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Hydrophilic vs. Lipophilic Statins

The objectives of this presentation are to discuss the differences between hydrophilic and lipophilic statins and to highlight the clinical findings on the use of each statin type. Moreover, we will review the use of pitavastatin and its advantages given that it is the least lipophilic statin. Statins are spread out across a spectrum from most hydrophilic to most lipophilic. As you can see in this slide, Rosuvastatin and Pravastatin are the only two statins which are hydrophilic. On the other hand, Pitavastatin, Fluvastatin, Atorvastatin, Lovastatin and Simvastatin are lipophilic with Simvastatin being the most lipophilic and Pitavastatin being the least lipophilic. The main differences between hydrophilic statins and lipophilic statins are highlighted here. Hydrophilic statins are water-soluble, thus requiring active transport to be transported through cell membranes. Moreover, they are liver specific and display more active renal secretion. Lipophilic statins are fat soluble and thus pass through cell membrane more readily through passive diffusion. They are also widely distributed across different tissues and are mainly excreted by the liver. You will also note that all lipophilic statins, with Pitavastatin as the exception, are metabolized through the CYP450 enzymes. Clinical studies have compared hydrophilic to lipophilic statins in terms of their efficacy. A meta-analysis of 8 randomized control trials have shown similar efficacy of both statin categories in Coronary Artery Disease patients. Another study has also shown that the 1-year outcomes of hydrophilic and lipophilic statins are similar in patients with acute myocardial infarction. Studies investigating the effects of statins on liver function have shown that high-dose hydrophilic statins significantly increase the incidence of transaminase elevation and liver toxicity. On the other hand, high-dose lipophilic statins have been associated with increased risk of CK elevation. Lipophilic statins may have adverse metabolic consequences. Pitavastatin was first introduced in Japan in 2003. It was then approved in the United States by the FDA as pitavastatin calcium in 2009. The pitavastatin molecule has a unique structure which contributes to a high affinity for HMG-CoA reductase, has effects on LDL-C and HDL-C and has a reduced potential for certain drug to drug interactions  Pitavastatin is the least lipophilic statin and this may provide an advantage for the following reasons. First, Pitavastatin has an adequate half-life allowing this statin to maintain continual HMG-CoA Reductase inhibition using a practical dosing schedule. Pitavastatin also has been shown to raise adiponectin levels which consequently lowers insulin resistance and improves insulin secretion. Pitavastatin shares advantages with statins from both hydrophilic and lipophilic statin families including: Reducing LDL-C and increasing HDL-C levels as well as reducing the potential for certain drug-drug interactions. It is also important to note that the myalgia rates with pitavastatin at the highest dose of 4mg are only 3.1%