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Correlation between plasma physostigmine concentrations and percentage of acetylcholinesterase inhibition over time after controlled release of physostigmine in volunteer subjects

S Knapp, ML Wardlow, K Albert, D Waters and LJ Thal

Department of Psychiatry, School of Medicine, University of California, San Diego.

Five to six subjects ingested doses of controlled-release physostigmine salicylate tablets (9, 12, and 15 mg) followed by sequential blood drawing for measurement of plasma physostigmine concentrations and percentage of acetylcholinesterase (AChE) inhibition. Both plasma physostigmine concentrations and percentage of AChE inhibition demonstrated dose proportionality to three doses of ingested drug. Plasma physostigmine concentrations correlated with percentage of AChE inhibition across time by dose and across all doses and subjects tested. These data should be helpful to physicians in adjusting physostigmine dosing, enabling them to use the relatively simple and widely available AChE assay to approximate plasma physostigmine concentrations.

Volume 19, Issue 2, pp. 400-404, 03/01/1991
Copyright © 1991 by American Society for Pharmacology and Experimental Therapeutics






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Copyright © 1991 by the American Society for Pharmacology and Experimental Therapeutics.