Literature DB >> 2493245

Tissue selectivity of the cholesterol-lowering agents lovastatin, simvastatin and pravastatin in rats in vivo.

J I Germershausen1, V M Hunt, R G Bostedor, P J Bailey, J D Karkas, A W Alberts.   

Abstract

Tissue selectivity of lovastatin, simvastatin and pravastatin was determined in male rats. Peak levels of active drug were found in all tissues examined between 0.5 and 2 hours after oral administration. The area under the curve describing 24 hour exposure of the tissues to drug indicated that the drugs were preferentially concentrated in the liver. However, the concentration of pravastatin was approximately 50% that of either lovastatin or simvastatin in the liver and 3-6 times higher in peripheral tissues. These studies demonstrate that the hydrophobic prodrugs, lovastatin and simvastatin show greater selectivity than the hydrophilic agent pravastatin towards the liver which is the target organ for inhibitors of 3-hydroxy-3-methylglutaryl-coenzyme A reductase.

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Year:  1989        PMID: 2493245     DOI: 10.1016/0006-291x(89)92773-3

Source DB:  PubMed          Journal:  Biochem Biophys Res Commun        ISSN: 0006-291X            Impact factor:   3.575


  51 in total

1.  Pharmacokinetic and pharmacodynamic evaluation for tissue-selective inhibition of cholesterol synthesis by pravastatin.

Authors:  T Hatanaka; S Honda; S Sasaki; K Katayama; T Koizumi
Journal:  J Pharmacokinet Biopharm       Date:  1998-06

2.  Short- and long-term effects of lovastatin and pravastatin alone and in combination with cholestyramine on serum lipids, lipoproteins and apolipoproteins in primary hypercholesterolaemia.

Authors:  B G Jacob; W Möhrle; W O Richter; P Schwandt
Journal:  Eur J Clin Pharmacol       Date:  1992       Impact factor: 2.953

Review 3.  HMG-CoA reductase inhibitor use in the aged. A review of clinical experience.

Authors:  C J Lintott; R S Scott
Journal:  Drugs Aging       Date:  1992 Nov-Dec       Impact factor: 3.923

4.  Lipid lowering drugs.

Authors:  T S Bocanegra; J A Tobert
Journal:  BMJ       Date:  1990-05-05

5.  Hypercholesterolemia promotes an osteoporotic phenotype.

Authors:  Kristine Pelton; Jaclynn Krieder; Danese Joiner; Michael R Freeman; Steven A Goldstein; Keith R Solomon
Journal:  Am J Pathol       Date:  2012-07-04       Impact factor: 4.307

Review 6.  Pleiotropic effects of statins.

Authors:  James K Liao; Ulrich Laufs
Journal:  Annu Rev Pharmacol Toxicol       Date:  2005       Impact factor: 13.820

Review 7.  Effects of statins on 3-hydroxy-3-methylglutaryl coenzyme a reductase inhibition beyond low-density lipoprotein cholesterol.

Authors:  James K Liao
Journal:  Am J Cardiol       Date:  2005-09-05       Impact factor: 2.778

8.  Transdermal application of lovastatin to rats causes profound increases in bone formation and plasma concentrations.

Authors:  G E Gutierrez; D Lalka; I R Garrett; G Rossini; G R Mundy
Journal:  Osteoporos Int       Date:  2006-05-03       Impact factor: 4.507

9.  Tissue-selective inhibition of sterol synthesis in mice by pravastatin sodium after a single or repeated oral administrations.

Authors:  T Koga; T Kikuchi; A Miyazaki; H Koike
Journal:  Lipids       Date:  1995-08       Impact factor: 1.880

10.  Short-term effects of treatment with simvastatin on testicular function in patients with heterozygous familial hypercholesterolaemia.

Authors:  K Purvis; A Tollefsrud; H Rui; E Haug; J Norseth; L Viksmoen; L Ose; H Lund
Journal:  Eur J Clin Pharmacol       Date:  1992       Impact factor: 2.953

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