Linked Life Data

3433801

Source:http://linkedlifedata.com/resource/pubmed/id/3433801

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
11
pubmed:dateCreated
1988-3-4
pubmed:abstractText
1. The imidazole antifungal agents, ketoconazole, miconazole and clotrimazole have been shown to be potent inhibitors of the phenobarbital-induced cytochromes P-450 and the 3-methylcholanthrene-induced cytochromes P-448-dependent rat hepatic microsomal mixed-function oxidases. 2. All three drugs were more potent inhibitors of the phenobarbital-induced O-deethylation of ethoxycoumarin than of the 3-methylcholanthrene-induced activity indicating selective inhibition of the phenobarbital-induced cytochromes P-450. In both types of microsomes ketoconazole was always the weakest inhibitor. 3. All three compounds elicited type II spectral interactions with both types of microsomes, and had similar Ks values. Miconazole and clotrimazole, and to a lesser extent ketoconazole, also interacted with the substrate binding sites of both phenobarbital-induced cytochromes P-450 and to a lesser extent with the 3-methylcholanthrene-induced cytochrome P-448. 4. It is concluded that at least part of the inhibitory effect of these antifungal agents may reflect competitive inhibition at the substrate binding site.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Nov
pubmed:issn
0049-8254
pubmed:author
pubmed:issnType
Print
pubmed:volume
17
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
1315-27
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1987
pubmed:articleTitle
Spectral and kinetic studies of the interaction of imidazole anti-fungal agents with microsomal cytochromes P-450.
pubmed:affiliation
Department of Biochemistry, University of Surrey, Guildford, UK.
pubmed:publicationType
Journal Article, In Vitro