Fmk

In its racemic form, fluvastatin is approximately four times more potent in vitro than lovastatin, while the pure (3R,5S) enantiomer is approximately 10-fold more potent than lovastatin in biochemical assays. As a hydroxy-acid analog, fluvastatin has intermediate physiochemical properties, being about twice as hydrophilic as lovastatin and about 40 times more lipophilic than pravastatin.62 In contrast to other statins, orally administered fluvastatin is nearly completely absorbed. However, the high protein binding (99%) of fluvastatin dictates that the overall plasma-free drug concentration is very low and thus limits its exposure to peripheral tissue. The metabolism of fluvastatin is mediated by CYP2C9 and not by CYP3A4, and as a result has a lower potential for drug-drug interactions with CYP3A4 inhibitors. Oral administration of fluvastatin dose-dependently reduced plasma VLDLc and LDLc concentrations in a variety of animal species at daily doses between 2 and 50 mg kg_ 1.64,65 Fluvastatin sodium 5 was approved for human use in Europe in 1995 and was launched in the US in 2000.

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