|
|
 |
|
Agent
|
Considerations
|
Lovastatin
(Mevacor®)
Simvastatin (Zocor®) |
Extensively
metabolized by CYP3A4; toxicity likely when combined with PIs. |
| Fluvastatin
(Lescol®) |
Metabolized
by CYP2C9; interaction with nelfinavir likely.
|
Cerivastatin
(Baycol®)
|
Newest
agent; relatively limited published data on drug interactions.
May have low likelihood for interactions.
|
| Atorvastatin
(Lipitor®) |
Some
CYP3A4 metabolism; small amount of anecdotal and research experience
in HIV. Modest increases in AUC when coadministered with ritonavir-saquinavir.
|
Pravastatin
(Pravachol®)
|
No
significant p450 interactions; primarily renal excretion. Minimally
decreased AUC when coadministered with ritonavir-saquinavir.
|
Dube MP et al. Clin
Infect Dis. 2000; 31:1216-24.
•
All of the statins produce a similar cholesterol-lowering effect,
although atorvastatin and simvastatin reduce levels somewhat more
significantly.
• The statins are metabolized by the CYP3A4 pathway. Since protease
inhibitors inhibit this pathway, the resulting increased levels of
statins may place patients at a greater risk for skeletal muscle toxicity.
• Pravastatin is the statin least susceptible to interaction
with CYP3A4 inhibitors. None of the statins are known to be strong
inhibitors or inducers of CYP3A4.
• In vitro, fluvastatin selectively inhibits the CYP2C9 enzyme
involved in the metabolism of nelfinavir. Significant drug interactions
may result in decreased levels of the active metabolite of nelfinavir.
• Given the potential for drug interactions, it is reasonable
to use initial low doses of either pravastatin or atorvastatin in
patients who are taking protease inhibitors. Since both lovastatin
and simvastatin are extensively metabolized by CYP3A4, these should
be avoided.1
Reference:
1. Dube MP, Sprecher D, Henry WK et al. Preliminary guidelines for
the evaluation and management of dyslipidemia in HIV-infected adults
receiving antiretroviral therapy. Recommendations of the adult ACTG
cardiovascular disease focus group. Clin Infect Dis. 2000;31:1216-24.
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