The role of cytochromes P-450 in cyclosporine metabolism.
Article Details
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Watkins PB
The role of cytochromes P-450 in cyclosporine metabolism.
J Am Acad Dermatol. 1990 Dec;23(6 Pt 2):1301-9; discussion 1309-11. doi: 10.1016/0190-9622(90)70358-o.
- PubMed ID
- 2277139 [ View in PubMed]
- Abstract
In most patients, the rate-limiting step in the elimination of cyclosporine from the body is its conversion to metabolites by cytochrome P-450 IIIA enzymes in the liver and, possibly, intestine. The significant differences found among patients in the daily dose of cyclosporine required to attain target blood levels has been attributed directly to corresponding interpatient differences in the catalytic activities of P-450 IIIA enzymes. Competitive inhibition or induction of P-450 IIIA activity appears to explain most of the clinically significant interactions of drugs with cyclosporine metabolism that have been reported. The critical importance of P-450 IIIA in the body's handling of cyclosporine has made it possible to identify potential drug interactions before they are reported. Future investigations in this field are likely to result in reduction in the cost and toxicity associated with cyclosporine therapy.
DrugBank Data that Cites this Article
- Drug Enzymes
Drug Enzyme Kind Organism Pharmacological Action Actions Cyclosporine Cytochrome P450 3A4 Protein Humans UnknownSubstrateInhibitorDetails - Drug Interactions
Drugs Interaction Integrate drug-drug
interactions in your softwareCyclosporineButalbital The metabolism of Cyclosporine can be increased when combined with Butalbital. CyclosporinePentobarbital The metabolism of Cyclosporine can be increased when combined with Pentobarbital. CyclosporineSecobarbital The metabolism of Cyclosporine can be increased when combined with Secobarbital. CyclosporineMethohexital The metabolism of Cyclosporine can be increased when combined with Methohexital. CyclosporineThiopental The metabolism of Cyclosporine can be increased when combined with Thiopental.