Comparative pharmacokinetics and pharmacodynamics of pravastatin and lovastatin

Journal of Clinical Pharmacology
H Y PanA A Sugerman

Abstract

The oral bioavailability of two HMG-CoA reductase inhibitors, pravastatin and lovastatin, was investigated in this randomized, two-way crossover study. Twenty healthy men were randomly assigned to treatment with a 40-mg dose of pravastatin or lovastatin once daily for 1 week; steady state kinetics were assessed after the last dose. After 1 week of washout, each subject received the alternate treatment. Serum specimens were assayed by gas chromatography/mass spectrometry (GC/MS) for intact pravastatin or lovastatin acid and by bioassay for active inhibitor concentration and, after hydrolysis of lactones, for total inhibitor concentration. The systemic bioavailabilities of total (active plus potentially active) inhibitors for the two drugs were different, with the mean AUC value for lovastatin being 50% higher than that of pravastatin (mean +/- SEM AUC0-24 values of 285 +/- 25 and 189 +/- 13 ng-equiv x hr/mL, respectively, P less than .0001). Pravastatin, which is administered as the monosodium salt, is present in the systemic circulation as the open acid; lovastatin, which is administered as the lactone, is present as both open-acid active metabolites (62%) and closed-ring lactone metabolites (38%), which are potentially active....Continue Reading

References

Feb 1, 1990·British Journal of Clinical Pharmacology·S M SinghviD A Willard
May 1, 1989·Rapid Communications in Mass Spectrometry : RCM·D Wang-IversonA I Cohen
Dec 1, 1989·Journal of Veterinary Pharmacology and Therapeutics·D R HennessyR K Prichard
Jun 12, 1987·JAMA : the Journal of the American Medical Association·N NakayaY Goto
Jul 7, 1988·The New England Journal of Medicine·S M Grundy
Jan 1, 1987·Pharmacotherapy·J J Krukemyer, R L Talbert
Jan 14, 1988·The New England Journal of Medicine·A Garg, S M Grundy
Dec 1, 1987·American Family Physician·J R DiPalma
Jul 1, 1980·Proceedings of the National Academy of Sciences of the United States of America·A W AlbertsJ Springer

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Citations

Feb 1, 1992·Journal of Clinical Pharmacology·C E HalstensonH Pan
Feb 1, 1992·Journal of Clinical Pharmacology·P J PentikainenJ D Rogers
Sep 1, 2005·Cancer Chemotherapy and Pharmacology·Sarah A HolsteinRaymond J Hohl
Dec 4, 2008·Endocrine·Paul S PhillipsUNKNOWN Scripps Mercy Clinical Research Center
Nov 21, 1993·Biochimica Et Biophysica Acta·K Ziegler, S Hummelsiep
Oct 18, 1996·Biochimica Et Biophysica Acta·N UmetaniT Takeda
Jul 8, 1998·Journal of Chromatography. B, Biomedical Sciences and Applications·K Otter, C Mignat
May 2, 2009·FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology·Peirang CaoStewart H Lecker
Sep 1, 1993·British Journal of Clinical Pharmacology·J TriscariH Y Pan
May 5, 1999·Fundamental & Clinical Pharmacology·L BecquemontP Jaillon
Jan 1, 1993·The Journal of Clinical Investigation·M P O'DonnellW F Keane
Nov 10, 2007·The Journal of Clinical Investigation·Jun-ichi HanaiStewart H Lecker
May 23, 2007·Clinical Drug Investigation·Heleen E WiersmaChris J van Boxtel
Aug 14, 2012·EMBO Molecular Medicine·Apana A L TakwiYong Li
Sep 24, 2008·Expert Opinion on Investigational Drugs·Quen Oak TangEleftherios Tsiridis
Feb 6, 2016·Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences·Leon van HaandelJonathan B Wagner
Nov 2, 2011·European Journal of Pharmacology·Teemu J MurtolaTeuvo L J Tammela
Jan 13, 2009·Prostaglandins & Other Lipid Mediators·Qi ZhouFred A Kummerow
Oct 11, 2003·Journal of Clinical Pharmacology·Katsutoshi OgawaKatsuji Oguchi
Jul 1, 2009·British Journal of Pharmacology·C Minichsdorfer, M Hohenegger
Feb 12, 2009·Journal of Neurochemistry·Woo-Yang KimPamela J Lein
Feb 12, 2009·Pharmacoepidemiology and Drug Safety·Christopher RowanMark Avigan
Apr 30, 2005·International Journal of Cardiology·Vincent Launay-VacherGilbert Deray
Jun 22, 2005·Brain Research. Molecular Brain Research·Chaohua YanNina Felice Schor
Apr 9, 2016·Biomarkers : Biochemical Indicators of Exposure, Response, and Susceptibility to Chemicals·David PellerinFrançois Corbin

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