Bioavailability of Oral Pyridostigmine and Inhibition of Red Blood Cell Acetylcholinesterase by Oral and Intravenous Pyridostigmine
Abstract
Pyridostigmine bromide pretreatment has been shown to reduce the mortality from organophosphate exposure in animal studies. This human study was performed (1) to determine the bioavailability of oral pyridostigmine syrup, (2) to examine the pharmacokinetics and safety of pyridostigmine given orally and intravenously, and (3) to determine the relationship between pyridostigmine plasma levels and erythrocyte acetylcholinesterase inhibition after the oral and intravenous administration of pyridostigmine. The first six subjects received oral and intravenous pyridostigmine (in a dose-ranging phase) in an effort to approach, but not exceed, 40% inhibition of erythrocyte acetylcholinesterase. This target level of inhibition was chosen as a compromise between effective protection against organophosphate poisoning on the one hand and toxicity from the drug on the other. After the proper doses to achieve approximately 40% erythrocyte acetylcholinesterase inhibition were determined, 18 additional subjects received oral and intravenous pyridostigmine to address the objectives mentioned above.
Document Details
- Document Type
- Technical Report
- Publication Date
- Mar 22, 1989
- Accession Number
- ADA541408
Entities
People
- Brent G. Petty
- David M. Kornhouser
- Paul S. Lietman
Organizations
- Johns Hopkins University