The fate of pridinol in the organism: Pharmacokinetics and distribution in animals
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The pharmacokinetics of Pridinol were tested in dog, mouse and rat. When Pridinol is administered intravenously to dogs, only 2% of the dose is found in plasma immediately after administration; less than 9% of the dose is recovered in urine in 2hours as unchanged Pridinol and a similar quantity as its glucuronoconjugate. No Pridinol is recovered in urine collected from 2 to 7 hours after administration.
After oral administration, of14C-Pridinol t0 mice, 94% of the radioactivity leaves the digestive tract in 12 hours; maximum blood radioactivity is reached within 1 hour; then, 30 to 40% of the dose is found in bile and tissues, mainly liver and kidneys. The radioactivity is eliminated at 80% in 24 h and at 96% in 4 days, from which 56% by urinary excretion.
After i.v. administration of14C-Pridinol to mice, only 4.5% of the radioactivity is found in blood after 30 s and 0.15% after 24 h; 90% of the dose is eliminated in 24 h and 96% in 4 days, from wich 70% by urinary excretion.14C-Pridinol was administered intravenously to anaesthetized rats bearing a catheter implanted in ductus choledocus; 10 mn after administration, the radioactivity per ml was 1000 times higher in bile than in blood; 30 mn after administration, one find 30% of the radioactivity in bile, 17% in liver and 0,7% in blood. The highest levels of radioactivity were found in spleen, liver, gastrointestinal tract walls, kidneys, adrenals and diaphragm. In bile, less than 1% of the radioactivity pertained to unchanged Pridinol and less than 20% to its glucuronoconjugate.
Key wordsPridinol pharmacokinetics spasmolytic animals
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