PubMed · 5997166
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A S Sokolov. [Oxazile].. https://pubmed.ncbi.nlm.nih.gov/5997166/
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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.
A sensitive and selective analytical method for the determination of ambenonium ion in biological samples is described. The procedure involves ion-pair extraction of the drug, followed by reversed-phase ion-pair chromatographic analysis with ultraviolet detection at 217 nm. The detection limits at a signal-to-noise ratio of 5 were 100 pmol/ml using 0.2 ml of plasma and bile, 250 pmol/ml using 0.2 ml of urine and 200 pmol/g using 1 ml of tissue homogenates containing 0.1 g/ml of each tissue. This assay procedure was used to study the pharmacokinetics of ambenonium ion after intravenous administration in rats.
A patient with myasthenia receiving treatment with anticholinesterase agents and plasma exchanges for an acute episode, developed three successive periods of neurological deterioration during which plasma cholinesterase levels were determined. The risk of onset of a cholinergic crisis under these circumstances has been reported in the literature but not documented. The accidents in the present case were related to cumulative overdose effects of anticholinesterase agents and depletion of cholinesterase, suggesting caution in the use of anticholinesterase agents when frequent plasma exchanges are being carried out in a patient with myasthenia.