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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
1
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pubmed:dateCreated |
1994-8-22
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pubmed:abstractText |
The in vitro metabolism of FK 506 and its inhibition by other drugs was studied with hepatic microsomes from rats pre-treated with dexamethasone, a selective cytochrome P-450 IIIA inducer. Nonspecific inhibitors of cytochrome P-450, such as ketoconazole, itraconazole, fluconazole and SKF 525 A, and most of the cytochrome P-450 IIIA specific substrates used in this study significantly inhibited FK 506 metabolism. Although cyclosporine is a known substrate of cytochrome P-450 IIIA, it had no effect on FK 506 metabolism. Cytochrome P-450 II substrates had minimal but significant effect on FK 506 metabolism. This data supports our earlier observations that FK 506 metabolism is mediated predominantly by the steroid inducible cytochrome P-450 IIIA enzyme subfamily. The results of this study indicate that in transplant patients there is a potential for an interaction of FK 506 with other drugs that are metabolized by the cytochrome P-450 IIIA subfamily or those that alter the activity of cytochrome P-450 IIIA subfamily. Careful monitoring and FK 506 dosing adjustment may be necessary to maintain therapeutic concentration and minimize toxicity in patients receiving this agent.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Antifungal Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Cardiotonic Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Cytochrome P-450 Enzyme System,
http://linkedlifedata.com/resource/pubmed/chemical/Dexamethasone,
http://linkedlifedata.com/resource/pubmed/chemical/Tacrolimus
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pubmed:status |
MEDLINE
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pubmed:month |
Apr
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pubmed:issn |
0034-5164
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
84
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
35-46
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
pubmed-meshheading:7518966-Animals,
pubmed-meshheading:7518966-Antifungal Agents,
pubmed-meshheading:7518966-Cardiotonic Agents,
pubmed-meshheading:7518966-Cytochrome P-450 Enzyme System,
pubmed-meshheading:7518966-Dexamethasone,
pubmed-meshheading:7518966-Drug Interactions,
pubmed-meshheading:7518966-Male,
pubmed-meshheading:7518966-Microsomes, Liver,
pubmed-meshheading:7518966-Rats,
pubmed-meshheading:7518966-Rats, Sprague-Dawley,
pubmed-meshheading:7518966-Substrate Specificity,
pubmed-meshheading:7518966-Tacrolimus
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pubmed:year |
1994
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pubmed:articleTitle |
FK 506 (Tacrolimus) metabolism by rat liver microsomes and its inhibition by other drugs.
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pubmed:affiliation |
Department of Pharmaceutical Sciences, University of Pittsburgh, PA 15261.
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pubmed:publicationType |
Journal Article
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