Stereoselective inhibition by the diastereomers quinidine and quinine of uptake of cardiac glycosides into isolated rat hepatocytes.

  title={Stereoselective inhibition by the diastereomers quinidine and quinine of uptake of cardiac glycosides into isolated rat hepatocytes.},
  author={Ann Hedman and Dirk K. F. Meijer},
  journal={Journal of pharmaceutical sciences},
  volume={87 4},
  • A. HedmanD. Meijer
  • Published 1 April 1998
  • Biology, Medicine, Chemistry
  • Journal of pharmaceutical sciences
The pharmacokinetic interaction between quinidine and digoxin in patients is well-known, in general requiring a dose reduction of digoxin in patients concomitantly treated with quinidine. Quinine, the diastereomer of quinidine, has not been as extensively studied in this respect. In addition to an interaction with the renal clearance of digoxin by quinidine, both diastereomers have been reported to inhibit the biliary clearance of digoxin in man. To further investigate the mechanisms of these… 

Characterization of Digoxin Uptake in Sandwich-Cultured Human Hepatocytes

Investigation of hepatic uptake mechanisms of [3H]digoxin using sandwich-cultured human hepatocytes (SCHH) and transporter-expressing cells suggests that digoxin uptake in SCHH involves both saturable and passive processes.

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Metabolism of digoxin and digoxigenin digitoxosides in rat liver microsomes: involvement of cytochrome P4503A.

  • L. SalphatiL. Benet
  • Biology, Chemistry
    Xenobiotica; the fate of foreign compounds in biological systems
  • 1999
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No effects were observed in these experiments where the exposure levels of trans-1,2-cyclohexanediol were extremely high compared to those in humans given the maximum therapeutic dose of CC, it is unlikely that CC would induce arrhythmias in clinical use even in patients treated with cardiac glycosides.

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Effect of quinidine on the hepatic uptake of digoxin in guinea pigs.

It is concluded that the quinidine-induce decreases in the hepatic distribution of digoxin may be attributed both to the decreased tissue binding and to the inhibition of uptake, which might be related to the decrease hepatic clearance.

Interactions in the renal and biliary elimination of digoxin: Stereoselective difference between quinine and quinidine

Findings explain the difference in magnitude between quinidine and quinine in regard to the interaction with digoxin and imply a different degree of stereoselectivity for these isomers in the renal and biliary secretory systems of digoxin.

Stereoselective renal tubular secretion of quinidine and quinine

It is concluded that there is stereoselective net renal tubular secretion of quinidine over quinine indicating stereOSElectivity of this renal Tubular transport process.

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1 This study was designed to evaluate pharmacokinetically the digoxin-quinidine interaction in patients with atrial fibrillation. 2 Five patients on maintenance digoxin therapy were given

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Differences in the binding of quinine and quinidine to plasma proteins.

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