Pharmacokinetics of ambenonium, a reversible cholinesterase inhibitor, in rats

Abstract

The pharmacokinetics of ambenonium, a reversible cholinesterase inhibitor, in rats was investigated following intravenous administration of the drug. Mean residence time and steady state volume of distribution were 23-36 min and 0.20-0.311 kg-1, respectively, and were dose independent at the dose of 0.3-3 mumole kg-1. Total body clearance of 8.2 ml min-1 kg-1 over 0.3 mumole kg-1 was slightly increased to 11.3 ml min-1 kg-1 at 3 mumole kg-1. Renal clearance was also increased with the increase of the dose, while hepatobiliary clearance was substantially constant. Ambenonium was highly concentrated in the liver, kidney, spleen, and lung. About 30 per cent of the dose is concentrically stored in the liver at 6 h after administration, and had not disappeared after 24 h.

High‐Throughput Label‐Free Enzymatic Assays Using Desorption Electrospray‐Ionization Mass Spectrometry

“…The three fitted linear models, corresponding to the three evaluated substrate levels, intersect in the second quadrant of the plot, indicating that neostigmine is a competitive inhibitor of AChE, as is expected. Its K i was found to be 70.0±0.7 n m , which is in the order of previous reports (25–160 n m ) [58–60] . Over 3000 reaction mixtures were analyzed to obtain the Dixon plot and calculate this constant.…”