TABLE 1

Carboxyfluoroquinolone renal transport literature

			Suggested Possible Role for Transporter Family
Carboxyfluoroquinolone	System	Major Finding	Anionic			Cationic			Specific Transporter	Reference
			Apical	Basolateral	Apical	Basolateral
Ciprofloxacin	In vivo in humans (male and female)	Renal clearance was reduced to ∼1/3 of normal by probenecid	√	√	—	—	No	Jaehde et al., 1995
Norfloxacin	In vivo in humans, rabbits, and dogs (all male)	Renal clearance was reduced to ∼1/2 of normal by probenecid, no effect was apparent in dogs	√	√	—	—	No	Shimada et al., 1983
Ofloxacin	In vivo in humans	Reduced the plasma clearance of procainamide	—	—	√	√	No	Martin et al., 1996
	Rat renal cortical apical membrane vesicles	Inhibited uptake of TEA, cephalexin, and cephradine with no effect on PAH transport	√	—	√	—	No	Okano et al., 1990
Ciprofloxacin, enoxacin, enrofloxacin, fleroxacin, norfloxacin, ofloxacin, and pefloxacin	In vivo: stop-flow renal peritubular capillary perfusion in rats	All inhibited renal basolateral uptake of PAH and NMeN (weakly to moderately)	—	√	—	√	No	Ullrich et al., 1993
Ofloxacin	In vivo: i.v. administration in rats	Cimetidine and probenecid reduced total and renal clearance	√	√	√	√	No	Foote and Halstenson, 1998
Levofloxacin	LLC-PK₁ cells	Inhibited TEA apical transport; basolateral transport was not inhibited by TEA or cimetidine	—	—	√	No role	No	Ohtomo et al., 1996
	OK cells	Inhibited PAH basolateral uptake and apical efflux; transport was unaffected by PAH	√	√	—	—	No	Matsuo et al., 2001
	hOCT2 expressing HEK293 cells	Inhibited creatinine uptake	—	—	—	√	hOCT2	Okuda et al., 2006
	Isolated perfused rat kidney	Cimetidine and quinolones prolonged the transepithelial transit time	√	—	√	—	No	Ito et al., 2000

↵√ , suggested role in transport;—, undetermined role in transport; no role, study specifically suggested no role for the transporter family and membrane; NMeN, N¹-methyl-nicotinamide; OK, opossum renal proximal tubular cells; PAH, p-aminohippurate; TEA, tetraethylammonium.