Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
4
pubmed:dateCreated
1990-5-29
pubmed:abstractText
The effect of cationic drugs on the uptake of the prototypical organic cation N'-methylnicotinamide has been evaluated. Using purified brush border membrane vesicles prepared from dog kidney cortex and applying a rapid Millipore filtration technique, cationic drugs apparent inhibitory constants (Ki) were calculated from kinetic analysis of N'-methylnicotinamide uptake corrected for noncarrier-mediated transport (10 s uptake; outwardly directed H+ gradient; pH 7.4, 25 degrees C). All of the cationic drugs tested exhibited competitive inhibition of N'-methylnicotinamide uptake suggesting that they all share the organic base transport system at the renal proximal tubule. The Ki values were as follows, in order of decreasing apparent affinity: quinidine (0.7 microM), trimehoprim (1.3 microM), cimetidine (2.0 microM), famotidine (3.0 microM), quinine (7.0 microM), amiloride (5.8 microM), procainamide (21 microM), and nizatidine (30 microM). The different relative affinities of the drugs for the organic base transport system may explain the mutual competition for renal tubular secretion observed when cationic drugs are administered concurrently in vivo, e.g., trimethoprim--procainamide and cimetidine--procainamide. The approach outlined in the present study should prove useful to predict complex drug interactions in clinical pharmacology.
pubmed:commentsCorrections
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Apr
pubmed:issn
0008-4212
pubmed:author
pubmed:issnType
Print
pubmed:volume
68
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
467-75
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1990
pubmed:articleTitle
Inhibition kinetics of cationic drugs on N'-methylnicotinamide uptake by brush border membrane vesicles from the dog kidney cortex.
pubmed:affiliation
Faculty of Pharmacy, University of Toronto, Ont., Canada.
pubmed:publicationType
Journal Article, In Vitro, Research Support, Non-U.S. Gov't