DOI: 10.1002/j.1552-4604.1995.tb04015.x. Effect of Food on the Bioavailability of Atorvastatin, an HMG‐CoA Reductase Inhibitor

Effect of Food on the Bioavailability of Atorvastatin, an HMG‐CoA Reductase Inhibitor

10.1002/j.1552-4604.1995.tb04015.x

Crossref journal-article

Wiley

The Journal of Clinical Pharmacology (311)

Abstract

To determine whether atorvastatin, a new HMG‐CoA reductase inhibitor, could be administered with food in Phase II and III clinical trials, a nonblind, randomized, two‐way crossover study was conducted to assess the effect of food on rate and extent of atorvastatin absorption. Sixteen healthy volunteers received single 80‐mg atorvastatin capsule doses on two occasions one week apart: once after an 8‐hour overnight fast and once with a medium‐fat breakfast. The single 80‐mg atorvastatin capsule doses were well‐tolerated. Mean maximum plasma atorvastatin equivalent concentration (Cmax) and area under the concentration—time curve (AUC) values with food were 47.9% and 12.7% lower, respectively, than without food. Mean time of maximum observed concentration (tmax) and elimination half‐life (t1/2) values were 5.9 and 32.0 hours, respectively, with food and 2.6 and 35.7 hours, respectively, without food. A medium‐fat breakfast decreased the rate of atorvastatin absorption significantly, but had little impact on extent of drug absorption. Changes in rate of atorvastatin absorption are not expected to have a clinically significant effect, as subsequent multiple‐dose clinical studies have shown that dose but not plasma atorvastatin concentration profiles correlates with lipid‐lowering effects.

Bibliography

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 HMGâCoA Reductase Inhibitor. The Journal of Clinical Pharmacology, 35(10), 990â994. Portico.

Authors 5

Louis L. Radulovic (first)
Donald D. Cilla (additional)
Edward L. Posvar (additional)
Allen J. Sedman (additional)
Lloyd R. Whitfield (additional)

References 15 Referenced 49

{'key': 'e_1_2_1_2_2', 'first-page': '36', 'article-title': 'The clinical significance of food—drug interactions: a review', 'volume': '150', 'author': 'Neuvonen PJ', 'year': '1989', 'journal-title': 'Therapeutics'} / Therapeutics / The clinical significance of food—drug interactions: a review by Neuvonen PJ (1989)
10.1016/0005-2760(92)90103-3
{'key': 'e_1_2_1_4_2', 'first-page': 'S‐332', 'article-title': 'Safety, tolerance and pharmacokinetic profiles following single‐doses of CI‐981, a potent HMG‐CoA reductase inhibitor (abstract PPDM 8134)', 'volume': '10', 'author': 'Cilla DD', 'year': '1993', 'journal-title': 'Pharm Res'} / Pharm Res / Safety, tolerance and pharmacokinetic profiles following single‐doses of CI‐981, a potent HMG‐CoA reductase inhibitor (abstract PPDM 8134) by Cilla DD (1993)
{'key': 'e_1_2_1_5_2', 'first-page': 'S‐340', 'article-title': 'Single‐ and multiple‐dose pharmacokinetics of CI‐981, a potent HMG‐CoA reductase inhibitor (abstract PPDM 8167)', 'volume': '10', 'author': 'Whitfield LR', 'year': '1993', 'journal-title': 'Pharm Res'} / Pharm Res / Single‐ and multiple‐dose pharmacokinetics of CI‐981, a potent HMG‐CoA reductase inhibitor (abstract PPDM 8167) by Whitfield LR (1993)
{'key': 'e_1_2_1_6_2', 'first-page': '21', 'article-title': 'Lovastatin: a new cholesterol‐lowering agent', 'volume': '7', 'author': 'McKenny JM', 'year': '1988', 'journal-title': 'Clin Pharm'} / Clin Pharm / Lovastatin: a new cholesterol‐lowering agent by McKenny JM (1988)
10.2165/00003088-199324030-00002
{'key': 'e_1_2_1_8_2', 'first-page': '552', 'article-title': 'Focus on pravastatin: an HMG‐CoA reductase inhibitor for the treatment of hypercholesterolemia', 'volume': '26', 'author': 'Broisman L', 'year': '1991', 'journal-title': 'Hosp Formul'} / Hosp Formul / Focus on pravastatin: an HMG‐CoA reductase inhibitor for the treatment of hypercholesterolemia by Broisman L (1991)
{'key': 'e_1_2_1_9_2', 'first-page': '153', 'article-title': 'Hypercholesterolemia update: review of lovastatin and other pharmacologic agents', 'volume': '24', 'author': 'Murphy FL', 'year': '1989', 'journal-title': 'Hosp Formul'} / Hosp Formul / Hypercholesterolemia update: review of lovastatin and other pharmacologic agents by Murphy FL (1989)
10.1093/ajh/6.11.375S
10.1016/0002-9149(94)90627-0
{'key': 'e_1_2_1_12_2', 'first-page': '588a', 'article-title': 'Effects of food on the pharmacokinetics and pharmacodynamics of pravastatin, an HMG CoA reductase inhibitor (abstract)', 'volume': '8', 'author': 'Pan H', 'year': '1988', 'journal-title': 'Arteriosclerosis'} / Arteriosclerosis / Effects of food on the pharmacokinetics and pharmacodynamics of pravastatin, an HMG CoA reductase inhibitor (abstract) by Pan H (1988)
{'key': 'e_1_2_1_13_2', 'first-page': '291', 'article-title': 'Effect of food on pravastatin pharmacokinetics and pharmacodynamics', 'volume': '31', 'author': 'Pan HY', 'year': '1993', 'journal-title': 'Int J Clin Pharmacol Ther Toxicol'} / Int J Clin Pharmacol Ther Toxicol / Effect of food on pravastatin pharmacokinetics and pharmacodynamics by Pan HY (1993)
{'key': 'e_1_2_1_14_2', 'volume-title': "SAS User's Guide.", 'author': 'SAS Institute', 'year': '1987'} / SAS User's Guide. by SAS Institute (1987)
10.1016/0002-9149(94)90626-2
{'key': 'e_1_2_1_16_2', 'first-page': '590a', 'article-title': 'Effect of food on the low density lipoprotein cholesterol lowering response to twice daily pravastatin (abstract)', 'volume': '8', 'author': 'Cressman MD', 'year': '1988', 'journal-title': 'Arteriosclerosis'} / Arteriosclerosis / Effect of food on the low density lipoprotein cholesterol lowering response to twice daily pravastatin (abstract) by Cressman MD (1988)

Dates

Type	When
Created	12 years, 5 months ago (March 8, 2013, 2:44 p.m.)
Deposited	1 year, 10 months ago (Oct. 26, 2023, 11:39 p.m.)
Indexed	3 months, 1 week ago (May 30, 2025, 2:06 a.m.)
Issued	29 years, 11 months ago (Oct. 1, 1995)
Published	29 years, 11 months ago (Oct. 1, 1995)
Published Online	12 years, 5 months ago (March 8, 2013)
Published Print	29 years, 11 months ago (Oct. 1, 1995)

Funders 0

None

BibTeX

@article{Radulovic_1995, title={Effect of Food on the Bioavailability of Atorvastatin, an HMG‐CoA Reductase Inhibitor}, volume={35}, ISSN={1552-4604}, url={http://dx.doi.org/10.1002/j.1552-4604.1995.tb04015.x}, DOI={10.1002/j.1552-4604.1995.tb04015.x}, number={10}, journal={The Journal of Clinical Pharmacology}, publisher={Wiley}, author={Radulovic, Louis L. and Cilla, Donald D. and Posvar, Edward L. and Sedman, Allen J. and Whitfield, Lloyd R.}, year={1995}, month=oct, pages={990–994} }

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