Drug-Drug Interactions With Statins and HIV Medications

Wiggins BS, Lamprecht DG Jr, Page RL 2nd, Saseen JJ
Recommendations for Managing Drug-Drug Interactions With Statins and HIV Medications. Am J Cardiovasc Drugs 2017; Apr 1 [Epub ahead of print].

The following are 10 key points from this review, which is intended to provide clinicians with a practical guide to managing drug-drug interactions between statins and human immunodeficiency virus (HIV) medications:

  1. HIV is essentially a chronic disease, and individuals with HIV are at high risk for cardiovascular events.
  2. Dyslipidemia is common in patients with HIV and is characterized by increases in total cholesterol, triglycerides, and low-density lipoprotein cholesterol and decreases in high-density lipoprotein cholesterol.
  3. Statins are as effective at reducing atherogenic lipoproteins in the HIV population as they are in the general population. Therefore, individuals infected with HIV should be treated similarly.
  4. The absorption, bioavailability, distribution, metabolism, and excretion of statins can be affected by antiretroviral medications, creating potentially significant drug-drug interactions that increase statin exposure and the potential for statin-related adverse effects (e.g., myalgia).
  5. Lipophilic statins (e.g., simvastatin and lovastatin) are CYP3A4 substrates; hydrophilic statins (e.g., pravastatin) are not significantly metabolized by CYP enzymes.
  6. The protease inhibitors (PIs) and pharmacokinetic boosters pose the greatest risk of clinically significant drug-drug interactions with statins. Most of these therapies are substrates, inducers, and/or inhibitors of several important CYP enzymes (e.g., CYP3A4) and transporters (e.g., P-glycoprotein).
  7. Simvastatin and lovastatin should be avoided in all patients receiving a PI-based regimen or a pharmacokinetic booster.
  8. Non-nucleoside reverse-transcriptase inhibitors (NNRTIs) are generally substrates or inhibitors of CYP enzymes; however, dose adjustments are often unnecessary. Close monitoring is still recommended, especially if higher statin doses are clinically indicated.
  9. Although the chemokine receptor-5 inhibitors, fusion inhibitors, integrase inhibitors, and nucleoside reverse-transcriptase inhibitors have not been shown to contribute to significant drug-drug interactions with statins, they are often used in combination with PIs and NNRTIs, which are known to have significant interactions with certain statins.
  10. It is recommended that clinicians follow the dosing recommendations provided by the U.S. Department of Health and Human Services Panel on Antiretroviral Guidelines for Adults and Adolescents and the International Antiviral Society—USA Panel.

Clinical Topics: Diabetes and Cardiometabolic Disease, Dyslipidemia, Heart Failure and Cardiomyopathies, Hypertriglyceridemia, Lipid Metabolism, Nonstatins, Novel Agents, Statins, Heart Failure and Cardiac Biomarkers

Keywords: Antiviral Agents, Cholesterol, HDL, Cholesterol, LDL, Chronic Disease, Cytochrome P-450 CYP3A, Drug Interactions, Dyslipidemias, HIV Infections, HIV Integrase Inhibitors, HIV Protease Inhibitors, Hydroxymethylglutaryl-CoA Reductase Inhibitors, Lipoproteins, HDL, Lovastatin, Myalgia, ATP Binding Cassette Transporter, Subfamily B, Member 1, ATP Binding Cassette Transporter, Subfamily B, Pravastatin, Receptors, Chemokine, Reverse Transcriptase Inhibitors, Simvastatin, Triglycerides

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