Document Detail


The impact of everolimus versus mycophenolate on blood and lymphocyte cyclosporine exposure in heart-transplant recipients.
MedLine Citation:
PMID:  19458944     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
BACKGROUND: Trough- or 2-h post-dose (C2) blood cyclosporine (CsA) concentrations are used for prediction of efficacy and toxicity of CsA in transplant recipients concomitantly treated with antiproliferative agents, but information on utility of blood CsA levels in patients treated with proliferation signal inhibitors (PSIs), such as everolimus, is sparse. Because of the inhibitory effect of PSIs on the P-glycoprotein drug efflux pump present in lymphocytes, we hypothesized that CsA pharmacokinetics in blood and lymphocytes were dissociated in patients concomitantly treated with everolimus. METHODS: Twelve-hour pharmacokinetic studies of whole-blood and intralymphocytic CsA concentrations were conducted in long-term heart-transplant recipients treated with mycophenolate mofetil (MMF) + CsA (n = 8) and everolimus + CsA (n = 9). RESULTS: There was a highly significant correlation between blood CsA C2 levels and blood CsA AUC(0-12) in groups of patients treated with MMF or everolimus (R(2) 0.93 and 0.96, respectively; P < 0.001 for both). Whereas blood CsA C2 levels were closely associated with lymphocyte CsA AUC(0-12) in patients treated with MMF (R(2) = 0.98), there was poor correlation between whole-blood C2 and lymphocyte AUC(0-12) in patients treated with everolimus (R(2) = 0.24). CONCLUSION: Standard blood CsA levels accurately predict intralymphocytic exposure to CsA in patients concomitantly treated with MMF but not in patients treated with everolimus.
Authors:
Finn Gustafsson; David Barth; Diego H Delgado; Meerna Nsouli; Jill Sheedy; Heather J Ross
Related Documents :
9839074 - Lymphocyte recirculation, exercise, and immune responses.
7506384 - Cytogenetic monitoring of fishermen with environmental mercury exposure.
11200564 - Modification of immunologic and hematologic variables by method of co2 euthanasia.
9298834 - Analysis of variation in results of flow cytometric lymphocyte immunophenotyping in a m...
20357044 - Effects of resveratrol on cerebral blood flow variables and cognitive performance in hu...
10926154 - Results of animal experiments using an undulation pump total artificial heart: analysis...
Publication Detail:
Type:  Clinical Trial; Journal Article     Date:  2009-05-21
Journal Detail:
Title:  European journal of clinical pharmacology     Volume:  65     ISSN:  1432-1041     ISO Abbreviation:  Eur. J. Clin. Pharmacol.     Publication Date:  2009 Jul 
Date Detail:
Created Date:  2009-06-09     Completed Date:  2009-08-18     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  1256165     Medline TA:  Eur J Clin Pharmacol     Country:  Germany    
Other Details:
Languages:  eng     Pagination:  659-65     Citation Subset:  IM    
Affiliation:
Heart Failure and Transplant, Division of Cardiology, University Health Network, Toronto General Hospital, Toronto, ON, Canada. finng@dadlnet.dk
Export Citation:
APA/MLA Format     Download EndNote     Download BibTex
MeSH Terms
Descriptor/Qualifier:
Aged
Cyclosporine / blood,  therapeutic use*
Dose-Response Relationship, Drug
Female
Heart Transplantation / immunology*,  physiology
Humans
Immunosuppressive Agents / blood,  therapeutic use*
Lymphocytes / immunology
Male
Middle Aged
Mycophenolic Acid / analogs & derivatives*,  blood,  therapeutic use
Sirolimus / analogs & derivatives*,  blood,  therapeutic use
Chemical
Reg. No./Substance:
0/Immunosuppressive Agents; 128794-94-5/mycophenolate mofetil; 159351-69-6/everolimus; 24280-93-1/Mycophenolic Acid; 53123-88-9/Sirolimus; 59865-13-3/Cyclosporine

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


Previous Document:  Gene dysregulation in Huntington's disease: REST, microRNAs and beyond.
Next Document:  Horseshoe lung associated with left-lung hypoplasia, left pulmonary artery sling and bilateral agene...