Drug Metabolism and Disposition 1991-01-01

Metabolism and disposition of sulfluramid, a unique polyfluorinated insecticide, in the rat.

R O Manning, J V Bruckner, M E Mispagel, J M Bowen

Index: Drug Metab. Dispos. 19(1) , 205-11, (1991)

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Abstract

The objectives of this study were to characterize the absorption, distribution, and elimination of sulfluramid (N-ethyl perfluorooctane sulfonamide) and its major metabolite, perfluorooctane sulfonamide (DESFA), in order to assess the effect of dosage vehicle on their pharmacokinetics. In Trial 1, male and female Sprague-Dawley rats (170-240 g) were housed in Roth-type metabolism cages. Each rat received 50 mg/kg sulfluramid po, which contained 10 microCi of [14C] sulfluramid. Feces, urine, and expired air samples were collected for 72 hr post-dosing. Tissue samples also were collected at 72 hr and 14C distribution determined. Eighty percent of the radiolabel was eliminated within 72 hr, with the largest quantities of 14C recovered in expired air (56%) and feces (25%). Less radiolabel was recovered in urine (8%), and even smaller amounts in tissues (5%). The highest tissue concentrations of 14C were found in liver, kidneys, and adrenals, with significantly more radiolabel in the kidneys, gonads, and adrenals of the females than males. Male Sprague-Dawley rats (250-275 g) were used in Trials 2 and 3. In Trial 2, rats with a carotid artery cannula were given 50 mg/kg sulfluramid in a po bolus of polyethylene glycol 400 (PEG) or corn oil and blood samples were collected for 96 hr. In Trial 3, noncannulated rats were given 50 mg/kg sulfluramid po in PEG or corn oil and blood samples were collected from the caudal artery for 14 days. Blood samples were analyzed for sulfluramid and DESFA by gas chromatography.(ABSTRACT TRUNCATED AT 250 WORDS)