Pharmacokinetics of enteric-coated mycophenolate sodium in stable pediatric renal transplant recipients

:  This study aims to characterize the pharmacokinetics of mycophenolic acid (MPA) and its glucuronide metabolite (mycophenolic acid 7‐O‐glucuronide, MPAG) following single oral administration of enteric‐coated mycophenolate sodium (EC‐MPS, myfortic®) at an approximate dose level of 450 mg/m2 body s...

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Bibliographic Details
Published in:Pediatric transplantation 2005-12, Vol.9 (6), p.780-787
Main Authors: Ettenger, Robert, Bartosh, Sharon, Choi, Les, Zhu, Wei, Niederberger, Werner, Campestrini, Joelle, Bastien, Marie-Claude, Schmouder, Robert
Format: Article
Language:English
Subjects:
Adolescent
Area Under Curve
Biological and medical sciences
Child
Child, Preschool
enteric-coated mycophenolate sodium
Enzyme Inhibitors - administration & dosage
Enzyme Inhibitors - blood
Enzyme Inhibitors - pharmacokinetics
Female
Glucuronates - administration & dosage
Glucuronates - pharmacokinetics
Glucuronides
Humans
Kidney Transplantation - physiology
Male
Medical sciences
Mycophenolic Acid - administration & dosage
Mycophenolic Acid - analogs & derivatives
Mycophenolic Acid - blood
Mycophenolic Acid - pharmacokinetics
pediatric
pharmacokinetics
Reoperation
Surgery (general aspects). Transplantations, organ and tissue grafts. Graft diseases
Tablets, Enteric-Coated
transplantation
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Summary::  This study aims to characterize the pharmacokinetics of mycophenolic acid (MPA) and its glucuronide metabolite (mycophenolic acid 7‐O‐glucuronide, MPAG) following single oral administration of enteric‐coated mycophenolate sodium (EC‐MPS, myfortic®) at an approximate dose level of 450 mg/m2 body surface area (BSA) to 25 stable renal transplant recipients (aged 5–16 yr), and to evaluate the safety and tolerability of EC‐MPS in this pediatric population. Patients had been maintained on a cyclosporine emulsion, Neoral®‐based immunosuppressive regimen for at least 3 months and had received their first or second renal transplant more than 6 months prior to entry into the study. After a brief lag phase (tlag 0.75 h), MPA was rapidly absorbed (tmax 2.5 h) and rapidly converted to MPAG (tmax 3.25 h), with relatively high plasma concentrations of MPAG (Cmax 67.7 μg/mL) compared with MPA (Cmax 36.3 μg/mL). The elimination half‐life for MPAG was slightly longer than for MPA (approximately 13 h vs. 8.5 h), and the apparent oral clearance of MPA was approximately 0.2 L/h/kg. The pharmacokinetics of MPA or MPAG were not affected by age, body weight or BSA, within the study population. The pharmacokinetic results for pediatric patients are comparable with those obtained previously in adults, although exposure based on AUC0−∞ was approximately 23% higher, and this finding may be a result of dosing on the basis of BSA, rather than body weight. The recommended dose of EC‐MPS in pediatric patients is 400–450 mg/m2 twice daily or, alternatively, approximately 10–14 mg/kg twice daily when used in combination with cyclosporine microemulsion.
ISSN:1397-3142
1399-3046
DOI:10.1111/j.1399-3046.2005.00386.x