| pubmed-article:2390433 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:2390433 | lifeskim:mentions | umls-concept:C0683140 | lld:lifeskim |
| pubmed-article:2390433 | lifeskim:mentions | umls-concept:C0010592 | lld:lifeskim |
| pubmed-article:2390433 | lifeskim:mentions | umls-concept:C1999216 | lld:lifeskim |
| pubmed-article:2390433 | pubmed:issue | 1 | lld:pubmed |
| pubmed-article:2390433 | pubmed:dateCreated | 1990-10-1 | lld:pubmed |
| pubmed-article:2390433 | pubmed:abstractText | 1. The potential for a drug interaction between cyclosporin A and midazolam was investigated since both compounds appear to be metabolized by the same cytochrome P-450 isoenzyme. 2. In vitro evaluation of the binding of cyclosporin A to rat microsomal cytochrome P-450 indicated a Ks-value of 0.4 microM. In further studies with rat liver microsomes IC50-values of 6, 8 and 70 microM cyclosporin A were determined for the inhibition of the metabolism of midazolam to its alpha-OH-,4-OH- and di-OH-metabolites, respectively. 3. Comparative studies with human liver microsomes indicated IC50-values of approximately 300 microM for the formation of alpha-OH-midazolam and of 65 microM for the formation of 4-OH-midazolam. 4. The pharmacokinetics of a single intravenous dose of midazolam (0.075 mg kg-1) was studied in nine patients receiving cyclosporin A to prevent rejection of their transplanted kidneys. The average steady state blood concentrations of cyclosporin A, measured by r.i.a. using a specific monoclonal antibody, varied during a dosing interval between 175 and 600 ng ml-1. 5. In these patients the hepatic elimination of midazolam was characterized by a mean t1/2 (+/- s.d.) of 2.3 +/- 1.2 h and a plasma clearance (CL) of 414 +/- 95 ml min-1. These values were not different from those of normal human subjects (t1/2 = 1.5 to 4 h, CL = 350 to 700 ml min-1). 6. From the results of the in vitro experiments it is concluded that cyclosporin A may potentially inhibit drug metabolism.(ABSTRACT TRUNCATED AT 250 WORDS) | lld:pubmed |
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| pubmed-article:2390433 | pubmed:language | eng | lld:pubmed |
| pubmed-article:2390433 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2390433 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:2390433 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
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| pubmed-article:2390433 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:2390433 | pubmed:month | Jul | lld:pubmed |
| pubmed-article:2390433 | pubmed:issn | 0306-5251 | lld:pubmed |
| pubmed-article:2390433 | pubmed:author | pubmed-author:WerringloerJJ | lld:pubmed |
| pubmed-article:2390433 | pubmed:author | pubmed-author:KlotzUU | lld:pubmed |
| pubmed-article:2390433 | pubmed:author | pubmed-author:VEGAJ GJG | lld:pubmed |
| pubmed-article:2390433 | pubmed:author | pubmed-author:GOHK OKO | lld:pubmed |
| pubmed-article:2390433 | pubmed:author | pubmed-author:TreiberGG | lld:pubmed |
| pubmed-article:2390433 | pubmed:author | pubmed-author:MeinshausenJJ | lld:pubmed |
| pubmed-article:2390433 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:2390433 | pubmed:volume | 30 | lld:pubmed |
| pubmed-article:2390433 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:2390433 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:2390433 | pubmed:pagination | 71-7 | lld:pubmed |
| pubmed-article:2390433 | pubmed:dateRevised | 2009-11-18 | lld:pubmed |
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| pubmed-article:2390433 | pubmed:year | 1990 | lld:pubmed |
| pubmed-article:2390433 | pubmed:articleTitle | Is cyclosporin A an inhibitor of drug metabolism? | lld:pubmed |
| pubmed-article:2390433 | pubmed:affiliation | Dr Margarete Fischer-Bosch-Institute of Clinical Pharmacology, Stuttgart, FRG. | lld:pubmed |
| pubmed-article:2390433 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:2390433 | pubmed:publicationType | In Vitro | lld:pubmed |
| pubmed-article:2390433 | pubmed:publicationType | Research Support, Non-U.S. Gov't | lld:pubmed |
| http://linkedlifedata.com/r... | pubmed:referesTo | pubmed-article:2390433 | lld:pubmed |
