Logo Annals of Transplantation Logo Annals of Transplantation Logo Annals of Transplantation

01 January 2008

Pharmacokinetics of mycophenolic acid: A comparison between enteric-coated mycophenolate sodium and mycophenolate mofetil in renal transplant recipients

T. van Gelde

Ann Transplant 2008; 13(1): 27-27 :: ID: 880181

Abstract

Mycophenolate mofetil (MMF) is widely used in the field of solid organ transplantation. In combination with calcineurin inhibitors it has become the most often used drug to prevent acute rejection. In an attempt to reduce the incidence of the gastrointestinal adverse events associated with MMF use, the enteric-coated mycophenolate sodium (EC-MPS) was developed. Unfortunately, in two clinical trials EC-MPS 720 mg twice daily and MMF 1000 mg twice daily showed similar efficacy and safety profiles. The two formulations are therefore considered to be therapeutically equivalent. MPA exposure, measured as the area under the plasma concentration time curve (AUC), does not differ during administration of bioequivalent dosages of the two drugs (720 mg EC-MPS and 1000 mg MMF). Also the pharmacodynamic effect, measured as inhibition of the target enzyme inosine monophosphate dehydrogenase (IMPDH) has been shown to be comparable between the two formulations. However, due to the enteric coating the pharmacokinetic profile of EC-MPS is different, with a longer and more variable time to reach the peak concentration (T[sub]max[/sub]). This increased variability in pharmacokinetics impacts on the application of therapeutic drug monitoring in patients using EC-MPS. It is well known that the correlation between pre-dose concentrations and AUC is poor for MMF. At the same time we also realize that drawing full AUCs, consisting of 8-12 blood samples over the 12-hour dosing interval, poses practical problems in routine clinical practice. Therefore limited sampling strategies have successfully been developed, in order to reliably estimate AUC, using only 2 or 3 samples obtained in the first few hours after oral MMF intake. Such limited sampling strategies however require reproducible pharmacokinetic profiles. In contrast to MMF the profiles obtained with EC-MPS show too much variability to develop reliable limited sampling strategies. This implies that the only method to reliably measure the MPA-AUC in a patient treated with EC-MPS is to perform a full (8-12 blood sample) AUC curve.

Keywords: Mycophenolate Mofetil, Organ Transplantation, plasma concentration

Add Comment 0 Comments

In Press

Case report  

Pulmonary Embolism Following Living Donor Hepatectomy: A Report of 4 Cases and Literature Review

Ann Transplant In Press; DOI: 10.12659/AOT.946752  

Most Viewed Current Articles

03 Jan 2023 : Original article   6,527

Impact of Autologous Stem Cell Transplantation on Primary Central Nervous System Lymphoma in First-Line and...

DOI :10.12659/AOT.938467

Ann Transplant 2023; 28:e938467

15 Aug 2023 : Review article   6,222

Free-Circulating Nucleic Acids as Biomarkers in Patients After Solid Organ Transplantation

DOI :10.12659/AOT.939750

Ann Transplant 2023; 28:e939750

16 May 2023 : Original article   6,152

Breaking Antimicrobial Resistance: High-Dose Amoxicillin with Clavulanic Acid for Urinary Tract Infections ...

DOI :10.12659/AOT.939258

Ann Transplant 2023; 28:e939258

17 Jan 2023 : Original article   5,279

Non-Cryopreserved Peripheral Blood Stem Cell Graft for Autologous Hematopoietic Stem Cell Transplantation i...

DOI :10.12659/AOT.938595

Ann Transplant 2023; 28:e938595

Your Privacy

We use cookies to ensure the functionality of our website, to personalize content and advertising, to provide social media features, and to analyze our traffic. If you allow us to do so, we also inform our social media, advertising and analysis partners about your use of our website, You can decise for yourself which categories you you want to deny or allow. Please note that based on your settings not all functionalities of the site are available. View our privacy policy.

Annals of Transplantation eISSN: 2329-0358
Annals of Transplantation eISSN: 2329-0358