Document Detail

Pharmacokinetics and pharmacodynamics of mycophenolic acid after enteric-coated mycophenolate versus mycophenolate mofetil in patients with progressive IgA nephritis.
MedLine Citation:
PMID:  17526858     Owner:  NLM     Status:  MEDLINE    
Mycophenolic acid can be administered orally using mycophenolate mofetil or enteric-coated mycophenolate. In renal transplant patients on immunosuppressant combination therapy, the overall mycophenolic acid exposure after oral dosing with mycophenolate mofetil and enteric-coated mycophenolate is similar. This study compared pharmacokinetics and pharmacodynamics of mycophenolic acid after equivalent doses of enteric-coated mycophenolate (360 mg twice daily) or mycophenolate mofetil (500 mg twice daily) in 7 patients with progressive IgA nephritis (glomerular filtration rate 20-35 mL/min) using a randomized crossover design. The pharmacokinetics of mycophenolic acid concentrations and pharmacodynamics (using inosine 5'-monophosphate dehydrogenase activity as a bio-marker) were sequentially monitored for 12 hours. After enteric-coated mycophenolate treatment, the mycophenolic acid peak concentration (Cmax = 12.8 vs 6.0 microg/mL, P < .05) and the overall exposure were significantly higher (AUC = 60.9 vs 40.7 microg.h/mL, P < .05), and the apparent clearance was significantly lower (CL/F = 7.9 vs 10.7 L/h, P < .05) as compared to that after mycophenolate mofetil. Paradoxically, inosine 5'-monophosphate dehydrogenase activity was not significantly different. In conclusion, the steady-state mycophenolic acid exposure was higher during treatment with enteric-coated mycophenolate as compared to mycophenolate mofetil, which might be explained by more extensive enterohepatic recycling of mycophenolic acid after administration of enteric-coated mycophenolate, whereas inosine 5'-monophosphate dehydrogenase suppression was not different.
David Czock; Franz Maximilian Rasche; Alexander Carius; Petra Glander; Klemens Budde; Steffen Bauer; Frieder Keller; Lutz von Müller
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Publication Detail:
Type:  Comparative Study; Journal Article; Randomized Controlled Trial; Research Support, Non-U.S. Gov't     Date:  2007-05-25
Journal Detail:
Title:  Journal of clinical pharmacology     Volume:  47     ISSN:  0091-2700     ISO Abbreviation:  J Clin Pharmacol     Publication Date:  2007 Jul 
Date Detail:
Created Date:  2007-06-22     Completed Date:  2007-08-20     Revised Date:  2013-05-29    
Medline Journal Info:
Nlm Unique ID:  0366372     Medline TA:  J Clin Pharmacol     Country:  United States    
Other Details:
Languages:  eng     Pagination:  850-9     Citation Subset:  IM    
University Hospital Ulm, Medical Department I, Division of Nephrology, Robert-Koch-Str. 8, 89070 Ulm, Germany.
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MeSH Terms
Area Under Curve
Cross-Over Studies
Glomerulonephritis, IGA / physiopathology*
IMP Dehydrogenase / metabolism
Immunosuppressive Agents / administration & dosage,  pharmacokinetics*,  pharmacology*,  therapeutic use
Linear Models
Metabolic Clearance Rate
Middle Aged
Mycophenolic Acid / administration & dosage,  analogs & derivatives*,  pharmacokinetics,  pharmacology,  therapeutic use
Prodrugs / administration & dosage,  pharmacokinetics*,  pharmacology*,  therapeutic use
Renal Insufficiency / physiopathology
Tablets, Enteric-Coated
Therapeutic Equivalency
Reg. No./Substance:
0/Immunosuppressive Agents; 0/Prodrugs; 0/Tablets, Enteric-Coated; 24280-93-1/Mycophenolic Acid; 9242ECW6R0/mycophenolate mofetil; EC Dehydrogenase

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