for Health Care Providers
Lipid-Lowering Medications: ARV Interactions
Note: Some medications mentioned in this chapter may not be available on the VHA National Formulary. Consult VA pharmacists for alternatives.
Lipid-Lowering Medications: ARV Interactions
PIs and NNRTIs can affect hepatic metabolism of HMG-coenzyme A reductase inhibitors (statins). ARVs do not generally affect the metabolism of other classes of lipid-lowering agents.
| PIs | NNRTIs |
|---|---|
| Most PIs inhibit the metabolism of most statins and can significantly increase serum statin levels, thus increasing the risk of toxicity, including myopathy and rhabdomyolysis. | NNRTI effects vary according to specific NNRTI. |
| The degree to which statin metabolism is affected by PIs varies according to the statin as well as the specific PI. | EFV generally induces statin metabolism, resulting in lower serum statin levels. |
| In general, the potential for inhibition of statin metabolism is as follows: simvastatin and lovastatin > atorvastatin >> fluvastatin, pravastatin, rosuvastatin. | NVP has not been studied well in combination with statins, but its interactions with statins would be expected to be similar to those of EFV. |
| Fluvastatin and rosuvastatin have few recognized interactions with PIs. | ETR has not been studied thoroughly in combination with statins. Its interactions are expected to depend on the specific statin. |
| DLV inhibits hepatic cytochrome P450 metabolism. Thus, DLV increases statin levels and the risk of statin-related adverse effects. |
Medical providers should consult with a clinical pharmacist or review published information on drug interactions before prescribing statins for patients taking PIs or NNRTIs, as dosage adjustments are frequently required and some combinations are contraindicated.
Other classes of ARVs (NRTIs, fusion inhibitors, chemokine coreceptor antagonists, and integrase inhibitors) do not have recognized interactions with statins. Other types of lipid-lowering medications are not metabolized by hepatic cytochrome P450 and are not affected by ARVs.
| Lipid-Lowering Medication | Considerations |
|---|---|
| Statins | |
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| Fibrates |
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| Bile Acid Sequestrants |
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| Ezetimibe |
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| Niacin |
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| N-3 (Omega-3) Fatty Acids |
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References
- Fichtenbaum CJ, Gerber JG, Rosenkranz SL, et al. Pharmacokinetic interactions between protease inhibitors and statins in HIV seronegative volunteers: ACTG Study A5047
. AIDS. 2002 Mar 8;16(4):569-77. - Gerber JG, Rosenkranz SL, Fichtenbaum CJ, et al. Effect of efavirenz on the pharmacokinetics of simvastatin, atorvastatin, and pravastatin: results of AIDS Clinical Trials Group 5108 Study. J Acquir Immune Defic Syndr. 2005 Jul 1;39(3):307-12.
- Kiser JJ, Gerber JG, Predhomme JA, et al. Drug/drug interaction between lopinavir/ritonavir and rosuvastatin in healthy volunteers. J Acquir Immune Defic Syndr. 2008 Apr 15;47(5):570-8.
- McNicholl I. Database of Antiretroviral Drug Interactions. In: Coffey S, Volberding PA, eds. HIV InSite. San Francisco: UCSF Center for HIV Information; 2008. Accessed December 1, 2008.
- Pham PA, Lee L, Fuchs E, et al. Pharmacokinetic interaction between tipranavir/ritonavir and rosuvastatin. In: Program and abstracts of the 15th Conference on Retroviruses and Opportunistic Infections; February 3-6, 2008; Boston. Abstract 767.
- Sekar VJ, Spinosa-Guzman S, Marien K, et al. Pharmacokinetic drug-drug interaction between the new HIV protease inhibitor darunavir (TMC114) and the lipid-lowering agent pravastatin. In: Program and abstracts of the 8th International Workshop on Pharmacology of HIV Therapy; April 16-18, 2007; Budapest. Abstract 55.
- U.S. Department of Health and Human Services. Guidelines for the Use of Antiretroviral Agents in HIV-1-Infected Adults and Adolescents. November 3, 2008. Accessed December 1, 2008.
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