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A pharmacokinetic evaluation of pravastatin in middle-aged and elderly volunteers

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Summary

The pharmacokinetics of pravastatin, a serum-cholesterol-lowering drug, were studied in 20 middle-aged (46–59 years old,n=8) and elderly subjects (60–81 years old,n=12). Pravastatin serum levels were determined by HPLC and solid phase extraction. Cmax was 48.9±7.1 ng/ml (mean ± SEM,n=20), and the mean AUC0−4.5h was 104.4 ng·h/ml (n=5) for a 20 mg daily oral dose. A great interindividual variability was found for Cmax, which varied from 6.2 ng/ml to 117.8 ng/ml on the 20 mg dose. As could be expected, Cmax and AUC0−4.5h were dose-related, but Tmax and t1/2 were not. In six cases, the elimination of the drug in serum could be described by a single phase but in four cases with two phases. No significant difference was found in Cmax between the middle-aged and the elderly or between males and females.

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References

  1. Endo A., Kuroda M., Tsyhuta Y. (1976): ML-236A, ML-236B and ML-236C, new inhibitors of cholesterogenesis produced byPenicillium citrinum. J. Antibiot. (Tokyo), 29, 1346–1348.

    CAS  Google Scholar 

  2. Alberts A.W. (1988): Discovery, biochemistry and biology of lovastatin. Am. J. Cardiol., 62, 10J-15J.

    Article  CAS  PubMed  Google Scholar 

  3. Everett D.W., Chando T.J., Didonato G.C., Singhvi S.M., Pan H.Y., Weinstein S.H. (1991): Biotransformation of pravastatin sodium in humans. Drug. Metab. Dispos., 19, 740–748.

    CAS  PubMed  Google Scholar 

  4. Pan H.Y., Funke P.T., Willard D.A., McKinstry D.N. (1989): Pharmacokinetics, pharmacodynamics and safety of pravastatin sodium, a potent inhibitor of HMG-CoA reductase, in healthy volunteers. International. Congress Symposium Series no 162. London: Royal Society of Medicine, 9–21.

    Google Scholar 

  5. Pan H.Y. (1991): Clinical pharmacology of pravastatin, a selective inhibitor of HMG-CoA reductase. Eur. J. Clin. Pharmacol., 40(Suppl. 1), S15-S18.

    Article  PubMed  Google Scholar 

  6. Pan H.Y., Waclawski A.P., Funke P.T., Whigan D. (1993): Pharmacokinetics of pravastatin in elderly versus young men and women. Ann. Pharmacother., 27, 1029–1033.

    CAS  PubMed  Google Scholar 

  7. Kjartansdóttir T., Kristinsson J., Kristjansson, S. (1992): Determination of pravastatin in serum by high-performance liquid chromatography and solid-phase extraction. Scand. J. Clin. Lab. Invest., suppl. 211, 52, 101.

    Google Scholar 

  8. Funke P.T., Ivashkiv E., Arnold M.E., Cohen A.I. (1989): Determination of pravastatin sodium and its major metabolites in human serum/plasma by capillary gas chromatography/negative ion chemical ionisation mass spectrometry. Biomed. Environ. Mass Spectrom., 18, 904–909.

    Article  CAS  PubMed  Google Scholar 

  9. Morris M.J., Gilbert J.D., Hsie J.Y., Matuszewski B.K., Ramjit H.G., Bayne W.F. (1993): Determination of the HMG-CoA reductase inhibitors simvastatin, lovastatin and pravastatin in plasma by gas chromatography/chemical ionisation mass spectrometry. Biomed. Environ. Mass Spectrom., 22, 1–8.

    Article  CAS  Google Scholar 

  10. Pan H.Y., DeVault A.R., Swites B.J. et al. (1990): Pharmacokinetics and pharmacodynamics of pravastatin alone and with cholestyramine in hypercholesterolemia. Clin. Pharmacol. Ther., 48, 201–207.

    CAS  PubMed  Google Scholar 

  11. Pan H.Y., Willard, D.A., Funke P.T., McKinstry D.N. (1987): The clinical pharmacology of SQ 3100 (CS 514) in healthy subjects. Paoletti R. et al. (Eds). Drugs Affecting Lipid Metabolism. Heidelberg: Springer.

    Google Scholar 

  12. Vega G.L., Krauss R.M., Grundy S.M. (1990): Pravastatin therapy in primary moderate hypercholesterolaemia: changes in metabolism of apolipoprotein B-containing lipoproteins. J. Intern. Med., 227, 81–94.

    Article  CAS  PubMed  Google Scholar 

  13. Franceschini G., Sirtori M., Vaccarino V., Gianfranceschi G., Chiesa G., Sirtori C.R. (1989). Plasma lipoprotein changes after treatment with pravastatin and gemfibrozil in patients with familial hypercholesterolemia. J. Lab. Clin. Med., 114, 250–259.

    CAS  PubMed  Google Scholar 

  14. Johnson B.F., LaBelle P., Wilson J., Allan J., Zupkis R.V., Ronca P.D. (1990): Effects of lovastatin in diabetic patients treated with chlorpropamide. Clin. Pharmacol. Ther., 48, 467–472.

    CAS  PubMed  Google Scholar 

  15. Saito Y., Goto Y., Nakaya N. et al. (1988): Dose-dependent hypolipidemic effect of an inhibitor of HMG-CoA reductase, pravastatin (CS-514), in hypercholesterolemic subjects. A double blind test. Atherosclerosis, 72, 205–211.

    Article  CAS  PubMed  Google Scholar 

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Sigurbjörnsson, S., Kjartansdóttir, T., Jóhannsson, M. et al. A pharmacokinetic evaluation of pravastatin in middle-aged and elderly volunteers. European Journal of Drug Metabolism and Pharmacokinetics 23, 13–18 (1998). https://doi.org/10.1007/BF03189821

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  • DOI: https://doi.org/10.1007/BF03189821

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