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S T Kau

Publications and source records attributed to S T Kau.

48 records · Page 3Linked to original sources

Handling of triamterene by the isolated perfused rat kidney.

Quantitative studies on the renal handling of [3H]triamterene were performed in an isolated perfused rat kidney with near normal function and in an isolated kidney with negligible filtration rate, but preserved perfusate flow rate. The excretory pattern for [3H]triamterene is compatible with that of other weak bases such as quinine and quinacrine. Tubular secretion of [3H]triamterene is strongly inhibited by anoxia and iodoacetate. Tubular reabsorption of [3H]triamterene becomes pronounced when the urine is alkaline. Clearances were reported with and without correction for perfusate albumin binding which is about 75%. Bidirectional transport processes are operative in that [3H]triamterene is secreted by the renal tubule and passively diffuses back across the tubular epithelium by a pH-dependent mechanism.

Animals↗

Distribution and pharmacokinetics of triamterene in rats.

The tissue distribution of 14C-triamterene was examined in the fact. After intravenous administration of 14C-triamterene, high concentration ratios between tissues and blood were found in most tissues except the brain, fat, and testes. The maximal concentration of the drug was in the kidneys, liver, heart, lungs, and skeletal muscle within the first 20 min, when the maximal natriuresis was observed. No metabolite of triamterene was detected in these tissues. The pharmacokinetics of 14C-triamterene also were investigated. The volume of distribution of the drug was greater in the central compartment (60% of the dose) than in the peripheral compartment (40%). The binding of the drug to skeletal muscle is responsible for the fraction of the dose in the peripheral compartment. Rate constants indicate that slow elimination of triamterene is related to its binding to tissue in the central compartment.

Animals↗

Metabolism of triamterene in the rat.

The metabolism of 14C-triamterene (TA), 2,4,7-triamino-6-phenylpteridine, was investigated in rats. After administration of 14C-TA (2 mg/kg, sc), 45% and 50% of the total radioactivity was excreted in urine and feces, respectively, during 72 hr. 14C-TA and its metabolites were separated by paper chromatography and countercurrent distribution. Unchanged TA in the urine and feces accounted for 72-79% of the dose. The major metabolites in the excreted dose were free p-hydroxytriamterene (10-15%) and its conjugate (1-5%). Three hours after administration of the drug, the major metabolites were not found in gastrointestinal contents or urine when the bile duct was cannulated. They were formed in the liver and secreted in bile. A minor unidentified metabolite (2% of the dose) was also formed in the liver and excreted in urine and feces.

Animals↗