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Titolo:
STEREOSELECTIVE INHIBITION BY THE DIASTEREOMERS QUINIDINE AND QUININEOF UPTAKE OF CARDIAC-GLYCOSIDES INTO ISOLATED RAT HEPATOCYTES
Autore:
HEDMAN A; MEIJER DKF;
Indirizzi:
UNIV GRONINGEN,GIDS,CTR PHARM,DEPT PHARMACOKINET & DRUG DELIVERY GRONINGEN NETHERLANDS UNIV GRONINGEN,GIDS,CTR PHARM,DEPT PHARMACOKINET & DRUG DELIVERY GRONINGEN NETHERLANDS
Titolo Testata:
Journal of pharmaceutical sciences
fascicolo: 4, volume: 87, anno: 1998,
pagine: 457 - 461
SICI:
0022-3549(1998)87:4<457:SIBTDQ>2.0.ZU;2-#
Fonte:
ISI
Lingua:
ENG
Soggetto:
BILIARY ELIMINATION; UPTAKE SYSTEM; DIGOXIN; CLEARANCE; DRUG; TRANSPORTER; HUMANS; LIVER;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
22
Recensione:
Indirizzi per estratti:
Citazione:
A. Hedman e D.K.F. Meijer, "STEREOSELECTIVE INHIBITION BY THE DIASTEREOMERS QUINIDINE AND QUININEOF UPTAKE OF CARDIAC-GLYCOSIDES INTO ISOLATED RAT HEPATOCYTES", Journal of pharmaceutical sciences, 87(4), 1998, pp. 457-461

Abstract

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 byquinidine, both diastereomers have been reported to inhibit the biliary clearance of digoxin in man. To further investigate the mechanisms of these hepatobiliary transport interactions at the cellular level, we compared the effects of quinidine and quinine, as well as of the calcium antagonist verapamil, on the uptake of digoxin and ouabain in isolated rat hepatocytes. Initial uptake rates of digoxin and ouabain were determined in the presence of various concentrations of quinine and quinidine. A concentration dependent inhibition of the cellular uptakeof both cardiac glycosides by quinine and quinidine was found, quinine being a more potent inhibitor than quinidine. Our results indicate astereoselective inhibition of the hepatocellular uptake by the two diastereomers quinidine and quinine, the latter being about equipotent to verapamil. This unequal inhibitory potency of the two basic drugs was detected earlier in oocyte studies with the cloned organic cation transporter OCT1.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 28/11/20 alle ore 21:42:07