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Biochim Biophys Acta. 1992 Jul 7;1139(3):203-9.

Tissue-selective action of pravastatin due to hepatocellular uptake via a sodium-independent bile acid transporter.

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Institut für Pharmakologie und Toxikologie, Giessen, Germany.


Pravastatin is a foreign substrate of a sodium-independent transport system for bile acids. The tissue selectivity of pravastatin in inhibiting 3-hydroxy-3-methyl-glutaryl-coenzyme A reductase is due to the uptake via a transport system which exists predominantly in liver cells. Pravastatin competitively inhibits the sodium-independent hepatocellular uptake of cholate, taurocholate and ouabain, whereas the total uptake of cholate is non-competitively blocked. The affinity of pravastatin to the sodium-dependent taurocholate transporter is, however, low. Millimolar concentrations of pravastatin are needed to inhibit the sodium-taurocholate cotransporter. Pravastatin has no affinity to other transport systems in liver cells such as those for long-chain fatty acids, amino acids, rifampicin and bivalent organic cations.

[Indexed for MEDLINE]

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