Atorvastatin excretion

Lactation Lovastatin and atorvastatin are excreted in the milk of rats atorvastatin is likely to be excreted in breast milk it is not known whether lovastatin, rosuvastatin, and simvastatin are excreted in breast milk a small amount of pravastatin is excreted in breast milk fluvastatin is present in breast milk in a 2 1 ratio (milk plasma). 

Atorvastatin and its metabolites are primarily eliminated in the bile, and the drug does not undergo any enterohepatic circulation. The mean plasma elimination half-life of atorvastatin is approximately 14 h, but the half-life of its inhibitory activity for HMG-CoA reductase is 20-30 h due to the contribution from the active metabolites. Less than 2% of a dose of atorvastatin is excreted in urine following oral administration [5, 34]. 

It s apparent that CYPs are involved in the metabolism of all but one, Plavix (clopido-grel), and even for that compound they re important downstream, after initial hydrolysis of the ester. What s not apparent from the figure is that metabolism isn t always something that limits drug effectiveness. Some drugs like valsartan are mostly excreted unchanged, while for others, like the top-seller Lipitor (atorvastatin) metabolism affords compounds that are still active. In Lipitor s case, active metabolites are said to account for 70% of the pharmacodynamic (PD) effect the drug produces. Much more worrisome would be reactive (electrophilic) metabolites that make for toxicity or metabolites that affect GYP expression or function. 

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