Effect of Cimetidine on the Pharmacokinetics of Intraveneous Cyclosporine in Human Subjects

시메티딘 정맥투여가 사이크로스포린의 체내동태에 미치는 영향

  • Choi, In (Department of Pharmacy, Chosun university Hospital) ;
  • Choi, Jun Shik (College of Pharmacy, Chosun University)
  • 최인 (조선대학교 병원약국) ;
  • 최준식 (조선대학교 약학대학)
  • Published : 2000.06.01

Abstract

The effect of cimetidine on the pbarmacokinetic parameters of cyclosporine (intravenous administration) were determined in 6 healthy volunteers (22-48 years old, 48-62 kg) by cross-over design. Cyclosporine and cyclosporine metabolites in whole blood were analysed by fluororescence polarization immunoassay (TDx-FLX). The blood concentrations of cyclosporine After pretreatment with cimetidine (200 mg bid, for 3days) were increased significantly at 8-12 hrs compared to the control (p<0.05). The ratios of blood concentrations of cyclosporine metabolites (M1, M17) to parent drug were decreased significantly at 8-12 hrs (p<0.05). Total body clearance (CL) was also decreased significantly (p<0.05), and area under the curve $(AUC,\%)$ was increased but not significant.

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