Simvastatin: Difference between revisions
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* As with other statins which are metabolized by the CYP3A4 liver enzyme, the pharmacokinetics of Simvastatin are altered significantly by consumption of grapefruit juice. C<sub>max</sub> values of Simvastatin (40mg doses) increased by nearly 300%, t<sub>max</sub> increased 100%,, the half life decreased by 50%, and AUC increased by nearly 300%. These results are even more pronounced for active Simvastatin metabolites. <ref>DOI: 10.1111/j.1365-2125.2004.02095.x</ref> | * As with other statins which are metabolized by the CYP3A4 liver enzyme, the pharmacokinetics of Simvastatin are altered significantly by consumption of grapefruit juice. C<sub>max</sub> values of Simvastatin (40mg doses) increased by nearly 300%, t<sub>max</sub> increased 100%,, the half life decreased by 50%, and AUC increased by nearly 300%. These results are even more pronounced for active Simvastatin metabolites. <ref>DOI: 10.1111/j.1365-2125.2004.02095.x</ref> | ||
===The Jist=== | ===The Jist=== | ||
Along with the other statins, Simvastatin works well and is quite safe. Depending upon the patient, Simvastatin can be the most effective statin at reducing LDL, but can also have dramatically reduced efficacy. Since Simvastatin is the most powerful HMGR inhibitor with an IC<sub>50</sub> of 66nM, this allows for decreased long-term exposure to the drug (lower AUC) and negates the short half life of Simvastatin compared to Atorvastatin and Rosuvastatin. While on patent it was one of the best selling drugs in the world. To maintain its market share after losing patent protection, Merck dramatically reduced the price of Zocor, making the drug particularly attractive to US Health Insurers looking to reduce costs. | |||
===References=== | ===References=== | ||
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