensitive biochemical mechanisms. Here we review the evidence that cholesterol metabolism plays a role in the incidence of benign prostate disease and we highlight possible therapeutic approaches based on this concept.

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“…Ezetimibe lowered LDL-C by 17-18% 1)2)3)4). However, LDL-C was reduced by 25-27% when ezetimibe was added to an on-going statin therapy 8)9)10)14).…”

Section: Discussionmentioning

confidence: 99%

“…Ezetimibe, an inhibitor of intestinal cholesterol absorption, lowers the low density lipoprotein-cholesterol (LDL-C) by 17-18% 1)2)3)4). However, ezetimibe elevates the activity of 3-hydroxy-3-methylglutaryl coenzyme A (HMG CoA) reductase resulting in the increase of cholesterol synthesis 5)6)7).…”

Section: Introductionmentioning

confidence: 99%

Influence of Previous Statin Therapy on Cholesterol-Lowering Effect of Ezetimibe

et al. 2014

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Background and ObjectivesThe inhibition of cholesterol absorption by ezetimibe increases cholesterol synthesis. The effect of inhibition of cholesterol synthesis on cholesterol absorption is controversial. The influence of these interactions on cholesterol levels is unknown. We investigated on the extent to which cholesterol levels were affected by the reaction of one pathway to the inhibition of the other pathway.Subjects and MethodsThis case-controlled study enrolled 198 patients who needed cholesterol-lowering drugs. Ezetimibe (10 mg) was administered to the patients with (n=58) and without on-going statin therapy (n=58). Simvastatin (20 mg) was administered to the patients treated with (n=41) and without ezetimibe (n=41).ResultsEzetimibe without statin lowered the total cholesterol by 13.3±8.8% (p<0.001) and the low density lipoprotein-cholesterol (LDL-C) by 18.7±15.3% (p<0.001). Ezetimibe added to statin decreased the total cholesterol by 21.1±7.7% (p<0.001) and the LDL-C by 29.9±12.6% (p<0.001). The total cholesterol and LDL-C were reduced more by ezetimibe in patients with statin therapy than in those without statin therapy (p<0.001 and p<0.001, respectively). The differences in the effect of simvastatin on total cholesterol and LDL-C between the patients with and without ezetimibe showed borderline significance (p=0.10 and p=0.055, respectively).ConclusionA prior inhibition of cholesterol synthesis by statin enhanced the effect of ezetimibe on total cholesterol and LDL-C by 7.8% and 11.2%, respectively. This finding suggests that ezetimibe increased cholesterol synthesis, resulting in a significant elevation of cholesterol levels.

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Effects of ezetimibe, a new cholesterol absorption inhibitor, on plasma lipids in patients with primary hypercholesterolemia

Abstract: Ezetimibe, which significantly reduces LDL-C and favorably affects other lipid variables, may provide a well tolerated and effective new option for lipid management in the future.

Cited by 360 publications

References 12 publications

Dyslipidemia in HIV‐positive patients: a randomized, controlled, prospective study on ezetimibe+fenofibrate versus pravastatin monotherapy

Dyslipidemia in HIV‐positive patients: a randomized, controlled, prospective study on ezetimibe+fenofibrate versus pravastatin monotherapy

Cholesterol and benign prostate disease

Influence of Previous Statin Therapy on Cholesterol-Lowering Effect of Ezetimibe

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