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•Key
Point: Rosuvastatin is not metabolized by the CYP450 3A4 system, has no
clinically significant
metabolites, and is relatively hydrophilic, unlike atorvastatin and simvastatin.
•The
pharmacokinetic profiles of rosuvastatin, 3 other marketed statins, and
ezetimibe are shown on this
slide1-5
•Atorvastatin
and simvastatin are metabolized by the CYP450 3A4 pathway, have
clinically significant
metabolites, and are relatively lipophilic2-3
•In
contrast, rosuvastatin and pravastatin are not metabolized by CYP450
3A4, do not have clinically
significant metabolites, and are relatively hydrophilic1,4
•Because
it is known that the risk of myopathy increases with the dose of the
statin, factors that increase
the concentration of statin in muscle tissue may enhance its potential for myotoxic effects6-7
•Rosuvastatin,
pravastatin, atorvastatin, and simvastatin are hepatoselective and
cleared by the liver or by
the liver and the kidney1-4 |