Skip to main content
Log in

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

  • Published:
European Journal of Drug Metabolism and Pharmacokinetics Aims and scope Submit manuscript

Summary

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.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Similar content being viewed by others

References

  1. Nawrocki J.W., Weiss S.R., Davidson M.H. et al. (1995): Reduction of LDL-cholesterol by 25% to 60% in patients with primary hypercholesterolemia by atorvastatin, a new HMG-CoA reductase inhibitor. Arterioscler. Thromb. Vasc. Biol., 5, 678–682.

    Google Scholar 

  2. Radulovic L.L., Cilla D.D., Posvar E.L., Sedman A.J., Whitfield L.R. (1995): Effect of food on the bioavailability of atorvastatin, an HMG-CoA reductase inhibitor. J. Clin. Pharmacol., 35, 990–994.

    CAS  PubMed  Google Scholar 

  3. Shum Y.Y., Huang H., Walter G.A. et al. (1993): Development and validation of an enzyme inhibition assay for quantitation of CI-981 in human plasma [abstract PPDM 8467]. Pharm. Res., 10 (Suppl.), S-415.

    Google Scholar 

  4. Friedewald WT., Levy R.I., Fredrickson S.D. (1972): Estimation of the concentration of low-density cholesterol in plasma, without use of preparative ultracentrifuge. Clin. Chem., 18, 499–502.

    CAS  PubMed  Google Scholar 

  5. SAS Institute: SAS Users Guide. Statistical Version, 5th edn. Cary, NC: SAS Institute, 1987.

    Google Scholar 

  6. Smith H.T., Jokubaitus L.A., Troendle A.J., Hwang D.S., Robinson W.T. (1993) Pharmacokinetics of fluovastatin and specific drug interactions. Am. J. Hypertens., 6, 375S-382S.

    CAS  PubMed  Google Scholar 

  7. Deslypere J.P. (1994): Clinical implications of the biopharmaceutical properties of fluvastatin. Am. J. Cardiol., 73, 12D-17D.

    Article  CAS  PubMed  Google Scholar 

  8. Pan J., DeVault A., Glaess S. et al. (1993): Effects of food on the pharmacokinetics and pharmacodynamics of pravastatin, an HMG CoA reductase inhibitor [abstract]. Arteriosclerosis, 8, 588a.

    Google Scholar 

  9. Pan H.Y., DeVault A.R., Brescia D. et al. (1993): Effect of food on pravastatin pharmacokinetics and pharmacodynamics. Int. J. Clin. Pharmacol. Ther. Toxicol., 31, 291–294.

    CAS  PubMed  Google Scholar 

  10. Physicians’ Desk Reference: PDR. Oradell, NJ: Medical Economics, 1999.

Download references

Author information

Authors and Affiliations

Authors

Rights and permissions

Reprints and permissions

About this article

Cite this article

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). https://doi.org/10.1007/BF03190074

Download citation

  • Received:

  • Issue Date:

  • DOI: https://doi.org/10.1007/BF03190074

Keywords

Navigation