Dose-dependent pharmacokinetics of laevodopa and its metabolites in the rat

Xenobiotica; the Fate of Foreign Compounds in Biological Systems
L K Cheng, H L Fung

Abstract

1. Plasma levels of total radioactivity, unchanged laevodopa, dopamine, 3-O-methyldopa and non-amino phenolic acids were measured in rats treated orally with [3H]laevodopa at total laevodopa doses of 1, 10, 20 and 100mg/kg while the radioactive dose was maintained at 100muCi/kg for all animal groups. 2. Within the dosage range studied, non-linear pharmacokinetics were observed for unchanged laevodopa, non-amino phenolic acids and dopamine but not for 3-O-methyldopa. 3. The area under the plasma concentration-time curve for laevodopa increased exponentially with linear increments in the oral dose. This non-linear increase in laevodopa bioavailability is consistent with the hypothesis that high oral doses of laevodopa are required to saturate gastro-intestinal metabolism of the drug. 4. At the lower doses (1 and 20 mg/kg), only 2-3% of total radioactivity could be attributed to dopamine. At 100mg/kg, the dopamine metabolite fraction amounted to about 1/3 of total radioactivity in the plasma.

References

Oct 1, 1975·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·L K Cheng, H L Fung
Feb 13, 1969·The New England Journal of Medicine·G C CotziasR Gellene
Nov 1, 1974·Clinical Pharmacology and Therapeutics·N S SharplessR P Dinapoli
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Jan 1, 1968·Clinica Chimica Acta; International Journal of Clinical Chemistry·F KaroumM Sandler
Jun 1, 1969·Clinica Chimica Acta; International Journal of Clinical Chemistry·F KaroumM Sandler

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