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SIDE EFFECTS : Protease inhibitors and lipid-lowering drugs -- interactions

TreatmentUpdate 126 - 2002 March; Volume 14 Issue 3
Hosein SR
click here for french langage version of article

Background and summary

People with HIV/AIDS (PHAs) who use HAART can develop higher-than normal levels of lipids — cholesterol and triglycerides — in their blood. These changes can increase the risk of cardiovascular disease. To reduce this risk, doctors can prescribe lipid-lowering drugs, commonly called "statins," examples of which include the following:

Unfortunately, the enzymes in the intestine and liver that help absorb and break down these drugs also do the same to protease inhibitors. Thus, statins and protease inhibitors have the potential to interact as follows:

To find out about these potential interactions, researchers in the U.S. conducted a study called ACTG A5047. According to their results:

Study details

Researchers recruited 56 HIV negative subjects (59% female, 41% male) and divided them into four groups where, at some point over the course of 18 days, they were given the following drugs:

Blood samples were collected throughout the study, which lasted for about 18 days.

Results

In regard to the level of statins in the blood of subjects, researchers found that the following occurred:

Importantly, levels of all three protease inhibitors were not significantly affected by the use of statins. The doctors suggested the following courses of action for PHAs using ritonavir-saquinavir:

Although the impact of statins on the relatively new PI lopinavir (in Kaletra) was not researched in the current study, the authors did draw attention to other experiments using lopinavir. There, researchers found that Lipitor levels were increased about five times greater than normal with the use of Kaletra.

Although statins are generally safe, the study authors note that they can cause muscle pain, weakness and wasting in a small number of PHAs.

REFERENCE

Fichtenbaum CJ, Gerber JG, Rosenkranz SL, et al. Pharmacokinetic interactions between protease inhibitors and statins in HIV seronegative volunteers: ACTG study A5047. AIDS 2002;16(4):569-577.

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