Korean Journal of Pediatrics 2005;48(5):476-480.
Published online May 15, 2005.
Tacrolimus versus Cyclosporine Immunosuppression in Pediatric Renal Transplantation : Pharmacokinetic Consideration
Jung Sue Kim
Department of Pediatrics, Cheongju St.Mary's Hospital, Cheongju, Korea
신장 이식에 사용되는 주요 면역억제제와 약물 동력학 검사
청주성모병원 소아과
Jung Sue Kim, Email: youngped@hotmail.com
Immunosuppressive therapy in pediatric renal transplant recipients is changing consequence of the increasing number of available immunosuppressive agents. The optimal use of immunosuppressive agents requires a thorough understanding of the pharmacokinetic characteristics, but the information on the pharmacokinetic characteristics of these drugs in pediatric transplant recipients is still limited. In general, patients younger than 5 years old show higher clearance rates, therefore the need for higher dosages in younger patients seems evident. By the therapeutic drug monitoring, trough(Cmin) and peak level(Cmax) are measured and the area under the blood concentration-time curve(AUC), which is taken as being representative of total systemic exposure can be calculated. Cyclosporine A (CSA) has poor bioavailability, which contributes to high inter- and intra-patient pharmacokinetic variability. CSA concentration measured 2 hours after administration(C2) has better correlation with the AUC than Cmin and is an alternative technique that predicts the AUC. Tacrolimus(Tac) has a great deal of inter-individual variability like CSA but intra-individual variability in systemic exposure is considered to be low. Both CSA and Tac are metabolized by a cytochrome P-450 enzyme isoform(CYP3A4). We should consider changing the dosages when CSA or Tac is used in combination with the medicines that inhibit or induce the CYP3A4. In case of steroid-free immunosuppressive therapy, the blood concentration of Tac should be frequently checked and dosage adjustment may be needed.
Key Words: Cyclosporine , Tacrolimus , Pharmacokinetics

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