Pharmacodynamics and pharmacokinetics of eptastigmine in elderly subjects

A. Auteri, A. Mosca, N. Lattuada, M. Luzzana, L. Zecca, D. Radice, B. P. Imbimbo

Research output: Contribution to journalArticlepeer-review

Abstract

Eptastigmine is a new cholinesterase inhibitor, which may be potentially useful for the symptomatic treatment of Alzheimer's disease. A preliminary evaluation of its pharmacodynamic and pharmacokinetic profiles in the elderly has now been made in 6 healthy subjects (63-84 years of age) given 30 mg eptastigmine as a single oral dose. Blood was collected prior to and 1, 2, 3, 4, 6, 8, and 12 h after eptastigmine administration for measurement of cholinesterase inhibition in plasma and red blood cells and the plasma drug concentrations. The maximum plasma cholinesterase inhibition was 17%, which was reached 2.7 h after treatment. In red cells the maximum inhibition of the enzyme was 29% after 3.8 h. The estimated half-time of cholinesterase recovery was 12.4 h in plasma and 13.6 h in red blood cells. The peak plasma concentration of eptastigmine of 0.86 ng·ml-1 was reached after 1.4 h. Following absorption the drug was rapidly distributed into tissues (t1/2α = 0.44 h) and then eliminated with a half-life of 12.1 h. The drug was well tolerated in all but one subject, who showed bradycardia with hypertension and nausea for about 2 h after the dose. The results indicate that oral administration of eptastigmine to elderly subjects produces long lasting inhibition of cholinesterase activity in plasma and in red blood cells.

Original languageEnglish
Pages (from-to)373-376
Number of pages4
JournalEuropean Journal of Clinical Pharmacology
Volume45
Issue number4
DOIs
Publication statusPublished - Nov 1993

Keywords

  • adverse effects
  • Cholinesterase inhibition
  • Elderly subjects
  • Eptastigmine
  • pharmacokinetics

ASJC Scopus subject areas

  • Pharmacology, Toxicology and Pharmaceutics(all)
  • Pharmacology (medical)

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