Atorvastatin with Saquinavir Interaction Details
Brand Names Associated with Atorvastatin
- Atorvastatin
- Caduet® (as a combination product containing Amlodipine, Atorvastatin)
- Lipitor®
- Liptruzet® (as a combination product containing Atorvastatin, Ezetimibe)
Brand Names Associated with Saquinavir
- Invirase®
- Saquinavir
Medical Content Editor Dr. Brian Staiger, PharmD
Last updated
Mar 04, 2024
Interaction Effect
Increased atorvastatin exposure and risk of myopathy and rhabdomyolysis
Interaction Summary
Concomitant use of atorvastatin (a CYP3A4 substrate) and saquinavir (a potent CYP3A4 inhibitor) may result in elevated atorvastatin concentrations, thereby increasing the risk of myopathy. Coadministration of atorvastatin 40 mg with ritonavir-boosted saquinavir 400 mg twice daily led to a 3.9-fold increase in atorvastatin AUC and a 4.3-fold increase in Cmax. Evaluate the benefit/risk of concomitant use[1] and if coadministered, use the lowest atorvastatin dose necessary, titrate carefully, and do not exceed doses of 20 mg daily [2]. Patients should be monitored for signs and symptoms of myopathy or rhabdomyolysis (muscle pain, tenderness, or weakness), particularly during the initial months of therapy and during upward dosage titration of either drug. Consider monitoring CPK levels periodically. If myopathy is diagnosed or suspected or if CPK is markedly increased, discontinue atorvastatin [1].
Severity
Major
Onset
Delayed
Evidence
Probable
How To Manage Interaction
Concomitant use of atorvastatin and saquinavir/ritonavir may result in elevated atorvastatin concentrations and an increased risk of myopathy/rhabdomyolysis. Evaluate the benefit/risk of coadministration[1]. If used concomitantly, use the lowest atorvastatin dose necessary, titrate carefully, and do not exceed doses of 20 mg daily [2]. Monitor the patient for signs and symptoms of myopathy or rhabdomyolysis (muscle pain, tenderness, or weakness), particularly during the initial months of therapy and during upward dosage titration of either drug. Consider monitoring CPK levels periodically. If myopathy is diagnosed or suspected or if CPK is markedly increased, discontinue atorvastatin [1].
Mechanism Of Interaction
Inhibition of CYP3A4-mediated atorvastatin metabolism by saquinavir/ritonavir
Literature Reports
A) Coadministration of atorvastatin 40 mg once daily for 4 days with ritonavir-boosted saquinavir 400 mg twice daily for 15 days led to a 3.9-fold increase in atorvastatin AUC and a 4.3-fold increase in Cmax [1].
References
1 ) Product Information: LIPITOR(R) oral tablets, atorvastatin calcium oral tablets. Pfizer (Per FDA), New York, NY, 2012.
2 ) Product Information: INVIRASE(R) oral capsules, oral tablets, saquinavir mesylate oral capsules, oral tablets. Genentech USA, Inc. (per FDA), South San Francisco, CA, 2012.
Atorvastatin Overview
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Atorvastatin is used together with diet, weight loss, and exercise to reduce the risk of heart attack and stroke and to decrease the chance that heart surgery will be needed in people who have heart disease or who are at risk of developing heart disease. Atorvastatin is also used to decrease the amount of fatty substances such as low-density lipoprotein (LDL) cholesterol ('bad cholesterol') and triglycerides in the blood and to increase the amount of high-density lipoprotein (HDL) cholesterol ('good cholesterol') in the blood. Atorvastatin may also be used to decrease the amount of cholesterol and other fatty substances in the blood in children and teenagers 10 to 17 years of age who have familial heterozygous hypercholesterolemia (an inherited condition in which cholesterol cannot be removed from the body normally). Atorvastatin is in a class of medications called HMG-CoA reductase inhibitors (statins). It works by slowing the production of cholesterol in the body to decrease the amount of cholesterol that may build up on the walls of the arteries and block blood flow to the heart, brain, and other parts of the body.
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Accumulation of cholesterol and fats along the walls of your arteries (a process known as atherosclerosis) decreases blood flow and, therefore, the oxygen supply to your heart, brain, and other parts of your body. Lowering your blood level of cholesterol and fats with atorvastatin has been shown to prevent heart disease, angina (chest pain), strokes, and heart attacks.
Saquinavir Overview
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Saquinavir is used in combination with ritonavir (Norvir) and other medications to treat human immunodeficiency virus (HIV) infection. Saquinavir is in a class of medications called protease inhibitors. It works by decreasing the amount of HIV in the blood. Although saquinavir does not cure HIV, it may decrease your chance of developing acquired immunodeficiency syndrome (AIDS) and HIV-related illnesses such as serious infections or cancer. Taking these medications along with practicing safer sex and making other lifestyle changes may decrease the risk of transmitting the HIV virus to other people.
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Definitions
Severity Categories
Contraindicated
These drugs, generally, should not be used together simultaneously due to the high risk of severe adverse effects. Combining these medications can lead to dangerous health outcomes and should be strictly avoided unless otherwise instructed by your provider.
Major
This interaction could result in very serious and potentially life-threatening consequences. If you are taking this drug combination, it is very important to be under close medical supervision to minimize severe side effects and ensure your safety. It may be necessary to change a medication or dosage to prevent harm.
Moderate
This interaction has the potential to worsen your medical condition or alter the effectiveness of your treatment. It's important that you are monitored closely and you potentially may need to make adjustments in your treatment plan or drug dosage to maintain optimal health.
Minor
While this interaction is unlikely to cause significant problems, it could intensify side effects or reduce the effectiveness of one or both medications. Monitoring for changes in symptoms and your condition is recommended, and adjustments may be made if needed to manage any increased or more pronounced side effects.
Onset
Rapid: Onset of drug interaction typically occurs within 24 hours of co-administration.
Delayed: Onset of drug interaction typically occurs more than 24 hours after co-administration.
Evidence
Level of documentation of the interaction.
Established: The interaction is documented and substantiated in peer-reviewed medical literature.
Theoretical: This interaction is not fully supported by current medical evidence or well-documented sources, but it is based on known drug mechanisms, drug effects, and other relevant information.
How To Manage The Interaction
Provides a detailed discussion on how patients and clinicians can approach the identified drug interaction as well as offers guidance on what to expect and strategies to potentially mitigate the effects of the interaction. This may include recommendations on adjusting medication dosages, altering the timing of drug administration, or closely monitoring for specific symptoms.
It's important to note that all medical situations are unique, and management approaches should be tailored to individual circumstances. Patients should always consult their healthcare provider for personalized advice and guidance on managing drug interactions effectively.
Mechanism Of Interaction
The theorized or clinically determined reason (i.e., mechanism) why the drug-drug interaction occurs.
Disclaimer: The information provided on this page is for informational purposes only and should not be considered medical advice. Always consult with a qualified healthcare professional regarding your specific circumstances and medical conditions.
Where Does Our Information Come From?
Information for our drug interactions is compiled from several drug compendia, including:
The prescribing information for each drug, as published on DailyMED, is also used.
Individual drug-drug interaction detail pages contain references specific to that interaction. You can click on the reference number within brackets '[]' to see what reference was utilized.
The information posted is fact-checked by HelloPharmacist clinicians and reviewed quarterly.