Abstract Pitavastatin is an HMG-CoA reductase inhibitor that significantly reduces the plasma levels of total cholesterol, LDL-C and triglycerides, while also causing modest elevation of the plasma high-density cholesterol (HDL-C) level. This statin is minimally metabolized by the cytochrome P-450 (CYP) isozymes; it is glucuronized and converted to the inactive lactone form, which is also minimally metabolized by human hepatic microsomes; therefore, it is associated with a low frequency of drug interactions. Pitavastatin has also been shown to have various pleiotropic effects on platelets, monocytes/macrophages and endothelial cells. In addition, a new effect of pitavastatin of increasing the serum for adiponectin level has been reported recently. Pitavastatin has been reported to be associated with a lower frequency of adverse drug effects such as hepatic dysfunction and rhabdomyolysis, therefore, it may be judged as one of the safer among the strong statins. Several clinical trials of pitavastatin have been conducted. At present, its evaluation in actual clinical use by clinicians around the world is underway. Pitavastatin is an effective and safe drug for patients with hypercholesterolemia.

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