Is Absorption Profile of Cyclosporine Really Important for Effective Immunosuppression?(Biopharmacy)

概要

論文の詳細を見る
The clinical significance of cyclosporine (CsA) concentration 2h postdose (C_2) monitoring is widely recognized in organ transplantation, because C_2 value is considered to be a predictable surrogate marker of full area under the concentration-time curve (AUC), and/or a peak concentration value exhibits potent inhibition of calcineurin activity. However, the pharmacological advantage of absorption profile (AP) has not been fully elucidated. In a rat skin allotransplantation model, the authors evaluated the efficacy of AP by different dosage regimens (20, 25 or 30mg/kg/d, once or twice daily) and routes (p.o. or i.v.), and examined whether high C_2 or AUC_<0-4> is intrinsically valuable for effective immunosuppression. Graft survival was CsA dose-dependent and correlated with full AUC_<0-24>, rather than AP. The difference between the once and twice daily administrations did not influence full AUC_<0-24> or immunosuppressive effect. Continuous intravenous infusion with flat pharmacokinetics also produced adequate immunosuppression as was observed in enteral administration at the same level of total exposure. The impact of high peak concentration in AP on immunosuppressive effect could not be found. It was suggested that AP would not have intrinsic pharmacodynamic value. However, absorption profiling was considered to be clinically useful in that C_2 value is a good surrogate marker of total exposure (AUC_<0-24>).
公益社団法人日本薬学会の論文
2006-02-01

Is Absorption Profile of Cyclosporine Really Important for Effective Immunosuppression?(Biopharmacy)

スポンサーリンク

概要

著者

関連論文

スポンサーリンク