PubMed · 5997166
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A S Sokolov. [Oxazile].. https://pubmed.ncbi.nlm.nih.gov/5997166/
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The relationship between the concentration of ambenonium (AMB), a selective and reversible acetylcholinesterase (AChE) inhibitor, in plasma and the potentiation of contractile muscle tension was investigated using a sciatic nerve-muscle preparation of rat. The developed isometric contraction was enhanced dose-dependently after i.v. administration of low doses (5-20 nmol/kg) of AMB, but the contraction was weakened when AMB was administered at high doses (100-1000 nmol/kg), and the concentration-effect relationship was bell-shaped. The muscle contraction profile after 50 nmol/kg administration without previous administration, with 20 nmol/kg and with 50 nmol/kg administered previously were quite different from each other. These findings suggest that the potentiation of contractile muscle tension by AMB may be acutely tolerated and the concentration-effect relationship may change time-dependently.
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.