Cyclosporine is metabolized by hepatic cyto-chrome P-450 enzymes; concomitant administra-tion of drugs that interact with the P-450 system may affect cyclosporine's metabolism (Table I). Elimination is by hepatic metabolism and biliary excretion. Most circulating cyclosporine is associ-ated with lipoproteins of high, low, or very low den-
Cyclosporine: Uses, Interactions, Mechanism of Action - DrugBank …
Metabolism. Cyclosporine is metabolized in the intestine and the liver by CYP450 enzymes, predominantly CYP3A4 with contributions from CYP3A5. 2,9 The involvement of CYP3A7 is not clearly established. 9 Cyclosporine undergoes several metabolic
Cyclosporine - StatPearls - NCBI Bookshelf
2023年8月28日 · The mechanism of action of cyclosporine is as a calcineurin inhibitor, a cytochrome P450 3A4 inhibitor, and a P-glycoprotein inhibitor. Cyclosporin A (CsA) inhibits the synthesis of interleukins (IL), including IL-2, which is essential for the self-activation of T lymphocytes (LT) and their differentiation.
Cyclosporine metabolism in human liver: identification of a …
The data suggest that this cytochrome P-450 is the major cyclosporine-metabolizing enzyme in human liver. The substrate specificity and the known inducers and inhibitors of this cytochrome P-450 explain several clinically observed drug interactions with cyclosporine.
Functional evaluation of cyclosporine metabolism by CYP3A4 …
The aim of this study is to investigate the effects of CYP3A4 genetic polymorphisms on the metabolism of cyclosporine (CsA) in vitro and identify drugs that interact with CsA. An enzymatic incubation system was developed to evaluate the kinetic ...
Metabolic Pathway of Cyclosporine A and Its Correlation with ...
In this review, we have summarized the specific metabolic profiles of CsA in humans, especially renal-transplant patients. Moreover, the specific metabolizing enzymes and the potential roles that CsA metabolism plays in CsA nephrotoxicity were summarized and discussed.
Cyclosporin clinical pharmacokinetics - PubMed
Cyclosporin is extensively metabolised in the liver by the cytochrome P450 3A system, which is subject to considerable interindividual variation. Distribution of cyclosporin depends not only on physicochemical characteristics, but also on biological carriers such as lipoproteins and erythrocytes in blood.
Pharmacology and pharmacokinetics of cyclosporine
1991年2月1日 · Cyclosporine metabolism in human liver: identification of a cytochrome P-450III gene family as the major cyclosporine-metabolizing enzyme explains interactions of cyclosporine with other drugs
CYP3A5 Gene Variation Influences Cyclosporine A Metabolite …
2013年3月3日 · We evaluated the hypothesis that CYP3A5 genotype, and inferred enzyme expression, affects systemic CsA metabolite exposure and intra-renal CsA accumulation. An oral dose of CsA was administered to 24 healthy volunteers who were selected based on their CYP3A5 genotype. CsA and its six main metabolites in …
Cyclosporin A Metabolism and Drug Interactions | SpringerLink
Cyclosporin A (CsA) has revolutionized post-transplantation immune suppressive therapy, due to its potent selective immunological properties, and also has potential advantages over conventional treatments in the area of autoimmune diseases.
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