Evaluation of Food Effects on the Oral Pharmacokinetics of Rosuvastatin

Rosuvastatin is commonly prescribed for the treatment of hypercholesterolemia and exerts its effect through targeted accumulation in the liver. Current United States and Canadian dosing guidelines indicate no preference for fed or fasted rosuvastatin administration. In this study, we demonstrate for the first time that concomitant administration with food substantially reduced mean plasma rosuvastatin exposure in healthy Canadian East Asian and Caucasian subjects. In mice lower plasma level was also noted with food 2 hours after an oral rosuvastatin dose, while liver concentration was unaffected. Moreover, through retrospective analysis of rosuvastatin patient data, we conclude that taking an oral dose with food as opposed to on an empty stomach, does not significantly affect the cholesterol-lowering capacity of rosuvastatin. Since a common adverse event noted with statin therapy is muscle pain/damage associated with high circulating statin levels, our findings have the potential to serve as a novel and simple strategy for mitigating statin myopathy risk.

Name thesis:degree_name

M Sc

Discipline thesis:degree_discipline

Physiology and Pharmacology

Grantor dc:publisher

The University of Western Ontario

Year dc:date.issued

2016

Author dc:creator

• McLean, Cheynne C.

Advisor dc:contributor.advisor

• Richard B. Kim

• rosuvastatin
• HMG-CoA reductase inhibitors
• oral pharmacokinetics
• food effect
• hepatic uptake transport
• drug transporter pharmacogenetics

Language dc:language.iso

en_ca

Handle dc:identifier.uri

https://hdl.handle.net/20.500.14721/33763

OAI identifier oai:identifier

oai:uwo.scholaris.ca:20.500.14721/33763