Pharmacokinetics of furosemide in endolymph.

To investigate the pharmacokinetics of organic anions in the endolymph of the guinea pig, 100 mg/kg furosemide, an organic anion, was intravenously given to measure the concentration in the cochlear endolymph by high-performance liquid chromatography with fluorescence detection. In the endolymph, the concentration of the furosemide increased slowly for 1 hr to 1.6 micrograms/ml and gradually declined thereafter. Pretreatment with 200 mg/kg probenecid, an anion transport inhibitor, had no effect on the furosemide elimination in the endolymph except on the concentration at 2 hr. This was contrary to the drastic change observed in the perilymph of the scala tympani by the same pretreatment. Analogous to the effect in the endolymph, probenecid showed no change in the concentration of the serum, while a pronounced gradient of furosemide concentration existed between them. The present results suggest that the furosemide passively transfers from blood to the endolymph at a relatively low penetrability.