Pharmacodynamic interaction between ezetimibe and rosuvastatin

Kosoglou, Teddy; Statkevich, Paul; Yang, Bo; Suresh, Ramachandran; Zhu, Yali; Boutros, Tanya; Maxwell, Stephen E.; Tiessen, Renger G.; Cutler, David L.

doi:10.1185/030079904125004213

Cited by 61 publications

(38 citation statements)

References 39 publications

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“…Likewise, coadministration of ezetimibe with rosuvastatin is well tolerated in patients with hypercholesterolemia (Kosoglou et al, 2004). In contrast, no interactions of dalcetrapib, an inhibitor of cholesteryl ester transfer protein, with pravastatin, rosuvastatin, or simvastatin were found in healthy men (Derks et al, 2010).…”

mentioning

confidence: 85%

Pharmacological Actions of Statins: A Critical Appraisal in the Management of Cancer

Gazzerro

Proto²,

Gangemi³

et al. 2011

Pharmacol Rev

401

370

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mentioning

confidence: 85%

Pharmacological Actions of Statins: A Critical Appraisal in the Management of Cancer

Gazzerro

Proto²,

Gangemi³

et al. 2011

Pharmacol Rev

401

370

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“…Capuzzi et al [27•] documented that the combination of 10 to 40 mg/d of rosuvastatin and extended-release niacin at 500 to 2000 mg/d was very effective in reducing triglyceride and LDL cholesterol, and as expected produced very striking increases in HDL cholesterol and apoA-I in patients with combined hyperlipidemia. Kosoglou et al [28] documented that the addition of 10 mg/d of ezetimibe to 10 mg/d of rosuvastatin provided additional LDL cholesterol lowering of 16.4%, above and beyond the 44.9% lowering achieved with rosuvastatin alone, making the total LDL cholesterol reduction achieved 61.4% [28]. There was no additional effect of ezetimibe on lowering triglycerides or raising HDL cholesterol [28].…”

Section: Studies On Subgroups Of Patientsmentioning

confidence: 95%

The effects of statins on high-density lipoproteins

Schaefer

Asztalos²

2006

Curr Atheroscler Rep

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Statins inhibit cholesterol synthesis and are effective in lowering total cholesterol levels in plasma or serum due to reductions in low-density lipoprotein and very low-density lipoproteins, as well as reducing progression of coronary atherosclerosis, coronary heart disease, and stroke morbidity and mortality. These agents also modestly raise levels of high-density lipoprotein (HDL) cholesterol and its major protein, apolipoprotein (apo) A-I. The more effective statins can also raise the levels of large alpha-1 HDL particles as assessed by two-dimensional gel electrophoresis. High levels of these particles promote reverse cholesterol transport and protect against coronary heart disease and progression of coronary atherosclerosis. The mechanism whereby statins alter HDL and its subspecies appears to be due to reduction of triglyceride-rich lipoproteins, with a secondary decrease in cholesteryl ester transfer protein activity, and less transfer of HDL cholesterol to triglyceride-rich lipoprotein acceptor particles. Increasingly, statins will be combined with other agents such as ezetimibe, fibrates, niacin, and cholesteryl ester transfer protein inhibitors to optimize the entire lipoprotein profile to alter not only low-density lipoprotein, but also HDL, triglycerides, lipoprotein(a), and C-reactive protein, and also to reduce cardiovascular morbidity and mortality.

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“…[13] There is no known significant PK drug interaction between rosuvastatin and ezetimibe. [14] FDCs are known to improve compliance in those patients with chronic disease. [8] Primary objective of the study was to compare PK profile between two formulations: FDC of rosuvastatin 20 mg / ezetimibe 10 mg and concurrent administration of corresponding individual tablets.…”

Section: Discussionmentioning

confidence: 99%

Pharmacokinetics of fixed-dose combination of rosuvastatin 20 mg and ezetimibe 10 mg compared to concurrent administration of individual tablets in healthy Korean subjects

Hwang

Park

Lee

et al. 2018

Transl Clin Pharmacol

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This study aimed to compare the pharmacokinetics of fixed-dose combination (FDC) tablet of rosuvastatin 20 mg/ezetimibe 10 mg with that of concurrent administration of individual rosuvastatin 20 mg tablet and ezetimibe 10 mg tablet in healthy subjects. A randomized, open label, single-dose, two-way crossover study was conducted. Subjects randomly received test formulation (FDC tablet of rosuvastatin 20 mg/ezetimibe 10 mg) or reference formulation (co-administration of rosuvastatin 20 mg tablet and ezetimibe 10 mg tablet). After 2 weeks of washout, subjects received the other treatment. Blood samples were collected up to 72 hours post-dose in each period. Plasma concentrations of rosuvastatin, ezetimibe and total ezetimibe (ezetimibe + ezetimibe glucuronide) were analyzed by liquid chromatography-tandem mass spectrometry (LC/MS/MS). The geometric mean ratio (GMR) of C max and AUC last (90% confidence interval, CI) for rosuvastatin was 1.036 (0.979-1.096) and 1.024 (0.981-1.070), respectively. The corresponding values for ezetimibe were 0.963 (0.888-1.043) and 1.021 (0.969-1.074), respectively. The corresponding values for total ezetimibe were 0.886 (0.835-0.940) and 0.983 (0.946-1.022), respectively. FDC tablet containing rosuvastatin 20 mg and ezetimibe 10 mg is bioequivalent to the co-administration of commercially available individual tablets of rosuvastatin and ezetimibe as GMR with 90% CI of C max and AUC last of rosuvastatin, ezetimibe and total ezetimibe were contained within conventionally accepted bioequivalence criteria.

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Pharmacodynamic interaction between ezetimibe and rosuvastatin

Abstract: Co-administration of ezetimibe 10 mg with rosuvastatin 10 mg daily caused a significant incremental reduction in LDL-C compared with rosuvastatin alone. Moreover, co-administering ezetimibe and rosuvastatin was well tolerated in patients with hypercholesterolemia.

Cited by 61 publications

References 39 publications

Pharmacological Actions of Statins: A Critical Appraisal in the Management of Cancer

Pharmacological Actions of Statins: A Critical Appraisal in the Management of Cancer

The effects of statins on high-density lipoproteins

Pharmacokinetics of fixed-dose combination of rosuvastatin 20 mg and ezetimibe 10 mg compared to concurrent administration of individual tablets in healthy Korean subjects

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