Atorvastatin interactions with food
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Atorvastatin Interactions with Food
Impact of Food on Atorvastatin Bioavailability
Reduced Absorption Rate and Extent
When atorvastatin is taken with food, its absorption rate and extent are significantly affected. A study involving 16 healthy volunteers demonstrated that consuming a medium-fat breakfast with atorvastatin led to a 47.9% reduction in the maximum plasma concentration (Cmax) and a 12.7% decrease in the area under the concentration-time curve (AUC) compared to fasting conditions1. This indicates that food can substantially lower the peak levels of atorvastatin in the bloodstream.
Delayed Time to Maximum Concentration
Food intake also delays the time to reach maximum concentration (tmax) of atorvastatin. In the same study, the tmax was extended from 2.6 hours in fasting conditions to 5.9 hours when taken with food1. Another study confirmed this finding, showing a 29.8% longer tmax when atorvastatin was administered with evening meals compared to after meals2. This delay suggests that food slows down the absorption process of atorvastatin.
Pharmacokinetic and Pharmacodynamic Effects
Consistent Lipid-Lowering Efficacy
Despite the changes in pharmacokinetics, the lipid-lowering efficacy of atorvastatin remains consistent whether taken with or without food. Research has shown that reductions in LDL-C, total cholesterol, and triglycerides are similar regardless of food intake2. This suggests that while food affects the absorption rate and peak concentration, it does not significantly impact the overall therapeutic effect of atorvastatin.
Fixed-Dose Combination with Metformin
In a study examining the fixed-dose combination (FDC) of atorvastatin and metformin, food was found to delay the time to reach maximum concentration and decrease the Cmax of atorvastatin by 32%3. However, these changes were consistent with the effects observed when atorvastatin and metformin were taken as individual tablets with food. This indicates that the presence of food alters the pharmacokinetics of both drugs in a predictable manner.
Conclusion
Food intake significantly affects the pharmacokinetics of atorvastatin by reducing its absorption rate and peak concentration, and delaying the time to reach maximum concentration. However, these changes do not appear to impact the drug's lipid-lowering efficacy. Therefore, atorvastatin can be administered with or without food, depending on patient preference and convenience.
Sources and full results
Most relevant research papers on this topic
Effect of Food on the Bioavailability of Atorvastatin, an HMG‐CoA Reductase Inhibitor
A medium-fat breakfast significantly decreased the rate of atorvastatin absorption, but had little impact on the extent of drug absorption.
RCTEffect of food on the pharmacodynamics and pharmacokinetics of atorvastatin, an inhibitor of HMG-CoA reductase
Atorvastatin can be administered with or without food, but its pharmacokinetics may be affected by food, but LDL-C reductions remain similar.
RCTPharmacokinetics of fixed-dose combination of atorvastatin and metformin compared with individual tablets
No clinically relevant pharmacokinetic interaction was observed when atorvastatin was co-administered with metformin, but food may affect the absorption of both drugs from an FDC formulation.
RCT
Rigorous JournalSimultaneous intake of oat bran and atorvastatin reduces their efficacy to lower lipid levels and atherosclerosis in LDLr-/- mice.
Simultaneous intake of oat bran and atorvastatin reduces their efficacy in lowering lipid levels and atherosclerosis in LDLr-/- mice, possibly due to oat bran inhibiting atorvastatin's intestinal absorption.
Absence of a significant pharmacokinetic interaction between atorvastatin and fenofibrate: a randomized, crossover, study of a fixed-dose formulation in healthy Mexican subjects
Aatorvastatin and fenofibrate have no significant pharmacokinetic interaction in healthy Mexican volunteers.
RCTPharmacokinetic Interaction between Atorvastatin and Omega-3 Fatty Acid in Healthy Volunteers
Atorvastatin and omega-3 fatty acids show a pharmacokinetic interaction in healthy volunteers, with 90% CIs for primary endpoints outside typical bioequivalence ranges.
Non-RCTEffects of atorvastatin and/or probucol on recovery of atherosclerosis in high-fat-diet-fed apolipoprotein E-deficient mice.
Atorvastatin and/or probucol can help recover atherosclerosis in high-fat-diet-fed apolipoprotein E-deficient mice by suppressing ER stress and increasing TLR-4 levels.
RCT
Animal StudyRigorous JournalAtorvastatin Induces Hepatotoxicity in Diabetic Rats via Oxidative Stress, Inflammation, and Anti-Apoptotic Pathway
Atorvastatin can cause severe liver injury in diabetic rats by increasing oxidative stress, inflammation, and inhibiting apoptosis through modulation of oxidative/antioxidative status, pro-inflammatory cytokine production, and anti-apoptotic pathways.
RCTAnimal StudyRigorous JournalAtorvastatin: safety and tolerability
Atorvastatin is generally well tolerated across its therapeutic dosage range, with rare adverse events (liver function abnormalities and muscle-related side effects) occurring in specific populations.
Systematic ReviewMultiple‐dose pharmacokinetics, pharmacodynamics, and safety of atorvastatin, an inhibitor of HMG‐CoA reductase, in healthy subjects
Atorvastatin doses of up to 80 mg/day were well tolerated and had significant cholesterol-lowering effects in healthy subjects.
RCT
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