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

시메티딘 정맥투여가 사이크로스포린의 체내동태에 미치는 영향

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.