Rapid potentiometric determination of cholinesterases in plasma and red cells: Application to eptastigmine monitoring

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

Research output: Contribution to journalArticle

Abstract

Eptastigmine (MF 201) is a new physostigmine derivative with potent inhibitory activity on cholinesterases. Here we present a new potentiometric cholinesterase activity assay suitable for MF 201 monitoring. The analysis is performed on a differential pH system and has the following characteristics: (a) within-run precision: C.V. 2.0% (plasma cholinesterase), 1.8% (red cell cholinesterase); (b) between-run precision: C.V. 4.0% (plasma cholinesterase); (c) linearity: 1-10 kU/l (plasma cholinesterase), 6-70 U/g Hb (red cell cholinesterase); (d) comparison with a reference method (x, HITACHI 737 Boerhinger Mannheim, Italy): y = 0.785x - 0.07; n = 37; r = 0.998. The assay has been applied to the determination of plasma and red cell cholinesterase activity in volunteers over 60 years of age treated with a single oral dose of 30 mg eptastigmine. We found that red cell cholinesterase is selectively inhibited after MF 201 administration with the following kinetics (time, % of inhibition, mean ± S.E., n = 6): 0 h, 0; 1 h, 17 ± 4.6; 2 h, 24 ± 4; 4 h, 23 ± 4.4; 12 h, 14 ± 3. Eptastigmine plasma levels were also determined by a HPLC method: maximum concentration was found one hour after drug administration.

Original languageEnglish
Pages (from-to)265-268
Number of pages4
JournalChemico-Biological Interactions
Volume87
Issue number1-3
DOIs
Publication statusPublished - 1993

Fingerprint

Cholinesterases
Plasma Cells
Cells
Plasmas
Monitoring
Assays
physostigmine heptyl
Physostigmine
Italy
Volunteers
High Pressure Liquid Chromatography
Derivatives
Kinetics

Keywords

  • Acetylcholinesterase
  • Cholinesterase inhibitors
  • Differential pH
  • Erythrocytes

ASJC Scopus subject areas

  • Toxicology

Cite this

Rapid potentiometric determination of cholinesterases in plasma and red cells : Application to eptastigmine monitoring. / Cazzola, E.; Lattuada, N.; Zecca, L.; Radice, D.; Luzzana, M.; Imbimbo, B. P.; Auteri, A.; Mosca, A.

In: Chemico-Biological Interactions, Vol. 87, No. 1-3, 1993, p. 265-268.

Research output: Contribution to journalArticle

Cazzola, E. ; Lattuada, N. ; Zecca, L. ; Radice, D. ; Luzzana, M. ; Imbimbo, B. P. ; Auteri, A. ; Mosca, A. / Rapid potentiometric determination of cholinesterases in plasma and red cells : Application to eptastigmine monitoring. In: Chemico-Biological Interactions. 1993 ; Vol. 87, No. 1-3. pp. 265-268.
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AU - Cazzola, E.

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AU - Radice, D.

AU - Luzzana, M.

AU - Imbimbo, B. P.

AU - Auteri, A.

AU - Mosca, A.

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N2 - Eptastigmine (MF 201) is a new physostigmine derivative with potent inhibitory activity on cholinesterases. Here we present a new potentiometric cholinesterase activity assay suitable for MF 201 monitoring. The analysis is performed on a differential pH system and has the following characteristics: (a) within-run precision: C.V. 2.0% (plasma cholinesterase), 1.8% (red cell cholinesterase); (b) between-run precision: C.V. 4.0% (plasma cholinesterase); (c) linearity: 1-10 kU/l (plasma cholinesterase), 6-70 U/g Hb (red cell cholinesterase); (d) comparison with a reference method (x, HITACHI 737 Boerhinger Mannheim, Italy): y = 0.785x - 0.07; n = 37; r = 0.998. The assay has been applied to the determination of plasma and red cell cholinesterase activity in volunteers over 60 years of age treated with a single oral dose of 30 mg eptastigmine. We found that red cell cholinesterase is selectively inhibited after MF 201 administration with the following kinetics (time, % of inhibition, mean ± S.E., n = 6): 0 h, 0; 1 h, 17 ± 4.6; 2 h, 24 ± 4; 4 h, 23 ± 4.4; 12 h, 14 ± 3. Eptastigmine plasma levels were also determined by a HPLC method: maximum concentration was found one hour after drug administration.

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