Question - Why is the use of the HMG-CoA reductase inhibitors simvastatin and lovastatin contraindicated for patients taking protease inhibitors (PI)?
Answer- The cited article emphasizes that “simvastatin and lovastatin are exclusively metabolized by CYP3A, and because most PIs are potent inhibitors of CYP3A4, their concentrations are significantly increased when co-administered with a PI. As such, lovastatin and simvastatin are contraindicated in patients taking PIs.” These authors go on to state “Furthermore, co-administration of simvastatin and boosted saquinavir resulted in a 31.59-fold increase in the area under the curve (AUC) of simvastatin. When this FDA-labeled contraindicated combination is not recognized and corrected, devastating consequences (e.g. fatal rhabdomyolysis) can result.” (Stolbach A et al. A review if the toxicity of HIV medications II: Interactions with drugs and complementary and alternative medicine products. 2015 J Med Toxicol. 11:326-341)