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Effect of food on the pharmacodynamics and pharmacokinetics of atorvastatin, an inhibitor of HMG-CoA reductase


The pharmacodynamics and pharmacokinetics of atorvastatin, an HMG-CoA reductase inhibitor, were characterized in 16 healthy subjects following administration of 10 mg atorvastatin tablets with, or 3 h after, evening meals for 15 days in an open-label, randomized, 2-way crossover study. Atorvastatin was well tolerated. Atorvastatin administration with evening meals resulted in 25.2% lower mean Cmax and 29.8% longer mean, tmax values relative to administration after meals. The mean AUC0−24 value was 8.6% lower for atorvastatin administration with meals compared to after meals. In contrast to the effect of food on pharmacokinetics, LDL-C reductions were similar after atorvastatin administration with or after evening meals. Average reductions from baseline were 24.4% for total cholesterol, 39.6% for LDL-C and 10% for triglycerides. Therefore, atorvastatin may be administered with or without food.

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Correspondence to L. R. Whitfield.

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Whitfield, L.R., Stern, R.H., Sedman, A.J. et al. Effect of food on the pharmacodynamics and pharmacokinetics of atorvastatin, an inhibitor of HMG-CoA reductase. Eur. J. Drug Metab. Pharmacokinet. 25, 97–101 (2000).

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  • Atorvastatin
  • food
  • pharmacokinetics
  • pharmacodynamics
  • HMG-CoA reductase