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08:38
Quantification of the Immunosuppressant Tacrolimus on Dried Blood Spots Using LC-MS/MS
Published on: November 8, 2015
Mycophenolate, clinical pharmacokinetics, formulations, and methods for assessing drug exposure
Susan E Tett1, Franck Saint-Marcoux, Christine E Staatz
1The University of Queensland, Faculty of Health Sciences, Brisbane, QLD 4072, Australia. s.tett@uq.edu.au
Transplantation Reviews (Orlando, Fla.)
|December 31, 2010
Summary
Therapeutic drug monitoring of mycophenolate (MPA) is crucial due to dose-concentration variability. Measuring MPA exposure and adjusting doses are key for optimal outcomes, with AUC 0-12 as the gold standard for monitoring.
Area of Science:
- Pharmacology
- Clinical Pharmacy
- Transplantation Medicine
Background:
- Mycophenolate (MPA) is a vital immunosuppressant in transplantation.
- Variability in MPA dose-concentration relationships necessitates therapeutic drug monitoring.
- Different MPA formulations (mycophenolate mofetil and enteric-coated mycophenolate sodium) exhibit distinct pharmacokinetic profiles.
Framework:
- The area under the concentration-time curve (AUC 0-12) is the criterion standard for MPA exposure monitoring.
- Limited sampling strategies and Bayesian estimation require careful validation for specific populations and formulations.
- Trough concentrations are practical but less informative for MPA exposure assessment, especially for enteric-coated mycophenolate sodium.
Implementation:
- AUC 0-12 measurement is essential for reliable MPA exposure estimates with enteric-coated mycophenolate sodium.
- Limited sampling protocols should be developed and validated for specific patient populations.
- Consideration of free MPA exposure is beneficial in patients with renal impairment or hypoalbuminemia.
Implications:
- Optimizing MPA dosing improves clinical outcomes in transplant recipients.
- Understanding pharmacokinetic differences between MPA formulations is critical for effective monitoring.
- Pharmacogenetic assessment (e.g., UGT1A9 polymorphisms) may aid in preemptive dosing strategies.
- Repeated MPA exposure monitoring and dose adjustments are necessary post-transplant, especially during cyclosporine tapering.
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