Metabolic Fate of Pergolide Mesylate. (2): Absorption, Distribution, Excretion of 14C-Pergolide Mesylate in Rats after Repeated Administration.
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The absorption, distribution and excretion of <SUP>14</SUP>C-PERGOLIDE MESYLATE were investigated after daily oral administration to male rats.<BR> 1. The radioactivity in the blood of rats receiving daily oral doses of <SUP>14</SUP>C-PERGOLIDE MESYLATE showed a continuous increase at 24 hours after each dose for up to 18 doses. The amount of radioactivity in the blood 24 hours after the 18th dose was 4.2 times higher than that observed at 24 hours after the first dose. The rate of elimination of radioactivity from the blood after the 21st dose was slower than that observed after a single dose.<BR> 2. The excretion of radioactivity in the urine and feces reached near steady state after 4 doses. The excretion of radioactivity in the urine and feces was 24.4% and 72.1% of the cumulative dose, respectively, during 168 hours after the 21st dose.<BR> 3. The distribution of radioactivity in the tissues was measured 24 hours after the 1st, 7th, 14th and 21st dose, and in most tissues the radioactivity accumulated throughout the dosing period. The radioactivity accumulated greatly in the spleen, submaxillary gland, thyroid gland, bone marrow and kidney with continuous dosing. The radioactive content in the rest of the tissues after the 21st dose was less than 6 times as high as that after the 1st dose. Also, the elimination of radioactivity from all tissues was slower after the 21st dose than that after the 1st dose.
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日本薬物動態学会 | 論文
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