Many HMG-CoA reductase inhibitors (statins) and some ARV drugs are metabolized by the same cytochrome P450 isoenzyme CYP3A4. Inhibition of CYP3A4 may result in excessively high levels of statins.1
|Drug class||Drug||Dose (mg QD)||Use with PI/ritonavir||Use with NNRTI|
|Statin||atorvastatin||10–80||Start with low dose* (max. 40 mg)||Consider higher dose†|
|fluvastatin||20–80||Consider higher dose†||Consider higher dose†|
|pravastatin||20–80||Consider higher dose†‡||Consider higher dose†|
|rosuvastatin||5-40||Start with low dose* (max. 20 mg)||Start with low dose*|
|simvastatin||10-40||Contraindicated||Consider higher dose†|
|Cholesterol uptake ↓||ezetimibe||10||No known drug-drug interactions with ART|
*The ART drug may inhibit the excretion of the statin (statin toxicity, ↓ dose) †The ART drug may induce the excretion of the statin (=less effect of statin, ↑ dose gradually to achieve expected benefit) ‡Exception: if used with darunavir/ritonavir, start with lower dose of pravastatin NNRTI = non-nucleoside reverse transcriptase inhibitor. Signs of statin toxicity include: gastrointestinal symptoms, headache, insomnia, rhabdomyolysis (rare), toxic hepatitis and myalgia.
Adapted with permission from the European AIDS Clinical Society Guidelines. Version 6.0.
The use of bile acid sequestrants is not recommended as they are thought to increase triglyceride levels and their effects on the absorption of ARV drugs have not been studied.3
For further information on drug-drug interactions: