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KMID : 0606920070150020102
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Biomolecules & Therapeutics
2007 Volume.15 No. 2 p.102 ~ p.107
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Effect of Cimetidine on the Transport of Quinolone Antibiotics in Caco-2 Cell monolayers
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Kim Seon-Hwa
Jung Seo-Jeong
Um So-Young
Na Mi-Ae
Choi Min-Jin
Chung Myeon-Woo
Oh Hye-Young
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Abstract
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Cimetidine, a substrate for P-glycoprotein (P-gp), is a well known drug interacting with a variety of drugs and results in alteration of pharmacokinetic parameters by concomitant administration. The aim of present study was to investigate whether cimetidine affects the transport of various quinolone antibiotics in human colorectal cancer cell line (Caco-2) system which has been typically used to investigate drug transport via P-gp. The apparent permeability coefficients (P$_{app}$) value of 9 quinolone antibiotics in the co-treatment with cimetidine was examined. Apical to basolateral (AP-to-BL) transport of fleroxacin in the co-treatment with cimetidine was increased to 1.5-fold (p<0.01) compared with that of fleroxacin alone, whereas basolateral to apical (BL-to-AP) transport of fleroxacin was decreased to 0.83-fold significantly (p<0.05). Ofloxacin was decreased to 0.8-fold (p<0.01) and 0.72-fold (p<0.01) significantly in AP-to-BL and BL-to-AP direction, respectively by cimetidine cotreatment. The P$_{app}$ values of gatifloxacin, moxifloxacin, ciprofloxacin and rufloxacin also were changed by cimetidine. These results have a potential that cimetidine influences on the pharmacokinetics of quinolone antibiotics. It suggests that careful drug monitoring and dosage adjustment may be necessary during the co-administration of quinolone antibiotics with cimetidine.
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KEYWORD
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Cimetidine, P-glycoprotein, Quinolone antibiotics, Caco-2, Apparent permeability coefficients
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